PHARMACOKINETICS OF

BENZODIAZEPINES
Absorption & Distribution:
• Since Benzodiazepines are lipophyllic, they are rapidly and completely absorbed after oral administration.
• Due to the same reason, Benzodiazepine can also penetrate into the CNS.

Duration of action:
The Benzodiazepines are divided into three classes;
1. Short acting 2) Intermediate acting 3) Long acting
This classification is necessarily does not corelate with the actual half-life.

Fate:
• Most benzodiazepines ( Chlordiazepoxide, diazepam) are metabolized with hepatic microsomal system to
compounds that are also active. For these benzodiazepines, the apparent half-life of the drug represents the
combined actions of the parent drug and its metabolite.
• The drug action is not only decreased by excretion but also by redistribution.
• The benzodiazepines are excreted as glucronides or oxidized metabolites.
• Benzodiazepines are not recommended in pregnancy because they can cross the placenta and may depress the
CNS of the newborn.
• The pharmacokinetics is simplified in the following manner.
 DRUG INTERACTION WITH BENZODIAZEPINES
Traditional benzodiazepines can be associated with overdoses and fatal consequences when combined with alcohol,
opioids, other sedatives, or illicit drugs. While it is rare that an overdose of benzodiazepines by itself would be fatal,
when combined with other drugs that depress the central nervous system, the risk dramatically increases.
Examples of other drugs that may be additive to the central nervous system depression if combined with
benzodiazepine include:

MAO
phenothiazines opioids barbiturates
inhibitors

antidepressant alcohol Illicit drugs