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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5648_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

332 Pharmaceutical Chemistry
218. Select the opioid analgesic which is used in the treatment of acute pulmonary
oedema:
(a) Codeine (b) Fentanyl
(c) Morphine (d) Loperamide
219. In contrast to morphine, methadone
(a) Is more effective orally.
(b) Has less severe withdrawal, although more prolonged.
(c) Causes tolerance and physical dependence more slowly.
(d) All of the above
220. Which of the following statements concerning the anti-inflammatory effect of
NSAIDs are true?
(a) Anti-inflammatory effect of NSAIDs results from inhibition of cyclooxygenase.
(b) Anti-inflammatory effect of NSAIDs results from inhibition of phospholipase A2
and reducing prostaglandin and leukotriene synthesis.
(c) Anti-inflammatory effect of NSAIDs results from induction of cyclooxygenase-II
expression which results in reducing the amount of an enzyme available to
produce prostaglandins.
(d) All of the above
221. Which of the following NSAIDs is a selective COX-2 inhibitor?
(a) Piroxicam (b) Indomethacin
(c) Celecoxib (d) Diclofenac
222. The following statements concerning aspirin are true, except:
(a) In contrast to most other NSAIDs, aspirin irreversibly inhibits COX.
(b) Aspirin interferes with the chemical mediators of the kallikrein system.
(c) Aspirin inhibits phospholipase A2.
(d) Aspirin inhibits tromboxane A2 formation.
223. Indication for aspirin administration are the following, except:
(a) Inflammatory conditions
(b) Decreasing the incidence of transient ischemic attack, unstable angina, coronary
artery thrombosis with myocardial infarction, and thrombosis after coronary
artery bypass grafting.
(c) Relieving severe visceral pain (myocardial infarction, cancer pain condition,
renal orbiliary colic).
(d) Reducing elevated body temperature.

Multiple-Choice Questions and Answers 333
224. The following structure is more active than morphine as an analgesic.
HO
AcO
O
NMe
H
H
What is this structure called?
(a) 6-Acetylmorphine (b) 3-Acetylmorphine
(c) Heterocodeine (d) Heteromorphine
225. Propose the likely analgesic activity of 3-acetylmorphine relative to diamorphine
and 6-acetylmorphine.
(a) 3-acetylmorphine should be more active than 6-acetylmorphine and diamorphine.
(b) 3-acetylmorphine should be less active than 6-acetylmorphine and diamorphine.
(c) 3-acetylmorphine should be more active than 6-acetylmorphine and less active
than diamorphine.
(d) 3-acetylmorphine should be less active than 6-acetylmorphine and more active
than diamorphine.
226. Which one of the following is not an opium alkaloid?
(a) Codeine (b) Morphine
(c) Nalorphine (d) Papaverine
227. Benzodiazepine antagonist includes one of the following:
(a) Alprazolam (b) Clorazepate
(c) Flumazenil (d) Sufentanil
228. The binding site of analgesic receptors has two hydrophobic binding regions in the
vicinity of the ionic binding region. One is responsible for agonist activity and the
other is responsible for antagonist activity. Which of the following statements is
true?
(a) The antagonist hydrophobic binding region is closer to the ionic binding
region than the agonist hydrophobic binding region.
(b) The agonist hydrophobic binding region is closer to the ionic binding region than
the antagonist hydrophobic binding region.
(c) The antagonist hydrophobic binding region and agonist hydrophobic binding
region are equidistant from the ionic binding region.
(d) The relative positions of the hydrophobic regions vary depending on the type of
analgesic receptor concerned.

334 Pharmaceutical Chemistry
229. Consider the following analgesic:
H2N
O
N
H
O
OH
O
H
N
N
H
H
N
COOH
O
SMe
What is the source of this structure?
(a) Opium
(b) Frog
(c) An endogenous compound present in the body
(d) Snake venom
230. Morphine is the structure chiefly responsible for the biological activity of opium.
What is the name given to the chemical that is chiefly responsible for the biological
activity of a natural extract?
(a) Lead compound (b) Active principle
(c) Pharmacophore (d) Lead principle
231. Which of the following anaesthetics is preferred for outdoor procedures and the
patient is ambulatory on the same day?
(a) Propofol (b) Midazolam
(c) Halothane (d) Thiopentone
232. Toxicity of which anaesthetic agent causes megaloblastic anaemia on prolonged
use?
(a) Ketamine (b) Halothane
(c) Nitrous oxide (d) Desflurane
233. Zolpidem, a non-benzodiazepine hypnotic agent has the following characteristic:
(a) It possesses little muscle relaxing property.
(b) It has no anticonvulsant properties.
(c) Acts on a subset of benzodiazepine receptors.
(d) Development of tolerance is common on prolonged use.
234. SSRIs are less effective than tricyclic anti-depressant in the management of:
(a) Generalized anxiety disorder
(b) Premenstrual dysphoric disorder
(c) Chronic pain of neuropathic origin
(d) Obsessive compulsive disorder

