pharmacokinetics of probenecid

: Renal tubular mechanisms for excretion of organic acids and bases. PubMed Google Scholar. and Dayton, P.G. : The interaction of methotrexate and probenecid in man and dog. Journal of Clinical Pharmacology 18: 491–499 (1978). : Influence of probenecid on gentamycin pharmacokinetics. : Application of steadystate kinetics to studies of the transfer of 5-hydroxyindoleacetic acid from brain to plasma. The fraction of drug excreted in the urine was low. Probenecid and its oxidised metabolites are extensively bound to plasma proteins, mainly to albumin. Tjandramaga, T.B. Annals of the New York Academy of Sciences 123: 273–286 (1965). Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits. Annals of Internal Medicine 33: 18–31 (1950a). Annals of the New York Academy of Sciences 226: 172–194 (1973a). Small amounts of unchanged probenecid are filtered … Conway, W.D. Patients received sorafenib (200-800 mg daily) in combination with probenecid (500 mg two times daily (b.i.d.)) European Journal of Pharmacology 8: 244–252 (1969). : Apparent effect of probenecid on the distribution of penicillins in man. Archives Internationales de Pharmacodynamie et de Therapie 211: 197–210 (1974). International Journal of Neuro-Pharmacology 3: 117–122 (1964). The drug is extensively metabolised by glucuronide conjugation and by oxidation of the alkyl side chains; oxidation of the aromatic ring does not occur. Journal of Pharmacology and Experimental Therapeutics 158: 305–316 (1967). Acta Medica Scandinavica 191: 221–224 (1974). ; Matteucci, W.V. The prototypical uricosuric agent. The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. CAS  Bishop, C.; Rand, R. and Talbott, J.H. Nineteenth rheumatism review. Pharmacokinetic sampling was performed in 16 patients on steady-state sorafenib treatment at days 1 and 15 of the study. Van Praag, H.M.; Korf, J.; Dols, L.C.W, and Schut, T.: A pilot study of the predictive value of the probenecid test in application of 5-hydroxytryptophan as antidepressant. Dayton, P.G. Clin Pharmacokinet 6, 135–151 (1981). ; Nelson, R.L. Constant, M.: Distribution of 5,5-dimethyl-2,4-oxazolidinedione in intraocular fluids of rabbits. Journal of Pharmacology and Experimental Therapeutics 210: 186–195 (1979). Frey, H.H. Dayton, P.G. and Sirota, J.H. https://doi.org/10.2165/00003088-198106020-00004. Letter: British Journal of Pharmacology 63: 369P (1978a). Chemical, physical, and pharmacological studies. Sjöström, R.: Steady-state levels of probenecid and their relation to acid monoamine metabolites in human cerebrospinal fluid. : On the mechanism of action of probenecid on renal tubular secretion. : Prolongation and enhancement of serum methotrexate concentrations by probenecid. Despopoulos, A. and Weissbach, H.: Renal metabolism of 5-hydroxyindolacetic acid. : Metabolic studies of allopurinol, an inhibitor of xanthine oxidase. Biological Psychiatry 3: 105–112 (1971). Bergan, T.; Westlie, L. and Brodwall, E.K. ; Dayton, P.G. Adams, H., Holmes, K.; Israili, Z. and Dayton, P.: Interaction of probenecid with penicillin G in man. The unbound fraction was found to increase non‐linearly with increasing total concentration, yielding a maximum free fraction of 49 per cent. FOIA ; Kislak, J.W. Dosage schedule in children. PHARMACOKINETICS. ; Brunson, M.K. Physiological significance of the uricosuric effect of carinamide. Although probenecid has been in use for over half a century, and has been recommended as part of the treatment of gonorrhea in pregnancy, very little clinical data exist on its safety in pregnancy. These are based on spectrophotometry, spectrofluorometry, gas and liquid chromatography and radioimmunoassay. ; Bronsky, D. and Pascale, L.R. Boger, W.P. ; Reeves, D.S. and Beatty, J.O. Brater, D.C.: Effects of probenecid and furosemide response. Elion, G.B. ; Plowden, J.F. Google Scholar. Letter. and Yü, T.F. The effect of probenecid