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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

322 Pharmaceutical Chemistry
131. The most important toxicity of amphoterecin B is
(a) Hepatoxicity (b) Nephrotoxicity
(c) Alopecia (hair loss) (d) Bone marrow depression
132. A drug predominantly excreted in bile is
(a) Tetracycline (b) Streptomycin
(c) Erythromycin (d) Benzylpenicillin
133. Broad spectrum antimicrobials sterilize the gut resulting in a fatal inflammation
called pseudomembranous colitis by the growth of one of the following organisms:
(a) Clostridium difficile (b) E. coli
(c) Bacillus anthrabis (d) Clostridium welcbii
134. Gram-positive bacteria appear:
(a) Pink (b) Violet
(c) Both (a) & (b) (d) None of these
135. Gram-negative bacteria appear:
(a) Pink (b) Violet
(c) Both (a) & (b) (d) None of these
136. Rifampicin, an essential anti-TB drug is very safe. The following adverse effects are
common on prolonged use except:
(a) Thrombocytopenia (b) Flu-like syndrome
(c) Light colour urine, sweat and tears (d) Inhibition of Cytochrome P450
137. The macrolid antibiotics have bacteriostatic and bactericidal effects by binding with
(a) 30 S ribosomal subunit of RNA (b) 50 S ribosomal subunit of RNA
(c) 40 S ribosomal subunit of RNA (d) 70 S ribosomal subunit of RNA
138. Antiviral drugs act in many different ways which can be classified as:
(a) RNA inhibitors only (b) DNA inhibitors only
(c) RNA and DNA inhibitors (d) All are correct
139. AIDS virus is:
(a) RNA virus (b) DNA virus
(c) Retrovirus (d) Enterovirus
140. AIDS is caused by:
(a) HTLV-I (b) Bunya virus
(c) HTLV-III (d) All of the above
141. AIDS patients suffer from pneumonia due to:
(a) Pneumocystisis carinii (b) Cryptospodidium
(c) S. pneumoniae (d) Toxoplasma

Multiple-Choice Questions and Answers 323
142. The genetic material in HIV is:
(a) dsDNA (b) ssDNA
(c) sRNA (d) None of these
143. Viral encephalitis, a CNS infection, may best be treated by which of the following
agents?
(a) Benzyl penicillin (b) Vancomycin
(c) Acyclovir (d) Streptomycin
144. A disease which is due to viral infection:
(a) Poliomyelitis (b) Rabies
(c) Chicken pox (d) All of the above
145. mRNA synthesis from DNA is termed:
(a) Transcription (b) Transformation
(c) Translation (d) Replication
146. In AIDS, Kaposis sarcoma may respond to:
(a) Interleukin-2 infusion (b) Azathioprine
(c) Alpha interferon (d) All of the above
147. A patient with AIDS is treated with a combination of agents, which includes
Indinavir. What is the mechanism of action of Indinavir?
(a) Inhibition of RNA synthesis
(b) Inhibition of DNA synthesis
(c) Inhibition of nucleoside reverse transcriptase
(d) Inhibition of viral proteases
148. Example for DNA virus:
(a) Polio virus (b) Adeno virus
(c) Echo virus (d) Poty virus
149. The drug of choice for Varicella-Zoster virus is:
(a) Acyclovir (b) Azidothymidine
(c) Riobavirin (d) Amantadine
150. Which of the following enzymes is responsible for processing HIV proteins during
the production of new viruses?
(a) Integrase (b) Protease
(c) Reverse transcriptase (d) DNA polymerase
151. AIDS disease is caused by a virus belonging to:
(a) Retrovirus group (b) Rhabdo virus group
(c) Hepatitis virus group (d) Adeno virus group

