Description of the drug RELIUM

pharmachologic effect

The tablets contain a medicinal substance that is a derivative of 1,4-benzodiazepine and has sedative , anticonvulsant and anxiolytic effects.

The action of the active substance is associated with the receptor complex. It includes gamma-aminobutyric acid, GAM-A receptor, benzodiazepine receptor and chloride channel. The active substance inhibits several structures in the central nervous system, in particular the spinal column, limbic system, cerebral cortex, hypothalamus and cerebellum. This substance has a strong anxiolytic effect, hypnotic and sedative activity, reduces the severity of seizures and the tone of skeletal muscles.

Relium in ampoules has hypnotic, anticonvulsant, sedative and anxiolytic effects. The action of the active substance is to influence GABA-A receptors and gamma-aminobutyric acid, which is an endogenous neurotransmitter involved in inhibition processes in the central nervous system. When using the solution, patients experience a decrease in seizures and slight relaxation of skeletal muscles. It also has some hypnotic effects.

General information about the drug Relanium

Relanium is a drug with a fairly wide spectrum of action. It can be prescribed only by specialists who are authorized to work with such drugs. To understand the effect of a drug on the body, you should study its basic properties.

Drug group, INN, scope of application

Relanium is an anxiolytic. International nonproprietary name (INN) – Diazepam. This is a psychotropic substance that is used in many medical fields. In psychiatry and neurology, it is prescribed to relieve acute conditions. Long-term use of the product is also possible.

• Possible side effects and overdose of Relanium
• General information about the drug Relium
• General information about the drug Relium
• Side effects
• Directions for use and dosage
• special instructions
• Indications and contraindications
• Indications and detailed instructions

Classification of anxiolytics

Anesthesiologists use it before administering anesthesia. Thanks to its use, the patient’s condition is alleviated during various diagnostic procedures that require muscle relaxation. It is less commonly used in obstetric practice. Due to its property of relaxing smooth muscles, it is indispensable in traumatology.

Release forms and prices for the drug, average in Russia

The medication is available in the form of an injection solution in ampoules. Tablets with this trade name are not produced.

A cardboard package may contain 5, 10 or 50 ampoules with 2 ml of clear, colorless or light green/yellow liquid. The average price for the drug is shown in the table. Relanium can only be purchased with a prescription.

Compound

Diazepam is the active component of the drug. It belongs to the benzodiazepine group of tranquilizers. The main properties of the substance are inhibition of impulse transmission to areas of the brain and spinal cord, resulting in relaxation of smooth muscles and calming of the nervous system.

With prolonged use it causes addiction and dependence. According to WHO, diazepam-based drugs are included in the list of some of the most necessary medications in the state’s healthcare system. The medication is also necessary to provide emergency care in the event of many dangerous conditions.

Properties of diazepam

But working with this substance requires special permission and knowledge. To prevent misuse and uncontrolled distribution of diazepam-based drugs, Relanium is included in the list of psychotropic drugs subject to strict control and recording.

To extend the shelf life and preserve the properties of the main component, Relanium includes excipients:

• propylene glycol;
• benzyl alcohol;
• ethanol;
• sodium benzoate;
• acetic acid;
• water for injections.

Pharmacodynamics and pharmacokinetics

Inhibits the functions of the nervous system, acting on the hypothalamus, thalamus and limbic system. Due to the inhibition of the action of GABA, it helps to inhibit the passage of nerve impulses to the brain. Reduces the excitability of subcortical structures of the brain (hereinafter - GM). In the spinal cord it leads to inhibition of spinal reflexes.

The distribution and rate of absorption of Relanium depends on the location and method of administration of the solution. Intravenous administration of the drug ensures its faster distribution throughout the body and onset of action.

Half-life of the drug

The maximum concentration in the blood is observed 50-60 minutes after intramuscular administration and 15 minutes after intravenous administration. Once in the liver, Relanium is processed into bile acids, after which it is excreted from the body in the urine.

