Pharmacokinetics of fostedil, a new calcium antagonist, in beagle dogs following oral and intravenous administration.
Twelve adult beagle dogs received both an oral and intravenous dose (12 mg/kg) of fostedil in a cross-over design. The plasma levels and urinary excretion of intact fostedil were measured, and the pharmacokinetic parameters of the drug were defined. The results indicate that fostedil was at least 68% bioavailable after an oral dose given as a suspension or solution. The terminal half-life was about 7-8 h. The in vitro protein binding, at concentrations of 0.1-100 micrograms/mL, ranged from 95 to 97%. The binding was not concentration dependent, and saturation of the binding sites was not apparent at concentrations up to 100 micrograms/mL. Excretion of unchanged drug from the kidneys accounted for only a small percentage of drug clearance.
D000284:Administration, Oral; D000818:Animals; D052160:Benzothiazoles; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000378:metabolism*; D002214:Capsules; D004285:Dogs; D005260:Female; D006207:Half-Life; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D011485:Protein Binding; D012996:Solutions; D013535:Suspensions; D013844:Thiazoles / Q000008:administration & dosage / Q000378:metabolism*
D052160:Benzothiazoles; D002121:Calcium Channel Blockers; D002214:Capsules; D012996:Solutions; D013535:Suspensions; D013844:Thiazoles; C035950:fosfedil