OBJECTIVE To investigate the activity of fleroxacin in acute uncomplicated infections with N. gonorrhoeae in comparison with conventional penicillin G plus probenecid treatment. DESIGN Multicentre open label randomised parallel group study. SUBJECTS Male patients aged 18 years or over from university departments of urology, epidemiology and dermatology and a clinic for sexually transmitted ...

OBJECTIVE Canagliflozin, a sodium-glucose co-transporter 2 inhibitor, approved for the treatment of type-2 diabetes mellitus (T2DM), is metabolized by uridine diphosphate-glucuronosyltransferases (UGT) 1A9 and UGT2B4, and is a substrate of P-glycoprotein (P-gp). Canagliflozin exposures may be affected by coadministration of drugs that induce (e.g., rifampin for UGT) or inhibit (e.g. probenecid ...

6β-Hydroxycortisol (6β-OHF) is a substrate of the organic anion transporter 3 (OAT3) and the multidrug and toxin extrusion proteins MATE1 and MATE-2K in the corresponding cDNA-transfected cells. This study aimed to examine the contribution of OAT3 and MATEs to the urinary excretion of 6β-OHF in humans using the appropriate in vivo inhibitors, probenecid and pyrimethamine, for OAT3 and MATEs, re...

The site where furosemide is metabolized and the location where probenecid reduces furosemide metabolism remain poorly defined. The liver appears to play a minor role, and there is indirect evidence suggesting that the kidneys could be responsible for the metabolism of furosemide. To assess the role of the kidneys in the metabolism of furosemide, its intravenous kinetics have been studied in co...

Delivery of valproic acid (VPA) to the human brain is relatively inefficient as reflected by a low brain-to-unbound plasma concentration ratio (< or =0.5) at steady state. Previous pharmacokinetic studies suggested that the unfavorable brain-to-plasma gradient is maintained by coupled efflux transport processes at both the brain parenchymal cells and blood-brain barrier (BBB); one or both of th...

Probenecid is an orally bioavailable, uricosuric agent that was first approved in 1951 for the treatment of gout, but later found to have potent, broad-spectrum antiviral activity against several respiratory viruses including SARS-CoV-2. We conducted a phase 2 randomized, placebo-controlled, single-blind, dose-range finding study non-hospitalized patients with symptomatic, mild-to-moderate COVI...

There is no proven alternative to penicillin for treatment of maternal syphilis. We report 2 case-patients with maternal syphilis who were successfully treated without penicillin. We used amoxicillin and probenecid for the first case-patient and amoxicillin, probenecid, and ceftriaxone for the second case-patient.

several transporters appear to be important in transporting various drugs. many patients, who receive morphine as analgesic medication, also receive other medications with potency of changing morphine transport by affecting p-glycoprotein (p-gp) and oatp2 transport system. this could influence morphine pharmacokinetics and pharmacodynamics. the aim of present study was to elucidate the transpor...

The effects of pyrazinamide, probenecid, and benzbromarone on renal excretion of oxypurinol were investigated. Pyrazinamide decreased the mean (SEM) fractional clearance of oxypurinol from 19.2 (2.1) to 8.8 (1.5). Probenecid increased the fractional clearance of oxypurinol from 14.1 (3.5) to 24.8 (4.1). Benzbromarone increased the fractional clearance of oxypurinol from 15.6 (2.3) to 33.8 (2.8)...

Two oral 0.5-g doses of probenecid given 7 and 1 h before a single 1-g intramuscular dose of cefamandole resulted in higher serum levels of cefamandole than when cefamandole was given alone: 37 versus 20 mug per ml of serum, respectively. Cefamandole was not measurable (<0.3 mug/ml) at 8 h when it was given alone, whereas an average 8-h value of 2.9 mug/ml was obtained after pretreatment with p...