Gy 0% By : @ WORK BOOK FOR PHARMACY TECHNICIANS 2nd Year 2019 Edition ACCORDING TO THE LATEST PAPER PATTERN 300 PLUS MCQS AND 150 PLUS SHORT QUESTIONS rece) AOTC CEPI CR Cate UOT Reviewed by: Rph Asif Mehmood (Pharm D, MPhil) Edited by :Yasir Hussain (Medical Coder)Index PHARMACOLOGY COMPUTER SOCIAL BEHAVIOUR, LAW AND ETHICS PHARMACEUTICS-II (Industrial and Quality Control) PHARMACEUTICS-III (hospital and Community Pharmacy) 01 50 55 67 92PREFACE & ACKNOWLEDGEMENT All praise to ALLAH (SWT), the most Benevolent, the Merciful. | am honoured to announce that we have prepared an easy, comprehensive, basic yet conceptual Work book for Pharmacy technicians (B Category) according to the syllabus Pattern provided by Punjab Pharmacy council. This book has been prepared with reference to renowned pharmacy books taught in pharm-D curriculum and related course material, so to provide students with conceptual context about the subject and its practical approach. ‘Keeping in view, the subject wise marks division, multiple choice and short questions are included in this book, covering the entire content of syllabus. Hope you will be amused to solve tricky mcqs and memorize important short questions. Thankful for my family members for their care and encouragement during preperation of book. | express my gratitude to my team members Rph. Asif Mehmood for his proofreading and review efforts and my student Yasir Hussain for his editing skills. To err is human, we prepared the book with full dedication and tireless efforts regarding time specifically. Hope you students will find it helpful in getting basic pharmacy subjects’ knowledge & clearing your exam with good score. Your feedback will be valuable. Good luck students! Rph. Saadia Arshad (Pharm D, MPhil (Pharmacy Practice) DEDICATION My humble efforts | dedicate to my beloved FATHER whose love, affection, efforts in upbringing & struggle in provision of education, ever appreciation & encouragement in every endeavour i made & ‘making capable to accomplish this noble task of writing.Pharmacology Topic 1: Introduction to Pharmacology Important Terminologies Pharmacology: can be defined as the study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes. Sub-divisions of Pharmacology i. Pharmacokinetics: branch of pharmacology which deals with the absorption, distribution, biotransformation and excretion of the drugs and its metabolites from the body or simply, the effects of the body on the drug. ii, Pharmacodynamics: branch of pharmacology which deals with the biochemical and physiological effect of the drug as well as its mechanism of action or simply, it studies the effects of a drug on the body. Pharmacokinetic processes govern the absorption, distribution, and elimination of drugs and are of great practical importance in the choice and administration of a drug for a patient, e.g., a patient with impaired renal function. Drug absorption: The transfer of a drug from its site of administration to blood stream. The drug may be absorbed from the GIT tract mainly either by 1- Passive diffusion 2- Active transport. Drug distribution: The drug leaves the bloodstream and enters the cells of tissues. It depends on; A) Blood flow B) Capillary permeability C) Binding of drugs to plasma- albumin D) Volume of distribution Drug metabolism: Elimination of drug and excreted into the urine or bile. Liver is the major site for drug metabolism. It occurs in two phases A) Phase 1: Oxidation -reduction-hydrolysis B) Phase 2: Conjugation reaction Drug excretion: Kidney is the most important organ for excreting drugs. Volume of distribution (Vd): also known as the apparent volume of distribution, is a hypothetical volume of fluid into which a drug is dispersed. It relates the amount of drug in the body to the concentration of drug (C) in blood or plasma. Its formula is Vd= D/ C Where C= the plasma concentration of the drug and D = the total amount of drug in the body. Half-life (t 1/2): is the time required to change the amount of drug in the body by one-half during elimination. The time course of drug in the body will depend on both the volume of distribution and the clearance. Formula ty2=0.7*V/CLjing the systemic circulation Bioavailability: is defined as the fraction of unchanged drug reaching the sy: following administration by any route. : in liver prior to reaching First-Pass Elimination: The rapid metabolism of an orally administered drug in liver pr the systemic circulation. drug binds and Receptor: Pharmacology defines receptor as any biologic molecule to which a drug produces a measurable response. Affinity: the tendency of drug to bind with a receptor. Efficacy or Intrinsic activity: is the ability of a drug to illicit a physiologic response when it interact with a receptor (effect produced by a drug) Potency of a drug is a measure of the amount of drug necessary to produce an effect of a given magnitude. Agonist: is defined as drug having affinity as well as efficacy. Full agonists: occupy receptors to cause maximal activation; intrinsic activity = 1. Partial agonists: can occupy receptors but cannot elicit a maximal response. Such drugs have have efficacies (intrinsic activities) less than 1 Antagonists: are drugs having affinity but lacking efficacy. Antagonists bind to the receptor but do Not initiate a response; that is, they block the action of an agonist or endogenous substance that works through the receptor. Therapeutic index: of a drug is the ratio of the dose that produces toxicity to the dose that produces a clinically desired or effective response in a population of individuals, TDso/EDso (ie., the ratio of the dose that produces a toxic effect in half of the population to the dose that produces the desired effect in half of the population) Bloequivalence: Two related drugs are bioequivalent if they show comparable bioavailability and similar times to achieve peak blood concentrations. Therapeutic equivalence: Two similar drugs are therapeutically e uivalent if they have comparable efficacy and safety. Tachyphylaxis: Rapid development of tolerance on repeated administ e.g. Ephedrine, amphetamine and nitroglycerine which produce tach administration. ration is called tachyphylaxis phylaxis on repeatedMegs 1, Which of the following is known as Father of pharmacology? a) Robert koch b) Oswald Schmiedeberh c) Louis Pasture d) Frederich Serturner 2. Pharmacokinetics is study of a) Therapeutic effects of drugs on body b) Absorption, distribution, metabolism and excretion of drugs c) Mechanisms of drug action d) New drug development methods 3. Pharmacodynamics involves the study of a) Absorption of drugs b) Elimination of drugs c) Mechanism of drug action on body d) Adverse drugs effects 4. Phase | reactions include reaction(s). a) Oxidation b) Reduction c) Hydrolysis d) All of these 5. If two drugs have comparable efficacy and safety, they are: a) Bioequivalent b) Agonists c) Therapeutic equivalents d) Antagonists 6. What kind of substances cannot permeate membranes by passive diffusion? a) Lipid-soluble b) Non-ionized substances c) Hydrophobic substances d) Hydrophilic substances 7. The time required to change the amount of drug in the body by one-half during elimination is a) Bioavailability b) Half-life c) Shelf life d) Efficacy 8. The main mechanism of most drugs absorption in Gl tract is: a) Active transport b) Filtration c) Endocytosis and exocytosis d) passive diffusion 9. An agonist that produce maximal effects and has high efficacy is called a) Partial agonist b) Antagonist c) Receptor d) Full agonist 10. Any factor that increases the volume of distribution can lead to a) Decrease in the half-life of drug b) Constant half life ¢) Increase in half-life of drug 4) No effect on half-life of drug 11. The bioavailability of a drug administered by intravenous route is a) 100% b)0% c)50% d) Unpredictable 12, The fraction of unchanged drug that reaches the systemic circulation is a) Drug- protein binding b) Bioavailability c) Affinity d) First pass effect 13. Major site for drug metabolism for majority of drugs is/are a) Small intestine b) Kidneys c) Liver d) Blood plasma14. Any biologic molecule to which a drug binds and produces a measurable response is called a) Hormone b) Neurotransmitter c) Receptor d) Agonist 15. The term active transport refers to? a) Transport of drugs along concentration gradient b) Transport without energy consumption c) Engulfment of drug by a cell membrane d) Energy dependent transport against concentration gradient 16. Protein bound drugs are pharmacologically a) Inactive b) Active c) Toxic d) Free 17. Removal of a drug from the body occurs via route a) Kidney b) Small intestine c) Bile d) Secretions as sweat and saliva e) all of these 18. The ability of a drug to exhibit a physiologic response when it interacts with a receptor, is called a) Affinity b) Potency c) Efficacy d) Volume of distribution 19. . If an agonist can produce submaximal effects and has moderate efficacy it’s called a) Partial agonist b) Antagonist c) Agonist-antagonist action d) Full agonist 20. An antagonist is a substance that has a) Affinity and Efficacy Both b) Affinity but no efficacy c) No affinity but efficacy d) No affinity and no efficacy Drug molecules usually binds to which of the following plasma protein? a) Globulin b) Heparin c) Haemoglobin d) Albumin . Conjugation reactions refer to 21. 