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Pharmacokinetics of methylamine and its metabolite formaldehyde in animals Article Abstract

Abstract by : TsingHua
Visits : 18  words: 300   Published: April 25, 2006
AIM For further understanding the physiological and pathological significance of plasma semicarbazide-sensitive amine oxidase(SSAO) activity and endogenous formaldehyde. METHODS Plasma SSAO activity,methylamine hydrochloride(MA) and its metabolite formaldehyde(FA) concentrations were determined by HPLC after iv MA to mice,rats and rabbits. RESULTS Plasma SSAO activities of mice, rats and rabbits were(4.1±1.0), (2.0±0.3) and (326±24)μmol·h -1 ·L -1 ,respectively. MA was distributed and cleared quickly in mice,rats and rabbits. After iv 4.2 mg·kg -1 MA to mice,FA increased and reached maximum concentration between 20-40 min,and then eliminated slowly. However,FA did not changed obviously compared with its baseline in rats after iv 4.2 mg·kg -1 MA. In rabbits, Cl decreased with the increase in MA dosage and AUC was not in proportion to the dosage after iv 2.3,9.6 and 36.8 mg·kg -1 MA,showing the characteristics of nonlinear kinetics. FA was distributed rapidly,AUC was in proportion to MA dosage and Cl did not change obviously. However,k_e decreased and t_ 1/2 extended significantly with the increase in MA dosage. CONCLUSION The pharmacokinetics of MA was similar, but its metabolite FA was different in mice, rats and rabbits. The difference of MA dosage administrated may change the pharmacokinetics of MA and have an impact on FA′s metabolism.

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