Diazepam is a drug with anxiolytic, hypnotic, anticonvulsant, sedative and central muscle relaxant effects. Diazepam lowers the severity of emotional stress, reduces anxiety, and also lowers increased muscle tone. The effect of the drug is based on its ability to enhance the central effect of gamma-aminobutyric acid (one of the inhibitory mediators of the central nervous system) on the receptors of the reticular formation of the brain column. Diazepam leads to a decrease in excitation of the cerebral cortex, hypothalamus, thalamus and limbic system. Diazepam has a muscle relaxant effect due to the slowing down of postsynaptic spinal reflexes.
With alcohol withdrawal, diazepam helps to reduce the severity of the acute state of agitation, tremor, acute alcoholic delirium, hallucinations and negativism.
With constant administration, the effect of the drug is enhanced due to the mellen excretion and, as a result, the accumulation of diazepam in the tissues.
The initial levels of diazepam decrease quite rapidly within 6 hours, after which the decline in plasma concentrations slows down. The half-life of diazepam ranges from 20 to 70 hours, depending on the individual characteristics of patients.
Diazepam is metabolized in the liver with the formation of active substances (the main metabolite N-desmethyldiazepam is determined in plasma 24-36 hours after drug administration).
Diazepam and its metabolites are excreted mainly by the kidneys.

Indications for use

Diazepam in the form of a parenteral solution is used to treat patients with acute neuropsychic stress, which is accompanied by insomnia, tension, anxiety and fear.
Diazepam is used to treat patients with epilepsy, severe emotional manifestations and spastic paralysis.
Diazepam may also be prescribed for alcohol withdrawal and delirium tremens.

Mode of application

Diazepam solution is intended for parenteral use. The drug is administered intravenously or intramuscularly. Intravenous Diazepam is allowed to be administered drip and jet. Intramuscularly, it is suggested to inject only into large muscles (in particular, the gluteal muscle), observing the rules for intramuscular administration of solutions. The duration of therapy and dosage of the drug Diazepam is determined by the doctor individually.
Adults with diseases that are accompanied by severe psychomotor agitation and convulsions, as well as for the relief of epileptic seizures, are mainly prescribed the introduction of 10 mg of diazepam (2 ml of Diazepam 0.5%) up to 3 times a day.
The highest recommended single dosage of diazepam is 30 mg, the highest daily dosage is 70 mg. With epileptic status, a single dosage of diazepam can be increased to 40 mg. If necessary, in patients with status epilepticus, injections are repeated every 3-4 hours, but not more than 4 times a day.
A sedative result develops within a few minutes after intravenous administration of diazepam and within 30-40 minutes after intramuscular administration.
The recommended duration of therapy is 3 to 10 days.
After stopping the acute symptoms of the disease, it is proposed to continue therapy with the oral form of diazepam.
Recommended dosage for children:
With febrile convulsions, children 1-6 years old are mainly prescribed the introduction of 2-5 mg of diazepam per day.
With febrile convulsions, children aged 6-14 years are mainly prescribed the introduction of 5-10 mg of diazepam per day.
Children are encouraged to inject diazepam solution intravenously slowly.
After prolonged therapy, the withdrawal of Diazepam should be carried out gradually.

Side effects

Diazepam is often well tolerated by patients. In some cases, when using Diazepam, patients are likely to develop drowsiness, dizziness, lethargy, myasthenia gravis, and skin allergic reactions.
With prolonged use of the drug Diazepam, the development of drug dependence is likely.
With intravenous administration of Diazepam, local inflammatory reactions may develop; in order to prevent this undesirable effect, it is proposed to change the injection site with each injection.

Contraindications

Diazepam is not prescribed to patients with a history of intolerance reactions to the components of the solution, as well as drugs of the benzodiazepine group.
Diazepam is not used in the treatment of patients with myasthenia gravis and glaucoma.
Diazepam should not be used in patients with occupational limitations.
Diazepam is not prescribed to patients with alcoholism (with the exception of cases of alcohol withdrawal and alcoholic delirium).
Diazepam solution in pediatric practice is used only for the treatment of children older than 1 year.
Caution should be exercised when prescribing diazepam to patients at increased risk of developing drug dependence.
Potentially unsafe activities should be avoided during diazepam therapy.

