Probenecid is sometimes used along with penicillin antibiotics (e.g., penicillin, ampicillin, nafcillin) to increase antibiotic blood levels.

Combined Drug Responses/ Drug to Drug reactions

Probenecid is sometimes used along with penicillin antibiotics (e.g., penicillin, ampicillin, nafcillin) to increase antibiotic blood levels. This increase makes the antibiotic work better at treating certain infections. Probenecid has no antimicrobial activity and works by decreasing the kidneys' ability to remove the antibiotic from the body, thereby increasing the effect of the antibiotic. How would you describe this drug to drug interaction? Explain?

Expert Solution

The pharmacokinetics of penicillin antibiotics is mainly dominated by rapid renal excretion.

as soon as the drug reaches the systemic circulation it is filtered and excreted by kidney.

kidney eliminates penicillin mainly by two mechanisms. a) glomerular filteration b) tubular secretion.

about 10% of the drug is eliminated via glomerular filteration, rest 90% of the drug is excreted by tubular secretion into the tubular lumen of nephrons by an organic acid transporter protein(OATP).

thus due to this reason the plasma half life of penicillin is just 30 minutes.

but when the penicillin is combined with probenecid, its plasma half life increases because the probenecid blocks the OATP through which the penicillin is excreted out into the tubular lumen. As a result of which the excretion of penicillin is slowed down which helps in mainting a greater concentration of drug in plasma for a greater time.

thus the desirable action is used in giving single dose therapy of penicillin.

Nightingale answered 2 years ago

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