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PubMed1976

[Cerebral metabolism of dopamine and of serotonin during Alzheimer and Pick's diseases. Dynamic study by the test using probenecid].

A study of the cerebral metabolism of dopamine and serotonin has been realized by the probenecid test in 17 patients. The diagnosis of Alzheimer's disease (13 patients) and Pick's disease (4 patients) has been made on clinical and radiological grounds. No important anomaly of this metabolism was discovered. In subjects with Alzheimer's disease, the renewal rates of H.V.A. and 5 H.I.A.A. were diminished in comparison to the values measured in normal individuals, but this difference was not significant. In patients with Pick's disease, the accumulation of H.V.A. after probenecid was in the normal bounds, whereas that of 5 H.I.A.A. was non-significantly decreased. The results are compared with those of the literature.

Aged↗
PubMed1975

[Results of the treatment of acute gonorrhea with spectinomycin. Comparison with the combination of aqueous penicillin and probenecid].

Results following treatment of acute gonorrhea with aqueous penicillin combined with probenecid and spectinomycin hydrochloride (2.0 g) are compared and found to be statistically equivalent. Therefore, if a patient is allergic to penicillin, spectinomycin hydrochloride can be regarded as a valuable alternative. The results appear to be the same whether probenecid is administered simultaneously or 1/2-2 h before penicillin. It is advisable to control all patients one week after therapy. A second control after 2 weeks for men and after the next menstruation for women is highly desirable. If the patient fails to respond to treatment, not only an increase in the antibiotic dose, but also prolongation of therapy by administering the same dose on 3 consecutive days, is effective.

Drug Therapy, Combination↗
PubMed2004

[Synthesis of polymeric drug nanomicrospheres containing probenecid].

Nonsteroidal antiinflammatory drug, probenecid, was covalently linked with 2-hydroxyethyl methacrylate (HEMA). The drug linked HEMA(abbreviated as HP) can be copolymerized with methy methacrylate (MMA) to obtain polymeric drug nanomicrospheres in ethanol/water system. Polymers were characterized with 1H-NMR, FTIR, GPC and TEM. The results showed that probenecid was linked with HEMA by ester bond, the microspheres were composed of copolymer of HP and MMA, whose statistical average diameters were (90 +/- 5) nm, containing 47.4% HP, and drug content was high.

Adjuvants, Pharmaceutic↗
PubMed1991

Nephrotoxicity of the glutathione conjugate of menadione (2-methyl-1, 4-naphthoquinone) in the isolated perfused rat kidney. Role of metabolism by gamma-glutamyltranspeptidase and probenecid-sensitive transport.

The renal processing of the glutathione conjugate of menadione, 2-methyl-3-S-glutathionyl-1,4-naphthoquinone (thiodione) was studied in the isolated perfused rat kidney. Thiodione at an initial concentration of 600 microM was eliminated rapidly from the perfusate (clearance = 6.0 ml/min). Renal disposition could be ascribed to metabolism and transport of the glutathione conjugate. Renal metabolism by gamma-glutamyltranspeptidase was inhibited by AT-125 [L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid] (0.5 mM) resulting in a reduction of the thiodione clearance to 0.86 ml/min. Further reduction of the renal clearance of thiodione was achieved by a combination of AT-125 (0.5 mM) and probenecid (0.5 mM), resulting in a renal clearance of 0.58 ml/min which equalled glomerular filtration rate. Addition of thiodione to the perfusate caused loss of renal function and cellular damage, as reflected by a decreased glucose reabsorption and an increased urinary secretion of lactate dehydrogenase, respectively. Thiodione-induced nephrotoxicity was ameliorated by AT-125 and prevented completely by a combination of AT-125 and probenecid. Aminooxyacetic acid (0.5 mM), an inhibitor of beta-lyase, did not afford protection against the nephrotoxic action of thiodione. From our results it can be concluded that the thiodione-mediated toxicity in the isolated perfused rat kidney can be linked to cellular uptake by anionic transport systems and metabolism by gamma-glutamyltranspeptidase.

Animals↗
PubMed2006

Efficacy of probenecid for a patient with juvenile dermatomyositis complicated with calcinosis.

Calcinosis of juvenile dermatomyositis (JDM) is a crucial problem because it is refractory to various therapies. An 11-year-old boy who had been treated for JDM with interstitial pneumonia developed calcinosis of both legs despite treatment with corticosteroid and cyclosporin A. Images of his knees showed massive calcinosis with restricted range of motion. Probenecid was used to reduce calcinosis, resulting in remarkable improvement of calcinosis accompanied by normalization of serum phosphorus level and disability after 17 months of administration. We suggest that probenecid is useful for the treatment of calcinosis of JDM.

