Estazolam

Chemical name

8-Хлор-6-фенил-4H-[1,2,4]три азоло[4,3-а][1,4]бензодиа��епин

Gross

C16-H11-Cl-N4

Characteristics

Triazolovoe benzodiazepine derivative. White powder odourless, soluble in alcohol, nerastvorim almost in the water.

Of drugs

Drugs, the pills, sedative. Has also antifobicescoe, protivosudorozhnoe and weak miorelaksirutee (central) действие.Взаимодейст��ует to the specific benzodiazepinovmi receptor located in postsinapticescom Gamk_a-retseptornom complex limbic system gippocampa, upstream activating retikuliarna formations barrel cord neuronal inserted horns lateral spinal cord. Increases sensitivity to Gamk-retseptorov mediatoru (GABA), which leads to an increase in the frequency of opening channels to zitoplazmaticescoy neuronal membrane for incoming ion currents chlorine giperpoliarization postsinapticescoy neirona membranes resulting increased braking power GABA in Zns.snotvornyi and sedative effect mainly due to oppression activity retikuliarna activating system barrel brain limbicakih and subcortical divisions and Kora.ukoracivaet period sleep, reduces the number of night probujdeni increases Sna.effectiven duration for the treatment of temporary insomnia related to drastic changes in the Sna.v two studies in mice receiving estazolam food in doses 0.8; 3, and 10 mg / kg / day, and rats (in doses 0.5; 2, and 10 mg / kg / day) HPV is not found. With the mice doses of 3 and 10 mg / kg / day revealed an increase in the frequency of liver giperplazirovannah door, but the significance of this phenomenon is not Opredeleno.v relevant tests on mice, rats, and bacteria found to be lacking mutagennogo Actia.ne identified impact on the fertility of male and female rats with doses up to 30 times higher than normally recommended for Cheloveka.posle intake of a well-absorbed from the digestive tract. C_max achieved through two hours (from 0.5 to 6900). Linking blood protein 93%. Equilibrium concentration in the plasma is achieved in a few days. Passes gistogematicalkie barriers, including GEB is determined in the tissues of the central nervous system. Passes through the placenta. Is not known whether the move estazolam in breast milk (studies in humans should be held), but experiments showed that estazolam and its metabolites enter the milk of rats. Metabolised in the liver, is oxidized and gidrauxilirovaniu c low education or inactive metabolites, including 4-gidroksi-estazolama (concentration of 12% of the dose estazolama through 8 h after administration) and 1-okso-estazolama. T_1/2 - 10-24 hours (average 17 hours). Report the news is in the form of metabolites (less than 5% in an unmodified form), 4% in unaltered with faeces. In repeated moves koumouliruet slightly.

Indications

Sleep disorders (sleep difficulty, frequent night and / or early morning awakening), fear, increased arousal, irritability and nervousness and psihopaticakih violations, and psychosomatic disorders (including cardiovascular); Premedikation (on the preparation of operations and complicated diagnostic manipulation).

Restrictions on the use of

Under the liver and / or kidney age to 18 (security and the effectiveness of the variables).

Pregnancy and lactation

Contraindicated in pregnancy (the risks related to estazolama in pregnant women exceeds the potential benefits). At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, infants expressed respiratory distress, violation of consciousness and / or balance zakratougolnaya glaucoma, the propensity to abuse drugs, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : sleepiness (42%), headache (16%), fatigue (11%), hypokinesia (8%), irritability (8%), dizziness (7%), malaise (5%), the coordination of movements (4%), sputannosti consciousness (2%), of thinking (2%), depression (2%); 1% emotional lability, reducing memory and concentration, slow reactions, visual impairments, Strange reaction (agitation, insomnia, aggressiveness, muscle tremor). For part of the intestine : nausea (4%), diarrhoea phenomenon (2%); 1% Rvota.so the circulatory system and blood (blood, gemostaz) : 1% heartbeat, irregular, fear, lakopenia, Agranulozitoz.prochie : myshern-sustaus pain (1%); 1% lung muscles, allergic reactions, including Zud.vozmojna addiction, drug dependency (with a long reception), the syndrome (see "Precautions").

Patient interaction

Setback impact on the central nervous system increase barbiturates gipotenzivee preparations Tricyclic antidepressants, antihistamines PP with sedative effects, anti-convulsants, narcotic analgesics and other means, depressing central nervous system. Alcohol increases the estazolama and could provoke paradoxical reaction. Oral contraceptives and smoking tobacco accelerates metabolism estazolama and weaken its effect.

Overdosing

Symptoms : expressed drowsiness, respiratory depression, sputannosti consciousness, the coordination of movements, baffling speech Koma.lechenie : induction vomiting (if the patient is in the minds of) washed through the stomach probe (if the patient is unconscious), the admission of activated carbon symptomatic therapy, monitoring vital functions, / in a liquid, if necessary IVL. Haemodialysis ineffective. As a specific antidote used benzodiazepines antagonist flumazenil (in the hospital).

Precautions

The paradoxical reactions more likely, the combination treatment of hosting alcohol, as well as in older patients. In the event of a paradoxical reactions should immediately discontinue use of the Estazolama.s caution was necessary to appoint people with the symptoms of depression (possible traumas). Prolonged use can lead to addiction, to promote the development of mental dependence. Remove product gradually to avoid withdrawal Development syndrome (agitation, fear, lunch violations insomnia). During treatment, and within three days after the end should be deleted reception alcohol; Drivers of vehicles and people whose work requires quick mental and physical reactions, and was linked to elevated concentrations of attention during this period should not engage in professional Deatelnostu.v the long-term care needs periodic monitoring picture peripheral blood.

Dosing and Administration

Inside, adults. The mode set individually, and treatment should start with the lowest effective dose. As a listed vehicle : 1-2 mg for 30 minutes before sleep, nervousness in the average dose of 2-4 mg / day in divided doses for Then 2 mg of Operatiei.u weakened patients, patients over 65 years of age, patients with hepatic and / or renal failure treatment start with half-doses.

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