Elzepam
Elzepam: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Elzepam
ATX code: N05BX
Active ingredient: bromdihydrochlorophenylbenzodiazepine (bromdihydrochlorphenylbenzodiazepine)
Producer: ELLARA, LLC (Russia)
Description and photo update: 2018-21-11
Prices in pharmacies: from 69 rubles.
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Elzepam is an anxiolytic drug that helps to reduce or suppress fear, anxiety, anxiety, emotional stress.
Release form and composition
Dosage forms of Elzepam:
- tablets: flat-cylindrical, white, with a chamfer (10 pcs. in blister contour packages, in a cardboard box 1, 2, 3 or 5 packages);
- solution for intravenous (intravenous) and intramuscular (intramuscular) administration: clear liquid, slightly yellowish or colorless (1 or 2 ml in ampoules, in a blister strip of 5 ampoules, in a cardboard pack 2 contour packaging with a scarifier; in a cardboard box of 10 ampoules with a scarifier).
Composition for 1 tablet:
- active substance: bromodihydrochlorophenylbenzodiazepine - 0.5 or 1 mg;
- auxiliary ingredients: milk sugar (lactose monohydrate), gelatin, potato starch, calcium stearate.
Composition for 1 ml of solution for intravenous and intramuscular administration:
- active substance: bromodihydrochlorophenylbenzodiazepine - 1 mg;
- auxiliary ingredients: low-molecular-weight medical polyvinylpyrrolidone, sodium disulfite, glycerol, polysorbate-80, decimolar sodium hydroxide solution (solution pH 6.0–7.5), water for injection.
Pharmacological properties
Pharmacodynamics
The active component of Elzepam - bromodihydrochlorophenylbenzodiazepine (trade name - phenazepam), is an anxiolytic agent (tranquilizer) of the benzodiazepine series. It has sedative, hypnotic, anxiolytic, anticonvulsant and central muscle relaxant efficacy. It potentiates the inhibitory effect of GABA (gamma-aminobutyric acid) on synaptic transmission, stimulates the binding sites with benzodiazepines located in the allosteric center of postsynaptic GABA receptors, reduces the excitability of the subcortical structures of the brain (limbic system, thalamus, hypothalamus), inhibits polysynaptic spins.
Pharmacodynamic efficacy of phenazepam:
- anxiolytic: due to the influence on the amygdala of the limbic system, emotional stress decreases, anxiety, anxiety, fear are weakened;
- sedative: due to the effect of the substance on the reticular formation of the brain stem and nonspecific (relay) nuclei of the thalamus, expressed by suppression of symptoms of neurotic origin (fear, anxiety);
- hypnotic: it is associated with the suppression of cells of the reticular formation of the brain stem, reduces the effect of autonomic, emotional and motor stimuli that upset the mechanism of falling asleep;
- anticonvulsant: it is carried out by increasing presynaptic inhibition, reduces the spread of a convulsive impulse, but does not contribute to the removal of the excited state of the focus;
- central muscle relaxant: due to inhibition of polysynaptic (at least monosynaptic) spinal afferent pathways with possible direct inhibition of motor nerves and muscle contractility.
Pharmacokinetics
When administered orally, Elzepam is well absorbed from the gastrointestinal tract (gastrointestinal tract), C max (time to reach the maximum concentration) of bromodihydrochlorophenylbenzodiazepine in plasma - 1-2 hours.
When administered parenterally, bromodihydrochlorophenylbenzodiazepine is widely distributed in the body.
Elzepam is metabolized mainly in the liver. The half-life (T 1/2) of all forms of the drug is from 6 to 10-18 hours. Elimination occurs mainly through the kidneys with urine in the form of metabolites.
