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At least 451 records · Page 25Linked to original sources
PubMed1984

Regional distribution of the histamine metabolite, tele-methylimidazoleacetic acid, in rat brain: effects of pargyline and probenecid.

tele-Methylimidazoleacetic acid (t-MIAA), a major brain histamine metabolite, was measured in nine rat brain regions by a gas chromatography-mass spectrometric method that also measures the precursor amine, tele-methylhistamine (t-MH). The t-MIAA concentration of cerebellum, medulla-pons, midbrain, caudate nucleus, hypothalamus, frontal cortex, hippocampus, and thalamus varied 15-fold, hypothalamus showing the highest level (2.21 nmol/g) and cerebellum the lowest (0.15 nmol/g). The concentrations of t-MIAA and t-MH were significantly correlated in all regions except midbrain, which had relatively more t-MIAA. Probenecid did not alter whole-brain t-MIAA levels. Treatment with pargyline, an inhibitor of monoamine oxidase, lowered the t-MIAA levels in all regions.

Animals↗
PubMed1979

Effects of central administation of probenecid on fevers produced by leukocytic pyrogen and PGE2 in the rabbit.

1. Single intracerebroventricular (I.C.V.) injections of probenecid (PBCD, 0.125--0.5 mg) enhanced and prolonged fever caused by I.V. administration of leukocytic pyrogen (LP) in rabbits resting in neutral (23 degrees C), cold (10 degrees C) and hot (30 degrees C) environments. Similar effects were produced by single I.C.V. injections of PBCD given before PGE2 (0.5 microgram) was injected I.C.V. in the three ambient temperatures. 2. Fever produced by IV. LP was also prolonged by infusion and by multiple injections of PBCD. 3. PBCD given I.P. (100 mg/kg) enhanced and prolonged fever caused by I.V. injection of Salmonella typhosa endotoxin. 4. Hyperthermia produced by I.C.V. PGE2 was not augmented by subsequent PBCD infusion. However, pre-treatment with PBCD followed by PGE2 injection and PBCD infusion caused hyperthermia that was very high and prolonged, and, in some cases, lethal. 5. Acetaminophen (2 mg, I.C.V.) and indomethacin (10 mg/kg, I.V.) lowered body temperature when given during fever induced by LP and prolonged by PBCD infusion. 6. The concentration of PGE in cerebrospinal fluid (c.s.f.) samples taken from the third or lateral ventricles rose or stabilized during PBCD infusions made during LP fever. However, similar changes in PGE concentration also occurred during control infusions when body temperature was low. 7. We conclude that termination of the actions of both central endogenous pyrogen and centrally administered PGE2, and the subsequent reduction of fevers produced by them, require a PBCD-sensitive facilitated transport system. The reduction of PBCD-prolonged PL fevers by antipyretics which block PGE synthesis suggests that prolongation by PBCD of LP fever is not due to blockade of PGE transport in a subsequent step in fever mediation per se, but is due to inhibition of transport of LP itself, or of other mediators associated with it.

Animals↗
PubMed1990

Single-dose oral cefixime versus amoxicillin plus probenecid for the treatment of uncomplicated gonorrhea in men.

In this randomized study, a single 800-mg oral dose of cefixime cured 96 of 97 men with uncomplicated gonococcal urethritis, compared with 44 cures of 46 men who received standard therapy with amoxicillin (3 g) plus probenecid (1 g). Both regimens were ineffective against coexistent infection with Chlamydia trachomatis and Ureaplasma urealyticum. Cefixime was well tolerated, and all side effects were mild and self-limited.

Adolescent↗
PubMed1993

Effects of probenecid on the pharmacokinetics of allopurinol riboside.

Allopurinol riboside is an experimental agent for the treatment of leishmaniasis and American trypanosomiasis. Previous studies showed that after oral administration, unexpectedly low levels of allopurinol riboside in plasma are attributable to incomplete absorption and rapid renal clearance. In this randomized, crossover evaluation in healthy volunteers, probenecid reduces the renal clearance of allopurinol riboside, extends the half-life of allopurinol riboside in plasma, and triples the levels of allopurinol riboside in plasma.

Adult↗
PubMed1972

Treatment of calcinosis circumscripta with probenecid.

A 23-year-old woman presented with an 11-year history of peripheral joint pains and stiffness slowly progressing to the development of gross calcinosis circumscripta. She had no definite evidence of systemic scleroderma. She was first treated for one year with frequent intravenous sodium EDTA, which increased urinary calcium and enhanced negative calcium balance but did not lessen her calcinosis. She was then treated with probenecid up to 2 g daily and her calcinosis lessened steadily over three years. Plasma levels of both phosphorus and urate fell during this time.

