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Titolo:
Pharmacokinetics, metabolism and excretion of megazol in a Trypanosoma brucei gambiense primate model of human African trypanosomiasis - Preliminary study
Autore:
Enanga, B; Ndong, JMM; Boudra, H; Debrauwer, L; Dubreuil, G; Bouteille, B; Chauviere, G; Labat, C; Dumas, M; Perie, J; Houin, G;
Indirizzi:
Fac Pharmaceut Sci, Lab Cinet Xenobiot, Toulouse, France Fac Pharmaceut Sci Toulouse France Lab Cinet Xenobiot, Toulouse, France Fac Med, Inst Epidemiol Neurol & Neurol Trop, Limoges, France Fac Med Limoges France Epidemiol Neurol & Neurol Trop, Limoges, France Ctr Int Rech Med Franceville, Franceville, Gabon Ctr Int Rech Med Franceville Franceville Gabon ille, Franceville, Gabon Lab Xenobiot, Toulouse, France Lab Xenobiot Toulouse FranceLab Xenobiot, Toulouse, France Univ Toulouse 3, CNRS, UMR 5623, Grp Chim Organ Biol, F-31062 Toulouse, France Univ Toulouse 3 Toulouse France F-31062 n Biol, F-31062 Toulouse, France
Titolo Testata:
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
fascicolo: 2, volume: 50, anno: 2000,
pagine: 158 - 162
SICI:
0004-4172(200002)50:2<158:PMAEOM>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
INFECTIONS; MICE;
Keywords:
CAS 145-63-1; CAS 19622-55-0; megazol, cerebrospinal fluid, elimination, metabolism, pharmacokinetics, primate; suramin; Trypanosoma brucei gambiense, primate;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
13
Recensione:
Indirizzi per estratti:
Indirizzo: Houin, G CHU Rangueil, Lab Pharmacocinet & Toxicol Clin, 1 Ave Jean Poulthes, F-31054 Toulouse, France CHU Rangueil 1 Ave Jean Poulthes Toulouse France F-31054 France
Citazione:
B. Enanga et al., "Pharmacokinetics, metabolism and excretion of megazol in a Trypanosoma brucei gambiense primate model of human African trypanosomiasis - Preliminary study", ARZNEI-FOR, 50(2), 2000, pp. 158-162

Abstract

The pharmacokinetics of megazol (2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazol, CAS 19622-55-0) was investigated after a 100 mg/kg oral administration to six primates infected with Trypanosoma brucei gambiense. The plasma levels of megazol were between 0.2 mu g/ml and 46 mu g/ml 24 h after dosing in all animals. In animals with prolonged infection, megazol absorption was accelerated (T-max was 4 h compared with 8 h, for day 53 and day 39 post inoculation) but the amount absorbed was not modified. The megazol concentrations in the cerebrospinal fluid represented between 5.5 % and 10.6 %, of the plasma levels at the same rimes. Unchanged megazol was eliminated predominantly via the kidneys: 46-96 % of the ingested dose was recovered in the urine, compared with 0-5 % in the faeces. Furthermore, this urinary elimination of megazol was altered in animals with prolonged infections. In the urine, 4 unknown metabolites were observed, unchanged megazol wascharacterized by LC-MS/MS. This study indicates that megazol crosses the blood-brain barrier after oral administration. Prolonged infections affect the absorption of megazol and its urinary elimination.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 22:57:29