Pregnancy

Diazepam is not used during pregnancy. According to vital indications, Diazepam can be used during pregnancy under the supervision of a physician for a minimum period of time and in the minimum effective doses.
If it is necessary to regularly use the drug Diazepam during lactation, it is necessary to decide on the termination of breastfeeding of the child.

Interaction with other drugs

Do not mix Diazepam solution in the same syringe with other medicines.
Diazepam potentiates the effects of barbiturates, phenothiazines, monoamine oxidase inhibitors, and other psychotropic drugs.
Drugs that depress the central nervous system, including hypnotics, sedatives, analgesics, antipsychotics and anesthetics, as well as antidepressants, potentiate the inhibitory effect of diazepam on the central nervous system.

Overdose

When using excessive doses of Diazepam, patients are likely to develop drowsiness, dysarthria, myasthenia gravis, and paradoxical arousal. With a further increase in dosage, patients developed a decrease in reflexes, loss of consciousness and coma. A lethal outcome with an overdose of diazepam is unlikely, but the risk increases significantly when using excessive doses of diazepam in combination with ethyl alcohol and other substances that potentiate the effects of benzodiazepines.
With an overdose of Diazepam, the development of arterial hypotension, respiratory depression and paradoxical reactions, including sleep disturbances, hallucinations and arousal, is also likely.
In case of an overdose of Diazepam, supportive therapy and constant monitoring of the patient's condition are prescribed. If necessary, use stimulants of the central nervous system and cardiovascular agents.

Release form

Solution for parenteral use Diazepam 2 ml in ampoules, 10 ampoules placed in blister packs are placed in a cardboard box.

Storage conditions

Diazepam in the form of a solution for parenteral use should be stored in rooms that maintain a temperature regime of 8 to 25 degrees Celsius.
The shelf life of Diazepam is 2 years.

Synonyms

Sibazone injection 0.5%.

Compound

2 ml of Diazepam (1 ampoule) contains:
Diazepam - 10 mg;
Additional substances.

A tranquilizer of the benzodiazepine group, it has an anxiolytic, sedative, muscle relaxant and anticonvulsant effect, potentiating the effects of the GABAergic system by stimulating the central action of GABA, the main inhibitory mediator of the brain. Benzodiazepine derivatives act in the same way as benzodiazepine receptor agonists, which form a component of a functional supramolecular unit known as the benzodiazepine-GABA-chlorionophore receptor complex, located on the neuron membrane.
Due to the selective stimulating effect on GABA receptors in the ascending reticular formation of the brain stem, it reduces the excitation of the cortex, limbic region, thalamus and hypothalamus and has an anxiolytic and sedative-hypnotic effect. Due to the inhibitory effect on polysynaptic spinal reflexes, it has a muscle relaxant effect.
Diazepam is quickly and completely absorbed in the digestive tract; The maximum plasma concentration is reached 30-90 minutes after ingestion. After an intramuscular injection, it is also completely absorbed, although this process is not always faster than after oral administration. The elimination curve of diazepam has a biphasic character: an initial phase of rapid and extensive distribution with a half-life of up to 3 hours is followed by a long terminal phase of elimination (with a half-life of up to 48 hours). Diazepam is metabolized to the pharmacologically active nordiazepam (half-life 96 hours), hydroxydiazepam and oxazepam. Diazepam and its metabolites bind to plasma proteins (98% diazepam); excreted mainly in the urine (about 70%) in the form of free or conjugated metabolites.
The half-life may increase in newborns, elderly and senile patients and in patients with liver or kidney disease; at the same time, a longer time may be required to achieve an equilibrium concentration in the blood plasma. Diazepam and its metabolites pass through the BBB and the placental barrier. They are also found in breast milk at a concentration of approximately 1/10 of the concentration in maternal plasma.

