Temazepam - Pharmacokinetics


Oral administration of 15 to 45 mg temazepam in man resulted in rapid absorption with significant blood levels achieved in less than 30 minutes and peak levels at 2 to 3 hours. In a single and multiple dose absorption, distribution, metabolism, and excretion (ADME) study, using tritium (3H) labelled drug, temazepam was well absorbed and found to have minimal (8%) first pass drug metabolism. There were no active metabolites formed and the only significant metabolite present in blood was the O-conjugate. The unchanged drug was 96% bound to plasma proteins. The blood level decline of the parent drug was biphasic with the short half-life ranging from 0.4-0.6 hours and the terminal half-life from 3.5–18.4 hours (mean 8.8 hours), depending on the study population and method of determination.

Temazepam has very good bioavailability with almost 100% being absorbed from the gut. The drug is metabolized through conjugation and demethylation prior to excretion. Most of the drug is excreted in the urine, with about 20% appearing in the feces. The major metabolite was the O-conjugate of temazepam (90%); the O-conjugate of N-desmethyl temazepam was a minor metabolite (7%).

Read more about this topic:  Temazepam

Other articles related to "pharmacokinetics":

Seletracetam - Pharmacodynamics and Pharmacokinetics
... Seletracetam exhibits first-order mono-compartmental pharmacokinetics, in which there is a simple linear relationship between the amount of drug that was administered, the time ... This contrasts the nonlinear pharmacokinetics typical of previously available anticonvulsants such as phenobarbital, phenytolin, valproate and carbamazepine ...