Probenecid

Indications
 Oral
Hyperuricaemia with gout
Adult: 250 mg bid for 1 wk increased to 500 mg bid. Dose may be increased up to 2 g daily by increments of 500 mg every 4 wk if needed.
Oral
Adjunct to antibacterial therapy
Adult: 500 mg 4 times daily. As a single dose treatment of gonorrhoea: 1 g as a single dose is given together with an oral antibacterial, or 30 min before an injected antibacterial.
Child: >2 yr weighing <50 kg: Initially, 25 mg/kg (700 mg/m2) followed by 10 mg/kg (300 mg/m2) every 6 hr.
Contraindications
 Hypersensitivity, acute gout attack, history of uric acid nephrolithiasis, blood dyscrasias, childn <2 yr, as an antibacterial adjunct in patients with known renal impairment.
Warnings / Precautions
 Pregnancy and lactation; renal impairment, history of peptic ulcer, G6PD deficient individuals. Adequate fluid intake is recommended especially during the first few mth of treatment.
Adverse Reactions
 Seizures (overdosage), headache, anorexia; nausea, vomiting, urinary frequency, sore gums, dizziness, dermatitis, uric acid nephrolithiasis and pruritus.
Potentially Fatal: Hepatic necrosis, aplastic anaemia, anaphylaxis.
Drug Interactions
 Pyrazinamide and salicylates antagonize uricosuric effects of probenecid. May reduce clearance of methotrexate, ganciclovir and aciclovir. Probenecid may increase the plasma concentrations of penicillins or β-lactams.
Potentially Fatal: Reduced renal clearance of sulphonylurea antidiabetic and ketorolac.
See Below for More probenecid Drug Interactions
Lab Interactions
 Interferes with the determination of urinary 17-ketosteroids and may give false-positive with both Benedict test and Clinitest for urine-sugar.
Mechanism of Actions
 Probenecid increases excretion of uric acid by competitively blocking its reabsorption at the proximal convoluted tubule thus lowering serum uric acid levels and eventually reducing urate deposits in the tissues. It also causes plasma levels of weak organic acids (eg, penicillins and most cephalosporins) to increase by competitively inhibiting their renal tubular secretion.
Administration
 Should be taken with food. (Take w/ meals or antacids. Ensure adequate fluid intake.)
ATC Classification
 M04AB01 - probenecid ; Belongs to the class of preparations increasing uric acid excretion. Used in the treatment of gout.
Available As
  • Probenecid 125 mg
  • Probenecid 250 mg
  • Probenecid 500 mg

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