2 8 a) Phase | reactions b) Phase Il reactions c) Drug distribution d) Phase | and Il reactions A ratio used to evaluate the safety and usefulness of a drug for indication is called a) Toxicity b) Adverse reaction c) Bioavailability d) Therapeutic index 24. Receptors are divided into, a) Five b)Seven c) Four d) Two 23. major families. Answer key 1) b 2) b 3) ¢ 4d 5) ¢ 6) d 7 b 8) d 9) d 10) b lija 12)b B)c 14) ¢ 15) d 16) a je 18) ¢ 19) a 20) b 21) d 22) b 23) d 24)Topic 2: Routes of Drugs Administration Common Routes of Drug Administration ‘Aural/ Otic Into the Ear Buccal Between the cheek and gum Sublingual Placed under the tongue Oral By mouth Gastric Through the stomach Inhalation In to the lungs Transdermal Drug delivered across the skin for systemic distribution Subcutaneous Between the dermis and muscle layer Intramuscular Injection deeply into muscle tissue Intravenous Injection directly into veins (most rapid) Intrathecal/intraventricular Injection directly into spine Intranasal Within the nose Ocular In to eye Rectal Into rectum, urethra and Vagina Megs s Routes of drug administration that avoid "first-pass" effect a) Sublingual b) Transdermal c) Inhalation d) Parenteral ¢) All of these Drug administered through the following route is most likely to be subjected to first-pass metabolism: a) Oral b) Sublingual c) Subcutaneous d) Rectal Which of the following is a disadvantage of using oral dosage form? a) First pass effect b) Low bioavailability c) Overdose overcome by antidotes a)aandb e)bandc Which of the following is an advantage of sublingual administration? a) Rapid absorption b) Convenient c) Avoid first pass-metabolism d) All the above Which of the following routes have the highest bioavailability? a) Oral b)IM c)IV d)SC e) Allofthese What phenomenon can occur in case of using a combination of drugs? a) Tolerance b) Tachyphylaxis c) Accumulation d) Synergism Placement of drug under the tongue refers to__ route. a) Transdermal b) Buccal c) Sublingual d) Subcutaneous Delivery of drug through skin patch is called a) Intramuscular b) Transdermal c) Subcutaneous d) IntrathecalAnswer key ie 2) a .: 4) 5) 6) d ne 8) b Short Questions & Answers Q1) Elaborate phase | and phase II reactions of drug biotransformation? Ans: For kidney to eliminate lipid-soluble drugs effectively, they must first be metabolized in the liver using two general sets of reactions, called Phase | and Phase Il reactions. Phase I: Phase | reactions function to convert lipophilic molecules into more polar molecules by introducing or unmasking a polar functional group, such as -OH or -NH2. Phase I metabolism may increase, decrease, or leave unaltered the drug's pharmacologic activity. Phase | reactions include oxidations, reductions, and hydrolysis reactions. Phase Il: This phase consists of conjugation reactions. If the metabolite from Phase | metabolism is sufficiently polar, it can be excreted by the kidneys. However, many Phase | metabolites are too lipophilic to be retained in the kidney tubules. A subsequent conjugation reaction with an endogenous substrate, such as glucuronic acid, sulfuric acid, acetic acid, or an amino acid, results in polar, usually more water-soluble compounds that are most often therapeutically inactive. The highly polar drug conjugates may then be excreted by the kidney or bile. Q2) Define term Receptor and classify its type? Ans: Receptors are specialized target macromolecules, present on the cell surface or intracellularly, with which drugs bind form complex and initiate events leading to alterations in biochemical and/or biophysical activity of a cell, and thus the function of an organ. Drugt receptor<———> drug- receptor complex — biologic effect Receptors may be divided into four families, namely: i, ligand gated ion channels (example: nicotinic receptor and (GABA) receptor) ii, G protein-coupled receptors (example: muscarinic receptors) enzyme-linked receptors and iv. _ intracellular receptors 3) Define the term first pass effect? Ans: After absorption from the stomach or small intestine, a drug must pass through the liver, wher® they undergo extensive metabolism, before reaching the general circulation and its target site. This process is called the first-pass effect. For example, isoproterenol and morphine. QA) State three merits and demerits of oral and parenteral drug administration? Ans: Advantages of oral route : Oral drug route is most convenient, economical, and common route of administration: Limit the number of systemic infections that could complicate treatment.*. Toxicities or overdose by the oral route may be overcome with antidotes such as activated charcoal. Demerits * First-pass metabolism by the intestine or liver limits the efficacy of many drugs when taken orally. * Gastric emptying time and passage of drug to the intestine may be influenced by gastric contents and intestinal motility. * Enteric coating is needed as stomach acid and inactivating enzymes may destroy certain drugs. * Cannot be used for unconscious and uncooperative patients. Advantages of parenteral route * Parenteral administration is used for drugs that are poorly absorbed from the Gl tract (for example heparin) and for agents that are unstable in the GI tract (for example, insulin. * It's most rapid means of introducing drugs in to the body and is particularly useful in the treatment of emergencies. * These routes have the highest bioavailability (IV=100%) and are not subject to first-pass metabolism or harsh Gl environments. Demerits © these routes are irreversible and may cause pain, irritation fear, and infections * greater risk of adverse drug effects (phlebitis and embolism) Q5) Briefly explain transport of a drug from the Gl tract after its absorption? /mechanisms of drug absorption across cell membrane? Ans: Passive diffusion: passage of drug molecule along the concentration gradient (from a region of high concentration to one of lower concentration). © Active transport: it’s the movement of drug molecule by specific carrier proteins, against concentration gradient (from a region of low drug concentration to one of higher drug concentration) that requires energy which is generated by enzyme ATP. * Endocytosis involves engulfment of a drug molecule by the cell membrane and transport into the cell by pinching off the drug-filled vesicle. For example, transport of Vit B12 across the gut wall. © Exocytosis: is responsible for secretion of substances from cells. For example, norepinephrine) are stored in membrane-bound vesicles in the nerve terminal and are released by exocytosis.Q6) Differentiate an agonist and antagonist drug? ‘Agonists “Antagonist ‘Are drugs having affinity as well as efficacy ‘Are drugs having affinity but lacking efficacy. Can bind to a receptor and elicit a biologic They decrease the actions of another drug or response, that mimics the response to the endogenous ligand. endogenous ligand. Example: phenylephrine is an agonist at a11- Example: Binding of atropine to muscarinic adrenoceptors, because it produces effects that | receptors resemble the action of the endogenous ligand, norepinephrine. Q7) Define the term competitive and non-competitive antagonism? ‘Ans: Antagonism may be competitive or non-competitive. Competitive antagonism: In this type of antagonism, the agonist and antagonist compete for the same receptors and the extent to which the antagonist opposes the pharmacological action of the agonist. This antagonism may be reversible, the effect can be overcome by increasing the concentration of the agonist at the receptor site. eg. acetylcholine and atropine antagonism at muscarinic receptors. Non-competitive antagonism: In this type of the antagonism an antagonist inactivates the receptor (R) so that the effective complex with the agonist cannot be formed, irrespective of the agonist concentration.eg: acetyl choline and decamethonium on neuromuscular junction Q8) Define the following terms: A) Pharmacokinetics B) pharmacodynamics C) Volume of distribution C) half-life E) Therapeutic index F) Affinity and efficacy G) Bioavailability Ans: All definitions are given in the introductory section of topic-1Topic 3: Posology Important Terminoloy Posology is the branch of medicine dealing with doses or it is the study of how medicines are dosed. Drug: a drug is a chemical substance which when administered to a living organism, produces a biological effect. a chemical substance used to treat, cure, prevent, Pharmaceutical drug, medication or medicine: or diagnose a disease or to promote well-being Placebo: a substance having no pharmacological effect but administered as a control in testing experimentally or clinically the efficacy of a biologically active preparation. Prodrug: an inactive precursor chemical that is converted to the active drug by biologic processes inside the body after administration. For example: « Loratadine, an antihistamine, is the prodrug of desloratadine * Levodopa is a prodrug converted into dopamine Dose: is the amount of drug or medicinal substance to be administered at one time. Dosage: is determination of the amount, frequency and number of doses for a patient. Therapeutic effect: desired drug effect to alleviate some condition or symptom of disease. Therapeutic dose: dose required to produce the optimal therapeutic effect. Side effect: Any unintended effect of a pharmaceutical product occurring at normal therapeutic doses and is related to its pharmacological properties. Adverse drug reactions: A response to a drug which is noxious and unintended, and which occurs at diagnosis, or therapy of disease or for the modification doses normally used in man for prophylaxis, of physiologic function.” Fatal dose: amount of dose that can cause death of 100% of experimental animals. ED: Dose of drug that produces 50% of its maximum response or effect. Can be a term used in vitro or in vivo (although it is more common in vivo). LDsp The dose of a chemical which produces death in 50% of a population of test animals to which it is administered. is a large dose needed initially when the therapeutic concentration of a drug in the Loading dose: idly (e.g., a life-threatening situation in which one cannot wait for 5 plasma must be achieved rap! half-lives for the drug to reach the desired steady-state level) OR A large first dose or first dose by injection to reach effective blood levels quickly. Maintenance dose rate is the dose of a drug required per unit time to maintain a desired steady- state level in the plasma to sustain a specific therapeutic effect.Note: Short question about any of the above-mentioned terminologies may be asked, Learn welll!! Mcqs 1. The dosage form of a drug administered under the skin is termed as a) Subcutaneous b) Transdermal c) Topical d) both subcutaneous and transdermal 2. Drug dose is calculated using Young’s rule for child age a)3 months b) 18 years c) 2-17 years d) 1 year 3, The therapeutic index of a drug is a measure of its a) Dose variability b) Potency c) Efficacy d) Safety 4, Undesirable effects of a drug that occurs at therapeutic doses a) Side effect b) Toxic effect c) Allergic reaction d) Idiosyncrasy 5. Which of the following formula refer to paediatric dase calculation based on welght? a) Young's rule b) Smith’s rule c) Cowling’s ruled) Clark’s rule 6. When infant age is in months, dose is calculated by a) Friend’s rule b) Smith’s rule Clark's rule d) Young’s rule Answer key 1) a 2) ¢ 3) d 4) a ye, ox | Short Questions & Answers Q1) What factors should be taken into consideration while suggesting dose of drug to patient? Ans: The following are some of the factors that influence the dose of a drug. Patients age Sex Body weight Route of administration Dosage form Pathological state Drug interactions Q2) State formulas used for paediatric dose calculations? Ans: Following formulas are used to calculate paeds dose; Clark’s rule: Infant dose= infant weight in pounds xadult dose 150 Fried’s rule: Infant dose= age in months x adult dose 150 Young's rule: child dose = age in years x adult dose age in years+12 