324 Pharmaceutical Chemistry
152. Most common cause of disseminated opportunistic infection in AIDS patients in
western world is:
(a) M. avium intracellulare complex (b) Pneumocystis carinii
(c) Cryptosporidium (d) Zygomycetes
153. Reverse transcriptase is an enzyme involved in the synthesis of:
(a) DNA (b) Soluble RNA
(c) m-RNA from DNA (d) Nucleotides
154. Which of the following statements is true for non-nucleoside reverse transcriptase
inhibitors?
(a) They cannot be used alongside nucleoside reverse transcriptase inhibitors.
(b) They bind to an allosteric binding site.
(c) Resistance can arise due to mutation where an asparagine in the target binding
site is mutated to lysine.
(d) Binding interactions between NNRTIs and the main protein chain in the binding
site are not important.
155. In an HIV infected person, the blood tests will indicate:
(a) High level of CD4 cells.
(b) Severe depletion of CD4 cells.
(c) Low level of T-cells.
(d) High level of T-cells.
156. Cyclic AMP is a secondary messenger that is formed ‘downstream’ of a receptor
activated process. What are the two main targets currently used in anti-HIV therapy?
(a) Reverse transcriptase and protease
(b) Reverse transcriptase and integrase
(c) Protease and integrase
(d) The viral glycoproteins gp120 and gp41
157. Which of the following protease inhibitors was developed by a hybridisation
strategy?
(a) Ritonavir (b) Indinavir
(c) Saquinavir (d) Amprenavir
158. Immunosuppression occurs when HIV destroys significant numbers of:
(a) Plasmacells (b) Erythrocytes
(c) Lymphocytes (d) Thrombocytes
159. The protease enzyme in HIV has two identical amino acids involved in the catalytic
mechanism which leads to peptide bond hydrolysis. Name those identical acids.
(a) Glutamic acid (b) Aspartic acid
(c) Lysine (d) Serine

Multiple-Choice Questions and Answers 325
160. The HIV protease enzyme is symmetrical, whereas mammalian proteases are not.
What significance might this have?
(a) Inhibitors of the HIV protease enzyme must also be symmetrical.
(b) It is possible to design inhibitors that prove selective for the HIV protease over
mammalian proteases.
(c) Only symmetrical substrates are cleaved by HIV protease.
(d) There is no significance.
161. Which of the following statements is false regarding the characteristics of a good
protein target for antiviral drugs?
(a) It should be important to the life cycle of the virus.
(b) It should bear little resemblance to human proteins.
(c) It should be common to different types of virus.
(d) It should be important in the late stages of the virus life cycle.
162. Which one inhibits viral DNA synthesis?
(a) Acyclovir (b) Interferon
(c) Saquinavir (d) Amantadine
163. ________ inhibits uncoating of the viral RNA.
(a) Rimantadine (b) Acyclovir
(c) Vidarabine (d) Didanozine
164. The drug which inhibits viral reverse transcriptase is:
(a) Vidarabine (b) Zidovudine
(c) Gancyclovir (d) Rimantadine
165. The drug which inhibits viral protease:
(a) Vidarabine (b) Saquinavir
(c) Acyclovir (d) Rimantadine
166. The drug of choice for herpes and cytomegalovirus infection treatment is:
(a) Interferon alfa (b) Didonozine
(c) Saquinavir (d) Acyclovir
167. Which one of the following HIV drugs leads to the formation of kidney stones?
(a) Indenavir (b) Lopinavir
(c) Nelfinavir (d) Ritonavir
168. Which of the following is the best surrogate marker for HIV infection?
(a) CD4 count <250 cells/mm
3
(b) Kaposi sarcoma
(c) Pneumocystis carinii pneumonia (d) Oral thrust
169. Which is the most likely to cause pancreatitis?
(a) Lamivudine (b) Stavudine
(c) Zalcitabine (d) Zidovudine

326 Pharmaceutical Chemistry
170. Paclitaxel, the potent anticancer drug, was isolated from:
(a) The Pacific Ocean (b) A fungus
(c) The Pacific Yew tree (d) A bacteria
171. What term is used to indicate the ability of a cancer to invade other parts of the body
and to produce secondary tumours?
(a) Carcinogenesis (b) Apoptosis
(c) Metastasis (d) Mutagenesis
172. Which molecules are involved in the anchoring of cells to an extracellular matrix?
(a) Integrins (b) Interleukins
(c) Angiostatin (d) Cyclins
173. What is the term used to indicate the growth of new blood vessels?
(a) Biosynthesis (b) Angiogenesis
(c) Apoptosis (d) Metastasis
174. Cyclophosphamide is commonly used in anticancer therapy.
O
SR1HN
O
NHR
2
Which of the following statements is not true of the above structure?
(a) It is relatively non-toxic.
(b) It acts as a prodrug.
(c) It cannot be taken orally.
(d) The structure is metabolised to release acrolein.
175. Which of the following inhibits angiogenesis?
(a) VEGF (b) FGF-2
(c) Angiostatin (d) Interleukin-6
176. What sort of therapy involves administration of an antibody linked to an enzyme,
such that the enzyme activates a prodrug?
(a) ADAPT (antibody-directed enzyme prodrug therapy)
(b) GDAPT
(c) ADEPT (antibody-directed enzyme prodrug therapy)
(d) GDEPT (gene-directed enzyme prodrug therapy)
177. Which of the following is a clinical use for a muscarinic agonist?
(a) Treatment of myasthenia gravis
(b) ‘Switching off’ the gastrointestinal tract prior to surgery
(c) ‘Switching on’ the urinary tract after surgery
(d) Increasing heart muscle activity in certain heart defects

