Temazepam

Chemical name

7-Хлор-1,3-дигидро-3-гидр окси-1-метил-5-фенил-2H-1, 4-бензодиазепин-2-он

Gross

C16-H13-Cl-N2-O2

Characteristics

Derived Benzodiazepina.beloe TNT substance. Very bad rastvorimo water well rastvorimo in ethanol.

Of drugs

Drugs, the pills, sedative. Interacts with specific receptors benzodiazepinovmi located in postsinapticescom Gamk_a-retseptornom compound in the limbic system of the brain, activating blood retikuliarna formation gippocampe, inserted neuron horns lateral spinal cord. Increases sensitivity to Gamk-retseptorov mediatoru (GABA). As a result of increasing frequency transmembrannah opening channels for incoming currents chlorine ions occurs giperpoliarization membranes and eventually potenziruetsa the endogenous mediator brake - GABA. Hypnotic and sedative effect largely due to oppression activity of cells retikuliarna activating system barrel Mozga.effectiven head for the short-term treatment of insomnia characterized by difficulty sleep, frequent nightmares, and / or early morning probujdeniami. It may be effective in preventing and treating insomnia related to drastic changes in the Sna.kak in preclinical studies, as well as out-patient has been shown that the admission temazepama within 30 minutes prior to the night of sleep shorter period sleep and increases the depth of sleep in patients with chronic insomnia. Similar effects were observed and the people with a short-term (temporary) insomnia related to adaptation to the new Meste.proavlet moderate protivosudorozhnoe, miorelaksirutee (central) and antifobicescoe действие.Исследовани�� reproduction in animals showed that the introduction of rats doses of 60 mg / kg / day of the interior of increased mortality sossounkov, doses of 120 mg / kg / day, an increase in the frequency of rezorbtion fruit doses above 240 mg / kg / day, showing a rudimentary ribs. Introduction krolikam doses of 40 mg / kg / day and above increases the frequency of the 13th rib. Is such abnormalities in rabbits as exenzefalia and merging or asymmetry ribs, regardless of Dozy.issledovanie carcinogenicity if added to food temazepama revealed that the rats exposed to 160 mg / kg / day taken for a period of two years, and in mice doses of 160 mg / kg / day for one and a half years, did not cause cancer-causing, although high doses of female rats in the liver found giperplazirovanne Uzelki.vlijania fertility not Vemeno.v experimental studies showed that ELD_50 temazepama with ingestion of 1963 mg / kg (mouse), 1833 mg / kg (rats), more than 2400 mg / kg (rabbits). Once inside quickly and well absorbed from the digestive tract. In a small extent (8%) are primary metabolizmu in the liver. C_max achieved in 1-2 hours Equilibrium concentration in the blood is usually for a few (about 3) days after the start of the regular admission temazepama. Linking plasma protein is 96%. Passes through GEB and placental barrier, enters the breast milk. Biotransformiroetsa in the liver with the formation of active metabolites : major metabolite - O-kongugat temazepama (90%), as well as O-kongugat N-desmetil-temazepama (7%). There is a two-phase eliminatiu from plasma with T_1/2 first phase 0.4-0.6 h, the second-3,5-18,4 p (average 8.8 hours). Report mostly kidneys (90%) as inactive glukuronidov, T_1/2 - 8-12 hours Metabolites koumouliruut not.

Indications

Violations sleep different genesis, premedikation in preparation for the operational surgical and diagnostic procedures.

Restrictions on the use of

Violation of the liver and / or kidney problems, depression.

Pregnancy and lactation

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

Contraindications

Hypersensitivity, violations of respiratory central origin, expressed respiratory distress, drug or alcohol dependence, the sense of violation, male, zakratougolnaya glaucoma, pregnancy, breast-feeding, age and 18 years of age (the safety and effectiveness of the variables).

Side-Effects

According to the results of controlled clinical Ispatani.so the nervous system and sensory organs : drowsiness (9.1%), headache (8.5%), fatigue (4.8%), irritability (4.6%), lethargy (4.5%), dizziness (light-4.5% expressed 1.2%), posleactie (2.5%), anxiety (2.0%), depression (1.7%) or euphoria (1.5%), weakness (1.4%), sputannosti consciousness (1.3%), lack of (1.3%) nightmares (1.2%); 0.5-0.9%, loss of appetite, coordination of movements and balance, tremor, insomnia (sleep better, the increase in the number IDulcinea); less than 0.5% amnesia, hallucinations, horizontal movement, paradoxical reactions (including ajitation). For part of the intestine : nausea (3.1%), dry mouth (1.7%), diarrhea (1.7%), the sense of discomfort in the abdomen (1.5%) vomiting (0.5-0.9%). Other : 0.5-0.9% breath, rapid heartbeat, pain in the back, in the lower back, sweating, pain in Glazah.vozmozhno of Drug Dependence, the syndrome (see "Precautions").

Patient interaction

Funds depressing central nervous system (neiroleptiki, barbiturates, narcotic analgesics, antidepressants, for narcosis, etc.) make temazepama effect. Alcohol, in addition to strengthening the depressive effect on the central nervous system, can cause paradoxical reaction (agitation aggressive behaviour, the state of pathological intoxication).

Overdosing

Symptoms : drowsiness, disorientation, indiscriminate speech oppression reflexes, coma; Possible respiratory depression, Gipotenzia.lechenie : induction vomiting and the appointment of activated charcoal (if the patient is in the minds of) washed through the stomach probe (if the patient is unconscious), monitoring vital functions, symptomatic treatment, in / with the introduction of liquids (for enhanced diureza). In the case should not be used barbiturates. Specific antidote - flumazenil (BZ antagonist receptors).

Precautions

Be wary of patients over 65 years of age (polovinne recommended dose). For patients with impaired liver and / or kidney recommended reducing Dozy.otsutstvie clinical effect in the treatment of insomnia in one week to 10 days may be an indication of other diseases. In patients taking temazepam over 2-3 weeks, a periodic reassessment of the effectiveness to determine whether further Ispolzovania.pri admission temazepama possible development of drug dependence and withdrawal syndrome. To prevent the syndrome dose gradually reduce (Quick aside, especially in the long-term therapy or therapy high doses can sleep disorders and mood, and personality disorders). During treatment, and within 3 days after the lifting temazepama to refrain from driving motor vehicles and other classes that require greater attention, rapid mental and motor Reackzi.ne should simultaneously use other means, depressing central nervous system, as well as alcohol.

Dosing and Administration

Inside. The dosage and duration of treatment set individually. Treatment starts with the minimum effective dose. The average intake for adults 10 to 20 mg (30 mg) once for 30 minutes before sleep. Duration of therapy averages 7-10 Dnei.premedikation : 20-40 mg for 30 to 60 minutes before the surgery or diagnostic procedures.

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