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Review of Pharmacology - 9E (2015)

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Central Nervous System<br />

39. Ans. (b) Phenothiazine; (c) Haloperidol (Ref: KDT 6/e p431)<br />

40. Ans. (b) Decreases formation <strong>of</strong> 3-OMD (Ref: KDT 6/e p421)<br />

• Levo-dopa is converted to dopamine by dopa decarboxylase (that cannot cross blood brain barrier).<br />

• Carbidopa is an inhibitor <strong>of</strong> dopa decarboxylase in the periphery. It therefore increases the amount <strong>of</strong> l-dopa<br />

that reaches the brain (due to inhibition <strong>of</strong> peripheral metabolism to dopamine).<br />

• Due to inhibition <strong>of</strong> l-dopa metabolism (by dopa decarboxylase), an alternative pathway <strong>of</strong> metabolism by<br />

catechol-o-methyl transferase (COMT) is activated.<br />

• COMT metabolizes l-dopa to 3-o-methyl dopa (3-OMD) that can complete with l-dopa for entry in the brain.<br />

• Entacapone and tolcapone is useful in Parkinsonism by inhibiting COMT.<br />

41. Ans. (a) Involuntary movements (Ref: KDT 6/e p419)<br />

Carbidopa can decrease all the adverse effects <strong>of</strong> levodopa except<br />

• Involuntary movements<br />

• Behavioural effects<br />

42. Ans. (a) Pramipexole (Ref: KDT 6/e p419, 420)<br />

Directly acting D 2<br />

receptor agonists can be<br />

• Ergot derivatives e.g. bromocriptine and pergolide<br />

• Non-ergot compounds e.g. pramipexole and ropinirole<br />

43. Ans. (c) It is a cerebroselective anticholinesterase that affords symptomatic improvement in Alzheimer’s disease (Ref:<br />

KDT 6/e p472, 473)<br />

44. Ans. (d) All <strong>of</strong> the above (Ref: KDT 6/e p419, 420)<br />

Pramipexole and ropinirole are newer non-ergot dopamine agonists. Now, these are first choice drugs for the treatment <strong>of</strong><br />

Parkinsonism (preferred over levo-dopa).<br />

45. Ans. (d) Catechol-o-methyl transferase inhibition (Ref: KDT 6/e p415)<br />

46. Ans. (d) Reserpine (Ref: KDT 6/e p549)<br />

• Neurotransmitters (like dopamine, serotonin and adrenaline) are stored in the vesicles after their synthesis.<br />

These stores <strong>of</strong> neurotransmitters are released on stimulation <strong>of</strong> the neuron. Reserpine inhibits the vesicular<br />

transport <strong>of</strong> these neurotransmitters resulting in depletion <strong>of</strong> dopamine, serotonin and adrenaline.<br />

• Severe depression (due to deficiency <strong>of</strong> serotonin) leading to suicidal tendencies and extrapyramidal symptoms<br />

(due to deficiency <strong>of</strong> dopamine in the brain) are the adverse effects <strong>of</strong> this drug.<br />

General Central Nervous <strong>Pharmacology</strong> System<br />

47. Ans. (b) Vitamin B complex (Ref: KDT 6/e p418, 419)<br />

• Pyridoxine is a component <strong>of</strong> vitamin B complex.<br />

• Pyridoxine is a c<strong>of</strong>actor for the enzyme, dopa decarboxylase and therefore, administration <strong>of</strong> vitamin B complex can<br />

stimulate the activity <strong>of</strong> this enzyme.<br />

• Dopa decarboxylase converts levo-dopa to dopamine. Increased formation <strong>of</strong> dopamine in the periphery is undesirable<br />

because it cannot cross blood brain barrier. Therefore, stimulation <strong>of</strong> dopa decarboxylase decreases the therapeutic<br />

effect <strong>of</strong> l-dopa.<br />

• If the enzyme, dopa decarboxylase is already inhibited with carbidopa, there will be no interaction with<br />

pyridoxine.<br />

48. Ans. (c) Vitamin B complex (Ref: KDT 6/e p418)<br />

49. Ans. (b) Benzhexol (Ref: KDT 6/e p421)<br />

Central anticholinergics like trihexy phenydyl (Benzhexol) are the only drugs effective in drug induced Parkinsonism.<br />

50. Ans. (c) Pyridoxine (Ref: KDT 6/e p418)<br />

‘Pyridoxine abolishes therapeutic effect <strong>of</strong> levodopa by enhancing peripheral decarboxylation <strong>of</strong> levodopa, less is available<br />

to cross to the brain.<br />

51. Ans. (a) Tacrine (Ref: KDT 6/e p472)<br />

371<br />

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