Application of Relium in neurological practice: instructions and reviews. Relium Relanium - instructions for use

film-coated tablets 5 mg

Registration number:

P No. 015047/02-2003

Tradename

RELIUM

International nonproprietary name

Diazepam

Dosage form, dose

film-coated tablets, 5 mg

Compound:

active substance:
diazepam 5 mg

Excipients:
potato starch, gelatin, Tween 80, talc, quinoline yellow magnesium stearate E 104, lactose

shell composition:
cellulose acetate phthalate, polyethylene glycol 6000

Description

Film-coated tablets, round, convex on both sides, without frayed edges or cracks, yellow in color. Yellow at the break.

Pharmacological group:

Group affiliation according to the ATS classification: N 03 AE, N 05 BA.
Anxiolytic drug from the group of benzodiazepines

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics

Diazepam belongs to the group of benzodiazepine derivatives.

The drug acts on many structures of the central nervous system. The mechanism of action of the drug is closely related to the inhibitory endogenous neurotransmitter gamma-aminobutyric acid (GABA) and the GABA-A receptor, through which the neurotransmitter realizes its effects in the central nervous system.

Like all other benzodiazepines, diazepam enhances the inhibitory effect of GABAergic neurons in the central nervous system.

The clinical effect of diazepam is manifested by a pronounced anxiolytic and anticonvulsant effect; The hypnotic and central muscle relaxant effect is somewhat less pronounced.

Pharmacokinetics

Suction

After oral administration, diazepam is well and quickly absorbed from the digestive tract, bioavailability is 98%.

After oral administration of one dose of the drug 20 mg, the maximum concentration of the drug in the blood serum (Cmax) is reached after 50-90 minutes and is approximately 500 ng/ml.

Distribution

Diazepam is approximately 94-99% bound to blood proteins. The drug passes through the blood-brain and placental barrier and penetrates into mother's milk. Shows great affinity for adipose tissue, in which it is deposited and from there gradually released into the blood.

The volume of distribution is 1.1-1.5 l/kg.

Metabolism

Diazepam is extensively metabolized in the liver to the active metabolites N-desmethyldiazepam (nordazepam) and N-methyloxazepam. Both metabolites undergo conversion to the pharmacologically active oxazepam, which binds to glucuronic acid.

The half-life (t 1/2) is 24-48 hours; may be prolonged in newborns and elderly patients (active metabolites prolong the half-life; the half-life of N-desmethyloxazepam can reach up to 100 hours, depending on age and liver activity).

Selection

The drug is excreted mainly in the urine in the form of metabolites; up to 25% of the drug can be excreted unchanged by the kidneys. Repeated doses of the drug may lead to accumulation of the drug and its metabolites.

INDICATIONS FOR USE

• neuroses, borderline states with symptoms of tension, anxiety, anxiety, fear
• for alcohol withdrawal syndrome, in order to reduce symptoms of agitation
• in complex therapy for diseases associated with increased skeletal muscle tone (after injuries, spastic conditions after cerebral strokes)
• sleep disorders
• in complex therapy of epilepsy (in combination with other anticonvulsants)
• motor agitation of various etiologies
• in preparation for surgical interventions and diagnostic procedures

The drug should be used strictly as prescribed by the doctor to avoid complications.

METHOD OF APPLICATION AND DOSES

The dosage and duration of treatment should be selected individually for each patient in order to obtain maximum treatment effects.

The following doses are usually used:

Adults

Conditions of fear: 2-10 mg 2-4 times a day.

Alcohol withdrawal syndrome: 10 mg 3-4 times a day during the first 24 hours, then (if necessary) 5 mg 3-4 times a day.

Diseases accompanied by increased skeletal muscle tone: 2-10 mg 3-4 times a day.

Sleep disorders: 5-15 mg in a single dose before bedtime.

Epilepsy (in combination with other drugs): 2-10 mg 2-4 times a day.

Preparation for surgical interventions and diagnostic procedures: 5-20 mg in a single dose or in divided doses before surgery.

Maximum daily dose: up to 60 mg/day (in complex therapy of epilepsy, often in spastic conditions)

0.1-0.8 mg per 1 kg of child’s body weight per day.

From 1 year to 3 years: 1-1.5 mg – 2-3 times a day. Daily dose 2.5 – 5.0 mg.

3 – 7 years: 1.5-2.5 mg - 2-3 times a day. The daily dose is 5-7 mg.

The drug should not be used in children under 1 year of age.

Elderly patients (over 65 years old)

Diazepam should be used with caution in elderly patients. A dose reduction is recommended. Usually 2 – 2.5 mg 1 – 2 times a day. If necessary, the dose can be gradually increased (provided the drug is well tolerated).

Patients with impaired liver and kidney function.

The duration of therapy is usually 4 weeks (including the time of gradual reduction of the drug dose). Do not take the drug for more than 4 weeks without re-evaluating the need to continue therapy.

