Triazolam

Chemical name

8-Хлор-6-(2-хлорфенил)-1-м етил-4H-[1,2,4]триазоло[4,3- a][1,4]бензодиазепин

Gross

C16-H12-Cl2-N4

Characteristics

Red means triazolovoe benzodiazepine derivative. The white crystalline powder. Rat in alcohol, poorly soluble in water.

Of drugs

Drugs, the pills, sedative. Interacts with specific receptors benzodiazepinovmi 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 for incoming ion currents chlorine, giperpoliarization postsinapticescoy neuronal membranes resulting increased braking power GABA in Zns.snotvornyi and sedative effect mainly due to oppression activity of cells retikuliarna activating the barrel head Mozga.v preclinical studies and in the treatment of outpatients showed that triazolam shorter period sleep, reduces the number of night probujdeni increases the duration of sleep. There is a significant impact on the III and IV stages of sleep and rapid phase of the eye apples, which have little impact on the structure of sleep, causing sleep close to the natural. After receiving triazolama sleep is a 10-30 minutes and continued until 0730 Effective in the treatment of temporary insomnia related to the sudden changes in sleep. Weak in the early probujdeniah, morning and afternoon Trevoge.ustanovleno that after weeks of admission to the night hypnotic effect triazolama down. The first and / or second night after the lifting of a syndrome "impact" (rebound-sindrom), reflecting Bessonnica.posle reception inside quickly and almost completely absorbed from the digestive tract. C_max achieved within 1-2 hours Associated with the plasma protein of 89%. Treated biotransformation in the liver. T_1/2 of 1.5 p (2.7 h). Passes through the placenta, enters the breast milk. Report the news is in the form of metabolites (80%) and unchanged to (1%), 8% from faeces. When taken repeated doses up Minimalnoe.pri oral introduction Guard carbon (14 ^ C) triazolama pregnant mice showed that it creates in the brain of the fruit, nearly the same with that determined by the brain Materi.v two studies in mice with a dose 4,000 times exceeding dose for humans, cancer is not detected.

Indications

Short-term and temporary sleep disturbance; Prolonged sleep disturbance (short course of combination therapy).

Restrictions on the use of

Depression, suicidal tendencies expressed pulmonary insufficiency, patients in a dream, drug addiction (including propensity to its development), the functions of the liver.

Pregnancy and lactation

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

Contraindications

Hypersensitivity, incl. other benzodiazepines, pregnancy, breast-feeding, age and 18 years of age.

Side-Effects

According to the плацебо-контролируем��х clinical studies of 1003 patients with an oral application for the 1-42 Dnei.so the nervous system and sensory organs : sleepiness (14%), headache (9.7%), dizziness (7.8%), feeling dizziness (4.9%), nervousness (5.2%), the coordination of movements / ataxy (4.6%); less than 1% euphoria, fatigue, impaired memory, vision and taste, ringing in the ears, depression, increase in the number of IDulcinea or when nightmares, insomnia, paresthesia, dizestesia, Slabostj.prochie : nausea / vomiting (4.6%); less than 1% tachycardia, causes / pain, constipation / diarrhea, dry mouth, hyperemia, �ерматит/аллергически е Reaktion.vozmozhno of addiction, drug dependence, the syndrome, as well as the syndrome "impact" (rebound-sindroma) (see "Precautions"); recorded death from insufficient liver function in the patient receiving a dioretiki.

Patient interaction

Together appointment of oppressive central nervous system (neiroleptiki, barbiturates, and anaesthetic gipotenzivee PP, some antihistamines PP, alcohol, etc.) increased action. Zimetidin increases triazolama concentration in the blood. Macrolides down triazolama metabolism in the liver, increasing its concentration in the blood (twice) and T_1/2. Drugs slows down and increases triazolama concentration in the blood.

Overdosing

Symptoms : slumber, sleep, sputannosti consciousness, the coordination of movements, convulsions, smazannaya speech respiratory depression, patients, Koma.lechenie : washing stomach, monitoring vital functions, symptomatic therapy, in / in a liquid, if necessary IVL. As a specific antidote used BZ antagonist flumazenil receptors (the стационара).Гемодиали з ineffective.

Precautions

Not designed for long-term use. It is desirable to limit the reappointments patients who are not under the supervision of Vracha.s use caution in patients with depression (possible traumas). In addition to the above undesirable effects (see "Side Effects"), there have been reports of a following violations related to the treatment triazolam : amnesticskie symptoms (anterogradnaya amnesia with the ordinary or unusual behaviour), the consciousness (disorientation, derealization, clouded consciousness, etc.), distonia, fatigue, sedation, it sputannaya, sleeping, somnambulism, monster, anorexia, jaundice, prurit, dizartria, changing face, the menstrual cycle, urinary and delay �очеиспускания.Имеютс я reports that a process of thinking and / or behavior related to the treatment triazolam, in the form of new aggressiveness, hallucinations nonsense, hands behaviour ajitation, depersonalization (the so-called paradoxical reaction). Growing insomnia, or the emergence of new violations of the process of thinking and behaviour in the face of triazolam treatment may be due to nerspoznannogo mental or somatic Rasstroistva.v event of a paradoxical reaction, discontinue use of multiple Triazolama.pri application for more than two weeks may be a recreational (hypnotic effect can be somewhat alleviated) and Drug Dependence (as in the application of therapeutic doses, and to the reception of high doses). The risk of addiction elevated in patients with alcohol and drug dependency and personal and behavioural Narusheniami.sleduet bear in mind that such side effects such as drowsiness, dizziness and amnesia are Dozozawisimami.pri a dramatic admission to a lifting syndrome (tremor, convulsions, abdominal or muscle cramps, nausea, perspiration, suffering, perception disorder, insomnia) most often comes to the reception of high doses or after long-term care insurance, even though the syndrome can be and to the reception of therapeutic doses triazolama within 1-2 weeks. Lifting should be implemented in a gradual manner, especially in patients with Epilepsiei.imeutza reported on the development of some patients phenomenon of "value" after 10 days of continuous employment (manifested in the form of insomnia at night and pervasive anxiety day). If there has been increasing daily concerns triazolam treatment recommended Prekratiti.v the long-term care needs periodic monitoring picture peripheral Krovi.esli triazolam is wasting time, it may be designated by the people profession which requires prompt and propulsion reaction (patients should be alerted to the possibility of lowering the speed of response when dealing with the mechanisms and driving). The treatment should not drink alcoholic �апитки.Антероградная �mnesia is more often while admission triazolama with other benzodiazepines. There are reports of a "Jewish tourists", occurred in the admission triazolama as listed in the travel (for instance, the flight of aircraft). This effect, in some cases, was due to a lack of sleep (before awakening and the start of activity) and the accompanying admission alcohol.

Dosing and Administration

Inside. The dosage and duration of treatment set individually, depending on the testimony of clinical effect endurance, etc. Treatment should start with the smallest effective dose. The average dose for adults 0,125-0,25 mg once at night; Maximum dose of 1 mg. For the elderly and handicapped patients average dose of 0,125 mg (the maximum is 0.25 mg).

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