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PubMed1989

Clinical comparison of single-oral-dose cefuroxime axetil and amoxicillin with probenecid for uncomplicated gonococcal infections in women.

Four hundred sixty-six female patients were enrolled in a randomized study that compared the clinical efficacies of single oral doses of cefuroxime axetil and amoxicillin with probenecid in the treatment of uncomplicated gonorrhea. Two hundred ninety-five patients had culture-positive gonococcal infections and completed the investigation. Cure rates for the patients treated with cefuroxime axetil and those treated with amoxicillin with probenecid were high (greater than 95%) for genitorectal infections. Pharyngeal infections, however, were not uniformly eradicated by either cefuroxime axetil (60%) or amoxicillin with probenecid (64%). Approximately 13% of each patient group suffered adverse events, which were gastrointestinal in the majority and were transient. Compared with amoxicillin plus probenecid, cefuroxime axetil in a single oral dose was an equally safe and effective drug for the treatment of uncomplicated gonorrhea in women caused by penicillin-susceptible strains.

Adolescent↗
PubMed1974

Comparative therapeutic and pharmacological evaluation of amoxicillin and ampicillin plus probenecid for the treatment of gonorrhea.

Single doses of 3.5 g of ampicillin with 1.0 g of probenecid or of 3.0 g of amoxicillin alone were administered orally to 58 males and 56 females with uncomplicated gonococcal infection. The failure rate for genital or anal infection, or both, was 1.7% for ampicillin plus probenecid and 4.2% for amoxicillin alone. However, patients with oropharyngeal infection responded poorly. Seventy-five isolates of Neisseria gonorrhoeae recovered from patients in this study were all inhibited by 1.0 mug or less of ampicillin or amoxicillin per ml; penicillin G, ampicillin, and amoxicillin had similar activity in vitro against these isolates. Serum concentrations of amoxicillin in 10 volunteers remained above the minimal inhibitory concentration for most strains of N. gonorrhoeae for periods up to 10 h after a 3.0-g oral dose. After 2.0 g of ampicillin was given with probenecid, the serum levels during the 5- to 12-h period approached those achieved with 3.5 g of ampicillin plus probenecid, and actually exceeded levels attained during the same interval with 3.0 g of amoxicillin administered alone.

Amines↗
PubMed1986

Three regimens of procaine penicillin G, Augmentin, and probenecid compared for treating acute gonorrhoea in men.

The efficacy of three penicillin regimens in treating uncomplicated gonorrhoea in men was evaluated. The regimens consisted of: Augmentin 3.25 g plus probenecid 1 g orally: aqueous procaine penicillin G 4.5 MIU intramuscularly and probenecid 1 g plus one tablet of Augmentin 375 mg orally; or aqueous procaine penicillin G 4.5 MIU intramuscularly and probenecid 1 g plus two tablets of Augmentin 375 mg orally. Cure rates for infections caused by penicillinase (beta lactamase) producing Neisseria gonorrhoeae (PPNG) were 87% (20/23) for regimen 1, 97% (28/29) for regimen 2, and 95% (19/20) for regimen 3. Thus the addition of one or two tablets of Augmentin 375 mg to aqueous procaine penicillin G and probenecid cured 96% (47/49) of infections caused by PPNG strains. All three regimens were 100% effective in eradicating infections caused by non-PPNG strains. Post gonococcal urethritis occurred in 24% of cases treated with regimen 1, 14% of cases treated with regimen 2, and 15% of cases treated with regimen 3. The geometric minimum inhibitory concentrations (MIC90) of Augmentin for 72 PPNG and 162 non-PPNG isolates of N gonorrhoeae obtained before treatment were 1.98 and 0.55 mg/l, respectively. Regimen 2, besides being effective against infections caused by PPNG or non-PPNG strains, has the advantage of cost effectiveness and low toxicity. This regimen may be useful in treating gonorrhoea in areas of high prevalence of PPNG strains, such as South East Asia and Africa.

Acute Disease↗
PubMed1979

Effects of intraluminal D-glucose and probenecid on urate absorption in the rat proximal tubule.