Indications for use
- neurotic and neurosis-like disorders, accompanied by fear, anxiety, emotional lability / tension, increased irritability, autonomic dysfunction;
- hypochondriac-senestopathic syndrome (syndromum hypochondriacum senesthopathicum), including with resistance to the action of other tranquilizers;
- sleep disturbance (difficulty falling asleep, insufficiency, discontinuity, etc.);
- temporal and myoclonic epilepsy (as adjuvant therapy as an anticonvulsant);
- increased muscle tone, hyperkinesis and rigidity due to damage to the central nervous system (CNS).
Elzepam tablets are recommended to be included in the complex treatment of alcohol withdrawal syndrome.
The solution is also used to prevent states of emotional stress, fear and for the treatment of reactive psychoses.
Contraindications
Absolute contraindications for all forms of Elzepam release:
- myasthenia gravis, angle-closure glaucoma (predisposition / acute attack), shock, coma;
- ONE (acute respiratory failure);
- COPD (chronic obstructive pulmonary disease) in severe course with a possible increase in respiratory failure;
- the period of pregnancy (for the solution - especially the first trimester) and breastfeeding;
- children and adolescents up to 18 years old;
- increased individual sensitivity to benzodiazepines, phenazepam and auxiliary components of the drug.
Additional absolute contraindications for Elzepam tablets:
- severe (deep) depression (due to the possibility of manifestation of suicidal tendencies);
- acute alcohol poisoning up to the weakening of vital functions, overdose of hypnotics and narcotic analgesics;
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
According to the instructions, Elzepam is prescribed with caution to patients with hepatic and / or renal insufficiency, cerebral and spinal ataxia, a history of drug dependence, a tendency to abuse psychoactive substances, organic brain diseases, hyperkinesis, psychoses (due to possible paradoxical reactions), hypoproteinemia and elderly patients. Additionally: for tablets - sleep apnea (established / estimated); for the solution - hyperkinesis, depression.
Instructions for the use of Elzepam: method and dosage
The duration of the course of treatment with Elzepam, like other benzodiazepines, in order to avoid the formation of drug dependence, is two weeks. In some cases, as prescribed by the attending physician, it is allowed to increase: with parenteral administration - up to 3-4 weeks, with oral administration - up to 8-9 weeks.
A single dose of bromodihydrochlorophenylbenzodiazepine is usually 0.5–1 mg.
Cancellation of the drug is carried out by gradually decreasing the dose.
Pills
Elzepam tablets are intended for oral administration.
Recommended dosage according to indications:
- sleep disorders: 0.5 mg 20-30 minutes before the expected time of falling asleep;
- neurotic, neurosis-like disorders, hypochondriac-senestopathic syndrome: 0.5-1 mg 2 or 3 times a day; after 2–4 days, the dose may be increased to 4–6 mg per day, taking into account the tolerability and effectiveness of the drug; morning and afternoon intake - 0.5-1 mg, dose at night - 2.5 mg;
- severe anxiety: the initial dose is 3 mg per day, then the dose is rapidly increased until the required therapeutic effect is obtained;
- alcohol withdrawal syndrome (as part of complex therapy): 2.5–6 mg per day;
- temporal lobe and myoclonic epilepsy (as an adjuvant): 2-10 mg per day;
- increased muscle tone, hyperkinesis and rigidity in case of CNS damage: 2-3 mg 1 or 2 times a day; the maximum daily dose is 10 mg.
Solution
Elzepam solution is injected intramuscularly or intravenously (jet / drip).
Recommended dosage according to indications:
- sleep disorders: 0.5–1 mg once a day before bedtime;
- relief of anxiety, fear, psychomotor agitation, vegetative paroxysms and psychotic states: initial dose of 0.5-1 mg, average daily dose - 3-5 mg, in severe cases - up to 7-9 mg; the solution is injected i / m or i / v;
- status epilepticus and serial epileptic seizures: initial dose - 0.5 mg; the solution is injected i / m or i / v;
- alcohol withdrawal: 2.5–5 mg per day; the solution is injected i / m or i / v;
- increased muscle tone, hyperkinesis and rigidity in case of CNS damage: 0.5 mg 1-2 times a day; the solution is injected / m;
- preoperative preparation: 3-4 mg; the solution is injected intravenously slowly.
