Dry granulation is a powder agglomeration process used in the pharmaceutical industry to improve the flowability of powders by increasing the particle size (granules). This operation is achieved using a roller press, which can have different configurations and equipment designs. In simple terms Granulation is the process in which primary powder particles are made to adhere to form larger multiparticle entities called granules.
Dry Granulation Advantages & Limitations:
(Slugging of rollercompaction) Advantages: * Eliminates exposure to moisture and drying. * Dusty procedure.
This is also called double compression or slugging method, this is valuable alternative to direct compression, where the dose of drug is too high or to wet granulation when the drug is sensitive to heat, moisture or both. This method is also used when other methods of granulation yield granules with poor flow or compression properties, because there are less chances of segregation of drug and excipients.
Limitations: * Not suitable for all compounds. * Slow process.
Long processing time, a relatively high capital investment on heavy duty presses or compactors.
Steps involved in dry granulation process
I. Milling of drugs and excipients II. Mixing of milled powders III. Compression into large, hard tablets to make slug IV. Screening of slugs V. Mixing with lubricant and disintegrating agent VI. Tablet compression
In dry granulation method the primary powder particles are aggregated at high pressure. There are two main processes – either a large tablet (known as slug) is produced in a heavy duty tableting press( known as slugging) or the powder is squeezed between two rollers to produce a sheet of material (roller compaction) . The two different types are illustrated in below:
how well a material may slug will depend on the below terms
Compressibility or cohesiveness of the matter,
Compression ratio of powder
Density of the powder
Punch and die size
Speed of compression
Pressure used to produce slug
Granulation by slugging is the process of compressing dry powder of tablet formulation with tablet press having die cavity large enough in diameter to fill quickly. The accuracy or condition of slug is not too important. Only sufficient pressure to compact the powder into uniform slugs should be used. Once slugs are produced they are reduced to appropriate granule size for final compression by screening and milling
Slugging (Old Method)Slugging (Old Method) • material to be granulized is first made into a large compressed mass or “slug” typically by way of a tablet press using large flat-faced too long.
Disadvantages of Slugging:
single batch processing
frequent maintenance changeover
poor process control
poor economies of scale
low manufacturing output per hour
excessive air and sound pollution,
Increased use of storage containers,
more energy and time required to produce
In a roller compactor material particles are consolidated and densified by passing the material between two high-pressure rollers. The densified material from a roller compactor is then reduced to a uniform granule size by milling. Roller compaction dry granulation process is capable of handling a large amount of material in a short period of time. As a special subtype briquetting utilizes special designed compaction rolls which divides the compacted powder in pieces (briquettes). For dry granulation the compaction force in extend and uniformity of distribution is essential in regard to uniformity of granules porosity to ensure uniform hardness and disintegration of the final product. Because of its advantages, roll compaction is being increasingly used as a granulation technique, but it is not a simple process and may involve many variables for example roll pressure, roll speed, horizontal/vertical feed screw speed, roller gap, screen size. These parameters need to be optimized depending on the materials and the type of equipment used in order to obtain products of desirable quality.
Pneumatic Dry Granulation:
The pneumatic dry granulation process is a new and patent pending technology. The granulation process is based on the use of roller compaction with very low compaction force together with a proprietary air classification method. The method enables production of granules with extraordinary combination of flow ability and compressibility. The granules produced by Pneumatic Dry Granulation and tablets produced show fast disintegration properties, offering the potential for fast release dosage forms, and Release time can be tailored to requirements. PDG technology can achieve, high drug loading, even with difficult APIs and combinations along with Taste masking and Excellent stability
Himanshu.K.Solanki, Tarashankar Basuri, Jalaram H.Thakkar, “Recent advances in granulation technology, International Journal of Pharmaceutical Sciences Review and Research, 3(5), 48,2010 . 11.
Nidhi Prakash Sapkal, Vaishali A. Kilor, Minal Nandkumar Bonde. Application of a convenient and cost and effective granulation technology for the formulation of tablets using conventional excipients, Asian Journal of Pharmaceutics – 225-254, 2014.
Rudnic EM, Schwartz JD. Oral solid dosage forms In: Remington: The science and practice of pharmacy Gennaro, Lippincott Williams and Wilkins, USA, 2000: 858.
Gohel MC. A review of co-processed directly compressible excipients. J Pharm Pharmaceut Sci 2005; 8: 76-93.
Schwartz JB, Fonner DE, Anderson NR, Banker GS. Granulation and tablet characteristics, Lieberman HA, Lachman L, eds. Pharmaceutical Dosage Forms: Tablets. Vol. 2, New York, Marcel Dekker, 1981:201.
Oxytocin is a hormone, predominately belonging to mammalian family; it is secreted by the posterior pituitary gland. After its release in the blood stream it cannot re-enter the brain due to the presence of blood brain barrier .Oxytocin is a hormone that has both peripheral and central actions. y are synthesized in the magnocellular neurons present in the supra–optic and Para –ventricular nucleus present in the hypothalamus. The universally known functions would include its role at the time of labour and ejection of milk. The functions which remain partially unknown are in erectile responses, ejaculation, bonding, and feeling of love and maintenance of eye contact during a conversation.
Functions and roles of Oxytocin:
Oxytocin plays a key role in establishing trust , falling in love , parturition , milk ejection, mother – child bond , erection and ejaculatory response in males. Oxytocin insuffiency is leads to increased stress and sleep disturbances. The solution to the above mentioned problem lies in creating a drug which can mimic the functional properties of Oxytocin, which was achieved. Oxytocin has been widely used in the field of gynaecology to induce labour. It is also administered to patients i.e. mothers who are unable to produce milk after parturition. The invention of Oxytocin nasal sprays is not unknown. Recommended doses when administered to autism patients are proven to increase the sense of trust at the time of communication.
Mechanism of OXYTOCIN
Oxytocin is a naturally occurring nonapeptide hormone which acts through a G-protein coupled cell surface receptor to stimulate contractions of the uterus. A synthetic version of this hormone is used to induce contractions of the uterus which are indistinguishable from spontaneous labour.
Oxytocin is administered as a slow intravenous infusion (to induce or augment labour), or as a single intramuscular or intravenous injection to help prevent and treat uterine atony and postpartum haemorrhage. In pregnant women, oxytocin is metabolised very quickly in the maternal circulation by an aminopeptidase enzyme which cleaves the protein leaving it without biological function. This oxytocinase activity is also seen within the placenta and uterine tissue, and activity increases throughout pregnancy where at term the half -life of oxytocin is between 2 and 20 minutes.
The main side effects are related to overstimulation of the uterus which can compromise the placental blood supply and fetal well-being, and can also contribute to rupture of the uterus especially in women who have had a previous caesarean delivery. Oxytocin is similar in structure to Vasopressin which is also produced by the posterior pituitary, and prolonged administration with intravenous fluids may lead to fluid overload, pulmonary oedema and water intoxication.
Oxytocin Molecular Formula
It has a molecular formula of C43H66N12O12S 2.
Oxytocin is also known as Pitocin, Syntocinon, Ocytocin, Endopituitrina, Oxitocina, Oxytocine, Oxytocinum, Oxytocic hormone and Orasthin.
It has a molecular formula of C43H66N12O12S 2. They are commercially available as intravenous and intramuscular injections , nasal sprays and sublingual tablets .The commonly used Anirudha kabilan /J. Pharm. Sci. & Res. Vol. 6(4), 2014, 220-223 221 drug types are pitocin and syntocinon, the chemical resemblance to Oxytocin makes them an ideal drug of choice for various cases for example at time if parturition . Pitocin is composed of oxtocic acid/ml along with chlorobutanol , a chloroform derivative. However medical supervision is mandatory to rule out the onset of complications (20,31). The general uses of these Oxytocin drugs would include induction of labour .Under appropriate level , at the time delivery, Oxytocin binds to the receptors present in the myometrium , activates the pathway of hydrolysis of phoshotidyl inositol and diacyl glycerol, there by activating the same. This activation causes the release of intracellular Ca+ which causes contraction of the uterus .In conditions associated with low level of Oxytocin production this process is carried out by Oxytocin drugs (29, 27) Incase of people suffering from autism, administration of pitocin is said to reduce repetitive behaviour and also enhances speech. Few researches have proved the improvement of trust in people affected by autism when they were given pitocin nasal sprays. It also enhances eye to eye contact in these individuals. Pitcoin helps in social interaction in people who suffer from schizophrenia . So pitocin may not only combat hallucinogens and psychosis, but also make human interaction easier . Being a new field if research there is not enough evidence to prove the role pitocin in both autism and schizophrenia. Further, they are also used to cure problems in erectile responses, ejaculation, depression, anxiety, and stress management
Dosage of Oxytocin:
10 units by intravenous route or 20-40 mUnit/min by Intramuscular route are injected for post partum haemorrhage. 0.5-1 mUnit/min by intravenous route for the induction of labour.10-20 mUnit/min is administered along with other drugs for termination of pregnancy.
Uterine contractions are seen after 3-5 minutes and approx 1 minute of aministration through intramuscular and intravenous routes respectively. A steady state of the drug is reached after 40 mins of parenteral route of administration. It is distributed throughout extracellular fluid compartment of the mother; small amounts may cross the placental barrier and reach foetus. Metabolism takes place rapidly via the liver and plasma by the enzyme oxytocinase a few steps of metabolism also takes place via mammary gland. It has a half-life of 1-5 minute. Kidney and liver help in the elimination of Oxytocin drugs( 9) unchanged form of this drug is rarely excreted in urine (30). Overdose can cause titanic uterine contractions, impaired blood flow to the uterus, uterine ruptures, seizures and amniotic fluid embolism contractions, impaired blood flow to the uterus, uterine ruptures, seizures and amniotic fluid embolism.
Significant cephalopelvic disproportion Unfavourable foetal positions Obstetric emergencies which favours surgery Hyperactive or hypertonic uterus When vaginal delivery is contraindicated, Anaphylactic patients, Foetal distress Polyhydramnios Partial placenta pervia Elective labour induction
Nausea or vomiting Memory problems or confusion Runny nose, sore throat, or coughing severe headaches hallucinations vomiting confusion Seizures and severe hypertension
Clinical Scenario 1
Which of the following abnormalities of labor is associated with a significantly increased incidence of neonatal morbidity? a. Prolonged latent phase b. Protracted descent c. Secondary arrest of dilation d. Protracted active-phase dilation Answer: c (Secondary arrest of dilation) Explanation: Three significant advances in the treatment of uterine dysfunction have reduced the risk of perinatal morbidity (PNM) and mortality: (1) the avoidance of undue prolongation of labor, (2) the use of intravenous oxytocin in the treatment of some patterns of uterine dysfunction, and (3) the liberal use of cesarean section (rather than midforceps) to affect delivery when oxytocin fails.