10o Ry xX o 4:6 v ic 4: General Introduction to The Drugs Action on Various Systems e nomi ‘Sj A) Autonomic Nervous System and drugs action on ANS Introduction & Terminologies fn : cele 72) nervous system (PN) the connection between the central nervous system and the rest of the body. The PNS can be divided into the autonomic nervous system, which controls bodily functions without conscious control, and the sensory-somatic nervous system, which transmits sensory information from the skin, muscles, and sensory organs to the CNS and sends motor commands from the CNS to the muscles, There are two divisions of the ANS ‘The sympathetic nervous system The parasympathetic nervous system Preganglionic neurons ~ originate in the brain or spinal cord. ic neurons — originate in the ganglion located outside the CNS n: The preganglionic fibers of the sympathetic nervous system produce acetylcholine while most of the postganglionic fibers produce norepinephrine (noradrenalin) and are called adrenergic fibers. Parasympathetic division: All pre and postganglionic fibers product acetylcholine neurotransmitter and are cholinergic. > Acetylcholine is released at preganglionic fibers of both the sympathetic and parasympatheti nervous system. For most groups, one or more prototype drugs can be identified that typify the most important characteristics of the group. Sympathomimetics: refers to the action of an adrenergic drug or an action that increases sympathetic activity. Or drugs that mimic actions of norepinephrine or epinephrine. ‘Sympatholytic: refers to the action of an adrenergic blocking drug or an action that decreases sympathetic activity. Parasympathomimetics: drugs which mimic the effects of acetylcholine by binding directly to cholinergic receptors. Parasympatholytics: drugs which bind with the cholinergic receptors and block the action of the Ach or Ach like drugs. They are also called anticholinergics. 11ANS effects on various body organs Organs ‘Sympathetic response a — Eyes Dilation of pupil (a1) Constriction/ot puny Heart Increase heart rate (B1, B2) Decrease heart rate Increase contractility (B1, B2) Decrease contractility Increase conduction velocity Decrease conduction velocity Arterioles Vasoconstriction (a) Vasodilatation Lungs Bronchodilatation (B2) Bronchoconstriction Gut Decrease peristalsis and tone Increase peristalsis and tone Contraction of sphincter (a) Relaxation of sphincter Bladder Sphincter contraction (a) Sphincter relaxation Uterus Salivary glands Thick, viscous secretion (a1) Profuse, watery secretion Classification of ANS drugs Cholinergic agonists Direct acting Indirect acting Indirect acting Reactivation of acetyl (reversible) (irreversible) cholinesterase acetylcholine edrophonium ecothiophate pralidoxime carbachol neostigmine pilocarpine physostigmine Cholinergic antagonists Antimuscarinic agents Ganglionic blockers Neuromuscular blockers atropine(prototype) ‘Mecamylamine rocuronium Ipratropium Nicotine Succinylcholine ‘scopolamine tubocurarine ‘Adrenergic Agonists Direct acting Indirect acting Mixed acting Clonidine amphetamine ephedrine dopamine cocaine pseudoephedrine epinephrine (prototype) norepinephrine Adrenergic blockers a-blockers 6-blockers Drugs affecting neurotransmitter uptake or release Alfuzosin Acebutolol Atenolol Reserpine Doxazocin Carvedilol Labetalol Prazosin Metoprolol Propranolol 12Meqs 10. 11. 12. 8 13. & 1 1 a = Nerves that transmit their impulses by releasing acetylcholine are known as nerves. i a) eeeneee b) Cholinergic. c) sympathetic d) Dopaminergic Atropine produces the following actions except: ade E a) Bradycardia_b) Mydriasis c) Dryness of mouth d) Miosis — beth Pe Acetylcholine has re a) Adrenergic actions b) Muscarinic and nicotinic actions c) aand b both. d) Parasympatholytic actions Which of the following is drug of choice in the emergency treatment of glaucoma? a) Pilocarpine b) Acetazolamide c) Acetylcholine d) Physostigmine Which of the following enzyme cleaves acetylcholine into acetyl and choline? a) Renin b) Aldosterone c) Acetylcholinesterase d) Norepinephrine Which of the following drug is used for treatment of anaphylactic shock? a) Ephedrine b) Acetylcholine c) Morphine d) Epinephrine Acetylcholine is instilled into the eye to produce miosis during ophthalmic surgery as a) 2% solution b) 0.5% solution c) 1% solution d) 0.9% solution Actions of epinephrine include a) Increase heart rate b) Bronchodilator c) Vasoconstriction d) All of these Pilocarpine is a) Indirect muscarinic agonist b) az-agonist c) Br-antagonist a d) Direct-acting muscarinic agonist Which of the following is a short-acting acetylcholinesterase inhibitor? a) Physostigmine b) Adrenaline c) Edrophonium d) Atropine Indicate an antimuscarinic drug used in the treatment of mushroom poisoning a) Epinephrine b) Physostigmine c)Atropine d) Dopamine Which one of the following is a non-selective & blocker? a) Esmolol b) Atenolol c}Propranolol d) Metoprolol Which of the following acetylcholinesterase Innes irreversible? a) Physostigmine b) Pralidoxime c) Pilocarpine d) Ecothiophate “Fight or flight” response is exhibited by a) parasympathetic NS b)SomaticNS c)SympatheticNS d)aandc Preganglionic fibers of both the sympathetic and parasympathetic nervous system release a) Adrenaline b) Dopamine ¢)Acetylcholine d) Norepinephrine 1316. “Sandy eyes” is the adverse effect of i a) Norepinephrine b) Atropine c) Propranolol d) Nicotine 1 Sg . Which of the following drugs is used in treating motion sickness? a) Epinephrine bJScopolamine c) Ipratropium d) Pilocarpine 18. The primary neurotransmitters in the autonomic nervous system are a) Acetylcholine and serotonin b) Adrenaline and histamine c/acetylcholine and norepinephrine 19. Catecholamines include following except a) Epinephrine b) Dopamine c) Norepinephrine d) All of these 20. All are alpha - adrenergic agonists except: a) Scopolamine b) Dopamine c) Dobutamine d) Phenylephrine 21. Which of following drug is au agonist? a) Atropine b) Clonidine c) Epinephrine d) Ephedrine 22. Which of the following drug is used to treat hypertension? AfPrazosin b) Ephedrine c) Dopamine d) Physostigmine 2 B . All the following are Bz antagonists except a) Isoproterenol b) Metoprolol c) Labetalol d) Atenolol. 24. Indicate acetylcholinesterase reactivator a) Pralidoxime b) Edrophonium c) Pilocarpine d) Propranolol 25. Adrenergic receptors include a) a-receptors b) Muscarinic receptors c) B- receptors d) Aand C Answer key 1) b 2) d 3) b 4) a 5) ¢ 6) d ame 8) d 9) d 10) li)ec 12) ¢ 13) d A 14) ¢ 15)c 16) b 17) b 18) c 19) d 20) a 21) b 22)a 23)a 24) a 25) d Short questions & Answers Q1) State therapeutic uses and adverse effects of atropine? Ans: Therapeutic uses: * Ophthalmic: In the eye, topical atropine exerts both mydriatic and cycloplegic effects. + Antidote: for cholinergic agonists: Atropine is used for the treatment of overdoses of cholinesterase inhibitor insecticides and some types of mushroom poisoning. + Antisecretory: The drug is sometimes used as an antisecretory agent to block secretions in the upper and lower respiratory tracts prior to surgery. 14e effects: i adverse effects: Depending on the dose, atropine may cause dry mouth, blurred vision, sandy eves, dia, and constipati tachycardia, and constipation. CNS effects include restlessness, confusion, hallucinations, and delirium, which may progress to depression h collapse of the circulatory and respiratory systems, and death. Q2) Write a short note on propranolol? ‘Ans: Propranolol is the prototype B-adrenergic antagonist and blocks both B1 and B2 receptors. Pharmacological action: a) Cardiovascular: Propranolol diminishes cardiac output, having both negative inotropic and chronotropic effects. It directly depresses sinoatrial and atrioventricular activity. b) Peripheral vasoconstriction: Blockade of B receptors prevents B2-mediated vasodilation. The reduction in cardiac output leads to decreased blood pressure. There is a gradual reduction of both systolic and diastolic blood pressures in hypertensive patients. ¢) Bronchaconstriction: Blocking B2 receptors in the lungs of susceptible patients causes contraction of the bronchiolar smooth muscle. d) Increased Na+ retention: Reduced blood pressure causes a decrease in renal perfusion, resulting in an increase in Na+ retention and plasma volume. e) Disturbances in glucose metabolism: B-blockade leads to decreased glycogenolysis and decreased glucagon secretion. Therefore, if a Type | diabetic is to be given propranolol, very careful monitoring of blood glucose is essential. Therapeutic effects + Hypertension + Glaucoma: + Migraine: (prophylactically) + Hyperthyroidism + Angina pectoris + Myocardial infarction Adverse effects: Bronchoconstriction, arrhythmias, sexual impairment, disturbances in metabolism. Q3) Enlist therapeutic applications and adverse effects of epinephrine? Ans: Therapeutic applications + Bronchospasm: In treatment of acute asthma and anaphylactic shock, epinephrine is the drug of choice. ; : * Glaucoma: In ophthalmology, 2%t epinephrine solution may be used topically to reduce intraocular pressure in open-angle glaucoma. + Anaphylactic shock: Epinephrine is the drug of choice for the treatment of Type | hypersensitivity reactions in response to allergens, + Cardiac arrest: Epinephrine may be used to restore cardiac rhythm in patients with cardiac arrest regardless of the cause. tS+ Anaesthetics: Local anaesthetic solutions usually contain 1:100,000 parts epinephrine. The effect of the drug is to greatly increase the duration of the local anaesthesia. Adverse effects: + CNS disturbances: anxiety, fear, tension, headache, and tremor. + Hemorrhage: The drug may induce cerebral hemorrhage as a result of a marked elevation of blood pressure. + Cardiac arrhythmias: particularly if the patient is receiving digitalis. + Pulmonary edema Q4) Write a brief note on pharmacology of acetylcholine? Ans: Acetylcholine (ACh) is the neurotransmitter of parasympathetic and somatic nerves as well as autonomic ganglia. Acetylcholine has both muscarinic and nicotinic receptor activity. Pharmacological actions: * Decrease in heart rate and cardiac output * Decrease in blood pressure * In GIT, it increases tone and peristalsis, relaxes sphincters, hence propulsion and evacuation of Gl contents * Increases secretion of all glands viz. lacrimal, salivary, tracheobronchial, nasopharyngeal, gastric, intestinal and sweat. * in the urinary system, ACh stimulates cholinergic receptors to promote urination. + Inthe eye, ACh cause marked constriction of the pupil (miosis) Therapeutic use: Acetylcholine (1% solution) is instilled into the anterior chamber of the eye to produce miosis during ophthalmic