Probenecid is a uricosuric and renal tubular transport blocking agent.
Probenecid tablets are indicated for the treatment of the hyperuricemia associated with gout and gouty arthritis.
As an adjuvant to therapy with penicillin or with ampicillin, methicillin, oxacillin, cloxacillin, or nafcillin, for elevation and prolongation of plasma levels by whatever route the antibiotic is given.
Published Studies Related to Probenecid
Pharmacokinetic properties and bioequivalence of two compound formulations of 1500 mg ampicillin (1167 mg)/probenecid (333 mg): a randomized-sequence, single-dose, open-label, two-period crossover study in healthy Chinese male volunteers. [2010.03]
BACKGROUND: Ampicillin/probenecid is an antimicrobial formulation indicated for the treatment of respiratory, urinary tract, and gastrointestinal infections. Ampicillin sodium is the active antimicrobial ingredient that can act on the phase of bacterial breeding and inhibit the biosynthesis of bacterial mucopeptide in the cell wall. Probenecid acts synergistically by competitively inhibiting an organic anion transporter in renal tubules, increasing the plasma concentrations, and thus extending the plasma elimination t(1/2). OBJECTIVE: The aim of this study was to assess and compare the pharmacokinetic (PK) properties, bioavailability, and bioequivalence of a newly developed dispersible tablet formulation (test) of ampicillin/ probenecid with those of an established branded capsule formulation (reference) in healthy Chinese male volunteers... CONCLUSIONS: In this small study in healthy Chinese male volunteers, a single 1500-mg dose of the dispersible tablet formulation (test) of ampicillin/probenecid met the SFDA's regulatory criteria for bioequivalence to the reference capsule formulation based on the rate and extent of absorption. Both formulations were well tolerated. Copyright 2010 Excerpta Medica Inc. All rights reserved.
Efficacy and tolerability of urate-lowering drugs in gout: a randomised controlled trial of benzbromarone versus probenecid after failure of allopurinol. [2009.01]
OBJECTIVES: To investigate the efficacy and tolerability of allopurinol as the first-choice antihyperuricaemic treatment for gout, and compare the efficacy and tolerability of benzbromarone and probenecid as second-choice treatment... CONCLUSION: This study showed that allopurinol 300 mg/day has a poor efficacy and tolerability profile when used to attain a biochemical predefined target level of sUr < or =0.30 mmol/l, following 2 months of treatment. In stage 2, benzbromarone 200 mg/day was more effective and better tolerated than probenecid 2 g/day.
Pharmacokinetics and tolerability of oseltamivir combined with probenecid. [2008.09]
Oseltamivir is an inhibitor of influenza virus neuraminidase, which is approved for use for the treatment and prophylaxis of influenza A and B virus infections.Alternate-day dosing of oseltamivir plus dosing with probenecid four times daily achieved trough oseltamivir carboxylate concentrations adequate for neuraminidase inhibition in vitro, and this combination should be studied further.
Reduction in non-glomerular renal clearance of the caffeine metabolite 1-methylxanthine by probenecid. [2007.08]
OBJECTIVE: Urinary caffeine metabolic ratios used to quantify the activity of numerous drug-metabolizing enzymes are an established component of cocktail approaches for metabolic phenotyping. Because in vitro evidence suggests that 1-methylxanthine (1-MX), a major caffeine metabolite, is actively secreted into urine by organic anion transporters (hOATs), coadministration of renal hOAT inhibitors like probenecid may impair these procedures... CONCLUSIONS: 1-MX undergoes renal tubular secretion which is substantially reduced by probenecid, possibly due to inhibition of renal hOATs. This inhibition may explain the influence of probenecid on urinary caffeine metabolic ratios and, thus, its impact on the assessment of enzyme activities. It also suggests that 1-MX might serve as a model substrate for the renal tubular transport of organic anions.
Effect of probenecid on the pharmacokinetics of carbamazepine in healthy subjects. [2005.06]
OBJECTIVES: Carbamazepine (CBZ) undergoes biotransformation by CYP3A4 and CYP2C8, and glucuronide conjugation. There has been no clear demonstration to reveal the role of glucuronidation in the disposition of CBZ. We evaluated the effect of probenecid, a UDP-glucuronosyltransferase inhibitor, on the pharmacokinetics of CBZ in humans... CONCLUSION: Although probenecid showed a minimal effect on the glucuronidation of CBZ and CBZ-E, it increased CBZ biotransformation to CBZ-E, most likely reflecting the induction of CYP3A4 and CYP2C8 activities, in humans. These results demonstrate that glucuronide conjugation plays a minor role in the metabolism of CBZ and CBZ-E in humans, and that probenecid has an inducing effect on the disposition of CBZ.
Clinical Trials Related to Probenecid
Comparison of Intravenous Cefazolin Plus Oral Probenecid With Oral Cephalexin for the Treatment of Cellulitis [Completed]
The purpose of this study is to determine whether oral cephalexin is equivalent to
intravenous cefazolin plus oral probenecid for the treatment of uncomplicated skin and soft
tissue infections in patients that present to the emergency department.
A Study to Assess the Effects of Multiple-Dose Probenecid on the Multiple-Dose Pharmacokinetics of Canagliflozin in Healthy Volunteers [Completed]
The purpose of this study is to assess the effects of multiple doses of probenecid on the
multiple-dose pharmacokinetics of canagliflozin and its metabolites in healthy volunteers.
Safety and tolerability will also be assessed.
Repurposing Probenecid as a Positive Inotrope for the Treatment of Heart Failure [Recruiting]
Probenecid is an FDA approved drug for the treatment gout and hyperuricemia. It has been
used safely in humans for decades for this and other indications. The investigators have
recently discovered that this drug can also stimulate other receptors in the heart and
therefore improve its function. The hypothesis of this study is that probenecid can be used
to improve the function of the heart and therefore the symptoms in patients with heart
Drug-interaction Trial in Healthy Subjects With Oral Administration of Empagliflozin (BI 10773), Rifampicin and Probenecid [Completed]
Effect of Probenecid on Synovial Fluid ATP Levels in CPPD [Recruiting]
This study will investigate the hypothesis that probenecid, a medication currently used for
gout, reduces levels of ATP in the joint fluid of patients with calcium pyrophosphate
deposition disease (CPPD), another common type of crystal-related arthritis. There is
good evidence that CPPD results from an excess of ATP in joints. We will measure levels of
ATP in joint fluid before and after 5 days of treatment with probenecid. This study will
serve to rationalize larger studies of probenecid in CPPD.
Reports of Suspected Probenecid Side Effects
Myelodysplastic Syndrome (4),
Therapeutic Response Decreased (4),
Blood Creatinine Increased (1),
Decreased Appetite (1),
Nausea (1), more >>
Page last updated: 2010-10-05