Relium

Relium is an anxiolytic with sedative and anticonvulsant properties.

Indications Relium

It is used in the following conditions:

• a feeling of restlessness or anxiety, as well as neuroses and borderline conditions accompanied by signs of tension;
• premature detachment of the placenta or the onset of labor, as well as tetanus and facilitation of the labor process;
• for premedication before anesthesia;
• epistatus;
• bursitis with arthritis and myositis, against the background of which tension in the skeletal muscles occurs, as well as spastic conditions caused by damage to the brain and spinal cord;
• alcohol withdrawal, which has a chronic form;
• sleep disorders;
• motor excitation of various origins (in neurology or psychiatry);
• cardioversion.

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Release form

The drug is released in tablets (20 pieces per pack) or in the form of a therapeutic solution in 2 ml ampoules.

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Pharmacodynamics

The tablets of the drug contain an element that is a derivative of 1,4-benzodiazepine compounds; it has an anxiolytic, sedative and anticonvulsant effect.

The effect of the active component of the drug is associated with a complex of endings, which includes the GAM-A ending, GABA, chloride channel and benzodiazepine ending. The drug suppresses some structures within the central nervous system (including the cerebral cortex, spinal column, visceral brain, cerebellum and hypothalamus). The drug has a powerful anxiolytic effect, sedative and hypnotic activity; it also reduces skeletal muscle tone and the severity of seizures.

The drug in ampoules has a sedative, hypnotic, anticonvulsant and anxiolytic effect. Its active element affects the endings of GABA-A and GABA (is an endogenous mediator), involved in the processes of slowing down the activity of the central nervous system. The use of the solution leads to a decrease in the severity of convulsions, as well as to a slight relaxation of the skeletal muscles. At the same time, the drug also has some hypnotic effect.

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Pharmacokinetics

When taken orally, the level of its bioavailability is 98%. At the same time, its Cmax values in the serum are noted after 0.9-1.3 hours and are equal to 500 ng/ml. Most of the active component is in the serum in a synthesized form.

The half-life is about 2 days. Diazepam passes through the hematoplacental barrier and the BBB, and in addition, a small part of it is found in breast milk. Metabolism occurs in the liver, and excretion occurs through the urinary system.

After the drug is administered by injection, the active component is concentrated inside the synovium and amniotic fluid, as well as inside the mother's milk. This element is capable of accumulating inside fatty tissues, subsequently being released into the bloodstream. About 25% of the element is excreted unchanged.

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Dosing and administration

Taking the medicine in tablets is allowed without regard to food intake, and the dosage is selected for each patient individually.

For anxiety conditions, usually take 1 tablet of LS per day. The maximum daily dose is 30 mg.

During spastic conditions, 5-15 mg of the drug is used per day. A maximum of 60 mg of the substance is allowed per day.

In cases of insomnia caused by anxiety, it is necessary to take 5-15 mg of the drug. It is recommended to take the tablet 20-30 minutes before bedtime.

For premedication, it is necessary to use 5-20 mg of diazepam.

During treatment, it is necessary to take the medication only in minimal doses that have a medicinal effect (increasing the dosage is allowed only in situations where there is a significant need to potentiate the effect). It is recommended to use the full dosage a maximum of 4 times a week.

Therapy can last a maximum of 1 month, and in cases of anxiety – within 2-3 months (these periods also include the time required to discontinue the medication).

The medicinal solution must be administered intramuscularly or intravenously. Injections may be given at intervals of at least 3-4 hours (hourly administration of the drug is permitted in extremely severe conditions). Intravenous injection must be given at an extremely low rate to avoid collapse. People over 65 years of age, as well as weakened patients, must be prescribed only minimal dosages.

Intravenous administration may be performed only in the area of large veins; intra-arterial injections are unacceptable. Intramuscular injections should also be performed only in the area of large muscles. The drug must be administered exclusively separately, because it is not compatible with other drugs.

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Use Relium during pregnancy

The medication should not be prescribed to pregnant women.

Since diazepam is excreted in breast milk, if there is a need to use the drug during lactation, breastfeeding should be discontinued during this period.

When prescribing Relium to women of reproductive age, they must be warned that therapy must be discontinued if pregnancy occurs or if there is a suspicion of conception.

Contraindications

Main contraindications:

• the presence of strong sensitivity to the active component of the drug and other benzodiazepines;
• a history of alcohol and drug dependence (excluding acute withdrawal);
• severe hypercapnia of a chronic nature;
• myasthenia gravis, which has a severe degree of expression.

