Temazepam

• Approved Indications:
• Short-term treatment of insomnia characterized by difficulty falling asleep, frequent awakenings during the night, or early morning awakenings.
• Indicated when insomnia results in significant distress or impairment in daytime functioning.
• Off-label Uses:
• Occasionally used as a premedication for sedation before minor procedures.
• Occasionally prescribed for anxiety-related sleep disturbances (clinical discretion required).

• Adults:
• Typical oral dose: 7.5 mg to 30 mg taken once daily at bedtime.
• Treatment duration usually limited to 7–10 days, not exceeding 2–4 weeks to minimize risk of dependence.
• Elderly or Debilitated Patients:
• Start at lower dose (e.g., 7.5 mg at bedtime).
• Careful monitoring recommended due to increased sensitivity and fall risk.
• Pediatrics:
• Safety and efficacy not established; use not recommended.
• Renal/Hepatic Impairment:
• Use with caution; no formal dose adjustments but close clinical monitoring advised.
• Administration Route:
• Oral, swallowed whole with water approximately 30 minutes before sleep.

Temazepam is a benzodiazepine that potentiates the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) by binding to GABA_A receptor sites in the central nervous system. This enhances chloride ion influx into neurons, causing hyperpolarization and reduced neuronal excitability. The result is sedative-hypnotic, anxiolytic, muscle-relaxant, and anticonvulsant effects, with the hypnotic property utilized for inducing and maintaining sleep.

• Absorption: Rapid oral absorption; peak plasma concentrations reached within 1–2 hours.
• Bioavailability: Approximately 90%.
• Distribution: Widely distributed, crosses blood-brain barrier; about 96% plasma protein bound.
• Metabolism: Primarily hepatic via conjugation to inactive metabolites; minimal involvement of cytochrome P450 enzymes.
• Half-life: Approximately 8–15 hours.
• Elimination: Metabolites excreted renally.

• Pregnancy: Classified as FDA Pregnancy Category D. Contraindicated due to risk of fetal harm including floppy infant syndrome and neonatal withdrawal.
• Lactation: Excreted in breast milk; potential for sedation and respiratory depression in infants. Breastfeeding is not recommended during treatment.

• Benzodiazepine hypnotic.

• Known hypersensitivity to temazepam or other benzodiazepines.
• Acute narrow-angle glaucoma.
• Severe respiratory insufficiency.
• Severe hepatic impairment.
• Myasthenia gravis.
• Sleep apnea syndrome.

• Risk of dependence, tolerance, and withdrawal symptoms; limit duration of therapy.
• Increased risk of CNS depression, respiratory depression, and falls in elderly or debilitated patients.
• Avoid concomitant use with other CNS depressants (e.g., alcohol, opioids).
• Use caution in patients with a history of substance abuse, depression, or suicidal ideation.
• Monitor for paradoxical reactions such as agitation, aggression, or hallucinations.
• Gradual dose tapering recommended to discontinue.

• Common: Drowsiness, dizziness, fatigue, headache, impaired coordination, daytime sedation.
• Gastrointestinal: Nausea, dry mouth.
• CNS: Confusion, memory impairment, paradoxical reactions (e.g., agitation).
• Rare/Serious: Respiratory depression, dependence, withdrawal seizures, severe allergic reactions.

• Additive CNS depressant effects with alcohol, opioids, barbiturates, antihistamines, antipsychotics, and antidepressants.
• Minimal CYP450 involvement; however, enzyme inducers/inhibitors may alter temazepam metabolism slightly.
• Caution with other respiratory depressants.

• Guidelines emphasize short-term use only, prioritizing non-pharmacologic treatments like cognitive behavioral therapy for insomnia.
• FDA warnings highlight risks of complex sleep behaviors (e.g., sleep-driving).
• Enhanced monitoring recommended in elderly and patients with respiratory disorders.

• Store at controlled room temperature: 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep out of reach of children.
• No refrigeration or special handling required.