Elenium

Elenium is a psycholeptic medicine from the category of anxiolytics. It is also a benzodiazepine derivative.

[1]

Indications of the elenium

It is used for short-term treatment when eliminating the symptoms of disorders, and also in emergency cases:

• at disturbances of an alarming type having a different etiology (against which there are psychotic manifestations or psycho-organic syndromes);
• anxiety disorders, during which there are problems with sleep;
• alcohol withdrawal syndrome in acute form;
• increased muscle tone (of different origin).

Release form

Release in tablets, 25 pieces each inside a blister pack. In a separate pack contains 2 such blisters.

Pharmacodynamics

The substance chlordiazepoxide is a benzodiazepine derivative. The medicine affects most of the structures of the central nervous system, first of all - the hypothalamus with the limbic system, which are responsible for regulating the emotional sphere of the body. Like other benzodiazepines, the drug enhances the inhibitory effect of GABAergic neurons on the cerebral cortex, as well as the thalamus with the hypothalamus. Specific form-specific protein bundles, a protein-type structure inside the membranes of individual cells that are synthesized with a complex including the chlorine channel together with the GABA-A receptor, are found.

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

Among the properties of chlordiazepoxide - sedative and anxiolytic, and in addition to sleeping pills (moderate expression). Also, the substance has an anticonvulsant effect and reduces the muscle tension of the skeleton.

Pharmacokinetics

Chlordiazepoxide is absorbed fairly well from the digestive tract. After using the pill, the peak concentration of the substance is observed after 1-2 hours.

The medicine passes through the placenta and BBB, and also penetrates into the mother's milk.

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

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

[2], [3], [4], [5]

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 taking of tablets takes place orally, before meals or with it. It is required to wash them with water.

Often, to treat anxiety, you need to take no more than 30 mg of LS per day. Dosage is divided into several doses at intervals of 6-8 hours. In exceptional situations, admission may be allowed in higher quantities (taking into account the individual's individual need). Do not exceed the maximum possible daily dosage, which is 100 mg.

To eliminate anxiety conditions with insomnia taking place against the background, it is required to take 10-30 mg in one session, before bedtime.

When an excited state during alcohol withdrawal is required to drink 20-100 mg of Elenium. If this is necessary, you can repeat the procedure after 2-4 hours. It is forbidden to exceed the daily dose limit of 200 mg. Further, the dosage can be reduced to a minimum maintenance level, which will be sufficient to eliminate the signs of excitation.

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

Elderly patients (over 65 years of age).

Since this category of patients has increased sensitivity with respect to drugs affecting the function of the central nervous system, it is required to prescribe chlordiazepoxide in the lowest effective dosages, which do not exceed half-adult.

The medicine should be used short course (maximum 1 month), as the patients can develop addiction.

[7], [8]

Use of the elenium during pregnancy

Pregnant women can take Elenium exclusively in the presence of absolute indications, and also in the absence of the possibility of using an alternative safe preparation (especially in the 1st and 3rd trimesters).

Use of drugs with pregnant women, especially prolonged, can lead to the appearance of anomalies in the fetal development, the emergence of signs of drug dependence, and in addition to the withdrawal syndrome in a newborn.

In the case of Elenium on the 3rd trimester in large doses or in small, but for a long time, the baby may develop hypothermia or hypotension, and also attenuate the sucking reflex.

Women who are in reproductive age should be warned that before taking drugs during conception planning or when a pregnancy is suspected, it is necessary to consult a doctor.

Since the active ingredient LS passes into the mother's milk, during the treatment should abandon breastfeeding.

Contraindications

The main contraindications:

• the presence of hypersensitivity to chlordiazepoxide, as well as other benzodiazepines or other elements of drugs;
• suppression of respiratory center function or respiratory failure in acute form;
• sleep apnea syndrome;
• the presence of phobias or obsessions;
• psychoses of a chronic type;
• myasthenia gravis;
• use of chlordiazepoxide in childhood.