Multiple-Choice Questions and Answers 327
178. Atropine has been used to decrease gastrointestinal motility and to counteract
anticholinesterase poisoning.
Me
N
H
CH OH
2
O
O
What function does this molecule have?
(a) Muscarinic agonist (b) Muscarinic antagonist
(c) Nicotinic agonist (d) Nicotinic antagonist
179. What sort of receptor is the nicotinic receptor?
(a) A G-protein coupled receptor (b) A kinase linked receptor
(c) An intracellular receptor (d) An ion channel
180. What sort of receptor is the muscarinic receptor?
(a) A G-protein coupled receptor
(b) A kinase linked receptor
(c) An intracellular receptor
(d) An ion channel
181. Several aromatic amino acid residues present in the cholinergic binding site are
thought to interact with acetylcholine by means of an induced dipole-dipole
interaction. Which part of the acetylcholine is involved?
(a) The acyl methyl group
(b) The ester
(c) The ethylene bridge
(d) The quaternary ammonium head group
182. The following structure (carbachol) is a cholinergic agonist.
HN
O
2
O
+
NMe
3
What is the purpose of the amino group in red?
(a) It acts as a metabolically susceptible group.
(b) It interacts with a hydrophilic pocket in the binding site.
(c) It acts as a steric shield to protect the ester group.
(d) It protects the neighbouring ester group by means of an electronic effect.

328 Pharmaceutical Chemistry
183. Aspirin is converted into salicylic acid in your body by which of the following
reactions?
(a) Hydrolysis (b) Oxidation
(c) Reduction (d) Substitution
184. The structure of diamorphine differs from that of morphine by the addition of which
functional group or groups?
(a) Two acetyl groups (b) Two hydroxyl groups
(c) Two methyl groups (d) One hydroxyl group
185. Which of the following plays a major role in chronic management of arthritis?
(a) Nonsteroidal anti-inflammatory drugs
(b) Glucose
(c) Glucocorticoids
(d) All of the above
186. First cells on the site of inflammation are
(a) Basophils (b) Neutrophils
(c) Platelets (d) Golgi bodies
187. Enkephalins are peptides that:
(a) Have narcotic antagonist activity.
(b) Exert actions resembling those of opiates.
(c) Are found only in the central nervous system.
(d) Cause blood vessel wall relaxation.
188. Gamma aminobutyric acid (GABA) is:
I. The major inhibitory neurotransmitter in the brain.
II. Found primarily in interneurons.
III. Synthesized from glycine.
(a) I (b) III
(c) I & II (d) II & III
189. The mediator most likely to promote pain is:
(a) Prostaglandins (b) Bradykinin
(c) Serotonin (d) Histamine
190. All of the following statements are true regarding chronic inflammation, except:
(a) It may develop as a granulomatous inflammation.
(b) It may be caused by persistent infections such as tuberculosis.
(c) Lymphocytes and eosinophils are rarely involved in its development.
(d) Large number of macrophages are found in the infiltrate.

Multiple-Choice Questions and Answers 329
191. Mediator of promoting greatest increase in vascular permeability, associated with
the acute inflammation is:
(a) Bradykinin (b) Leukotrienes
(c) Prostaglandins (d) Serotonin
192. Which functional group is responsible for the instability of the aspirin?
(a) Ester functional group (b) Alcohol functional group
(c) Ketone functional group (d) Ether functional group
193. _______ is responsible for the synthesis of prostaglandins in the human body:
(a) Stearic acid (b) Arachidonic acid
(c) Myristic acid (d) Lignoceric acid
194. Isozyme primarily responsible for prostaglandin production by cells involve
inflammation of:
(a) COX-I (b) COX-II
(c) Tyrosinase (d) Zymage
195. Codeine is used as an analgesic.
MeO
O
HO
NMe
H
H
Which of the following statements is false?
(a) The structure is a weaker analgesic than morphine.
(b) The structure acts as a prodrug.
(c) The structure is converted to morphine in the brain.
(d) The coloured methyl group masks an important binding group.
196. Phases of inflammation include:
(a) The immune response (b) Acute inflammation
(c) Chronic inflammation (d) All of the above
197. Analgesic effect of aspirin:
(a) Subcortical site of action (b) Peripheral action (inflammation)
(c) Both a and b (d) No effect
198. Drug associated with the hepatic/renal toxic metabolites: N-acetyl-p-benzoqui-
none is:
(a) Aspirin (b) Indomethacin
(c) Acetaminophen (d) Diclofenac

