Pharmacokinetics, metabolism and excretion of megazol in a Trypanosoma brucei gambiense primate model of human African trypanosomiasis: Preliminary study

Arzneimittel-Forschung/Drug Research

Volumn 50, Issue 2, 2000, Pages 158-162

  Enanga, Bertin ^a,b   Ndong, Jerôme Mezui Me ^c   Boudra, Hamid ^a   Debrauwer, Laurent ^d   Dubreuil, Guy ^c   Bouteille, Bernard ^b   Chauvière, Gérard ^e   Labat, Christian ^a   Dumas, Michel ^b   Périé, Jacques ^e   Houin, Georges ^a,f  

^a UNIVERSITÉ DE TOULOUSE   (France)

^b FR 3503 GEIST EA 1069 Laboratoire de Chimie des Substances Naturelles GDR CNRS 3049 Faculte de Ph   (France)

^c Ctr Intl de Rech Medicales de Fr   (France)

^d Laboratoire des Xenobiotiques   (France)

^e CNRS   (France)

^f CHU RANGUEIL   (France)

Author keywords

CAS 145 63 1; CAS 19622 55 0; Megazol, cerebrospinal fluid, elimination, metabolism, pharmacokinetics, primate; Suramin; Trypanosoma brucei gambiense, primate

Indexed keywords

2 AMINO 5 (1 METHYL 5 NITRO 2 IMIDAZOLYL) 1,3,4 THIADIAZOLE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD BRAIN BARRIER; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG ELIMINATION; DRUG METABOLISM; FEMALE; MALE; NONHUMAN; TRYPANOSOMA BRUCEI; TRYPANOSOMIASIS;

EID: 0003044419     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1300182     Document Type: Article

References (13)

1. André, L. J. Treatment of amoebiasis by secnidazole. Ann. Gastroenterol. Hépathol. 15, 221 (1979)
2. Bouteille, B., Marie-Daragon, A., Chauvière, G. et al., Effect of megazol on Trypanosoma brucei brucei acute and subacute infections in Swiss mice. Acta Trop. 60, 73 (1995)
3. Bouteille, B., Keita, M., Enanga, B. et al., Experimental models for new chemotherapeutic approches to human African trypanosomiasis, in: Progress in Human African Trypanosomiasis, Sleeping Sickness, M. Dumas et al. (eds.), pp. 289-300, Edition Springer-Verlag, Paris (1999)
4. 3H-megazol. J. Labelled Compounds Radiopharm. 41, 47 (1998)
5. Enanga, B., Boudra, H., Chauvière, G. et al., Pharmacokinetics, metabolism and excretion of megazol, a new potent trypanocidal in animals. Arzneim.-Forsch./Drug Res. 49 (I), 441 (1999)
6. Enanga, B., Keita, M., Chauvière, G. et al., Megazol combined with suramin: a chemotherapy regimen which reversed the CNS pathology in a model of Human African Trypanosomiasis in mice. Trop. Med. Int. Health 3, 736 (1998)
7. Enanga, B., Labat, C., Boudra, H. et al., Simple high-performance liquid Chromatographic method to analyse megazol in human and rat plasma. J. Chromatogr. B 696, 261 (1997)
8. Friedheim, E. A. H., Mel B in the treatment of human trypanosomiasis. Am. J. Trop. Med. 29, 173 (1949)
9. Gillis, J. C., Wiseman, L. R., Secnidazole: a review of its antimicrobial activity, pharmacokinetic properties and therapeutic use in the management of protozoal infections and bacterial vaginosis. Drugs 51, 621 (1996)
10. Nau, R., Sörgel, F., Prange, H. W., Pharmacokinetic optimisation of the treatment of bacterial central nervous system infections. Clin. Pharmacokinet. 35, 223 (1998)
11. Piquette-Miller, M., Pak, a., Kim, H. et al., Decreased expression and activity of P-glycoprotein in rat liver during acute inflammation. Pharm. Res. 15, 706 (1998)
12. Smith, D. H., Pepin, J., Stich, A. H. R., Human African trypanosomiasis: an emerging public health crisis. Br. Med. Bull. 54, 341 (1998)
13. Van Nieuwenhove, S., Present strategies in the treatment of human African trypanosomiasis, in: Progress in Human African Trypanosomiasis, Sleeping Sickness, M. Dumas et al. (eds), pp. 253-280, Edition Springer-Verlag, Paris (1999)