Clinical Scenario 2
Management of obstructed labor includes all, except: [AIIMS May 2004] a. IV fluids b. Oxytocin use c. Antibiotics d. Cesarean section Answer: b (Oxytocin use) Explanation: Two main principles in management of obstructed labor are: 1. Never wait and watch. 2. Never use oxytocin. In patients of obstructed labor, the uterine contractions (power) are always adequate. There is a problem with the passage or the passenger. By increasing the power (by giving oxytocin) we are increasing the risk of rupture uterus. It is like flogging a dead horse. Uterus is already contracting, and there is no point in increasing the contractions further in a case of obstructed labor. The patient should be given IV fluids to correct the dehydration and ketoacidosis, which usually develops due to prolonged labor. Patient should be given antibiotics to prevent infection, and then steps should be taken to immediately relieve the obstruction either by instrumental deliver or by LSCS. LSCS may have to be done even if the baby is dead and if vaginal delivery is not possible, or else rupture uterus will occur. NOTE: In cases of prolonged labor where there are hypotonic uterine contractions, oxytocin is justified.
The term “labeling” designates all labels and other written, printed, or graphic matter upon an immediate container of an article or upon, or in, any package or wrapper in which it is enclosed, except any outer shipping container.
The term “label” designates that part of the labeling upon the immediate container. A shipping container containing a single article, unless such container is also essentially the immediate container or the outside of the consumer package, is labeled with a minimum of product identification (except for controlled articles), lot number, expiration date, and conditions for storage and distribution. Articles in these compendia are subject to compliance with such labeling requirements as may be promulgated by governmental bodies in addition to the compendial requirements set forth for the articles.
Label: Amount of Ingredient Per Dosage Unit:
The strength of a drug product is expressed on the container label in terms of micrograms or milligrams or grams or percentage of the therapeutically active moiety or drug substance, whichever form is used in the title, unless otherwise indicated in an individual monograph. Both the active moiety and drug substance names and their equivalent amounts are then provided in the labeling. Official articles in capsule, tablet, or other unit dosage form shall be labeled to express the quantity of each active ingredient or recognized nutrient contained in each such unit; except that, in the case of unit-dose oral solutions or suspensions, whether supplied as liquid preparations or as liquid preparations that are constituted from solids upon addition of a designated volume of a specific diluent, the label shall express the quantity of each active ingredient or recognized nutrient delivered under the conditions prescribed in Deliverable Volume 〈698〉. Official drug products not in unit dosage form shall be labeled to express the quantity of each active ingredient in each milliliter or in each gram, or to express the percentage of each such ingredient (see 8.140., Percentage Concentrations), except that oral liquids or solids intended to be constituted to yield oral liquids may, alternatively, be labeled in terms of each 5-mL portion of the liquid or resulting liquid. Unless otherwise indicated in a monograph or chapter, such declarations of strength or quantity shall be stated only in metric units.
Labeling: Use of Leading and Terminal Zeros
To help minimize the possibility of errors in the dispensing and administration of drugs, the quantity of active ingredient when expressed in whole numbers shall be shown without a decimal point that is followed by a terminal zero (e.g., express as 4 mg [not 4.0 mg]). The quantity of active ingredient when expressed as a decimal number smaller than 1 shall be shown with a zero preceding the decimal point (e.g., express as 0.2 mg [not .2 mg]).
Labeling of Salts of Drugs
It is an established principle that official articles shall have only one official title. For purposes of saving space on labels, and because chemical symbols for the most common inorganic salts of drugs are well known to practitioners as synonymous with the written forms, the following alternatives are permitted in labeling official articles that are salts: HCl for hydrochloride; HBr for hydrobromide; Na for sodium; and K for potassium. The symbols Na and K are intended for use in abbreviating names of the salts of organic acids, but these symbols are not used where the word Sodium or Potassium appears at the beginning of an official title (e.g., Phenobarbital Na is acceptable, but Na Salicylate is not to be written).
Labeling Vitamin-Containing Products
The vitamin content of an official drug product shall be stated on the label in metric units per dosage unit. The amounts of vitamins A, D, and E may be stated also in USP Units. Quantities of vitamin A declared in metric units refer to the equivalent amounts of retinol (vitamin A alcohol). The label of a nutritional supplement shall bear an identifying lot number, control number, or batch number. 10.40.50. Labeling Botanical-Containing Products The label of an herb or other botanical intended for use as a dietary supplement bears the statement, “If you are pregnant or nursing a baby, seek the advice of a health professional before using this
Labeling Parenteral and Topical Preparations
The label of a preparation intended for parenteral or topical use states the names of all added substances (see 5.20., Added Substances, Excipients, and Ingredients and see Labeling under Injections 〈1〉), and, in the case of parenteral preparations, also their amounts or proportions, except that for substances added for adjustment of pH or to achieve isotonicity, the label may indicate only their presence and the reason for their addition.
The concentration and dosage of electrolytes for replacement therapy (e.g., sodium chloride or potassium chloride) shall be stated on the label in milliequivalents (mEq). The label of the product shall indicate also the quantity of ingredient(s) in terms of weight or percentage concentration.
The content of alcohol in a liquid preparation shall be stated on the label as a percentage (v/v) of C2H5OH.
Symbols Commonly Employed for SI Metric Unit
Symbols commonly employed for SI metric units and other units are as follows: Bq = becquerel dL = deciliter kBq = kilobecquerel L = liter MBq = megabecquerel mL = milliliterc GBq = gigabecquerel μL = microliter Ci = curie Eq = gram-equivalent weight mCi = millicurie mEq = milliequivalent μCi = microcurie mol = gram-molecular weight (mole) nCi = nanocurie Da = dalton (relative molecular mass) Gy = gray mmol = millimole mGy = milligray Osmol = osmole m = meter mOsmol = milliosmole dm = decimeter Hz = hertz cm = centimeter kHz = kilohertz mm = millimeter MHz = megahertz μm = micrometer (0.001mm) V = volts nm = nanometera MeV = million electron volts kg = kilogram keV = kilo-electron volt g = gram mV = millivolt mg = milligram psi = pounds per square inch μg; mcg = microgramb Pa = pascal ng = nanogram kPa = kilopascal pg = pictogram g = gravity (in centrifugation) fg = femtogram a Previously the symbol mμ (for millimicron) was used. b One milliliter (mL) is used herein as the equivalent of one cubic centimeter (cc). c The symbol μg is used in the USP and NF to represent micrograms, but micrograms may be represented as “mcg” for labeling and prescribing purposes. The term “gamma,” symbolized by γ, frequently is used to represent micrograms in biochemical literature
Today Pharmawiki is here with very important 40+ Pharmacology multiple choice questions along with answers. These are published especially for all our pharmacy students who are ready to take up different competitive exams like NEET PG GPAT PHARMACIST qualifying examinations. These questions are also very helpful to all the students and professionals of Nursing to take up different examinations for their career growth. This article specifically provides questions with answers pdf Book at the end for our readers convenience. You can click on the right side and download the entire copy to study easily.
Pharmacology MCQ for Anti Cancer Chemotherapy Drugs
ANTIVIRAL AGENTS. AGENTS FOR CHEMOTHERAPY OF CANCER
All of the following antiviral drugs are the analogs of nucleosides, EXCEPT:
Tick the drug, a derivative of adamantane:
Tick the drug, a derivative of pyrophosphate:
Tick the drug, inhibiting viral DNA synthesis:
Tick the drug, inhibiting uncoating of the viral RNA:
Tick the drug, inhibiting viral reverse transcriptase:
Tick the drug, inhibiting viral proteases:
Tick the drug of choice for herpes and cytomegalovirus infection treatment:
b) Interferon alfa
Tick the drug which belongs to nonnucleoside reverse transcriptase inhibitors:
All of the following antiviral drugs are antiretroviral agents, EXCEPT:
Tick the drug used for influenza A prevention:
Tick the drug used for HIV infection treatment, a derivative of nucleosides:
Tick the antiviral drug which belongs to endogenous proteins:
c) Interferon alfa
Tick the drug which belongs to nucleoside reverse transcriptase inhibitors:
All of the following antiviral drugs are anti-influenza agents, EXCEPT:
Tick the unwanted effects of zidovudine:
a) Hallucinations, dizziness
b) Anemia, neutropenia, nausea, insomnia
c) Hypertension, vomiting
d) Peripheral neuropathy
Tick the unwanted effects of intravenous acyclovir infusion:
a) Renal insufficiency, tremors, delerium
b) Rash, diarrhea, nausea
c) Neuropathy, abdominal pain
d) Anemia, neutropenia, nausea, insomnia
Tick the drug that can induce peripheral neuropathy and oral ulceration:
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Pharmacodynamics. We exactly know what pharmacodynamics is. It involves how the drugs act on target cells to alter cellular function. Let us discuss Dose Response relationship in this article. The exact relationship between the dose and the response depends on the biological object under observation and the drug employed is called Dose Response relationship.
Dose Response relationship
When a logarithm of dose as abscissa and responses as ordinate are constructed graphically, the “S” shaped or sigmoid type curve is obtained. The lowest concentration of a drug that elicits a response is minimal dose, and the largest concentration after which further increase in concentration will not change the response is the maximal dose.
1. Graded dose effect:
As the dose administered to a single subject or tissue increases, the pharmacological response also increases in graded fashion up to ceiling effect. – It is used for characterization of the action of drugs. The concentration that is required to produce 50 % of the maximum effect is termed as EC50 or ED50.
2. Quantal dose effect:
It is all or none response, the sensitive objects give response to small doses of a drug while some will be resistant and need very large doses. The quantal dose effect curve is often characterized by stating the median effective dose and the median lethal dose.
Median lethal dose or LD50:
This is the dose (mg/kg), which would be expected to kill one half of a population of the same species and strain.
Median effective dose or ED50:
This is the dose (mg/kg), which produces a desired response in 50 per cent of test population.
It is an approximate assessment of the safety of the drug. It is the ratio of the median lethal dose and the median effective dose. Also called as therapeutic window or safety. Herapeutic index (T. I) = The larger the therapeutic index, the safer is the drug.
Penicillin has a very high therapeutic index, while it is much smaller for the digitalis preparation.
D. Structural activity relationship The activity of a drug is intimately related to its chemical structure. Knowledge about the chemical structure of a drug is useful for: (i) Synthesis of new compounds with more specific actions and fewer adverse reactions (ii) Synthesis of competitive antagonist and (iii) Understanding the mechanism of drug action. Slight modification of structure of the compound can change the effect completely.
ROUTES OF DRUG ADMINISTRATION: The possible routes for drug entry into the body. Most drugs can be administered by a variety of routes. The choice of appropriate route in a given situation depends both on drug as well as patient related factors. Mostly common sense considerations, feasibility and convenience dictate the route to be used. Generally routes of drug administration refer to the right path or the required route through which a drug has to be administered into the body to obtain maximum benefit. Here is the list of 5, 10+ outes of drug administration.
Subcutaneous (under the skin)
Intramuscular (in a muscle)
Intravenous (in a vein)
Intrathecal (around the spinal cord
Factors governing choice of route
Physical and chemical properties of the drug (solid/ liquid/gas; solubility, stability, pH, irritancy).
Site of desired action—localized and approachable or generalized and not approachable.
Rate and extent of absorption of the drug from different routes.
Effect of digestive juices and first pass metabolism on the drug.
Rapidity with which the response is desired (routine treatment or emergency).
Accuracy of dosage required (i.v. and inhalational can provide fine tuning).
Condition of the patient (unconscious, vomiting).
Routes of Administration can be broadly divided into those for
(a) Local action and (b) Systemic action.