The average daily dose of Elzepam solution is 1.5–5 mg, the maximum daily dose is 10 mg.
Upon reaching a stable therapeutic effect, it is advisable to switch to oral dosage forms of the drug.
Side effects
The frequency and nature of the side effects of Elzepam depend on its dose, the duration of therapy and the individual sensitivity of the patient. After reducing doses or stopping the drug, side effects go away on their own.
Possible side effects:
- CNS: at the beginning of therapy (more often observed in elderly patients) - a feeling of fatigue, drowsiness, dizziness, ataxia, impaired concentration, disorientation, confusion, slowing of mental / motor reactions; rarely - depression, headache, euphoria, tremor, impaired coordination of movements (use of high doses), memory loss, dystonic extrapyramidal reactions (uncontrollable movements, including the eyes), decreased mood, myasthenia gravis, asthenia, dysarthria; additionally for tablets - convulsions in patients with epilepsy; very rarely - paradoxical reactions (psychomotor agitation, outbursts of aggression, muscle spasm, fear, suicidal tendencies, anxiety, hallucinations, sleep disturbances);
- hematopoietic organs: anemia, neutropenia, leukopenia, agranulocytosis (hyperthermia, chills, sore throat, unusual fatigue / weakness), thrombocytopenia;
- digestive system: dry mouth, drooling, nausea, vomiting, heartburn, decreased appetite, constipation / diarrhea, hepatic dysfunction, increased liver enzyme activity, jaundice;
- cardiovascular system: lowering blood pressure, tachycardia;
- genitourinary system: urinary retention, urinary incontinence, impaired renal function, dysmenorrhea, decreased / increased libido;
- hypersensitivity reactions: skin rash, itching;
- effect on the fetus: teratogenicity (especially in the first trimester), respiratory failure, depression of the central nervous system, suppression of the sucking reflex in newborns whose mothers received Elzepam;
- other reactions: addiction, drug dependence syndrome; rarely - diplopia, weight loss; in the event of a sharp dose reduction or discontinuation of therapy - withdrawal syndrome, expressed by sleep disturbance, dysphoria, spasm of smooth muscles (skeletal muscles and internal organs), depersonalization, increased sweating, depression, nausea, vomiting, tremors, perceptual disorders, incl. hyperacusis, paresthesia, photophobia, tachycardia, convulsions, in rare cases - psychotic reactions);
- local reactions (for solution): venous thrombosis or phlebitis (swelling, redness, or pain at the injection site).
Overdose
Symptoms of moderate overdose are increased therapeutic efficacy and dose-dependent side effects. As a result of a significant overdose, a pronounced depression of cardiac, respiratory activity and consciousness is possible.
In case of an overdose of tablets, first of all, measures are taken to remove the unabsorbed drug from the body - gastric lavage and intake of activated carbon. In parallel, it is necessary to control the vital functions of the body, maintain cardiovascular, respiratory activity and conduct symptomatic therapy.
Hemodialysis for the elimination of phenazepam is ineffective. As a specific antagonist, IV flumazenil can be used in 5% dextrose solution or 0.9% NaCl solution at an initial dose of 0.2 mg, maximum up to 1 mg.
In case of an overdose of the solution as antagonists of the muscle relaxant action of phenazepam, it is recommended to use parenteral strychnine nitrate 0.1% solution of 1 ml 2-3 times a day or a solution of corazole 10% 1 ml 1-2 times a day.
special instructions
Patients with renal / hepatic insufficiency, as well as with prolonged therapy with Elzepam, require monitoring of the peripheral blood picture and the level of hepatic enzymes.
Like other benzodiazepines, phenazepam can cause drug dependence, especially when taken for a long time (more than two weeks) in high doses (more than 4 mg per day).
