Probenecid
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Trade names | Probalan |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682395 |
Routes of administration | By mouth |
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Pharmacokinetic data | |
Protein binding | 75-95% |
Elimination half-life | 2-6 hours (dose: 0.5-1 g) |
Excretion | kidney (77-88%) |
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Probenecid, also sold under the brand name Probalan, is a medication that increases uric acid excretion in the urine. It is primarily used in treating gout and hyperuricemia.
Probenecid was developed as an alternative to caronamide[1] to competitively inhibit renal excretion of some drugs, thereby increasing their plasma concentration and prolonging their effects.
Medical uses
Probenecid is primarily used to treat gout and hyperuricemia.
Probenecid is sometimes used to increase the concentration of some antibiotics and to protect the kidneys when given with cidofovir. Specifically, a small amount of evidence supports the use of intravenous cefazolin once rather than three times a day when it is combined with probenecid.[2]
It has also found use as a masking agent,[3] potentially helping athletes using performance-enhancing substances to avoid detection by drug tests.
Adverse effects
Mild symptoms such as nausea, loss of appetite, dizziness, vomiting, headache, sore gums, or frequent urination are common with this medication. Life-threatening side effects such as
Drug interactions
Some of the important clinical interactions of probenecid include those with
Pharmacology
Pharmacodynamics
In gout, probenecid competitively inhibits the reabsorption of uric acid through the
Probenecid also inhibits pannexin 1.[7] Pannexin 1 is involved in the activation of inflammasomes and subsequent release of interleukin-1β causing inflammation. Inhibition of pannexin 1 thus reduces inflammation, which is the core pathology of gout.[7]
Historically, probenecid has been used to increase the duration of action of drugs such as penicillin and other
Pharmacokinetics
In the
History
During World War II, probenecid was used to extend limited supplies of penicillin. This use exploited probenecid's interference with drug elimination (via urinary excretion) in the kidneys and allowed lower doses of penicillin to be used.[9]
Probenecid was added to the International Olympic Committee's list of banned substances in January 1988.[10]
References
- PMID 13171805.
- S2CID 11449580.
- S2CID 20282106.
- PMID 25392987.
- S2CID 24497865.
- ^ "Probenecid". PubChem. U.S. National Library of Medicine. Retrieved 2022-06-12.
- ^ PMID 18596212.
- ISBN 978-0-08-046884-6.
- PMID 16267514.
- ISBN 0-7360-0329-0.