Elzepam - instructions for use, dose, side effects, contraindications

Active substance: bromodihydrochlorophenylbenzodiazepine 1.0 g; auxiliary substances: low molecular weight polyvinylpyrrolidone (molecular weight 12,600 ± 2,700) 9,0 g, glycerol 100,0 g sodium disulfite 2.0 g, polysorbate 80 50.0 g, sodium hydroxide solution 0.1 M up to pH 6.0-7.5, water for injection up to 1 liter.

Description:

Colorless or slightly yellowish liquid.

Pharmacotherapeutic group:Anxiolytic agent (tranquilizer).

ATX: & nbsp

N.05.B.X Other anxiolytics

Pharmacodynamics:

ELZEPAM® is a benzodiazepine derivative.

Pharmacodynamics.Has a pronounced anxiolytic, hypnotic, sedative, as well as anticonvulsant and central muscle relaxant action.

Has a depressing effect on the central nervous system (CNS), which is realized mainly in the thalamus, hypothalamus and limbic system. Enhances the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of nerve impulse transmission in the central nervous system.

The mechanism of action of ELZEPAM® is determined by the stimulation of the benzodiazepine receptors of the supramolecular GABA-benzodiazepine-chloronophore compounding complex, which leads to the activation of the GABA receptor, which causes a decrease in the excitability of the subcortical structures of the brain, inhibition of polysynaptic spinal reflexes.

Pharmacokinetics:

Widely distributed in the body. Metabolised in the liver. Half-life from the body from 6 to 10 - 18 hours, the excretion of the drug is mainly carried out through the kidneys in the form of metabolites.

Indications:

The drug is used for various neurotic, neurotic-like psychopathic, psychopathic and other conditions, accompanied by anxiety, fear,increased irritability, tension, emotional lability. With reactive psychoses, hypochondriacal-sensopathic syndrome (including those resistant to the action of other tranquilizers), vegetative dysfunctions and sleep disorders, for the prevention of states of fear and emotional stress.

As an anticonvulsant drug is used to treat patients with temporal and myoclonic epilepsy.

In neurological practice, they are used to treat hyperkinesis and tics, muscle stiffness, vegetative lability.

Contraindications:

Hypersensitivity (including to other benzodiazepines), coma, shock, myasthenia gravis, zakratougolnaya glaucoma (acute attack or predisposition), severe chronic obstructive pulmonary disease (possibly increased respiratory failure), acute respiratory failure, pregnancy (especially I trimester) , the period of breastfeeding; age under 18 years (safety and efficacy not determined).

Carefully:

hepatic and / or renal failure, cerebral and spinal ataxia, hyperkinesis, a tendency to abuse psychotropic drugs,organic brain diseases (paradoxical reactions are possible), hypoproteinemia, elderly age, depression (see "Special instructions").

Dosing and Administration:

ELZEPAM® is administered intramuscularly or intravenously (either jet or drip).

A single dose is usually 0.0005 to 0.001 g (0.5 to 1 mg), and for sleep disorders, 0.0005 to 0.001 g (0.5 to 1 mg) before bedtime.

For the relief of anxiety, anxiety, psychomotor agitation, as well as in autonomic paroxysms and psychotic conditions, ELZEPAM® is used intramuscularly or intravenously, the initial dose is 0.0005-0. 001 g (0.5-1 ml 0.1% solution), the mean daily dose 0.003 - 0,005 g (3 -5 ml of 0,1% solution), in severe cases to 0,007 - 0,009 g.

With epileptic status and serial epileptic seizures, the drug is administered intramuscularly or intravenously at a dose of 0.0005 g (0.5 mg).

For the treatment of alcohol withdrawal, the drug is administered intramuscularly or intravenously at a dose of 0.0025-0.005 (2.5-5 mg) per day.

In neurological practice for diseases with increased muscle tone, the drug is prescribed intramuscularly at 0.0005 g (0.5 mg) once or twice a day.

For preoperative preparation - intravenously, slowly introduce 0.003 - 0.004 g (3-4 ml of 0.1% solution).

The average daily dose of ELZEPAM® is 0.0015-0.005 g (1.5-5 mg). The maximum daily dose of 0.01 g (10 mg).

After achieving a stable therapeutic effect, it is advisable to switch to taking oral dosage forms of the drug.

In order to avoid the development of drug dependence, in course treatment, the duration of the use of ELZEPAM®, as well as of other benzodiazepines, is 2 of the week. But in some cases, the duration of treatment can be increased to 3-4 weeks.

With the withdrawal of the drug, the dose is reduced gradually.

Side effects:

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, fatigue, dizziness, impaired concentration, ataxia, disorientation, slowing of mental and motor reactions, confusion; rarely - headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially at high doses), mood reduction, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), asthenia, myasthenia gravis, dysarthria; extremely rarely - paradoxical reactions (aggressive outbreaks, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, sleep disturbance).

