Probenecid ๐
Always check the
BNF link here or equivalent for prescribing advice
- ๐งช Probenecid is a uricosuric drug that has historically also been used to boost concentrations of other drugs (e.g. penicillin).
- ๐ Occasionally misused to mask drugs in athletesโ urine screens.
โ๏ธ Actions
- ๐ซ Blocks transport of organic acids across renal tubular membranes, reducing their excretion.
- ๐ง Actively excreted in the proximal convoluted tubule, reabsorbed in the distal tubule.
- โฌ๏ธ Reduces uric acid reabsorption and โฌ๏ธ increases renal excretion of urate.
๐ฏ Indications
- ๐ฆถ Gout / Hyperuricaemia: increases uric acid clearance.
- ๐ Historically used to prolong penicillin levels in plasma.
- ๐ซ Misuse in sport: used to mask drug presence in urine analysis (banned in competitive athletics).
๐ Interactions
- โฌ๏ธ Increases blood concentrations of oseltamivir and some antivirals.
- ๐ซ Aspirin reduces the uricosuric effect and should be avoided.
- ๐ Can affect levels of some antibiotics and antivirals (consult BNF for full list).
โ ๏ธ Side Effects
- ๐คข Dyspepsia, GI upset.
- ๐ธ Allergic reactions (rash, pruritus).
- ๐งช Rare: nephrolithiasis, anaemia, or uric acid kidney stones with long-term use.
๐ Dose
- ๐ Start: Probenecid 250 mg BD PO.
- โฌ๏ธ Titrate according to serum urate levels.
- ๐ Usual maximum dose: 2 g/day.
- โ ๏ธ Ensure good hydration to reduce kidney stone risk.
๐ Teaching Points
- ๐ Not first-line for gout - now largely replaced by allopurinol and febuxostat.
- ๐ง Uricosuric effect requires good renal function; avoid in renal impairment.
- ๐ซ Contraindicated in patients with history of uric acid kidney stones.
- โ๏ธ Interesting historically: used in WWII to prolong scarce penicillin supplies.