You cannot abruptly discontinue the drug; a gradual, doctor-controlled, dose reduction is always necessary. Abrupt withdrawal of diazepam can lead to sleep and mood disorders, and even mental disorders. Abrupt withdrawal during long-term therapy or when using large doses of the drug is especially dangerous. Withdrawal symptoms are then more pronounced.

SIDE EFFECT

The most common undesirable effects during drug therapy are: drowsiness, tiredness, tiredness, impaired coordination of movements.

Less common: dizziness and headache, disorders of the digestive tract (nausea, constipation), blurred vision, slurred speech, liquefaction of blood pressure, depression, states of disorientation, decreased libido, skin allergic reactions, urination disorders, neutropenia, yellowness of the skin (during long-term therapy, periodic monitoring of blood patterns and liver function tests is indicated), paradoxical reactions (states of psychomotor agitation, insomnia, fear).

If paradoxical reactions occur, treatment should be interrupted immediately.

Systematic use of the drug for more than 2-3 weeks can lead to the development of drug dependence, as well as withdrawal syndrome in case of abrupt withdrawal.

Warnings

Long-term use of diazepam leads to a gradual weakening of the effect of the drug as a result of the development of the phenomenon of tolerance.

Long-term use of the drug contributes to the development of psychophysical drug dependence and withdrawal syndrome in case of abrupt withdrawal of diazepam. Withdrawal syndrome is characterized by psychomotor agitation, fear, autonomic disorders and insomnia.

During treatment with diazepam and for 3 days after its completion, you should not drink any alcoholic beverages.

CONTRAINDICATIONS

• hypersensitivity to benzodiazepines,
• breathing disorders of central origin and severe conditions of respiratory failure, regardless of the cause,
• myasthenia gravis,
• angle-closure glaucoma,
• disturbances of consciousness.

Do not use in children under 1 year of age.

USE IN PREGNANCY AND BREAST-FEEDING

The use of a medicine during pregnancy is allowed only if its use by the mother has absolute indications, and the use of a safer, alternative remedy is impossible or contraindicated. During treatment with diazepam, you should not breastfeed.

INTERACTIONS WITH OTHER MEDICINES

Pharmaceutical

Pharmaceutical types of incompatibility are not defined

Pharmacodynamic

The inhibitory effect of diazepam on the central nervous system is enhanced by all drugs with a similar effect: hypnotics (eg barbiturates), drugs that lower blood pressure with central action, antipsychotics, antidepressants, anticonvulsants, narcotic analgesics.

Ethyl alcohol exhibits a similar effect. Drinking alcohol during treatment with diazepam, in addition to its cumulative depressant effect on the central nervous system, can provoke paradoxical reactions: psychomotor agitation, aggressive behavior.

The drug enhances the effect of drugs that reduce skeletal muscle tone.

Pharmacokinetic

Oral contraceptives may slow down the metabolism of diazepam and enhance its effect.

Smoking may reduce the effect of diazepam.

OVERDOSE

As a result of an overdose of diazepam, the following symptoms may appear: drowsiness, disorientation, slurred speech, and in severe cases, loss of consciousness and coma.

In case of acute poisoning, it is necessary to induce vomiting and rinse the stomach.

Treatment for diazepam overdose is primarily symptomatic and consists of monitoring vital signs (respiration, pulse, blood pressure).

A specific antidote is flumazenil (a benzodiazepine receptor antagonist).

SPECIAL INSTRUCTIONS

Impact on the ability to drive vehicles and maintain moving mechanical devices

During treatment with the drug and for 3 days after its completion, you should not drive a vehicle, service moving mechanical devices, or perform work that requires special attention and quick response.

RELEASE FORM

Film-coated tablets 5 mg

Package

20 tablets per blister.
One blister along with instructions for use is placed in a cardboard box.

STORAGE CONDITIONS

Store at temperatures up to 25°C. Protect from light and moisture.
List of potent and toxic substances No. I according to PKKN
Keep out of the reach of children.

BEST BEFORE DATE

3 years
Before using the drug, you must check the expiration date indicated on the packaging.
The drug should not be used after the date indicated on the package.

CONDITIONS FOR DISCHARGE FROM PHARMACIES:

according to a doctor's prescription.

MANUFACTURER

Tarkhoma Pharmaceutical Plant "Polfa" Joint Stock Company

st. A. Fleming 2

Relium is a drug based on a potent psychotropic substance with a calming effect. It is used in the treatment of mental illnesses and disorders, in the complex treatment of neurological disorders.

Relium is a drug based on diazepam, a potent psychotropic substance with a sedative effect.

Pharmacotherapeutic group

ATC code – N05B - ​​psycholeptic drugs of the anxiolytics group. International nonproprietary name – Relium.

In Latin the name is Relium.