330 Pharmaceutical Chemistry
199. Which of the following is important in successful pain management?
(a) Dosing appropriately
(b) One-time measurement of pain status
(c) Treating all cases in the same way
(d) Use the strongest drugs available
200. In the treatment of rheumatoid arthritis, the salicylates:
(a) Stop and often reverse the progressive joint involvement.
(b) Specifically reverse the cause of the disease.
(c) Provide only analgesic and anti-inflammatory effects.
(d) Are effective because they are uricosuric agents.
201. Non-narcotic analgesics are mainly effective against pain associated with:
(a) Surgery (b) Inflammation or tissue damage
(c) Trauma (d) Myocardial infarction
202. Non-narcotic agents cause:
(a) Physical dependence (b) Antipyretic effect
(c) Respiratory depression (d) Euphoria
203. Which class of drug is Diclofenac sodium (Voltaren)?
(a) Carboxylic acids (salicylates) (b) Acetic acids
(c) Non-acidic compounds (d) Natural opioids
204. Non-narcotic analgesics are all of the following drugs, except:
(a) Acetylsalicylic acid (b) Butorphanol
(c) Paracetamol (c) Ketorolac
205. Which of the following non-narcotic agent is a salicylic acid derivative?
(a) Aspirin (b) Ketamine
(c) Paracetamol (d) Phenylbutazone
206. Select the Pirazolone derivative:
(a) Paracetamol (b) Methyl salicylate
(c) Analgin (d) Ketorolac
207. An oral chelating agent used in the treatment of rheumatoid arthritis is:
(a) Allopurinol (b) Sulphinpyrazone
(c) Indomethacin (d) Penicillamine
208. In the treatment of rheumatoid arthritis, the salicylates:
(a) Stop and often reverse the progressive joint involvement.
(b) Specifically reverse the cause of the disease.
(c) Provide only analgesic effect.
(d) Are effective because they are uricosuric agents.

Multiple-Choice Questions and Answers 331
209. The use of Indomethacin in gout treatment:
(a) Inhibits the acute gout arthritis inflammation by inhibition of prostaglandin
formation.
(b) Inhibits tubulin synthesis.
(c) Accelerates renal excretion of uric acid.
(d) Inhibits uric acid synthesis.
210. Select the non-narcotic agent which inhibits mainly COX in CNS:
(a) Acetylsalicylic acid (b) Paracetamol
(c) Ketorolac (d) Ibuprofen
211. Most of non-narcotic analgesics have:
(a) Antipyretic effect (b) Analgesic effect
(c) Anti-inflammatory effect (d) All of the above
212. Select the non-narcotic drug which lacks an anti-inflammatory effect:
(a) Aspirin (b) Paracetamol
(c) Naloxone (d) Metamizole
213. Narcotic analgesics should:
(a) Relieve severe pain.
(b) Induce a stupor or somnolent state.
(c) Induce loss of sensation.
(d) Reduce anxiety and exert a calming effect.
214. In the brain and spinal cord regions, which are involved in the transmission of pain?
(a) The substantia gelatinosa
(b) The ventral and medial parts of the thalamus
(c) The limbic system, including the amygdaloidal nucleus and the hypothalamus
(d) All of the above
215. Mu (P) receptors are associated with
(a) Dysphoria, hallucinations, respiratory and vasomotor stimulation
(b) Analgesia, euphoria, respiratory depression, physical dependence
(c) Analgesia, euphoria, respiratory stimulation, physical dependence
(d) Spinal analgesia, mydriasis, sedation, physical dependence
216. Which analgesic is a strong Mu receptor agonist?
(a) Pentazocine (b) Buprenorphine
(c) Naloxone (d) Morphine
217. Select the natural agonist narcotic analgesics:
(a) Naloxone (b) Meperidine
(c) Fentanyl (d) Morphine
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