The in vivo microperfusion technique was employed to examine urate absorption in the proximal convoluted tubule of the rat kidney using [2-14C]urate as the marker for fractional urate absorption. With NaCl as the perfusion solution, water absorption averaged 2.53 +/- 0.16 nl.min-1.mm tubule-1, and the fractional absorption of [2-14C]urate averages 11.6 +/- 1.0%/mm tubule. The addition of D-glucose (50 mg/100 ml) enhanced water absorption to 3.62 +/- 0.19 nl.min-1.mm tubule-1, but inhibited fractional urate absorption to 6.6 +/- 1.2%/mm tubule. Phloridzin (4.4 mg/100 ml), 2-deoxy-D-glucose (45.6 mg/100 ml), and 3-O-methyl-D-glucose (53.9 mg/100 ml) also inhibited the absorption of [2-14C]urate to the same degree as did D-glucose despite differing effects on water absorption. The addition of probenecid (2.8 mg/100 ml) to the NaCl perfusion solution had no effect on water absorption but inhibited [2-14C]urate absorption to 6.4 +/- 0.6%/mm tubule. The addition of both probenecid and phloridzin further reduced [2-14C-A1urate absorption to 3.8 +/- 0.7%/mm tubule. Probenecid alone had no effect on glucose transport. These studies suggest that the presence of either certain hexose sugars, phloridzin, or probenecid in the lumen of the proximal convoluted tubule inhibits the tubular absorption of urate.

Absorption↗
PubMed1981

Dose-dependent kinetics of probenecid in rhesus monkeys-intravenous bolus studies.

14 bolus studies with probenecid in a dose range of 8.2--164 mg/kg were carried out in 3 monkeys. The protein binding of probenecid in the plasma was studied by an ultracentrifugation method. Plasma clearances of both total and unbound probenecid decreased with increasing doses, while the volume of distribution and fraction of metabolites excreted in the urine remained constant. The urinary excretion rates of probenecid and it metabolites were measured in a bladder-catheterized monkey and were found to be urine flow dependent. Since the rate-limiting step for the excretion of the metabolites did not depend on the formation rate only, biliary recycling was speculated.

Animals↗
PubMed1981

Benzbromarone therapy in hyperuricaemia; comparison with allopurinol and probenecid.

The purpose of this study was to compare the serum uric acid lowering effect of benzbromarone (Minuric), allopurinol, probenecid and placebo in patients suffering from confirmed hyperuricaemia. This was a multiple dose, placebo-controlled, crossover study in six hyperuricaemic patients to compare the effects on uric acid of three different active treatments: benzbromarone 100 mg daily, probenecid 1000 mg daily and allopurinol 300 mg daily. Each patient was assessed clinically and biochemically before and after the study and blood samples for serum uric acid determinations were taken thirteen times during the study period. For the six trialists it was found that benzbromarone is superior to both probenecid and allopurinol in the lowering of serum uric acid, and that probenecid is also superior to allopurinol.

Adult↗
PubMed1983

Effect of probenecid on the pharmacokinetics of aminophylline.

The authors investigated the effect of probenecid on the pharmacokinetics of aminophylline. Seven normal volunteers served as their own controls in a crossover study. In the first phase, subjects received an oral dose of aminophylline after an overnight fast. In the second phase, probenecid was given orally 30 minutes prior to the administration of aminophylline. Serum and urine theophylline levels were determined by high performance liquid chromatography. Statistical analysis showed that probenecid had no significant effect on any of the pharmacokinetic parameters measured. Probenecid appears to have little or no influence on the liver metabolism of theophylline.

Aminophylline↗
PubMed2003

Effect of chronic probenecid therapy on cefazolin serum concentrations.

OBJECTIVE: To prospectively assess the effectiveness of probenecid at maintaining therapeutic serum concentrations of cefazolin at steady-state by comparing cefazolin serum concentrations produced by intravenous cefazolin 2000 mg every 8 hours with concentrations produced by once-daily administration of intravenous cefazolin 2000 mg plus oral probenecid 500 mg 4 times daily. METHODS: Patients in this prospective, nonrandomized, unblinded study were identified after an order was written for intravenous cefazolin 2000 mg every 8 hours or once daily plus oral probenecid 500 mg 4 times daily in the emergency department. For both study arms, a peak cefazolin serum concentration was obtained 1 hour after the infusion was started and 23 hours later, prior to the next scheduled dose. Doses of cefazolin for days 2-4 were then administered as ordered. On day 5, peak and trough serum concentrations were drawn 1 hour after the infusion started and 23 hours later, respectively. RESULTS: A total of 26 patients were prospectively assessed from April 2000 to October 2001. In patients who received cefazolin once daily, the average serum peak and trough concentrations on day 1 were 146.53 and 2.02 mg/L, respectively. Peak and trough concentrations on day 5 were 148.30 and 2.67 mg/L, respectively. In patients who received cefazolin every 8 hours, peak and trough concentrations were 122.15 and 18.65 mg/L on day 1 and, on day 5, 136.51 and 16.98 mg/L, respectively. CONCLUSIONS: Probenecid 500 mg given orally 4 times daily was effective in maintaining therapeutic serum concentrations of cefazolin at steady-state when given with intravenous cefazolin 2000 mg once daily.

Administration, Oral↗
PubMed2001

Treatment of calcinosis in juvenile dermatomyositis with probenecid: the role of phosphorus metabolism in the development of calcifications.

