Elenium

Elenium is a psycholeptic drug from the anxiolytic category. It is also a benzodiazepine derivative.

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Indications Elenium

It is used for short-term treatment to eliminate symptoms of disorders, and also in emergency cases:

• in anxiety-type disorders of different etiology (against the background of which psychotic manifestations or psychoorganic syndromes are observed);
• in anxiety disorders, during which sleep problems are observed;
• acute alcohol withdrawal syndrome;
• increased muscle tone (of various origins).

Release form

Released in tablets, 25 pieces inside a blister pack. A separate pack contains 2 such blisters.

Pharmacodynamics

The substance chlordiazepoxide is a benzodiazepine derivative. The drug affects most of the structures of the central nervous system, primarily the hypothalamus with the limbic system, which are responsible for regulating the emotional sphere of the body. Like other benzodiazepines, the drug enhances the suppressive effect of GABAergic neurons on the cerebral cortex, as well as the thalamus with the hypothalamus. Specifically shaped ligaments inherent to benzodiazepines have been discovered - protein-type structures inside the membranes of individual cells that are synthesized with a complex that includes a chloride channel together with a GABA-A receptor.

The mechanism of medicinal action of the substance chlordiazepoxide is due to modulation of the sensitivity of the GABAergic receptor, and also stimulates an increase in the affinity of this recipient with GABA. It acts as an internal slowing neurotransmitter. After activation of the benzodiazepine or GABA-A receptor, the processes of movement of Cl ions into the neuron through the chloride channel are enhanced. This process causes hyperpolarization of the cell membrane, due to which neuronal activity is suppressed.

Among the properties of chlordiazepoxide are sedative and anxiolytic, and also a hypnotic (moderate). The substance also has an anticonvulsant effect and reduces skeletal muscle tension.

Pharmacokinetics

Chlordiazepoxide is fairly well absorbed from the gastrointestinal tract. After taking a tablet, the peak concentration of the substance is observed after 1-2 hours.

The drug crosses the placenta and the blood-brain barrier, and also penetrates into breast milk.

The half-life of the substance is 6-30 hours. Chlordiazepoxide undergoes intrahepatic transformation, during which it is converted into medicinally active decay products (dimethylchlordiazepoxide with demoxipam), prolonging the effect of the drug.

Unchanged chlordiazepoxide together with its metabolites is excreted from the body in the urine.

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Dosing and administration

The duration of the course and the size of the doses are selected exclusively by the doctor for each individual patient. The tablets are taken orally, before or with meals. They must be washed down with water.

Often, to treat anxiety conditions, it is necessary to take no more than 30 mg of the drug per day. The dosage is divided into several doses with an interval of 6-8 hours. In exceptional situations, it may be allowed to take higher amounts (taking into account the individual needs of the person). It is prohibited to exceed the maximum possible daily dosage, which is 100 mg.

To eliminate anxiety states with accompanying insomnia, it is necessary to take 10-30 mg at one time, before bedtime.

In case of an excited state during alcohol withdrawal syndrome, it is necessary to drink 20-100 mg of Elenium. If necessary, you can repeat the intake after 2-4 hours. In this case, it is prohibited to exceed the daily dose limit - 200 mg. Then the dosage can be reduced to the minimum maintenance level, which will be sufficient to get rid of the signs of excitement.

To reduce increased muscle tone, you need to take 10-30 mg per day, and do this in several separate doses.

Elderly patients (over 65 years old).

Since this category of patients has increased sensitivity to drugs affecting the central nervous system, it is necessary to prescribe chlordiazepoxide in the lowest effective doses, which do not exceed half the adult dose.

The drug should be used for a short course (maximum 1 month), as patients may develop addiction.

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Use Elenium during pregnancy

Pregnant women can take Elenium only if there are absolute indications, as well as if it is not possible to use an alternative safe drug (this is especially true for the 1st and 3rd trimesters).

The use of drugs by pregnant women, especially long-term, can cause abnormalities in fetal development, signs of drug dependence, and withdrawal syndrome in the newborn.

If Elenium is taken in the 3rd trimester in large doses or in small doses but over a long period of time, the baby may develop hypothermia or hypotension, and the sucking reflex may be weakened.

Women of reproductive age should be warned that before taking medications during the period of conception planning or if pregnancy is suspected, they must consult a doctor.

Since the active component of the drug passes into breast milk, breastfeeding should be discontinued during treatment.

Contraindications

Main contraindications:

• the presence of hypersensitivity to chlordiazepoxide, as well as other benzodiazepines or other components of the drug;
• suppression of the respiratory center function or acute respiratory failure;
• sleep apnea syndrome;
• the presence of phobias or obsessive states;
• chronic psychosis;
• myasthenia gravis;
• Use of chlordiazepoxide in children.