surgery. Adverse effects: sweating, salivation, flushing, decreased blood pressure, nausea, abdominal pain, diarrhea, and bronchospasm. Q5) Write a short note on mixed acting adrenergic drugs? ‘Ans: Ephedrine and pseudoephedrine are plant alkaloids. These drugs are mixed-action adrenergic agents. They not only release stored norepinephrine from nerve endings but also directly stimulate both a and B receptors. Ephedrine has been used to treat asthma, as a nasal decongestant and to raise blood pressure. Pseudoephedrine is primarily used to treat nasal and sinus congestion or congestion of the eustachian tubes. Q6) Write a short note on neuromuscular blocking drugs? Ans: These drugs block cholinergic transmission between motor nerve endings and the nicotinic receptors on the neuromuscular end plate of skeletal muscle. These neuromuscular blockers are structural analogs of acetylcholine, and they are divided into a) Nondepolarizing neuromuscular blocking drugs interact with the nicotinic receptors to prevent the binding of acetylcholine. These drugs thus prevent depolarization of the muscle cell membrane and inhibit muscular contraction. Because these agents compete with acetylcholine at the receptor 16without stimulating the receptor, they are called competitive blockers. These include tubocurarine, pancuronium, atracurium. b) Depolarizing neuromuscular blocking drugs attaches to the nicotinic receptor and act like acetylcholine. This drug remains attached to the receptor for longer time and providing a constant stimulation of the receptor. These include succinylcholine and decamethonium. ‘Therapeutic use; Neuromuscular blockers are clinically useful during surgery for producing complete muscle relaxation, without having to employ higher anaesthetic doses to achieve comparable muscular relaxation. Q7) Write a note on pharmacology of reversible acetylcholine inhibitors? Ans: Acetylcholinesterase is an enzyme that specifically cleaves acetylcholine to acetate and choline and, thus, terminates its actions. Acetylcholinesterase Inhibitors may be reversible agents such as physostigmine, neostigmine, edrophonium, these drugs inhibit AChE and increase ACh levels at both muscarinic and nicotinic receptors to mimic the physiologic effects of ACh and stimulation of parasympathetic division of the ANS. * Therapeutic uses: physostigmine is used to treat glaucoma. «treatment of overdoses of drugs with anticholinergic actions, such as atropine, phenothiazines, and tricyclic antidepressants. ¢ Neostigmine has found use in symptomatic treatment of myasthenia gravis Q8) Write a short note on ecothiophate? ‘Ans: Ecothiophate is an irreversible anticholinesterases inhibitor, it covalently binds via its phosphate group to the serine-OH group at the active site of acetylcholinesterase. Once this occurs, the enzyme is permanently inactivated, and restoration of acetylcholinesterase activity requires the synthesis of new enzyme molecules. Following covalent modification of acetyicholinesterase, the phosphorylated enzyme slowly releases one of its ethyl groups. The loss of an alkyl group, which i called aging. If given before aging ofthe alkylated enzyme, pralidoxime can reverse the effects of ecothiophate, except for those in the CNS. Q9) State therapeutic applications of dopamine? ‘Ans: Dopamine is the drug of choice for shock and is given by continuous infusion. It raises the blood pressure by stimulating the Bi receptors on the heart to increase cardiac output, and a. receptors on blood vessels to increase total peripheral resistance. In addition, it increased blood flow to the kidney, enhances the glomerular filtration rate and causes sodium excretion. 10) Explain briefly about pharmacology of a-blockers? ‘Ans: All ovadrenergic blockers reverse the actions of epinephrine such as (prevents vasoconstriction of peripheral blood vessels, decrease in systemic blood pressure) Therapeutic uses: « prazosin terazosin doxazosin are useful in the treatment of hypertension, * Tamsulosin and alfuzosin are indicated for the treatment of benign prostatic hyperplasia (BPH). 17Phenoxybenzamine is used in chronic management of pheochromocytoma ( of adrenal medulla) Adverse effects: a Blockers may cause dizziness, a lack of energy, nasal congestion, headache, drowsiness, and orthostatic hypotension. B) Drugs acting on Central Nervous System NEURODEGENERATIVE DISEASES Neurodegenerative diseases of the CNS include > a) b) Alzheimer's disease, Parkinson's disease and Huntington's disease Alzheimer's disease is characterized by the loss of cholinergic neurons resulting in dementia (memory loss) and, behavioural issues. Parkinsonism is a progressive neurological disorder of muscle movement, characterized by tremors, muscular rigidity, bradykinesia (slowness in initiating and carrying out voluntary movements), and postural and gait abnormalities. It is characterized by, loss of dopaminergic neurons in the substantia nigra (part of midbrain). Antiparkinson drugs Anti-Alzheimer drugs Carbidopa donepezil Levodopa memantine Others: Amantadine Selegiline, Rasagilene tivastigmine Mcqs 1. Alzheimer's disease is characterized by the loss of. neurons a) Dopaminergic neurons b) Adrenergic c) Cholinergic d) Muscarinic Which of following drug is a metabolic precursor of dopamine? a) Nicotine b)Levodopa c) Lorazepam d) Carbidopa ‘Administration of levodopa and monoamine oxidase (MAO) inhibitors together results in a) Hypertensive crisis b) Depression c) Gl upset d) Sedation Which of following is a specific adverse effect of Levodopa? a) Vomiting b) Dyskinesias c) Anorexia d) Heart failure Which of following drug is used to treat Alzheimer’s disease? a) Levodopa b)Haloperidol c) Memantine d) Phenytoin Dementia means a) Loss of blood b) Loss of memory c) Excitement d) Tremors Answer key 1) c 2) b 3) a 4) b 5) ¢ caneShort Question & Answers ~~ Q1) Write down mechanism of action of Levodopa? ‘Ans: As parkinsonism results from insufficient dopamine in specific regions of the brain. Levodopa, (precursor of dopamine) is actively transported into the CNS and is converted to doparnine in the brain, thus, replenish the dopamine defi iency. Large doses of levodopa are required, because much of the drug is decarboxylated to dopamine in the periphery, resulting in side effects so, levodopa is co-administered with carbidopa as it diminishes the metabolism of levodopa in the GIT and thus, increases the availability of levodopa to the CNS, > Sedative (anxiolytic) agent should reduce anxiety and exert a calming effect. Sedation is characterized by decreased anxiety, motor activity, and cognitive acuity. » Hypnotic drug should produce drowsiness and encourage the onset and maintenance of @ state of sleep. % Allsedative become hypnotics at large dose ‘Anxiolytic and Hypnotic drugs classification benzodiazepines | Benzodiazepine | Other anxiolytic | barbiturates Other hypnotic antagonist agents agents. Drugs included as | Flumazenil buspirone Drugs included as | Antihistamine classified below antidepressants _| classified below | Chloral hydrate Ethanol Benzodiazepines menemonics — short acting (1/2life: 3-8hrs) TO (Oxzaepam, Triazolam) — Intermediate acting (1/2life: 10-20hr) ALET (alprazolam, lorazepam, estazolam, temazepam) : 1-3days) (chlordiazepoxide/clonazepam, diazepam and flurazepam) — Long acting (1/21 Barbiturates mnemonics STAPP ( Secobarbital, thiopental, amobarbital, pentobarbital and phenobarbital) (CNS STIMULANTS: PSYCHOMOTOR STIMULANTS HALLUCINOGENS ‘Amphetamine Lysergic acid diethylamide (LSD) Caffeine Phencyclidine (PCP) Cocaine Nicotine Theophylline Antidepressants f t + y + SSRI (selective “SNRI (Serotonin- Atypical AD TCA’s (Tricyclic Monoaminwondase serotonin reuptake | Norepinephrine : Antidepressants) (MAO) Inhibiters Inhibitors) Reuptake inhibitor) | bupropion Utecel es imipramine (the Phenelzine Fluoxetine Duloxetine prototype drug), | setegine Escitalopram amitriptyline Citalopram 19Neuroleptics drugs Or Antipsychotic drugs Typical neuroleptic (low typical neuroleptic (high Atypical neuroleptic - potency) potency) Chlorpromazine haloperidol clozapine Prochlorperazine risperidone Antiepileptic drugs Barbiturates Benzodiazepines | GABA Analogues | Phenytoin Phenobarbital | Diazepam Gabapentin lorazepam Mcqs 1. Depending on the nature of the action, neurotransmitters in brain can be a) Excitatory b) Inhibitory c) Inflammatory d) Both a or b 2. Dopamine is a neurotransmitter a) Excitatory b) Inhibitory c) Inflammatory d) Botha orb 3. Hypnotic drugs are used to treat: a) psychosis b) Sleep disorders c) Hypertension d) Parkinson disorder 4, The benzodiazepines action depends on their interaction with which of the following receptors? a) GABA b) Serotonin c) Cholinergic d) dopamine 5. Which of following is therapeutic application of benzodiazepines? a) Anxiolytic b) Anticonvulsant c) Muscle relaxant. d) All of these 6. Indicate the specific antidote for benzodiazepines a) Flumazenil b) Buspirone c) Morphine d) Diazepam 7. Which of the following is a long acting benzodiazepine? a) Lorazepam b) Buspirone c) Diazepam d) Nicotine 8. Which of the following drug is ultra-short acting barbiturate? a) Phenobarbital b) Thiopental c) Pentobarbital d) Alprazolam 9. Which of the following drug acts as anti-depressant? a) Fluoxetine B)Carbidopa c) Cocaine d) Ethanol 10. Prototype tricyclic antidepressant is a) Duloxetine b) Epinephrine c) Imipramine d) Lorazepam 11. Which of the following drug belongs to monoamine oxidase inhibitors? 2 a) Ephedrine b) Diazepam c)Phenelzine d) Levodopa 2042. Phenytoin is a(n) a) Antidepressant b) Sedative ¢) Anxiolytic d) Antiepileptic Answer key Fae 2) d 3) b aa sa | 6a 7) 8) b 9) a 10) ¢ ajc | _1a)d short Questions & Answers Q1) Classify benzodiazepines and barbiturates? Ans: Both classes of drugs are classified according to their duration of action, for benzodiazepines refer introductory section of this chapter. Barbiturates are classified as: long acting (1-2 days) eg: phenobarbital «short acting (3-8 hours) eg: pentobarbital, secobarbital, amobarbital * ultra-short acting (20 minutes) eg: thiopental Q2) Write pharmacological actions of benzodiazepines? Ans: Reduction of anxiety: At low doses, the benzodiazepines are anxiolytic. ‘Sedative and hypnotic actions: All the benzodiazepines used to treat anxiety have some sedative properties, and some can produce hypnosis at higher doses. * Anterograde amnesia: temporary impairment of memory. «Anticonvulsant: Several of the benzodiazepines have anticonvulsant activity and some are used to treat epilepsy and seizure disorders. © Muscle relaxant: At high doses, the benzodiazepines relax the spasticity of skeletal muscles. Q3) Enlist therapeutic applications of barbiturates? © Anesthesia: Ultrashort-acting barbiturate, thiopental is used intravenously to induce anesthesia. * Anticonvulsant: Phenobarbital is used in long-term management of tonic-clonic seizures, status epilepticus, and eclampsia. «Anxiety: Barbiturates have been used as mild sedatives to relieve anxiety, nervous tension, and insomnia. 