Amodiaquine

0 comments
Absorption Rapidly absorbed following oral administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic biotransformation to desethylamodiaquine (the principal biologically active metabolite) is the predominant route of amodiaquine clearance with such a considerable first pass effect that very little orally administered amodiaquine escapes untransformed into the systemic circulation.
Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 2C8 desethylamodiaquine N-deethylation 2000 0
Route of elimination Not Available
Half life 5.2 ± 1.7 (range 0.4 to 5.5) minutes
Clearance Not Available
Toxicity LD50 (mouse, intraperitoneal) 225 mg/kg, LD50 (mouse, oral) 550 mg/kg. Symptoms of overdose include headache, drowsiness, visual disturbances, vomiting, hypokalaemia, cardiovascular collapse and cardiac and respiratory arrest. Hypotension, if not treated, may progress rapidly to shock. Electrocardiograms (ECG) may reveal atrial standstill, nodal rhythm, prolonged intraventricular conduction time, broadening of the QRS complex, and progressive bradycardia leading to ventricular fibrillation and/or arrest.
Affected organisms
  • Plasmodium

0 comments:

Post a Comment

Copyright 2011 Pharmacokinetics of Drugs.
Blogger Template by Noct.