Mechanism of action

A drug with a wide range of actions: sedative, anxiolytic and anticonvulsant.

Diazepam, the main component, has a depressant effect on individual, selective centers of the central nervous system: the cerebellum, hypothalamus and cerebral cortex. The effect also extends to the spinal column.

The principle of action is to influence the receptor complex involving the chlorine channel, GABA-A receptors and the benzodiazepine receptor. When ingested, Diazepam has a stimulating effect on gamma-aminobutyric acid, resulting in an increase in the biological effect of the GABA receptor. The degree of permeability of chloride ions increases, which enhances the inhibitory effect on the neuron.

For cerebral etiology, the medication helps reduce the frequency and severity of muscle cramps. Calms the central nervous system, reduces muscle tone.

Pharmacokinetics: absorption reaches 98%. The peak concentration in the blood is detected 1.5-2 hours after taking the drug. The half-life is from 1 to 2 days. The process of metabolism of components takes place in the liver. It is excreted from the body through the kidneys with urine.

Composition and release form

The main substance in the composition is diazepam. Related components: magnesium stearate, dyes, lactose, starch. Release form: tablets and solution for injection.

Pills

One tablet contains 5 mg of the active ingredient.

Injection

1 ml of solution contains 5 mg of diazepam. Additional components: sodium benzoate, benzoic acid, water for injection, benzyl alcohol.

Indications for use

The medication is prescribed to patients for the following diseases and mental disorders:

• neurotic disorders;
• tremor;
• diseases accompanied by hypertonicity of muscle fibers: sclerosis, torticollis, extensive injuries, cerebral strokes;
• somatic disorders;
• frequent attacks of anxiety and restlessness;
• sleep disorders, insomnia;
• excessive emotional arousal caused by withdrawal syndrome due to alcoholism;
• spasm of skeletal muscles due to illness or injury;
• status epilepticus;
• tetanus.

Used in surgical procedures during patient preparation. Can be used with other medications for complex treatment:

• arterial type hypertension;
• stomach diseases;
• duodenal ulcer;
• psychosomatic disorders in gynecology and obstetrics;
• gestosis;
• disorders caused by menopause and menopause;
• excessive irritability.

The medication is used in the treatment of severe allergic reactions accompanied by severe itching of the skin.

Contraindications

• individual intolerance to individual components of the drug;
• breathing disorders, incl. and the development of respiratory failure;
• sleep apnea;
• moderate and severe stages of liver and kidney failure;
• state of obsession;
• psychoses occurring in the chronic stage;
• myasthenia gravis.

Directions for use and dosage

The required dose and duration of the therapeutic course are selected for each patient individually. Regardless of the diagnosis, it is necessary to start taking it with the lowest dosage that can provide positive dynamics. In the absence of a negative reaction from the body to the drug, the dose is gradually increased.

Dosage for adult patients:

1. Therapy of anxiety – 5 mg. Per day, no more than 30 mg is allowed, divided into 2-3 doses; The frequency is determined by the doctor.
2. Sleep disturbance, insomnia – from 5 to 15 mg, depending on the severity of the disorder.
3. Treatment of spastic muscle contractions - from 50 to 15 mg per day, the dosage of 10 and 15 mg is divided into several doses. Rarely, in case of intense symptoms of a clinical case, only by the doctor’s decision and in the absence of positive dynamics from the minimum and average dosage, the amount of the drug is increased to 50-60 mg per day.
4. Premedication (preparation for surgery) – from 5 to 15 mg.
5. Withdrawal syndrome from alcohol abuse - 10 mg, divided into 3 doses, the dose can be increased to 60 mg.

The duration of treatment for insomnia is from 1 to 2 months. Treatment of anxiety conditions – from 2 to 3 months.

Dosage for children by age:

• from 2 to 3 years, 2 mg is prescribed, which can be increased to 5 mg, which are divided into several doses;
• from 4 to 7 years, the dose is from 4 to 6 mg, 2-3 doses per day;
• age category from 8 years - twice a day, total dosage per day - from 5 to 8 mg.

The medication is prescribed to children under 5 years of age only if there are special indications when other medications cannot provide the necessary therapeutic effect.

Application of solution for injection: the product is injected intramuscularly, only into large muscle fibers, deeply.

For the treatment of adults, intravenous administration of the drug can be used:

• anxiety states with severe intense symptoms - intramuscularly or intravenously, the dosage per administration is from 5 to 10 mg, if necessary, the administration of the solution can be repeated, but after 3-4 hours;
• phobic disorders - intravenously, intramuscularly, dose from 5 to 10 mg, repeated administration of the solution is allowed on the same day, after 4 hours;
• relief of abstinence syndrome due to alcoholism - 10 mg of solution at a time, repeated dosage - from 5 to 10 mg, administration is carried out after 4 hours;
• tetanus therapy, treatment of muscle spasms - intravenously or intramuscularly from 5 to 10 mg; when treating tetanus, the amount of medicine can be increased;
• therapy for status epilepticus, treatment of frequent relapses of convulsive seizures - the initial dosage is from 5 to 10 mg, if necessary, the injection can be repeated after 15 minutes, repeated administration of 30 mg of the drug is allowed;
• conducting electrical pulse therapy - 5 to 10 mg is administered 10 minutes before the procedure.

