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Monday, July 28, 2025

Temazepam


Generic name: Temazepam
Drug class: Benzodiazepine – intermediate-acting hypnotic
Formulation: Oral capsules
Available strengths: 7.5 mg, 15 mg, 22.5 mg, 30 mg
Route of administration: Oral
Controlled substance status: Schedule IV (moderate potential for abuse and dependence)

Temazepam is a benzodiazepine derivative used primarily for the short-term treatment of insomnia. It exerts sedative, anxiolytic, and muscle relaxant properties by enhancing the activity of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the central nervous system. Due to its intermediate half-life, it is suitable for patients who experience both sleep initiation and sleep maintenance difficulties.

2. Mechanism of Action

Temazepam acts as a positive allosteric modulator at the GABA-A receptor complex. It binds to a specific site on the receptor, distinct from the GABA binding site, and enhances the receptor’s response to GABA. This results in increased chloride ion influx into neurons, leading to hyperpolarization and decreased neuronal excitability.

  • Sedation is achieved through CNS depression via limbic, thalamic, and hypothalamic regions.

  • Anxiolytic effects emerge from limbic system inhibition.

  • Sleep-inducing actions involve suppression of REM and stage 4 sleep, although deep sleep architecture is generally preserved more than with other benzodiazepines.

3. Pharmacokinetics

Absorption: Well absorbed orally, with peak plasma concentrations reached within 1.5 to 2 hours after ingestion.
Distribution: Highly lipophilic and widely distributed throughout body tissues.
Protein binding: Approximately 96%.
Metabolism: Primarily hepatic through conjugation (glucuronidation); minimal cytochrome P450 involvement.
Half-life: Approximately 8 to 20 hours, which allows overnight efficacy with less residual next-day sedation compared to longer-acting benzodiazepines.
Excretion: Eliminated mostly in the urine as inactive conjugates.

4. Therapeutic Indications

4.1 Insomnia

Indicated for the short-term management (typically 7 to 10 days) of insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings, or early morning awakening. It improves sleep onset latency and increases total sleep time.

4.2 Preoperative Sedation (off-label)

Sometimes used for preoperative anxiety reduction or sedation due to its calming effect and intermediate duration of action.

5. Dosage and Administration

Adults

  • Initial dose: 15 mg taken orally 30 minutes before bedtime.

  • Usual range: 7.5 mg to 30 mg once daily at bedtime.

  • Maximum dose: 30 mg per day.

  • Patients who are older, frail, or debilitated may be started on 7.5 mg to minimize adverse effects.

Geriatric population

  • Recommended dose: 7.5 mg once daily at bedtime.

  • Caution due to increased sensitivity to CNS depressants and higher fall risk.

Administration notes

  • Capsule should be taken immediately before going to bed.

  • The user should have a full 7 to 8 hours available for sleep to reduce the risk of residual drowsiness.

  • Avoid use with alcohol or other CNS depressants.

6. Contraindications

  • Known hypersensitivity to temazepam or other benzodiazepines.

  • Pregnancy (especially in the first trimester due to teratogenic risks and in late pregnancy due to neonatal CNS depression).

  • Myasthenia gravis.

  • Severe respiratory insufficiency or sleep apnea syndrome.

  • Acute narrow-angle glaucoma.

  • History of substance abuse or dependence (relative contraindication).

7. Warnings and Precautions

  • CNS depression: May impair alertness, coordination, and reaction times. Avoid driving or operating machinery.

  • Respiratory depression: Risk is increased in patients with compromised pulmonary function or when combined with opioids or alcohol.

  • Dependence and tolerance: Use should be limited to short durations (≤4 weeks) due to risks of physical and psychological dependence.

  • Withdrawal: Abrupt discontinuation after prolonged use may result in withdrawal symptoms such as anxiety, tremors, insomnia, seizures, and agitation.

  • Paradoxical reactions: Behavioral disinhibition, aggression, agitation, and hallucinations may occur, especially in the elderly.

  • Amnesia: Anterograde amnesia may occur at therapeutic doses; patients may perform activities without memory.

  • Depression and suicidality: Caution in patients with depression, as it may worsen underlying symptoms or facilitate suicidal behavior.

8. Adverse Effects

Very Common

  • Drowsiness

  • Fatigue

  • Dizziness

Common

  • Headache

  • Impaired coordination

  • Confusion (especially in elderly)

  • Nausea

  • Weakness

  • Ataxia

  • Next-day hangover effect

Uncommon or Rare

  • Depression

  • Paradoxical reactions (e.g., agitation, hallucinations)

  • Memory impairment

  • Double vision

  • Allergic reactions

  • Hypotension

  • Respiratory depression (dose-dependent)

  • Skin rashes

  • Dependence and withdrawal symptoms with prolonged use

9. Drug Interactions

  • Other CNS depressants: Additive effects may occur with alcohol, opioids, antihistamines, antipsychotics, or sedative antidepressants.

  • Opioids: Concomitant use may result in profound sedation, respiratory depression, coma, or death.

  • Antiepileptics: May increase the sedative effects of benzodiazepines.

  • Muscle relaxants: Enhanced muscle-relaxing effects when combined.

  • Alcohol: Potentiates sedative effects and increases risk of overdose.

  • Minimal CYP450 interaction: Temazepam metabolism is via conjugation, not cytochrome P450—therefore fewer metabolic drug–drug interactions.

10. Use in Special Populations

Elderly

  • Increased risk of cognitive impairment, falls, and sedation.

  • Dose reduction necessary (≤7.5 mg nightly).

Pregnancy

  • Contraindicated. May cause congenital malformations, neonatal withdrawal symptoms, and floppy infant syndrome.

Lactation

  • Excreted in breast milk. Use is not recommended. May cause sedation or feeding difficulties in nursing infants.

Renal Impairment

  • No significant changes in pharmacokinetics; use cautiously in severe renal dysfunction.

Hepatic Impairment

  • Metabolism may be prolonged; adjust dose cautiously in moderate to severe hepatic impairment.

11. Overdose

Symptoms

  • CNS depression: drowsiness, confusion, hypotonia, respiratory depression, coma

  • Hypotension

  • Ataxia

  • Slurred speech

Management

  • Supportive care including airway, breathing, and circulation support

  • Activated charcoal if early presentation

  • Flumazenil may be administered cautiously as a benzodiazepine antagonist; however, it can precipitate seizures or withdrawal in dependent individuals

12. Monitoring Parameters

  • Evaluate sleep latency and quality periodically

  • Assess for signs of dependence or tolerance if used beyond 2 weeks

  • Monitor elderly for falls, confusion, daytime sedation

  • Reassess need regularly and taper slowly to prevent withdrawal

  • Monitor respiratory status in patients with respiratory comorbidities

  • Liver function tests if prolonged use or hepatic concerns



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