These routes can only be used for localized lesions at accessible sites and for drugs whose systemic absorption from these sites is minimal or absent. Thus, high concentrations are attained at the desired site without exposing the rest of the body. Systemic side effects or toxicity are consequently absent or minimal. For drugs (in suitable dosage forms) that are absorbed from these sites/routes, the same can serve as systemic route of administration, e.g. glyceryl trinitrate (GTN) applied on the skin as ointment or transdermal patch. The local routes are:
This refers to external application of the drug to the surface for localized action. It is often more convenient as well as encouraging to the patient. Drugs can be efficiently delivered to the localized lesions on skin, oropharyngeal/ nasal mucosa, eyes, ear canal, anal canal or vagina in the form of lotion, ointment, cream, powder, rinse, paints, drops, spray, lozengens, suppositories or pesseries. Nonabsorbable drugs given orally for action on g.i. mucosa (sucralfate, vancomycin), inhalation of drugs for action on bronchi (salbutamol, cromolyn sodium) and irrigating solutions/jellys (povidone iodine, lidocaine) applied to urethra are other forms of topical medication.
Certain deep areas can be approached by using a syringe and needle, but the drug should be in such a form that systemic absorption is slow, e.g. intra-articular injection (hydrocortisone acetate in knee joint), infiltration around a nerve or intrathecal injection (lidocaine), retrobulbar injection (hydrocortisone acetate behind the eyeball).
Close intra-arterial injection is used for contrast media in angiography; anticancer drugs can be infused in femoral or brachial artery to localise the effect for limb malignancies.
The drug administered through systemic routes is intended to be absorbed into the blood streamand distributed all over, including the site of action, through circulation
Oral ingestion is the oldest and commonest mode of drug administration. It is safer, more convenient, does not need assistance, noninvasive, often painless, the medicament need not be sterile and so is cheaper. Both solid dosage forms (powders, tablets, capsules, spansules, dragees, moulded tablets, gastrointestinal therapeutic systems— GITs) and liquid dosage forms (elixirs, syrups, emulsions, mixtures) can be given orally.
Limitations of oral route of administration
Action of drugs is slower and thus not suitable for emergencies.
Unpalatable drugs (chloramphenicol) are difficult to administer; drug may be filled in capsules to circumvent this.
May cause nausea and vomiting (emetine).
Cannot be used for uncooperative/unconscious/ vomiting patient.
Absorption of drugs may be variable and erratic; certain drugs are not absorbed (streptomycin).
Others are destroyed by digestive juices (penicillin G, insulin) or in liver (GTN, testosterone, lidocaine).
Sublingual (s.l.) or buccal
The tablet or pellet containing the drug is placed under the tongue or crushed in the mouth and spread over the buccal mucosa. Only lipid soluble and non-irritating drugs can be so administered. Absorption is relatively rapid—action can be produced in minutes. Though it is somewhat inconvenient, one can spit the drug after the desired effect has been obtained. The chief advantage is that liver is bypassed and drugs with high first pass metabolism can be absorbed directly into systemic circulation. Drugs given sublingually are—GTN, buprenorphine, desamino-oxytocin.
Certain irritant and unpleasant drugs can be put into rectum as suppositories or retention enema for systemic effect. This route can also be used when the patient is having recurrent vomiting or is unconscious. However, it is rather inconvenient and embarrassing; absorption is slower, irregular and often unpredictable, though diazepam solution and paracetamol suppository are rapidly and dependably absorbed from the rectum in children. Drug absorbed into external haemorrhoidal veins (about 50%) bypasses liver, but not that absorbed into internal haemorrhoidal veins. Rectal inflammation can result from irritant drugs. Diazepam, indomethacin, paracetamol, ergotamine and few other drugs are some times given rectally.
Highly lipid soluble drugs can be applied over the skin for slow and prolonged absorption. The liver is also bypassed. The drug can be incorporated in an ointment and applied over specified area of skin. Absorption of the drug can be enhanced by rubbing the preparation, by using an oily base and by an occlusive dressing.
Transdermal therapeutic systems (TTS)
These are devices in the form of adhesive patches of various shapes and sizes (5–20 cm2) which deliver the contained drug at a constant rate into systemic circulation via the stratum corneum (Fig. 1.2). The drug (in solution or bound to a polymer) is held in a reservoir between an occlusive backing film and a rate controlling micropore membrane, the under surface of which is smeared with an adhesive impregnated with priming dose of the drug. The adhesive layer is protected by another film that is to be peeled off just before application. The drug is delivered at the skin surface by diffusion for percutaneous absorption into circulation. The micropore membrane is such that rate of drug delivery to skin surface is less than the slowest rate of absorption from the skin. This offsets any variation in the rate of absorption according to the properties of different sites. As such, the drug is delivered at a constant and predictable rate irrespective of site of application. Usually chest, abdomen, upper arm, lower back, buttock or mastoid region are utilized. Transdermal patches of GTN, fentanyl, nicotine and estradiol are available in India, while those of isosorbide dinitrate, hyoscine, and clonidine are marketed elsewhere. For different drugs, TTS have been designed to last for 1–3 days. Though more expensive, they provide smooth plasma concentrations of the drug without fluctuations; minimize interindividual variations (drug is subjected to little first pass metabolism) and side effects. They are also more convenient— many patients prefer transdermal patches to oral tablets of the same drug; patient compliance is better. Local irritation and erythema occurs in some, but is generally mild; can be minimized by changing the site of application each time by rotation. Discontinuation has been necessary in 2–7% cases.
Volatile liquids and gases are given by inhalation for systemic action, e.g. general anaesthetics. Absorption takes place from the vast surface of alveoli—action is very rapid. When administration is discontinued the drug diffuses back and is rapidly eliminated in expired air. Thus, controlled administration is possible with moment to moment adjustment. Irritant vapours (ether) cause inflammation of respiratory tract and increase secretion.
The mucous membrane of the nose can readily absorb many drugs; digestive juices and liver are bypassed. However, only certain drugs like GnRH agonists and desmopressin applied as a spray or nebulized solution have been used by this route. This route is being tried for some other peptide drugs like insulin, as well as to bypass the bloodbrain barrier.
Conventionally, parenteral refers to administration by injection which takes the drug directly into the tissue fluid or blood without having to cross the enteral mucosa. The limitations of oral administration are circumvented. Drug action is faster and surer (valuable in emergencies). Gastric irritation and vomiting are not provoked. Parenteral routes can be employed even in unconscious, uncooperative or vomiting patient. There are no chances of interference by food or digestive juices. Liver is bypassed. Disadvantages of parenteral routes are—the preparation has to be sterilized and is costlier, the technique is invasive and painful, assistance of another person is mostly needed (though self injection is possible, e.g. insulin by diabetics), there are chances of local tissue injury and, in general, parenteral route is more risky than oral.
The important parenteral routes are:
(i) Subcutaneous (s.c.)
The drug is deposited in the loose subcutaneous tissue which is richly supplied by nerves (irritant drugs cannot be injected) but is less vascular (absorption is slower than intramuscular). Only small volumes can be injected s.c. Self-injection is possible because deep penetration is not needed. This route should be avoided in shock patients who are vasoconstricted— absorption will be delayed. Repository (depot) preparations that are aqueous suspensions can be injected for prolonged action. Some special forms of this route are:
In this method needle is not used; a high velocity jet of drug solution is projected from a microfine orifice using a gun like implement. The solution passes through the superficial layers and gets deposited in the subcutaneous tissue. It is essentially painless and suited for mass inoculations.
(b) Pellet implantation
The drug in the form of a solid pellet is introduced with a trochar and cannula. This provides sustained release of the drug over weeks and months, e.g. DOCA, testosterone.
(c) Sialistic (nonbiodegradable) and biodegradable implants
Crystalline drug is packed in tubes or capsules made of suitable materials and implanted under the skin. Slow and uniform leaching of the drug occurs over months providing constant blood levels. The nonbiodegradable implant has to be removed later on but not the biodegradable one. This has been tried for hormones and contraceptives (e.g. NORPLANT).
(ii) Intramuscular (i.m.)
The drug is injected in one of the large skeletal muscles—deltoid, triceps, gluteus maximus, rectus femoris, etc. Muscle is less richly supplied with sensory nerves (mild irritants can be injected) and is more vascular (absorption of drugs in aqueous solution is faster). It is less painful, but self injection is often impracticable because deep penetration is needed. Depot preparations (oily solutions, aqueous suspensions) can be injected by this route. Intramuscular injections should be avoided in anticoagulant treated patients, because it can produce local haematoma.
(iii) Intravenous (i.v
.) The drug is injected as a bolus (Greek: bolos–lump) or infused slowly over hours in one of the superficial veins. The drug reaches directly into the blood stream and effects are produced immediately (great value in emergency). The intima of veins is insensitive and drug gets diluted with blood, therefore, even highly irritant drugs can be injected i.v., but hazards are—thrombophlebitis of the injected vein and necrosis of adjoining tissues if extravasation occurs. These complications can be minimized by diluting the drug or injecting it into a running i.v. line. Only aqueous solutions (not suspensions, because drug particles can cause embolism) are to be injected i.v. and there are no depot preparations for this route. Chances of causing air embolism is another risk. The dose of the drug required is smallest (bioavailability is 100%) and even large volumes can be infused. One big advantage with this route is—in case response is accurately measurable (e.g. BP) and the drug short acting (e.g. sodium nitroprusside), titration of the dose with the response is possible. However, this is the most risky route—vital organs like heart, brain, etc. get exposed to high concentrations of the drug.
The drug is injected into the skin raising a bleb (e.g. BCG vaccine, sensitivity testing) or scarring/multiple puncture of the epidermis through a drop of the drug is done. This route is employed for specific purposes only.
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What are Local anaesthetics? Local anaesthetics – Local anesthetics are drugs which produce insensitivity in a limited area around the site of application or injection of the drug by preventing generation and conduction of impulses along nerve fibers and nerve ending and the effects are reversible. What are Anthelmintics Anthelmintics – The drugs which are used to kill or remove the parasitic worms, the term anthelmintic should not be restricted just to drugs acting locally to expel worms from the g.i.t. Various types of worms are able to penetrate tissues, & the drugs used to act against systemic infections should be included also under the general term anthelmintic. What are anticoagulants? Anticoagulants – An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting & anticoagulants are given to people to stop thrombosis (blood clotting inappropriately in the blood vessels).
What are Diagnostic agents? Diagnostic agents – These are the agents or chemicals used to detect abnormalities in tissues & organs or to test an organ function, these are thus useful for the clinical diagnosis of the diseases & these agents do not usually have any medicinal values or pharmacological effect.
What are sympathomimetics?
Sympathomimetics – Drugs that mimic the actions obtained as a result of stimulation of the sympathetic or adrenergic nerves are called Sympathomimetics.
The drugs that produce pharmacological effects like adrenaline or nor adrenaline or drugs which bring about stimulation of adrenergic nerves are called Sympathomimetics.
Diuretics – Drugs which promote excretion of water & electrolytes from body through kidneys in the form of urine are called diuretics.
Define antimalarials, Classify them with suitable examples and give the structure of
Anti-malarial drugs: – The drugs which are used in the treatment of malaria caused due
to Plasmodium Species like Plasmodium Vivax, P. falcifrum, P.malariae, P. ovale are called as Anti-malarial drugs.
Quinine salts e.g. Quinine sulphate, Quinine phosphate, Quinine dihydrochloride.