4) State briefly about mechanism of action of benzodiazepines? ine actions ave the y-aminobutyric acid (GABA) receptors. GABA is major inhibitory neurotra' the CNS. Binding of GABA to its receptor triggers an opening of a chlorite channel, which leads to an increase in chloride conductance thus, inhibits the formation of es generalized CNS depression leading to anxiolytic, sedative/hypnotic, of benzodiazepines. Ans: The targets for benzodiazepi nsmitter i action potentials. This caus and muscle relaxant effects 21Q5) Write a short note on pharmacology of SSRI’s? Ans: The selective serotonin reuptake inhibitors (SSRIs) are a group of antidepressant drugs that block the reuptake of serotonin, leading to increased concentrations of the neurotransmitter in the synaptic cleft leading to greater postsynaptic neuronal activity. Antidepressants typically take at least 2 weeks to produce significant improvement in mood, and maximum benefit may require up to 12 weeks or more. Therapeutic uses: depression, obsessive-compulsive disorder, panic disorder generalized anxiety disorder, posttraumatic stress disorder, social anxiety disorder. Adverse effects: headache, sweating, anxiety and agitation, gastrointestinal effects (nausea, vomiting, diarrhea), weakness and fatigue, sexual dysfunction, changes in weight, sleep disturbances {insomnia and somnolence) Q6) Write a short note on Nicotine? Ans: Nicotine is a constituent of tobacco, along with various gases (e.g., CO, hydrogen cyanide) and particulate matter. Mechanism of action: Nicotine mimics the action of Acetylcholine at cholinergic nicotinic receptors of ganglia in skeletal muscle, and in the CNS. In low doses, nicotine causes ganglionic stimulation while at high doses, nicotine causes ganglionic blockade. Adverse effects: The CNS effects of nicotine include irritability and tremors. Nicotine may also cause intestinal cramps, diarrhea, and increased heart rate and blood pressure. Physical dependence on nicotine develops rapidly and can be severe. The transdermal patch and chewing gum containing nicotine have been shown to reduce nicotine withdrawal symptoms and to help smokers stop smoking. Q7) Write short note on phenytoin? ‘Ans: Mechanism of action: Phenytoin blocks voltage-gated sodium channels by selectively binding to the channel in the inactive state and slowing its rate of recovery. At very high concentrations, phenytoin can block voltage-dependent calcium channels Therapeutic use: Phenytoin is effective for treatment of partial seizures, generalized tonic-clonic seizures and in the treatment of status epilepticus. Adverse Effects: Hirsutism & coarsening of facial features, acne, gingival hyperplasia. Q8) Write a note on pharmacology of MAO inhibitors? Ans: Three MAO inhibitors include drugs such as, phenelzine, lsocarboxazid and selegiline. These drugs are well absorbed after oral administration, but antidepressant effects require at least 2 to4 weeks of treatment. Mechanism of action of MAO!’s: MAO is a mitochondrial enzyme found in nerve and other tissues. Monoamine oxidase breaks down norepinephrine, serotonin, and dopamine. The MAO inhibitors non selectively and irreversibly inhibit both MAO-A and MAO-B, increasing the concentration of all three neurotransmitters in the brain, leading to antidepressant action of these drugs. 2Therapeutic Uses: Indicated for depressed patients who are unresponsive or allergic to TCAS. + Patient with low psychomotor activity. «Treatment of phobic states Adverse effects: include Postural hypotension, headache, dry mouth, sexual dysfunction (phenelzine), weight gain, and sleep disturbance. Drug-food interaction: The consumption of tyramine-containing foods (cheese, beer, sausage, etc.) while on MAOIs can result in drastic increases in blood pressure, leading to stroke or myocardial infarction, So should be avoided, ) Drugs acting on Gastrointestinal Tract (GIT) i) Drugs used to treat peptic ulcers Causative factors for peptic ulcers: Nonsteroidal anti-inflammatory drug (NSAID) Infection with gram-negative Helicobacter pylori * Increased hydrochloric acid secretion, and inadequate mucosal defence against gastric acid. > For eradication of H. pylori, either triple therapy consisting of a PPI with either metronidazole or amoxicillin plus clarithromycin, or quadruple therapy of bismuth subsalicylate and metronidazole plus tetracycline plus a PPI, are administered for a 2-week course. This usually results in a 90 percent or greater eradication rate. > Antacids are weak bases that react with gastric hydrochloric acid to form a salt and water. Their principal mechanism of action is reduction of intragastric acidity. Clinical use: Aluminium and magnesium containing antacids are used for symptomatic relief of peptic ulcer disease and GERD, they may also promote healing of duodenal ulcers. ‘ADR's: Aluminium hydroxide tends to be constipating, and magnesium hydroxide tends to produce diarrhea. Preparations that combine these agents aid in normalizing bowel function. le. It binds to positively > sucralfate is a polysaccharide complexed with aluminium hydro charged groups in proteins of both normal and necrotic mucosa, so, creates a physical barrier that impairs diffusion of HCl and prevents degradation of mucus by pepsin and acid.it protects ulcerated areas from further damage and promotes healing. Sucratfate also stimulates mucosal production of prostaglandins and inhibits pepsin. Therapeutically use, for treatment of duodenal ulcers and as long-term maintenance therapy to prevent their recurrence. ADR's include, constipation. constipation and nausea. chemotherapy-induced emesis, and diarrhea and =Classification of drugs used for treatment of Peptic ulcer Antimicrobial | H2- Proton pump | Prostaglandins | Anti- ‘Antacids | Mucosal agents receptor —_| inhibitors (PPI) muscarinic protective blockers agents drugs. Amoxicillin | Cimetidine | Esomeprazole | Misoprostol | Dicyclomine | Aluminium Bismuth Prototype hydroxide _|__subsalicylate Bismuth Famotidine | Lansoprazole Magnesium compounds hydroxide Sucralfate Clarithromycin tidine | Omeprazole Calcium carbonate Metronidazole Pantoprazole pod bicarbonate Tetracycline Rabeprazole Mcqs 1 7. 10. Gastric acid secretion by parietal cells of the gastric mucosa is stimulated by a) Acetylcholine _b) Acetylcholine and gastrin c)Histamine __d) Acetylcholine, histamine and gastrin Which of following pathogen is responsible for peptic ulcer? a) E.coli b) Salmonella typhi c) Helicobacter pylori d) Yeast coated? Which of the following drug is manufactured as ente a) Proton pump inhibitors b) Antibiotic c) H2-receptor blockers d) Antacids Which of the following drug is prescribed prophylactically to prevent risk of NSAID-induced ulcer? a) Omeprazole b) Misoprostol c) Amoxicillin d) Aluminium hydroxide 1e belongs to, class of drugs. Cimeti a) Proton pump inhibitors b) Antibiotic c) H2-receptor blockers d) Antacids are weak bases that react with gastric acid to form water and a salt a) Prostaglandins b) PPls c) H2-receptor antagonists d) Antacids The most common side effect associated with aluminum containing antacids is a) Constipation b) Vomiting c) Diarrhea d) Hypertension Which of following drug produces uterine contractions and is contraindicated during pregnancy? a) Aluminium hydroxide b) Omeprazole c) Misoprostol d) Cimetidine Which of following is a cytoprotective compound? a) Aluminium hydroxide b) Sucralfate c) Omeprazole d) Famotidine Zantac is brand name of A) Ranitidine B) Omeprazole C) Adrenaline D) Amoxicillin 24‘Answer key aa ac 3d ab 5) 2) a a) ¢ 9) b 10) Short Questions & Answers Q1) Explain mode of action of Ho-receptor antagonists in treatment of peptic ulcer? be The H2-receptor antagonists such as cimetidine, ranitidine act as competitive inhibitors of the if ieee H2-receptors on the parietal cel. This results in a marked decrease in histamine stimulated basal and meat-stimulated gastric acid secretion and are used in the treatment of ulcers and heartburn, 2) Enlist therapeutic uses of H,-receptor antagonists? * H2-receptor antagonists are used to treat peptic ulcer disease to promote the healing of gastric and duodenal ulcers. * Treat GERD and Zollinger-Ellison syndrome. * Provide rapid relief from dyspepsia. ¢ 7 administered lV lence of stress-related ulcers. tensive care settings to reduce the Q3) What are adverse effects of H2-antagonists? Ans: Diarrhea, headache, fatigue, myalgias, and constipation, mental confusion. Q4) Briefly explain mechanism of action of Proton Pump inhibitors? Ans: Proton pump inhibitors are irreversible inhibitors of the H+/K+ATPase proton pump in parietal cells, Thereby suppressing secretion of hydrogen ions into the gastric lumen. The proton pump is the final step in the secretion of gastric acid. These agents reduce both meal-stimulated and basal acid secretion. Q5) Enlist therapeutic uses of proton pump inhibitors? + pPI’S are superior over the H2 antagonists for suppressing acid production and healing peptic ulcers for treating erosive esophagitis, active duodenal ulcer and Zollinger-Ellison syndrome. igs for treatment of all forms of GERD. * most effective dru * to reduce Helicobacter pylori-associated ulcers and NSAID therapy induced gastric ulcers Q6) Classify drugs used in treatment of peptic ulcer? ‘Ans: For answer, refer to the topic 4(Part C) introductory notes. aaii) Antidiarrheals > Increased motility of the gastrointestinal tract and decreased absorption of fluid ee factors in diarrhea. Antidiarrheal drugs include antimotility agents, adsorbents, and drugs that modify fluid and electrolyte transport. ' ' > Adsorbents, act by adsorbing intestinal toxins or microorganisms and/or by coating or protecting the intestinal mucosa. (kaolin and pectin). : ne > Bismuth subsalicylate is effective for both treatment and prophylaxis of traveller's diarrhea and other forms of diarrhea. ; a > Loperamide is an opioid agonist, activate opioid receptors in the enteric nervous system to inhibit acetylcholine release and decrease peristalsis. Side effects include drowsiness, abdominal cramps, and dizziness. jarrheals Adsorbents Antimotility agents Aluminium hydroxide Diphenoxylate Bismuth Subsalicylate Loperamide iii) Laxatives Bulk-forming laxatives are indigestible, hydrophilic colloids that absorb water, forming a bulky, emollient gel that distends the colon and