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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5406_Библиотеки_им_академика_М_И_Перельмана.pdf
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- •Preface
- •Contents
- •1.1 Introduction
- •1.3 Drug Discovery: A Historical Perspective
- •1.4 Drug Discovery and Development Processes
- •1.5 Modern Approach of Research and Development Strategies
- •Questions
- •2.1 Introduction
- •2.2 Retrosynthetic Analysis: The Concepts
- •1.6 Role of Natural Products in Target Identification
- •1.7 Bioisosterism
- •1.8 Role of Stereochemistry in Drug Discovery
- •2.3 Basic Synthetic Strategies: General Approaches Used for Synthesis Problems
- •2.4 Retrosynthetic Analysis: Other Simplification Rules
- •2.5 Retrosynthetic Analysis: Synthetic Impropriety to Avoid
- •Questions
- •3.1 Introduction
- •3.2 Classification
- •3.3 Mechanism of Action
- •3.4 Analgesic Agents
- •3.5 Anti-Inflammatory Drugs
- •3.6 Opioid Receptor Discovery
- •3.7 Aspirin
- •3.8 Ibuprofen
- •3.9 Paracetamol
- •3.10 Diclofenac
- •Questions
- •4.1 Introduction
- •4.2 Antibacterial Agents
- •4.3 Antifungal Agents
- •4.4 Chloramphenicol
- •4.5 Sulfonamides
- •4.6 Sulfamethoxazole
- •4.7 Sulfacetamide
- •4.8 Trimethoprim
- •Questions
- •5.1 Introduction
- •5.2 Drugs Acting on CNS and Peripheral Nervous System (PNS)
- •5.3 Barbiturates
- •Questions
- •6.1 Introduction
- •6.2 Cardiovascular Drugs
- •6.3 Organic Nitrates
- •Questions
- •7.1 Introduction
- •7.2 The Organism
- •7.3 Drug Testing Systems
- •7.4 Chemotherapy
- •7.5 Classification of Leprosy and the Clinical Symptoms
- •7.6 Leprosy Co-existing Factors
- •7.7 Dapsone
- •7.8 Clofazimine (Lamprene)
- •7.9 Solapsone (Sulphetrone)
- •7.10 Ethionamide (Ethionamidum)
- •7.11 Rifampicin (Rifampin)
- •7.12 Clarithromycin
- •7.13 Minocycline
- •7.14 Other Sulfone Derivatives Active Against Leprosy
- •7.15 Treatment of Leprosy Using Chaulmoogra Oil
- •7.16 WHO Recommended Chemotherapeutic Regimens
- •Questions
- •8.1 Introduction
- •8.2 Structure of Viruses
- •8.3 Life Cycle of Viruses
- •8.4 Antiviral Drug Targets
- •8.5 Antiviral Drugs Acting Against RNA Viruses: HIV
- •8.6 Acquired Immune Deficiency Syndrome (AIDS)
- •Questions
- •9.1 Introduction
- •9.2 Life Cycle of the Malaria Parasite
- •9.3 Antimalarial Drugs
- •9.4 National Drug Policy on Malaria
- •9.5 WHO Guidelines for the Treatment of Malaria
- •Questions
- •10.1 Introduction
- •10.2 Production of Ethyl Alcohol and Citric Acid
- •10.3 Production of Antibiotics
- •10.4 Production of Lysine
- •10.5 Production of Glutamic Acid
- •10.6 Production of Vitamin B2 (Riboflavin)
- •10.7 Microbial Production of Vitamin B12
- •10.8 Production of Vitamin C (Ascorbic Acid)
- •Questions
- •11.1 Medicinal Importance of Haldi or Curcumin (Curcuma longa)
- •11.2 Medicinal Importance of Neem (Azadirachta indica)
- •11.3 Medicinal Value of Vitamin C (Ascorbic acid)
- •11.4 Medicinal Importance of Ranitidine
- •11.5 Medicinal Importance of Ginger (Zingiber officinale)
- •11.6 Medicinal Importance of Tulsi (Ocimum tenuiflorum)
- •11.7 Medicinal Importance of Garlic (Allium sativum)
- •11.8 Medicinal Importance of Ajwain (Trachyspermum ammi)
- •Questions
- •Abbreviations
- •Bibliography
- •Index

