Relanium - instructions for use, reviews, analogues and forms of release (injections in ampoules for injections in solution, tablets) for the treatment of epilepsy and seizures in adults, children and pregnancy

In this article, you can read the instructions for using the drug Relanium. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Relanium in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Relanium with available structural analogues. Use for the treatment of epilepsy and seizures in adults, children, as well as during pregnancy and lactation.

Relanium - anxiolytic drug (tranquilizer), benzodiazepine derivative.

Diazepam (the active substance of the drug Relanium) has a depressing effect on the central nervous system, 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. It has anxiolytic, sedative, hypnotic, miorelaxing and anticonvulsant action.

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

Composition

Diazepam + excipients.

Pharmacokinetics

After intramuscular administration, Relanium is absorbed slowly and unevenly, depending on the site of administration; when introduced into the deltoid muscle, absorption is rapid and complete. Bioavailability is 90%. Binding to plasma proteins is 98%.Diazepam and its metabolites penetrate the blood-brain barrier (BBB) ​​and the placental barrier, excreted in breast milk in concentrations corresponding to 1/10 concentration in blood plasma. With repeated use of the drug, a pronounced cumulation of diazepam and its active metabolites is observed. It is metabolized in the liver with the participation isozymes CYP2C19, CYP3A4, CYP3A5 and CYP3A7 98-99% to form a very active metabolite desmetildiazepama and less active - oxazepam and temazepam. It is excreted by the kidneys - 70% (in the form of glucuronides), unchanged - 1-2%, and less than 10% - with feces. After discontinuation of treatment, metabolites persist in the blood for several days or even weeks.

Indications

• treatment of neurotic and neurosis-like disorders with anxiety;
• suppression of psychomotor agitation associated with anxiety;
• suppression of epileptic seizures and convulsive conditions of various etiologies;
• states, accompanied by increased muscle tone (including tetanus, acute disorders of cerebral circulation);
• relief of withdrawal syndrome and delirium in alcoholism;
• for premedication and ataralgesia in combination with analgesics andother neurotropic drugs with various diagnostic procedures, in surgical and obstetrical practice;
• in the clinic of internal diseases: in complex therapy of arterial hypertension (accompanied by anxiety, increased excitability), hypertensive crisis, vasospasms, climacteric and menstrual disorders.

Forms of release

Solution for intravenous and intramuscular injection (injections in ampoules for injection).

Other dosage forms, be it powder or tablets, do not exist.

Instructions for use and dosage

With the aim of arresting the psychomotor agitation associated with anxiety, prescribe 5-10 mg slowly, intravenously, if necessary, 3-4 hours later, the drug is administered again in the same dose.

When tetanus is prescribed for 10 mg intravenously slowly or deeply intramuscularly, then intravenously drip 100 mg of diazepam in 500 ml of a 0.9% solution of sodium chloride or 5% glucose solution at a rate of 5-15 mg / h.

With epileptic status, I / m or IV is prescribed for 10-20 mg, if necessary, 3-4 hours later, the drug is given again in the same dose.

For the removal of spasm of skeletal muscles - 10 mg IM for 1-2 hours before the operation.

In midwifery appoint in / m for 10-20 mg with the opening of the cervix for 2-3 fingers.

Newborns after 5 th week of life (over 30 days) are prescribed IV slowly 100-300 μg / kg body weight to the maximum dose of 5 mg, if necessary, the administration is repeated after 2-4 hours (depending on the clinical symptoms).

Children aged 5 years and older receive I / O slowly 1 mg every 2-5 minutes to a maximum dose of 10 mg; if necessary, the administration can be repeated after 2-4 hours.

Side effect

• drowsiness;
• dizziness;
• increased fatigue;
• violation of concentration of attention;
• disorientation;
• blunting of emotions;
• slowing of mental and motor reactions;
• anterograde amnesia (develops more frequently than with other benzodiazepines);
• headache;
• euphoria;
• depression;
• tremor;
• confusion of consciousness;
• dystonic extrapyramidal reactions (uncontrolled movements);
• asthenia;
• muscle weakness;
• paradoxical reactions (outbreaks of aggression, psychomotor agitation, fear, suicidal tendencies, muscle spasm, confusion, hallucinations, anxiety, sleep disturbances);
• leukopenia, neutropenia, agranulocytosis, anemia, thrombocytopenia;
• dry mouth or hypersalivation;
• heartburn;
• hiccough;
• nausea, vomiting;
• decreased appetite;
• constipation;
• arterial hypotension;
• tachycardia;
• urinary incontinence or retention;
• impaired renal function;
• increased or decreased libido;
• dysmenorrhea;
• respiratory depression (with too rapid administration of the drug);
• skin rash;
• itching;
• phlebitis or venous thrombosis (redness, swelling, pain) at the injection site;
• drug dependence;
• depression of the respiratory center;
• bulimia;
• decreased body weight;
• withdrawal syndrome (increased irritability, headache, anxiety, fear, psychomotor agitation, sleep disorders, dysphoria, spasm of smooth muscles of the internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, including hyperaemia, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - psychotic disorders);
• hypothermia.

Contraindications

• severe myasthenia gravis;
• coma;
• shock;
• angle-closure glaucoma;
• indication in the history of the phenomenon of dependence on drugs, alcohol (except for the treatment of alcohol withdrawal syndrome and delirium);
• sleep apnea syndrome;
• the state of alcohol intoxication of varying severity;
• acute intoxication with drugs that exert a depressing effect on the central nervous system (narcotic, hypnotics and psychotropic drugs);
• severe chronic obstructive pulmonary disease (risk of progression of respiratory failure);
• acute respiratory failure;
• children up to 30 days inclusive;
• pregnancy (especially 1 and 3 trimesters);
• lactation period (breastfeeding);
• increased sensitivity to benzodiazepines.

