Homework SourseA inactive active B active active C active inactive D inacti
A. inactive; active
B. active; active
C. active; inactive
D. inactive; inactive
| Generally speaking, the long-acting benzodiazepines are biotransformed into _____ products; the short-acting benzodiazepines are biotransformed into ______ products. |
Solution
C.active; inactive
Benzodiazepines, barbiturates, Ethchlorvynhol, Choral Hydrate, Glutethimide, Methypryion etc are CNS depressants and these will acts on the receptors for the neurotransmitter gamma-aminobutryic acid (GABA). Bothe short-acting drugs and long acting drugs are available and short acting drugs will last for a few hours and long-acting drugs can last up to two to three days.
These benzodiazepines will be metabolized by hepatic microsomal enzymes. They undergo biotransformation like N-dealkylation and aliphatic hydroxylation and then will conjugated to inactive glucuronides to get excreted in the urine.
The long acting benzodiazepines (clorazepate, chlordiazepoxide, diazepam etc) will first dealkylated to the active compound called N-desmethyldiazepam and this will have a half life of 30 to 200 hours and will show long duration of action.
Whereas the short acting benzodiazepines will be directly conjugated, that is the reason why this conjugated products will be essentially inactively and will be water soluble and our kidneys will clear them easily and readily.
