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

Anxiolytic agent (tranquilizer) of benzodiazepine series. Has anxiolytic, sedative, hypnotic, anticonvulsant and central muscle relaxant effect. Increases the inhibitory effect of gamma-aminobutyric acid on the transmission of nerve impulses. Stimulates binding sites with benzodiazepines located in the allosteric center of the postsynaptic gamma-aminobutyric acid receptors; reduces the excitability of subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spinal reflexes.

Anxiolytic action is due to the influence on the amygdala of the limbic system and is manifested in a decrease in emotional tension, easing anxiety, fear, anxiety.

The sedative effect is due to the influence on the reticular formation of the brainstem and the nonspecific nuclei of the thalamus and is manifested by a decrease in the symptomatology of neurotic origin (anxiety, fear).

Sleeping effect is associated with depression of the cells of the reticular formation of the brain stem.Reduces the impact of emotional, vegetative and motor stimuli, which break the mechanism of falling asleep.

Anticonvulsant action is realized by strengthening presynaptic inhibition, the drug suppresses the spread of convulsive impulse, but does not relieve the excited state of the focus.

Central miorelaksiruyuschee effect due to inhibition of the polysynaptic spinal afferent inhibitory pathways (less monosynaptic).

Perhaps direct inhibition of motor nerves and muscle contractility.

Pharmacokinetics:

When ingested, the drug is well absorbed from the gastrointestinal tract, the time to reach the maximum concentration of bromodihydrochlorophenylbenzodiazepine in the blood from 1 to 2 hours Metabolized in the liver, the half-life is 6 to 18 hours. It is excreted mainly by the kidneys in the form of metabolites.

Indications:

Neurotic, neurosis-like disorders, accompanied by anxiety, fear, increased irritability, emotional lability and tension, autonomic disorders, hypochondriacal-senesthetic syndrome (including resistant to other tranquilizers).

Sleep disorders.

As part of a comprehensive therapy of alcohol withdrawal syndrome.

As an auxiliary for the treatment of patients with temporal and myoclonic epilepsy.

Treatment of increased muscle tone, hyperkinesia and rigidity in the defeat of the central nervous system.

Contraindications:Hypersensitivity to the components of the drug, as well as to other benzodiazepine derivatives; coma, shock, myasthenia gravis, closed angle glaucoma (acute attack or predisposition), acute alcohol poisoning (with impaired vital functions), narcotic analgesics and hypnotics, severe chronic obstructive pulmonary disease (possibly increased respiratory failure), acute respiratory failure, severe depression (suicidal tendencies may appear); age under 18 years (safety and efficacy not established), lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:

Hepatic and / or renal insufficiency, cerebral and spinal ataxia, drug dependence in history, propensity to abuse psychoactive drugs, hyperkinesis,organic brain diseases, psychosis, paradoxical reactions are possible), hypoproteinemia, nocturnal apnea (established or presumed), elderly age.

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

Inside.

A single dose is usually 0.5-1 mg, with sleep disorders - 0.5 mg for 20-30 minutes before sleep.

With neurotic, neurosis-like disorders, hypochondriacelo-sensopathic syndrome, 0.5-1 mg 2-3 times a day. After 2-4 days, taking into account the effectiveness and tolerability of the drug, the dose can be increased to 4-6 mg / day, morning and daytime doses are 0.5-1 mg, at night 2.5 mg.

If anxiety is expressed, treatment starts with a dose of 3 mg / day, rapidly increasing the dose to obtain a therapeutic effect.

In the complex therapy of alcohol withdrawal symptoms are prescribed in a dose of 2.5-6 mg per day.

As an auxiliary for the treatment of patients with temporal and myoclonic epilepsy, the dose is 2-10 mg / day.

With increased muscle tone, hyperkinesia and rigidity in the CNS lesion, the drug is prescribed 2-3 mg once or twice a day.

The maximum daily dose is 10 mg.

To avoid the development of drug dependence, with course treatment, the duration of the drug, as well as other benzodiazepines, is 2 weeks. In some cases, the duration of treatment can be increased to 2 months.

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; headache, euphoria, depression, tremor, memory loss, movement coordination disorders (especially high doses), mood reduction, dystonic extrapyramidal reactions (uncontrolled movements, including the eye), asthenia, myasthenia gravis, dysarthria, convulsions ( in patients with epilepsy); paradoxical reactions (outbreaks of aggression, psychomotor agitation, fear, suicidal tendencies, muscle spasm, hallucinations, anxiety, sleep disturbance).

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

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

From 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 in the first trimester), depression of the central nervous system, respiratory failure and suppression of the sucking reflex in newborns whose mothers used the drug.

Other: addiction, drug dependence; lowering blood pressure; impaired vision (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, perception disorders, including hyperacuscus , paresthesia, photophobia, tachycardia, seizures, psychotic reactions).

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

Overdose:

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

Treatment: gastric lavage, reception of activated charcoal, control of vital body functions, maintenance of respiratory and cardiovascular activity, symptomatic therapy. Hemodialysis is ineffective. As a specific antagonist can be used flumazenil - intravenously (on a 5% solution of dextrose or 0.9% solution of sodium chloride) at an initial dose of 0.2 mg (if necessary, up to a dose of 1 mg).

Interaction:

Compatible with other drugs that cause depression of the central nervous system (hypnotics, anticonvulsants, neuroleptics, etc.), however, in complex application it is necessary to take into account the mutual enhancement of their action.

Reduces the effectiveness of levodopa.

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

Increases the concentration of imipramine in the blood serum.

Hypotensive drugs can increase the severity of lowering blood pressure. Simultaneous use with clozapine may cause respiratory depression.

Special instructions:

With renal / hepatic insufficiency and long-term treatment, control over the picture of peripheral blood and "hepatic" enzymes is necessary.

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

Like other benzodiazepines, it has the ability to induce drug dependence when taken for more than 2 weeks.

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

The drug enhances the effect of alcohol, so the use of alcoholic beverages during treatment with the drug is contraindicated.

Effect on the ability to drive transp. cf. and fur:

When taking the drug is prohibited to drive vehicles and engage in other activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets 0.5 mg or tablets 1.0 mg.

Packaging:

10 tablets per contour cell pack.

1 contour mesh package with instructions for use in a pack of cardboard.
2 contour mesh packages with instructions for use in a pack of cardboard.

5 contour mesh packages with instructions for use in a pack of cardboard.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 of the year. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000853

Date of registration:14.10.2011

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

Manufacturer: & nbsp

GosMPS, FSUE Russia

PRANAFARM, LLC Russia

Information update date: & nbsp09.12.2015

Illustrated instructions

Instructions

Elzepam® (Elzepam)