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Review of Pharmacology - 9E (2015)

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<strong>Review</strong> <strong>of</strong> <strong>Pharmacology</strong><br />

Autonomic Nervous System<br />

22. Ans. (c) It has additional direct agonistic action on nicotinic receptors at muscle end plate (Ref: KDT 6/e p103)<br />

Neostigmine is a quaternary ammonium derivative and is lipid insoluble. Its absorption from GIT and penetration in the<br />

brain and cornea is much less than physostigmine. It produces additional action on N M<br />

receptors.<br />

23. Ans. (b) It is longer acting (Ref: KDT 7/e p108)<br />

• Pyridostigmine acts for 3-6 hours as compared to 0.5-2 hour duration <strong>of</strong> action <strong>of</strong> neostigmine.<br />

• It is less potent than neostigmine.<br />

• Rest <strong>of</strong> the properties are similar to neostigmine.<br />

24. Ans. (a) Shorter duration <strong>of</strong> action (Ref: KDT 6/e p101)<br />

25. Ans. (d) α 2<br />

Receptors (Ref: KDT 6/e p146)<br />

Stimulation <strong>of</strong> α 2<br />

receptors located on ciliary epithelium reduces secretion <strong>of</strong> aqueous humor.<br />

26. Ans. (a) Strong local anaesthetic activity (Ref: KDT 6/e p144)<br />

Timolol and betaxolol are the preferred β-blockers for the treatment <strong>of</strong> glaucoma because they lack local anaesthetic activity.<br />

Drugs possessing this property increase the risk <strong>of</strong> corneal ulcers.<br />

27. Ans. (b) Betaxolol (Ref: KDT 6/e p145)<br />

Betaxolol is a cardioselective β-block useful in glaucoma. It is longer acting than timolol. Another non-selective<br />

β-blocker used topically for the treatment <strong>of</strong> glaucoma is levobunolol.<br />

28. Ans. (b) Cycloplegia (Ref: KDT 6/e p93)<br />

Botulinum toxin interferes with the release <strong>of</strong> ACh and thus acts as a parasympatholytic agent. Bronchospasm and diarrhoea<br />

are the symptoms <strong>of</strong> muscarinic stimulation whereas muscle spasms may be seen on nicotinic stimulation. Cholinergic<br />

drugs cause cyclospasm whereas anticholinergics result in cycloplegia.<br />

29. Ans. (c) Pilocarpine (Ref: KDT 6/e p98)<br />

Pilocarpine is a directly acting and physostigmine is an indirectly acting cholinomimetic useful for glaucoma.<br />

30. Ans. (a) Atropine (Ref: KDT 6/e p104)<br />

31. Ans. (c) Organophosphate poisoning (Ref. KDT 6/e p104, 105)<br />

All the symptoms are <strong>of</strong> anticholinesterase poisoning except raised blood pressure and heart rate. At high doses, ACh can<br />

stimulate N N<br />

and N M<br />

receptors. These symptoms may occur due to the nicotinic actions <strong>of</strong> ACh.<br />

32. Ans. (c) Muscle paralysis (Ref. KDT 6/e p104, 105)<br />

Atropine is a non-selective antagonist at muscarinic receptors. It can penetrate blood brain barrier and reverse the muscarinic<br />

action in the CNS. It can also reverse hypertension and bronchoconstiction caused due to stimulation <strong>of</strong> muscarinic<br />

receptors. However, muscle paralysis is due to Nicotinic (N N<br />

) action on which it has no activity.<br />

33. Ans. (d) Postural hypotension (Ref. KDT 6/e p115)<br />

Postural hypotension is due to blockade <strong>of</strong> sympathetic system. Ganglion blockers inhibit the transmission through both<br />

sympathetic as well as parasympathetic ganglia whereas muscarinic blockers inhibit only parasympathetic activity.<br />

34. Ans. (b) Diarrhea (Ref. KDT 6/e p101)<br />

Neostigmine and pyridostigmine are reversible cholinesterase inhibitors that can cause cholinergic adverse effects like<br />

diarrhoea and increased secretions.<br />

35. Ans. (d) It interferes with the action <strong>of</strong> acetyl cholinesterase (Ref: Katzung 11/e p105)<br />

Neostigmine acts by inhibiting the enzyme acetylcholinesterase. This enzyme is involved in degradation <strong>of</strong> ACh, consequently<br />

neostigmine increases the synaptic level <strong>of</strong> ACh. Muscle weakness can be improved by stimulation <strong>of</strong> N M<br />

receptors<br />

at muscle end plate due to increased ACh.<br />

36. Ans. (c) Cause muscles to relax and be unable to contract (Ref: KDT 6/e p340)<br />

Drugs competing with Ach at neuromuscular junction are competitive or non-depolarizing neuromuscular blockers. These<br />

drugs are used as muscle relaxants. In contrast to depolarizing muscle relaxants, these donot cause initial fasciculations.<br />

37. Ans. (d) Memantine (Ref: KDT 6/e p472, 473)<br />

• Donepezil, rivastigmine, gallantamine and tacrine are cholinergic (due to inhibition <strong>of</strong> cholinesterase enzyme) drugs<br />

useful for Alzheimer’s disease.<br />

• Memantine is an NMDA blocker, used for Alzheimer’s disease.<br />

38. Ans. (d) Quarternary structure (Ref: KDT 6/e p101)<br />

Quarternary ammonium compounds are water soluble and thus cannot cross blood brain barrier. Neostigmine is a quarternary<br />

derivative whereas physostigmine is a tertiary amine.<br />

96<br />

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