Zolpidem Tartrate

Indications

Zolpidem Tartrate is used for: Insomnia

Adult Dose

Oral Short-term management of insomnia Adult: As immediate release tab: 5-10 mg immediately before bedtime. Max: 10 mg/day. Max duration of treatment: 4 wk including tapering. Elderly: As immediate release tab: 5 mg immediately before bedtime. Max duration of treatment: 4 wk including tapering. Hepatic impairment: As immediate release tab: 5 mg immediately before bedtime. Max duration of treatment: 4 wk including tapering. Severe: Contraindicated.

Child Dose

Not recommended

Renal Dose

Renal impairment: No dosage adjustment needed.

Administration

Should be taken on an empty stomach. Do not take w/ or immediately after a meal.

Contra Indications

Severe hepatic impairment.

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. Patient Counseling Patients should be warned about performing activities involving mental alertness or physical coordination after drug intake. Lactation: Very low amounts secreted in breast milk; effect on infant unknown; use caution; advise mother to observe breastfeeding infant for lethargy, increased sedation, and changes in feeding habits

Pregnancy-Lactation

Pregnancy Category: C Lactation: small amount secreted in breast milk, not recommended

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.

Adverse Effects

Side effects of Zolpidem Tartrate : >10% Dizziness (5-12%), Headache (7-19%), Drowsiness (6-15%) 1-10% Allergy (4%), Hallucinations (4%), Myalgia (4%), Sinusitis (4%), Memory disorder (3%), Visual disturbance (3%), Pharyngitis (3%), Lightheadedness (2%), Palpitation (2%), Rash (2%), Constipation (2%), Depression (2%), Drowsiness (2%), Asthenia (1%), Diarrhea (1%), Dry mouth (1%), Flu-like symptoms (1%) Potentially Fatal: Hepatitis, anaphylactic reactions, angioedema, sleep-driving (driving while not fully awake after drug intake, w/ no recollection of the event).

Mechanism of Action

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.