352 Pharmaceutical Chemistry
392. The term ischemic heart disease (IHD) is used to designate all of the following
conditions, except:
(a) Angina pectoris (b) Sudden cardiac death
(c) Congestive heart failure (CHF) (d) Arrhythmias
393. Strong anticholinergic effects limit the antiarrhythmic use of:
(a) Quinidine (b) Procainamide
(c) Disopyramide (d) Flecainide
394. Glyceryl trinitrate is administered by all of the following routes, except:
(a) Oral (b) Sublingual
(c) Intramuscular (d) Intravenous
395. Propranolol should not be prescribed for a patient of angina pectoris who is already
receiving:
(a) Nifedipine (b) Felodipine
(c) Verapamil (d) Isosorbide mononitrate
396. In cardiac cells, adenosine:
(a) Causes shortening of action potential duration.
(b) Depolarization.
(c) Increase in normal automaticity.
(d) All of the above
397. Select the correct statement about the action of nitrates on coronary vessels:
(a) They mitigate angina pectoris by increasing total coronary flow.
(b) They preferentially dilate conducting arteries without affecting resistance
arterioles.
(c) They preferentially dilate autoregulatory arterioles without affecting the larger
arteries.
(d) They increase subepicardial blood flow without affecting subendocardial blood
flow.
398. Organic nitrates relax vascular smooth muscle by:
(a) Increasing intracellular cyclic AMP.
(b) Increasing intracellular cyclic GMP.
(c) Decreasing intracellular cyclic AMP.
(d) All of the above
399. The primary mechanism of beneficial effect of glyceryl trinitrate in classical angina
pectoris is:
(a) Increase in total coronary blood flow.
(b) Redistribution of coronary blood flow.
(c) Reduction of cardiac preload.
(d) Reduction of cardiac after load.

Multiple-Choice Questions and Answers 353
400. Which of the following drugs is a class IV antiarrhythmic that is primarily indicated
for the treatment of supraventricular tachyarrhythmias?
(a) Ibutilide (b) Propranolol
(c) Diltiazem (d) Quinidine
401. Which of the following groups of symptoms is most often associated with a patient
who has right-sided heart failure?
(a) Hepatojugular reflux, jugular venous distension, pedal oedema, abdominal
distension
(b) Paroxysmal nocturnal dyspnea, pedal oedema, jugular venous distension,
hepatojugular reflux
(c) Jugular venous distension, hepatojugular reflux, pedal oedema, shortness of
breath
(d) Paroxysmal nocturnal dyspnea, jugular venous distension, abdominal distension,
shortness of breath
402. Unfractionated heparin (heparin is anticoagulant drug) binds to antithrombin-III
and inactivates which of the following clotting factor(s)?
(a) Xa (b) Ixa
(c) Iia (d) All of the above
403. Heparin is
(a) Antiplatelet (b) Anticoagulant
(c) Fibrinolytic (d) Analgesic
404. When compared to unfractionated heparin, low molecular weight heparins have
(a) Preferential binding affinity to factor Xa relative to Iia (thrombin).
(b) Shorter half-lives.
(c) Dose-dependent renal clearance.
(d) All of the above
405. The action of quinidine differs from that of digitalis in
(a) Decreasing irritability of cardiac muscle.
(b) Preventing passage of impulses to the ventricle.
(c) Increasing irritability of heart muscle.
(d) Reducing conductivity.
406. Which of the following drugs is a potassium channel opener?
(a) Pinacidil (b) Hydralazine
(c) Glibenclamide (d) Amiloride

354 Pharmaceutical Chemistry
407. Nitrates and calcium channel blockers are also known as vasodilators, and they are
still used concurrently in angina pectoris because:
(a) They antagonize each other’s side effects.
(b) Nitrates primarily reduce preload while calcium channel blockers primarily
reduce afterload.
(c) Nitrates increase coronary flow while calcium reduce the flow.
(d) Both (b) & (c)
408. Cardiac glycosides are obtained from the following plant source:
(a) Rauwolfia serpentine (b) Strophanthus gratus
(c) Ricinus commounts (d) Atropa belladonna
409. Digoxin given for cardiac failure is extremely valuable in patients of:
(a) Thyrotoxicosis (b) Beri beri
(c) Cor pulmonale (d) Atrial fibrillation
410. The agent given sublingually in an acute attack of angina pectoris is:
(a) Glyceryl trinitrate (b) Amyl nitrite
(c) Erythrital tetranitrate (d) Pentaerythritol tetranitrate
411. Aspirin in small doses (50–150 mg per day):
(a) Is of benefit in patients of unstable angina.
(b) Has thrombolytic action.
(c) Preferentially inhibits prostacyclin synthetase enzyme.
(d) May alleviate need for Verapamil in variant angina.
412. Most effective drug used in acute pain of angina pectoris is:
(a) Mannitol hexanitrate (b) Erythrityl tetranitrate
(c) Sodium nitrate (d) Nitroglycerin
413. Tolerance to nitroglycerin may be overcome by:
(a) Initially using the largest safe dose of the drug.
(b) Using other nitrites.
(c) Temporarily discontinuing the drug for one or two weeks.
(d) Use of higher doses.
414. In heart, potassium channels determine:
(a) Pacemaker function (b) Resting potential
(c) Action potential duration (d) All of the above
415. Which is the MOST appropriate action for a nurse to take before administering
digoxin?
(a) Assess blood pressure (b) Evaluate urinary output
(c) Monitor potassium level (d) Avoid giving with thiazide diuretic