8-Aminoquinolines e.g. Pentaquine, Isopentaquine, Pamaquine, Primaquine.
4-Aminoquinolines e.g. Chloroquine , Amodiaquine.
9-Aminoacridines e.g. Quinacrine, Mepacrine.
Biguanides e.g. Proguanil, Cycloguanil
Artemisinin & its derivatives.
Miscellaneous: – They are further classified as mentioned below
Sulfones & sulfonamides.
Write physiological actions of histamine. Classify antihistaminics with examples.
Histamine is a biogenic amine involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
Histamine triggers the inflammatory response. As part of an immune response to foreign pathogens, histamine is produced by basophils and by mast cells found in nearby connective tissues.
marks physiological actions,
Physiological actions of histamine on various organs:
Blood vessels: Histamine causes dilation of blood vessels
Smooth muscle: It causes contraction of smooth muscle (Contraction of bronchi)
Excretory glands: Histamine has stimulant action on excretory glands. It increases nasal, lachrymal and bronchial secretion.
Acid secretion: Histamine increases acid secretion in stomach which causes peptic ulcer
Oedema: Excess secretion of histamine causes accumulation of fluid and water in the body.
Allergy: It plays an important role in human allergy and allergic reactions.
Classification of antihistaminics:
H1 blockers or H1 antagonist:
Aminoalkylethers/Ethanolamines e.g. Diphenhydramine, Doxylamine
Second generation antihistaminics: e.g. Cetrizine, Levocetrizine, Fexofenadine, Terfenadine
H2 Blockers or H2 receptor antagonist e.g. Ranitidine, Cimetidine, Famotidine An inhibitor of histamine release e.g.Sodium Cromoglycate
Define vitamins. Write the important uses of vit. A, Nicotinic acid and ascorbic acid. 1 mark each.
Vitamins may be defined as potent organic substances which are essential for normal growth and maintenance of life of human and animals, which are not able to synthesize in adequate quantity.
Uses of Niacin or Nicotinic acid-
It is used for preventing vitamin B3 deficiency and related conditions such as pellagra.
Biochemically active form of Nicotinic acid is NAD (Nicotinamide adenine dinucleotide) and its phosphate (NADP). These two coenzymes are required in protein and amino acid metabolism and electron transfer reaction in respiratory chain. It causes peripheral vasodilation
Large dose of nicotinic acid decreases serum cholesterol level.
Uses of Vitamin A-
It is used for treating vitamin A deficiency.
Prevention and treatment of Night blindness, Xerophthalmia and keratomalacia.
A is important for growth, development and maintenance of immune system.
Some people use vitamin A for improving vision and treating eye disorders including age-related macular degeneration (AMD), glaucoma and
Vitamin A is also used for skin conditions including acne, eczema, psoriasis, cold sores, wounds, burns, sunburn.
Uses of Ascorbic acid-
In general this drug is used for the prevention and treatment of scurvy. This condition is caused by a lack of vitamin C often due to a lack of fresh fruit and vegetables. Symptoms of scurvy include a general feeling of being unwell, tiredness, muscle and joint pain, bleeding into the skin, around bones, into joints and from the gums, and loose teeth. Ascorbic acid is involved in many redox reactions
Uses of Pethidine-
Analgesic activity: It is used in the treatment of severe pain like labor pain.
Spasmolytic agent: Pethidine is useful in the treatment of spasm of intestine, urinary bladder
Used as a substitute for morphine for the relief of most types of moderate to severe pains.
Used in combination with chlorpromazine & promethazine to produce narcosis.
It also produces mild euphoria.
Give storage conditions for
The aqueous solution is stable for at least 7 years at pH 7 to 8.
It is stored in sealed, sterile container so as to exclude microorganism and moisture.
It is stored in metal cylinder designed to hold compressed gases and kept in a cool room free from inflammable material.
The whole cylinder is painted orange. The shoulder should be stenciled with name or symbol “C3H6”. The name or symbol should be clearly stamped on the cylinder valve.
d) Write the difference between general anaesthetics and local anaesthetics. Give the
structure and chemical name of procaine.
2 marks for
Structure of procaine
H2N C O C2H5
Chemical name – 4-amino-(2-diethyl amino ethyl) benzoate or 2-(Diethyl amino)
Distinguish between general anaesthetics and local anaesthetics
GENERAL ANAESTHETICS LOCAL ANAESTHETICS
1. General anaesthetics are the agents which It may be defined as any substance bring about loss of all modalities of sensation, applied topically or by localized particularly pain, along with a reversible loss injection or infiltration to dull or block of consciousness.
. pain sensation.
2. General anesthesia is induced either by Local anesthesia is induced by topical inhalation of volatile & gaseous anesthetics application of drugs to skin or mucous like diethyl ether, halothane or parenteral membrane (surface anesthesia) or by administration of intravenous anesthetics injection into area subjected to surgical like thiopentone sodium. operation (infiltration anaesthesia) or
injection into dual membrane of spinal
cord (spinal anesthesia)
3. General anaesthesia is produced before Local Anaesthesia is produced in short carrying out surgical operation or in surgical procedures & in dentistry. obstetrics.
4.Care of Vital organs essential Care of Vital organs is not essential
E.g. halothane ,cycloprapane etc. E.g. procaine, lignocaine, benzocaine
Define and classify antihypertensive drugs.
Any agent used for reducing elevated blood pressure is known as antihypertensive agent or hypotensive agent.
Antihypertensive agents can be classified as follows below:-
Centrally acting agents: e.g. α-methyldopa, clonidine
Ganglion blockers : e.g. Pentolinium, Mecamylamine
Adrenergic neuron blockers e.g. Reserpine, Guanethidine
β-adrenergic blockers e.g. Propranalol, Atenolol
α-adrenergic blockers e.g. Prazosin, Tolazoline
Direct-acting vasodilators e.g. Hydralazine, Minoxidil
Narcotic analgesics are derivatives of opium, semi synthetic or synthetic agents having potent analgesic & narcotic activity and effective for the treatment of severe pain. Classification of Narcotic analgesics
Narcotic analgesic are classified as:-
Morphine and related compounds (Natural alkaloids of opium) e.g. Morphine, Codeine.
Semi-synthetic derivatives of morphine- Heroin, Brown Sugar Marks Classification 1Mark str.
What do you know about sex hormones? Give the uses of Progesterone and Cortisone.
Sex hormones are the hormones which are produced mainly in gonads, ovaries or testes. They influence the development and maintenance of the structures directly and indirectly associated with reproduction. Three main types of sex hormones are
Androgenic or anabolic steroids :-
The androgens are mainly able to maintain the development and maintenance of the secondary male sex characters, thereby increasing virility and libido.
Oestrogens :- Oestrogens influence development and maintenance of secondary female sex characters. They are also essential for maintenance of pregnancy. They also exert anabolic effect on protein metabolism & water retention.
Progestogens are necessary for various changes takes place in uterus & vagina during menstrual cycle, for developing mammary tissue and for maintain pregnancy.
Uses of Progesterone:
It is used as a hormonal replacement therapy in deficiency of progesterone.
It is used in treatment of dysfunctional uterine bleeding.
It is also used along with estrogen in menstrual disorders, premenstrual tension
It is used in treatment of neoplasm of breast and endometriosis.
It has also been incorporated into an intra-uterine device for female contraception.
Treatment of habitual abortion.
Maintenance of pregnancy if it occurs.
Uses of Cortisone:
Anti-inflammatory action: Cortisone is a steroid that prevents the release of substances in the body that cause inflammation.
Cortisone is used to treat many different conditions such as allergic disorders, skin conditions, ulcerative colitis, arthritis, lupus, psoriasis, or breathing disorders.
1 Mark sex hormones,
1.5 Marks to uses of each drug
Subject Title: Pharmaceutical Chemistry-I I Subject Code:
Treatment of rheumatoid arthritis and osteoarthritis
Treatment of lung infection
Treatment of allergic conjunctivitis
It has immune suppressant action hence used in organ transplantation and autoimmune disorder.
Treatment of Addison’s disease.
Write the structure and uses of
Atropine has antispasmodic action on smooth muscles, hence used for the treatment of gastric and duodenal ulcers and for the relief of renal and biliary colics. Useful in symptomatic treatment of Parkinsonism.
It is one of the components of pre-anaesthetic medication, where it is given to reduce salivary and bronchial secretions and to diminish the risk of vagal inhibition of the heart.
It is used by ophthalmologist for its mydriatic effects.
Treatment of hyperhidrosis (Abnormal increased sweating)
Treatment of various cardiac diseases like Cardiac arrhythmia, Arterial hypertension,
What are anti-amoebic agents? Classify them with suitable examples.
Anti-amoebic agents: The drugs which are used in the treatment of amoebic infection caused by Entamoeba histolytica are called as antiamoebic drugs.
Classification of antiamoebic drugs:
Drugs of natural origin: g. emetin
Quinoline derivative e.g. Chloroquine
Halogenated-8-hydroxyquinoline derivative e.g. quinidochlor, Diiodohydroxyquinoline
Nitro-imidazole derivative e.g. Metronidazole, Tinidazole
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Antibiotic: e.g. Paramomycin, Tetracycline, chlortetracycline, oxythromycin
Organic arsenicals: e.g. carbarsone
Miscellaneous e.g Diloxanide furoate
Explain the process of blood coagulation. Write the structure and chemical name of
Process of blood coagulation:
Thrombin and several clotting factors present in plasma and calcium ions are involved in the coagulation. Process of blood coagulation can be described as follows.
Whenever there is an injury to a blood vessel, there is formation of rough surface. When blood platelets come in contact with such a rough surface, they are injured.
Due to injury, they release the substance called thromboplastin. In the presence of thromboplastin and calcium in the blood plasma prothrombin is converted into thrombin which helps in conversion of fibrinogen to fibrin.
The fibrin is insoluble and forms threads. The threads of fibrin form a net. In the holes of this net, blood cells are entangled. This mass then contracts to form a blood clot.
Anti-inflammatory and analgesic in rheumatoid arthritis
Treatment of spondylitis, osteoarthritis and in gout
Treatment of dysmenorrhea and migraine.
To relieve bronchial spasm in acute attacks of asthma.
It is used to increase blood pressure in treatment of hypotension.
Intra venous administration of Adrenaline is used to treat acute circulary collapse or cardiac arrest.
Treatment of allergic disorder.
Treatment of superficial bleeding due to its vasoconstriction effect.
Added to local anesthetic to prolong the duration of effect.
It has mydriatic effect.
Define and classify cholinergic drugs. Write the uses of Acetylcholine Definition:
The agents that mimic the action of acetylcholine or produce the effect of parasympathetic nerve stimulation are called as cholinergic drugs or parasympathomimetic agents.
Pharmacodynamics the branch of pharmacology concerned with the effects of drugs and the mechanism of their action.
“Pharmacodynamics involves how the drugs act on target cells to alter cellular function.”
A. Receptor and non-receptor mechanisms: Most of the drugs act by interacting with a cellular component called receptor. Some drugs act through simple physical or chemical reactions without interacting with any receptor.
• Receptors are protein molecules present either on the cell surface or with in the cell e.g. adrenergic receptors, cholinoceptors, insulin receptors, etc. • The endogenous neurotransmitters, hormones, autacoids and most of the drugs produce their effects by binding with their specific receptors. • Aluminium hydroxide and magnesium trisilicate, which are used in the treatment of peptic ulcer disease act by non-receptor mechanism by neutralizing the gastric acid.
