Zolpidem

Zolpidem
ATC Code N05CF02
Formula C19H21N3O
Molar Mass (g·mol−1) 307,3895
Physical State solid
Melting Point (°C) 193-197
PKS Value 5,65
CAS Number 82626-48-0
PUB Number 5732
Drugbank ID DB00425
Solubility low in water

Basics

Zolpidem is a hypnotic drug used for the short-term treatment of sleep disorders and to improve sleep duration and quality due to its sedative and sleep-inducing effects. The active ingredient is characterized by its low risk of dependence, withdrawal and tolerance, and may also be effective in restoring brain function after brain injury.
In den USA und in Deutschland ist der Arzneistoff das momentan meistverordnete Schlafmittel.

Pharmacology

Pharmacodynamics

In the central nervous system, zolpidem binds with high affinity to the α- and γ-subunit of the GABAA receptor, interacts with it, and enhances the sedative and sleep-promoting responses of the neurotransmitter GABA (gamma-amino-butyric acid). This triggers muscle relaxant and anticonvulsant effects and facilitates sleep onset and duration.

Pharmacokinetics

The hypnotic is rapidly absorbed from the gastrointestinal tract and acts quickly after oral administration. The bioavailability in this case is about 70%. In the blood, the maximum plasma concentration is reached after 0.5-3 hours and it circulates about 90% bound to proteins. The volume of distribution is 0.54-0.68 l/kg, decreasing in the elderly and increasing in patients with chronic renal insufficiency.
Verstoffwechselt wird Zolpidem in der Leber durch verschiedene Cytochrom P450 Isoenzyme in inaktive Stoffwechselprodukte, welche hauptsächlich über die Nieren ausgeschieden werden. Die Halbwertzeit beträgt durchschnittlich 2,4 Stunden.

Drug Interactions

While taking zolpidem, interactions may occur with alcohol, centrally depressant drugs and antidepressants(bupropion, desipramine, venlafaxine, sertraline, fluoxetine), fluvoxamine, narcoanalgesics, ciprofloxacin, and drugs metabolized by CYP3A4 and CYP450.

Toxicity

Side effects

Common side effects include:

  • Hallucinations, restlessness, nightmares, depression
  • drowsiness, fatigue, headache, dizziness, cognitive dysfunction, reduced memory
  • diarrhea, nausea, vomiting, abdominal pain
  • Back pain

Furthermore, zolpidem greatly affects the ability to drive and operate machinery.

Toxicological data

Symptoms and consequences of zolpidem overdose may range from impaired consciousness, morbid drowsiness and coma to cardiorespiratory collapse with fatal outcome.
Der LD50-Wert nach oraler Gabe an männlichen Ratten liegt bei 695 mg/kg.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

Your personal medicine assistent

afgis-Qualitätslogo mit Ablauf Jahr/Monat: Mit einem Klick auf das Logo öffnet sich ein neues Bildschirmfenster mit Informationen über Medikamio GmbH & Co KG und sein/ihr Internet-Angebot: medikamio.com/ This website is certified by Health On the Net Foundation. Click to verify.
Drugs

Search our database for drugs, sorted from A-Z with their effects and ingredients.

Substances

All substances with their common uses, chemical components and medical products which contain them.

Diseases

Causes, symptoms and treatment for the most common diseases and injuries.

The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.