Adult: As treatment of hyperuricaemia associated with gout or gouty arthritis: 250 mg bid for 1 week, followed by 500 mg bid thereafter. May increase daily dose in increments of 500 mg every 4 weeks based on tolerance if symptoms are not controlled. Usual maintenance dose: Up to 2,000 mg daily.
Oral Adjunct to antibacterial therapy
Adult: As an adjunct to certain β-lactams for the elevation and prolongation of plasma levels: 2,000 mg daily in divided doses. Child: As an adjunct to certain β-lactams for the elevation and prolongation of plasma levels: ≥2 years ≤50 kg: Initially, 25 mg/kg or 700 mg/m2 as a single dose, followed by 40 mg/kg daily or 1,200 mg/m2 daily in 4 divided doses; >50 kg: Same as adult dose. Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Renal Impairment
Hyperuricaemia with gout:
eGFR <30 mL/min/1.73m2: Not recommended.
Administration
Should be taken with food. Take w/ meals or antacids. Ensure adequate fluid intake.
Contraindications
Blood dyscrasias, uric acid kidney stones; initiation during an acute gout attack. Children <2 years. Concomitant use with salicylates.
Special Precautions
Patient with peptic ulcer disease. Renal impairment. Children ≥2 years. Pregnancy and lactation.
Adverse Reactions
Significant: Severe hypersensitivity reactions (including anaphylaxis), exacerbation of acute gouty attack. Gastrointestinal disorders: Nausea, vomiting, gingival pain. General disorders and administration site conditions: Fever. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: Urinary frequency, nephrolithiasis. Skin and subcutaneous tissue disorders: Pruritus, urticaria, dermatitis, alopecia. Vascular disorders: Flushing.
Patient Counseling Information
Maintain adequate fluid intake.
Monitoring Parameters
Monitor CBC, kidney function and serum uric acid.
Overdosage
Symptoms: Gastric intolerance, CNS stimulation with convulsions, respiratory failure. Management: Symptomatic and supportive treatment. Induce emesis or perform gastric lavage for severe cases. May administer parenteral short-acting barbiturates for signs of CNS excitation.
Drug Interactions
Concurrent use with salicylates (e.g. aspirin) or pyrazinamide diminishes the therapeutic effect of probenecid. Increases serum concentrations of methotrexate, certain antibiotics (e.g. dapsone, penicillins, rifampicin), lorazepam, indometacin, ketoprofen, naproxen and paracetamol. Increased risk of hypoglycaemia with oral sulfonylureas. May enhance the adverse effects of thiopental Na.
Lab Interference
May cause false-positive glucosuria with Clinitest®.
Action
Description: Mechanism of Action: Probenecid, a sulfonamide derivative, is a uricosuric and renal tubular blocking agent. It competitively inhibits uric acid reabsorption at the proximal convoluted tubule, thus promoting its urinary excretion and decreasing serum uric acid levels. Additionally, it increases plasma levels of weak organic acids (e.g. cephalosporins, penicillins or other β-lactam antibiotics) by competitively inhibiting their renal tubular secretion. Pharmacokinetics: Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 2-4 hours. Distribution: Crosses the placenta. Plasma protein binding: 85-95%. Metabolism: Slowly metabolised in the liver into probenecid monoacyl glucuronide, 2 monohydroxylated compounds, a carboxylated metabolite, and an N-depropylated compound. Excretion: Via urine (mainly as metabolites). Elimination half-life: Approx 6-12 hours.
Chemical Structure
Probenecid Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4911, Probenecid. https://pubchem.ncbi.nlm.nih.gov/compound/Probenecid. Accessed May 28, 2024.
M04AB01 - probenecid ; Belongs to the class of preparations increasing uric acid excretion. Used in the treatment of gout.
References
AFT Pharmaceuticals Ltd. Probenecid-AFT 500 mg Film Coated Tablets data sheet September 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 06/05/2024.Anon. Probenecid. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/05/2024.Buckingham R (ed). Probenecid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/05/2024.Probenecid Tablet, Film Coated (Marlex Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/05/2024.Probenecid. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/05/2024.SW Probenecid Tablet 500 mg (Sunward Pharmaceutical Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 06/05/2024.
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