Last updated: October 24, 2014
Trade Names: Ambien, Ambien CR
Drug Class: Hypnotic
Preparations: Immediate release: 5-, 10 mg tablets; Controlled release: 6.25-, 12.5 mg
Use lowest effective dose, food decreases absorption.
Females: 5 mg immediate release or 6.25 mg extended release immediately before bedtime
Males: 5-10 mg immediate release or 6.25 -12.5 mg extended release immediately before bedtime
Indications: Short-term treatment of insomnia
Mechanism of Action: Selective benzodiazepine-1 (BZ1) receptor agonist and thus increases activity of GABA, an inhibitory neurotransmitter. Because has little effect on BZ2 receptors, has minimal anxiolytic or anticonvulsant actions.
Contraindications: Hypersensitivity, hepatic impairment
Precautions: Depression, sleep apnea, respiratory depression, drug abuse, elderly, impairs ability to operate machinery, increased risk of falls, abrupt withdrawal can lead to withdrawal symptoms, cytochrome P450 3A (CYP3A) drug interactions
Pregnancy Risk: C
Common: Drowsiness, dizziness, headache
Less common: Abnormal dreams, confusion, depersonalization, disorientation, ataxia, memory impairment, performing complex activities while asleep (e.g., walking eating, driving), amnesia, abuse
Rare: Allergy (including anaphylaxis and angioedema), behavioral changes, hallucinations
CYP3A inhibitors (strong inhibitors include clarithromycin, telithromycin, ketoconazole, itraconazole, nefazodone and many HIV drugs; moderate inhibitors include aprepitant, diltiazem, verapamil, erythromycin, fluconazole, posaconazole, voriconazole, grapefruit juice): Increased zolpidem concentrations.
Alcohol and CNS depressants: Increased CNS depression
Patient Instructions: Avoid grapefruit juice; rapid onset therefore only take once in bed; do not drive or operate machinery after after taking (increased risk may extend to the next day with the extended release preparation and also in some people with the immediate release drug), increases risk of falls.
Comments: Use lowest effective dose for as short a time as possible
Clinical Pharmacology: Onset 30 minutes (immediate release), duration 6-8 h (immediate release), half-life 1.4-4.5 h. Women have 50% higher levels than men. Metabolized by CYP3A4.