Zolpidem


Generic Medicine Info
Indications and Dosage
Oral
Short-term management of insomnia
Adult: As immediate release tab: 5-10 mg immediately before bedtime. Max: 10 mg/day. As extended release tab: 6.25-12.5 mg immediately before bedtime. Max: 12.5 mg/day. Max duration of treatment: 4 wk including tapering.
Elderly: As immediate release tab: 5 mg immediately before bedtime. As extended release tab: 6.25 mg immediately before bedtime. Max duration of treatment: 4 wk including tapering.
Renal Impairment
No dosage adjustment needed.
Hepatic Impairment
As immediate release tab: 5 mg immediately before bedtime. As extended release tab: 6.25 mg immediately before bedtime. Max duration of treatment: 4 wk including tapering. Severe: Contraindicated.
Administration
Should be taken on an empty stomach. Do not take w/ or immediately after a meal.
Contraindications
Severe hepatic impairment.
Special Precautions
Obstructive sleep apnoea, myasthenia gravis, compromised respiratory function. Patients exhibiting symptoms of depression. History of drug or alcohol abuse. Avoid abrupt withdrawal and rapid dose reduction after prolonged therapy. Re-evaluate if insomnia fail to remit after 7-10 days as this may indicate the presence of underlying psychiatric and/or medical condition. Pregnancy, lactation, childn <18 yr.
Adverse Reactions
Atypical thinking and behaviour, hallucination, nightmare, somnolence, somnambulism, headache, nausea, vomiting, dizziness, vertigo, drowsiness, asthenia, ataxia, rebound insomnia, amnesia, GI disturbances, upper and lower respiratory tract infection, fatigue, visual disturbances, increased ALT serum concentrations, abnormal LFT.
Potentially Fatal: Hepatitis, anaphylactic reactions, angioedema, sleep-driving (driving while not fully awake after drug intake, w/ no recollection of the event).
Patient Counseling Information
Patients should be warned about performing activities involving mental alertness or physical coordination after drug intake.
Overdosage
Symptoms: Drowsiness, impairment of consciousness from somnolence to coma, compromised CV and respiratory function. Management: Treatment is largely symptomatic and supportive. IV fluids should be administered as needed. Activated charcoal may be given if presented w/in 1 hr of ingestion of >1 mg/kg zolpidem in adults or childn. Gastric lavage may be considered if presented w/in 1 hr of ingestion of >100 mg zolpidem and monitor for at least 12 hr. Flumazenil may be used if there is severe CNS depression, but generally not needed. Haemodialysis is unlikely to be useful.
Drug Interactions
Flumazenil reverses the sedative/hypnotic effect of zolpidem. Increased depressant effects w/ CNS depressants (e.g. sedatives, antihistamines, alcohol). Additive effect on decreased alertness and psychomotor performance w/ imipramine and chlorpromazine. Increased plasma concentration w/ itraconazole, ketoconazole and other CYP3A4 inhibitors. May decrease plasma concentration w/ CYP3A4 inducers (e.g. carbamazepine). Reduced hypnotic effect w/ rifampicin.
Potentially Fatal: Increased risk of prolonged sedation and respiratory depression w/ ritonavir.
Food Interaction
Avoid combination w/ St John's wort, alcohol and grapefruit juice.
Action
Description: Zolpidem is an imidazopyridine derivative that acts by binding to the benzodiazepine (BZD) receptors of the GABA receptor complex resulting in neuronal hyperpolarisation, action potential inhibition, increased in chloride conductance and decreased in neuronal excitability. It has strong sedative action but only minimal anxiolytic, myorelaxant and anticonvulsant properties due to its selectivity for the BZ1-receptor over the BZ2-receptor. Zolpidem has a rapid onset but short duration of hypnotic action.
Onset: Immediate release: 30 min.
Duration: Immediate release: 6-8 hr.
Pharmacokinetics:
Absorption: Rapidly absorbed from GI tract. Food reduces both the rate and extent of GI absorption. Absolute bioavailability: Approx 70%. Time to peak plasma concentration: Immediate release: 1.6 hr; extended release: 1.5 hr.
Distribution: Distributed into breast milk. Volume of distribution: 0.54 kg/L. Plasma protein binding: Approx 92%.
Metabolism: Undergoes first pass metabolism, metabolised primarily by CYP3A4 isoenzyme.
Excretion: Via urine (48-67%) and faeces (29-42%) as inactive metabolites. Elimination half-life: Approx 2.5 hr.
Storage
Store between 20-25°C.
MIMS Class
Hypnotics & Sedatives
Disclaimer: This information is independently developed by MIMS based on Zolpidem from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
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