VOPROSY MEDITSINSKOI KHIMII (ISSN 0042-8809)

Pharmacokinetic of benzimidazole derivatives

   
Spasov A.A.1, Smirnova L.A.1, Iezhitsa I.N.1, Sergeeva S.A.2, Ozerov A.A.1

1. Research of Pharmacology, Volgograd Medical Academy
2. Pharmacology, Russian Academy of Medical Sciences
Section: Review
PubMed Id: 12243082
Year: 2002  Volume: 48  Issue: 3  Pages: 233-258
Pharmacokinetic properties of benzimidazole derivatives drug possessing antipsychotic, actoprotector, antiarrhythmic, antiulcerogenic, antiallergic, uricosuric, anthelmintic activities have been summarized. Pharmacokinetics of benzimidazole derivatives used in veterinary practice as anthelmintic drugs is also considered. Benzimidazoles derivatives are characterised by multicompartment and ambiguous pharmacokinetic models. The derivatives of benzimidazoles are subjected to the first pass metabolism in the liver, and, therefore, they are converted to both active, and inactive metabolites. It is necessary to take into account for coadministration of benzimidazoles with other drugs. Hepatoduodenal circulation and repeated adsorption of unchanged drug and its metabolites in the gut is observed for benzimidazole. Many derivatives of benzimidazoles are characterised by rather low absolute bioavailability during peroral intake (from 2 up to 60%). Benzimidazsole derivative may bind to proteins and cell elements of blood. More often pharmacokinetic profile of benzimidazoles is linear for low doses, however, at high doses the linearity is lost. For animals and men pharmacokinetic models are always nearly identical.
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Spasov A.A., Smirnova L.A., Iezhitsa I.N., Sergeeva S.A., Ozerov A.A. (2002) Voprosy meditsinskoi khimii, 48(3), 233-258.
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