Index of drugs

Short-term and short-term in the treatment of sleep disorders: difficulty in falling asleep, frequent night awakening, early morning awakening.

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

Triazole benzodiazepine derivative. It works on many CNS structures, primarily on the limbic system and hypothalamus - structures associated with the regulation of emotional activities. It intensifies the inhibitory action of GABAergic neurons within the cerebral cortex, hippocampus, cerebellum, thalamus and hypothalamus. It increases the affinity of the GABA receptor for gamma-aminobutyric acid (GABA), which is an endogenous inhibitory neurotransmitter. The consequence of activating the benzodiazepine receptor or GABA-A is to increase the influx of chloride ions to the inside of the neuron via the chloride channel. This leads to hyperpolarization of the cell membrane and, as a result, to the inhibition of neuronal function. The clinical effect of estazolam is manifested by the hypnotic effect - it shortens the time of falling asleep, to a lesser extent it affects the lengthening of sleep and the number of night revivals. It also has low anticonvulsant properties and slightly reduces skeletal muscle tone. Estazolam is well absorbed from the gastrointestinal tract, reaching C_{It has}x after about 2 hours (0.5 - 6.0 h). It is 93% bound to plasma proteins. It penetrates the blood-brain barrier, across the placenta barrier and into the milk. It is metabolised in the liver to 4-hydroxy-estazolam and 1-oxo-estazolam, compounds with low activity. It is excreted in the form of metabolites mainly in the urine (> 90% of the dose) and in a small amount (approximately 4%) with faeces. Less than 5% of the administered dose is excreted unchanged in the urine. T_0,5 estazolam is 10-24 h.

Hypersensitivity to estazolam, other benzodiazepine derivatives or to any of the excipients. Severe respiratory failure, regardless of the cause. Sleep apnea syndrome. Dizziness, balance disorders. Disturbances of consciousness. Myasthenia gravis. acute porphyria. Alcohol poisoning or CNS depressants.

Benzodiazepines are not indicated for the treatment of psychotic disorders. They should not be used in monotherapy of depression or anxiety associated with depression, because such monotherapy may intensify suicidal tendencies. Benzodiazepines should be used with caution in patients with a history of alcohol, drug or drug addiction - closely observe patients, due to the risk of developing habituation and mental addiction. During the use of estazolam, post-amelioration may occur (especially if 7-8 h of uninterrupted sleep after taking the drug is not present), paradoxical reactions (in which case the drug should be discontinued), tolerance and addiction (especially during long-term use and in high doses and in abusing patients) alcohol and drugs or with personality disorders), the phenomenon of "rebound" and withdrawal symptoms (in case of sudden cessation of use). Do not use estazolam in patients with severe hepatic impairment (risk of encephalopathy). Caution in patients: elderly and / or weak (risk of worsening of side effects, mainly disorders of orientation and coordination, reduce the dose); with chronic respiratory failure (risk of respiratory depression, reduce the dose); with impaired renal function (take common precautions); with impaired liver function; with porphyria (the risk of worsening symptoms of this disease). During prolonged treatment with estazolam, a periodic blood test (morphology with a smear) and urine is recommended. The safety and efficacy of the medicine in children and adolescents <18 years has not been established. Due to the lactose content, do not use the preparation in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The use of estazolam in pregnancy, especially in the first and third trimester, is only permitted in a situation of absolute necessity when the use of a safer drug is impossible or contraindicated.Use in the last trimester of pregnancy or perinatal period may cause hypothermia, hypotension, cardiac arrhythmias, abnormal breathing and weakness of the sucking reflex in the newborn. In children of mothers receiving chronic benzodiazepines in the late pregnancy, physical dependence develops and there is a risk of symptoms of withdrawal syndrome after birth. You should not breast-feed during treatment with estazolam. If it is necessary to give the drug to the mother who is breastfeeding, the child should be put away from the breast.

Rare: nausea, stomach complaints, dry mouth. Very rare: anaphylactic reactions. Frequency unknown: paradoxical reactions - psychomotor restlessness, insomnia, increased excitability and aggressiveness, muscle tremors, convulsions (paradoxical reactions most often occur after alcohol consumption, in elderly patients and patients with mental illness); drowsiness, slow reaction, pain and dizziness, confusion and confusion, ataxia and, especially at high doses, dysarthria may occur with speech blurred and abnormal pronunciation, memory disorders, libido disorders; disorders in blood morphology, skin hypersensitivity reactions (rash, pruritus, urticaria), lack of appetite, blurred vision (blurred, double vision), bradycardia, chest pain, slight decrease in blood pressure, slight elevation of aminotransferase, liver dysfunction with jaundice, muscle tremors, muscle weakness, urinary retention, urinary incontinence, menstrual disorders, general weakness, fainting. During treatment with estazolam, pre-existing undiagnosed depression may appear. During the use of estrazolam (in therapeutic doses) psychological and physical addiction may develop. Abrupt discontinuation of treatment may result in withdrawal syndrome: headache, muscle pain, increased anxiety, tension, excitement, convulsion, sleep disturbances, irritability; in more severe cases: loss of sense of reality, personality disorders, hypersensitivity to sound, light, touch, numbness and tingling of limbs, hallucinations, epileptic seizures. During the withdrawal of estazolam, especially sudden, the "rebound" phenomenon may temporarily appear - the severity of the symptoms that caused the use of bezodiazepines; they may be accompanied by other symptoms such as mood swings, anxiety, sleep disturbances and insomnia.

Orally. Dosage and treatment time are determined for each patient individually. The drug should be used as short as possible (7-10 days). In individual cases, treatment may take longer. Do not prolong the treatment time without re-evaluating the patient's condition. Adults: usually 1-2 mg (1/2 - 1 tabl.) 30 minutes before bedtime. In elderly patients (> 65 years), it is recommended to reduce the dose by half. In patients with renal and / or hepatic insufficiency, it may be necessary to reduce the dose.