Sarmazenil

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Sarmazenil


Sarmazenil is a benzodiazepine derivative drug that is a partial inverse agonist of the GABA_A receptor. It was developed by Hoffmann-La Roche in the 1980s as a potential treatment for benzodiazepine dependence and withdrawal syndrome.

Pharmacology[edit | edit source]

Sarmazenil acts as a partial inverse agonist at the GABA_A receptor, meaning it produces effects opposite to those of benzodiazepine drugs, which are GABA_A receptor agonists. This makes it useful in the treatment of benzodiazepine dependence and withdrawal syndrome, as it can help to reverse the effects of benzodiazepine drugs and reduce withdrawal symptoms.

Clinical Use[edit | edit source]

Sarmazenil has been studied in clinical trials for the treatment of benzodiazepine dependence and withdrawal syndrome. However, it has not been widely adopted in clinical practice, possibly due to its partial inverse agonist activity, which can potentially cause withdrawal symptoms in patients who are dependent on benzodiazepines.

Side Effects[edit | edit source]

As a partial inverse agonist of the GABA_A receptor, sarmazenil can potentially cause side effects such as anxiety, restlessness, and insomnia. These side effects are similar to those of benzodiazepine withdrawal syndrome, which can make it difficult to distinguish between the effects of the drug and the symptoms of withdrawal.

See Also[edit | edit source]

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Contributors: Prab R. Tumpati, MD