Nepinalone

Nepinalone

Nepinalone is a sedative and analgesic drug that belongs to the cyclopyrrolone family of nonbenzodiazepine GABA_A receptor agonist drugs. Nepinalone was developed in the late 1980s and is used primarily in the treatment of insomnia and as a premedication for surgery or medical procedures.

Pharmacology

Nepinalone acts as a full agonist at the benzodiazepine site of the GABA_A receptor, leading to increased activity of the inhibitory neurotransmitter GABA. This results in sedative, anxiolytic, and muscle relaxant effects. The drug has a rapid onset of action, with effects typically beginning within 15 minutes of administration and lasting for several hours.

Medical Uses

Nepinalone is primarily used for the short-term treatment of insomnia. It is also used as a premedication for surgery or medical procedures to reduce anxiety and induce sedation. In some cases, it may be used for the treatment of certain types of seizure disorders.

Side Effects

Common side effects of Nepinalone include drowsiness, dizziness, and impaired coordination. Less common side effects can include amnesia, confusion, and changes in mood or behavior. Long-term use of Nepinalone can lead to tolerance, dependence, and withdrawal symptoms upon discontinuation.

History

Nepinalone was developed in the late 1980s as part of a new class of nonbenzodiazepine GABA_A receptor agonists. These drugs were designed to have the beneficial effects of benzodiazepines, such as sedation and anxiolysis, without the associated risks of dependence and withdrawal.

See Also

• Cyclopyrrolone
• GABA_A receptor
• Insomnia
• Benzodiazepine

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