ZolpidemRx

Trade Names: Ambien, Ambien CR

Drug Class: Hypnotic

Preparations: Immediate release: 5-, 10 mg tablets; Controlled release: 6.25-, 12.5 mg

Dose
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

Adverse Effects
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

Drug Interactions
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.

Cost: $$$