Many drugs are similar to or have similar chemical groups to the naturally occurring chemical and have the ability to bind onto a receptor where one of two things can happen- either the receptor will respond or it will be blocked. A drug, which is able to fit onto a receptor, is said to have affinity for that receptor. Efficacy is the ability of a drug to produce an effect at a receptor. An agonist has both an affinity and efficacy whereas antagonist has affinity but not efficacy or intrinsic activity. When a drug is able to stimulate a receptor, it is known as an agonist and therefore mimics the endogenous transmitter. When the drug blocks a receptor, it is known as antagonist and therefore blocks the action of the endogenous transmitter (i.e. it will prevent the natural chemical from acting on the receptor). However, as most drug binding is reversible, there will be competition between the drug and the natural stimulus to the receptor.
Covalent bond is the strongest bond and the drug-receptor complex is usually irreversible. K1 K3 DR Biological effect D+R K2 Where D = Drug, R= receptor DR= Drug receptor complex (affinity) K1 = association constant K2 = dissociation constant K3 = intrinsic activity When first messengers like neurotransmitters, hormones, autacoids and most of drugs bind with their specific receptors, the drug receptor complex is formed which subsequently causes the synthesis and release of another intracellular regulatory molecule termed as second messengers e.g. cyclic AMP, calcium, cyclic GMP, inositol triphosphate (IP3), diacylglycerol and calmodulin which in turn produce subcellular or molecular mechanism of drug action.
B. Site of drug action:
– A drug may act: (i) Extracellularly e.g: osmotic diuretics, plasma expanders. (ii) On the cell surface e.g.: digitalis, penicillin, catecholamines (iii) Inside the cell e.g.: anti-cancer drugs, steroid hormones. C. Dose Response relationship The exact relationship between the dose and the response depends on the biological object under observation and the drug employed. When a logarithm of dose as abscissa and responses as ordinate are constructed graphically, the “S” shaped or sigmoid type curve is obtained. The lowest concentration of a drug that elicits a response is minimal dose, and the largest concentration after which further increase in concentration will not change the response is the maximal dose. 1. Graded dose effect: As the dose administered to a single subject or tissue increases, the pharmacological response also increases in graded fashion up to ceiling effect. – It is used for characterization of the action of drugs. The concentration that is required to produce 50 % of the maximum effect is termed as EC50 or ED50.50
2. Quantal dose effect: It is all or none response, the sensitive objects give response to small doses of a drug while some will be resistant and need very large doses. The quantal dose effect curve is often characterized by stating the median effective dose and the median lethal dose. Median lethal dose or LD50: This is the dose (mg/kg), which would be expected to kill one half of a population of the same species and strain. Median effective dose or ED50: This is the dose (mg/kg), which produces a desired response in 50 per cent of test population. Therapeutic index: It is an approximate assessment of the safety of the drug. It is the ratio of the median lethal dose and the median effective dose. Also called as therapeutic window or safety.
The larger the therapeutic index, the safer is the drug. Penicillin has a very high therapeutic index, while it is much smaller for the digitalis preparation.
D. Structural activity relationship
The activity of a drug is intimately related to its chemical structure. Knowledge about the chemical structure of a drug is useful for: (i) Synthesis of new compounds with more specific actions and fewer adverse reactions (ii) Synthesis of competitive antagonist and (iii) Understanding the mechanism of drug action. Slight modification of structure of the compound can change the effect completely.
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Pharmacodynamics of atropine:
Atropine, a naturally occurring belladonna alkaloid, is a racemic mixture of equal parts of d- and l-hyoscyamine, whose activity is due almost entirely to the levo isomer of the drug. Atropine is commonly classified as an anticholinergic or antiparasympathetic (parasympatholytic) drug. More precisely, however, it is termed an antimuscarinic agent since it antagonizes the muscarine-like actions of acetylcholine and other choline esters. Adequate doses of atropine abolish various types of reflex vagal cardiac slowing or asystole. The drug also prevents or abolishes bradycardia or asystole produced by injection of choline esters, anticholinesterase agents or other parasympathomimetic drugs, and cardiac arrest produced by stimulation of the vagus. Atropine may also lessen the degree of partial heart block when vagal activity is an etiologic factor. Atropine in clinical doses counteracts the peripheral dilatation and abrupt decrease in blood pressure produced by choline esters. However, when given by itself, atropine does not exert a striking or uniform effect on blood vessels or blood pressure.
Pharmacodynamics of Furosemide
Furosemide, a sulfonamide-type loop diuretic structurally related to bumetanide, is used to manage hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome.
Furosemide, a loop diuretic, inhibits water reabsorption in the nephron by blocking the sodium-potassium-chloride cotransporter (NKCC2) in the thick ascending limb of the loop of Henle. This is achieved through competitive inhibition at the chloride binding site on the cotransporter, thus preventing the transport of sodium from the lumen of the loop of Henle into the basolateral interstitium. Consequently, the lumen becomes more hypertonic while the interstitium becomes less hypertonic, which in turn diminishes the osmotic gradient for water reabsorption throughout the nephron. Because the thick ascending limb is responsible for 25% of sodium reabsorption in the nephron, furosemide is a very potent diuretic.
Pharmacodynamics of Heparin
Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.
Mechanism of action
Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.
Pharmacodynamics of paracetamol Pharmacodynamics of Acetaminophen
Acetaminophen (USAN) or Paracetamol (INN) is a widely used analgesic and antipyretic drug that is used for the relief of fever, headaches, and other minor aches and pains. It is a major ingredient in numerous cold and flu medications and many prescription analgesics. It is extremely safe in standard doses, but because of its wide availability, deliberate or accidental overdoses are not uncommon. Acetaminophen, unlike other common analgesics such as aspirin and ibuprofen, has no anti-inflammatory properties or effects on platelet function, and it is not a member of the class of drugs known as non-steroidal anti-inflammatory drugs or NSAIDs. At therapeutic doses acetaminophen does not irritate the lining of the stomach nor affect blood coagulation, kidney function, or the fetal ductus arteriosus (as NSAIDs can). Like NSAIDs and unlike opioid analgesics, acetaminophen does not cause euphoria or alter mood in any way. Acetaminophen and NSAIDs have the benefit of being completely free of problems with addiction, dependence, tolerance and withdrawal. Acetaminophen is used on its own or in combination with pseudoephedrine, dextromethorphan, chlorpheniramine, diphenhydramine, doxylamine, codeine, hydrocodone, or oxycodone.
Mechanism of action:
Acetaminophen is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1, COX-2, and COX-3 enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme’s active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation, sweating and hence heat dissipation.
Pharmacodynamics of salbutamol
Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is sold in its pure form as Levalbuterol. The manufacturer of levalbuterol, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side-effects.
Mechanism of action:
Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In addition to bronchodilation, salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leakage, and enhances mucociliary clearance.
Pharmacodynamics of vamana
The overall Pharmacodynamic of Vamanopaga dasemāni drugs is based on guna concept. Most of the drugs (90%) are having property of Laghu and Ruksa guna. These are based on Vāyu, Agni and Ākasa mahābhaūtik (one of the five elements of the universe) composition. Ācarya Caraka has mentioned only the role of gunas in the Pharmacodynamic of Vamana karma (Bhadanta Nāgārjunā, Rasavaisesika, 2010). In fact guna is the thing which represents a drug. So, the selection of a drug should be on the basis of gunas for Vamana karma. Ācarya has mentioned predominance of Vāyu and Agni mahābhūta drugs for Vamana karma. Rasas (taste) of vamana dravyas are chiefly katu and kasāya rasa which are composition of the same mahābhūtas. Most of drugs are katu Vipāka having similar bhaūtic constitution. Other drugs are supportive to the therapy or to avoid complications during Vamana karma. As an example; honey which is mentioned in Vamanopaga dasemāni is added to Vamana kalpa (prepared medicine) for increasing the palatability and giving soothing effect. Āyurveda says it is a good kapha chedaka (expectorant), helps in better expulsion of malarūpī kapha by vamana karma. Likewise Saindhava (salt) should be added to Vamana kalpa for Vilāyana (Agnivesa, Caraka Samhita, 2001) (liquefying) of sticky Kaphadosa in channels. Effect of both the drugs is to help in a comfortable and irritation less procedure. added to Vamana kalpa for Vilāyana (Agnivesa, Caraka Samhita, 2001) (liquefying) of sticky Kaphadosa in channels. Effect of both the drugs is to help in a comfortable and irritation less procedure.
Pharmacodynamics of basti
Basti is chief Panchakama procedure used in Ayurveda. The pharmacodynamics of systemic effect of Basti may be understood through absorption mechanism, concept of system biology, neural stimulation mechanism, and excretory mechanism. As Basti is homogenous emulsion mixture of Honey, Saindhava,Sneha Dravya, Kalka, and decoction of crude drugs and Prakshepa Dravya, which is given through rectum, is absorbed, hence Basti is used as route of drug administration. Through rectal route large quantity of drugs can be delivered for systemic circulation and act accordingly. Concept of system biology opines that a change at cellular level of a system can bring changes in tissue, organ and system and in another system consequently & finally in whole body. As per recent advancement intestine not only is highly vascular but also highly innervated organ which forms ‘Enteric Nervous System’ (ENS).ENS may works in synergism with Central Nervous System of body. The cleansing action of Basti is related with the facilitation of excretion of morbid substances responsible for the disease process into the colon, from where it is evacuated.
Basti being the most widely used and highly effective treatment modality in the Ayurveda, it is the prime subject of interest for modern scientific community. With this background the basic question which comes forward regarding Basti is, “do active principles of drugs used in Basti get absorbed in systemic circulation. Triphaladi decoction Basti containing biomarker gallic acid and after Basti they traced it in the circulation. The rectum has rich blood and lymph supply and drugs can cross the rectal mucosa like other lipid membrane. Thus unionised and lipid soluble substances are readily absorbed from the rectal mucosa. Small quantity of short chain fatty acid fatty acids, such as those from butterfat are absorbed directly into portal blood rather than being converted into triglycerides. This is because short chain fatty acids are more water soluble and allow direct diffusion from the epithelial cells into capillary blood of villi. However decoction Basti gets a very little time maximum 48 minutes to absorb from colon and rectum how so ever these areas have very large surface area and highly vascular needed for absorption. Retention time for Anuvashana Basti is relatively more so probability of absorption also increases. Anuvasana Basti after reaching in the rectum and colon causes secretion of bile from gall bladder which leads to the formation of conjugate micelles which is absorbed through passive diffusion. Especially short chain fatty acid present in Sneha of Anuvasana Basti may absorb from colon and large intestine part of gastrointestinal tract and break the pathology of disease. In Basti Karma, a homogenous emulsion
2) By System Biology Concept of Honey, Saindhava, Sneha Dravya, Kalka, and decoction mixed in remarkable combination after proper churning (break the large and middle chain fatty acid into small chain fatty acids) is given which facilitates absorption better then a single drug per rectum. In Ayurveda classics, various Basti Dravya are mentioned in diverse proportion in different diseases, it again confirms pharmacodynamics of Basti through absorption mechanism
Pharmacodynamics of phenytoin
Phenytoin is an antiepileptic drug which can be useful in the treatment of epilepsy. The primary site of action appears to be the motor cortex where spread of seizure activity is inhibited. Phenytoin reduces the maximal activity of brain stem centers responsible for the tonic phase of tonic-clonic (grand mal) seizures. Phenytoin acts to dampen the unwanted, runaway brain activity seen in seizure by reducing electrical conductance among brain cells. It lacks the sedation effects associated with phenobarbital. There are some indications that phenytoin has other effects, including anxiety control and mood stabilization, although it has never been approved for those purposes by the FDA. Phenytoin is primarily metabolized by CYP2C9.
