Relij

Relium is an anxiolytic with sedative and anticonvulsant properties.

Indications Relief

It is used in the following conditions:

• feeling of anxiety or anxiety, and in addition neurosis and borderline states, accompanied by signs of tension;
• the premature detachment of the placenta or the onset of labor, as well as tetanus and facilitation of the birth process;
• for sedation before anesthesia;
• epistatus;
• Bursitis with arthritis and myositis, against which skeletal muscle tension 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 arousal of different nature (in neurology or psychiatry);
• cardioversion

[1], [2], [3], [4], [5],

Release form

The release of the medication is realized in tablets (in the amount of 20 pieces inside a pack) or in the form of a therapeutic solution inside ampoules with a capacity of 2 ml.

[6], [7], [8]

Pharmacodynamics

Drug tablets contain an element that is a derivative of 1,4-benzodiazepine compounds; It has anxiolytic, sedative and anticonvulsant effects.

The effect of the active component of the drug is associated with a complex of endings, which includes the GAM-A-termination, GABA, the chlorine channel and the benzodiazepine end. The drug inhibits certain structures within the central nervous system (among them the cerebral cortex, spinal column, visceral brain, cerebellum, and hypothalamus). The drug substance has a powerful anxiolytic effect, sedative and hypnotic activity; it also reduces the muscle tone of the skeleton 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 (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 reduction in the severity of seizures, as well as to a slight relaxation of the skeletal muscles. Along with this, the drug also has some soporific effect.

[9], [10], [11], [12], [13],

Pharmacokinetics

When ingested, the level of its bioavailability is 98%. The values of its Cmax inside the serum are noted after 0.9-1.3 hours and equal to 500 ng / ml. Most of the active component resides inside the serum in a synthesized form.

The half-life is about 2 days. Diazepam passes through the hemato-placental barrier and BBB, and in addition, a small part of it is found inside the mother's milk. Metabolism takes place inside the liver, and excretion is carried out through the urination system.

After the introduction of drugs through injection, the active ingredient is concentrated inside the synovia and amniotic fluid, as well as inside the mother's milk. This element is able to accumulate inside the fatty tissue, subsequently released into the bloodstream. About 25% of the element is excreted in an unchanged state.

[14], [15], [16],

Dosing and administration

To take medicine in pills is allowed without reference to the use of food, and the dosage is selected for each patient separately.

In anxiety states, it is usually taken on the first tablet of drugs per day. The size of the maximum daily portion is 30 mg.

During spastic conditions, 5–15 mg of the drug are applied per day. During the day, a maximum of 60 mg of the substance is allowed.

In cases of insomnia due to anxiety, 5–15 mg of medication is required. It is recommended to take the pill for 20-30 minutes before bedtime.

For sedation requires the use of 5-20 mg of diazepam.

During treatment, it is necessary to take the drug only in the minimum portions that have a medicinal effect (it is allowed to increase the dosage only in situations where there is a significant need for potentiation of the effect). It is recommended to use the full dosage a maximum of 4 times per week.

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

Drug solution is required to enter the / m or / in the method. It is allowed to carry out injections through the intervals making at least 3-4 hours (at extremely severe conditions hourly introduction of a drug is allowed). Intravenous injection should be carried out at extremely low speeds - to avoid the development of collapse. People from 65 years old, and in addition to the weakened patients, it is required to prescribe only minimal dosages.

Intravenous administration can be carried out exclusively in the area of large veins; intraarterial injections are unacceptable. V / m injections should also be performed only in the area of large muscles. The drug must be administered exclusively separately, because it does not have compatibility with other drugs.

[26]

Use Relief during pregnancy

You can not prescribe medication for pregnant women.

Since diazepam is excreted with breast milk, when the need is to use the medication during lactation, breastfeeding should be abandoned for this period.

When appointing Relium to women in reproductive age, it is necessary to warn them that the therapy should be canceled upon the occurrence of pregnancy or if there is a suspicion of conception.

Contraindications

Main contraindications:

• the presence of strong sensitivity in relation to the active component of drugs and other benzodiazepines;
• a history of indications of alcohol and drug dependence (excluding abstinence, which has an acute form);
• severe hypercapnia of a chronic nature;
• myasthenia, with severe severity.

