Products
Probenecid is commercially available in tablet form (Santuril). Santuril has been approved in many countries since 2005.
Structure and properties
Probenecid (C13H19NO4S, Mr = 285.4 g/mol) is a white crystalline powder that is practically insoluble in water.
Effects
Probenecid (ATC M04AB01) inhibits tubular reabsorption of uric acid and secretion of organic anions. It thus promotes renal excretion of uric acid. The effects are due in part to inhibition of the transporter URAT1, which is partly responsible for the reabsorption of uric acid.
Indications
Probenecid is approved for the treatment of gout (symptomatic hyperuricemia) as a 2nd-line agent.
Contraindications
- Hypersensitivity
- Impaired kidney function
- Renal stone diathesis
- Children under 2 years
- Probenecid should not be used during an acute attack of gout.
For complete precautions, see the drug label.
Interactions
Probenecid is an organic anion and thus can lead to numerous desirable or undesirable drug interactions with other organic anions by inhibiting their secretion at the kidney and increasing concentrations. Probenecid was developed during World War 2 to “stretch” the organic anion penicillin (pharmacokinetic booster). However, it came on the market too late to be actually used. Because the active metabolite of oseltamivir (Tamiflu) is also an organic anion and its availability is increased by inhibition of excretion when given concomitantly with probenecid, it has been discussed that probenecid could be used to “stretch” Tamiflu in pandemic influenza (see under the article Swine Flu). Cidofovir must be mandatorily co-administered with probenecid. This may reduce the nephrotoxicity of cidofovir.
Adverse effects
The most common potential adverse effects include skin reactions, hair loss, pruritus, gingivitis, poor appetite, headache, drowsiness, and digestive symptoms such as nausea and bloating.