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Side effects Elenium

The severity and frequency of side effects depend on the dosage and the person's sensitivity. Negative reactions are often mild and disappear after the drug is discontinued. Among the disorders:

• manifestations from the cardiovascular system: development of bradycardia, slight decrease in blood pressure, as well as chest pain;
• disorders of the lymph and hematopoietic system: pathological changes in the morphological parameters of the blood;
• NS reactions: a feeling of disorientation or confusion, and with it dizziness, inhibition of reactions, a feeling of drowsiness, headaches and ataxia. Such symptoms usually occur at the initial stage of therapy in elderly people, and often disappear on their own, without stopping treatment. If such disturbances increase, their frequency and severity can be reduced by appropriate reduction of the dosage. As with the use of other benzodiazepines (especially high doses), dysarthria may occur, accompanied by incorrect pronunciation and inexpressiveness of speech, as well as libido and memory disorders;
• manifestations from the visual organs: visual disturbances (the appearance of diplopia or blurred vision);
• gastrointestinal dysfunction: dyspepsia, nausea, constipation and dry mouth (rarely observed);
• disorders of the kidneys and urinary system: incontinence or urinary retention;
• reactions of connective tissues and the structure of muscles and bones: muscle weakness, as well as tremors;
• eating and metabolic disorders: loss of appetite;
• systemic disorders: fainting and feeling of general weakness;
• immune disorders: anaphylactic reactions are observed occasionally;
• reactions of the subcutaneous layer with the skin: skin allergies (itching, rashes and urticaria);
• disorders of the hepatobiliary system: problems with the liver, which lead to jaundice, as well as a slight increase in the level of aminotransferase;
• manifestations in the area of the mammary glands and reproductive organs: menstrual cycle disorders;
• Mental disorders: the appearance of paradoxical symptoms such as insomnia, psychomotor anxiety, aggressiveness and increased excitability, as well as nightmares, inappropriate behavior, anterograde amnesia and psychosis. Convulsions, tremors and hallucinations may also occur.

The development of paradoxical symptoms is often observed as a result of alcohol consumption, and also in elderly people and people suffering from mental illnesses.

Physical and psychological dependence may also occur when using drugs in recommended medicinal doses. Withdrawal syndrome may occur after abruptly stopping the use of the drug. Dependence on the drug is more likely in people who abuse drugs or alcohol.

Overdose

Symptoms of overdose include impaired consciousness, decreased muscle tone, and a pronounced feeling of drowsiness. If severe intoxication is observed, a comatose state can be expected, in which a decrease in blood pressure with collapse is observed.

In case of poisoning, it is necessary to take measures to ensure rapid elimination of the substance from the body (before it has time to be absorbed) or to reduce the rate of absorption from the gastrointestinal tract. To do this, the stomach should be washed, vomiting should be induced, and the victim should be given activated carbon (if he is conscious).

In case of intoxication, symptomatic therapy and monitoring of vital functions (blood pressure, pulse and breathing) are prescribed, as well as their support.

The antidote to Elenium is flumazenil (an antagonist of benzodiazepine receptor substances), administered intravenously in emergency situations. Flumazenil has a shorter period of action than the active component of the drug, so it is necessary to continue monitoring the pulse, blood pressure and respiration of the victim in order to reuse the antidote if intoxication relapses.

It is prohibited to use sedatives even if a person becomes agitated.

There is no information on the advisability of the hemodialysis procedure.

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Interactions with other drugs

Medicines that have an effect on the central nervous system (such as opioid analgesics, neuroleptics, anesthetics, hypnotics, sedatives, antidepressants, as well as antihistamines with sedative properties) enhance the central sedative effect of Elenium.

Anticonvulsants used in combination with chlordiazepoxide can potentiate the negative properties and toxicity of the drug, so they should be combined with great caution.

Medicines that inhibit liver enzymes (including erythromycin with cimetidine, as well as ketoconazole with disulfiram) slow down the biotransformation of the chlordiazepoxide component, as well as other benzodiazepines, due to which the properties of the latter are enhanced.

Drugs that induce liver enzymes (such as phenytoin with rifampicin, as well as carbamazepine) increase the rate of biotransformation of the substance chlordiazepoxide and other benzodiazepines, due to which the effect of the latter is reduced.

Ethyl alcohol potentiates the sedative properties of Elenium.

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Storage conditions

The tablets should be kept in a dark place, out of reach of small children. The temperature level is a maximum of 25 ^o C.

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Special instructions

Reviews

Elenium is considered to be quite an effective remedy that helps relieve emotional stress and eliminates problems with falling asleep. Another advantage of the drug is its low price. Among the disadvantages is the increased risk of developing addiction, as a result of which it is prohibited to take the drug for a long time.

Shelf life

Elenium is permitted to be used for a period of 4 years from the date of manufacture of the medicine.