Nitrazepate

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Nitrazepate

Chemical structure of Nitrazepate

Nitrazepate is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative, and muscle relaxant properties. It is primarily used in the treatment of anxiety disorders and epilepsy.

Pharmacology

Nitrazepate acts on the central nervous system by enhancing the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABA_A receptor. This action results in increased neuronal inhibition and produces the characteristic effects of benzodiazepines, such as sedation and anxiolysis.

Mechanism of Action

The drug binds to specific sites on the GABA_A receptor, which is a ligand-gated ion channel. This binding increases the frequency of chloride ion channel opening events, leading to hyperpolarization of the neuron and decreased neuronal excitability.

Clinical Uses

Nitrazepate is used in the management of:

Side Effects

Common side effects of nitrazepate include:

Long-term use can lead to tolerance and dependence, and abrupt discontinuation may result in withdrawal symptoms.

Contraindications

Nitrazepate should not be used in individuals with:

Interactions

Nitrazepate can interact with other central nervous system depressants, such as alcohol, opioids, and other benzodiazepines, leading to enhanced sedative effects.

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Contributors: Prab R. Tumpati, MD