Pharmacodynamics and pharmacokinetics

Bioavailability after oral administration is 98 percent. The maximum level of the active substance in the serum is observed after 0.9-1.3 hours and is 500 ng/ml. The main part of the active substance in the serum is in bound form. The half-life lasts up to two days. Diazepam penetrates the blood-brain and blood-placental barriers, and is also detected in small amounts in breast milk. Metabolization occurs in the liver and is excreted through the urinary system.

When administered by injection, high concentrations of the active substance are observed in amniotic and synovial fluids, as well as in breast milk. This substance tends to accumulate in adipose tissue and is subsequently released into the bloodstream. Approximately 25 percent is excreted unchanged.

General information about the drug Relium

Relium is a standard psycholeptic of European quality. It is produced in Warsaw (Poland) at the Polfa pharmaceutical concern. The medication has a combined effect, providing anticonvulsant and sedative effects. The drug is on the list recommended for availability in medical institutions compiled by the World Health Organization.

Drug group, INN, scope of application

Relium belongs to the pharmacological group of psycholeptic drugs, a subgroup of anxiolytics, benzodiazepine derivatives. A special feature of this group is that all drugs included in its composition are sold strictly according to prescription. International nonproprietary name (INN) is Diazepam.

The drug is actively used in psychiatric, neurological and drug addiction practices. It can also be used in selected clinical cases of infectious diseases.

Release forms

Available in the form of film-coated tablets. Each tablet is round, biconvex, yellow in color. Dosage is exclusively 5 mg.

The price of medicine in Russian pharmacies differs slightly.

Composition of Relium

The active substance of the drug is diazepam. This component is a chemical derivative of 1,4-benzodiazepine. It has the ability to influence the GABAergic system, changing its sensitivity. The amount of diazepam in a tablet is directly proportional to its dosage. Auxiliary components are:

• potato starch;
• dry gelatin;
• yellow quinoline dye (E 104);
• talc;
• magnesium stearate;
• sodium starch glycolate.

The coating covering the tablet consists of cellulose acetate phthalate, polyethylene glycol 6000.

Pharmacodynamics and pharmacokinetics

The basis of the mechanism of action of Relium is the pharmacodynamic effects of diazepam. The medication has a direct effect on all components of the central nervous system. While taking the medication, changes occur especially actively in the centers of the brain responsible for emotionality - these are, directly, the limbic system and the hypothalamus.

Relium has an inhibitory effect on neurons of the GABAergic system located in the cerebral cortex, hippocampus, and cerebellum. As a result of this, there is a change in the activity of various groups of neurons: dopamine, norepinephrine, serotonin and cholinergic. Against the background of all these processes, the sensitivity and susceptibility to stimuli of the GABA receptor changes, which leads to an increase in its affinity for gamma-aminobutyric acid, which itself is an internal inhibitory transmitter.

Thanks to the combination of these processes, complex sedative effects occur: feelings of fear and anxiety are eliminated, muscle tension is reduced, and sleep improves.

Relium is absorbed by the mucous membrane of the gastrointestinal tract. Metabolism occurs in the liver. Here the active component begins to be divided into two components - N-desmethyl-diazepam and N-methyloxazepam. These, in turn, are converted to oxazepam, which has an affinity for glucuronic acid. Its half-life is a day or two. In the form of these metabolites, the drug is excreted from the body in the urine.

The peak concentration of the drug in the circulatory system occurs an hour after taking the tablet. Relium has the ability to penetrate the blood-brain and placental barrier.

Indications for use of Relium

Indications for use are as follows:

• neuroses , anxiety , restlessness , borderline states with manifestations of tension;
• tetanus , premature placental abruption, premature birth , facilitation of labor;
• premedication before anesthesia;
• status epilepticus;
• arthritis , bursitis , myositis , which are accompanied by tension in the skeletal muscles, spastic conditions that are associated with damage to the spinal cord and brain;
• withdrawal syndrome in chronic alcoholism, motor excitation of various etiologies in psychiatry and neurology, sleep disorders;
• cardioversion.

Indications and contraindications

The medicine "Relanium" (analogs of this drug are dispensed from pharmacies only with a doctor's prescription) is used for anxiety, regular insomnia, and painfully low mood. The medicine is recommended for spastic conditions, as well as for spasms of the skeletal muscles, which usually occurs due to injuries. Prescribed medication for arthritis, myositis, bursitis.