Mechanism of action
Phenytoin acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. By promoting sodium efflux from neurons, phenytoin tends to stabilize the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing membrane sodium gradient. This includes the reduction of post-tetanic potentiation at synapses. Loss of post-tetanic potentiation prevents cortical seizure foci from detonating adjacent cortical areas.
Pharmacodynamics of Aspirin
Acetylsalicylic acid is an analgesic, antipyretic, antirheumatic, and anti-inflammatory agent. Acetylsalicylic acid’s mode of action as an antiinflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. Acetylsalicylic acid appears to produce analgesia by virtue of both a peripheral and CNS effect. Peripherally, acetylsalicylic acid acts by inhibiting the synthesis and release of prostaglandins. Acting centrally, it would appear to produce analgesia at a hypothalamic site in the brain, although the mode of action is not known. Acetylsalicylic acid also acts on the hypothalamus to produce antipyresis; heat dissipation is increased as a result of vasodilation and increased peripheral blood flow. Acetylsalicylic acid’s antipyretic activity may also be related to inhibition of synthesis and release of prostaglandins.
Mechanism of action:
The analgesic, antipyretic, and anti-inflammatory effects of acetylsalicylic acid are due to actions by both the acetyl and the salicylate portions of the intact molecule as well as by the active salicylate metabolite. Acetylsalicylic acid directly and irreversibly inhibits the activity of both types of cyclooxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. This makes acetylsalicylic acid different from other NSAIDS (such as diclofenac and ibuprofen) which are reversible inhibitors. Salicylate may competitively inhibit prostaglandin formation. Acetylsalicylic acid’s antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms; the therapeutic effects are not due to pituitary-adrenal stimulation. The platelet aggregation-inhibiting effect of acetylsalicylic acid specifically involves the compound’s ability to act as an acetyl donor to cyclooxygenase; the nonacetylated salicylates have no clinically significant effect on platelet aggregation. Irreversible acetylation renders cyclooxygenase inactive, thereby preventing the formation of the aggregating agent thromboxane A2 in platelets. Since platelets lack the ability to synthesize new proteins, the effects persist for the life of the exposed platelets (7-10 days). Acetylsalicylic acid may also inhibit production of the platelet aggregation inhibitor, prostacyclin (prostaglandin I2), by blood vessel endothelial cells; however, inhibition prostacyclin production is not permanent as endothelial cells can produce more cyclooxygenase to replace the non-functional enzyme.
Pharmacodynamics of pantaprazole
Pantoprazole is a substituted benzimidazole indicated for the short-term treatment (up to 16 weeks) in the healing and symptomatic relief of erosive esophagitis. Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production.
Mechanism of action:
Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by forming a covalent bond to two sites of the (H+,K+ )- ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect is dose- related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus.
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What is Pharmacology:
Pharmacology is the study of interaction of drugs with living organisms. It also includes history, source, physicochemical properties, dosage forms, methods of administration, absorption, distribution mechanism of action, biotransformation, excretion, clinical uses and adverse effects of drugs. Pharmacology is both a basic and an applied science. It forms the backbone of rational therapeutics.Whereas the medical student and the prescribing physician are primarily concerned with the applied aspects, correct and skillful application of drugs is impossible without a proper understanding of their basic pharmacology. Medical pharmacology, therefore, must include both fundamental background and clinical pharmacological information. Objective and quantitative data on the use of drugs in man, i.e., relationship between plasma concentration and intensity of therapeutic/toxic actions, plasma half lives, relative efficacy of different medications and incidence of adverse effects etc., are being obtained with the aim of optimising drug therapy. The concepts regarding mechanism of action of drugs are changing. In addition, new drugs are being introduced in different countries at an explosive pace. A plethora of information thus appears to be important.
Here is a overview of General Pharmacology Text Books:
Section 1 General Pharmacological Principles 1. Introduction, Routes of Drug Administration 2. Pharmacokinetics: Membrane Transport, Absorption and Distribution of Drugs 3. Pharmacokinetics: Metabolism and Excretion of Drugs, Kinetics of Elimination 4. Pharmacodynamics: Mechanism of Drug Action; Receptor Pharmacology 5. Aspects of Pharmacotherapy, Clinical Pharmacology and Drug Development 6. Adverse Drug Effects 82 Section 2 Drugs Acting on Autonomic Nervous System 7a. Autonomic Nervous System: General Considerations 7b. Cholinergic System and Drugs 99 8. Anticholinergic Drugs and Drugs Acting on Autonomic Ganglia 9. Adrenergic System and Drugs 10. Antiadrenergic Drugs (Adrenergic Receptor Antagonists) and Drugs for Glaucoma
Section 3 Autacoids and Related Drugs 11. Histamine and Antihistaminics 2. 5-Hydroxytryptamine, its Antagonists and Drug Therapy of Migraine 13. Prostaglandins, Leukotrienes (Eicosanoids) and Platelet Activating Factor 14. Nonsteroidal Antiinflammatory Drugs and Antipyretic-Analgesics 15. Antirheumatoid and Antigout Drugs Section 4 Respiratory System Drugs 16. Drugs for Cough and Bronchial Asthma Section 5 Hormones and Related Drugs 17a. Introduction 17b. Anterior Pituitary Hormones 18. Thyroid Hormone and Thyroid Inhibitors 19. Insulin, Oral Hypoglycaemic Drugs and Glucagon 20. Corticosteroids 282 21. Androgens and Drugs for Erectile Dysfunction 22. Estrogens, Progestins and Contraceptives 23. Oxytocin and Other Drugs Acting on Uterus 24. Drugs Affecting Calcium Balance Section 6 Drugs Acting on Peripheral (Somatic) Nervous System 25. Skeletal Muscle Relaxants 26. Local Anaesthetics Section 7 Drugs Acting on Central Nervous System 27. General Anaesthetics 28. Ethyl and Methyl Alcohols 29. Sedative-Hypnotics 30. Antiepileptic Drugs 31. Antiparkinsonian Drugs 32. Drugs Used in Mental Illness: Antipsychotic and Antimanic Drugs 33. Drugs Used in Mental Illness: Antidepressant and Antianxiety Drugs 454 34. Opioid Analgesics and Antagonists 469 35. CNS Stimulants and Cognition Enhancers 486
Section 8 Cardiovascular Drugs 36a. Cardiac Electrophysiological Considerations 36b. Drugs Affecting Renin-Angiotensin System and Plasma Kinins 37. Cardiac Glycosides and Drugs for Heart Failure 512 38. Antiarrhythmic Drugs 526 39. Antianginal and Other Anti-ischaemic Drugs 40. Antihypertensive Drugs 558 Section 9 Drugs Acting on Kidney 41a. Relevant Physiology of Urine Formation 41b. Diuretics 579 42. Antidiuretics 593 Section 10 Drugs Affecting Blood and Blood Formation 43. Haematinics and Erythropoietin 599 44. Drugs Affecting Coagulation, Bleeding and Thrombosis 45. Hypolipidaemic Drugs and Plasma Expanders 634 Section 11 Gastrointestinal Drugs 46. Drugs for Peptic Ulcer and Gastroesophageal Reflux Disease 47. Antiemetic, Prokinetic and Digestant Drugs 48. Drugs for Constipation and Diarrhoea 672 Section 12 Antimicrobial Drugs 49. Antimicrobial Drugs: General Considerations 50. Sulfonamides, Cotrimoxazole and Quinolones 51. Beta-Lactam Antibiotics 716
52. Tetracyclines and Chloramphenicol (Broad-Spectrum Antibiotics) 53. Aminoglycoside Antibiotics 743 54. Macrolide, Lincosamide, Glycopeptide and Other Antibacterial Antibiotics; Urinary Antiseptics 752 55. Antitubercular Drugs 56. Antileprotic Drugs 57. Antifungal Drugs 58. Antiviral Drugs 59. Antimalarial Drugs 60. Antiamoebic and Other Antiprotozoal Drugs 61. Anthelmintic Drugs 849 Section 13 Chemotherapy of Neoplastic Diseases 62. Anticancer Drugs 857 Section 14 Miscellaneous Drugs 63. Immunosuppressant Drugs 64. Drugs Acting on Skin and Mucous Membranes 65. Antiseptics, Disinfectants and Ectoparasiticides 66. Chelating Agents 905 67. Vitamins 909 68. Vaccines and Sera 69. Drug Interactions
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1. Define various terminologies used in Pharmacology. 2. Know about nature and sources of drugs. 3. Understand pharmacodynamics like mechanism of drug action, dose relation ship and pharmacokinetics like absorption, distribution, metabolism and excretion (ADME) of drugs. 4. Understand theoritical pharmacokinetics like half-life, order of kinetics, steady state plasma concentration. 5. Understand drug safety and effectiveness like factors affecting drug action and adverse drug reactions. 6. Understand new drug development and evaluation
Here is a great article for our readers especially D Pharmacy 1st Year B Pharm First Sem students who are struggling to learn Anatomy & Physiology Subjects. Hence we provide Notes as Solved Question Paperwhich are very important for your examinations.
Give functions of mitochondria & endoplasmic reticulum. (1 mark each)
Mitochondria is known as power house of cell. They are involved in cellular respiration, the process by which chemical energy is made available in the cell. When nutrients and oxygen come in contact with the oxidative enzymes of mitochondria, they combine to form CO2, water & energy, this is in the form of ATP. (aerobic oxidation)
Endoplasmic reticulum are of two types. Smooth and rough. Smooth ER synthesizes lipids and steroid hormones and associated with detoxification of drugs. Rough ER is studded with ribosomes. It is a site of synthesis of proteins that are exported from
iii) White fibrous tissue iv) Yellow elastic tissue
Specialised connective tissue: i) Bone ii) Cartilage
Vascular tissue: i) Blood ii) Lymphoid tissue
c) What are true ribs & false ribs? ( 2 marks)
There are 12 pairs of ribs. Anteriorly, the first seven pairs of ribs are attached to the sternum via costal cartilage & are known as true ribs. The next three ribs are attached indirectly via seventh rib & known as false ribs
d) Write composition of blood. (2 marks)
It is composed of a liquid matrix plasma (55%) & different cells suspended in it (45%).
SA node(sinoatrial node) This is small mass of specialized neuromuscular cells in the walls of myocardium of right atrium near the opening of the superior vena cava. It is known as pacemaker of the heart as it initiates the impulses.
AV node- (atrioventricular node): This is the mass of neuromuscular cells in the wall of the atrial septum near the AV valves. Normally it conducts the impulses that are originated by SA node. It is known as secondary pace maker as it generates the impulses when there is problem with SA node.
g) Give the functions of CSF. (4 functions, 2 marks)
To support & protect brain & spinal
Maintain uniform pressure around
Acts as cushion & shock absorber
Keeps brain & spinal cord
h) Define (any two) (each 1 mark)
Presbyopia: As a process of aging, the lens loses its elasticity; the distant objects are seen clear but close objects are
Cataract: This is opacity of lens which may be age related or congenital bilateral or unilateral.
