Flunitrazepam

Chemical name

5-(2-Фторфенил)-1,3-дигид��о-1-метил-7-нитро-2H-1,4-б��нздиазепин-2-он

Gross

C16-H12-F-N3-O3

Characteristics

Red means of a group of benzodiazepine derivatives.

Of drugs

Drugs, the pills. Benzodiazepinove stimulates receptors and increases sensitivity to Gamk-retseptorov mediatoru increases braking influence GABA in the CNS. Decreases anxiety subcortical structures of the brain, slowing polisinapticalkie spinale though. Hypnotic effect develops rapidly and lasts from 6 to 8 pm Has also sedative, anxiolytic, miorelaksirutee (central) and protivosudorozhnoe effect. Decreases psihomotornuyu activity and emotional stress reduces anxiety, fear, anxiety, it Amneziu.posle intake of the dose of 1 mg C_max through the 0.75-2 h is 6-11 ng / J Bioavailability - 70-90%. Away reduces speed and the degree of suction. Linking blood protein is 78%. Daily admission by moderate cumulation plasma. When multiple admission equilibrium concentration flunitrazepama plasma achieved in 5 days, and the dose of 2 mg at least 3-4 ng / J Equilibrium concentration of the pharmacologically active N-demetil-metabolita almost identical to one substance. The plasma-klirens 120-140 ml / min. The distribution in the equilibrium state is 3-5 l / kg Quickly penetrates into spinnomozgovu liquid. Slowly passes through the placental barrier, enters the breast milk. Metabolised in the liver (10-15% with a "first pass"). The major metabolites in plasma were 7-aminoflunitrazepam N-desmetilflunitrazepam and, in the urine-7-aminoflunitrazepam. Report the news is mostly in the form of metabolites and faeces. T_1/2 flunitrazepama is 16-35 hrs, T_1/2 N-деметилфлунитразепа ма - 28 am

Indications

Insomnia, premedikation, the introduction of anaesthesia, the maintenance of narcosis.

Pregnancy and lactation

Contraindicated in pregnancy (especially in the first trimester). If necessary, use in the last trimester of pregnancy or during the first year of birth, it should be borne in mind that the babies may develop hypotonia, hypothermia and respiratory depression. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, gipercapnia, severe respiratory distress, the syndrome patients in a dream, severe kidney and / or liver failure, male, acute ethanol poisoning, pills, painkillers, or antipsychotic antidepressivei means lithium; Drug addiction, chronic alcoholism in history, pregnancy (especially I trimester), breast-feeding.

Side-Effects

From the nervous system and sensory organs : headache, dizziness, increased fatigue, weakness, the concentration, sputannosti consciousness slow physical and mental reactions, muscle weakness, parestesia, anterogradnaya amnesia (can be accompanied by strange behavior), disorientation and awakening, paradoxical reaction (anxiety, hallucinations, causing irritability, aggressiveness, crazy, deep anger, nightmares, depression), insomnia, drowsiness during the day, a latent depression, fatigue, ataxy, diplopia, epileptic seizures, the phenomenon Posleactia.prochie : lakopenia, agranulozitos, difficulty in breathing, gipotenzia, diarrhoea phenomenon, skin rashes, swelling angioneuroticeski whose influence, changing Libido.vozmojna addiction, drug dependency, the syndrome and "impact" (see "Precautions").

Patient interaction

Do deprimirotee antipsihoticeskih the funds, other sexually PP, anxiety, antidepressants, narcotic analgesics, protivosudorozhnykh of anaesthetics, some antigistaminnah drugs. Ethanol, inhibitors mikrosomalnogo increased oxidation effects (including off). If you are receiving drug analgetikami may increase euphoria and psychological dependence.

Overdosing

Symptoms : drowsiness, sputannosti consciousness, weakness, ataxy, muscle hypotension, arterial gipotenzia, respiratory depression, coma, possible death Ishod.lechenie : induction vomiting, stomach wash, reception activated carbon, the road respiratory tract jiznennovazhnykh monitoring functions, a specific antagonist benzodiazapine receptors flumazenila (in the hospital).

Precautions

Treatment of insomnia start with the smallest recommended dose and continue as soon Koroche.vo time, and after the application flunitrazepama should be careful when driving, as well as in the performance of work requiring higher concentration and accurate coordination Dwijeni.sleduet bear in mind that, after applying the product in the next few weeks may decrease its effectiveness. Risk of Drug Dependence increases with the increase of dose and duration of treatment, as well as in patients with ill information about alcohol or drugs. In developing physical dependence sudden removal of the drug accompanied by symptoms (headache, muscle pain, anxiety, stress, anxiety, sputannosti consciousness, irritability, depersonalization, giperakuzia, numbness and pricking in the extremities, increased sensitivity to light, noise, the physical contact, hallucinations, epileptic seizures). Following the lifting of drug development may impact syndrome, which is characterized by a temporary increase in symptoms, which led to the appointment of the drug (insomnia, mood changes, anxiety, anxiety). The temporary increase symptoms after drug should warn the patient. The paradoxical reactions requires the preparation. When planning pregnancy or suspected its existence w bce2 ould have to consult with the doctor on the receiving medication.

Dosing and Administration

Inside, 1-2 mg for 20 minutes before sleep. Older weakened and sick, 0.5-1.0 mg. The course of treatment for 2-5 days to 2-3 weeks (no more than four weeks, including the phasing out). Dropped in dose 0,015-0,03 mg / kg Then for the 60 minutes before the start of narcosis in / m to give anaesthesia-in / in slowly at the speed of 2 mg / min.

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