Oxazepam

Chemical name

7-Хлор-1,3-дигидро-3-гидр окси-5-фенил-2Н-1,4-бензо диазепин-2-он

Gross

C15-H11-Cl-N2-O2

Characteristics

Anksiolitik benzodiazepinovogo Rada.bely or white with a slightly yellowish white crystalline powder odourless. Virtually nerastvorim water, little soluble in ethanol, chloroform, ether, soluble in dimethylformamide.

Of drugs

Drugs, the anxiolytic, sedative, sleeping. Interacts with specific receptors benzodiazepinovmi located in postsinapticescom Gamk_a-retseptornom compound in the limbic system of the brain, activating blood retikuliarna formations barrel brain and neuron inserted horns lateral spinal cord. Increases sensitivity to Gamk-retseptorov mediatoru (GABA). As a result of increased frequency of discoveries in zitoplazmaticescoy neuronal membrane transmembrannah channels for incoming currents chlorine ions. The giperpoliarization membranes and oppression neironalna activity. Thus increasing braking vlijaniae GABA in Zns.okazavaet soothing anxiolytic and widespread effect on the central nervous system. Answers emotional stress, reduces anxiety, fear, anxiety, offensive to sleep. Ease the symptoms of acute alcohol withdrawal. Provides weak miorelaksirutee (central) and protivosudorozhnoe Actie.dl oxazepamum characterized by a high range of therapeutic action (big difference between an effective dose and the dose causing side effects). The studies tolerance and toxicity oxazepamum different species (mice, rats, dogs), a significant difference in effective doses (anxioliticeski effect), and doses of side effects. Thus, in mice oral oxazepamum effective doses were almost 10 times lower doses of atakshiyu (rotabar-test) and sedatia (lifting spontaneous motor activity). In two studies in rats with a dose 30 times higher than MRDC, found an increase in the frequency of a sound фолликулярноклеточны х neoplastic thyroid, testicular Adenomas ( интерстициальноклето чных) Adenomas and prostate gland. The nine study in rats at doses of admission, in the 35-100 times higher than the daily dose for a person who found dozozawisimoe increase the frequency Adenomas liver. At the same time, there is no evidence that clinical use oxazepamum pose Opouholei.posle intake of slowly absorbed from the digestive tract. C_max achieved through 1-4 hours Linking blood protein, 97%. Equilibrium concentration in the blood is achieved within a few days after the start of the reception. Distributed in tissues. Passes through GEB, placental barrier, enters the breast milk. Treated glukuronirovaniu in the liver, and the active metabolites not. T_1/2 averaged 8.2 p (5.7 - 10.9 p). Report the news is in the form of glukuronidov. When taken repeated doses minimal accumulation.

Indications

Neuroses, Psychopathy, and neurozopodobne psihopatopodobne state, accompanied by fear, anxiety, high hadst, violations of sleep, etc.; сенесто-ипохондричес��ие disorders and navazchivosti (especially in poor Portability other treating); lunch disorders in women of klimaksom, pre syndrome; reactive depression (in a combination therapy with antidepressants), alcohol withdrawal syndrome (in a combination therapy).

Restrictions on the use of

The propensity to abuse of psychotropic drugs.

Pregnancy and lactation

Contraindicated in pregnancy (especially in the first trimester). At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, psychoses expressed infants, severe kidney and / or liver failure, pregnancy (especially I trimester), breast-feeding, age up to six years.

Side-Effects

From the nervous system and sensory organs : clothes (usually in the early days of treatment), weakness, dizziness, increased fatigue, headache, impaired memory, muscle weakness, ataxy, tremor, smazannaya speech paradoxical 127b1 reaction to the mentally ill, including agitation Bespokoistvo.prochie : dry mouth, nausea, diarrhoea phenomenon lakopenia violation of the liver (including jeltukhu), allergic reactions, fear, the change Libido.vozmojna addiction, drug dependency, the syndrome (see "Precautions").

Specific guidance

Recommended for the treatment of anxiety, tension, ajitation, irritability, a weakened patients, people aged patients, as well as patients with residual effects of traumatic or infectious disease Zns.sleduet bear in mind that anxiety or stress in the day-to-day stress, usually do not require treatment anxiolitikami.

Patient interaction

Do effect of oppressive central nervous system, including sleeping, protivosudorozhnykh drugs, alcohol, etc.

Overdosing

Symptoms : oppression CNS varying degrees of symptoms (from itching to coma), drowsiness, sputannosti consciousness, lethargy; In the more serious cases (especially against the backdrop of the admission of the other LAN, oppressive central nervous system, or alcohol), ataxy, gipotenzia, hypnotic state Koma.lechenie : induction vomiting, stomach wash, symptomatic therapy, monitoring vital functions. When expressed hypotension, a norepinephrine. Specific antidote - benzodiazapine antagonist flumazenil receptors (introduction only in the hospital). Haemodialysis weak.

Precautions

The caution used in the predisposition to arterial hypotension, especially in older patients (with regard to the possibility of heart activity), increased risk of drug Zawisimosti.ne should be appointed with MAO inhibitors, fenotiazina derivatives. The likelihood of symptoms increases overdose while receiving funds oppressive central nervous system, or alcohol. During treatment precluded admission alcoholic Napitkov.ne should be used long-term (at the risk of drug addiction). The long-term care insurance (several months) course to be pursued in an intermittent therapy, closing reception for a few days, followed by the appointment of the same individually tailored dose. Lifting should be conducted gradually. In sharp lifting oxazepamum potentially a lifting syndrome (tremor, convulsions, abdominal or muscle cramp, vomiting, perspiration), the most often appears after taking high doses or long Lechenia.pri extended treatment needed to be monitored liver and peripheral images Krovi.ne should apply to drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside (regardless of the meal). Dose and duration of treatment chosen a case-by-case basis, depending on the evidence and therapeutic effect. Initial single dose for adults, 5-10 mg, for outpatient treatment average daily intake of 30-50 mg, in a hospital a maximum dose of 120 mg / sut. Mean duration of the course is 2-4 Ned.doza for children 6-12 years of age are not established.

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