Indications for the use of the drug Diazepam

Inside for the symptomatic treatment of patients in a state of anxiety (may be manifested by a pronounced anxious mood, behavior and / or its functional, vegetative or motor equivalents - palpitations, excessive sweating, insomnia, tremors, anxiety, etc.), agitation and tension in neurosis and transient reactive states; as an aid in severe mental and organic disorders.
Used parenterally to provide a sedative effect before stressful medical or diagnostic procedures such as electrical impulse therapy, cardiac catheterization, endoscopy, certain x-ray examinations, small volume surgeries, reduction of dislocations and reposition of bones in fractures, biopsy, burn wound dressing, etc .; to eliminate anxiety, fear, prevent acute stress; for premedication before surgery in patients experiencing a feeling of fear or tension; in psychiatry to eliminate the state of excitation associated with acute anxiety and panic, as well as motor agitation, paranoid-hallucinatory states, alcoholic delirium; for the emergency treatment of status epilepticus and other convulsive conditions (tetanus, eclampsia); in order to facilitate the course of the first stage of childbirth.
Both routes of administration are used to eliminate reflex muscle spasms in case of local damage (trauma, wound, inflammation); as an effective adjuvant for the relief of spastic conditions caused by damage to the spinal and supraspinal intermediate neurons (for example, with cerebral palsy and paraplegia, with athetosis and stiffness syndrome).

The use of the drug Diazepam

To achieve the optimal effect, the dose is selected individually. The usual oral dose for adults is 5-20 mg/day, depending on the severity of the symptoms. A single oral dose should not exceed 10 mg.
In urgent cases or in life-threatening conditions, as well as with insufficient effect from oral administration, parenteral administration of diazepam in higher doses is possible.
Treatment of anxiety conditions is usually carried out for several weeks, depending on the type of pathology and etiological factors. Positive clinical dynamics is observed within 6 weeks from the start of the use of diazepam; in the future, maintenance therapy is usually carried out. Systematic clinical studies of the effectiveness of long-term (more than 6 months) use of diazepam have not been conducted. In elderly and senile patients, oral treatment should begin with half the usual adult dose, gradually increasing it depending on need and tolerability.
Children are prescribed orally at a dose of 0.1-0.3 mg / kg / day.
In diseases of the kidneys or liver, the dose should be selected individually.
To achieve a sedative effect with the preservation of consciousness, before carrying out stressful procedures, adults are injected intravenously with 10-30 mg, children - 0.1-0.2 mg / kg of body weight. The initial dose is 5 mg (children - 0.1 mg / kg), then re-introduced every 30 seconds at a dose 50% higher than the initial one.
For premedication, adults are injected intramuscularly with 10-20 mg, children - 0.1-0.2 mg/kg 1 hour before induction of anesthesia; induction anesthesia - 0.2-0.5 mg / kg is injected intravenously.
In states of excitation (acute anxiety states, motor agitation, alcoholic delirium), the initial dose is 0.1-0.2 mg / kg IM or IV every 8 hours until the severity of acute symptoms decreases; maintenance therapy is carried out by oral administration.
In case of status epilepticus, it is administered intravenously in a stream every 10-15 minutes or in / in a drip of 0.15-0.25 mg / kg; the highest daily dose is 3 mg/kg.
With tetanus - 0.1-0.3 mg / kg IV every 1-4 hours. Diazepam can be administered intravenously by drip or through a gastric tube (3-4 mg / kg per day).
In the case of muscle spasm (with injuries, spinal and supraspinal paralysis), diazepam is used in the same doses as for achieving a sedative effect while maintaining consciousness.
With preeclampsia and eclampsia, 10-20 mg is administered intravenously; if necessary, prescribe an additional injection of intravenous jet or drip (the highest daily dose is 100 mg).
To facilitate labor activity - 10-20 mg intramuscularly (in the presence of pronounced excitation - intravenously) with the opening of the cervix by 2-3 fingers.