OBJECTIVE: To report the efficacy of probenecid for calcinosis of juvenile dermatomyositis (JDM) and assess the changes in phosphorus metabolism during treatment. METHODS: Biochemical studies of calcium and phosphorus metabolism were performed in a 9-year-old girl with JDM and extensive calcifications before and during probenecid treatment. RESULTS: The calcifications resolved over 18 months of treatment. Probenecid was found to be effective in reducing calcifications by increasing renal phosphate clearance. CONCLUSIONS: The tendency for calcifications in some patients with JDM might be related to an increase in renal phosphate reclamation, and therefore, probenecid treatment may be effective in these patients.

Calcinosis↗
PubMed1991

Influence of probenecid on P-amino hippurate kinetics.

The influence of probenecid on p-amino hippurate (PAH) kinetics was investigated in rat. Probenecid was administered i.p. (25, 50, 100, 150 and 200 mg/kg) two hours before PAH administration (25 mg/kg i.v.). The distribution and the rate of elimination of PAH was influenced by probenecid co-administration: the distribution decreased after probenecid doses higher than 150 mg/kg and the rate of elimination decreased after doses higher than 50 mg/kg.

Animals↗
PubMed1990

Pharmacokinetic and pharmacodynamic actions of enalapril in humans: effect of probenecid pretreatment.

The pharmacokinetic and pharmacodynamic profiles of oral enalapril (20 mg), in absence and in presence of probenecid pretreatment (1 g twice daily for 5 days), were investigated in 12 healthy volunteers on normal salt intake (150 mmol/24 hr). Mean peak serum concentration of enalapril rose from 158 +/- 7 to 216 +/- 1 ng/ml (P less than .01), whereas that of its metabolite, enalaprilat, rose from 62 +/- 6 to 84 +/- 8 ng/ml (P less than .01) in the presence of probenecid pretreatment. Area under the curve of both enalapril and enalaprilat increased by 50% (P less than .001), which was accompanied by a reduction in renal excretion of both compounds. The renal clearance of enalapril decreased from 229 +/- 19 to 61 +/- 4 ml/min (P less than .001) and that of enalaprilat from 108 +/- 4 to 66 +/- 2 ml/min (P less than .001). The total drug recovery fell from 48 +/- 3 to 38 +/- 2% (P less than .01) of the administered dose with no accompanying changes in plasma elimination half-lives of the parent drug or metabolite. The pharmacodynamic response of enalapril such as fractional excretions of sodium, calcium, magnesium and urate were enhanced by probenecid pretreatment. Absolute urinary excretion of sodium increased from 51 +/- 5 to 91 +/- 8 mmol/6 hr (P less than .001) after enalapril and from 55 +/- 4 to 113 +/- 13 mmol/6 hr (P less than .01) after enalapril in presence of probenecid pretreatment, despite a significant decrease in the renal excretion of enalapril and enalaprilat over the same interval.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1989

Pharmacokinetics of ceftazidime given alone and combination with probenecid to unweaned calves.

Ceftazidime pharmacokinetic values were studied in unweaned calves given the antibiotic alone or in combination with probenecid. Ceftazidime was administered IV to 9 calves at a dosage of 10 mg/kg of body weight and IM (10 mg/kg) to 8 calves, to 7 calves (10 mg/kg plus probenecid [40 mg/kg]), and to 9 calves (10 mg/kg plus probenecid [80 mg/kg]). Serum concentration-vs-time data were analyzed, using noncompartmental methods based on statistical moment theory. The data for IV ceftazidime administration also were fitted by use of a linear, open 2-compartment model. The mean (+/- SD) terminal half-life was 138.7 +/- 23.6 minutes and 126.3 +/- 10.5 minutes after IV and IM administrations, respectively. The mean residence time was 167.3 +/- 21.1 minutes and 201.4 +/- 16.8 minutes after IV and IM administrations, respectively. Coadministeration of probenecid did not affect the terminal half-life or mean residence time values. The total body clearance was 1.75 +/- 0.26 ml/min/kg, and the volume of distribution at steady state was 0.294 +/- 0.064 L/kg. The estimated mean absorption time was 34.1 minutes. There were no significant differences between the mean residence time calculated by statistical moment theory or by compartmental analysis, indicating central compartment output of ceftazidime. The 90% minimal inhibitory concentration values of ceftazidime determined for Escherichia coli, Salmonella spp, Pasteurella multocida, and P haemolytica isolates ranged from less than 0.01 to 0.1 micrograms/ml.

Animals↗
PubMed1985

Hypouricemia due to renal tubular defect. A study with the probenecid-pyrazinamide test.