promotes peristalsis. These agents are the treatment of choice for chronic constipation. Osmotic laxatives are nonabsorbable salts (anions and cations) that hold water in the intestine by osmosis and distend the bowel, increasing intestinal activity and producing defecation in a few hours. They are used for the treatment of acute constipation or the prevention of chronic constipation. Stool softeners or surface-active agents, become emulsified with the stool, produce softer feces and ease passage. Mineral oil and glycerine suppositories are lubricants, These agents lubricate fecal material, retarding water absorption from the stool. Mineral oil should be taken orally in an upright position to avoid its aspiration and potential for lipid pneumonia. Irritant (stimulant) laxatives such as aloe, bisacodyl, senna and castor oil. These agents stimulate smooth muscle contractions resulting from their irritant action on the bowel mucosa, drugs used to relieve constipation (Laxatives) Bulk laxatives Saline and osmotic Stool softeners Lubricant laxative’ laxatives (surfactants or emollients) Methylcellulose magnesium citrate docusate sodium mineral oil psyilium seeds magnesium sulphate docusate calcium glycerine suppositories Bran ‘magnesium hydroxide a castor oil lactulose polyethylene glycol (PEG) 26Mcqs 1. Which of followi \ WINE agent is used to clean bowel before gastrointestinal endoscopic procedure? a) Castor oil b) Mi i ) Mineral oil c) Magnesium hydroxide d) PEG solution 2. Aloe, senna, and castor oil are a) Bulk laxati ; i ) tives b) Osmotic laxatives ¢) irritants or stimulants d) Lubricant laxatives 3. Loperamide acts on receptors, a) Muscarinic b) Adrenergi ©) Opioid (mu receptor) d) Pr-receptors Answers: 1)D 2)C 3)c Q1) What are laxatives, classify them? For answer, refer to the topic 4[Part C(ii)] introductory notes] D) Drugs acting on Respiratory system Asthma, chronic obstructive pulmonary disease (COPD) and allergic rhinitis are commonly encountered respiratory diseases. > Asthma is an inflammatory disease of the airways characterized by episodes of acute bronchoconstriction causing shortness of breath, cough, chest tightness, wheezing, and rapid respiration. Inhaled corticosteroids (ICS) are the drugs of first choice in patients with any degree of persistent asthma (mild, moderate, or severe), COPD & hay fever. Drugs in this class include beclomethasone, fluticasone. ADR’s include, hoarseness and oral can budesonide, Oral/systemic corticosteroids: Patients with severe persistent asthma may require intravenous administration of methylprednisolone or oral prednisone. > These drugs targets underlying airway inflammation by decreasing the inflammatory cascade croahile, macrophages, and T mphoctes), reversing mucosal edema, decreasing the (eosin Cae of capillaries, and inhibiting the release of leukotrienes. permea Methyxanthines are theophylline, theobromine and caffeine. These agents cause bronchodilation by jethylxanthin in the airways. action on the smooth muscles in the airway" jxanthines are considered adjuncts to inhaled corticosteroids and are used to treat bea Clinical use: Methyl at is unresponsive to inhaled corticosteroids or b-adrenoceptor agonists; acute or chronic asthma th ically. they can be administered prophyiactical¥ iting, and gastrointestinal bleedi ‘as, nervousness, vorni ding. Adverse effects: arrhythmias, including, zafirlukast, montelukast, are selective, reversible inhibitors of the Leukotriene antagonists +4) thereby blocking the effects of cysteiny! leukotrienes. They approved for leukotriene-1 receptor (LT 27the prophylaxis of asthma especially in young children. Adverse effects: headache and elevation in liver enzymes. Anticholinergic agents are competitive antagonists at muscarinic receptor and inhibits constriction of bronchial airways. Drugs such as atropine& ipratropium. Inhaled ipratropium is useful in patients who are unable to tolerate adrenergic agonists. They are useful in patients who are refractory to, or intolerant of, sympathomimetics or methylxanthines. Cromolyn and nedocromil are effective prophylactic anti-i flammatory agents. However, they are not Useful in managing an acute asthma attack, because they are not direct bronchodilators. These agents can block the initiation of immediate and delayed asthmatic reactions. they can also be used to treat rhinitis. > Rhinitis is a decrease in nasal airways due to thickening of the mucosa and increased mucus secretion. Allergic rhinitis is characterized by itchy, watery eyes, runny nose, and a non-productive cough. Antihistamines (H1-receptor blockers) are the most frequently used agents in the treatment of sneezing and watery rhinorrhoea associated with allergic rhinitis. H1- blockers include; diphenhydramine, chlorpheniramine, loratadine, and fexofenadine, are useful in treating the symptoms of allergic rhinitis caused by histamine release. g-Adrenoceptor agonists (nasal decongestants) may be administered as nasal aerosols or as oral agents. These agents include epinephrine (nasal aerosols), pseudoephedrine (orally) and phenylephrine, which (oral or nasal aerosol). These agents reduce airway resistance by constricting dilated arterioles in the nasal mucosa. Adverse effects nervousness, tremor, insomnia, dizziness, and risk of rebound nasal congestion. > Cough is produced by the cough reflex, which is integrated in the cough centre in the medulla. Cough receptors located in the trachea and bronchial tree, send signals to the cough centre and trigger the cough reflex. Codeine and Dextromethorphan (opiates) are anti-tussive agents. Codeine decreases the sensitivity of cough centres in the central nervous system to peripheral stimuli and decreases mucosal secretion. Dextromethorphan is a synthetic derivative of morphine that suppresses the response of the central cough centre. Side effects include; constipation, nausea and fatigue. Classification of drugs to treat respiratory disorders Drugs used to treat Drugsusedtotreat | Drugsusedtotreat | Drugs used to asthma allergic rhinitis corp treat Cough Bx-adrenergic agonists | a-adrenergic agonist __| B.-adrenergic agonists _| dextromethorphan corticosteroids Antihistamine Corticosteroids opiates Cromolyn, nedocromil__| Corticosteroids Ipratropium ipratropium Cromolyn Montelukast, zafirlukast Theophylline 28Mcqs 1. Which of the following is ' ? first line therapy for treatment of mild asthma? a) B2-agonists b) Corticx 7 ‘osteroids c) Theophylline d) Propranolol 2+ 2Which of the following is the gold-standard treatment for cough suppression 3) Salmeterol b) Beclomethasone c) Codeine d) Loratadine 3. Which of the following drug is a long-acting B2 agonist? a) Salmeterol_b) Theophylline ¢) Albuterol d) Adrenaline 4. Adverse effects seen with high blood levels of theophylline include a) Nausea and vomiting b) Archythmias c) Nervousness.) all of theses 5. Which of the following drug act as nasal decongestant? a) Codeine b) Theophylline ¢)Salbutamol d) Phenylephrine 6. Long-acting B2 ‘agonists provides bronchodilators for about a) 4-6 hours b) 12 hours c) 24 hours d) 2 hours: 7. Which of the following class are first choice in patients with any degree of persistent asthma? a) Cholinergic antagonists_b) a-agonists c) Inhaled corticosteroids d) B2-agonists 8. An inflammation of the mucous membranes of the nose, characterized by sneezing, itchy watery nose/eyes is called a) Asthma b) Allergic rhinitis) Dermatitis d) Cough 9. Montelukast belongs to group of class called a) B2-agonists b) Corticosteroids c) Leukotriene antagonists d) Theophylline 10. Dextromethorphan is an a) Analgesic b) Antitussive ) Expectorant d) Antihista Answer key 2) ¢ 3) a 4) d 5) d De x 8) de 1b Short Question & Answer rt note on pharmacoloBy OF B2-agonists? ists include short-acting agonists es as albuterol, pirbuterol, terbutaline. They have Ans: B2-agonis' ction (5-30 minutes) and provide relief for 4 to 6 hours, They are used for symptomatic feed oheeios ro gm, providing suck rei fate bronchocontiction, Long-acting agents treatment of ee and formoterol, with long duration of action, providing bronchodilation for at least such as salmete! 12 hours. Q1) Write a shor 29MOA: Adrenergic agonists stimulate B2-receptors, resulting in relaxation of bronchial smooth muscle, These agents also inhibit the release of mediators and stimulate mucociliary clearance. Therapeutic uses: Short-acting agents are best reserved for treatment of acute asthma and prophylaxis for exercise induced bronchospasm. © Long acting agents are used as Maintenance therapy in moderate and severe persistent asthma in combination with inhaled corticosteroids. * Management of chronic obstructive pulmonary disease (COPD) Adverse effects: tachycardia, hyperglycaemia, hypokalaemia, and hypomagnesemia. Q2) Classify drugs used to treat asthma? Ans: For answer, refer to the topic 4(Part D) introductory notes. E) Drugs acting on Cardiovascular System i) Heart failure (HF) is a complex, progressive disorder in which the heart is unable to pump sufficient blood to meet the needs of the body. CHF results when the output of the heart is insufficient to supply adequate levels of oxygen for the body. Symptoms: Dyspnea, fatigue, and fluid retention. Cause: Heart failure is due to an impaired ability of the heart to adequately fill with and/or eject blood. Underlying causes of HF include arteriosclerotic heart disease, myocardial infarction, hypertensive heart disease, valvular heart disease, dilated cardiomyopathy, and congenital heart disease. Renin Angiotensin System blockers consist of «Angiotensin converting enzyme (ACE) inhibitors © Angiotensin receptor blockers (ARB’s) piuretics (Mechanism of action) Diuretics decrease plasma volume and, subsequently, decrease venous return to the heart (preload). This decreases the cardiac workload and the oxygen demand. ‘Therapeutic use of diuretics: combined with an ACE inhibitor in mild CHF © Used for acute pulmonary edema Hypertension Direct vasodilators (MOA) they provide a reduction in preload (through venodilation), or reduction in afterload (through arteriolar dilation), or both. Vasodilators are used to treat severe, decompensated CHF refractory to diuretics and digitalis. 