Zolpidem is a hypnotic drug belonging to the group of imidazopyridines, and is a selective agonist of the subclass of omega1-benzodiazepine receptors. The drug has sedative action, while the normal doses do not have anxiolytic, anticonvulsant and central muscle relaxant actions.



Pharmacological action

Zolpidem is a hypnotic drug belonging to the group of imidazopyridines, and is a selective agonist of the subclass of omega1-benzodiazepine receptors. The drug has sedative action, while the normal doses do not have anxiolytic, anticonvulsant and central muscle relaxant actions. It stimulates benzodiazepine receptors (omega) in the alpha-subunit of GABA-receptor complexes localized in the region of the IV-th  plate of sensory-motor areas of the cortex, reticular departments of black substance, visual hillocks of ventral thalamic complex, bridge, pale globe and other interaction with omega-receptors leads to the discovery of neuronal Informix channels for ions chlorine.

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It shortens the time to fall asleep, reduces the number of night awakenings, increases total sleep duration and improves its quality. It extends phase II of sleep and the deeper stages of sleep (III and IV phases). It does not cause drowsiness during the day.


Zolpidem is rapidly absorbed from the gastrointestinal tract. The time to reach Cmax in plasma after oral administration is 0.5-3 hours. Bioavailability is 70%, tying with the plasma protein – 92%. There is a linear relationship between the magnitude of the dose and its concentrations in plasma. It is metabolized in the liver to form three active metabolites, which are excreted by the kidneys (56%) and through the intestine (37%). The average T1/2 is 2.4 h Vd – 0.5±0.02 l/kg. It does not induce liver enzymes. Clearance in plasma of elderly people can be reduced without a significant increasing of T1/2 (average 3 hours), while Cmax is increased by 50%. Clearance increases slightly in case of patients with acute violations of the kidneys. Patients with liver disorders experience the increasing of bioavailability, T1/2 increases up to 10 h. It stands out in small quantities in breast milk.

Indications for use

— sleep disturbances: difficulty falling asleep, early night awakening.

Dosing regimen

It is taken inside (just before bedtime) in a dose of 10 mg.

The treatment starts with a dose of 5 mg in case of old patients with live disorders. If necessary (lack of clinical effect) and good tolerability, the dose may be increased to 10 mg. The maximum daily dose is 10 mg. The treatment course should not exceed 4 weeks. If you experience transient insomnia, the recommended course of treatment is 2-5 days, the course of the situational insomnia is 2-3 weeks.

Very short treatment periods do not require gradual withdrawal of the drug. Zolpidem cancellation should be done gradually (at first – the reduction of the daily dose and then the withdrawal of the drug) in the case of long-term reception of medication to minimize the development of rebound insomnia.

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Side effects

Zolpidem is usually well tolerated.

The incidence of adverse reactions: very often – more 10%, often -more than 1% and less than 10% infrequently – more than 0.1% and less than 1%) rarely – more than 0.01% and less than 0.1%, very rare – less than 0.01% (including isolated cases), frequency is unknown (based on the available information establishing the frequency of occurrence of impossible).

From the nervous system: often – drowsiness, feeling of intoxication, headache, dizziness, increased insomnia, anterograde amnesia (amnesia effects may be associated with behavioral responses), the risk of which increases in proportion to the dose, hallucinations, agitation, nightmares; infrequently – confusion, irritability; the frequency is unknown – impaired consciousness, dysphoria, aggression, visual and auditory hallucinations, irritability, behavioral responses, somnambulism, drug dependency (can develop even when using therapeutic doses), in case of removal of the drug – withdrawal or rebound insomnia, decreased libido, impaired gait, ataxia, falls (mainly elderly patients), drug addiction (decrease of sedative and hypnotic action when applying for weeks). Most of the side effects from psychiatric are paradoxical reactions.

From the digestive system: often – diarrhea, nausea, vomiting, abdominal pain; frequency is unknown – increase in liver enzymes.

From the side of musculoskeletal system: frequency unknown – muscle weakness.

From the skin: incidence unknown rash, pruritus, urticaria, hyperhidrosis.

Allergic reactions: frequency unknown – angioedema.

Other: often – fatigue; rare – diplopia.

Drugs contraindications.

— acute and/or severe respiratory distress;

— severe acute or chronic liver failure;

— sleep apnea (including in advance);

— in connection with the presence of lactose: hereditary lactose intolerance, lactase deficiency or malabsorption syndrome of glucose-galactose;

— pregnancy;

— lactation;

— children’s age (under 18);

— hypersensitivity to zolpidem or other component of the drug.

Caution: myasthenia gravis, respiratory failure, hepatic failure of mild and moderate severity, depression, alcoholism, drug abuse and other addictions.


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