Zolpidem

Indications
Oral
Short-term management of insomnia
Adult: As conventional release tab: 10 mg immediately before bedtime; max: 10 mg/day. As controlled release tab: 12.5 mg immediately before bedtime.
Elderly: As conventional tab: Initiate with a 5-mg dose before bedtime. As controlled release tab: 6.25 mg immediately before bedtime.
Hepatic impairment: As conventional tab: Initiate with 5 mg before bedtime. Severe: contra-indicated.

Special Populations: Dosage in hepatic impairment: Same dose given to elderly patients.
Contraindications
Severe hepatic insufficiency.
Warnings / Precautions
Obstructive sleep apnoea, myasthenia gravis, compromised respiratory function, hepatic impairment. Caution in patients exhibiting symptoms of depression. Patients should be warned from doing any work involving mental alertness or motor coordination after ingestion of the drug. Pregnancy and lactation. Re-evaulate if insomnia fail to remit after 7-10 days. Max duration of treatment: 4 wk including tapering.
Adverse Reactions
Amnesia, drowsiness, dizziness, diarrhoea, nausea, vomiting, abnormal thinking and behaviour, drugged feelings, back pain, ataxia, hiccups, confusion, euphoria, insomnia, vertigo, diplopia, abnormal vision.
Potentially Fatal: Hepatitis, anaphylactic reactions, sleep-driving (driving while not fully awake after drug ingestion, with no recollection of the event).
Overdose Reactions
Symptoms: impairment of consciousness from somnolence to coma, compromised CV and respiratory function. Management: Treatment is largely symptomatic and supportive. Activated charcoal may be given if presented within one hour of ingestion of >100 mg zolpidem in adults and >5 mg in children. Gastric lavage may be considered if presented within 1 hr of ingestion of >100 mg zolpidem. Flumazenil may be used if there is severe CNS depression, but generally not needed. Haemodialysis unlikely to be useful.
Drug Interactions
Increased sedation and incoordination with TCA. Increased sedation with haloperidol and alcohol. Small increase in zolpidem concentration with ketoconazole. Reduced effect of hypnotic effects with rifampicin.
Potentially Fatal: Increased risk of prolonged sedation and respiratory depression with ritonavir.
See Below for More zolpidem Drug Interactions
Mechanism of Actions
Zolpidem acts by binding to the benzodiazepine (BZD) receptors of the GABA receptor complex. It has a selective affinity to BZD receptors prevalent in the cerebellum (omega-1 receptors). It has strong sedative actions but only minor anxiolytic properties. It has also less effects on skeletal muscle and seizure threshold. Zolpidem has a rapid onset but short duration of hypnotic action.
Absorption: Rapidly absorbed from GI tract. Peak plasma concentration: 3 hr. Absolute bioavailability: 70%. Food reduce both the rate and extent of GI absorption.
Distribution: Protein binding: 92%. Distributed into breast milk.
Metabolism: Undergoes first pass metabolism, metabolised primarily by the cytochrome P450 isoenzyme CYP3A4. Elimination half life: 2.5 hr.
Excretion: Excreted in urine and faeces as inactive metabolites.
Administration
Should be taken on an empty stomach. (Do not take w/ or immediately after a meal.)
Storage Conditions
Oral: Store at 20-25°C (68-77°F).
ATC Classification
N05CF02 - zolpidem ; Belongs to the class of benzodiazepine related agents. Used as hypnotics and sedatives.
Storage
Oral: Store at 20-25°C (68-77°F).
Available As
  • Zolpidem 10 mg
  • Zolpidem 12.5 mg
  • Zolpidem 5 mg
  • Zolpidem 6.25 mg
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