[6]

Side effects of the elenium

The degree of severity, as well as the frequency of side effects, depend on the size of the dosage and the sensitivity of the person. Negative reactions often appear in mild form and disappear after the end of the drug use. Among the violations:

• manifestations on the part of the CAS: the development of bradycardia, a slight decrease in blood pressure, as well as pain in the sternum;
• disturbance of the function of the lymph and hematopoietic system: a pathological change in the morphological parameters of the blood;
• reactions of NS: a sense 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 the elderly, and often disappear themselves, without discontinuing treatment. If these disorders increase, reduce their frequency and severity will help to reduce the dosage accordingly. As with the use of other benzodiazepines (especially high doses), there may be a dysarthria, accompanied by an improper pronunciation and ineffectiveness of speech, and in addition a disorder of libido and memory;
• manifestations on the part of the visual organs: visual disturbances (appearance of diplopia or visual fuzziness);
• dysfunction of the gastrointestinal tract: dyspepsia, nausea, constipation and dry mouth of the mucous membranes (rarely noted);
• disorders in the work of the kidney and urinary system: incontinence or delay urination;
• the reaction of connective tissues and the structure of muscles and bones: weakness in muscles, as well as tremor;
• eating disorders and metabolic processes: loss of appetite;
• systemic disorders: fainting and feeling of general weakness;
• immune disorders: anaphylactic manifestations are isolated;
• reactions of the subcutaneous layer with the skin: skin allergy (itching, rashes and urticaria);
• disorders of the hepatobiliary system: problems in the work of the liver, against which jaundice develops, as well as a slight increase in the level of aminotransferase;
• manifestations in the area of mammary glands and reproductive organs: menstrual cycle disorder;
• mental disorders: the emergence of paradoxical symptoms - such as insomnia, psychomotor-type anxiety, aggressiveness and increased excitability, and besides nightmares, inadequacy of behavior, anterograde-type amnesia and psychosis. Cramps, tremors and hallucinations can also occur.

The development of paradoxical symptoms is often noted as a result of the use of alcoholic beverages, and in addition in the elderly and people suffering from mental illness.

Dependence of physical and psychological nature can arise and when using drugs in the recommended dosage. After a sharp stopping the use of medication, withdrawal can occur. Dependence on the drug is more likely in people who abuse drugs or alcohol.

Overdose

Among the symptoms of overdose - a disorder of consciousness, a decrease in muscle tone and a pronounced sense of drowsiness. If there is severe intoxication, you can expect a coma, in which there is a decrease in blood pressure with collapse.

In case of poisoning, it is necessary to take measures to ensure the rapid removal of the substance from the body (until it has absorbed) or a decrease in the rate of absorption from the digestive tract. To do this, you should rinse the stomach, induce vomiting, and give the affected person activated charcoal (if he is conscious).

In intoxication, symptomatic therapy and control of important functions for life (blood pressure, pulse and respiration) and their support are supposed.

The antidote of Elenium is the substance flumazenil (it is an antagonist of substances-receivers of benzodiazepine), administered iv in a method in emergency situations. Flumazenil has a shorter exposure time than the active drug component, therefore it is necessary to continue monitoring the heart rate, blood pressure and respiration parameters of the victim so that when the relapse intoxication occurs, use the antidote again.

It is forbidden to use sedative drugs even when a person develops an arousal.

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

[9], [10]

Interactions with other drugs

Medications that have an effect on the central nervous system (such as opioid analgesics, antipsychotics, anesthetics, hypnotics, sedatives, antidepressants, and antihistamines, which have calming properties) increase the central sedative effect of Elenium.

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

Drugs-inhibitors of liver enzymes (among them erythromycin with cimetidine, as well as ketoconazole with disulfiram) slow down the biotransformation of the component chlordiazepoxide, 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, because of which the effect of the latter is reduced.

Ethyl alcohol potentiates the sedative properties of Elenium.

[11], [12]

Storage conditions

Tablets should be kept in a dark place inaccessible to small children. The temperature level is a maximum of 25 ^° C.

[13]

Special instructions

Reviews

Elenium is considered a fairly effective tool that helps to remove emotional tension, as well as eliminating problems with falling asleep. Another advantage of the medicine is its low price. Among the shortcomings, there is an increased risk of dependence, which is why it is forbidden to take the drug for a long time.

Shelf life

Elenium is allowed to be used in the period of 4 years from the date of manufacture of the medicine.