Application in pregnancy and lactation

The drug is contraindicated for use in pregnancy and lactation.

Relanium has a toxic effect on the fetus and increases the risk of congenital malformations when applied in the first trimester of pregnancy. Taking the drug in therapeutic doses at a later time of pregnancy can cause oppression of the fetal CNS. Continuous use during pregnancy can lead to physical dependence - there may be withdrawal symptoms in a newborn.

When using Relanium in doses of more than 30 mg for 15 hours before delivery or during childbirth may cause a respiratory depression in the newborn (up to apnea),a decrease in muscle tone, a decrease in blood pressure, hypothermia, a weak act of sucking ("sluggish child syndrome").

Application in elderly patients

With caution appoint elderly patients.

Use in children

Children, especially young children, are very sensitive to the depressing effect of benzodiazepines on the central nervous system.

Newborns are not recommended to prescribe drugs containing benzyl alcohol (part of the drug Relanium), tk. possibly the development of a toxic syndrome manifested by metabolic acidosis, CNS depression, difficulty breathing, kidney failure, arterial hypotension and, possibly, epileptic seizures, as well as intracranial hemorrhage.

Newborns after the 5th week of life (older than 30 days) are prescribed intravenously slowly at 100-300 μg / kg body weight to a maximum dose of 5 mg, if necessary, the administration is repeated after 2-4 hours (depending on the clinical symptoms).

Children aged 5 years and older receive I / O slowly 1 mg every 2-5 minutes to a maximum dose of 10 mg; if necessary, the administration can be repeated after 2-4 hours.

special instructions

With extreme caution, diazepam should be given in severe depression, becausethe drug can be used to implement suicidal intentions.

The intravenous solution of Relanium should be administered slowly, to a large vein, for at least 1 minute for every 5 mg (1 ml) of the drug. It is not recommended to carry out continuous intravenous infusion - it is possible to form a precipitate and adsorption of the preparation with materials from PVC infusion bottles and tubes.

In renal or hepatic insufficiency and long-term use, it is necessary to control the picture of peripheral blood and the activity of hepatic enzymes.

The risk of forming drug dependence increases with the use of Relanium in high doses, with a significant duration of treatment in patients who previously abused alcohol or drugs. Without special need, the drug should not be used for a long time. It is unacceptable to severely discontinue treatment because of the risk of withdrawal, but due to the slow elimination of diazepam, the manifestation of this syndrome is much weaker than in other benzodiazepines.

When patients develop such unusual reactions as increased aggressiveness, psychomotor agitation, anxiety, a sense of fear, suicidal thoughts, hallucinations,strengthening of muscle cramps, difficult falling asleep, superficial sleep treatment should be discontinued.

The beginning of treatment with Relanium or its abrupt reversal in patients with epilepsy or with epileptic seizures in an anamnesis can accelerate the development of seizures or epileptic status.

With extreme caution and not exceeding the recommended dose, Relanium should be used in elderly patients.

If it is necessary to use the drug in patients with liver and kidney disease, the risk-benefit ratio of therapy should be assessed.

Relanium is not administered intraarterially because of the risk of developing gangrene.

With prolonged use of the drug, it is possible to develop addiction.

During the period of treatment, alcohol consumption is prohibited.

Impact on the ability to drive vehicles and manage mechanisms

Patients receiving the drug should refrain from engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Drug Interactions

MAO inhibitors, strychnine and corazole are antagonistic to the effects of Relanium.

With the simultaneous use of Relanium with hypnotics, sedatives, opioid analgesics, other tranquilizers, benzodiazepine derivatives, muscle relaxants, general anesthetic agents, antidepressants, neuroleptics, and also with ethanol (alcohol), there is a dramatic increase in the inhibitory effect on the central nervous system.

When used simultaneously with cimetidine, disulfiram, erythromycin, fluoxetine, as well as with oral contraceptives and estrogen-containing drugs that competitively inhibit liver metabolism (oxidation processes), it is possible to slow the metabolism of diazepam and increase its concentration in the blood plasma.

Isoniazid, Ketoconazole and Metoprolol also slow down the metabolism of diazepam and increase its concentration in the blood plasma.

Propranolol and valproic acid increase the concentration of diazepam in the blood plasma.

Rifampicin can induce the metabolism of diazepam, which leads to a decrease in its concentration in the blood plasma.

Inductors of microsomal liver enzymes reduce the effectiveness of Relanium.

Opioid analgesics increase the inhibitory effect of Relanium on the CNS.

With simultaneous use with antihypertensive drugs, it is possible to intensify the hypotensive effect.

With simultaneous application with clozapine, an increase in respiratory depression is possible.

With the simultaneous use of Relanium with cardiac glycosides, it is possible to increase the concentration of the latter in the blood serum and the development of digitalis intoxication (as a result of competition with plasma proteins).

Relanium reduces the effectiveness of levodopa in patients with Parkinsonism.

Omeprazole prolongs diazepam clearance time.

Respiratory analeptics, psychostimulants reduce the activity of Relanium.

With simultaneous application with Relanium, zidovudine toxicity can be increased.

Theophylline (in low doses) can reduce the sedation effect of Relanium.

Premedication Relanium reduces the dose of Fentanyl required for an introductory general anesthesia and reduces the onset of general anesthesia.

Pharmaceutical interaction

Relanium is incompatible in one syringe with other drugs.

Analogues of the medicinal product Relanium

Structural analogs for the active substance:

• Apaurin;
• Valium Rosh;
• Diazepabene;
• Diazepam;
• Diazepec;
• Diapam;
• Relium;
• Seduxen;
• Sibazon.

Similar medicines:

Other medicines: