[Pharmacokinetics and metabolism of gallopamil].
Despite its almost complete absorption following oral administration, gallopamil has an absolute bioavailability of only 15% due to an extensive hepatic first-pass metabolism. During multiple oral dosing bioavailability increases to approximately 25% indicating a partial saturation of first-pass metabolism. Since the half-life time of gallopamil is on average 3-6 h a minimum of three times daily dosing of the instant-release 50 mg tablet is required in order to maintain therapeutic plasma concentrations. The sustained-release 100 mg tablet which recently became available has a relative bioavailability comparable to the instant release preparation. Due to the delayed drug liberation therapeutic plasma concentrations are maintained for 24 h following once or twice daily administration of this drug preparation.
Eichelbaum
M
M
Dr. Margarete Fischer-Bosch-Institut für Klinische Pharmakologie, Stuttgart.
D000284:Administration, Oral; D001682:Biological Availability; D005711:Gallopamil / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D007262:Infusions, Intravenous; D008657:Metabolic Clearance Rate / Q000502:physiology
D005711:Gallopamil
Pharmakokinetik und Metabolismus von Gallopamil.