Contraindications to the use of the drug Diazepam

Hypersensitivity to benzodiazepines in history; alcohol dependence (with the exception of the treatment of acute withdrawal symptoms); severe form of chronic hypercapnia, severe liver failure.

Side effects of diazepam

Most often - lethargy, drowsiness and muscle weakness (usually depends on the dose); rarely - confusion, constipation, depression, dullness of emotions, decreased attention, diplopia, dysarthria, headache, arterial hypotension, urinary incontinence, increased or decreased sexual desire, nausea, xerostomia or increased salivation, skin rash, slurred speech, tremor, delay urine, headache, dizziness, blurred vision; very rarely - increased activity of transaminases and alkaline phosphatase, as well as jaundice.
Paradoxical reactions such as acute agitation, anxiety, sleep disturbances, and hallucinations have been described; when they appear, diazepam should be discontinued.
With parenteral use - thrombosis and thrombophlebitis, local irritation (especially after rapid intravenous administration). Diazepam solution should not be injected into very small veins; it is unacceptable to / and the introduction and ingress of the solution into the adjacent tissues. IM injections may be accompanied by soreness and erythema.

Special instructions for the use of the drug Diazepam

The use of benzodiazepine derivatives and similar drugs can lead to the formation of physical and mental dependence, the risk of which increases with high doses and prolonged treatment. It also increases in patients with a burdened history (abuse of alcohol and drugs). Individuals taking diazepam at recommended doses are less likely to develop physical dependence. Abrupt withdrawal of diazepam after prolonged use may cause withdrawal symptoms (headache and myalgia, severe anxiety, tension, restlessness, confusion and irritability). In severe cases, the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling in the limbs, light, sound and tactile hypersensitivity, hallucinations and epileptic seizures. Therefore, the dose of diazepam is recommended to be reduced gradually.
When prescribing diazepam to patients with severe pseudoparalytic myasthenia gravis, their muscle weakness should be taken into account.
Use with caution in heart and respiratory failure, since sedatives can aggravate respiratory depression; however, sedation may be beneficial for some patients as it reduces respiratory effort.
As in the case of the use of other psychotropic drugs, the dose of diazepam should be selected taking into account individual tolerability in patients with organic changes in the brain (especially atherosclerosis) or with heart and respiratory failure. As a rule, diazepam should not be administered parenterally to such patients.
It is necessary to warn patients against drinking alcohol while taking diazepam, since this combination can potentiate the negative effect of each of them.
Before prescribing diazepam during pregnancy, it is necessary to compare the expected therapeutic effect for the mother and the potential harm to the fetus. It should be borne in mind that in newborns, the enzyme system involved in the metabolism of diazepam is underdeveloped (especially in preterm infants) and that diazepam and its metabolites pass through the placental barrier and penetrate into breast milk. Therefore, if possible, long-term use of diazepam during pregnancy and lactation should be avoided. The results of clinical observations indicate that the use of diazepam in obstetric practice is safe for the fetus.
Patients should refrain from driving and working with potentially dangerous mechanisms that require concentration and quick response.

Diazepam drug interactions

The simultaneous use of cimetidine (but not ranitidine) reduces the clearance of diazepam. There are also reports that diazepam interferes with the metabolism of phenytoin. There are no data on interaction with antidiabetic agents, anticoagulants and diuretics.
In the case of the combined use of diazepam and neuroleptics, tranquilizers, antidepressants, hypnotics, anticonvulsants, analgesics and anesthetics, mutual potentiation of effects is possible.
Diazepam in the form of a solution for injection should not be mixed in the same volume with other solutions, as this may lead to precipitation of the active substance.

Diazepam overdose, symptoms and treatment

It is manifested by a pronounced sedative effect, muscle weakness, deep sleep or paradoxical arousal. Intentional or accidental overdose of diazepam is rarely life-threatening. Significant overdose, especially when combined with other centrally acting agents, can cause coma, areflexia, cardiac and respiratory depression, and respiratory arrest.
Treatment - in most cases, only the control of vital signs is required. In case of severe overdose, appropriate measures are necessary (gastric lavage, mechanical ventilation, measures to maintain cardiovascular activity). The benzodiazepine antagonist flumazenil is recommended as a specific antidote.