Adult↗
PubMed1975

Relationships between tryptophan in serum and CSF, and 5-hydroxyindoleacetic acid in CSF of man: effect of cirrhosis of liver and probenecid administration.

Tryptophan was measured in the lumbar CSF and serum of patients undergoing neurological investigation (controls) and in patients with hepatic cirrhosis. Samples were taken from the fasting patients at 8:00 a.m. Under these conditions, in the controls the mean CSF, free )mpm-albumin-bound) and total serum tryptophan were in the approximate ratio 1:4:24. In this cross-sectional study, for the controls, CSF tryptophan was correlated significantly and positively with the total serum but not with the free serum tryptophan. In patients with advanced hepatic cirrhosis the mean CSF tryptophan concentration was greatly elevated. However, the mean total serum tryptophan was unchanged and the free serum tryptophan only slightly elevated. Administration of probenecid, which displaces tryptophan from binding sites on serum albumin, and thereby increases the proportion of serum tryptophan in the free form, did not affect CSF tryptophan.

Adult↗
PubMed1975

Treatment of gonorrhoea in the female with fortified procaine penicillin plus probenecid and with spectinomycin.

513 cases of uncomplicated gonorrhoea in females with positive results to cultures were treated with two regimens of treatment between January 1, 1972, and February 28, 1973, at the Department for Females, Bangrak Hospital, Bangkok. The highest incidence was found in the age group 20 to 24 years (215 out of 513). The patients were divided into two groups. In the first, probenecid 1 g. was given orally 1 hour before an intramuscular injection of 4 million units fortified procaine penicillin, and in the second an intramuscular injection of 2 g. spectinomycin dihydrochloride was given. 335 cases were followed in the first group and there were no failures; 132 cases were followed in the second group and there was one failure (0.7 per cent.). The fact that gonococci were found in the rectum in 23.7 per cent. of cases (117 out of 493) indicates that rectal tests are of considerable importance and should be included in the routine investigations. There was no evidence that gonorrhoeal infection of the rectum was more resistant to treatment than infection at other sites.

Adolescent↗
PubMed1979

Double-blind trial of amoxycillin and ampicillin plus probenecid in the treatment of gonorrhoea in men.

In a double-blind study amoxycillin 3 g or ampicillin 3 g plus probenecid 1 g were randomly administered as a single oral dose to 160 men with uncomplicated gonococcal urethritis. The cure rate for each drug group was 98.6%. Tolerance to oral medication was good and no evidence of allergy or toxicity to either drug was shown. No case of post-gonococcal urethritis was observed over a 14-day follow-up period. Thus, both drug regimens proved very effective in treating uncomplicated gonococcal urethritis in men.

Adolescent↗
PubMed1983

Renal handling of uric acid in normal subjects by means of the pyrazinamide and probenecid tests.

Pyrazinamide and probenecid tests were used to study the renal mechanisms for urate excretion in 10 normal subjects in the state of low serum uric acid levels (below 3.5 mg/dl), normal serum urate concentrations (between 3.6 and 6.4 mg/dl) and high serum uric acid levels (above 6.5 mg/dl). Presecretory reabsorption of urate was above 99% in all three conditions of uricemia, indicating that filtered urate is nearly completely reabsorbed in the proximal tubule regardless of serum uric acid concentrations. Urate secretion was significantly higher and postsecretory reabsorption was significantly lower when serum uric acid was raised than when serum urate levels were normal or low. The findings indicate that both urate secretion and postsecretory reabsorption play a role in urate homeostasis in states of hyperuricemia.

Adult↗
PubMed1987

Evaluation of the renal mechanisms for urate homeostasis in uremic patients by probenecid and pyrazinamide test.

The tubular transport of urate was studied in 47 uremic patients and in 20 normal subjects using probenecid and pyrazinamide tests. There was a marked increase in urate excretion per nephron as the renal function deteriorated. Presecretory reabsorption of urate per nephron, which was almost complete in normal subjects, showed a diminution with increasing severity of chronic renal failure. Until the creatinine clearance had decreased to less than 10 ml/min, the secreted urate per nephron remained almost constant, while in the end stage of renal failure it was markedly decreased. With the progression of renal disease, the postsecretory reabsorption of urate per nephron diminished. In patients with a creatinine clearance less than 10 ml/min, it was 4 times lower than in normal subjects. These findings indicate that urate secretion does not contribute to the increase of urate excretion per nephron at any level of renal failure, whereas the impairment of both reabsorptive components accounts for the augmented urate excretion per nephron in uremic patients.

Absorption↗
PubMed1988

Renal excretion of purine bases. Effects of probenecid, benzbromarone and pyrazinamide.