From the hematopoiesis: leukopenia, neutropenia, agranulocytosis (chills, hyperthermia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.

On the part of the digestive system: dry mouth or salivation, heartburn, nausea, vomiting, decreased appetite, constipation or diarrhea; a violation of liver function, increased activity of "liver" transaminases and alkaline phosphatase, jaundice.

On the part of the genitourinary system: urinary incontinence, urinary retention, impaired renal function, decreased or increased libido, dysmenorrhea.

Allergic reactions: skin rash, itching.

Influence on the fetus: teratogenicity (especially I trimester), CNS depression, respiratory failure and suppression of sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence; lowering of blood pressure (BP); rarely - visual impairment (diplopia), weight loss, tachycardia. With a sharp decrease in dose or discontinuation of reception - the syndrome of "withdrawal" (sleep disturbance, dysphoric reactions, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor,Perceptual disorder, incl. hyperaemia, paresthesia, photophobia, tachycardia, seizures, rarely - psychotic reactions).

Local reactions: phlebitis or venous thrombosis (redness, swelling or pain at the injection site).

Overdose:

With a moderate overdose - increased therapeutic effect and side effects; with a significant overdose - marked depression of consciousness, cardiac and respiratory activity.

Treatment: control of vital body functions, maintenance of respiratory and cardiovascular activity, symptomatic therapy. As antagonists of the muscle relaxant action of ELSEPAM®, strychnine nitrate is recommended (injections of 1 ml of a 0.1% solution 2-3 times a day) or a solution of corazole (injections of 1 ml of a 10% solution 1-2 times a day). As a specific antagonist, flumazenil (anexat) - intravenously (on a 5% solution of glucose (dextrose) or 0.9% sodium chloride solution) at an initial dose of 0.2 mg (if necessary, up to a dose of 1 mg).

Interaction:

ELZEPAM® is compatible with other drugs that cause depression of the CNS function (hypnotics, anticonvulsants, neuroleptics, etc.), however, in case of complex application it is necessary to take into account the mutual enhancement of their function.

Reduces the effectiveness of levodopa in patients with Parkinsonism.

Increase the toxicity of zidovudine.

Inhibitors of microsomal oxidation increase the risk of toxic effects. Inducers of microsomal liver enzymes reduce efficacy.

Increase the concentration of imipramine in the blood serum.

Hypotensive drugs can increase the severity of blood pressure lowering.

Against the background of simultaneous administration of clozapine, an increase in respiratory depression is possible.

Special instructions:

It is necessary to observe special care when appointing ELZEPAM® in severe depression, the drug can be used to implement suicidal intentions. It is necessary to use the drug with caution in elderly and weakened patients. When Q) renal / hepatic insufficiency and long-term treatment requires monitoring of the picture of peripheral blood and "hepatic" enzymes.

The frequency and nature of side effects depend on the individual sensitivity, dose and duration of treatment. With reduced doses or discontinuation of ELSEPAM®, side effects disappear.

Like other benzodiazepines, it has the ability to induce drug dependence in long-term admission in large doses (more than 4 mg / day).

With a sudden discontinuation of reception may be a syndrome of "withdrawal" (depression, irritability, insomnia, increased sweating, etc.), especially with long-term admission (more than 8-12 weeks).

During pregnancy apply only for "vital" indications. Has a toxic effect on the fetus and increases the risk of developing congenital malformations when used in the first trimester of pregnancy. Taking therapeutic doses at a later time of pregnancy can cause depression of the newborn's central nervous system. Continuous use during pregnancy can lead to physical dependence with the development of the "cancellation" syndrome in a newborn.

Children, especially at a young age, are very sensitive to the CNS depressing action of benzodiazepines.

Use immediately before childbirth or during childbirth can cause a respiratory depression in the newborn, a decrease in muscle tone, hypotension, hypothermia, and a weak act of sucking ("sluggish child" syndrome).

The drug enhances the effect of alcohol, so the use of alcohol during the treatment with ELZEPAMom ® is not recommended.

ELZEPAM® is contraindicated during work by drivers of transport and other persons performing work,requiring quick reactions and precise movements.

Form release / dosage:

Solution for injection 30%.

Packaging:5 ampoules of 1 or 2 ml in a contour mesh package made of PVC and foil or without foil, followed by the insertion of 2 outline packages together with the instructions for use and the scarifier in the pack. 10 ampoules together with instructions for use and scarifier in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of up to 20 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001201 / 01

Date of registration:21.05.2008

The owner of the registration certificate:ELLARA, LTD. ELLARA, LTD. Russia

Manufacturer: & nbsp

ELLARA, LTD. Russia

Representation: & nbspMC ELLARA LLC MC ELLARA LLC Russia

Information update date: & nbsp10.12.2015

Illustrated instructions

Instructions

Elzepam® (Elzepam)