Diazepam (Diazepamum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Anxiolytics

Included in the formulation
  • Apaurin
    pills inwards 
    KRKA, dd, Novo mesto, AO    
  • Apaurin
    solution w / m in / in 
    KRKA, dd, Novo mesto, AO    
  • Relanium®
    solution w / m in / in 
    Pharmaceutical factory "POLFARMA" JSC     Poland
  • The Relium
    pills inwards 
    Tarkhominsky pharmaceutical factory "Polfa", A.O.     Poland
  • The Relium
    solution w / m in / in 
    Tarkhominsky pharmaceutical factory "Polfa", A.O.     Poland
  • Seduxen
    pills inwards 
    GEDEON RICHTER-RUS, CJSC     Russia
  • Sibazon
    pills inwards 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Sibazon
    pills inwards 
    ORGANICS, JSC     Russia
  • Sibazon
    solution w / m in / in 
    DALHIMFARM, OJSC     Russia
  • Sibazon
    solution w / m in / in 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    VED

    АТХ:

    N.05.B.A.01   Diazepam

    Pharmacodynamics:

    Anxiolytic group of benzodiazepines, has anxiolytic, sedative, miorelaxing, anticonvulsant action. Anxiolytic action is associated with increased GABA-ergic inhibition in the central nervous system. In complex GABAA-receptor - C1 ~ -channel contains a benzodiazepine receptor, the stimulation of which leads to conformational changes GABAA-receptor, resulting in increased its sensitivity to GABA.This leads to an increase in the permeability of the GABA channelA-receptor for chlorine ions. The ingress into the neuron of negatively charged chloride ions leads to hyperpolarization of the membrane and inhibition of neuronal activity.

    Anticonvulsant effect of diazepam is associated with the inhibition of epileptogenic activity due to the enhancement of inhibitory GABAergic processes in the central nervous system.

    Miorelaksiruyuschee action is associated with the inhibition of spinal polysynaptic reflexes and a violation of their supraspinal regulation.

    In small doses, it is sedative, with an increase - a hypnotic effect.

    With prolonged use, drug dependence is formed. After the end of taking the drug manifestations of withdrawal syndrome are possible.

    Pharmacokinetics:

    After oral administration, fasted to 75% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 90 minutes. The connection with plasma proteins is 98%. Deposited in adipose tissue. Penetrates through the blood-brain and placental barrier, enters the breast milk.

    Metabolism in the liver with the formation of active metabolites (desmethyldiazepam) with a half-elimination period of 40 to 200 hours.

    The half-life is 24-48 hours. Elimination of the drug by the kidneys.

    Indications:

    It is used for neurotic-like and neurotic states, accompanied by fear and anxiety. Used for premedication before surgery and for anesthesia. It is used to relieve the status epilepticus and for diseases manifested by increased muscle tone: epilepsy, schizophrenia, psychopathic agitation, specific personality disorders, insomnia.

    ICD-10

    I.A30-A49.A35   Other forms of tetanus

    V.F10-F19.F10.3   Mental and behavioral disorders caused by alcohol use - withdrawal symptoms

    V.F40-F48.F40   Phobic anxiety disorders

    V.F40-F48.F43   Reaction to severe stress and adaptation disorders

    V.F40-F48.F45.3   Somatoform dysfunction of the autonomic nervous system

    V.F40-F48.F48.0   Neurasthenia

    V.F50-F59.F51.2   Sleep and wakefulness disorder inorganic etiology

    VI.G40-G47.G41   Epileptic status

    XV.O30-O48.O45   Premature detachment of the placenta [abruptio placentae]

    XV.O60-O75.O60   Premature birth

    XV.O60-O75.O62   Violations of labor [of the clan]

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Hepatic and renal failure, angle-closure glaucoma, myasthenia gravis, pregnancy, individual intolerance.

    Carefully:

    Kidney and liver diseases, chronic respiratory failure, sleep apnea syndrome, age up to six months - according to vital indications and only in a hospital.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Use in children

    Inside to 0.1-0.3 mg / kg per day.

    Adults

    The initial dose of 5-10 mg, daily: 5-20 mg.

    The highest daily dose: 100 mg.

    The highest single dose: 10 mg.

    Side effects:

    Central and peripheral nervous system: drowsiness, lethargy, ataxia, dullness of emotions, tremor, dysarthria, confusion, dizziness, hallucinations, inadequate behavior, anterograde amnesia.

    Respiratory system: possible respiratory failure with intravenous administration of the drug.

    The system of hematopoiesis: neutropenia.

    The cardiovascular system: bradycardia, hypotension.

    Digestive system: nausea, constipation, dry mouth.

    Dermatological reactions: soreness and erythema with intramuscular injection.

    Sense organs: nystagmus, diplopia.

    Reproductive system: increased or decreased libido.

    Allergic reactions.

    Overdose:

    Oppression of the central nervous system from drowsiness to coma, decreased muscle tone, confusion, ataxia, respiratory depression, hypotension.

    Antidote - flumazenil, is used in a hospital. Treatment is symptomatic. Hemodialysis is ineffective.

    Interaction:

    Simultaneous use of cimetidine reduces the clearance of diazepam.

    Disrupts the metabolism of phenytoin.

    Potentiates the effects of neuroleptics, tranquilizers, hypnotics, anticonvulsants, analgesics and anesthetics.

    Incompatible with alcohol.

    Special instructions:

    When parenteral administration is not recommended to mix the drug with other solutions, because there is a fallout of the active substance in the sediment.

    When treating diazepam, patients are not advised to drive and work with moving machinery.

    It is recommended to smoothly cancel the drug in order to avoid recoil syndrome. With prolonged admission, drug dependence develops. Cases of benzodiazepine addiction have been noted.

    Instructions
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