Experiments were conducted which revealed the renal transport mechanism(s) of oxypurines by employing uricosuric agents and pyrazinamide. All specimens being drawn from healthy, normal subjects, the data showed that probenecid increased fractional uric acid, fractional hypoxanthine and fractional xanthine clearance, 3.97-, 1.52- and 2.31-fold, respectively, while benzbromarone increased fractional uric acid clearance 2.11-fold, decreased fractional xanthine clearance 0.48-fold and had no effect on fractional hypoxanthine clearance. In addition, pyrazinamide decreased both fractional uric acid clearance 0.35-fold and fractional xanthine clearance 0.44-fold but increased fractional hypoxanthine clearance 1.49-fold. These results suggest the possibility of differing renal transport mechanisms among the purine bases, uric acid, hypoxanthine and xanthine.

Adult↗
PubMed1978

Treatment of urogenital/rectal gonorrhoea in males and females with epicillin in combination with probenecid.

This paper describes the results of treatment of 124 patients (78 male and 46 female) with urogenital/rectal gonorrhoea with epicillin (3.5 g orally) in combination with 1 g of probenecid (instant therapy). High cure rates were found for both the male (98.6%) and female patients (100%). Serious drawbacks of this treatment are a high frequency of postgonococcal urethritis (45.6%) and a short-lived increase in the frequency and looseness of faecal discharge in a considerable amount of patients (6.8% in the male and 22.7% in the female patients).

Administration, Oral↗
PubMed1991

The folate receptor works in tandem with a probenecid-sensitive carrier in MA104 cells in vitro.

Previous studies have defined a novel route of internalization for the essential vitamin 5-methyltetrahydrofolate in MA104 cells that begins with binding of the vitamin to the membrane receptor for folate. One of the critical steps in the pathway is the passage of 5-methyltetrahydrofolate through the membrane into the cytoplasm. Utilizing both probenecid and low temperature as selective inhibitors, we have successfully blocked transmembrane movement of the vitamin into the cytoplasm without affecting binding to the receptor or the internalization of the vitamin-receptor complex, which suggests that passage is through an anion carrier. This anion carrier, which mediates inward movement of 5-methyltetrahydrofolate after it dissociates from the receptor, also appears to mediate the efflux of folylmonoglutamate, but not folylpolyglutamate, when the concentration of the former in the cytoplasm is sufficiently high. Since we also found that the synthesis of folylpolyglutamates is regulated in these cells, most likely the intracellular concentration of the vitamin is controlled by regulating the flux of folylmonoglutamate through this carrier.

Animals↗
PubMedDate not supplied

An open study of procaine penicillin G, clavulanate-potentiated amoxycillin and probenecid in the treatment of acute gonorrhoea.

In an open study 55 patients presenting with acute gonorrhoea were given 4.8 mega units procaine penicillin G, intramuscularly, and oral probenecid (1 g) plus one 375-mg tablet clavulanate-potentiated amoxycillin orally. Before this treatment, 53 patients (96.4%) had presented with a purulent discharge, and dysuria was present in 47 patients (85.5%). The presence of Neisseria gonorrhoeae was confirmed by bacterial culture in 54 patients (98.2%). The majority of pathogens (92.5%) were penicillin resistant. On day 3 after treatment, dysuria was absent in 53 patients (96.4%) and there was no discharge in 40 cases (72.7%). N. gonorrhoeae was eradicated in 53 patients (96.4%). Two further patients were bacteriologically cured, but were suffering from post-gonococcal urethritis. The patients in whom discharge was still apparent were further assessed on day 7; discharge was resolved or resolving in all but one patient. There was one treatment failure. No adverse reactions were reported.

Acute Disease↗
PubMed1995

Effect of probenecid, verapamil and progesterone on the concentration-dependent and temperature-sensitive human erythrocyte uptake and export of guanosine 3',5' cyclic monophosphate (cGMP).

Elevated extracellular cGMP levels have been observed in various clinical conditions, and the analyte has been proposed as a diagnostic marker of cardiovascular as well as malignant diseases. However, the use of extracellular cGMP as a pathophysiological marker requires detailed knowledge about the cellular biokinetics of cGMP (synthesis, metabolic conversion and export). In the present study the transport of cGMP in human erythrocytes has been further characterized. The uptake of cGMP was dependent on a concentration gradient and was temperature-sensitive, compatible with passive diffusion. The cGMP export was temperature-sensitive, saturable (Km = 3.4 +/- 1.0 mu mol l-1), inhibited by probenecid and verapamil and stimulated by progesterone. The results show that human erythrocytes possess a cGMP transport system similar to that found in other cells and that extracellular levels of cGMP are dependent on intracellular levels, membrane transport and influenced by physiological factors and pharmacological agents.

Biological Transport↗