A sleeping drug from the imidazopyridine group. The mechanism of action consists in binding to the benzodiazepine receptors of the GABA receptor complex, modulating the opening of the chloride channel. Zolpidem is a relatively selective agonist of the omega-1 (BZ1) subunit. In contrast to benzodiazepine derivatives that bind non-selectively to all three subtypes of the omega receptor, in hypnotic doses zolpidem does not exert anticonvulsive and anti-muscular effects. The drug accelerates falling asleep, reduces the number of awakenings at night, increases sleep time and improves the quality of sleep. After oral administration, zolpidem is rapidly absorbed from the gastrointestinal tract, reaching a maximum concentration in the blood after 0.5-3 h. The bioavailability is 70%. Plasma proteins are approximately 92% bound. It is metabolized in the liver to inactive metabolites, which are then excreted in urine (56%) and faeces (37%). T0,5 is about 2.4 hours. Increased blood levels are observed in the elderly and in patients with hepatic impairment. In patients with renal failure (regardless of dialysis), the clearance of the drug is reduced.
Contraindications:
Hypersensitivity to zolpidem or other ingredients of the preparation. Sleep apnea syndrome. Severe and / or severe respiratory failure. Myasthenia gravis. Severe hepatic failure. Poisoning with neuroleptic or antidepressant drugs. Children.
Precautions:
Carefully used in patients with depressive symptoms (the drug should be prescribed in the smallest amount due to the risk of intentional overdose), alcohol and drug abuse drugs in the elderly. Due to its lactose content, the preparation should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
The preparation should not be used during pregnancy (especially in the first trimester). The drug used in the third trimester of pregnancy or during delivery can cause hypothermia, hypotension and respiratory failure in the newborn. Zolpidem is excreted in small amounts in breast milk - it is not recommended to use the drug during breastfeeding.
Side effects:
Daytime sleepiness, reduced mental performance, confusion, fatigue, headache and dizziness, muscle weakness, gait disturbances or double vision usually occur at the beginning of treatment. Other activities have been described less frequently, such as gastrointestinal disorders, decreased libido or skin reactions. Post-mortem obliteration may occur after the use of therapeutic doses; the risk increases at higher doses. Psychological and paradoxical reactions may occur (insomnia, agitation, irritability, aggression, hallucinations, tantrums, nightmares, psychoses, inappropriate behavior, somnambulism) - the probability of these reactions is greater in the elderly. During the use of the drug, an existing depression may be revealed. Uncommon: sweating, paleness, orthostatic hypotension, agitation, decreased cognitive ability, decreased concentration, hallucinations, emotional instability, migraine, paresthesia, tremors, stupor, swallowing difficulties, flatulence, winds, hiccups, gastritis and intestinal inflammation, cerebrovascular disorders, hypertension, tachycardia, increased γ-glutamyltransferase activity, hyperglycemia, arthritis, menstrual disorders, vaginitis, bronchitis, cough, dyspnea, pruritus, urethritis, urinary incontinence, malaise, edema, injuries, fever . The drug may induce post-mortem. Long-term use of the drug may cause the development of tolerance to the drug and the occurrence of physical and mental dependence.Abrupt discontinuation of treatment in such cases may lead to withdrawal syndrome (headache and muscle pain, anxiety, mental tension, anxiety, confusion, irritability, in severe cases: derealization, depersonalization, hypersensitivity to touch, acoustic stimuli and light, numbness and tingling of the limbs) , hallucinations and fits) or transient insomnia "with rebound".
Dosage:
Orally. Adults: 10 mg / day. In patients with hepatic impairment, in the elderly, in patients who are debilitated, treatment should start with a 5 mg dose; if you do not respond to treatment, if the patient tolerates the medicine well, the dose can be increased to 10 mg. The maximum daily dose of zolpidem is 10 mg. The tablets should be taken immediately before sleep, do not chew or drink water. To reduce the risk of follow-up obstruction, the patient should be given an uninterrupted 7-8-hour sleep after taking the medicine. Treatment with the preparation should last as short as possible; the treatment period should usually be several days up to 2 weeks, up to 4 weeks including the dose reduction period.