Pharmacokinetics of diltiazem in selected animal species and human beings

Pharmacokinetics of diltiazem in selected animal species and human beings

The absorption, distribution and elimination of diltiazem hydrochloride in rodent and canine species are reviewed. The drug is well absorbed but undergoes first pass metabolism after oral administration. Diltiazem is extensively distributed, and 52 to 81 percent is bound to serum protein, depending...

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Bibliographic Details
Published in:The American journal of cardiology Vol. 49; no. 3; pp. 525 - 528
Main Authors: Piepho, Robert W., Bloedow, Duane C., Lacz, Joseph P., Runser, Dennis J., Dimmit, Daniel C., Browne, Ronald K.
Format: Journal Article
Language:English
Published: United States Elsevier Inc 01-01-1982
Subjects:
Animals
Benzazepines - blood
Biological Availability
Biotransformation
Cebidae
Diltiazem - blood
Dogs
Female
Humans
Intestinal Absorption
Maternal-Fetal Exchange
Metabolic Clearance Rate
Mice
Pregnancy
Protein Binding
Rats
Rats, Inbred Strains
Tissue Distribution
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Summary:The absorption, distribution and elimination of diltiazem hydrochloride in rodent and canine species are reviewed. The drug is well absorbed but undergoes first pass metabolism after oral administration. Diltiazem is extensively distributed, and 52 to 81 percent is bound to serum protein, depending on the species studied. Diltiazem is metabolized in the liver by several pathways; deacetylation, N-demethylation, and O-demethylation are the primary degradative steps. The metabolites are excreted in urine and feces, indicating that biliary excretion occurs. There is some evidence for enterohepatic cycling. Diltiazem is rapidly eliminated (t 1/2 = 2.24 hours) in beagle dogs, and the relatively short half-life appears to be a result of the high level of plasma clearance (46.1 ± 4.8 ml/min/per kg body weight). A comparison of the plasma diltiazem clearance with hepatic blood flow in the dog indicates that the drug is eliminated at a rate dependent on hepatic blood flow.
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ISSN:0002-9149
1879-1913
DOI:10.1016/S0002-9149(82)80006-4