Multiple-Choice Questions and Answers 335
235. Overdose of benzodiazepines can be reversed with:
(a) Glutamate (b) Flumazenil
(c) Naloxone (d) Nalmefene
236. Which one of the following is not a side effect of phenytoin?
(a) Alopecia (hair loss) (b) Hirsutism
(c) Nystagmus (d) Osteomalacia
237. Following statements about carbamazepine are true, except:
(a) Highly effective for generalized tonic-clonic seizures.
(b) Acts through blockade of Na-ion channels.
(c) Use is associated with drug dependence.
(d) Increases hepatic metabolism of other drugs.
238. All of the following drugs can be used for chronic ethanol intoxication, except:
(a) Methanol (b) Disulfiram
(c) Topiramate (d) Acamprossate
239. All of the following are excitatory neurotransmitters, except:
(a) Serotonin (b) GABA
(c) Nor epinephrine (d) Glutamate
240. Which of the following opioid analgesics is generally used in combination with
droperidol to produce neuroleptanalgesia?
(a) Pentazocine (b) Meperidine
(c) Fentanyl (d) Buprenorphine
241. Which of the following is a more potent analgesic as compared to morphine?
(a) Fentanyl (b) Tramadol
(c) Nalaxone (d) Pethidine
242. All of the following are partial opioid agonists except:
(a) Pentazocine (b) Codeine
(c) Buprenorphine (d) Nalbuphine
243. Disulfiram produces alcohol intolerance by inhibiting
(a) Xanthine oxidase (b) Aldehyde dehydrogenase
(c) Alcohol dehydrogense (d) Carbonic anhydrase
244. Which of the following barbiturates is used in the treatment of kernicterus?
(a) Oxybarbitone (b) Secobarbitone
(c) Phenobarbitone (d) Thiopentone
245. Which of the following is incorrect about barbiturates (may be more than one):
(a) They can cross BBB.
(b) They can cross the placental barrier to the foetus.
(c) They are bound to plasma proteins.
(d) They are absorbed into fatty tissues.

336 Pharmaceutical Chemistry
246. Hypotension resulting from spinal anaesthesia can be treated with:
(a) Epinephrine (b) Atropine
(c) Ephedrine (d) Phentolamine
247. A benzodiazepine that is converted into active form by gastric juice is:
(a) Desmethyldiazepam (b) Alprazolam
(c) Clorazepate (d) Midazolam
248. In local anaesthesia,
(a) Drugs having low water solubility are suitable for infiltration anaesthesia,
(b) Ester type drugs produce more hypersensitivity reactions than the amides.
(c) Efficacy of drugs is increased by low pH.
(d) Long acting local anaesthetics also bind with the proteins and cannot be displaced
by other drugs.
249. Which of the following antipsychotic acts on a wider variety of receptors:
(a) Lithium carbonate (b) Risperidone
(c) Chlorpromazine (d) Olanzapine
250. This is the only drug among older antipsychotics not effective as antiemetic:
(a) Fluphenazine (b) Thioridazone
(c) Thiothixine (d) Chlorpromazine
251. Tricyclic antidepressants may cause all of the following adverse effects, except:
(a) Retention of urine (b) Dryness of mouth
(c) Constipation (d) Insomnia
252. Regarding benzodiazepines:
(a) They can cause retrograde amnesia.
(b) They can cause dose related anterograde amnesia.
(c) They can cause irreversible confusion state in elderly.
(d) Most of benzodiazepines do not have muscle relaxant properties.
253. Desipramine can be used in the following conditions, except:
(a) Hyperkinetic syndrome (b) Endogenous depression
(c) Malignant hyperthermia (d) Chronic pain
254. Anti-cholinergic drugs may be used in pre-anaesthetic medication to
(a) Prevent bradycardia.
(b) Dilate the pupils.
(c) Slow down the gastric emptying.
(d) Prevent colic during visceral surgery.

Multiple-Choice Questions and Answers 337
255. Which of the following antipeptic ulcer drugs cause salt and water retention?
(a) Omeprazole (b) Ranitidine
(c) Sucralfate (d) Carbenoxolone
256. Drug of first choice for Bacteroides fragilis induced peritonitis is
(a) Chloramphenicol (b) Rifampicin
(c) Metronidazole (d) Ampicillin
257. Which of the following anti-TB drugs is structural analogue of PABA?
(a) Rifampicin (b) Ethambutol
(c) p-Amino salicylic acid (d) Thiacetazone
258. Which of the following is a natural chemical messenger for the adrenergic receptor?
(a) Acetylcholine (b) Dopamine
(c) Serotonin (d) Noradrenaline
259. What is the predominant adrenoceptor in heart muscle?
(a) D
(c) E
-adrenoceptor (b) D2-adrenoceptor
1
-adrenoceptor (d) E2-adrenoceptor
1
260. What is the predominant E-adrenoceptor in bronchial smooth muscle?
(a) E
(c) E
261. What is the main clinical use for agonists of the E
-adrenoceptor (b) E2-adrenoceptor
1
-adrenoceptor (d) E4-adrenoceptor
3
-adrenoceptor?
2
(a) Treatment of angina (b) Treatment of hypertension
(c) Treatment of asthma (d) Treatment of pain
262. What is the main clinical use for antagonists of the E
-adrenoceptor?
1
(a) Treatment of glaucoma (b) Treatment of hypertension
(c) Treatment of asthma (d) Treatment of pain
263. To which class of compounds do adrenaline, noradrenaline and dopamine belong?
(a) Phenethylamines (b) Diphenolethylamines
(c) Catecholamines (d) Adrenergics
264. ,GHQWLI\WKHWDFWLFZKLFKLVXVHGWRREWDLQǃDGUHQRFHSWRUVHOHFWLYLW\IRUDGUHQHUJLF
agonists:
(a) Introduction of a naphthalene ring
(b) Introduction of a bulky N-alkyl substituent
(c) Removal of one of the catechol OH groups
(d) Addition of an D-methyl group (alpha to the carbon bearing the amine)

338 Pharmaceutical Chemistry
265. Dopamine is useful in the treatment of cardiogenic shock because it:
I. Selectively dilates renal and mesenteric vascular beds.
II. Does not induce peripheral vasoconstriction.
III. Decreases the force of myocardial contraction.
(a) I (b) III
(c) I and II (d) II and III
266. What is the disadvantage of using adrenaline as an adrenergic agonist?
(a) Poor activity (b) Rapid metabolism
(c) Poor selectivity (d) All of the above
267. Salbutamol is an important clinical agent. The coloured groups are modifications
that distinguish the molecule from adrenaline or noradrenaline.
OH
H
HOH2C
H
N
CMe
3
HO
What role does the t-butyl group play?
(a) It acts as Steric shield to reduce metabolism.
(b) It increases hydrophobicity such that the molecule can cross cell membranes.
(c) ,WLQWURGXFHVVHOHFWLYLW\IRUǃDGUHQRFHSWRUV
(d) It introduces selectivity for D-adrenoceptors.
268. Salbutamol is an important clinical agent. The coloured groups are modifications
that distinguish the molecule from adrenaline or noradrenaline.
OH
HOH2C
H
HO
H
N
CMe
3
Why was the hydroxymethylene group introduced?
(a) It was a chain extension to place the OH group closer to its binding region in the
binding site.
(b) It was introduced to increase the area of conformational space available to the
OH group.
(c) It was introduced to reposition of the phenol OH such that it was not recognised
by metabolic enzymes.
(d) It was introduced to reduce the electronic influence of the OH group on the
aromatic ring.

Multiple-Choice Questions and Answers 339
269. True about malaria is that:
(a) All stages of the erythrocytic schizogony in P. falciparum occur in the peripheral
blood.
(b) The individuals harbouring gametocytes are carriers.
(c) Schizonts of P. vivax do not occupy the entire area in the RBC.
(d) Pre-erythrocyte stage in P. falciparum is longer than that in P. vivax.
270. Which is true of sporozoites of malaria parasite?
(a) Covered with cuticle (b) 14P long and 1P broad
(c) Prominent nucleus in the centre (d) All of the above
271. Asexual reproduction during schizogony of malaria parasite is:
(a) A type of fragmentation (b) A type of multiple fission
(c) A type of binary fission (d) A type of budding
272. Trophozoites, schizonts and gametocytes of all the malarial parasites are seen in the
peripheral blood smear, except:
(a) P. falciparum (b) P. malariae
(c) P. ovale (d) P. vivax
273. Example of drug used in prophylaxis of malaria is:
(a) Cloroquine (b) Quinine
(c) Primaquin (d) Quinine
274. Antimalarial drug used in the treatment of rheumatoid arthritis as DMRA-Disease-
Modifying Antirheumatic Drug is:
(a) Chloroquine (b) Quinine
(c) Primaquine (d) Hydroxychloroquine
275. Which of the following is known as tiger mosquito?
(a) Aedes (b) Monsoni
(c) Culex (d) Anopheles
276. Which of the following spreads Kala-azar?
(a) Aedes (b) Tsetse fly
(c) Male Phlebotomus (d) Female Phlebotomus
277. Which of the following harbours schizont stage of malaria parasite?
(a) Erythrocytes of man (b) Blood of Anopheles
(c) Stomach of Anopheles (d) Salivary gland of Anopheles
278. All of the following are examples of quinolone antimicrobial agents, except:
(a) Cephalexin (b) Ofloxacin
(c) Norfloxacin (d) Ciprofloxacin

