Adult: For the short-term management of insomnia characterised by difficulties with sleep initiation: As conventional tab: 5-10 mg at bedtime. Initial dose for women: 5 mg. Max: 10 mg daily. For the short-term management of insomnia characterised by difficulties with sleep initiation or sleep maintenance: As extended-release tab: 6.25-12.5 mg at bedtime. Initial dose for women: 6.25 mg. Max: 12.5 mg daily. Max duration of treatment: 4 weeks (including tapering-off period). Use the lowest effective dose for the shortest possible duration. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product guidelines). Elderly: For the short-term management of insomnia characterised by difficulties with sleep initiation: As conventional tab: 5 mg at bedtime. For the short-term management of insomnia characterised by difficulties with sleep initiation or sleep maintenance: As extended-release tab: 6.25 mg at bedtime.
Sublingual Insomnia
Adult: For the short-term management of insomnia characterised by difficulties with sleep initiation: 5-10 mg at bedtime. Initial dose for women: 5 mg at bedtime. Max: 10 mg daily. Max duration: 4 weeks (including tapering-off period). Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines). Elderly: For the short-term management of insomnia characterised by difficulties with sleep initiation: 5 mg at bedtime.
Special Patient Group
Debilitated patients: As conventional/sublingual tab: 5 mg before bedtime. As extended-release tab: 6.25 mg before bedtime.
Patient taking other CNS depressants: Dosage adjustment may be necessary.
Hepatic Impairment
Oral:
Mild to moderate: As conventional tab: 5 mg at bedtime. As extended-release tab: 6.25 mg at bedtime. Severe: Contraindicated.
Sublingual:
For the short-term management of insomnia characterised by difficulties with sleep initiation: 5 mg at bedtime.
Administration
Should be taken on an empty stomach. Do not take w/ or immediately after a meal.
Contraindications
Obstructive sleep apnoea syndrome, myasthenia gravis, acute or severe respiratory depression. History of complex sleep behaviour after use of zolpidem. Severe hepatic impairment (Child-Pugh class C).
Special Precautions
Patient with chronic respiratory insufficiency, COPD, depression, history of psychiatric disorders, alcohol or drug abuse or dependence. Debilitated patients. Concomitant use with other CNS depressants and opioids. Not recommended for primary treatment of psychosis. Long-term use is not recommended. Avoid abrupt withdrawal. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Impaired respiratory function, psychiatric and paradoxical reactions (e.g. restlessness, agitation, irritability, aggressiveness, delusion, nightmares, rage, psychosis, hallucinations, increased insomnia), next-day psychomotor impairment, treatment tolerance, drug abuse and/or physical and psychological dependence, rebound insomnia, withdrawal symptoms (following abrupt discontinuation), anterograde amnesia, increased risk of fall and consequent injury, hepatic encephalopathy (in patients with hepatic impairment). Ear and labyrinth disorders: Vertigo. Eye disorders: Double vision, blurred vision. Gastrointestinal disorders: Diarrhoea, nausea, vomiting, abdominal pain. General disorders and administration site conditions: Fatigue. Investigations: Elevated liver enzymes. Metabolism and nutrition disorders: Loss of appetite. Musculoskeletal and connective tissue disorders: Back pain, muscle weakness, arthralgia, myalgia, muscle spasm, neck pain. Nervous system disorders: Somnolence, headache, dizziness, ataxia, paraesthesia, tremor, speech disorder, reduced alertness. Respiratory, thoracic and mediastinal disorders: Upper and lower respiratory tract infection. Skin and subcutaneous tissue disorders: Skin reactions, rash, pruritus, hyperhidrosis. Potentially Fatal: Worsening depression and suicidal thoughts or attempts and suicide; severe anaphylactic and anaphylactoid reactions (e.g. angioedema involving the throat, larynx or glottis, airway obstruction); complex sleep behaviour (e.g. sleepwalking, sleep-driving, eating, engaging in other activities while not fully awake).
