Pharma MCQ 4 Flashcards

1
Q

by what mechanism do drugs cross the placenta?

A

down a concentration gradient

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2
Q

how does fetal pH compare to mothers?

A

relatively acidic

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3
Q

which of the following drugs are metabolised by esterases?

A. prilocaine
B. Esmolol
C. Aspirin
D. diamorphine
E. etomidate
A

all except prilocaine because it is an amide rather than an ester.

True. Metabolised rapidly by red cell esterases, esmolol has a short t1/2 of 10 minutes.

True. Aspirin is acetylsalicylic acid, metabolised by liver esterases to its components before undergoing further metabolism.

True. Diacetylmorphine, a pro-drug, requires to be broken down by esterases to 6-monoacetylmorphine and morphine in order to bind to opioid receptors.

True. Metabolism of etomidate is by non-specific liver esterases.

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4
Q

Structure of diamorphine molecule?

A

is a 3,6 diacetylmorphine, a di-ester of one molecule of morphine and two molecules of acetic acid.

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5
Q

How does diamorphine exert its activity at the opioid receptor?

A

It must first be broken down to 3- and 6-monoacetylmorphine, and on 6- is active. Then by a second ester hydrolysis to morphine.

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6
Q

Where must the hydroxyl group be present for diamorphine activity?

A

at the 3- position.

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7
Q

How do fentanyl and alfentanil compare in term of plasma clearance, initial volume of distribution and elimination half life.

A

Fentanyl
- initial volume of distribution,
and longer elimination half life.

But, also has a higher plasma clearance than alfentanil.

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8
Q

Salicylate intoxication may trigger which abnormality in bleeding?

A

hypoprothrombinaemia

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9
Q

Paracetamol bioavailability?

A

80% - extensively absorbed from small intestine.

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10
Q

Paracetamol time to peak plasma level?

A

after one hour of oral administration.

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11
Q

Side effect of giving Paracetamol IV?

A

Can cause hypotension.

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12
Q

Ketamine:

mixture form?

A

It is presented as a racemic mixture, or as the S-enantiomer, which is more potent than the R-form and has fewer side-effects.

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13
Q

Ketamine:

mode of action?

A

Ketamine is a non-competitive inhibitor of the excitatory NMDA receptor

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14
Q

Ketamine:

active metabolites?

A

Norketamine (demethylated metabolite of ketamine) is one third as potent as ketamine)..

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15
Q

Ketamine:

effect on blood flow?

A

increases cerebral blood flow, oxygen consumption and intracranial pressure.

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16
Q

What poison can cause muscle weakness, lethargy and eventually paralysis and why?

A

Organophosphates - acetylcholinerase enzyme inhibitors.

Cause over stimulation at the NMJ.