Hypermetropia: Also known as farsightedness. Far vision is normal but close vision is blurred, because the near image is focused behind the retina as eye ball length is too short or due to flattened
i) Write the functions of hypothalamus. ( 2 marks)
It controls the hormone release from pituitary
Control of autonomic nervous system, appetite & satiety, thirst, body , emotions, sexual behavior & biological clock.
j) Name any two cranial nerves with their function. (Any 2, 2 marks)
Olfactory – sense of smell
Optic – sense of light/vision
Occulomotor – movement of the eyeball, change shape of lens, Constriction of pupil, raising the upper lid.
Trochlear – movement of the eye
Trigeminal – receives impulses of pain temp. & touch for face & head, stimulates muscle of mastication
Abducent – abduction of eye ball
Facial – conveys impulse from taste buds & supplies muscles of facial expression
Auditory (vestibulocochlear) – conveys impulses to the cerebellum for posture &
Balance & sense of hearing
Glossopharyngeal – Sense of taste, production of saliva and movement of
Vagus – Secretion, movement in organs
Accessory – Movements of head, shoulder, pharynx and larynx
Hypoglossal – Supplies to the muscle of tongue & muscle surrounding the hyoid bone & helps in swallowing & speech.
k) What are auditory ossicles? (1 mark) Write their function. (1 mark)
Auditory ossicles: Malleus, incus & stapes are the three small bones in the middle ear extending from tympanic membrane to the oval window. Sound vibrations of tympanic membrane are amplified & transmitted by these bones.
l) What is B.P.? Name the factors affecting B.P. (def 1 mark and any 4 factors 1 mark)
B.P is the force or lateral pressure which the blood exerts on the wall of blood vessels. Factors affecting B.P. are exercise, nutrition, age, stress, circulating hormones, autonomic nervous system activity.
Q2. Solve any four of the following: 12
Define respiration. Write the process of external respiration. (def 1 mark, explanation 2 marks)
Respiration is a process of supply of oxygen present in atmosphere into the body & excretion for carbon dioxide.
External respiration- (cycle of breathing)
The normal human has 12-15 breath per min. Each breath consists of inspiration, expiration & pause.
Inspiration: The simultaneous contraction of intercostal muscles & diaphragm increases the capacity of thoracic cavity. This reduces the pressure in the lungs. To equalise the pressure the air from atmosphere enters the lungs. The process of inspiration is active as it needs energy for muscle contraction. It lasts for 2 sec.
Expiration: Relaxation of intercostal muscles & diaphragm results in decrease in the space in the lungs. As a result, the pressure inside the lungs increases as compared to atmospheric pressure. The air from the lungs is expelled from the lungs. This process is passive as does not require energy. The expiration lasts for 3 sec. After expiration there is pause & then the next cycle begins.
b) Write steps involved in urine formation. Describe selective reabsorption. (steps 1 mark, explanation 2 marks)
There are three processes of urine formation:
Selective reabsorption is the process by which the composition and volume of the glomerular filtrate is altered during its passage through the convoluted tubules, Loop of Henle and the collecting tubule. The purpose of this process is to reabsorb those constituents of the filtrate which are essential to the body, maintain the fluid and electrolyte balance and the alkalinity of blood.
Some constituents of the glomerular filtrate e.g. glucose; vitamins and amino acids get completely reabsorbed into the blood. These substances are called high- threshold substances.
Low-threshold substances like urea, uric acid are absorbed slightly.
Some substances e.g. creatinine are not at all absorbed.(no-threshold substances) Parathormone from parathyroid gland & calcitonin from thyroid gland regulate reabsorption of calcium & phosphate,
ADH from posterior pituitary increases the permeability of the tubule & increases water reabsorption.
Aldosterone by adrenal cortex increases reabsorption of sodium.
c)What is muscle tone? Give the functions of muscle. (muscle tone 1 mark, functions 2 marks)
Muscle tone is a sustained partial muscle contraction that allows maintenance of posture of the body.
Functions of the muscles are-
Skeletal muscles contract & help the movement of the body & stability of the joint. It also helps in generation of heat.Intercostal muscles help in respiration.
Smooth muscles helps contraction & relaxation of blood vessels & controls blood flow & movement of the food in the alimentary
Cardiac muscles help in the functioning of
d)Give the composition & function of gastric juice. (comp. 1 mark, functions 2 marks)
Composition of gastric juice:
Water, mineral salt, mucus, HCl, intrinsic factor, pepsinogen Functions of gastric juice-
Water liquifies the food.
HCl acidifies the food & stops the action of salivary
HCl kills the
Pepsinogen is activated to pepsin by HCl. This digests protein to smaller
Intrinsic factor absorbs vit. B12 from small
Mucus prevents mechanical injury to the stomach
e) Name hormones of adrenal cortex & mention their functions. (names 1 mark, functions 2 marks)
Adrenal cortex produces three groups of hormones namely glucocorticoids, Mineralocorticoid & androgens.
Glucocorticoids: Cortisol or hydrocortisone is the main glucocorticoid. Others are corticosterone & cortisone.
They regulate metabolism like gluconeogenesis, lipolysis and proteolysis. Mineralocorticoids (aldosterone.) It regulates water & electrolyte balance. It increases the reabsorption of Na ions.
Androgens: The compounds secreted are insignificant to show any action.
f) Define reproduction. Name the different reproductive organs of male reproductive system. (def 1 mark, organs 2 marks)
Reproduction is the process of formation of offspring OR It is defined as process by which genetic material is passed from one generation to another & thus maintains continuation of species.
The male reproductive system consists of the following organs:
Urethra & Penis
Q3. Solve any four of the following: 12
Give differences between striated and smooth muscles. (any 6 points, 3 marks)
It is also known as striated Muscle
Non‐ striated muscle
It is less extensible
It is more extensible
The fibres (cell) are cylindrical and has
The cells are spindle shaped
with only one central nucleus
They are under the control of our will. (voluntary)
They are not under the
control of our will.(involuntary)
The fibrous tissue enclosing
the whole muscle extends beyond the fibres to become the tendon which attaches the muscle to the bone or skin.
Bundles of fibres form sheets of muscle.
There is distinct sarcolemma
No distinct sarcolemma
Present in tongue, arms or hands, legs,
Present in oesophagus, stomach,
b) Define: ( 1 mark each)
Gout: Inflammation of joints due to deposition of sodium urate crystals in the joints.
Arthritis: Chronic disease that results in pain and restricted movement of
Sprain: Joint injury in which some of the fibres of supporting ligament are damaged OR If a ligament is stretched or torn; the injury is called a
c) Name different type of blood group. Explain the term universal donor and universal recipient. (name 1 mark, explanation 2 marks)
Different blood groups are: A, B, AB and O
Blood group “O” is called as Universal donor and Blood group “AB” is called as
Individuals have different antigens on the surface of their RBCs. These antigens determine their blood groups.
Blood group ‘O’ has neither A nor B antigen on their cell membrane. There will be no agglutination and thus blood can be safely transfused into A, B, AB and O. but can receive from only O.Therefore, blood group O is called universal donor.
Whereas blood group AB has neither antiA nor antiB antibodies. Transfusion of any group into these individuals is safe since there are no antibodies to react with them. But can donate only to AB. Hence it is called as universal recipient.
d) Define cardiac cycle. Write various events in cardiac cycle. (def 1 mark, explanation 2 marks)
Cardiac cycle: The events which occur in the heart during the circulation of blood during each heart beat is called cardiac cycle OR The series of events during one heart beat is known as cardiac cycle.
Events in cardiac cycle:
Atrial systole (0.1 sec)
Ventricular systole (0.3 sec)
Complete cardiac diastole (0.4 sec)
Description of cardiac cycle (2 marks)
The superior & inferior vena cava transport the deoxygenated blood into right atrium. At the same time four pulmonary veins transport oxygenated blood into the left atrium. The impulses from the SA node spreads over the atria, atria contracts, the AV valves open and & blood flows to ventricles. ( atrial systole-0.1 sec)
When the wave of contraction reaches AV node, it is stimulated & emits impulses which spreads over AV bundle, bundle branches & purkinje fibres resulting in contraction of ventricles pumping the blood into pulmonary artery & the aorta. (ventricular systole 0.3 sec). After the contraction of the ventricles there is complete cardiac diastole(0.4 sec) when both atria & ventricles relax. After this the next cycle begins.
e) What is reflex action? Draw a well-labelled diagram of reflex arc. (Reflex action 1 ½ marks, diagram 1 ½ marks)
Reflex action is an automatic motor response given by the spinal cord to the sensory stimulus without involving brain in action. They are a part of defensive mechanisms of the body.
Important reflex actions are:
Quick closing of an eyelid if eye is
Sudden withdrawal of hand if fingers touch something
Quick recovery of the balance of the body to prevent falling after a
Sudden coughing attack if a food particle is
Diagram of reflex arc:
f) Mention layers of epidermis of skin. State functions of skin. ( names of layers 1 mark, any 4 functions 2 marks)
Layers of epidermis:
Stratum corneum, stratum lucidum and stratum granulosum & stratum germinativum Functions of skin:
Protection – It forms the water proof layer & protects the inner delicate structures. It acts as the barrier against the invasion of the microbes, chemicals &dehydration. The melanin pigment protects against the harmful UV
Regulation of body temp.- The temp. is constant at 36.8o When the metabolic rate of the body increases the body temp increases & vice versa. To ensure constant body temp, a balance between heat production & heat loss is maintained by the skin.
Formation of vit. D.- 7-dehydroxycholesterol is present in the skin. The UV light from the sun converts it to vit.
Sensation – It contains nerve endings of many sensory nerves which act as organ of sensation of touch, temp, pressure and
Absorption- Some drugs & chemicals are absorbed through the
Excretion- Skin is a minor excretory organ & excretes NaCl, urea & sub. like garlic.
Q4. Solve any four of the following: 12
Define and give normal values: (1 mark for each)
Tidal volume: It is the volume of air moved in & out of lungs during normal breathing. Normal value is 500
Inspiratory reserve volume: It is the amount of air that can be breathed in and above the tidal volume by the deepest possible inspiration. Normal value is 1800 – 3000
Residual volume: It is the volume of air remaining in lungs after forced Normal value is 1.2 L in males and 1.1 L in females.
Give physiology of neuromuscular transmission. ( 3 marks)
When a nerve impulse reaches neuromuscular junction, passage of action potential over the sole feet causes the vesicles of acetylcholine to rupture into the synaptic cleft. The acetylcholine acts on the cell membrane to increase its permeability.
This allows spontaneous leakage of Na causing endplate potential. When the endplate potential increases, it stimulates the entire muscle fibre causing an action potential to travel in both directions along the fibre. When the action potential spread to inside of muscle fibre then Ca ions are released. This causes contraction of muscle fibres. Immediately after action potential is over, the previously released Ca ions recombine with reticulum and the muscle contraction stops.