List of pharmacies where you can buy Diazepam:

• St. Petersburg

Diazepam
Tranquilizers (anxiolytics) of the benzodiazepine series

Release form

Mechanism of action

Main Effects

Pharmacokinetics

Plasma protein binding of diazepam and its active metabolites is 95-98%. T1 / 2 in adults is 20-70 hours (diazepam), 30-100 hours (nordiazepam), 9.2-2.4 hours (temazepam), 5-15 hours (oxazepam). T1 / 2 may be prolonged in newborns, elderly patients, with liver diseases. Diazepam and its active metabolites cross the BBB, the placental barrier and can be secreted in breast milk. It is excreted mainly by the kidneys in the form of metabolites (70%) and the intestines (10%). With repeated use, accumulation of diazepam and its metabolites in the blood plasma is observed.

Indications

Dosage and administration

Inside: for premedication in adults at a dose of 5-10 mg 40-60 minutes before dental intervention. With course treatment, a single dose is 5-10 mg, a daily dose is 5-20 mg, on the eve of surgery in the evening - 10-20 mg.
The maximum single dose is 20 mg. The maximum daily dose is 60 mg.

With hypertonicity of masticatory muscles, 5 mg 2-3 times a day. Elderly and debilitated patients reduce the dose (usually 2.5 mg 1-2 times a day).

With intravenous and intramuscular administration, the average single dose for adults is 10-20 mg, the average daily dose is 30 mg, the maximum single dose is 30 mg, the maximum daily dose is 70 mg. The duration of treatment with injection of drugs should not exceed 3-5 days.

Children: at the age of 1-3 years - 1 mg 2 r / day, 3-7 years - 2 mg 3 r / day, over 7 years - 3-5 mg 2-3 r / day. The dose and duration of treatment in children are selected individually, depending on the indications, age and weight of the child.

Contraindications

Precautions, therapy control

Do not mix diazepam in the same syringe with other drugs.

During the period of treatment, one should refrain from driving vehicles, performing work that requires increased attention, speed of psychomotor reactions.

Benzodiazepines may reduce the analgesic effect of reflexology.

During the treatment period, the use of alcohol is unacceptable.

Prescribe with caution:
■ elderly and debilitated patients;
■ with heart, kidney and liver failure;
■ children under 6 months are used only for health reasons in a hospital.

Side effects

From the side of the central nervous system:
■ headache;
■ dizziness;
■ lethargy;
■ depression;
■ stunned;
■ muscle weakness;
■ increased fatigue;
■ tremor;
■ nystagmus;
■ blurred vision;
■ dysarthria, slurred speech;
■ diplopia;
■ dulling of emotions;
■ ataxia;
■ decrease in speed of reactions and concentration of attention;
■ drowsiness;
■ deterioration of short-term memory;
■ confusion;
■ fainting;
■ paradoxical reactions (excitement, anxiety, hallucinations, nightmares, fits of rage, inappropriate behavior);
■ anterograde amnesia.

From the genitourinary system:
■ incontinence or urinary retention;
■ decreased libido and potency;
■ violation of the menstrual cycle.

From the side of the cardiovascular system and the blood system:
■ bradycardia;
■ neutropenia.

Other effects:
■ drug dependence (with prolonged use);
■ allergic reactions. Local reactions:
■ phlebitis and thrombophlebitis at the injection site (with intravenous administration);
■ infiltrates at the injection site (for intramuscular injection).

Overdose

Treatment: drug withdrawal, gastric lavage (when diazepam is used orally), intravenous administration of a specific antagonist of benzodiazepine tranquilizers - flumazenil (aneksat), symptomatic supportive therapy.

Interaction

Synonyms

G.M. Barer, E.V. Zoryan