Pharmacokinetics of diltiazem in selected animal species and human beings
| Autor: | Robert W. Piepho, Dennis J. Runser, Duane C. Bloedow, Daniel C. Dimmit, Ronald K. Browne, Joseph P. Lacz |
|---|---|
| Rok vydání: | 1982 |
| Předmět: |
medicine.medical_specialty
Metabolic Clearance Rate Biological Availability Urine Pharmacology Beagle Intestinal absorption First pass effect Diltiazem Mice Dogs Pharmacokinetics Oral administration Pregnancy Internal medicine medicine Animals Humans Tissue Distribution Maternal-Fetal Exchange Biotransformation business.industry Rats Inbred Strains Benzazepines Rats Intestinal Absorption Anesthesia Cebidae Cardiology Diltiazem hydrochloride Female Cardiology and Cardiovascular Medicine business medicine.drug Protein Binding |
| Zdroj: | The American journal of cardiology. 49(3) |
| ISSN: | 0002-9149 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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