Hypouricemia with hyperuricosuria due to isolated renal tubular defects are rare conditions. Two patients with hypouricemia and hyperuricosuria were studied for derangements in the renal urate transport with the combined probenecid-pyrazinamide test. In the first patient a significant decrease (64.5%) in the urate clearance--creatinine clearance ratio was noted after pyrazinamide administration, suggesting a post-secretory urate reabsorption defect, whereas the significant rise (44.2%) in urate clearance after the administration of probenecid indicates that this defect may not be complete. In the second patient there was a rise of 96.9% in the urate clearance--creatinine clearance ratio after the administration of probenecid and a decline of 31.6% in that ratio after pyrazinamide. These results suggest a defect in the presecretory reabsorptive site, with a highly significant response most probably of the postsecretory reabsorptive site to probenecid.

Adult↗
PubMedDate not supplied

Effect of probenecid on serum rifampicin levels.

Serum Rifampicin levels were determined by a microbiological assay using Staphylococcus aureus in 22 cases of leprosy after administering the drug with and without probenecid. Most of the patients showed higher serum rifampicin levels when probenecid was given along with rifampicin. Six patients showed statistically significant increase in the serum levels of the drug when given in the dose of 300 mg along with 1 g of probenecid one hour before breakfast and these levels were comparable with those obtained following administration of 450 mg of rifampicin alone two hours after breakfast. Thus administration of probenecid preceding rifampicin may be employed to reduce cost of drug as well as hepatotoxicity in patients requiring rifampicin for long duration.

Drug Administration Schedule↗
PubMed1978

High pressure liquid chromatographic method for probenecid in flavored oral suspensions containing ampicillin: collaborative studies.

A high pressure liquid chromatographic method for determining probenecid in oral suspensions of amoxicillin was applied to the determination of probenecid in oral suspensions of ampicillin. Three preparations containing various known amounts of probenecid in synthetic mixtures of ampicillin oral suspensions were analyzed by 5 chemists in an intralaboratory study, with satisfactory results. Blind duplicates of 3 prepared oral suspensions were sent to 12 collaborators, who were instructed to analyze the samples in a fixed random order. The standards showed a satisfactory linear response. Average recoveries of probenecid in the interlaboratory study for the 6 mixtures ranged from 95.2 to 99.1%, and the coefficients of variation ranged from 1.63 to 4.9%.

Ampicillin↗
PubMed1983

A renal mechanism for the clofibric acid-probenecid interaction.

A rabbit model has been used to investigate two hypotheses for the decrease in clofibric acid plasma clearance on probenecid coadministration in man. Rabbits administered probenecid (10 mg/kg followed by 10 mg/kg/hr) showed a mean reduction from control values of 68% for clofibric acid plasma clearance, 80% for clofibric acid glucuronide renal clearance and an elevation in the area under the plasma clofibric acid glucuronide concentration-time curve of 5.2-fold. These findings support the hypotheses that the decrease in clofibric acid plasma clearance involves the inhibition of the renal secretion of clofibric acid glucuronide by probenecid and the subsequent hydrolysis of the glucuronide as the major mechanism, rather than direct inhibition of clofibric acid glucuronide synthesis by probenecid, but do not exclude a mechanism in which both processes operate.

Animals↗
PubMed1983

[Inhibition of the renal excretion of PAH by probenecid homologs].

The authors studied the effects of probenecid and five of its homologues on the renal excretion of p-amino-hippuric acid (PAH). All the compounds under study inhibited the excretion of PAH. Probenecid and its homologues were injected 15 min before the administration of PAH. With all the substances tested, the inhibition of the excretion of PAH was most marked during the first 30 min of the diuresis experiment. The extent of efficiency increases within the homologous series up to the diethyl compound; after that, the inhibitory effect decreases with the increase in chain length. In the dosage range under study, the probenecid homologues show linear dose-response relationships. With due regard to toxicity and efficiency, the authors conclude from the results obtained that the diethyl compound is the most potent substance; probenecid itself is less efficient, being twice as toxic.

Aminohippuric Acids↗
PubMed1981

[Stimulation of the renal excretion of p-aminohippuric acid by probenecid homologues (author's transl)].

Probenecid and five of its homologues showed increased lipophilicity with increasing chain length of the substituents. Parallel to this, the toxicity increased about 30 times. All the probenecide homologues under study stimulated the excretion of p-aminohippuric acid (PAH) when applied repeatedly. If a threshold dose is exceeded, an increase of the pretreatment dose will not result in a further increase in PAH excretion. As compared to non-pretreated control animals, the highest possible increase in PAH excretion lies between 40 and 80% independently of the structure of the respective probenecide homologue. Due to their more favourable therapeutic range (LD50 divided by D40-50), the probenecide homologues with shorter chains are better suited to stimulate the excretion of PAH, though the extent of stimulation is the same with all the probenicide homologues under study.

Aminohippuric Acids↗