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Pharmacology · General pharmacology and pharmacokinetics: P-glycoprotein
Sample itemLoperamide is an opioid agonist that normally causes no central effects, yet volunteers given loperamide with quinidine developed respiratory depression. Which transporter did quinidine inhibit to produce this effect?
Original practice item, not a recalled exam question. Nothing here is recorded.
The answer and the reasoning
A. P-glycoprotein efflux pump
P-glycoprotein in brain capillary endothelium pumps loperamide back into blood and keeps it out of the brain. Quinidine inhibits this pump, so loperamide reaches mu receptors in the brainstem. P-glycoprotein also affects digoxin and many cancer drugs.
Option by option
A. P-glycoprotein efflux pump (correct)
Correct. Inhibiting the efflux pump at the blood-brain barrier lets loperamide enter the brain.
B. Organic cation transporter OCT2
OCT2 mediates renal secretion of cations such as metformin and does not protect the brain.
C. Organic anion transporter OAT1
OAT1 handles renal secretion of organic anions and does not guard the brain from loperamide.
D. Uric acid transporter URAT1
URAT1 reabsorbs urate in the proximal tubule and is unrelated to brain entry.
Source note: Original NextPrep sample item — pending expert review. This item is original practice material awaiting independent expert review, so confirm important facts in a standard textbook.
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