Anti-Inflammatory Agents↗
PubMed1991

A nonprimate animal model applicable to zidovudine pharmacokinetics in humans: inhibition of glucuronidation and renal excretion of zidovudine by probenecid in rats.

The monkey is considered the best animal model to study the pharmacokinetics of zidovudine (azidothymidine, AZT) because humans and monkeys eliminate 60 to 75% of AZT by metabolism to the 5'-O-glucuronide (GAZT), in contrast to other experimental animals, which excrete most of the drug unchanged in the urine. It has become increasingly difficult and costly to use monkeys in research. Therefore, we undertook studies to determine the suitability of the rat as an alternative animal model to study the pharmacokinetics of AZT. In the initial experiments, [3H]AZT was administered i.v. at doses of 19, 60 and 187 mumol/kg to male Sprague-Dawley rats with intact bile ducts. The respective values (mean +/- S.D.) for total clearance of AZT were 2.4 +/- 0.2, 2.3 +/- 0.3 and 1.8 +/- 0.4 l/hr/kg and for renal clearance were 1.7 +/- 0.2, 1.8 +/- 0.4 and 1.5 +/- 0.4 l/hr/kg. The renal clearance of AZT was approximately equal to renal plasma flow of rats (1.5 l/hr/kg), suggesting that in addition to filtration, AZT is also efficiently secreted in the kidney of the rat. The respective values for volume of distribution at steady state were 1.3 +/- 0.2, 1.0 +/- 0.2 and 0.84 +/- 0.19 l/kg (P less than .05) and elimination half-life were (harmonic mean) 0.55, 0.44 and 0.46 hr. Urinary excretion of AZT as unchanged drug in intact rats accounted for 70 +/- 6, 79 +/- 6, and 83 +/- 12% of the dose, whereas only 0.7 to 0.8% of the dose was recovered in the urine as GAZT. Rats with exteriorized bile ducts, the proposed alternative animal model, were given an i.v. dose of 60 mumol/kg of [3H]AZT. To test the effect of a concurrently administered drug on the elimination of AZT in the model, some rats with bile duct cannulas were pretreated with probenecid, a known inhibitor of AZT elimination in humans. Urine and bile were collected to quantify the formation of GAZT. GAZT was identified by fast atom bombardment mass spectrometry as the major metabolite of AZT in the rat. GAZT excretion in the bile and urine accounted for 11 +/- 3% of the dose in saline-treated rats, compared to only 1.4 +/- 0.3% in rats treated with probenecid (P less than .001).(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMed1991

Probenecid pharmacokinetics in cystic fibrosis.

Probenecid pharmacokinetics were studied in 5 cystic fibrosis (CF) subjects and 5 control subjects at oral dosages of 5, 15, and 30 mg/kg. Serum and urine samples were collected for 8 h after administration and assayed by reverse phase high performance liquid chromatography. Pharmacokinetic parameters were estimated by model-independent methods. All parameters were compared by 2-tailed analysis of variance with two major groupings: patient and dose. Both CF subjects and controls demonstrated dose-dependent kinetics, i.e., decreased elimination constant and decreased total body clearance with increasing dosage. The volume of distribution and time to peak were the only parameters that were not significantly dose dependent. At all dosages studied, we found no significant difference in total body clearance by CF subjects. Urinary recovery in an 8-hour period was not significantly different between CF subjects and controls nor was the percentage of dose recovered in the urine at each dosage level. Time to peak concentration varied widely between 0.5 and 4 h in both CF subjects and controls. We conclude, that CF patients have normal probenecid clearance, and that the standard dose for a CF patient is sufficient to attain a serum area under the curve equivalent to that of controls.

Administration, Oral↗
PubMed1989

[Uncomplicated acute male and female gonorrhea: treatment with a single oral dose of epicillin-probenecid].

We treated 142 patients with acute uncomplicated gonorrhea with a single oral dose of epiciline-probenecid. All cases were confirmed by culture on Thayer Martin medium at the first day and they were all laboratory tested seven days after treatment. At the control time the patients were asked about drug tolerance. All isolated strains were tested for beta-lactamase producing capacity and susceptibility to epiciline and penicillin. All patients who were culture positive seven days after treatment were considered to be treatment failures. The treatment was effective in 94.4% and we detected 8 Neisseria gonorrhoeae strains resistant to penicillin (5.6%); seven of these were PPNG strains. Tolerance to the drug was excellent in 90% of all cases; 9% presented minor adverse reactions for a short period of time. Therefore, the combination of epiciline-probenecid is a valid alternative for routine treatment of acute uncomplicated gonorrhea.