Indications for use are vertebral syndrome, chronic polyarthritis, frequent headaches arising from excessive nervous tension. Relanium is prescribed to patients with angina pectoris, rheumatic pelvispondyloarthritis, and arthrosis.

The drug is prescribed for excessive nervous tension, alcohol withdrawal, tremors of the arms and legs, as well as transient reactive symptoms.

The drug is widely used in complex treatment if there are psychosomatic disturbances in the body, there is a digestive tract ulcer or arterial hypertension.

The drug is intended for use in epilepsy, gestosis, menstrual disorders, menopausal symptoms, eczema, constant irritability, drug intoxication, as well as Meniere's disease.

The drug is used before endoscopic and surgical interventions for premedication, before administering general anesthesia to the patient. They reduce anxiety and worry during myocardial infarction.

The drug is widely used in the field of psychiatry, neurology and to make it easier for women to give birth to a child. The doctor may prescribe medication if the placenta begins to separate prematurely, as well as in case of premature birth.

"Relanium" (analogs in tablets are not available without a doctor's prescription) is contraindicated in severe myasthenia gravis; it is not prescribed for coma, shock and closed glaucoma. The prohibition is sleep apnea syndrome. The medicine is not prescribed to people who are drunk. The drug should not be prescribed to persons with acute attacks of poisoning or in the presence of severe diseases of the respiratory system.

Do not use the drug in acute respiratory failure, in infancy up to one month

The medicine is not prescribed to pregnant and lactating women, as well as to patients with hypersensitivity to benzodiazepines. Persons with absence seizures and Lennox-Gastaut syndrome, as well as patients with epilepsy should use the drug with extreme caution. Patients with renal and hepatic failure, people diagnosed with cerebral and spinal ataxia and those suffering from hyperkinesis should be monitored

This category also includes patients with major depressive disorders, hypoproteinemia and the elderly.

Side effects

When using Relium, drowsiness, muscle weakness and fatigue are often observed, which spontaneously disappear after a couple of days. Other unwanted effects may also occur:

• allergic reactions: anaphylactic reactions, rash , itching and urticaria ;
• drug addiction;
• ECG changes, hyperhidrosis , convulsions , pain in joints, bones and muscles, increased risk of fractures, respiratory failure , liver dysfunction, increased activity of liver enzymes, jaundice , urinary incontinence or retention;
• bowel disturbances, nausea , colic , dry mouth or hypersalivation , vomiting , anorexia ;
• decreased visual acuity, vertigo , diplopia ;
• changes in blood composition, neutropenia ;
• confusion , emotional poverty, depression , decreased attention, deviant behavior , nightmares , psychosis , hostility, irritability , anxiety , hallucinations , agitation ;
• anterograde amnesia (with high doses of diazepam), anger, aggression , disorientation , dizziness , speech , tremor , headache , mood lability, loss of consciousness , dysarthria ;
• heart failure (up to cardiac arrest), arterial hypotension , bradycardia , circulatory failure, chest pain.

Instructions for use of Relium (Method and dosage)

According to the instructions for use of Relium, tablets are taken regardless of food, the dose is selected individually for each patient.

As a rule, in most cases for anxiety conditions, 1 tablet per day is prescribed. The maximum dose is 30 milligrams per day. For spastic conditions, 5 to 15 milligrams per day are prescribed. The maximum dose is 60 milligrams per day. For insomnia associated with anxiety, 5 to 15 milligrams are prescribed. It is recommended to take the medicine 20-30 minutes before bedtime. For premedication , 5 to 20 milligrams of diazepam .

During therapy, it is recommended to use only the minimum doses of the active substance that provide a therapeutic effect (the dose can be increased only in cases where there is a significant need to enhance the effect). It is not advisable to use the full dose more than four times a week.

The maximum duration of treatment is one month, for anxiety conditions - from 8 to 12 weeks (the time for drug withdrawal is included in the periods).