Multiple-Choice Questions and Answers 355
416. E-blockers should be avoided in which of the following conditions?
(a) Angina (b) Myocardial infarction
(c) Hypertension (d) Bronchoconstriction
417. Which of the following effects of calcium channel blockers cause a reduction in blood
pressure?
(a) Calcium influx into cardiac muscles
(b) Increased cardiac output
(c) Decreased renal blood flow
(d) Decreased peripheral vascular resistance
418. Blurred vision or halos are signs of:
(a) Blurred vision (b) Corneal side effects of digoxin
(c) Nothing related to digoxin (d) Digoxin toxicity
419. When administering dopamine (Intropin), it is most important for the nurse to know
that:
(a) The drug’s action varies according to the dose.
(b) The drug may be used instead of fluid replacement.
(c) The drug cannot be directly mixed in solutions containing bicarbonate or
aminophylline.
(d) The lowest dose to produce the desired effect should be used.
420. Competitive antagonism of which of the following occurs at E-receptor sites?
(a) Catecholamines (b) Adrenergic sites
(c) Acetylcholine (d) Norepinephrine
421. Routine laboratory monitoring in clients taking E-blockers should include:
(a) Thyrotropin (b) Creatine phosphokinase
(c) Glucose (d) Sodium
422. These two components are responsible for the hardness and pliability in bone is:
(a) Osteoclasts & collagen (b) Mineralized salts & osteocytes
(c) Mineralized salts & collagen (d) Collagen & elastic fibers
423. Which of the following is considered essential vitamin for breast-fed babies?
(a) Vitamin A (b) Vitamin B
(c) Vitamin C (d) Vitamin D
424. Which of the following vitamins has tetrahydrofolate coenzyme activity based on its
pteridine ring?
(a) Thiamine (b) Vitamin D
(c) Vitamin K (d) Folic acid

356 Pharmaceutical Chemistry
425. Pernicious anaemia is
(a) Due to dietary deficiency of Vitamin B12.
(b) Prevented by oral administration of a Vitamin B12 supplement.
(c) Treated by parenteral administration of folic acid.
(d) Treated by parenteral administration of Vitamin B12.
426. Which condition Michaelis-Menten equation (enzymatic reactions) will appear of
ZERO order (when, K
(a) The substrate concentration is much smaller than K
(b) When K
(c) When V
(d) When K
is much smaller than the substrate concentration.
m
is much smaller than Km.
max
approaches V
m
= half-saturation constant and Q = rate of reaction).
m
.
m
.
max
427. Which vitamin can be classified as a hormone?
(a) Vitamin B12 (b) Vitamin D3
(c) Vitamin E (d) Vitamin K
428. Which of the following is an essential amino acid?
(a) Histadiol (b) Cysteine
(c) Methionine (d) Aspartene
429. The conversion of E-carotene to Vitamin A is carried out in:
(a) Pancreas (b) Spleen
(c) Liver (d) Adrenal cortex
430. Keratin is an example of:
(a) Protein (b) Peptin
(c) Scleroprotein (d) All of the above
431. Degradation of haemoglobin in mammals involves:
(a) Formation of bile pigments (b) Formation of urobilinogen
(c) Formation of biliverdin (d) All are correct
432. Which of the following is an important enzymatic reaction involved in muscular
contraction?
(a) Glucose-6-phosphatase reaction
(b) Glycogenolysis
(c) ATP-Creatine phosphokinase reaction
(d) Glucogenolysis
433. Element found in the centre of Vitamin B12 cyanocobalamin is:
(a) Iron (b) Zinc
(c) Cobalt (d) Magnesium