This drug may cause dizziness, drowsiness, reduced alertness, and blurred or double vision, if affected, do not drive or operate machinery.
Monitoring Parameters
Assess underlying causes of insomnia before initiating treatment. Monitor daytime alertness, fall risk, behaviour profile, respiratory rate (in patients with compromised respiration); tolerance, abuse and dependence. Reevaluate patient if insomnia persists after 7-10 days of treatment.
Overdosage
Symptoms: Impaired consciousness ranging from somnolence to coma, CV and/or respiratory compromise. Management: Symptomatic and supportive treatment. Perform gastric lavage if necessary. May administer activated charcoal to reduce absorption. Monitor respiratory and CV functions. May give benzodiazepine antagonist (e.g. flumazenil) when serious symptoms are observed.
Drug Interactions
Increased risk of fall with muscle relaxants. Increased CNS depressant effects with antipsychotics/neuroleptics, anxiolytics, sedatives, hypnotics, muscle relaxants, narcotic analgesics, antidepressants, anaesthetics, sedative antihistamines, and antiepileptic drugs. May cause visual hallucinations with bupropion, desipramine, fluoxetine, venlafaxine, and sertraline. Increased risk of euphoria leading to increased psychological dependence with narcotic analgesics. Increased plasma concentration with fluvoxamine and CYP450 enzyme inhibitors (e.g. ciprofloxacin, ketoconazole). Decreased plasma concentration with CYP450 enzyme inducers (e.g. rifampicin, carbamazepine, phenytoin). Potentially Fatal: Additive CNS depressant effect leading to increased risk of respiratory depression, sedation, and coma with opioids.
Food Interaction
Increased sedative effect with alcohol. Decreased plasma concentration with St. John's wort.
Action
Description: Mechanism of Action: Zolpidem is an imidazopyridine hypnotic. It enhances the gamma-aminobutyric acid (GABA) neurotransmitter inhibitory effects by selectively binding to benzodiazepine-1 receptor, thus resulting in increased chloride conductance, neuronal hyperpolarisation, decreased neuronal excitability, and inhibition of action potential leading to sedative and hypnotic effect. Onset: 30 minutes (conventional tab). Duration: 6-8 hours (conventional tab). Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Food, particularly high-fat or high-caloric meals, decreases and delays peak plasma concentration. Absolute bioavailability: Approx 70% (tab). Time to peak plasma concentration: Within 3 hours. Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 93%. Metabolism: Metabolised in the liver primarily by CYP3A4 enzymes via methylation and hydroxylation into 3 inactive metabolites; undergoes first-pass metabolism. Excretion: Via urine (48-67%, mainly as metabolites); faeces (29-42%, mainly as metabolites). Elimination half-life: Approx 2.5 hours (conventional and extended-release tab); approx 3 hours (sublingual tab).
Chemical Structure
Zolpidem Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5732, Zolpidem. https://pubchem.ncbi.nlm.nih.gov/compound/Zolpidem. Accessed May 28, 2024.
Storage
Conventional/extended-release tab: Store between 15-30°C. Sublingual tab: Store between 20-25°C. Protect from light and moisture.
N05CF02 - zolpidem ; Belongs to the class of benzodiazepine related agents. Used as hypnotics and sedatives.
References
Ambien CR Tablet, Coated (Sanofi-Aventis U.S. LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/05/2024.Anon. Zolpidem Tartrate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/04/2024.Buckingham R (ed). Zolpidem Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/04/2024.Edluar 5 mg Sublingual Tablets (Mylan Products Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 02/05/2024.Edluar Tablet (Meda Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/05/2024.Joint Formulary Committee. Zolpidem Tartrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/04/2024.Stilnox 10 mg Film-coated Tablets (Sanofi-Aventis [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 12/04/2024.Zolpidem Tartrate 10 mg Tablets (Zentiva Pharma UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 12/04/2024.Zolpidem. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 17/05/2024.Zolpidem. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 12/04/2024.
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