Treatment of tetanus in children - intramuscular or intravenous administration (necessarily slow):

• from 5 weeks after birth – from 1 to 2 mg;
• age 5 or more years - from 5 to 10 mg, if necessary, repeat the administration of the medicine after 4 hours.

Treatment of epileptic seizures, relapses of convulsive seizures - intravenously, monitoring respiratory function:

• from 5 weeks after birth to 5 years – from 0.2 to 0.5 mg, solution administration lasting from 2 to 5 minutes, permissible dosage per day – 5 mg;
• 5 years or more - intravenously, 1 mg solution over 5 minutes, the maximum dose is 10 mg.

Premedication with a solution is 10 mg, the amount can be increased to 20 mg if the patient is not prescribed the use of narcotic analgesics. The solution is administered slowly intravenously. Intramuscular administration - dosage from 5 to 10 mg half an hour before surgery.

Intramuscular administration - dosage from 5 to 10 mg half an hour before surgery.

special instructions

To prepare a solution for intramuscular injection, the ampoule liquid must be diluted in 10 ml of saline or glucose (5% solution). The rate of administration of the finished solution is no more than 4 mg of the drug in 60 seconds. The preparation of a solution for intravenous drip administration is as follows: 10 ampoules are diluted in 0.5 liters of saline or glucose solution. The rate of administration by drip is 40 ml in 60 minutes.

It is important to warn the patient that the duration of therapy is limited. The dosage must be observed throughout the course. Abruptly stopping treatment is not recommended. When therapy comes to an end, the dose is gradually reduced to a minimum.

Patients with lactose intolerance should not take the medication. Use with caution if you have glaucoma or blood diseases that affect blood clotting.

During pregnancy and lactation

Not prescribed for pregnant and lactating women. Diazepam has the ability to penetrate the placental barrier and into breast milk. If pregnancy is suspected during therapy, it is recommended to immediately stop taking the medication.

In childhood

Prescribed from the age of 5 weeks from birth. Preference is given to using the product in the form of a solution, because It is extremely difficult to calculate a dosage of 1-1.5 mg when using a tablet with 5 mg of the active substance.

In old age

The dosage when treating elderly patients is always adjusted to a reduction. When taking standard dosages, the risks of adverse symptoms increase. Disorientation often occurs.

For liver dysfunction

Individual dose adjustment is required.

For impaired renal function

The amount of medication is adjusted downward.

Side effects

Common side effects when using Relium: weakness and drowsiness, muscle weakness, fatigue. Such negative reactions are temporary and disappear on their own after several doses of the medication.

Heart and blood vessels: development of bradycardia, pain in the heart area, arterial hypotension. Rarely: development of heart failure, including cardiac arrest.

Central nervous system: attacks of headaches, possibly increased dizziness, tremors, increased anger, irritability and aggression, impaired speech.

Mental disorders: increased anxiety, excessive emotional arousal, delusional states, frequent nightmares at night. In children and the elderly: changes in behavior that indicate immediate discontinuation of use.

Paradoxical reactions: agitation, aggression, psychosis, hallucinations. If paradoxical reactions develop, the medication must be discontinued immediately.

Allergic reactions: skin rash, urticaria.

Effect on driving

During the first 3 days from the start of taking Relium, when there is a high probability of developing temporary side effects such as dizziness and decreased concentration, it is recommended to refrain from driving.

Overdose

Taking an excessive amount of medication at one time leads to symptoms such as severe fatigue and nystagmus. Possible suppression of reflexes. Other signs of overdose: apnea, arterial hypotension. In some patients, an overdose provokes the development of conditions that pose a threat to life.

Treatment of overdose is the prescription of medications from the group of enterosorbents. Gastric lavage is not performed as an emergency measure for an overdose of Diazepam.

Drug interactions

The medication has an inhibitory effect on antipsychotics, narcotic analgesics, and antidepressants.

The simultaneous use of narcotic analgesics and Relium increases the feeling of euphoria.

The percentage of absorption of components decreases when used simultaneously with antacids.

Alcohol compatibility

Drinking alcoholic beverages during the entire therapy and the next 3 days after the end of treatment is prohibited.

Conditions for dispensing from pharmacies

On prescription.

Price

From 27 to 32 rubles.

Storage conditions

The temperature should not exceed 25°C, in a place where the sun's rays do not reach. The shelf life is 3 years; further use of the medicine is not recommended.

Analogs

Medicines with a similar spectrum of action: Diazepam, Sibazon, Diazepex.