Sudden discontinuation of treatment, especially after prolonged use (> 8-12 weeks), can cause withdrawal symptoms such as depression, insomnia, increased sweating, irritability, etc.
Bromodihydrochlorophenylbenzodiazepine enhances the effect of alcohol, therefore, the use of alcoholic beverages during the treatment period is contraindicated.
Prescribing Elzepam for severe depression requires special care, since patients can use it to implement suicidal intentions.
The drug is used with caution in debilitated patients and elderly patients.
Influence on the ability to drive vehicles and complex mechanisms
Patients taking Elzepam should refuse to drive vehicles and engage in potentially hazardous activities during treatment.
Application during pregnancy and lactation
Elzepam tablets are not prescribed for pregnant and lactating women.
The solution is contraindicated for use in the first trimester of pregnancy and during breastfeeding. Parenteral use of phenazepam in the II and III trimesters is allowed only for vital indications.
Bromodihydrochlorophenylbenzodiazepine has a toxic effect on the fetus, increasing the risk of developing congenital defects, especially in the first trimester. Taking therapeutic doses of a substance at a later stage of pregnancy can cause central nervous system depression in a newborn. With regular use of Elzepam by a woman during pregnancy, the fetus may develop physical dependence, and the newborn may develop withdrawal syndrome.
Children, especially young children, are highly sensitive to the inhibitory effect of benzodiazepines on the central nervous system. The use of Elzepam before childbirth or directly in delivery can cause a sluggish child syndrome, manifested by respiratory depression, decreased muscle tone, hypotension, hypothermia, and a weak sucking act in a newborn.
Pediatric use
In pediatric practice, due to the lack of data on the safety and effectiveness of therapy with Elzepam, its use in children and adolescents under 18 years of age is contraindicated.
With impaired renal function
Elzepam is prescribed with caution to patients with renal insufficiency.
For violations of liver function
Elzepam is prescribed with caution to patients with hepatic impairment.
Use in the elderly
Elzepam in the form of a solution should be prescribed with caution to elderly patients.
Drug interactions
- hypnotics, antipsychotics, anticonvulsants and other drugs that suppress the function of the central nervous system: bromodihydrochlorophenylbenzodiazepine is compatible with them, but it is necessary to take into account the mutual potentiation of their effects;
- inhibitors of liver microsomal enzymes: increase the risk of toxicity and reduce efficacy;
- inducers of microsomal liver enzymes: reduce the effectiveness of Elzepam;
- imipramine: its serum concentration increases;
- antihypertensive drugs: it is possible to increase the severity of lowering blood pressure;
- clozapine: the likelihood of increased respiratory depression;
- levodopa: Elzepam reduces its effectiveness in parkinsonism;
- zidovudine: its toxicity may increase.
Analogs
Elzepam analogues are: Tranquezipam, Fenazepam, Fezanef, Fensitat, Fenorelaxan, etc.
Terms and conditions of storage
Store in a dry place protected from light and out of reach of children. Storage temperature: tablets - up to 25 ° С, solution - up to 20 ° С.
Shelf life: tablets - 3 years, solution - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Elzepam
Mostly reviews about Elzepam are positive. Patients report good efficacy of both forms of the drug in the treatment of sleep disorders, anxiety disorders, panic attacks and other conditions that impair quality of life.
But one should not forget that the course of therapy should be short-lived, since addiction to Elzepam is likely to develop, which, upon completion of the course, can cause a withdrawal syndrome.
Price for Elzepam in pharmacies
Estimated price of Elzepam: solution for intravenous and intramuscular administration of 0.1%, 1 ml in an ampoule, for 10 ampoules - 95–130 rubles; tablets 0.5 mg, 50 pcs. in the package - 60 rubles, tablets 1 mg, for 50 pcs. in the package - 70 rubles.
Elzepam: prices in online pharmacies
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Drug name Price Pharmacy |
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Elzepam 1 mg / ml solution for intravenous and intramuscular administration 1 ml 10 pcs. RUB 69 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
