Resistance to drugs can result from changes in drug transport, and this resistance can sometimes be overcome by a second drug that modifies the transport mechanisms of the cell. This strategy has been exploited to partly reverse resistance to chloroquine in Plasmodium falciparum. Studies with human tumor cells have shown that probenecid can reverse resistance to the antifolate methotrexate, but...

This is a report on a clinical trial in which cefuroxime was used for treating 110 men with uncomplicated urethral gonorrhoea. Twenty-three men were given 1 g cefuroxime intramuscularly and 1 g probenecid orally, and 87 were treated with 1.5 g cefuroxime intramuscularly with 1 g probenecid orally. All 18 patients treated with 1 g cefuroxime and 1 g probenecid and seen at least once after treatm...

Two hundred and ten men suffering from uncomplicated gonococcal urethritis were treated with one of two treatment schedules. Of 109 patients treated with 3 g ampicillin and 2 g probenecid (group A) there were two recurrences in the first week after treatment and none in the second week. Of 101 patients treated with 1.5 g talampicillin and 2 g probenecid (group B), there were three recurrences i...

81 patients have been treated with single oral doses of 1-5 g. (6 tablets) of talampicillin without probenecid. The failure rate amongst those followed was only 4-2 per cent. No side-effects were reported. These results were superior to those obtained with 2-0g. or equivalent of ampicillin, amoxycillin, or pivampicillin with probenecid. Talampicillin is thus the most potent ampicillin-like anti...

Life-threatening drug interactions are known to occur between methotrexate and nonsteroidal anti-inflammatory drugs (NSAIDs), probenecid, and penicillin G. The purpose of this study was to characterize methotrexate transport, as well as to determine the site and the mechanism of drug interactions in the proximal tubule. Mouse proximal tubule cells stably expressing basolateral human organic ani...

In 1944, when gonorrhoea responded to 100,000 units of crystalline penicillin given in divided doses, Miller, Scott, and Moeller (1944) observed that the gonococcus was cleared from the urethral secretions within 1 to 6 hours. 23 years later, Holmes, Johnson, and Floyd (1967), in the Far East, noted that only one case, a therapeutic failure, out of twenty treated with 2-4 m.u. procaine penicill...

AIMS Soils at a commercial facility had become contaminated with the pharmaceutical chemical residues, Probenecid and Methaqualone, and required remediation. METHODS AND RESULTS Soil composting was investigated as an alternative to incineration for treatment. In laboratory trials, a factorial experimental design was used to evaluate organic matter amendment type and concentration, and incubat...

This study was designed to establish a strategy to predict drug interactions involving biliary excretion. The interaction between methotrexate and probenecid was examined as an interaction model since this interaction has already been clinically reported. Coadministration of probenecid reduced the biliary clearance of methotrexate in a dose-dependent manner in rats. This inhibition by probeneci...

PURPOSE To investigate the effects of probenecid and cimetidine on the pharmacokinetics of nemonoxacin in humans. METHODS Two independent, open-label, randomized, crossover studies were conducted in 24 (12 per study) healthy Chinese volunteers. In Study 1, each volunteer received a single oral dose of 500 mg of nemonoxacin alone or with 1.5 g of probenecid divided into three doses within 25 h...