Zolpidem information from DrugsUpdate
L - Caution when used during lactation
Zolpidem is a prescription medication used for the short-term treatment of insomnia, as well as some brain disorders. It is a short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to gamma-aminobutyric acid (GABAA) receptors at the same location as benzodiazepines. It works quickly (usually within 15 minutes) and has a short half-life (2–3 hours). Trade names of zolpidem include Adormix, Ambien, Ambien CR, Edluar, Damixan, Hypnogen, Ivedal, Lioran, Myslee, Nytamel, Sanval, Somidem, Stilnoct, Stilnox, Stilnox CR, Sucedal, Zoldem, Zolnod and Zolpihexal.
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.
Rapidly absorbed from GI tract. Peak plasma concentration: 3 hours. Absolute bioavailability: 70%. Food reduce both the rate and extent of GI absorption.
Protein binding: 92%. Distributed into breast milk.
Undergoes first pass metabolism, metabolised primarily by the cytochrome P450 isoenzyme CYP3A4. Elimination half life: 2.5 hours.
Excreted in urine and faeces as inactive metabolites.
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).
Because sleep disturbances may be the presenting manifestation of a physical and/or psychiatric disorder, symptomatic treatment of insomnia should be initiated only after a careful evaluation of the patient. The failure of insomnia to remit after 7 to 10 days of treatment may indicate the presence of a primary psychiatric and/or medical illness that should be evaluated. Worsening of insomnia or the emergence of new thinking or behavior abnormalities may be the consequence of an unrecognized psychiatric or physical disorder. Such findings have emerged during the course of treatment with sedative/hypnotic drugs, including Zolpidem tartrate tablets. Because some of the important adverse effects of Zolpidem tartrate tablets appear to be dose related, it is important to use the smallest possible effective dose, especially in the elderly.
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.
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 weeks including tapering.
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.
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.
May be taken with or without food
List of Contraindications
Caution when used during pregnancy
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Caution when used during lactation
Safety and effectiveness of Zolpidem have not been established in pediatric patients.
Severe hepatic insufficiency
Store at 20-25°C (68-77°F).
Information Not Available