on tubular secretion of organic anions was evaluated by determining the pharmacokinetics of IV cefazolin (11 mg/kg) administered alone and 15 minutes after probenecid (10 mg/kg orally). Epub 2007 Dec 3. : Cinoxacin: Pharmacokinetics and the effect of probenecid. Unable to load your collection due to an error, Unable to load your delegates due to an error. Toxicology and Applied Pharmacology 33: 246–257 (1975). Journal of Chromatography 115: 222–227 (1975). Google Scholar. Karney, W.W.; Turck, M. and Holmes, K.K. ; Levitt, M. and Dunner, D.L. : Observations on the disposition of probenecid in patients receiving allopurinol. Dr R. F. Cunningham. Psychopharmacologia 18: 129–132 (1970). Two randomized controlled trials were included in the systematic review and were Secondary objectives are to assess the safety and tolerability of pexidartinib alone and in combination with probenecid. Inhibition of ABC transporters abolishes antimony resistance in Leishmania Infection. : Selective ion monitoring assay for probenecid. Please enable it to take advantage of the complete set of features! Clinical Pharmacology and Therapeutics 23: 259–265 (1978a). ; Kovensky, A. and Hitchings, G.H. We administered i.v. : “Benemid” p-(din-propylsulfamyl)-benzoic acid: Lack of effect of aureomycin, chloromycetin, streptomycin and terramycin. Damm, K.H. : The gastric secretion of drugs: a pH partition hypothesis. Federation Proceedings 36: 1040 (1977). Talbott, J.H. Accessibility Israel, K.S. Lant, A.F. Probenecid given IV was characterized by a rapid disposition phase with a mean half-life of 14.0 minutes and a subsequent slower elimination phase with a mean half-life of 87.8 minutes in 5 of 6 mares. ; Bishop, C.; Norcross, B.M. ; Rogers, D.; Holmes, G.I. : Renal tubular excretion of drugs: Proximal tubule secretion and metabolism; in Fisher (Ed) Renal Pharmacology, pp.67–84 (Appleton-Century Crofts, New York 1971). and Levy, G.: Effect of probenecid on riboflavin absorption and excretion in man. Journal of Clinical Investigation 30: 889–895 (1951). Korf, J. and Van Praag, H.M.: The intravenous probenecid test A possible aid in evaluation of the serotonin hypothesis on the pathogenesis of depressions. Psychopharmacology 53: 305–308 (1977). Gibaldi, M.; Davidson, D; Plaut, M.E. Life Sciences 14: 837–852 (1974). ; Skrdlant, H.B. Cunningham, R.F. ; Bayne, G.M. IV. ; Perel, J.M. ; Piall, E.; Marks, V.; Mould, G.P. Journal of Pharmacology and Experimental Therapeutics 211: 509 (1979). and Moir, A.T.B. ; Chen, W.; Berger, L.; West, L.A. and Gutman, A.B. Transactions of the Association of American Physicians 64: 372–377 (1951). Gutman, A.B. Hansen, J.M. The half-life of probenecid in plasma (4 to 12 hours) is dose-dependent. and Mills, J.: Severe metabolic acidosis associated with nalidixic acid overdose. ; Dayton, P.G. Tillson, E.K. III. : A study, by simultaneous clearance techniques, of salicylate excretion in man. Dubin, A.; Kushner, D.S. & Dayton, P.G. Clinical Pharmacology and Therapeutics 9: 345–349 (1968). Glbaldi, M. and Schwartz, M.A. Jr: Factors basic to the development of useful inhibitors of renal transport mechanisms. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy. and Shepherd, A.M.M. Journal of Clinical Pharmacology 20: 347–351 (1980). : Dose-dependence of drug plasma level decline in dogs. Archives Internationales de Pharmacodynamie et de Therapie 48: 97–117 (1954). ; Gutman, A.B. Department of Medicine, Emory University, Atlanta, Georgia, USA, Dr R. F. Cunningham, Z. H. Israili & P. G. Dayton, Atlanta VA Medical Center, Decatur, Georgia, USA, Highland Drive VA Medical Center, Pittsburgh, Pennsylvania, USA, Department of Psychiatry, University of Pittsburgh, Pennsylvania, USA, You can also search for this author in ; Faraj, B.A. : Benemid (p-[di-n-propylsulfamyl]-benzoic acid) as uricosuric agent in chronic gouty arthritis. Rammelkamp, C.H. Hutchison, J.C.; Wilkinson, W.H. After