Relium, international name, is a general sedative. Effective in the fight against, fights insomnia.

Relaxes muscles after exercise, relieves nervous tension, anxiety and others. However, the drug can cause addiction.

Composition of the product

Relium is sold in the form of a solution and film-coated tablets. They belong to the group of benzodiazepines. Widely used in traditional medicine to treat neurological diseases.

One package contains 20 tablets of 5 mg. In addition to the main active ingredient diazepam, the product contains: gelatin, potato starch, talc, Tween 80, lactose, magnesium stearate.

There are packages of 24 tablets of 5 or 10 mg. Also available in the form of a solution for intramuscular and intravenous administration, 10 mg each ampoule.

pharmachologic effect

The medicine has anxiolytic, sedative, hypnotic, anticonvulsant and muscle relaxant effects on the body.

All these effects occur due to the unique chemical composition of the product. Benzodiazepines, which are included in the chemical composition of the drug, have a positive effect on the central nervous system, due to which various nervous disorders can be effectively treated.

The anxiolytic effect occurs due to the drug’s effect on the limbic system of the brain. As a result, the patient gets rid of spontaneous feelings of fear, anxiety, and excessive worry. Emotional stress is relieved.

Relium also affects the reticular formation of the brain. This structure activates the cerebral cortex and controls the reflex function of the spinal cord. Therefore, when using the medicine, neurotic sensations such as fears and anxiety decrease. This is the sedative effect of the drug.

Manifests itself in the form of a warning about the next one. Although the next attack can be stopped thanks to the drug, the focus of epilepsy in the brain remains in an excited state.

The muscle relaxant effect on the body is due to the effect of the drug on neurons and axons of the spinal cord. In this case, the spinal cord is inhibited, resulting in inhibition of muscles and motor nerves.

Relium can lower blood pressure, dilate coronary vessels, increase sensitivity to pain, reduce gastric acid secretion and suppress vestibular paroxysms.

The effect can be felt on the 7th day of treatment. But the drug does not affect the occurrence of acute delusional, hallucinatory, and affective disorders.

The use of Relium weakens the feeling of agitation and negativism.

In people with cardialgia or arrhythmia, by the end of the first week a positive therapeutic effect from taking the medication may be observed.

Pharmacokinetic properties

After consumption, the main active ingredient of the drug diazepam quickly dissolves in the digestive tract and is absorbed into the body.

It quickly enters into a chemical reaction with blood proteins and spreads throughout the body. It is deposited in adipose tissue, then gradually released and released back into the blood.

The period of elimination from the body ranges from 24 to 48 hours. The elimination process may be longer in infants and older people. It is excreted along with urine in the form of metabolites. Regular consumption can ensure the accumulation of metabolites in the body.

Scope of application

And also for those people who:

Regimen and prescribed dosages

Depending on the type of disease, the patient’s health status, sensitivity to the drug, the dosage is prescribed and selected by the attending physician.

Relium is taken orally, administered intravenously or intramuscularly, the instructions indicate the following dosages depending on the purpose of taking the drug:

Overdose and side effects of the drug

Using the drug in excess of the recommended dose before the prescribed period is not advisable. Otherwise, side effects may occur.

During treatment with this drug, you should be extremely careful when performing actions and work that require increased concentration and motor speed. Among others, driving a car.

Like any other medicine in this group, Relium can cause side effects that occur mainly at the beginning of the course of treatment. Among other things, you may experience:

Alcohol and Relanium - what, how and why?

Different medications interact with alcohol differently. The alcohol contained in alcoholic beverages can enhance, minimize, and sometimes even counteract the effects of taking medications.

Many patients wonder whether it is possible to use Relium with alcohol? Champagne and similar drinks enhance the effect of the drug on the body. However, after drinking alcohol, the patient develops physical and mental dependence on this medicine.

In some cases, alcohol increases the toxicity of diazepam, which can adversely affect the central nervous system or be fatal.

But on the other hand, if diazepam is used by people with alcohol dependence, it can dull feelings such as nervousness, restlessness, anxiety, fear, tremor, etc.

Special patients, special instructions

Relium is not contraindicated for patients with impaired renal and liver function. But the dose for them should be reduced. The attending physician, depending on the patient’s condition and the severity of kidney and liver disease, individually prescribes the required dose.

If you use the drug with antipsychotic, sedative, opioid drugs, as well as with sleeping pills, anesthesia, a negative effect may occur: arterial hypotension, a depressant effect on the nervous and respiratory systems. Therefore, the use of the drug with other types of medications is decided by the attending physician.

