Zolpidem: Drug Information
1. Drug Name
Generic Name
Zolpidem
Brand Name(s)
- Pakistan: BrandX
- India: BrandY
- US: Ambien
- UK: Zolpidem
2. Pharmacological Class
Class
Sedative-hypnotic
Subclass
Non-benzodiazepine
3. Mechanism of Action
Zolpidem acts as an agonist at the benzodiazepine site of the GABAA receptor complex in the brain. It enhances GABAergic neurotransmission, which results in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant effects.
4. Indications
Primary Indications
- Short-term treatment of insomnia characterized by difficulties with sleep initiation
- Middle-of-the-night awakenings with difficulty returning to sleep when taken as needed
Off-label Uses
- Adjunctive treatment for depression and anxiety disorders
- Use in patients with brain injury and stroke to improve recovery sleep
5. Dosage and Administration
Standard Dosage
The dosage of zolpidem should be individualized based on patient characteristics and response to therapy.
Route of Administration
Oral administration, usually as immediate-release tablets or sublingual tablets for rapid onset of action.
Special Populations
- Pediatric: Safety and efficacy have not been established.
- Geriatric: Use lower initial doses to avoid adverse effects.
6. Pharmacokinetics
Absorption
Zolpidem is rapidly absorbed from the gastrointestinal tract.
Distribution
Zolpidem has a rapid distribution into tissues, with high lipid solubility.
Metabolism
Zolpidem is metabolized in the liver via CYP3A4 and to a lesser extent by CYP1A2.
Excretion
The major route of elimination is renal excretion of metabolites.
Half-life
The elimination half-life is approximately 2.5 hours.
7. Contraindications
- Hypersensitivity to zolpidem or any component of the formulation
- Severe respiratory insufficiency
- Severe hepatic impairment
8. Warnings and Precautions
- Risk of next-day impairment: Avoid driving or operating machinery until at least 8 hours after taking zolpidem.
- Sleep behaviors: Patients may engage in activities while not fully awake (e.g., sleep-driving, preparing and eating food, making phone calls).
- Dependence and withdrawal: Prolonged use may lead to physical and psychological dependence.
9. Side Effects
Common Side Effects
- Drowsiness
- Dizziness
- Headache
Serious Side Effects
- Complex sleep behaviors
- Allergic reactions
- Severe skin reactions
10. Drug Interactions
Major Interactions
- Other CNS depressants (e.g., alcohol, opioids)
- Anticonvulsants
Moderate Interactions
- Antidepressants
- Antifungals
Minor Interactions
- Caffeine
- Antacids
11. Pregnancy and Lactation
Pregnancy Category
Category C - Risk cannot be ruled out.
Breastfeeding Considerations
Zolpidem is excreted into human milk; use with caution.
12. Patient Counseling Information
- Take zolpidem exactly as prescribed; do not increase your dose or use it more frequently than prescribed.
- Avoid alcohol and other sedative drugs while taking zolpidem.
- Discuss with healthcare provider before starting zolpidem, especially if pregnant, breastfeeding, or taking other medications.