57 out of 93
Flumazenil is (DNB Dec 2011)
|A||Agonist of diazepam|
Ans. B Diazepam antagonists
- Antagonism– When one drug decreases or inhibits the action of another, they are antagonistic. Usually in an antagonistic pain, one drug is inactive as such but decreases the effect of the other.
- Flumazenil, an imidazo-benzodiazepine, is a specific and competitive antagonist of benzodiazepines at benzodiazepine receptors.
- Flumazenil– It is a BZD analogue, which has little intrinsic activity (practically no effect on normal subjects), but competes with BZD receptor and reverses their depressant or stimulant effects respectively.
- It abolishes the hypnogenic, psychomotor, cognitive and EEG effects of BZDs. At higher doses it has some week BZD agonist like as well as an inverse agonist like activity, but these are of no clinical significance.
- On IV injection, action of flumazenil starts in seconds and lasts for
1–2 hr; elimination t1/2 is 1 hr, due to rapid metabolism.
- Uses: To reverse BZD anesthesia