Multiple-Choice Questions and Answers 357
434. Which of the following is the most important vitamin in pregnancy?
(a) Cyanocobalamin (b) Folic acid
(c) Niacin (d) Pyridoxine
435. Which of the following vitamins is derived from the amino acid tryptophan?
(a) Thiamine (b) Riboflavin
(c) Niacin (d) Folic acid
436. All of the following cause hyperglycemia, except?
(a) Hydrochlorothiazide (b) Cyclosporin
(c) Isotretinoin (d) Cytotoxic cells
437. Which of the following substances has the lowest renal clearance?
(a) Creatinine (b) Glucose
(c) Potassium ions (d) Sodium ions
438. Macrophages originate from:
(a) Mast cells (b) Plasma cells
(c) Cytotoxic cells (d) Monocytes
439. In which condition is itching the least prominent?
(a) Allergic dermatitis (b) Scabies
(c) Fungal infection (d) Psoriasis
440. Which of the following vitamin deficiencies leads to stomatitis?
(a) Vitamin B2 (b) Vitamin A
(c) Vitamin B1 (d) Vitamin E
441. Which of the following groups is least susceptible to cytochrome P450 enzymes?
(a) Terminal methyl groups (b) Allylic carbons
(c) Benzylic carbon atoms (d) Quaternary carbon atoms
442. Importance of Vitamin D in osteoporosis: I- Increase the absorption of calcium from
the small intestine. II- The best Vitamin D analogue to treat osteoporosis is calcitriol.
III- Antacids containing aluminium and magnesium may interfere with proper
activity of vitamin D.
(a) I (b) III
(c) I & II (d) All are correct
443. Which of the following vitamins is depleted in the blood by smoke?
(a) Vitamin C (b) Vitamin B
(c) Vitamin E (d) Vitamin A

358 Pharmaceutical Chemistry
444. Which of the following characteristics is detrimental to oral activity?
(a) Stability to digestive enzymes.
(b) Susceptibility to metabolic enzymes.
(c) Stability to stomach acids.
(d) Solubility in both aqueous and fatty environments.
445. Which of the following statements is the closest description of Phase I metabolism?
(a) Reactions which add a polar molecule to a functional group already present on
a drug or one of its metabolites.
(b) Reactions which occur in the blood supply.
(c) Reactions which add a polar functional group to a drug.
(d) Reactions which occur in the gut wall.
446. Heparin is classified as:
(a) Heteropolysaccharide (b) Oligosaccharide
(c) Homopolysaccharide (d) Monosaccharide
447. The initial distribution of a drug into tissue is determined chiefly by the:
(a) Rate of blood flow to tissue
(b) Glomerular filtration rate
(c) Stomach emptying time
(d) Plasma protein binding of the drug
448. What does onset time of a drug mean?
(a) Time for the drug to be completely absorbed from the intestine.
(b) Time for the drug to reach the steady state.
(c) Time for the drug to reach the maximum effective concentration.
(d) Time for the drug to reach the minimum effective concentration.
449. Which of the following hormone acts on cell walls?
(a) Insulin (b) Alanine
(c) Cortisol (d) Estrogen
450. Which of the following is considered the FIRST precursor of Vitamin A formation?
(a) Retinoic acid (b) Caroteno
(c) Cobalt (d) Calciferol
451. Which vitamin can be classified as hormone?
(a) Vitamin D (b) Vitamin D3
(c) Vitamin E (d) Vitamin K
452. Keratin is an example of:
(a) Protein (b) Peptin
(c) Scleroprotein (d) All of the above

