Pharmacology of Temazepam (Restoril) ; Mechanism of action, Pharmacokinetics, Uses, Effects

Tue, 26 Aug 2025 18:55:19 +0000

Temazepam, marketed under the brand name Restoril, is a benzodiazepine used primarily for the short-term treatment of insomnia. Here's an overview of its pharmacology:

Mechanism of Action
GABA-A Receptor Agonism: Temazepam enhances the activity of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) by binding to the benzodiazepine site of the GABA-A receptor complex. This increases chloride conductance, leading to neuronal hyperpolarization and a decrease in neuronal excitability, resulting in sedative and hypnotic effects2.

Indications
Insomnia: Temazepam is indicated for the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings2.

Dosage and Administration
Initial Dose: The typical starting dose for adults is 7.5 to 30 mg taken orally at bedtime.

Maximum Dose: The maximum recommended dose is 30 mg per day.

Adverse Effects
Common Side Effects: Include dizziness, drowsiness, headache, and gastrointestinal disturbances.

Serious Side Effects: Include complex sleep behaviors (e.g., sleep-walking, sleep-driving), which may result in serious injuries, including death.

Pharmacokinetics
Absorption: Temazepam is well absorbed from the gastrointestinal tract, with minimal first-pass metabolism.

Metabolism: It is extensively metabolized in the liver, primarily by conjugation.

Excretion: The metabolites are primarily excreted in the urine.

Half-Life: The elimination half-life of temazepam is approximately 8 to 20 hours