treatment by probenecid or placebo, pharmacokinetics of adefovir 10 mg/kg was studied via population modeling (NONMEM). Metabolism 5: 703–709 (1956). CAS  American Journal of Medicine 9: 799–817 (1950). ; Yü, T.F. Boger, W.P. ; Dayton, P.G. ; Goldring, W. and Chassis, H.: The measurement of the tubular excretory mass, effective blood flow, and filtration rate in the normal human kidney. P… : Comparative therapeutic and pharmacological evaluation of amoxicillin and ampicillin plus probenecid for the treatment of gonorrhea. and Dayton, P.G. American Journal of Medical Sciences 246: 129–146 (1963). ; Pessah, N.I. Dayton, P.G. Neff, N.H.; Tozer, T.N. Naunyn-Schmiedeberg’s Archiv für Experimentelle Pathologie und Pharmakologie 243: 429–438 (1962). ; Holohan, P.D. : Studies of the specificity of an antibody directed against probenecid. : Renal clearance of pantothenic acid in man: Inhibition by probenecid (“Benemid”). : Probenecid and serum rifampicin. : Benzoyl coenzyme A and hippurate synthesis. and Perel, J.M. and Melethil, S.: Excretion of probenecid and its metabolites in bile and urine of rats. Similarly probenecid affects the tubular secretion of a number of acidic endogenous substances by the kidney. Lancet 2: 1401–1405 (1973). To provide whole-body physiologically based pharmacokinetic (PBPK) models of the potent clinical organic anion transporter (OAT) inhibitor probenecid and the clinical OAT victim drug furosemide for their application in transporter-based drug-drug interaction (DDI) modeling. Renal excretion is the major route of elimination of the metabolites; excretion of the parent drug is minimal and is dependent on urinary pH. Journal of Laboratory and Clinical Medicine 36: 276–282 (1950b). and Erttmann, R.: Interaction of probenecid with digitoxin metabolism in rats. Fanelli, G.M. Jr; Wiebelhaus, V.D. American Journal of Medicine 4: 774 (1948). 6): 35–42 (1975). Shei, W.L. ; Clement, W.A. : Studies of the renal excretion of probenecid acylglucuronide in man. ; Cucinell, S.A.; Weiss, M. and Perel, J.M. ; Verwey, W.F. Perel, J.M. ; Israili, Z.H. Probenecid, an inhibitor of glucuronide conjugation, was studied to evaluate the potential effect of these inhibitors on the pharmacokinetics of bempedoic acid. Erttmann, R. and Damm, K.H. ; Israili, Z.H. Journal of Physiology 199: 397–425 (1968). and Gutman, A.B. Proceedings of the Society for Experimental Biology and Medicine 82: 604–608 (1953). Sabath, L.D. ; Anden, N.E. : Urinary excretion of probenecid and its metabolites in humans as a function of dose. : Renal clearance of oxipurinol, the chief metabolite of allopurinol. Transactions of the association of American Physicians 64: 279–288 (1951). Jr. and Weiner, I.M. There are a number of analytical procedures for the assay of probenecid. Schrogie, J.J.; Davies, R.O. : Probenecid and hepatic transport of JH-ouabain in rats. and Sabih, K.: Combined G.C. Clinical Pharmacology and Therapeutics 9: 314–317 (1968). Drug-dependent parameters and plasma concentration-time profiles following intravenous and oral probenecid … Barza, M. and Weinstein, L.: Some determinants of the distribution of penicillins and Cephalosporins in the body. American Journal of Physiology 166: 625–640 (1951). Jr; Peters, L.; Woodward, R. and Verwey, W.F. COVID-19 is an emerging, rapidly evolving situation. Perel, J.M. ; Piall, E. and P. White, W.F. : Effects of bumetanide on cation and anion transport. 