Acute Disease↗
PubMed1989

Effect of probenecid and benzbromarone on gluconeogenesis in isolated rat liver cells.

The effect of benzbromarone on gluconeogenesis from several gluconeogenic substrates in isolated rat liver cells is reported. Benzbromarone inhibited glucose synthesis from all substrates employed when the drug was used at concentrations half to ten times greater than its therapeutic plasma levels. This inhibition was more pronounced from lactate and pyruvate than from fructose and glycerol. The results are compared with those obtained for probenecid, a classical uricosuric drug. We found that probenecid inhibited the pathway in the same way as benzbromarone.

Animals↗
PubMed1989

[Effect of ethanol and probenecid on the excretory function of the cerebral choroid plexus in rats].

Probenecid at a dose 100 and 200 mg/kg, i.v. has been found to decrease in a dose-dependent manner the level of radioactivity of cerebrospinal fluid (CSF) measured at 1, 15, 30 and 60 min. after the intravenous injection of 14C-tyrosine, 14C-tryptophan and 14C-DOPA. Ethanol at a dose 2 and 4 g/kg, i. p. has not changed the level of radioactivity of the CSF. It is suggested that mentioned in the literature an increased accumulation of the labeled tyrosine, tryptophan and DOPA in the brain structures after their intravenous injection is not related to the inhibitory effect of ethanol on the excretory function of the choroid plexus of the brain. On the other hand, it is concluded that probenecid is able to inhibit the excretion from the brain of some acid compounds including tyrosine, tryptophan and DOPA.

Animals↗
PubMed1989

Hypouricemia due to familial isolated renal tubular uricosuria. Evaluation with the combined pyrazinamide-probenecid test.

A Jewish Iraqi woman with familial isolated renal tubular uricosuria, urate clearance of 60.5 +/- 5.7 ml/min and hypouricemia of 1.0 +/- 0.2 mg/dl is described. The combined pyrazinamide-probenecid test suggested a presecretory defect in urate reabsorption. Four offspring were moderately affected. This family represents the sixth Jewish Iraqi family with familial isolated presecretory uricosuria, and emphasizes the marked prevalence of this disease among the Iraqi Jewish population. Since the inheritance of the presecretory defect is autosomal recessive, we suggest that this family is an example of pseudodominant transmission. The combined pyrazinamide-probenecid test may cause a reduction in glomerular filtration rate and filtered load of urate and thereby affect urinary excretion rate of urate in patients with urate wasting.

Creatinine↗
PubMed1986

Probenecid induced immune hemolytic anemia.

We report a patient who, while receiving probenecid and colchicine for acute gouty arthritis, developed severe hemolytic anemia in association with a generalized rash. The hemolysis was immune mediated as shown by a positive direct Coombs' test. In vitro hematologic studies showed that a probenecid dependent antibody was present.

Anemia, Hemolytic, Autoimmune↗
PubMed1970

The effects of probenecid and thiazides and their combination on the urinary excretion of electrolytes and on acid-base equilibrium.

The effects of commonly used therapeutic doses of hydrochlorothiazide and probenecid, given singly and in combination, on the urinary excretion of monovalent and divalent ions and on acid-base equilibrium were studied in four patients with idiopathic hypercalciuria.Probenecid had no effect on the urinary excretion of monovalent ions but resulted in a sustained increase in the urinary excretion of calcium, magnesium and citrate and a temporary increase in the urinary excretion of ammonium, in addition to its well-known effects on uric acid metabolism. A temporary fall in serum phosphorus levels was also observed.Probenecid also modified the response to hydrochlorothiazide in that the urinary excretion of calcium, magnesium and citrate was greater during combined therapy than when hydrochlorothiazide was administered alone. Probenecid prevented or abolished the increase in serum uric acid levels associated with the use of thiazide but did not modify the effects of hydrochlorothiazide on the urinary excretion of sodium, chloride, potassiu, phosphorus, ammonium, titratable acid and bicarbonate.

Acid-Base Equilibrium↗
PubMed1982

[Pharmacokinetics of ceftizoxime with and without probenecid].

Serum concentrations and urinary recovery of ceftizoxime were investigated in 18 healthy volunteers. The substance was given as a bolus (2 min) i.v. injection. In volunteers the injection was preceded by orally administered probenecid, 500 mg, 7 and 1 h before (Group II); the remaining 12 volunteers received medication. 5 min after the injection, the serum concentration in Group I was 107 +/- 22 micrograms/ml and in II 93 +/- 18 micrograms/ml in the mean; 30 min after the injection in I 45 +/- 8 micrograms/ml and 44 +/- 10 micrograms/ml in II. The further of the serum concentration was slower in II than in I: serum concentration 6 h after the injection was 2.6 +/- 0.9 micrograms/ml in I and 4.4 +/- 2 micrograms/ml in II. During the first 8-h period 81% of the administered cephalosporin was recovered in the urine of I and 58% in the urine of II. t/2 beta was calculated for I with 1.76 h and 2.13 h for II. The distribution volume was equal, so that the differences in serum concentrations could be explained by the reduced renal clearance: from 2.1 to 1.4 ml/s. Because the comparison was done with two independent groups and furthermore only 6 volunteers participated in the probenecid group, only the difference in the urine in the first 2 h was statistically significant.