Multiple-Choice Questions and Answers 359
453. Protein disnaturation may happen due to:
(a) Exposure to air (b) Increase in temperature
(c) Chemical reagents (d) All are correct
454. Which of the following enzymes is responsible for the synthesis of DNA?
(a) DNA polymerase (b) DNA gyrase
(c) DNA ligase (d) RNA transferase
455. Glycogenesis is a process characterized by:
(a) The breakdown of glycogen into glucose.
(b) The transformation of glucose to glycogen.
(c) The breakdown of sugar into pyruvate.
(d) The formation of glucose from non-carbohydrates sources.
456. Element found in the centre of Vitamin B12 cyanocobalamin is:
(a) Iron (b) Zinc
(c) Magnesium (d) Calcium
457. Beri beri is caused by deficiency of which of the following vitamins?
(a) Thiamine (b) Riboflavin
(c) Niacin (d) Pyridoxine
458. Which of the following is the most important vitamin in pregnancy?
(a) Cyanocobalamin (b) Folic acid
(c) Pantothenic acid (d) Pyridoxine
459. Which of the following vitamin is derived from the amino acid tryptophan?
(a) Thiamine (b) Riboflavin
(c) Niacin (d) Folic acid
460. Vitamin A is called:
(a) Retinol (b) Pyridoxin
(c) Thiamine (d) Riboflavin
461. Vitamin B1 is called:
(a) Retinol (b) Pyridoxine
(c) Thiamine (d) Niacin
462. Vitamin B2 is called:
(a) Pyridoxin (b) Calcepherol
(c) Thiamine (d) Riboflavin
463. Vitamin B3 is called:
(a) Pyridoxin (b) Retinol
(c) Niacin (d) Folic acid

360 Pharmaceutical Chemistry
464. Vitamin B5 is called:
(a) Pantothenic acid (b) Retinol
(c) Tocopherol (d) Folic acid
465. Vitamin B6 is called:
(a) Pyridoxin (b) Retinol
(c) Niacin (d) Tocopherol
466. Vitamin B7 is called:
(a) Biotin (b) Retinol
(c) Niacin (d) Folic acid
467. Vitamin B9 is called:
(a) Tocopherol (b) Retinol
(c) Pantothenic acid (d) Folic acid
468. Which of the following vitamins has its chemical structure related to PABA?
(a) Cyanocobalamin (b) Folic acid
(c) Pantothenic acid (d) Niacin
469. Which of the following vitamins is the precursor of collagen synthesis?
(a) Vitamin A (b) Vitamin B
(c) Vitamin C (d) Vitamin D
470. Proteins are formed from:
(a) Purines (b) Carbohydrates
(c) Amino acids (d) Monosaccharides
471. The mechanism of action of antiepileptic drugs is:
(a) Enhancement of GAB-ergic (inhibitory) transmission
(b) Inhibition of excitatory amino acids.
(c) Modification of ionic conductance
(d) All of the above.
472. The antiepileptic drugs which produce inhibition of the central effects of excitatory
amino acids is:
(a) Ethosuximide (b) Lamotrigine
(c) Diazepam (d) Tiagabine
473. The drug which is not used for partial and generalized tonic-clonic seizures is:
(a) Carbamazepine (b) Valproate
(c) Phenytoin (d) Vigabatrine
474. The most effective drug in status epilepticus in adults is:
(a) Carbamazepine (b) Ethosuximide
(c) Diazepam (d) Zonisamide

Multiple-Choice Questions and Answers 361
475. Regarding phenytoin:
(a) It affects Ca
(b) It blocks Na
2+
currents, reducing the low-threshold (T-type) current.
+
channels.
(c) It inhibits GABA-transaminase, which catalyzes the breakdown of GABA.
(d) None of the above.
476. Phenytoin is used in the treatment of:
(a) Petit mal epilepsy (b) Grand mal epilepsy
(c) Myoclonic seizures (d) None of the above
477. Dose-related adverse effect caused by phenytoin is
(a) Physical and psychological dependence
(b) Gingival hyperplasia
(c) Exacerbated grand mal epilepsy
(d) Steven-Johnson syndrome
478. The drug of choice for partial seizures is:
(a) Carbamazepine (b) Diazepam
(c) Ethosuximide (d) Phenytoin
479. The mechanism of action of Carbamazepine appears to be similar to that of:
(a) Benzodiazepines (b) Sodium valproate
(c) Phenytoin (d) Ethosuximide
480. The most common adverse effects of Carbamazepine are:
(a) Diplopia, ataxia and nausea
(b) Gingival hyperplasia and hirsutism
(c) Sedation, physical and psychological dependence
(d) All of the above
481. Phenobarbital causes:
(a) Physical and phychological dependence
(b) Exacerbated petit mal epilepsy
(c) Sedation
(d) All of the above
482. Which of the following antiepileptic drugs may produce teratogenicity?
(a) Phenytoin (b) Valproate
(c) Topiramate (d) All of the above
483. The most dangerous effect of antiepileptic drugs after large overdoses is:
(a) Respiratory depression (b) Gastrointestinal irritation
(c) Alopecia (d) Sedation
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