Index of drugs

Temporary and short-term treatment of sleep disorders (difficulty falling asleep, frequent night awakening, early morning awakening).

1 tabl contains 2 mg estazolam. The preparation contains lactose.

A drug from the group of triazole derivatives of benzodiazepines. Works on o.u.n. (brain, cerebellum, limbic system, hypothalamus, spinal cord). It shows hypnotic and anticonvulsant effect, and slightly reduces skeletal muscle tone. The effect of the drug is related to γ-aminobutyric acid (GABA) and the receptor complex, which includes the chloride channel, the GABAergic receptor and the benzodiazepine receptor. Benzodiazepine derivatives increase the affinity of GABA and GABA agonists to receptors, enhancing the action of GABA in various brain structures. The preparation shortens the period of falling asleep by 15-20 minutes. compared to placebo. It affects the lengthening of sleep and the number of awakenings at night to a lesser extent. Following oral administration, estazolam is absorbed in the gastrointestinal tract, reaching C_maxmore or less after 2 hours. The blood proteins are 93% bound. The drug penetrates the blood barrier - the cerebrospinal fluid, through the placenta and into the breast milk of lactating women. The drug is metabolised in the liver to inactive derivatives. In patients with hepatic impairment a reduction in the constant rate of elimination of the drug by approximately 100%, prolongation of T is observed_0,5 by about 100% and increase the area under the concentration curve (AUC) by about 50%. T_0,5 is 10-24 h after single administration. Smoking increases the clearance of the drug and reduces the half-life. Estazolam is excreted in the urine (over 90% of the dose) and faeces (<4%) in the form of metabolites. Less than 5% of the dose is excreted unchanged in the urine.

Hypersensitivity to estazolam, other benzodiazepine derivatives or to any of the excipients. Myasthenia gravis. Severe respiratory failure. Pregnancy and breastfeeding. Severe hepatic failure. Sleep apnea syndrome. Glaucoma with closed angle of perception.

Tension and anxiety related to everyday problems are not an indication for the use of estazolam. Patients who use estazolam long-term or in high doses should remain under constant medical supervision. Long-term use of the drug leads to a gradual weakening of its effect as a result of the development of tolerance. Maintaining or increasing insomnia after a 7-10 day period of use of estazolam may indicate a different basis of the disorder and provide an indication for the verification of the diagnosis. Prolonged use of estazolam may lead to physical and mental dependence. The risk of addiction increases with increasing the dose and duration of the drug and in patients who abuse alcohol and drugs. Estazolam should be used with extreme caution in patients with mental illness and in patients after antidotal treatments after an overdose, eg drugs. Caution should be exercised in patients with hepatic impairment, renal insufficiency and in patients over 65 years of age. In these patients, it is recommended to reduce the initial dose and individual dose setting depending on the patient's condition. Elderly patients are at increased risk of side effects, especially orientation disorders and motor coordination. Estazolam may increase respiratory failure. Caution should be exercised in patients with impaired breathing and the lowest recommended doses should be used. The drug should be discontinued in case of paradoxical reactions (psychomotor agitation, insomnia, irritability, delusions, nightmares, hallucinations, psychosis, change in behavior). Estazolam may cause post-amelioration especially in the absence of 7-8 h of sleep after taking the drug. There are no data on the safety and efficacy of the medicine in children and adolescents under 18 years of age - use is not recommended. During long-term use of estazolam, a periodic blood test (morphology with a smear) and a urinalysis are recommended. During treatment with estazolam and up to 3 days after its completion, do not consume any alcoholic beverages.The product contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Estazolam is contraindicated for use in pregnancy and breast-feeding. If pregnancy is suspected, estazolam should be discontinued. Taking the medicine during the last three months of pregnancy and during delivery may cause hypothermia, hypotension and respiratory failure.

Common: drowsiness during the day, headaches and dizziness, drowsiness, asthenia, nervousness, thinking disorders, disorientation, prolonged reaction time; nausea, constipation; bow; dryness of the oral mucosa, malaise, weariness, general weakness. Rare: posteleval amnesia, apathy, dysgeusia, ataxia, decreased libido; vomiting, bloating; emotional lability, paradoxical reactions (states of psychomotor agitation, insomnia, irritability, delusions, nightmares, hallucinations, psychoses, change of behavior); rash, urticaria; palpitations, arrhythmia; fainting, increased thirst; change of appetite, change of taste, change of body weight; muscle spasms, joint and muscle pain; cough, asthma; blurred vision; menstrual disorders; changes in the blood picture (leukopenia, agranulocytosis). The frequency of side effects increases after exceeding the recommended therapeutic doses. Elderly people may experience neurological symptoms (feeling of fatigue, impaired coordination of movements, skeletal muscle tone disorders); these symptoms can cause falls and dangerous bone fractures. Sudden discontinuation of the drug after long-term use of high doses may cause symptoms of withdrawal syndrome, the symptoms of which are: insomnia, headaches, muscle pain, increased anxiety and tension, psychomotor agitation, splicing and irritability; in severe cases depersonalization, derealization, hyperaesthesia, numbness and tingling of limbs, hypersensitivity to light, noise and touch, hallucinations or epileptic seizures may occur. The severity of symptoms of the withdrawal syndrome depends on the time of application and the dose of the drug. In patients using high doses of the drug or using the drug for more than 4 weeks, the drug should be discontinued under the supervision of a doctor, gradually reducing the doses. The drug may cause post-mortem ambulance especially in the absence of 7-8 h of sleep after taking the preparation.

Orally. Dosage is selected individually depending on the age and patient's response to the drug. Adults: the initial dose administered is 1-2mg (1 / 2-1 tabl.) 30 minutes before bedtime. In older patients (over 65 years), the dose should be halved. In patients with renal and / or renal failure, a dose reduction is recommended. Treatment should start with the lowest recommended dose.