340 Pharmaceutical Chemistry
279. Antimalarial drugs chloroquine, amodiquine and mefloquine are effective against:
(a) Erythrocytic asexual stages (b) Cryptomerozoites
(c) Sporozoites (d) Exo erythocytic stage
280. Exflagellation in the life cycle of malaria parasite takes place in:
(a) Human liver (b) The cavity of mosquito stomach
(c) Human blood (d) The wall of mosquito stomach
281. Drug used together with chloroquine in the treatment of malaria with the purpose
to kill persistent parasites in the liver of a person infected with Plasmodium vivax is:
(a) Quinine (b) Sulfadoxine
(c) Primaquine (d) Quinidine
282. Cerebral malaria is caused by
(a) P. ovale (b) P. vivax
(c) P. malariae (d) P. falciparum
283. Incubation period of malaria due to P. vivax is
(a) 7-9 days (b) 10-14 days
(c) 4-6 days (d) 13-20 days
284. Patient is resistant to chloroquine and needs to be treated for malaria. Which of the
following drugs or combination is more appropriate for this patient?
(a) Chloroquine & primaquine (b) Quinine & doxacycline
(c) Mefloquine (d) (b) and (c)
285. The gametocyte in the life cycle of malaria parasite are formed in:
(a) Stomach of male Anopheles (b) Salivary gland of Anopheles
(c) Human blood (d) Stomach of female Anopheles
286. Incubation period of malaria parasite is:
(a) Duration between the times of entry of sporozoites in the blood accompanied
with fever.
(b) Duration required for completing Ross cycle.
(d) Duration between the times of entry of sporozoites in the blood and entry of
cryptomerozoites into the mosquito.
(d) Duration required completing one complete life cycle of malaria parasite.
287. Male Anopheles mosquitoes do not carry malarial parasite, because:
(a) They cannot digest the malarial parasite.
(b) Malarial parasite is digested in the male mosquito.
(c) It has no modified mouth parts to suck the human blood.
(d) It is too small to carry the parasite.

Multiple-Choice Questions and Answers 341
288. Black water fever is a special manifestation of malaria caused by:
(a) P. falciparum (b) P. malariae
(c) P. ovale (d) P. vivax
289. Giemsa stain is used to demonstrate:
(a) Eggs of Ascaris (b) Microfilariae
(c) Malarial parasite (d) Mycoplasm
290. Which of the following mosquitoes spreads malaria in India?
(a) Anopheles flunitis (b) Anopheles minus
(c) Anopheles stephensi (d) Anopheles culcifcies
291. After sporozoite gain entry into the human body it undergoes developmental cycle
first in the liver then in RBC, only after which fever is seen. This incubation period
varies between plasmodium species, and ………….. species has longest incubation
period.
(a) P. falciparum (b) P. malariae
(c) P. ovale (d) P. vivax
292. Leptomonad stage in the life cycle of L. donovani occurs in:
(a) Liver cells of man (b) Macrophages of man
(c) Male Phlebotomus (d) Midgut of female Phlebotomus
293. Plasmodium that causes malaria in man and apes is a:
(a) Ciliate (b) Actinopod
(c) Sporozoan (d) Flagellate
294. Mosquitoes is/are the vector in the following disorder(s):
(a) Onchocerciasis (b) Visceral leishmaniasis
(c) African trypanosomiasis (d) Bancroftian filariasis
295. In malaria, where do the asexual sporozoites undergo schizogony to form merozoites?
(a) In the stomach of the female Anopheles mosquito
(b) In liver cells
(c) In red blood cells
(d) In macrophages
296. Single hosted parasite is:
(a) Hookworm (b) Ascaris
(c) Strongyloides (d) Loa loa
297. Malaria parasite was first discovered by:
(a) James (b) Meckel
(c) Raffacle (d) Laveran
298. Who discovered Plasmodium?
(a) Losch (b) Meckel
(c) Laveran (d) James
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