30Classification of drugs used to treat heart failure Angiotensin | B-blockers | Diuretics Direct Inotropic _| Aldosterone Teceptor vasodilators | agents antagonist blockers Captopril | Losartan Spironolactone Atenolol | furosemide —_| Hydralazine (prototype) Enalapril | Valsartan | Carvedilol | Hiydrocloro- _ | Sodium nitroprusside Lsinopul Metoprolol Megs 1. Pick out a drug which act as angiotensin-receptor blocker? a) Hydralazine b) Valsartan c) Digoxin d) Captopril 2. Dry cough isa common side effect of a) Diuretics b) B-blockers c) ACE inhibitors d) angiotensin receptor blockers 3. Which of the following drugs act as ACE inhibitor? a) Digoxin b) Atropine c) Losartan d) Captopril 4. Which of following drugs act as direct vasodilators to treat heart failure and hypertension? a) Digoxin b) Captopril c) Hydralazine d) Metoprolol 5, Which of following therapeutic agent is obtained from digitalis plant? a) Digoxin b) Captopril c) Hydralazine d) Metoprolol 6. Which of following agents inhibit the conversion of angiotensin | to angiotensin II? a) Angiotensin receptor blockers b) B- blockers CYACE inhibitors d) Ca-channel blockers 7. Which of following is first-line drug or drug of choice in the treatment of HF? a) Peblockers b) Diuretics c) ACE inhibitors d) Ca-channel blockers 8, Which class of drugs is an alternative to the use of ACEI's in HF patients with severe cough or angioedema? a) Beblockers b) Digoxin c) ARBlockers d) Ca-channel blockers Answer key 1) b a8 Tm 4c sya 6) a 7) 3) 31Short Questions & Answers Qi) Brief about mechanism of action of ACE inhibitors? ‘Ans: ACE inhibitors inhibit the production of angiotensin I! from angiotensin-|. These agents counteract elevated peripheral vascular resistance and sodium and water retention resulting from angiotensin Il and aldosterone. Thus, ACE inhibitors decrease vascular resistance, venous tone, and blood pressure, resulting in an increased cardiac output. (Note: Angiotensin Il is a vasoconstricting agent and causes sodium retention via release of aldosterone) Q2) Enlist clinical uses of ACE inhibitors? * useful in the treatment of Congestive heart failure ‘© reducing risk of recurrent post-myocardial infarction (Ml) «and treating hypertension Q3) What are common adverse effects of ACE inhibitors? Ans: Adverse effects common to all ACE inhibitors include a persistent dry cough and, rarely, angioedema hypotension, and hyperkalaemia. Q4) What is mode of action of angiotensin receptor blockers? Ans: Angiotensin-receptor blockers (ARBs) works by blocking the binding of angiotensin II to the angiotensin II receptors. By blocking the receptor site, these agents inhibit the vasoconstrictor effects of angiotensin I! while also preventing the release of aldosterone from the adrenal glands. Thus, reducing salt and water retention, lowering BP and preventing subsequent heart failure. Note: IF QUESTION ASKED ABOUT ADRs of ARBsI! ARBs have an adverse effect profile like that of ACE inhibitors except they do not produce cough. Q5) Shortly describe mechanism of action of digoxin? Ans: Digoxin inhibits Na +/K + -ATPase (sodium pump), resulting in increased intracellular Na+ and decreased intracellular K+. Increased Na+ reduces the normal exchange of intracellular Ca2+ and yields elevated intracellular Ca2+ thus, increases the force of cardiac contraction and the cardiac output. Q6) What are therapeutic uses of digoxin? « Itis indicated in patients with severe left ventricular systolic dysfunction after initiation of ACE inhibitor and diuretic therapy. «HF with atrial fibrillation. Q7) What are the adverse effects of digoxin therapy? ‘Ans: digoxin toxicity, arrhythmia, anorexia, nausea, and vomiting, headache, fatigue, confusion, blurred vision. ii) Arrhythmias may be due to both improper impulse generation and impulse conduction (manifest as disturbances in the normal sequence of activation of atria and ventricles). Cardiac arrhythmias 32may cause the heart to beat too slowly (bradycardia) or to beat too rapidly (tachycardia), and to beat regularly (sinus tachycardia or sinus bradycardia) or irregularly (atrial fibrillation). > the antiarrhythmic drugs can modify impulse generation and conduction Mode of action > Class Il drugs are B-adrenoceptor antagonists, including propranolol, which act by reducing sympathetic stimulation. They inhibit phase 4 depolarization, depress automaticity, prolong AV conduction, and decrease heart rate and contractility. Therapeutic uses: Class II drugs are used to treat tachyarrhythmias caused by increased sympathetic act used for a variety of other arrhythmias, including atrial flutter and atrial fibrillation These drugs prevent reflex tachycardia produced by vasodilating agents. > Class Ill agents block potassium channels and, thus, diminish the outward potassium current during repolarization of cardiac cells. These agents prolong the duration of the action potential without altering Phase 0 of depolarization or the resting membrane potential Instead, they prolong the effective refractory period. All Class Ill drugs have the potential to induce arrhythmias. * Amiodarone is effective in the treatment of severe refractory (life-threatening) supraventricular and ventricular tachyarrhythmias Classification of Antiarrhythmics drugs Class | Class il Class tit Class IV Other Na channel B-adrenoceptor _| K- channel Ca- channel Antiarrhythmics blockers blockers blockers blockers drugs Lidocaine Esmolol ‘Amiodarone Diltiazem ‘Adenosine Procainamide Metoprolol Verapamil Digoxin Quinidine Propranolol (prototype) Mcqs 1. The term used for slow heart rate is: a) Bradycardia b) Tachyphylaxis c) Tachycardia d) Anaphylaxis 2. Innormal healthy heart electrical impulse is generated in a) AVnode b) Purkinjie fibres c) Aorta d) SAnode 3. Quinidine belongs to which of the following class of antiarrhythmic drugs? a) Class II b) Class ill c) Class! d) Ca-channel blocker 4. Inderal is generic name for a) Propranolol b) Adrenaline c) Labetalol d) Quinidine 5. Which of the following class of antiarrhythmic drugs are calcium-channel blockers? 33a) Class Il -b) Class Ill c) Class! d) Class IV drugs ig B-blocker used for intravenous administration in acute arrhythmias during 6. Ashort-act emergency? a) Esmolol b) Propranolol c) Labetalol d) Captopril ‘Answer key 2) A 2) d 3) ¢ 4) a 5) d 6) a Short Question & Answers Q1) Classify Antiarrhythmics drugs? Ans: For answer, refer to the topic 4(Part E) introductory notes. Q2) Define mode of action of quinidine? ‘Ans: Quinidine binds to sodium channels and prevents sodium influx, thus slowing the rapid upstroke during Phase 0 (depolarization), prolonging the effective refractory period, increasing the threshold of excitability, and reducing phase 4 depolarization. Q3) What are therapeutic uses of quinidine? the treatment of a wide variety of arrhythmias, including atrial, AV- Ans: Quinidine is use‘ junctional, and ventricular tachyarrhythmias. Q4) Enlist adverse effects of quinidine therapy? Ans: diarrhea, nausea, and vomiting «tinnitus (ringing of the ears and dizziness) toxic cardiac effects include excessive QT-interval prolongation and ventricular arrhythmias. Q5) What are clinical uses of verapamil? Ans: supraventricular tachycardia, © useful in reducing ventricular rate in atrial flutter and fibrillation, «to treat hypertension and angina. Q6) Define mode of action of verapamil? Ans: Verapamil blocks both activated and inactivated slow calcium channels across the myocardial cell membrane. It also reduces intracellular calcium concentration in smooth muscle cells of the coronary and peripheral vasculature. Q7) What possible adverse reactions can occur with Ca- channel blockers? Ans: Verapamil and diltiazem have negative inotropic properties and, therefore, may be contraindicated in patients with pre-existing depressed cardiac function 34iil) Angina pectoris is a characteristic sudden, severe, pressing chest pain radiating to the neck, jaw, back, and arms. ment of the Cause: The primary cause of angina pectoris is an imbalance between the oxygen requi heart and the oxygen supplied to it via the coronary vessels. Types Angina pectoris has 3 types: |) Stable or typical angina ii) unstable angina iii) Prinz metal 's or variant angina Stable angina (typical angina pectoris): most common form of angina. It is characterized by a burning, heavy, or squeezing feeling in the chest. It is caused by the reduction of coronary Perfusion due to a fixed obstruction produced by coronary atherosclerosis. Treatment involves rest or use of nitro-glycerine. fi, Unstable angina: In this type, chest pains occur with increased frequency and are Precipitated by progressively less effort. The symptoms are not relieved by rest or nitro- glycerine. Unstable angina requires hospital admission and more aggressive therapy to prevent death and progression to myocardial infarction. Prinz metal’s or variant or vasospastic angina: it’s an uncommon pattern of episodic angina that occurs at rest and is due to coronary artery spasm. Symptoms are caused by decreased blood flow to the heart muscle due to spasm of the coronary artery. This type generally responds promptly to coronary vasodilators, such as nitro-glycerine and calcium-channel blockers. > Mode of action of B-blockers: f-blockers decrease heart rate, blood pressure, and contractility, resulting in decreased myocardial oxygen requirements. Thus, reduce the frequency and severity of angina attacks. > Clinical uses: These agents are particularly useful in the treatment of patients with myocardial infarction and have been shown to prolong survival. The B-blockers can be used with nitrates to increase exercise duration and tolerance. They are, however, contraindicated in patients with asthma, diabetes, severe bradycardia, peripheral vascular disease, or chronic obstructive pulmonary disease. Classification of Antianginal drugs Organic nitrates B- blockers Ca- channel blockers Isosorbide dinitrate Acebutotol Amtodipine Nitro-glycerine (prototype) Atenolol biitiazem Metoprolol Nifedipine Propranolol (prototype) Verapamil 35Megs 1. Which of the following anti-anginal drugs belongs to organic nitrate class? a) Verapamil b) Propranolol c) Losartan. d) Nitro-glycerine 2. The time to onset of action for nitro-glycerine is a) 1-3 hours b) 1-3 minutes c)12hours d) 1-3 days 3, Which of following drug is contraindicated in patients with prior depressed cardiac functions or AV abnormalities? ed) Captopril a) Verapamil b) Nifedipine c) Nitro-glyce 4. Which of the following anti-anginal drug is administered sublingually for its rapid action and short duration? a) Verapamil b) Propranolol c) Losartan d) Nitroglycerine 5. Which of the following B-blocker is not cardio selective? a) Metoprolol b) Nitro-glycerine c) Propranolol d) Atenolol 6. Which of following drug is also available as transdermal patch? a) Verapamil b) Nitro-glycerine c) Adrenaline d) Propranolol 7. Beblockers are contraindicated in patients with a) Kidney failure b) Asthma c) Angina d) Hypertension 8. Which of following Ca- channel blockers are potent arteriolar vasodilator? a) Nitro-glycerine b) Verapamil c) Nifedipine d) Metoprolol Answer Key i) d 2) b 3) a 4) d 5) ¢ 6) b 7) b 8) ¢ Short Questions & Answers Q1) Brief about mode of action of Nitro-glycerine? ‘Ans: Nitrates decrease coronary vasoconstriction or spasm and increase perfusion of the myocardium by relaxing coronary arteries. Nitro-glycerine relax vascular smooth muscle by their intracellular conversion to nitrite ions, and then to nitric oxide, which in turn leads to activation of (cGMP). Elevated cGMP ultimately results in vascular smooth muscle relaxation. Q2) Enlist therapeutic uses of Nitro-glycerine? * For prompt relief of attack of angina precipitated by exercise or emotional stress, sublingual nitro-glycerine is the drug of choice. a. © Sublingual nitro-glycerine is most often used for severe, recurrent Prinz metal’s angina 36© Organic nit ni ; a a : ic nitrates are effective in stable and unstable angina as well as in variant angina pectoris. 