[17], [18]

Side effects Relief

The use of the medication can lead to fatigue or drowsiness, as well as muscle weakness. These feelings spontaneously pass after a few days. In addition, there may be other side signs:

• allergy symptoms: rashes, anaphylactic manifestations, urticaria and itching;
• drug dependence;
• changes in ECG, convulsions, pain in the area of bones, joints and muscles, as well as hyperhidrosis, respiratory failure, increased risk of fractures, disorders of the liver, jaundice, increased activity of hepatic enzymes, and urinary incontinence;
• nausea, anorexia, disorders of the chair, dryness of the oral mucosa, or vice versa hypersalivation, colic, and vomiting;
• vertigo, deterioration of visual acuity and diplopia;
• changes in blood composition or the development of neutropenia;
• depression, psychosis, feelings of excitement, confusion, hostility, anxiety, or irritability, and in addition, the impoverishment of emotions, weakening of attention, nightmares, hallucinations, and social deviation;
• feeling of aggression or anger, anterograde form of amnesia (when using large portions of diazepam), dizziness, speech or orientation disorder, headaches, loss of consciousness, tremor, dysarthria and mood instability;
• insufficiency of cardiac function (can reach complete cardiac arrest), bradycardia, a decrease in blood pressure values, pain in the sternum and circulatory failure.

[19], [20], [21], [22], [23], [24], [25]

Overdose

After intoxication Relium develops nystagmus, ataxia, dysarthria and drowsiness. In addition, sometimes it can be noted apnea, suppression of the work of the cardiovascular system or reflexes, coma and a decrease in blood pressure values. In individuals with diseases affecting the respiratory system, during an overdose, a more pronounced suppression of the respiratory process is observed.

Symptomatic and supportive measures (performing artificial respiration procedures (if the patient is unconscious), monitoring the functioning of the national system, cardiovascular system and respiratory system) are carried out to eliminate the violations. Enterosorbents are used to reduce absorption of diazepam (gastric lavage should not be performed).

[27], [28],

Interactions with other drugs

The combination of the drug with drugs that suppress the function of the central nervous system (among them hypnotic, anesthetic and sedative drugs, narcotic analgesics and neuroleptics) potentiates the suppressive effect on the central nervous system and respiratory center, and with it contributes to a pronounced decrease in blood pressure.

Combination with ethyl alcohol or drugs, which include this component, leads to potentiation of the overwhelming effect on the central nervous system (especially the respiratory center) and contributes to the occurrence of pathological intoxication.

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

Combining the drug with fluvoxamine increases the plasma values 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 occurrence of NNS.

The combination with metoprolol causes a weakening of psychomotor manifestations and reduces visual acuity. Use with lithium carbonate causes coma.

Simultaneous treatment with levodopa inhibits the anti-Parkinsonian effect; with clozapine - leads to the suppression of the respiratory process, loss of consciousness and a pronounced decrease in blood pressure.

Using together with diclofenac leads to potentiation of vertigo, and with bupivacaine - to an increase in its plasma parameters.

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 increases, and in addition, the likelihood of apnea increases.

Tricyclics (among which amitriptyline is also among them) potentiate the overwhelming effect on the central nervous system, increase the indicators of antidepressants and potentiate the cholinergic effect.

Combined use with caffeine leads to a decrease in the anxiolytic and sedative effects of drugs. Medications that can induce hepatic enzymes (among them, anticonvulsants - for example, carbamazepine or phenytoin), increase the rate of excretion of diazepam.

In individuals who have used SG for a long time, antihypertensive drugs with a central effect, anticoagulants and β-blockers, the degree and mechanisms of drug interaction may be unpredictable.

[29], [30], [31], [32], [33], [34]

Storage conditions

Relium is required to keep in a closed from the children, dark and dry place. Temperatures are standard.

Shelf life

Relium can be used within 36 months from the time of manufacture of the drug.

[35]

Application for children

Children should not be prescribed diazepam tablets, because their volume (5 mg) cannot be subjected to precise dosing (tablet separation).

Analogs

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

[36], [37], [38]

Reviews

Relium demonstrates high therapeutic efficacy, which is reflected in the reviews of most patients, but it should be used only in severe conditions. If the patient has mild neurosis, you should use other medicines that do not have a large number of negative symptoms and do not cause the development of dependence.