Catad_pgroup Anxiolytics (tranquilizers)

Relanium - instructions for use

Registration number:

Trade name of the drug:

International nonproprietary name:

Chemical name:

Dosage form:

Compound:

Composition 1 ml:
active substance: Diazepam 5 mg.
Excipients: propylene glycol 450.0 mg, ethanol 96% 100.0 mg, benzyl alcohol 15.0 mg, sodium benzoate 48.8 mg, glacial acetic acid 2.3 mg, acetic acid 10% to pH approx. 6.3 - 6.4, water for injection up to 1 ml.
2 ml ampoule contains 10 mg diazepam

Description:

Transparent, colorless or yellow-green liquid.

Pharmacotherapeutic group:

Anxiolytic (tranquilizer).

ATX code:

Pharmacological properties

Pharmacodynamics
Diazepam has a depressant effect on the central nervous system (CNS), occurring primarily in the thalamus, hypothalamus and limbic system. Enhances the inhibitory effect of gamma-aminobutyric acid (GABA), which is one of the main mediators of pre- and postsynaptic inhibition of the transmission of nerve impulses in the central nervous system.
It has anxiolytic, sedative, hypnotic, muscle relaxant and anticonvulsant effects. The mechanism of action of diazepam is determined by stimulation of benzodiazepine receptors of the supramolecular GABA-benzodiazepine-chlorionophore receptor complex, leading to activation of the GABA receptor, causing a decrease in the excitability of the subcortical structures of the brain, inhibition of polysynaptic spinal reflexes.

Pharmacokinetics
When administered intramuscularly, absorption of diazepam may be slow and variable (depending on the site of administration); when administered into the deltoid muscle, absorption is rapid and complete. Bioavailability -90%. Maximum concentrations in blood plasma are achieved after 0.5 -1.5 hours with intramuscular administration (hereinafter referred to as IM) and within 0.25 hours with intravenous (hereinafter referred to as IV); equilibrium concentrations are achieved with continuous use after 1-2 weeks.
Diazepam and its metabolites penetrate the blood-brain and placental barriers and are found in breast milk in concentrations corresponding to 1/10 of plasma concentrations. Communication with plasma proteins - 98%. Metabolized in the liver with the participation of the enzyme system CYP2C19, CYP3A4, CYP3A5 and CYP3A7 98-99% to pharmacologically very active derivatives (desmethyldiazepam) and less active ones (temazepam and oxazepam).
Excreted by the kidneys - 70% (in the form of glucuronides), unchanged - 1-2% and less than 10% - with feces. The half-life (T½) of desmethyldiazepam is 30-100 hours, temazepam - 9.5-12.4 hours and oxazepam -5-15 hours.
T½ can be prolonged in newborns (up to 30 hours), elderly and senile patients (up to 100 hours) and in patients with hepatic-renal failure (up to 4 days).
With repeated use, the accumulation of diazepam and its active metabolites is significant.
Refers to benzodiazepines with a long T½, elimination after cessation of treatment is slow, because metabolites remain in the blood for several days or even weeks.

Indications for use

• treatment of neurotic and neurosis-like disorders with anxiety.
• relief of psychomotor agitation associated with anxiety;
• relief of epileptic seizures and convulsive states of various etiologies. Used for conditions accompanied by increased muscle tone (tetanus, acute cerebrovascular accidents, etc.);
• relief of withdrawal syndrome and delirium in alcoholism;
• also used for premedication and ataralgesia in combination with analgesics and other neurotropic drugs in various diagnostic procedures, in surgical and obstetric practice;
• in the clinic of internal diseases: in the complex therapy of hypertension (accompanied by anxiety, increased excitability), hypertensive crisis, vascular spasms, menopausal and menstrual disorders.

Contraindications

Hypersensitivity to benzodiazepine derivatives, severe myasthenia gravis, coma, shock, angle-closure glaucoma, history of addiction (drugs, alcohol, with the exception of treatment of alcohol withdrawal syndrome and delirium), sleep apnea syndrome, alcohol intoxication of varying degrees of severity, acute drug intoxication drugs that have a depressant effect on the central nervous system (narcotic, hypnotic and psychotropic drugs), severe chronic obstructive pulmonary diseases (risk of progression of respiratory failure), acute respiratory failure, children up to 30 days inclusive, pregnancy (especially the 1st and 3rd trimester), breastfeeding feeding.
Carefully- absence seizure (petit mal) or Lennox-Gastaut syndrome (when administered intravenously, it can provoke the development of tonic status epilepticus); epilepsy or a history of epileptic seizures (initiation of treatment with diazepam or its abrupt withdrawal may accelerate the development of seizures or status epilepticus), liver and/or renal failure, cerebral and spinal ataxia, hyperkinesis, tendency to abuse psychotropic drugs, organic brain diseases (paradoxical ones are possible reactions), hypoproteinemia, old age, depression (see “Special Instructions”).

