Gastrointestinal tolerance of probenecid may be improved with food ingestion or an antiemetic prior to administration. Antihistamines or acetaminophen may be used for probenecid hypersensitivity reactions. CSF levels are undetectable. The elimination half-life of the active intracellular metabolite is 17 to 65 hours, permitting long intervals between doses. The major side effect is dose-dependent nephrotoxicity.
Proteinuria is an early indicator.
IV saline and probenecid must be used to reduce nephrotoxicity. Monitor renal function with serum creatinine and urine protein within 48 hours prior to each dose. Side effects usually resolved within 12 hours. Dose-limiting side effects are usually GI intolerance. Category C-use only if potential benefit justifies the risk.