The solution is administered intravenously or intramuscularly. Injections can be done no more often than every 3-4 hours, in extremely severe cases they can be done every hour. The drug must be injected into a vein very slowly, otherwise collapse . Patients over 65 years of age, as well as weakened patients, can be prescribed only minimal doses.

The solution can be administered intravenously only into large veins; intraarterial administration is unacceptable. It can be administered intramuscularly only into large muscles. This medicine can only be administered separately, as it is incompatible with other medicines.

General information about the drug Relium

Relium is a standard psycholeptic of European quality. It is produced in Warsaw (Poland) at the Polfa pharmaceutical concern. The medication has a combined effect, providing anticonvulsant and sedative effects. The drug is on the list recommended for availability in medical institutions compiled by the World Health Organization.

Drug group, INN, scope of application

Relium belongs to the pharmacological group of psycholeptic drugs, a subgroup of anxiolytics, benzodiazepine derivatives. A special feature of this group is that all drugs included in its composition are sold strictly according to prescription. International nonproprietary name (INN) is Diazepam.

The drug is actively used in psychiatric, neurological and drug addiction practices. It can also be used in selected clinical cases of infectious diseases.

Release forms

Available in the form of film-coated tablets. Each tablet is round, biconvex, yellow in color. Dosage is exclusively 5 mg.

The price of medicine in Russian pharmacies differs slightly.

Overdose

In case of overdose, dysarthria , nystagmus , drowsiness and ataxia . apnea , coma , depression of cardiac and vascular function, and arterial hypotension can also sometimes be observed . In people with diseases of the respiratory system, with an overdose, respiratory depression becomes more pronounced.

Treatment consists of eliminating symptoms, supportive therapy (carrying out artificial respiration (in the absence of consciousness), monitoring the functions of the cardiovascular, nervous and respiratory systems). To reduce the absorption of diazepam, enterosorbents are prescribed (gastric lavage is not recommended).

Interaction

Concomitant use with drugs that depress the central nervous system (including opioid analgesics , hypnotics , sedatives , antipsychotics and anesthetics respiratory center, and also contributes to the development of severe arterial hypotension .

Simultaneous use with ethanol or drugs containing ethanol enhances the inhibitory effect on the central nervous system (especially the respiratory center) and contributes to the development of pathological intoxication syndrome.

Concomitant use with disulfiram , omeprazole , cimetidine increases the intensity and duration of exposure to diazepam.

Concomitant use with fluvoxamine increases plasma concentrations and side effects of diazepam.

Phenytoin and phenobarbital accelerate the metabolism of diazepam, and rifampicin increases its elimination. Paracetamol reduces the excretion of diazepam, and simultaneous use with risperidone promotes the development of NMS.

Simultaneous use with metoprolol leads to a deterioration of psychomotor reactions and a decrease in visual acuity, with lithium carbonate - leads to the development of a coma, with levodopa - suppresses the antiparkinsonian effect, with clozapine - causes loss of consciousness, respiratory depression and severe arterial hypotension, with diclofenac - causes increased dizziness, with bupivacaine - increases its concentration in the blood plasma, with oral contraceptives - enhances the effect of diazepam and can lead to breakthrough bleeding , with muscle relaxants - enhances their effect and increases the risk of apnea , with tricyclic antidepressants (including amitriptyline ) - enhances a depressant effect on the central nervous system, enhances the cholinergic effect and increases the concentration of antidepressants.

Simultaneous use with caffeine reduces the sedative and anxiolytic effects of the drug. Medicines that cause induction of liver enzymes, including anti- epileptic ( phenytoin , carbamazepine ), accelerate the elimination of diazepam.

In people who have been taking cardiac glycosides , anticoagulants , beta-blockers , and antihypertensive drugs , the mechanisms and extent of drug interactions may be unpredictable.

Analogs

Level 4 ATC code matches:
Bromazepam

Helex

Rudotel

Nozepam

Tazepam

Xanax

Elenium

Valium Roche

Alprazolam

Tofisopam

Diazepam

Grandaxin

Mezapam

Sibazon

Seduxen

Relanium

Lorazepam

Analogues are:

• Apaurin;
• Seduxen;
• Diazepam;
• Relanium;
• Valium.