8600 Rockville Pike ; Pusey, N.W. Drug Metabolism and Disposition 1: 742–751 (1973b). II. Arthritis and Rheumatism 13: 458–711 (1970). Rennick, B. and Quebbemann, A.J. and Schwartz, M.A. Journal of Medicinal, Chemistry 9: 941–944 (1966). ; Smith, J. and Tyrell, W.F. and Dayton, P.G. Article  and Sparell, G.: Inhibition of dapsone excretion by probenecid. : Renal excretion of L-tyrosine and its derivatives. Influence of binding on drug metabolism and distribution. and Huang, K.C. Clin Pharmacokinet. Guerrini VH, Filippich LJ, English PB, Schneider J, Cao GR, Bourne DW. International Zeitschrift für Klinische Pharmakologie und Therapie Toxikologie 3: 182–189 (1970). and Loscher, W.: Distribution of Valproate across the interface between blood and cerebrospinal fluid. Israili, Z.H. European Journal of Clinical Pharmacology 12: 133–136 (1977). ; Matteucci, W.V. Welling, P.G. and Hogben, C.A.M. and Stocks, P.J. ; Skeggs, H. and Martin, C.M. : Biliary excretion of probenecid and its glucuronide. Listing a study does not mean it has been evaluated by the U.S. Federal Government. The half-life of probenecid in plasma (4 to 12 hours) is dose-dependent. Kinsella, J.L. Klein, J.O. Psychopharmacology 53: 315–318 (1977). Search for more papers by this author. Annals of the New York Academy of Sciences 179: 399–402 (1971). Roos, B.E. In the kidneys, probenecid is filtered at the glomerulus, secreted in the proximal tubule and reabsorbed in the distal tubule. : The metabolism of probenecid in man. ; Schuchardt, C.S. Forbes, M. and Becker, B.: The transport of organic anions by the rabbit eye. Probenecid is the classical competitive inhibitor of organic acid transport in the kidney and other organs. Korf, J. and Van Praag, H.M.: Amine metabolism in the human brain: Further evaluation of the probenecid test. Probenecid is the classical competitive inhibitor of organic acid transport in the kidney and other organs. and Perel, J.: Pharmacokinetic and clinical studies of carprofen in gout. ; Forrest, W.P. Probenecid is also involved in the block of transport of acidic metabolites of catecholamines, for example homovanillic and hydroxyindoleacetic acids, in the brain. Wolfson, W.Q. : Effect of hydrochlorothiazide on phosphorus during treatment with diphosphonate. Talseth, T.; Haegele, K.D. The maximum plasma probenecid concentration after 10 mg/kg orally averaged nearly 30 micrograms/ml. and Lockie, L.M. Aherne, G.W. Journal of Pharmacology and Experimental Therapeutics 140: 278–286 (1963). and Schimmel, N.H.: Renal clearances of penicillin, phenolsulphonphthalein, and para-amminohippurate (PAH) modified by “Benemid”. The protein binding of probenecid in pooled rat serum was estimated by equilibrium dialysis. Perel, J.M. © 2021 Springer Nature Switzerland AG. Coronavirus: ... Coadministeration of probenecid did not affect the terminal half-life or mean residence time values. ), intramuscular (i.m.) and McMahon, F.G.: Drug-induced hyperuricemia prevented by probenecid. Letter: Lancet 2: 1309 (1975). : Drug interactions with oral sulphonylurea hypoglycaemic drugs. : The effect of benemid (p-[di-n-propylsulfamyl]-benzoic acid) on uric acid metabolism in one normal and one gouty subject. and Gallagher, M.E. and Hitchings, G.H. and Wolny, J.D. : Management of gouty arthritis. A Study to Assess Pharmacokinetics of PF-04965842 and Its Metabolites and Effect of Probenecid in Healthy Participants. Participants will be confined to the clinic for approximately 32 days. Pharmacokinetics of oxypurinol and the pharmacodynamic effects of allopurinol alone or with probenecid for at least 7 days (500 or 1000 mg/day) in patients with gout. renal proximal tubule cells) and its use when combined with penicillins resulted in elevated blood levels of the penicillin and a longer duration of antimicrobial action. American Journal of Medicine 63: 723–728 (1977). ; Perel, J.M. Journal of Pharmaceutical Sciences 67: 434–436 (1978). Treatment with probenecid did not affect pharmacokinetic values of cefazolin. We studied adefovir clearance in rat after inhibition of transporters by probenecid and in TR- rats, in which MRP2 is lacking. and high resolution mass spectrometric determination with probenecid. Bulletin of the New York Academy of Medicine 27: 144–164 (1951a). : Effect of probenecid on the blood levels and urinary excretion of cefamandole. : Two hepatic cytoplasmic protein fractions, Y