Products
Zolpidem is commercially available as film-coated tablets, sustained-release tablets, and effervescent tablets (Stilnox, Stilnox CR, generics, USA: Ambien). It has been approved in many countries since 1990.
Structure and properties
Zolpidem (C19H21N3O, Mr = 307.39 g/mol) is an imidazopyridine that is structurally distinct from the benzodiazepines. It is present in drugs as zolpidem tartrate, a white crystalline powder that is very sparingly soluble in water.
Effects
Zolpidem (ATC N05CF02) has sleep-inducing and sedative properties. It facilitates falling asleep and increases total sleep time. The effects are due to binding to the GABAA receptor in the central nervous system. Zolpidem has a short half-life of 2.4 hours and is therefore administered in sustained-release tablet form.
Indications
For short-term treatment of insomnia (difficulty falling asleep and staying asleep). Treatment should usually be kept as short as possible.
Dosage
According to the professional information. The drug is taken in the evening before bedtime. When discontinuing, the dose should be gradually reduced to avoid possible withdrawal symptoms.
Dependence
Zolpidem may cause physical and psychological dependence. The risk is increased with prolonged use, high dosage, and appropriate predisposition. Increased risk also exists in patients with a psychiatric history and drug or alcohol dependence. Sudden discontinuation is associated with withdrawal symptoms such as tremors, sleep disturbances, headache, anxiety and tension, nervousness, and confusion.
Abuse
Zolpidem can be abused as a depressant narcotic.
Contraindications
- Children under 15 years of age
- Hypersensitivity
- Sleep apnea syndrome
- Acute respiratory failure
- Myasthenia gravis
- Severe hepatic insufficiency
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Concomitant administration of zolpidem with central depressant drugs or alcohol may increase central nervous system inhibition. Zolpidem is a substrate of CYP3A4. With concomitant administration of zolpidem and CYP3A4 inducers, the effect of zolpidem may be reduced and enhanced by CYP3A4 inhibitors. Concomitant administration of muscle relaxants may increase the muscle relaxant effect (risk of falls!).
Adverse effects
The most common adverse effects are hallucinations, restlessness, nightmares, daytime drowsiness, fatigue, headache, dizziness, worsening of insomnia, reduced memory for new awareness, diarrhea, nausea, vomiting, and abdominal pain. Confusion, irritability, and double vision are occasionally observed.