3) What are the adverse effects of organic nitrates? Ans: Orthostatic hypotension, tachycardia, and throbbing headache Q4) How will Ca channel-blockers prevent Angina pectoris? Ans: Ca channel-blockers produce a blockade of L-type (slow) calcium channels, which decreases cardiac contractile force and oxygen requirements. At clinical doses, these agents affect primarily the resistance of vascular smooth muscle and the myocardium. Q5) What are clinical Uses of Ca channel-blocking drugs? * Ans: These drugs are useful for both variant and chronic stable angina and in instances where nitrates are ineffective or when B-blockers are contraindicated © Other clinical uses include hypertension and supraventricular tachyarehythmias Q6) Specify common side effects of Ca-channel-blockers? Ans: flushing, headache, hypotension, peripheral edema and constipation usual side effects. iv) Hypertension is defined as either a sustained systolic blood pressure (SBP) of greater than 140 mm Hg or a sustained diastolic blood pressure (DBP) of greater than 90 mm Hg. Based on etiology hypertension may be; © Essential or primary hypertension: Patients in whom no specific cause can be identified, constitutes, 90% of all cases of systemic hypertension. The average age of onset is about 35 years. © Secondary hypertension, accounts for the remaining 2% t develops between the ages of 30 and 50. The Seventh Report of the Joint National Committee classifies hypertension into four categories for resulting from an identifiable cause, such as renal disease. It -0 5% of cases of systemic hypertension. This type usually treatment management. Normal (SBP/DBP, <120/<80), ii. Prehypertension (SBP/DBP, 120-139/80-89), iii, Stage 1 hypertension (SBP/DBP, 140-159/90 -99), iv. Stage 2 hypertension (SBP/DBP >— 160/>- 100). Arterial blood pressure: is @ product of the cardiac output and the peripheral vascular resistance. BP =CO x PVR Blood pressure controlling mechanisms: Cardiac output and peripheral resistance are controlled mainly by two overlapping control mechanisms: * The baroreflexes, which are mediated by the sympathetic nervous system, and 37‘© The renin-angiotensin-aldosterone system Actions of different classes of anti-hypertensives in lowering BP * Diuretics, lower blood pressure by increasing sodium and water exer volume. Diuretics can be used as first-line drug therapy for hypertension unless there are compelling reasons to choose another agent. 3 classes are used as antihypertensives; zide diuretics, loop diuretics and potassium-sparing diuretics. + Brblockers reduce blood pressure primarily by decreasing cardiac output. They may also decrease sympathetic outflow from the central nervous system and inhibit the release of renin from the kidneys, thus decreasing the formation of angiotensin I! and the secretion of aldosterone. * ACE Inhibitors: These drugs block the ACE that cleaves angiotensin | to form the potent vasoconstrictor angiotensin Il, thus, lower blood pressure by reducing total peripheral vascular resistance. * Angiotensin II-Receptor Antagonists: Block AT1 angiotensin receptors (produce arteriolar and venous dilation and block aldosterone secretion, thus lowering blood pressure and decreasing salt and water retention) © a-Adrenoceptor antagonists, lower total peripheral resistance by preventing stimulation (and consequent vasoconstriction) of a -receptors, which are located predominantly in resistance vessels of the skin, mucosa, intestine, and kidney. These drugs reduce pressure by dilating resistance and conductance vessels. ‘* Vasodilators: are direct-acting smooth muscle relaxants, such as hydralazine and minoxidil. They act by producing relaxation of vascular smooth muscle, which decreases resistance and, therefore, blood pressure. C Classification of Antihypertensive drugs Diuretics Blockers | ACE ‘Angiotensin | Renin | Ca- a- Other AH inhibitors | -Ilreceptor | inhibitors | channel Blockers | agents antagonist blockers Bumetanide | Atenolol | Captopril _| Candesartan | Aliskerin | Amlodipine | Doxazocin | Clonidine (prototype) Eplerenone | carvedilol_ enalapril | Losartan Diltiazem | Prazosin | Hydralazine (prototype) Furosemide | labetalol_| Lisinopril_| Valsartan Nifedipine | Terazosin_| Minoxidil Hydrocloro- | metoprolol Verapamil Sodium Thiazide nitroprussl Spironolactone | Propranolol a (prototype) methyldopaMcqs 1,_Kidney respond to reduced arterial pressure by releasing __enzyme. a) Prolactin b) Renin c) Pepsin d) Lipase 2. In hypertensive patient with no other disease, which class of drug should be used as first-line drug therapy? a) Ca-channel blockers b) Diuretics ¢) B-blocker d) ACE inhibitors 3. Angiotensin-1 is converted in to angiotensin I! in the presence of enzyme. a)Renin b) Progesterone c) Aldosterone d) Angiotensin-converting 4. Which of following is a selective B1- antagonist? a) Propranolol b) Verapamil c) Losartan d) Metoprolol 5. Which class of drugs should be preferred as first-line agents, if diuretics or Bblockers are ineffective? a) Ca» channel blockers _b) a- blockers c) k-sparing diuretics d) ACE inhibitors 6. Losartan is a drug of group. a) B-blocker b) ACEI c) Angiotensin II receptor blocker d) Diuretic 7. Which of the following stimulates secretion of aldosterone hormone? a) Renin b) Angiotensin-Il_c) Angiotensin-I_ d) Vasopressin 8 Which class of drugs are alternatives to the ACE inhibitors? a) B-blocker b) a- blockers c) Angiotensin Il receptor blockers d) Diuretics 9. Which of the following drug acts as selective renin inhibitor? a) Captopril b) Aliskerin ¢) Prazosin d) Hydralazine 10. Dry cough is the main side-effect of a) Captopril b) Propranolol ¢) Adrenaline d) Losartan 11, Which of following anti-hypertensive drug is safe to use in pregnant women? a) Atropine b) Losartan ¢) Propranolol d) Methyldopa 12. Common ADR of a-blockers is: ) Persistent cough ¢) Dryness of mouth d) Postural hypote a) Hypertension 6) Which of the following is az-agonist? Prazosin d) Levodopa 13, a) Hydralazine b) Clonidine ¢) 414. Which of the following drug is administered IV in hypertensive emergency? a) Losartan b) Propranolol ¢) Adrenaline d) Sodium nitroprusside 15, wo of the following drugs act as direct vasodilators? sf Hydralazine b) Losartan c) Spironolactone d) Methyldopa 39Answer key 1) b 2) b 3) d 4) d 5) d 6c 7b 8) c 9) _b 10) a lijd 12)d 13) b 14)d is)a Short Questions & Answers Q1) Classify antihypertensive drugs? Ans: For answer, refer to the topic 4 [Part E(iv)] introductory notes] Q2) Define following terms: a) Blood pressure b) Hypertension Ans: For answer, refer to the topic 4 [Part E(iv)] introductory notes. Q3) State shortly about role of Angiotensin Il in regulating blood pressure? Ans: Angiotensin Il is the body's most potent circulating vasoconstrictor, constricting both arterioles and veins, causing an increase in blood pressure. It’s vasoconstrictor action on the efferent arterioles of the renal glomerulus, increase glomerular filtration. It also, stimulates aldosterone secretion, leading to increased renal sodium reabsorption and increased blood volume, which contribute to a further increase in blood pressure. Q4) Mechanism of action, clinical use and ADR’ Questions (Answers are provided in intro section of the topic). of any of the mentioned class may be asked as short 40Topic 5: Genitourinary System Diuretics: lass of drugs that induce a state of increased urine flow are called diuretics. Therapeutic uses: Diuretic agents are generally used for the management of edema, hypertension, congestive heart failure (CHF), and abnormalities in body uid distribution Side effects: Diuretics can cause electrolyte imbalances such as hypokalaemia, hyponatremia, and hypochloraemia and disturbances in acid-base balance. Mechanism of action of all of diuretics ° » Thiazide diuretics inhibit Na and Cl reabsorption in proximal tubule Loop diuretics inhibit the cotransport of Na+/K+/2CI- in the luminal membrane in the ascending limb of the loop of Henle. Therefore, reabsorption of these ions is decreased. Potassium-sparing diuretics act in the distal collecting tubule to inhibit Na+ reabsorption and K+ excretion Carbonic anhydrase inhibitors inhibit the enzyme carbonic anhydrase in the proximal tubular epithelial cells. These drugs reduce HCO3~ reabsorption and concomitant Nat uptake. They also inhibit excretion of hydrogen(H+) and coupled Nat uptake. Osmotic agents are easily fiitered through glomerulus and are poorly reabsorbable. As a result, net reabsorption of Na+ is reduced. This is due to their ability to carry water with them into the tubular fluid, Classification of Diuretics Thiazide diuretics | Loop diuretics | K-sparing Carbonic ‘Osmotic diuretics anhydrase diuretics inhibitors Chlorothiazide bumetanide Amiloride Acetazolamide | mannitol Chlorthalidone Ethacrynic acid _| Eplerenone Urea Hydrochlorothiazide | Furosemide spironolactone Torsemide Megs 1. Which of following class of diuretics also have antihypertensive effects? a) Acetazolamide b) Urea )Yiydrochlorothiazide d) Adrenaline Potassium sparing diuretics have the primary effect upon the___region in the kidney. 2) Proximal convoluted tubule b) Loop of Henle ch€llecting duct 4) Distal convoluted tubule Which of the following diuretic is an aldosterone antagonist? a) Urea b) Furosemide c) Spironolactone d) Hydrochlorothiazide Which of following diuretic drug is used for treatment of glaucoma? a) Captopril b) Hydrochlorothiazide c) Pilocarpine d)\Xéetazolamide Furosemide have major action on the 41so/Ascending loop of Henle b) descending loop of Henle c) proxi d) collecting ducts 6. Which of the following diuretic acts by inhibiting, carbonic anhydrase enzyme in the proximal tubules? a) Furosemide b) Acetazolamide c) Hydrochlorothiazide d) Spironolactone 7. Major side effect of thiazide diuretics?

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