The enzyme acetylcholinesterase present in the synaptic cleft. causes hydrolysis of acetylcholine. The muscle fibre is repolaised again to receive successive stimuli.
d) Describe the structure of stomach. ( str 2 marks, diag 1 mark)
Stomach is a J-shaped dilated portion of the alimentary canal. It is continuous with the oesophagus at cardiac sphincter and with duodenum at pyloric sphincter. It has 2 curvatures – lesser curvature and greater curvature. The stomach is divided into three regions- fundus, body & antrum. There are three layers of smooth muscle fibres outer longitudinal, the middle circular layer & the inner oblique fibres. This helps the churning movement & peristaltic movement.
e) What is endocrine and exocrine gland? Name the endocrine glands. (each def 1 mark, any 4 endocrine glands 1 mark)
Endocrine glands are ductless glands which release their secretions (hormones) directly into the blood.
Exocrine gland: The glands that discharge their secretions through the duct are known as exocrine glands.
Endocrine glands: Pituitary gland, thyroid gland, parathyroid glands, pancreas (islets of Langerhans). adrenal glands, pineal gland, testes in male and ovaries in female.
Menstruation: This is the series of events occurring regularly in females every 26-30 days throughout the child bearing age. The cycle consists of menstrual phase for 4 days, proliferative phase for 10 days & secretary phase for 14 days.
Proliferative phase: It is characterized by release of oestrogen by the maturing ovarian follicle under the influence of FSH from the anterior pituitary. Oestrogen stimulates the proliferation of the endometrium in preparation of the fertilized ovum. The endometrium becomes thicker by rapid cell multiplication and this is accompanied by an increase in the number of mucus-secreting glands and blood capillaries. This phase lasts for 10 days and stops when ovulation occurs and oestrogen production is inhibited i.e. when the ovarian follicle ruptures.
Q.5 Solve any four of the following: (12 marks, 03 marks each)
State the factors which accelerate and retard the clotting of blood. (3 marks, 1.5 marks each)
There are various factors which accelerate and retard the clotting of blood.
(1) Factors accelerating clotting are( any 3 points, 1.5 marks)
During menstruation and parturition
Injury to the walls of the blood vessels: An injury in the form of cut bleeds more freely than the injury by the
The venom of viper snakes
Higher temperature (above 46 0 C)
Presence of calcium salts
(2) Factors retarding clotting are (any 3 points, 1.5 marks):
In clinical condition like haemophilia, liver disease, afibrinogenemia, Christmas disease,
Removal calcium ions from the blood by addition of sodium or potassium or citrate
(c ) Calcium deficiency in blood
(d)Lower temperature: However, lower temperature causes contraction of blood vessels. ( e)Deficiency of vitamin K
(b) Describe how circulation of blood takes place through heart chambers. (3 marks)
The superior vena cava (for upper body) and inferior vena cava (for lower body) receive deoxygenated /impure blood from various part of the body through different veins. This deoxygenated/ impure blood they pour into the right atrium of heart. The blood from right atrium enters the right ventricle through a tricuspid valve, which prevent back flow of blood from ventricle into atrium.
The deoxygenated/ impure blood from right ventricle is forced into pulmonary artery through pulmonary valve. The pulmonary arteries divide into two branches each enters the right and left lungs. In the lungs, the red blood cells (RBCs) release carbon dioxide and absorbs oxygen. This oxygenated blood from right and left lungs is collected by four pulmonary veins and poured into left atrium. From left atrium this blood enters into left ventricle through bicuspid valve which prevents back flow of blood into left atrium.This oxygenated blood from left ventricle is forced into the aorta through aortic valve which prevent back flow of blood into left ventricle.
Give the various functions of medulla oblongata. (03 marks, 1mark for each function The vital centres consisting of group of cells associated with autonomic reflex activity lie in Medulla oblongata. They are,
Cardiac centre– The cardiac centre controls the rate and force of cardiac contraction and blood
Respiratory centre – The respiratory centre controls the rate and depth of respiration. Nerve impulses pass to the phrenic and intercostal muscles which stimulate the contraction of diaphragm and intercostal muscles, thus initiating
Vasomotor centre – This controls the diameter of blood vessels especially small arteries and arterioles.
Reflex centre – When irritating substance are present in stomach or respiratory tract, nerve impulse pass on to the medulla oblongata stimulating the reflex centre which initiate reflex actions like vomiting, sneezing and
(d) Explain retina of eye. (3marks)
Retina is the innermost layer of the eye. It gets stimulated by the light rays. It is composed of several layers of nerve cell body & the axons. There are light sensitive cells mainly of two types: the rods and
The entire retina contains about 7 million cones and 75 to 150 million
Rods function mainly in dim light and provide black-and-white vision, The rods have rhodopsin or visual purple is photosensitive pigment. It gets bleached with light & gets regenerated by vit. A. The rods are present more in the periphery of the
Cones sensitive to bright light & colour. cone opsins (also known as photopsins or iodopsin) present in cone cells, are used in colour
The central retina has macula lutea or yellow spot made up of only cone cells. It has central depression called fovea centralis.All the nerve fibres of retina form the optic nerve. The small area of the retina where the optic nerve leave the eye is known as optic disc or blind spot as no light sensitive cells are present here.
(e) Define nephritis. Give function of kidney. (Definition 1 mark, any 4 functions 2 marks)
Nephritis: Nephritis refers to inflammation of one or both kidneys due to infection or autoimmune disease.
Functions of kidney are:
Formation of urine –Each kidney consist of nephron which filter waste product from blood & helps in urine ,
Maintenance of acid base balance it helps maintaining pH by excretion of H+ ions & reabsorption of HCO3–
Maintenance of electrolyte balance
Maintenance of blood pressure. it regulates B.P. by Renin Angiotensin Aldosterone system
Maintenance of water Balance.it helps in maintaining water balance with the help of
Formation of erythropoietin hormone for erythropoeisis
(f) Define (3 marks, 1 mark for each definition)
Mastication: It is the process by which food is chewed and mixed with saliva to form a soft mass or bolus which is swallowed. ORMastication means chewing process takes place in mouth cavity.
Chyme: The thick semisolid mass of partially digested food that is passed from the stomach to the
ii) Digestion: The conversion of complex food ( carbohydrate , proteins & fats) into simpler form (glucose, amino acids & fatty acid) by mechanical breakdown & chemical digestion so that it is easily absorbed into the blood and utilized for energy.
Q.6 Solve any four of the following: (16 marks, 4 marks each)
State eight (8) functions of liver. (0.5 marks for each function)
Functions of liver
Secretion of bile: Bile salts are helpful in digestion and absorption of fats by its emulsification.
Glycogenic function: The hepatic cells by the action of enzymes convert glucose into glycogen and it is then stored in the
Formation of urea: Hepatic cells by the action of the enzyme cause deamination of amino acid, i.e. amine group is set free which forms
Metabolism of fat: Whenever energy is needed, the saturated stored fat is converted to a form in which it can be used to provide
Formation of RBCs in foetal
Destruction of RBCs forming bile pigments and
Formation of plasma
Formation of heparin, a natural anticoagulant in the
Storage of iron and vitamin B
Maintenance of body temperature: As a number of chemical reactions occur in the liver, heat is generated which is helpful in maintaining body
Excretion of toxic substances: The toxic substances entering the body through alimentary canal are destroyed in
Carbohydrate metabolism: It helps in maintaining plasma glucose level with the help of insulin &
Fat metabolism: Stored fat can be converted to a form in which it can be used by the tissue to provide
Protein metabolism: Deamination of amino -removes nitrogenous portion from amino acid not required for formation of new protein. Urea is formed from the nitrogenous portion which is excreted in urine. Break down of nucleic acids to form uric acid which is excreted in urine. Transamination: Removes the nitrogenous portion of amino acid & attaches it to carbohydrate molecule forming new non-essential amino acid. .
Synthesis of plasma protein & most blood clotting factors from amino
Breakdown of RBCs & defense against This is carried out by Kupffer cells.
Detoxification of drugs & noxious
Inactivation of hormones
Production of heat
Secretion of bile
Storage of glycogen, iron, copper, & water fat soluble vit-A, D,E, K, soluble vit. Like B12.
(b) What is hepatic portal circulation? Give its importance. (4marks; circulation 3 marks, importance 1 mark)
The portal circulation (3 marks)
In all parts of the body, the venous blood passes from the tissues to the heart by the direct route.
But, in the portal circulation, venous blood from the capillary bed of the abdominal parts, the spleen & the pancreas passes to the liver via the portal vein. The portal vein is formed by union of gastric vein from stomach, superior & inferior mesenteric veins from small and large intestine, splenic vein from spleen & cystic vein from gall bladder. The blood
passes through the secondary capillary bed, the hepatic sinusoid in the liver before entering the general circulation via the inferior vena cava.
Importance of portal circulation (1mark)
Blood with the high concentration of nutrients absorbed from the stomach & intestine goes to liver first. In the liver certain modifications takes place including the blood nutrient level. The venous blood then leaves liver via hepatic vein & joins the inferior vena cava.
(c) State functions of Semen and Placenta (4 marks, 2 marks each) Functions of Semen: (2 marks)
Increase motility and fertility of spermatozoa.
Semen is slightly alkaline, to neutralize the acidity of
Prostaglandin present causes contraction of
It contains nutrients to nourish and support the sperm during their journey through the female reproductive
Functions of placenta: (2 marks)
To provide the foetus with nourishment and removal of waste material from the
To act as the foetal lung by providing oxygenation of the fetal blood
The placenta also acts as a barrier in preventing certain micro-organisms of disease reaching the fetus thus protects the
The placenta helps the ovaries in the production of estrogen & progesterone hormones necessary for the continuation and maintenance of
(d)What is sensory and motor neuron? (1+1 marks). Draw a well labeled diagram of typical neuron (2 marks).
Sensory neuron (1 mark): They carry information from the body to the spinal cord. The impulses may then pass to the brain or to connector neurons of reflex arcs in the spinal cord.
Motor neuron (1 mark): They originate in the brain, spinal cord and autonomic ganglia. They transmit impulses to the effector organs; muscles and glands.
(e) Write the effect of sympathetic and parasympathetic stimulation on:(4 marks, 2marks each )
Pupils:(0.5 + 0.5 marks)
Sympathetic stimulation: Dilation of pupils causing mydriasis.
Parasymp. stimulation: Constriction of pupils causing miosis.
(ii) Bronchioles 🙁 0.5+0.5 marks)
Sympathetic stimulation: Bronchodilation allowing greater amount of air to enter the lungs at each inspiration.
Other blood vessels: Vasoconstriction. Parasympathetic stimulation: Coronary artery: Vasoconstriction Skeletal blood vessels: Vasoconstriction Other blood vessels: Vasodilation
(e) Explain the role of insulin and glucagon in the body. (4 marks, 2 marks each) Role of insulin (3 marks):
Role of insulin
It increases the uptake of glucose by the
Increases the conversion of glucose to glycogen in the liver & skeletal
It increases the uptake of amino acids by the
It promotes the synthesis of fatty acids & storage of fats in adipose tissue
Prevents breakdown of protein, fat & gluconeogenesis
Role of glucagon (1 mark): Its function is to increase blood sugar level. Whenever the blood sugar level falls below the normal the glycogen stored in the liver is broken down to glucose by the hormone glucagon.
Thus the two hormones help to maintain the blood sugar level constant.
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