Pharma MCQ 4 Flashcards
by what mechanism do drugs cross the placenta?
down a concentration gradient
how does fetal pH compare to mothers?
relatively acidic
which of the following drugs are metabolised by esterases?
A. prilocaine B. Esmolol C. Aspirin D. diamorphine E. etomidate
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.
Structure of diamorphine molecule?
is a 3,6 diacetylmorphine, a di-ester of one molecule of morphine and two molecules of acetic acid.
How does diamorphine exert its activity at the opioid receptor?
It must first be broken down to 3- and 6-monoacetylmorphine, and on 6- is active. Then by a second ester hydrolysis to morphine.
Where must the hydroxyl group be present for diamorphine activity?
at the 3- position.
How do fentanyl and alfentanil compare in term of plasma clearance, initial volume of distribution and elimination half life.
Fentanyl
- initial volume of distribution,
and longer elimination half life.
But, also has a higher plasma clearance than alfentanil.
Salicylate intoxication may trigger which abnormality in bleeding?
hypoprothrombinaemia
Paracetamol bioavailability?
80% - extensively absorbed from small intestine.
Paracetamol time to peak plasma level?
after one hour of oral administration.
Side effect of giving Paracetamol IV?
Can cause hypotension.
Ketamine:
mixture form?
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.
Ketamine:
mode of action?
Ketamine is a non-competitive inhibitor of the excitatory NMDA receptor
Ketamine:
active metabolites?
Norketamine (demethylated metabolite of ketamine) is one third as potent as ketamine)..
Ketamine:
effect on blood flow?
increases cerebral blood flow, oxygen consumption and intracranial pressure.