A hypnotic drug not belonging to the benzodiazepine group. The mechanism of action is based on a significant and relatively selective binding to the omega benzodiazepine receptors1. It only slightly affects the benzodiazepine omega receptors2, practically does not affect the function of omega benzodiazepine receptors3. Zolpidem significantly shortens the time of falling asleep, reduces the frequency of nocturnal awakenings, increases the total sleep time and improves its quality. It does not affect the REM phase or respiratory function. It has low anxiolytic and myorelaxant properties that are not clinically relevant. After oral administration, zolpidem is rapidly absorbed (food reduces absorption of the drug). It is subject to the "first pass" effect in the liver, total bioavailability is about 70%. The maximum concentration of the drug in the blood is reached after 1.5-3 h after administration. 90-92% of the drug is bound to plasma proteins. T0,5 after one use it is 1.5-2.4 hours; after 15 days of treatment, it is reduced to 1-1.8 hours. In the case of liver failure, this period increases up to 9.9 hours. In the liver, the drug is metabolized to 3 main, inactive metabolites. 79-96% of the administered dose is excreted in the urine and faeces in the form of metabolites, less than 1% of the dose is excreted in the urine in unchanged form. The medicine in minimal amounts is excreted in breast milk.
Contraindications:
Hypersensitivity to zolpidem or other ingredients of the preparation. Do not use in children and adolescents under 18 years. Do not use in patients with sleep apnea syndrome, myasthenia gravis, severe hepatic impairment, acute respiratory distress, breathing disorders, and in patients with mental illness.
Precautions:
Long-term administration of zolpidem is not recommended. Use with caution in patients with depressive symptoms and use caution in people who abuse drugs or alcohol. If paradoxical reactions occur after use of zolpidem, discontinue use. Use with caution in the elderly and hepatic impairment. After a few weeks of use, tolerance to zolpidem may develop. Due to the possibility of chronic obstruction, the patient should be provided with 7-8 hours of sleep after using zolpidem. Long-term use of the drug (more than a few weeks) may cause the development of tolerance to the drug and the occurrence of psychological dependence. Abrupt discontinuation of treatment in such cases may lead to withdrawal symptoms (headache and muscles, increased anxiety and tension, restlessness, confusion, irritability). In addition, discontinuation of treatment may lead to temporary insomnia "from rebound". Some patients have paradoxical reactions (anxiety, agitation, aggression, hallucinations, psychoses) - the drug should be stopped immediately; these reactions may occur especially in the elderly. The drug contains lactose, therefore it should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
The safety of the drug during pregnancy - cat. B. Due to the lack of clinical experience, it is not recommended to use the drug during pregnancy, especially in the first trimester, and during breastfeeding. The use of the drug in the final period of pregnancy or during delivery may cause hypothermia, hypotonia and respiratory depression in the newborn.
Side effects:
Common: hallucinations, agitation, nightmares, dizziness, headache, severity of insomnia, aftermath; diarrhea, nausea, vomiting, abdominal pain; fatigue. Uncommon: confusion, irritability; double vision. Frequency unknown: anxiety (especially motor), aggression, delusions, inappropriate behavior, somnambulism, addiction, libido disorders, disturbances of consciousness; rash, pruritus, urticaria, hyperhidrosis, angioneurotic edema; muscle weakness; gait disturbances, tolerance to the drug; increase in liver enzymes.Zolpidem can mask depression. The incidence of adverse reactions (especially those related to o.u.n.n.n. and intestinal tract) increases with increasing dose.
Dosage:
Orally, individual depending on the patient's condition. Adults: usually 10 mg (1 tablet) immediately before going to bed. The beginning of the action occurs between 7 and 27 min. from taking. In patients with hepatic impairment, in patients over 65 years of age and in patients who are attenuated, treatment should be started with 5 mg. In people over 65, if necessary, the dose can be increased to 10 mg a day. Long-term use is not recommended - the duration of treatment should not exceed 2 to 4 weeks, including a gradual reduction of the dose.
(C)
