Probenecid has been shown to delay the plasma clearance of methotrexate in the rat and to reduce both hepatic and renal excretion of methotrexate in this animal model. In order to probe the mechanism by which probenecid alters hepatic excretion of the antifolate, studies assessed the effects of probenecid on transport, accumulation, distribution, and release of methotrex ate in the rat hepatocy...

In a study of eight, healthy adult volunteers given 3 g amoxycillin with or without 1g probenecid, significantly higher peak plasma levels of amoxycilin were recorded in the presence (34.96 microgram/ml) of probenecid than in its absence (22.72 microgram/ml). When plasma levels were plotted against time the mean area under the curve was significantly greater for subjects given probenecid than f...

Our earlier studies showed that both carrier-mediated influx and efflux of [3H]methotrexate in murine tumor cells was in hibited by probenecid. The concentration of probenecid re quired for inhibition of influx was 10-fold greater than that required to inhibit efflux. As a consequence, the intracellular exchangeable level of [3H]methotrexate at steady state was markedly increased. Since these e...

HART, LARRY G., ANTHONY M. GUARINO, AND RICHARD H, ADAMSON. Effects of phenobarbital on biliary excretion of organic acids 2*lz male and female rats. Am. J. Physiol. 2 17( 1) : 46-52. 1969.-The effects of phenobarbital pretreatment on the biliary excretion of four organic anions, indocyanine green (ICG), chlorothiazide (CTZ), phenol red, and probenecid, were investigated. Indocyanine green and ...

In this study, we were concerned with the effect of probenecid on the pharmacokinetics of 1,000 mg of cefmenoxime administered over a 30-min period by intravenous infusion. Each of a total of 10 subjects received cefmenoxime twice, once with and once without adjunctive probenecid. The data were fit by iterative nonlinear regression procedures to a two-compartment open pharmacokinetic model, wit...

Longer serum half-lives of perfluoroalkyl substances (PFAS) in humans compared to other species has been attributed differences the activity organic anion transporters (OAT). Among 56,175 adult participants community-based C8 Health Project, 23 subjects were taking uricosuric OAT-inhibitor probenecid, and 36 bile acid sequestrant cholestyramine. In regression models log transformed PFAS, medica...

BACKGROUND Transient receptor potential vanilloid 2 is a calcium channel activated by probenecid. Probenecid is a Food and Drug Administration-approved uricosuric drug that has recently been shown to induce positive lusitropic and inotropic effects in animal models through cardiomyocyte transient receptor potential vanilloid 2 activation. The aim of this study was to test the hypothesis that or...

The effects of probenecid and cimetidine on the pharmacokinetics of valaciclovir and its metabolite acyclovir have been investigated. Twelve healthy male volunteers participated in this open single-dose study with a four-way-crossover randomized and balanced design. At the first of four administrations, volunteers in four groups received 1 g of valaciclovir alone, valaciclovir with 1 g of probe...

The renal handling of fleroxacin was studied by renal clearance and stop-flow techniques in rabbits and dogs and by analyzing the pharmacokinetics with and without probenecid in humans. In rabbits the excretion ratios (fleroxacin intrinsic renal clearance/glomerular filtration rate) were greater than unity (2.01) without probenecid and were decreased to a value below unity (0.680) with probenec...