Biomaterial Database

Pharmacokinetics and metabolism of diltiazem in rats following a single intra-arterial or single oral dose. 1994

B C Tsui, and J D Feng, and S J Buckley, and P K Yeung

College of Pharmacy, Faculty of Health Professions, Dalhousie University, Halifax, Nova Scotia, Canada.

Diltiazem (DTZ) 20 mg/kg was given to male Sprague-Dawley rats either orally (p.o.) or intra-arterially (i.a.) over a 5 min period (n = 6 for each group). Plasma concentrations of DTZ and its major basic metabolites were determined by high performance liquid chromatography assay (HPLC) as previously described over a 10 h period. The major metabolites found in the rat plasma were M2, followed by M6, MA, M1, and then M4. The metabolite Mx was measurable only in some of the plasma samples, and MB was not detected in this species. The mean apparent half-life (t1/2) of the measurable metabolites were longer than the parent DTZ. The metabolism profiles were qualitatively similar between the two routes of administration. Quantitatively, however, the plasma concentrations of the metabolites were higher after the i.a. route. These results are in agreement with a previous study reported in rabbits, and suggest that deacetylation of DTZ and MA in the blood is extremely important in this species.

UI	MeSH Term	Description	Entries
D007261	Infusions, Intra-Arterial	Regional infusion of drugs via an arterial catheter. Often a pump is used to impel the drug through the catheter. Used in therapy of cancer, upper gastrointestinal hemorrhage, infection, and peripheral vascular disease.	Infusions, Regional Arterial,Infusions, Intra Arterial,Infusions, Intraarterial,Arterial Infusion, Intra,Arterial Infusion, Regional,Arterial Infusions, Intra,Arterial Infusions, Regional,Infusion, Intra Arterial,Infusion, Intra-Arterial,Infusion, Intraarterial,Infusion, Regional Arterial,Intra Arterial Infusion,Intra Arterial Infusions,Intra-Arterial Infusion,Intra-Arterial Infusions,Intraarterial Infusion,Intraarterial Infusions,Regional Arterial Infusion,Regional Arterial Infusions
D008297	Male		Males
D004110	Diltiazem	A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.	Aldizem,CRD-401,Cardil,Cardizem,Dilacor,Dilacor XR,Dilren,Diltiazem Hydrochloride,Diltiazem Malate,Dilzem,Tiazac,CRD 401,CRD401
D004334	Drug Administration Schedule	Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.	Administration Schedule, Drug,Administration Schedules, Drug,Drug Administration Schedules,Schedule, Drug Administration,Schedules, Drug Administration
D000284	Administration, Oral	The giving of drugs, chemicals, or other substances by mouth.	Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D017207	Rats, Sprague-Dawley	A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.	Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus