Phenazepamum

General characteristics. Structure:

Aktivone substance: бромдигидрохлорфенилбензодиазепин (Phenazepamum) of 1 mg; 500 mkg; 2,5 mg

Excipients: lactose (sugar milk), potato starch, povidone (коллидон 25), calcium stearate, talc.

Pharmacological properties:

Anxiolytic (tranquilizer), derivative benzodiazepine. Possesses the expressed anxiolytic, somnolent, sedative, and also anticonvulsant and central myorelaxation action.
Has the oppressing effect on TsNS which is implemented preferential in a thalamus, a hypothalamus and limbic system. Strengthens an inhibiting effect gamma аминобутировой acids (GABA) which is one of the main mediators pre-and postsynaptic braking of transfer of nervous impulses in TsNS.
The mechanism of action of Phenazepamum is defined by stimulation of benzodiazepine receptors supramolecular GABA-бензодиазепин-хлорионофор-рецепторного a complex, leading to activation of GABA receptors that, in turn, causes decrease in excitability of subcrustal structures of a brain and braking of polisinaptichesky spinal reflexes.

Pharmacokinetics. Absorption. At intake drug is well soaked up from a GIT. In blood there is from 1 to 2 h Cmax of Phenazepamum.

Metabolism. It is metabolized in a liver.

Removal. T1/2 makes from 6 to 18 h. Drug, generally with urine is removed.

Indications to use:

— the neurotic, neurosis-like, psychopathic, psychopatholike and other states which are followed by alarm, fear, an acrimony, tension, emotional lability;
— reactive psychoses;
— a hypochiondrial and senestopathetic syndrome (including resistant to action of other tranquilizers);
— vegetative dysfunctions;
— frustration of a dream;
— prevention of conditions of fear and emotional pressure;
— temporal and myoclonic epilepsy;
— hyperkinesias and tics;
— muscle tension;
— vegetative lability.

Route of administration and doses:

Drug should be accepted inside. The single dose of Phenazepamum usually makes 0.5-1 mg.
The average daily dose of Phenazepamum makes 1.5 - 5 mg, it is divided into 2-3 receptions: usually on 0.5-1 mg in the morning and in the afternoon, for the night - to 2.5 mg. The maximum daily dose of Phenazepamum makes 10 mg.
At sleep disorders it is necessary to use drug in a dose 0.25-0.5 mg in 20 - 30 min. prior to a dream.
At neurotic, psychopathic, neurosis-like and psychopatholike states the initial dose of drug makes 0.5-1 mg 2-3 In 2-4 days taking into account efficiency and portability of drug the dose can бьпь is increased to 4-6 mg /
At the expressed agitation, fear, alarm treatment begin with a dose 3 mg/, quickly increasing a dose before obtaining therapeutic effect.
At epilepsy the dose makes 2-10 mg /
At alcoholic abstinence Phenazepamum appoint in a dose 2.5-5 mg /
At diseases with повышенньм a muscle tone drug appoint 1-2 on 2-3 mg
In order to avoid development of medicinal dependence at course treatment duration of use of Phenazepamum makes 2 weeks. In some cases duration of treatment can be increased up to 2 months. At cancellation of npenapata the dose is reduced gradually.

Features of use:

Respect for extra care at purpose of Phenazepamum at heavy depressions as drug can be used for implementation of suicide intentions is required.

It is necessary to use with care drug at the elderly and weakened patients.

At a renal/liver failure and prolonged treatment control of a picture of peripheral blood and indicators of liver enzymes is necessary.

Frequency and the nature of side effect depend on individual sensitivity, a dose and duration of treatment. At reduction of doses or phase-out of Phenazepamum side effects disappear.

Like other benzodiazepines, Phenazepamum has ability to cause medicinal dependence at long reception in high doses (> 4 mg/).

At sudden phase-out of drug the withdrawal (can be noted especially at drug use more than 8-12 weeks).

Phenazepamum strengthens effect of alcohol therefore the use of alcoholic drinks during treatment by drug is not recommended.

Use in pediatrics
Children, especially younger age, are very sensitive to the oppressing TsNS to effect of benzodiazepines.

Influence on ability to driving of motor transport and to control of mechanisms
Phenazepamum is contraindicated to use to the drivers of transport and other persons performing the work demanding bystry and exact reactions.

Side effects:

From TsNS and peripheral nervous system: in an initiation of treatment (especially at elderly patients) - drowsiness, feeling of fatigue, dizziness, disturbance of concentration of attention, an ataxy, a disorientation, delay of mental and motor reactions, confusion of consciousness; seldom - a headache, euphoria, a depression, a tremor, decrease in memory, a lack of coordination of movements (especially at use in high doses), decrease in mood, dystonic extrapyramidal reactions, an adynamy, a myasthenia, a dysarthtia; very seldom - paradoxical reactions (aggressive flashes, psychomotor excitement, fear, suicide bent, a muscular spasm, hallucinations, alarm, a sleep disorder).

From system of a hemopoiesis: leukopenia, neutropenia, agranulocytosis, anemia, thrombocytopenia.

From the alimentary system: dryness in a mouth or hypersalivation, heartburn, nausea, vomiting, a loss of appetite, a lock or diarrhea, an abnormal liver function, increase in activity of hepatic transaminases and ShchF, jaundice.

From reproductive system: decrease or increase in a libido, dysmenorrhea; influence on a fruit - teratogenecity (especially the I trimester), oppression of TsNS, breath disturbance, suppression of a sucking reflex at newborns.

Allergic reactions: skin rash, itch.

Others: accustoming, medicinal dependence, decrease in the ABP; seldom - a vision disorder (diplopia), decrease in body weight, tachycardia; at a sharp dose decline or phase-out - a withdrawal.

Interaction with other medicines:

At simultaneous use of Phenazepamum with other drugs causing TsNS function oppression (including somnolent, anticonvulsant, antipsychotic), it is necessary to consider mutual strengthening of their action.
At simultaneous use of Phenazepamum with a levodopa at patients with parkinsonism efficiency of use of the last decreases.
At simultaneous use of Phenazepamum with a zidovudine toxicity of the last can increase.
At simultaneous use of Phenazepamum with inhibitors of a microsomal oxidation the risk of development of toxic effects of Phenazepamum increases.
At simultaneous use of Phenazepamum with inductors of microsomal enzymes of a liver efficiency of use of Phenazepamum decreases.
At simultaneous use of Phenazepamum with Imipraminum concentration of the last in blood serum increases.
At simultaneous use of Phenazepamum with antihypertensives strengthening of expressiveness of anti-hypertensive action is possible.
At simultaneous use of Phenazepamum with clozapine strengthening of respiratory depression is possible.

Contraindications:

— coma;
— shock;
— myasthenia;
— closed-angle glaucoma (bad attack or predisposition);
— heavy HOBL (strengthening of respiratory insufficiency is possible);
— acute respiratory insufficiency;
— pregnancy (especially I trimester);
— breastfeeding period;
— children's and teenage age up to 18 years (safety and efficiency are not defined);
— hypersensitivity to benzodiazepines.

With care it is necessary to use drug at a liver and/or renal failure, a cerebral and spinal ataxy, a hyperkinesia, tendency to abuse of psychotropic drugs, organic diseases of a brain (paradoxical reactions are possible), hypoproteinemias, depressions, at patients of advanced age.

Use of the drug FENAZEPAM® at pregnancy and feeding by a breast
At pregnancy Phenazepamum is applied only according to vital indications. Drug has toxic effect on a fruit and increases risk of development of inborn defects at use in the I trimester of pregnancy. Use of therapeutic doses in later durations of gestation can cause oppression of TsNS of the newborn. Constant use of Phenazepamum at pregnancy can cause a withdrawal in the newborn.

Use of drug just before childbirth or at the time of delivery can cause in the newborn respiratory depression, decrease in a muscle tone, hypotonia, a hypothermia, weakening of the act of suction (a syndrome of "the sluggish child").

Use at abnormal liver functions
With care it is necessary to use drug at a liver failure.

Use at renal failures
With care it is necessary to use drug at a renal failure.

Use for elderly patients
It is necessary to use with care drug at the elderly and weakened patients.

Use for children
Contraindication: children's and teenage age up to 18 years (safety and efficiency are not defined).

Overdose:

Symptoms: at moderate overdose - strengthening of therapeutic action and side effects; at considerable overdose - the expressed oppression of consciousness, cordial and respiratory activity.

Treatment: control of the vital functions of an organism, maintenance of respiratory and cardiovascular activity, symptomatic therapy. As antagonists of myorelaxation action of Phenazepamum nitrate is recommended strychnine (an injection on 1 ml of 0.1% of solution 2-3). As the specific antagonist it can be used flumazenit (анексат): in/in 0.2 mg (if necessary the dose can be raised to 1 mg) for 5% solution of glucose (dextrose) or 0.9% sodium chloride solution.

Storage conditions:

List B. Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (5) - packs cardboard.
25 pieces - planimetric strip packagings (2) - packs cardboard.
50 pieces - banks polymeric (1) - packs cardboard.