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Side effects Relium

Using the medication may cause a feeling of fatigue or drowsiness, as well as muscle weakness. These sensations spontaneously disappear after a few days. In addition, other side effects may occur:

• allergy symptoms: rashes, anaphylactic reactions, urticaria and itching;
• drug addiction;
• changes in ECG values, cramps, pain in the bones, joints and muscles, as well as hyperhidrosis, respiratory failure, increased risk of fractures, liver dysfunction, jaundice, increased activity of liver enzymes, as well as urinary retention or incontinence;
• nausea, anorexia, bowel disorders, dry mouth or, conversely, hypersalivation, colic, and vomiting;
• vertigo, decreased visual acuity and diplopia;
• changes in blood composition or development of neutropenia;
• a state of depression, psychosis, a feeling of agitation, confusion, hostility, anxiety or irritability, as well as a decrease in emotions, a decrease in attention, nightmares, hallucinations and social deviation;
• feelings of aggression or anger, anterograde amnesia (when using large doses of diazepam), dizziness, speech or orientation disorders, headaches, loss of consciousness, tremor, dysarthria and mood instability;
• cardiac insufficiency (may lead to complete cardiac arrest), bradycardia, decreased blood pressure, pain in the sternum and circulatory insufficiency.

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Overdose

After intoxication with Relium, nystagmus, ataxia, dysarthria and a feeling of drowsiness develop. In addition, apnea, suppression of the cardiovascular system or reflexes, comatose state and decreased blood pressure values can sometimes be observed. In individuals with diseases affecting the respiratory system, more pronounced suppression of the respiratory process is observed during an overdose.

Symptomatic and supportive measures are taken to eliminate the disorders (artificial respiration procedures (if the patient is unconscious), monitoring the work of the nervous system, cardiovascular system and respiratory system). Enterosorbents are used to reduce the absorption of diazepam (gastric lavage should not be performed).

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Interactions with other drugs

The combination of the drug with agents that suppress the function of the central nervous system (including hypnotics, anesthetics and sedatives, narcotic analgesics and neuroleptics) potentiates the suppressive effect on the central nervous system and the respiratory center, and at the same time contributes to a significant decrease in blood pressure.

Combination with ethyl alcohol or medications containing this component leads to a potentiation of the suppressive effect on the central nervous system (especially the respiratory center) and contributes to the development of pathological intoxication.

Use with omeprazole, disulfiram or cimetidine increases the intensity and prolongs the duration of the therapeutic effect of diazepam.

Combining the drug with fluvoxamine increases plasma levels and side effects of diazepam.

Phenobarbital with phenytoin increases the rate of metabolic processes of diazepam, while rifampicin potentiates its excretion. Paracetamol reduces the excretion of Relium, and the combination with risperidone leads to the development of NMS.

Combination with metoprolol causes weakening of psychomotor manifestations and decreases visual acuity. Use together with lithium carbonate causes coma.

Simultaneous administration with levodopa inhibits the antiparkinsonian effect; with clozapine, it leads to suppression of the respiratory process, loss of consciousness and a marked decrease in blood pressure.

Use together with diclofenac leads to potentiation of dizziness, and with bupivacaine – to an increase in its plasma indicators.

Combination with oral contraception causes potentiation of the effects of diazepam and can provoke the development of breakthrough bleeding.

When Relium is used together with muscle relaxants, their medicinal effect is enhanced, and in addition, the likelihood of apnea increases.

Tricyclics (including amitriptyline) potentiate the suppressive effect on the central nervous system, increase the effects of antidepressants and potentiate the cholinergic effect.

Combined use with caffeine leads to a decrease in the anxiolytic and sedative effects of the drug. Medicines that can induce liver enzymes (including anticonvulsants, such as carbamazepine or phenytoin) increase the rate of excretion of diazepam.

In individuals who have used CG, centrally acting antihypertensive drugs, anticoagulants and β-blockers for a long time, the degree and mechanisms of drug interactions may be unpredictable.

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Storage conditions

Relium should be kept in a dark, dry place, out of reach of children. Temperature values are standard.

Shelf life

Relium can be used within 36 months from the date of manufacture of the medicinal product.

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Application for children

Diazepam tablets should not be prescribed to children because their volume (5 mg) cannot be accurately dosed (split the tablet).

Analogues

Analogues of the drug are Apaurin, Relanium, Seduxen and Valium with Diazepam.

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Reviews

Relium demonstrates high therapeutic effectiveness, which is reflected in the reviews of most patients, but it should be used only in severe conditions. If the patient has mild neuroses, other drugs should be used that do not have a large number of negative symptoms and do not cause addiction.