Directions for use and doses

Relief of psychomotor agitation associated with anxiety and fear: an initial dose of 5-10 mg is administered slowly intravenously (IV); the dose can be repeated after 3-4 hours.
Condition of increased muscle tension and tetanus: dose for adults: first, 10 mg is administered in a slow intravenous injection or deep intramuscular (IM), and then 100 mg of diazepam is injected intravenously in 500 ml of 0.9% sodium chloride solution or 5% glucose solution with at a rate of 5-15 mg per hour.
For status epilepticus: prescribed IM or IV 10-20 mg, if necessary, repeat the dose after 3-4 hours.
For premedication (relieving skeletal muscle spasms): 10 mg IM 1-2 hours before surgery.
In obstetrics: 10-20 mg is prescribed intramuscularly when the cervix is ​​dilated by 2-3 fingers.
Newborns are prescribed after the 5th week of life (over 30 days) IV slowly at 0.1-0.3 mg/kg body weight up to a maximum dose of 5 mg, if necessary, injections are repeated after 2-4 hours (depending on clinical symptoms).
Children aged 5 years and older: IV slowly 1 mg every 2-5 minutes up to a maximum dose of 10 mg; if necessary, treatment can be repeated after 2-4 hours.

Side effect

From the nervous system: at the beginning of treatment (especially in elderly patients) - drowsiness, dizziness, increased fatigue, impaired concentration, ataxia, disorientation, dulling of emotions, slowing of mental and motor reactions, anterograde amnesia (develops more often than when taking other benzodiazepines); rarely - headache, euphoria, depression, tremor, catalepsy, confusion, dystonic extrapyramidal reactions (uncontrolled body movements), asthenia, muscle weakness, hyporeflexia, dysarthria; extremely rarely - paradoxical reactions (aggressive outbursts, psychomotor agitation, fear, suicidal tendencies, muscle spasms, confusion, hallucinations, anxiety, sleep disturbances).
From the hematopoietic organs: leukopenia, neutropenia, agranulocytosis (chills, pyrexia, sore throat, unusual fatigue or weakness), anemia, thrombocytopenia.
From the digestive system: dry mouth or hypersalivation, heartburn, hiccups, gastralgia, nausea, vomiting, loss of appetite, constipation; liver dysfunction, increased activity of liver transaminases and alkaline phosphatase, jaundice.
From the cardiovascular system: palpitations, tachycardia, decreased blood pressure (hereinafter referred to as blood pressure).
From the genitourinary system: urinary incontinence or retention, renal dysfunction, increased or decreased libido, dysmenorrhea.
Allergic reactions: skin rash, itching.
Effect on the fetus: teratogenicity (especially the first trimester), central nervous system depression, respiratory impairment and suppression of the sucking reflex in newborns whose mothers used the drug.
Local reactions: at the injection site - phlebitis or venous thrombosis (redness, swelling, or pain at the injection site).
Other: addiction, drug dependence; rarely - depression of the respiratory center, visual impairment (diplopia), bulimia, weight loss.
If you sharply reduce the dose or stop taking it- “withdrawal” syndrome (increased irritability, headache, anxiety, fear, psychomotor agitation, sleep disturbances, dysphoria, spasm of smooth muscles of internal organs and skeletal muscles, depersonalization, increased sweating, depression, nausea, vomiting, tremor, perception disorders, etc. including hyperacusis, paresthesia, photophobia, tachycardia, convulsions, hallucinations, rarely - psychotic disorders). When used in obstetrics - in newborns - muscle hypotension, hypothermia, dyspnea.

Overdose

Symptoms: drowsiness, depression of consciousness of varying severity, paradoxical excitation, decreased reflexes to areflexia, decreased response to painful stimuli, dysarthria, ataxia, visual impairment (nystagmus), tremor, bradycardia, decreased blood pressure, collapse, cardiac and respiratory depression (up to apnea) activity, coma.
Treatment: gastric lavage, forced diuresis, intake of activated charcoal. Symptomatic therapy (maintaining breathing and blood pressure), artificial ventilation. Flumazenil is used as a specific antagonist (in a hospital setting). Hemodialysis is ineffective. The benzodiazepine antagonist flumazenil is not indicated in patients with epilepsy who have been treated with benzodiazepines. In such patients, the antagonistic effect towards benzodiazepines can provoke the development of epileptic seizures.

Interaction with other drugs

When using Relanium together with other drugs, the following interaction reactions may occur:

