Probenecid


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Hyperuricaemia w/ gout 250 mg bid for 1 wk, then 500 mg bid thereafter. Up to 2 g/day may be given if needed. Adjunct to antibacterial therapy 500 mg 4 times/day.
Dosage Details
Oral
Hyperuricaemia with gout
Adult: 250 mg bid for 1 wk, followed by 500 mg bid thereafter. Further increases of up to 2 g daily by increments of 500 mg every 4 wk may be given if needed.

Oral
Adjunct to antibacterial therapy
Adult: 500 mg 4 times daily. Treatment of uncomplicated gonorrhoea: 1 g as a single dose together w/ an oral antibacterial, or 30 min before an injected antibacterial.
Child: ≥2 yr ≤50 kg: Initially, 25 mg/kg (700 mg/m2) followed by 40 mg/kg (1,200 mg/m2) in 4 divided doses.
Renal Impairment
Hyperuricaemia with gout:
CrCl (mL/min) Dosage
<30 Avoid use.
Adjunct to antibacterial therapy: Contraindicated.
Administration
Should be taken with food. Take w/ meals or antacids. Ensure adequate fluid intake.
Contraindications
History of uric acid renal calculi or blood disorders; gout patients w/ severe renal impairment. Antibacterial adjunct in patients w/ renal impairment. Childn <2 yr. Concomitant use w/ salicylates.
Special Precautions
Patient w/ history of peptic ulcer. Pregnancy and lactation.
Adverse Reactions
Nausea, vomiting, anorexia, headache, sore gums, flushing, alopecia, dizziness, anaemia, urinary frequency; hypersensitivity reactions w/ fever, dermatitis, pruritus, urticaria; leucopenia, hepatic necrosis, nephrotic syndrome, aplastic anaemia, haemolytic anaemia; precipitation of acute gout.
Potentially Fatal: Severe hypersensitivity reactions (e.g. Stevens-Johnson syndrome) and anaphylaxis.
Patient Counseling Information
Maintain adequate fluid intake (2-3 L/day).
MonitoringParameters
Monitor uric acid, renal function, CBC.
Overdosage
Symptoms: CNS stimulation, convulsions, resp failure. Management: Symptomatic and supportive treatment along w/ gastric lavage. IV short-acting barbiturates may be given.
Drug Interactions
May potentiate methotrexate toxicity. May increase peak plasma concentrations of paracetamol, naproxen, indometacin, ketoprofen, meclofenamate, lorazepam, rifampicin, aciclovir, ganciclovir and zidovudine. May decrease the renal excretion of conjugated sulfonamides. May prolong or enhance the action of oral sulfonylureas thereby increasing the risk of hypoglycaemia. Pyrazinamide may antagonise the uricosuric action of probenecid.
Potentially Fatal: Salicylates antagonise the uricosuric action of probenecid.
Lab Interference
May give false positive results w/ some tests for glucose in the urine. Reduces the excretion of some iodinated contrast media and may interfere w/ laboratory tests by decreasing the excretion of aminohippuric acid, phenolsulfonphthalein, and sulfobromophthalein.
Action
Description: Probenecid competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby promoting its excretion and reducing serum uric acid levels. It increases plasma levels of weak organic acids (e.g. penicillins, cephalosporins, or other β-lactam antibiotics) by competitively inhibiting their renal tubular secretion.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the GI tract. Time to peak plasma concentration: 2-4 hr.
Distribution: Crosses the placenta; concentrations in the CSF are approx 2% of plasma concentrations. Plasma protein binding: 85-95%.
Metabolism: Slowly metabolised by the liver to probenecid monoacyl glucuronide, 2 monohydroxylated compounds, a carboxylated metabolite and an N-depropylated compound.
Excretion: Via urine, mainly as metabolites. Plasma half-life: <5 to >8 hr.
Chemical Structure

Chemical Structure Image
Probenecid

Source: National Center for Biotechnology Information. PubChem Database. Probenecid, CID=4911, https://pubchem.ncbi.nlm.nih.gov/compound/Probenecid (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
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 Tablets data sheet November 2009. Medsafe. http://www.medsafe.govt.nz/. Accessed 02/02/2015.

Anon. Probenecid. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/02/2015.

Buckingham R (ed). Probenecid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/01/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Probenecid. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 02/02/2015.

Probenecid Tablet, Film Coated (Aphena Pharma Solutions-Tennessee, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 02/02/2015.

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