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Zolpidem

Medical Use and Guidelines: – Zolpidem is used for short-term treatment of insomnia. – It helps improve sleep onset and maintenance. – Recommended as a […]

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Medical Use and Guidelines:
– Zolpidem is used for short-term treatment of insomnia.
– It helps improve sleep onset and maintenance.
– Recommended as a second-line treatment after non-pharmacological options.
– Psychological effects are significant for its efficacy.
– Recommended after cognitive behavioral therapy for insomnia.

Contraindications and Adverse Effects:
– Avoid in obstructive sleep apnea, myasthenia gravis, severe liver disease.
– Not suitable for children, those with psychotic illnesses, or past substance addiction.
– Common side effects include headache, drowsiness, dizziness, and diarrhea.
– Long-term use can lead to various adverse effects like allergies, sinusitis, and back pain.
– Caution in older individuals due to increased sensitivity and risk of falls.

Tolerance, Dependence, and Withdrawal:
– Associated with drug tolerance and substance dependence.
– Tolerance can develop in weeks, leading to withdrawal symptoms.
– Abrupt withdrawal may cause delirium, seizures, or adverse effects.
– Treatment involves gradual dose reduction to minimize withdrawal symptoms.
– In severe cases, inpatient flumazenil administration may be necessary.

Chemical and Physical Data:
– Formula: C19H21N3O.
– Molar mass: 307.397g/mol.
– Structure: GABA receptor agonist of the imidazopyridine class.
– Half-life: Generally 2-3 hours, longer in individuals with liver issues.
– Melting point: 193–197°C (379–387°F).

Regulatory Information and Overdose:
– Approved for medical use in the US in 1992.
– Classified as a Schedule IV controlled substance.
– Over 10 million prescriptions filled annually in the US.
– Overdose can lead to coma or death and can be treated with flumazenil.
– Other drugs are often present in the system during overdose.

Zolpidem (Wikipedia)

Zolpidem, sold under the brand name Ambien among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and behavioral changes, such as sleep hygiene, have been tried. It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer. It is taken by mouth and is available in conventional tablets, sublingual tablets, or oral spray.

Zolpidem
Clinical data
Trade namesAmbien and Ambien CR, others
AHFS/Drugs.comMonograph
MedlinePlusa693025
License data
Pregnancy
category
  • AU: B3
Dependence
liability
Physical: High Psychological: Low–moderate
Addiction
liability
moderate
Routes of
administration
By mouth, sublingual, oromucosal (spray), rectal
Drug classNonbenzodiazepine, sedative-hypnotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability70% (by mouth)
Protein binding92%
MetabolismLiver through CYP3A4 (~60%), CYP2C9 (~20%), and CYP1A2 (~14%)
Metabolites(ZCA) zolpidem 6-carboxylic acid; (ZPCA) zolpidem phenyl-4-carboxylic acid
Onset of action≤ 30 Minutes
Elimination half-life2.0 - 3 hours
Duration of action3 hours
ExcretionKidney (56%)
fecal (34%)
Identifiers
  • N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide hemitartrate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.115.604 Edit this at Wikidata
Chemical and physical data
FormulaC19H21N3O
Molar mass307.397 g·mol−1
3D model (JSmol)
Melting point193–197 °C (379–387 °F)
  • CN(C)C(=O)Cc1c(nc2ccc(C)cn12)c3ccc(C)cc3
  • InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3 checkY
  • Key:ZAFYATHCZYHLPB-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. While flumazenil, a GABAA–receptor antagonist, can reverse zolpidem's effects, usually supportive care is all that is recommended in overdose.

Zolpidem is a nonbenzodiazepine or Z-drug which acts as a sedative and hypnotic. Zolpidem is a GABAA receptor agonist of the imidazopyridine class. It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines. It generally has a half-life of two to three hours. This, however, is increased in those with liver problems.

Zolpidem was approved for medical use in the United States in 1992. It became available as a generic medication in 2007. Zolpidem is a Schedule IV controlled substance under the Controlled Substances Act of 1970 (CSA). More than ten million prescriptions are filled each year in the United States, making it one of the most commonly used treatments for sleeping problems. In 2021, it was the 63rd most commonly prescribed medication in the United States, with more than 10 million prescriptions.

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