• with monoamine oxidase inhibitors, strychnine and corazole - antagonism regarding the effects of Relanium;
• with sleeping pills, sedatives, narcotic analgesics, other tranquilizers, benzodiazepine derivatives, muscle relaxants, general anesthesia, antidepressants, antipsychotics, alcohol - a sharp increase in the inhibitory effect on the central nervous system;
• with cimetidine, disulfiram, erythromycin, fluoxetine, as well as with oral contraceptives and estrogen-containing drugs that competitively inhibit metabolism in the liver (oxidation processes) - it is possible to slow down the metabolism of Relanium and increase its plasma concentration;
• isoniazid, ketoconazole and metoprolol also slow down the metabolism of Relanium and increase its concentration in the blood plasma;
• propranolol and valproic acid increase the level of Relanium in the blood plasma;
• rifampicin can increase the metabolism of Relanium and, as a result, reduce its concentration in the blood plasma;
• inducers of microsomal liver enzymes - reduce effectiveness;
• narcotic analgesics enhance the inhibitory effect on the central nervous system;
• antihypertensive drugs may increase the severity of the decrease in blood pressure;
• clozapine - possible increased respiratory depression;
• when used simultaneously with cardiac glycosides, it is possible to increase the concentration of the latter in the blood serum and develop digitalis intoxication (as a result of competitive interaction with plasma proteins);
• reduces the effectiveness of levodopa in patients with parkinsonism;
• omeprazole prolongs the elimination time of diazepam;
• monoamine oxidase inhibitors (MAOIs), respiratory analeptics, psychostimulants - reduce the activity of the drug.
• Potentially increased toxicity of zidovudine;
• theophylline (used in low doses) may reduce sedation.

Pharmaceutically incompatible in the same syringe with other drugs.
Premedication with diazepam reduces the dose of fentanyl required for induction of general anesthesia and shortens the time of onset of general anesthesia.

special instructions

Particular caution is required when prescribing diazepam for severe depression, because the drug can be used to realize suicidal intentions. An IV solution of diazepam must be administered slowly into a large vein, at least over 1 minute for every 5 mg (1 ml) of the drug. It is not recommended to carry out continuous intravenous infusions - sedimentation and adsorption of the drug by polyvinyl chloride materials of infusion balloons and tubes is possible.
In case of renal/liver failure and long-term treatment, monitoring of the peripheral blood picture and liver enzymes is necessary.
The risk of developing drug dependence increases when using large doses, a significant duration of treatment, and in patients who have previously abused alcohol or drugs. Should not be used for a long time without special instructions. Abrupt cessation of treatment is unacceptable due to the risk of “withdrawal syndrome”, however, due to the slow half-life of diazepam, its manifestation is much less pronounced than that of other benzodiazepines.
If patients experience such unusual reactions as increased aggressiveness, psychomotor agitation, anxiety, fear, thoughts of suicide, hallucinations, increased muscle cramps, difficulty falling asleep, shallow sleep, treatment should be stopped.
Initiation of treatment with diazepam or its abrupt withdrawal in patients with epilepsy or a history of epileptic seizures may accelerate the development of seizures or status epilepticus.
It has a toxic effect on the fetus and increases the risk of birth defects when used in the first trimester of pregnancy. Taking therapeutic doses later in pregnancy may cause depression of the fetal central nervous system. Chronic use during pregnancy can lead to physical dependence - possible withdrawal symptoms in the newborn.
Children, especially young children, are very sensitive to the CNS depressant effects of benzodiazepines. It is not recommended for newborns to be prescribed drugs containing benzyl alcohol - the development of a toxic syndrome, manifested by metabolic acidosis, central nervous system depression, difficulty breathing, renal failure, hypotension and possibly epileptic seizures, as well as intracranial hemorrhage, is possible.
Use in doses above 30 mg within 15 hours before or during childbirth can cause respiratory depression in the newborn (before apnea), decreased muscle tone, decreased blood pressure, hypothermia, and weak sucking (the so-called “floppy baby syndrome”). Elderly patients should be prescribed Relanium with extreme caution and should not exceed recommended doses.
The risk-benefit ratio should be carefully assessed when prescribed to pregnant women, as well as patients with kidney and liver diseases.
Administration of Relanium into the arterial bed is contraindicated due to the possible development of gangrene.

Impact on the ability to drive vehicles and operate machinery

While taking Relanium, patients are not recommended to perform work that requires quick reaction and involves risk, for example, driving vehicles and performing other potentially hazardous activities.
During treatment with Relanium, alcohol intake is prohibited.

Release form

Solution for intravenous and intramuscular administration 5 mg/ml.
2 ml in ampoules made of colorless or orange glass for ampoules of the first hydrolytic class (Eur.F.). Above the break point of the ampoule there is a white or red dot, as well as a red ring-shaped strip.
5 ampoules are placed in a PVC holder with a protective colorless PET film. One holder, or two holders, or ten holders in a cardboard box along with instructions for use.

Storage conditions

List III of the List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.
Store at a temperature of 15°C-25°C. Protect from light.
Keep out of the reach of children.

Best before date

5 years.
Do not use after the expiration date stated on the package.

Vacation conditions

Prescription release.

Manufacturer

Warsaw Pharmaceutical Plant Polfa JSC
st. Karolkowa 22/24, 01-207 Warsaw, Poland.

Organization receiving consumer complaints
OJSC Chemical and Pharmaceutical Plant AKRIKHIN
142450, Moscow region,
Noginsky district, Staraya Kupavna, st. Kirova, 29