and Z, and their possible role in the hepatic uptake of bilirubin, sulfobromophthalein, and other anions. Bulletin on Rheumatic Diseases 1: 11–12 (1951b). Journal of Pediatrics 42: 292–300 (1953). and Ross, C.R. British Journal of Clinical Pharmacology 8: 491–495 (1979). ; Dayton, P.G. and Weinstein, L.: Penetration of antibiotics into fibrin loci in vivo. : Benemid and carinamide: Comparison of effect of para-aminosalicylic acid (PAS) plasma concentrations. : Probenecid in CSF and plasma of rabbits and dogs measured by radioimmunoassay. American Journal of Medicine 36: 743–762 (1964). ; Russo, H.F. and Wilhoyte, K.M. Jr: The determination of probenecid (Benemid) in body fluids. Clinical Pharmacokinetics of Probenecid. : Effect of probenecid on serum cefoxitin concentrations. : Plasma and cerebrospinal fluid probenecid concentrations as related to accumulation of acidic biogenic amine metabolites in man. Probenecid has been associated with minor serum aminotransferase elevations and very rarely with hypersensitivity reactions which, even more rarely, can be accompanied by acute liver injury. Skeith, M.D. This study was designed to determine bioequivalence with … A clinical and pharmacokinetic study. Werdinius, B.: Effect of probenecid on the levels of monamine metabolites in the rat brain. ; Hatfield, A.R.W. SummaryA review of the clinical applications and of the disposition of probenecid in man, including drug interactions, is presented.Probenecid is the classical competitive inhibitor of organic acid transport in the kidney and other organs. Furthermore, no clinical studies have been done on the pharmacokinetics of probenecid in pregnancy. Allen, B.W. Journal of Pharmacology and Experimental Therapeutics 111: 385–394 (1954a). Plasma protein binding of probenecid was extensive, with 99.9% of the drug bound at plasma probenecid concentrations of 10 micrograms/ml. Recker, R.R. Life Sciences 9: 1337–1343 (1970). Pharmacokinetics of probenecid in sheep. ; Dow, R.C. Clinical Pharmacology and Therapeutics 24: 548–554 (1978b). Clinical Pharmacology and Therapeutics 22: 395–401 (1977). and Finland, M.: Ancillin (2-biphenylpenicillin), antimicrobial activity and clinical pharmacology. : Pharmacology of gout; in Lowenthal and Major (Eds) Clinical Therapeutics, pp.343–346 (Grune and Stratton, New York 1978). Practical and theoretical considerations. 8 The pharmacokinetics of probenecid were at that time well known and documented, 9 although the substance had never shown up in connection with doping control. Careers. Beyer, K.H. and Martin, C.M. Antimicrobial Agents and Chemotherapy 5: 114–118 (1974). Bulletin of the Johns Hopkins Hospital 106: 333–340 (1960). The significance of metabolic sites, especially lack of ring hydroxylation. and Perkins, W.H. Burns, J.J.; Cucinell, S.A.; Koster, R. and Conney, A.H.: Application of drug metabolism to drug toxicity studies. Table I. Clinically important drug interactions with probenecid - "Clinical Pharmacokinetics of Probenecid" and Beyer, K.H. and Perel, J.M. Beyer, K.H. Zacchei, A.G. and Weidner, L.: GLC determination of probenecid in biological fluids. American Journal of Ophthalmology 50: 867–875 (1960). ; Yeh, K.C. and Dayton, P.G. Beyer, K.H. and Beyer, K.H. : Inhibitors of urinary excretion of iodine131-labeled corticotropin by probenecid. 51, pp.211–255 (Springer-Verlag, Berlin 1978). : Urate Excretion: Drug Interactions. PubMed  and Healey, L.A.: The renal excretion of indomethacin and its inhibition by probenecid. A review of the clinical applications and of the disposition of probenecid in man, including drug interactions, is presented. Clinical Pharmacokinetics : Uric acid metabolism and gout. Psychopharmacologia 35: 83–90 (1974). At that time doping analysis was mainly a targeted analysis. Journal of Pharmacology and Experimental Therapeutics 119: 361–369 (1957).

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