Adult↗
PubMed1982

[Pharmacokinetics of mezlocillin. Comparison with ampicillin and influence of probenecid (author's transl)].

In a randomized cross-over study 10 healthy male volunteers received a single 1 g dose of 6-[R]-2-3-methylsulfonyl -2- oxo-imidazolisine -1- carboxamido) -2- phenyl-acetamido]-penicillanic acid sodium salt (mezlocillin) and of ampicillin, either intravenously or intramuscularly. Following the intravenous loading dose, mean peak serum levels of 101 micrograms/ml for mezlocillin and 91.5 micrograms/ml for ampicillin were recorded. The ultimate half-life t 1/2 of mezlocillin (46.4 min) was slightly shorter than that of ampicillin (52.4 min). Similarly, the total volume of distribution of mezlocillin (24.1 l) was slightly inferior to that of ampicillin (29.4 l). The proportions of the dose administered recovered in the urine of 24 hours were 50.4 % for mezlocillin and 69.9 % for ampicillin. The total clearances of the two antibiotics were not significantly different, but the renal clearance of mezlocillin (186.6 ml/min/1.73 m2) was significantly lower than that of ampicillin (309.5 ml/min/1.73 m2). Following intramuscular injection, the mean peak serum levels obtained were 15.6 microgram/ml with mezlocillin and 15.1 micrograms/ml with ampicillin. The half-lives of the antibiotics were 50.0 min and 57.2 min respectively. The bioavailable fractions of mezlocillin and ampicillin, as measured from the areas under the serum concentration curves wer 63 % and 75 % respectively of the values determined after intravenous injection. The oral administration of 1 g probenecid one hour before an intramuscular injection of mezlocillin increased the peak serum level and area under the curve by 65 % and decreased the total clearance, renal clearance and apparent volume of distribution by 38 %, 52 %, and 35 % respectively. However, the ultimate half-life was not significantly altered (50.5 min without, and 52.0 min with probenecid).

Adult↗
PubMed1983

Effect of probenecid on the dose-response relationship of bumetanide at steady state.

The present investigation was undertaken to clarify the determinants of the pharmacologic responses to bumetanide. The urinary excretion rate, plasma concentration and natriuretic and diuretic effects of bumetanide were evaluated under steady-state conditions in four mongrel dogs, before (Treatment I) and after (Treatment II) probenecid administration. To avoid fluid and electrolyte imbalance, urinary losses were replaced i.v. by equal volumes of lactated Ringer's solution over the time interval of the subsequent collection period. Probenecid administration caused a dramatic reduction in the renal clearance of bumetanide (5.05 +/- 1.11 for Treatment I vs. 0.716 +/- 0.285 ml/min . kg for Treatment II; P less than .002), resulting in significantly higher plasma concentrations (3-fold) and significantly lower urinary excretion rates (2.5-fold) of the diuretic. This was accompanied by concomitant reductions in bumetanide-induced diuresis and natriuresis. The results from this study demonstrate that adequate luminal levels of bumetanide are required for the pharmacodynamics of the drug.

Animals↗
PubMed1981

Probenecid and intraocular methicillin.

Probenecid was given intravenously to rabbits in an effort to extend the intraocular longevity of intravitreal methicillin. With relatively high levels of probenecid, an insignificant elevation of half-life was obtained. Aqueous levels of methicillin were measured after intravitreal injection and were found to be adequate to inhibit penicillinase-producing S. aureus for approximately 20 hours.

Animals↗
PubMed1980

Amino acid concentrations in cerebrospinal fluid: effects of aging, depression, and probenecid.

Cerebrospinal fluid (CSF) amino acid concentrations were measured in six Bipolar I, eight Bipolar II, eight Unipolar, and four other and control patients. All but four were also studied after administration of probenecid. Fourteen amino acids showed significant correlations of concentrations with age of subjects. Significant diagnostic group differences were found for five amino acids; only that of tyrosine persisted after taking subject's age into account. Following probenecid administration, there were statistically significant changes in CSF concentration of several amino acids, but these changes were small and likely indicative of diurnal changes.

Adult↗