Clonazepam (Clonazepamum)

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

Antiepileptic agents

Included in the formulation
  • Clonazepam
    pills inwards 
    Remedika Co., Ltd.     Cyprus
  • Clonazepam
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    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.03.A.E.01   Clonazepam

    Pharmacodynamics:

    Stimulates the benzodiazepine GABA-receptors of the limbic system, the hypothalamus, the lateral intercalary neurons of the spinal cord and the ascending reticular formation. As a result, sensitivity to gamma-aminobutyric acid increases, which leads to to an increase in the frequency of opening channels of the membrane of neurons for chloride ions, which enhances the inhibitory effect of GABA. As a result, inhibits interneuronal transmission in the central nervous system.

    Has a pronounced anticonvulsant effect, as well as anxiolytic, sedative, myorelaxing and moderate hypnotic effect.

    Pharmacokinetics:

    After oral administration, up to 90% is absorbed in the gastrointestinal tract, after intramuscular administration - 93%. The maximum concentration in the blood plasma is achieved in 1-2 hours. The connection with plasma proteins is 85%.

    Penetrates through the blood-brain and placental barrier, excreted into breast milk. Metabolism in the liver.

    The half-life is 6-7 days. Elimination with feces and kidneys.

    Indications:

    It is used for the treatment of epilepsy, convulsive syndrome of any etiology. Used for psychomotor crisis, somnambulism, insomnia, panic disorder, alcoholic delirium.

    ICD-10

    V.F10-F19.F12.4   Mental and behavioral disorders caused by the use of cannabinoids - abstinent state with delirium

    V.F10-F19.F10.4   Mental and behavioral disorders caused by alcohol use - abstinent state with delirium

    V   Mental and behavioral disorders

    V.F40-F48.F41.0   Panic disorder [episodic paroxysmal anxiety]

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

    VI.G40-G47.G40   Epilepsy

    VI.G40-G47.G41   Epileptic status

    Contraindications:

    Myasthenia gravis, acute respiratory, renal and cardiac failure, shock, angle-closure glaucoma, pregnancy and lactation, individual intolerance.

    Carefully:

    Open-angle glaucoma, chronic alcoholism, chronic respiratory failure.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Use in children

    Inside, in accordance with age:

    Infants and children aged 1-5 years - 250 mcg per day;

    5-12 years - 500 mcg per day;

    12 years is the dose of adults.

    Intravenously slowly, to 0.5 mg.

    Adults

    Inside, 1 mg per day with a gradual increase to 20 mg per day for 3 doses.

    In panic disorders (only adults over 18 years) - 1 mg per day, the maximum dose - 4 mg per day.

    For supervising epileptic status - intravenously slowly 1 mg, if necessary, make repeated injections.

    The highest daily dose: 20 mg per day for oral administration; 13 mg for intravenous administration.

    Side effects:

    Central and peripheral nervous system: lethargy, drowsiness, dizziness, headache, anterograde amnesia, ataxia, hallucinations, delirium, paradoxical reactions: agitation, aggressiveness, psychomotor agitation.

    Respiratory system: bronchospasm, apnea with intravenous injection.

    The cardiovascular system: arterial hypotension, tachycardia.

    Digestive system: hiccough, nausea, vomiting, diarrhea.

    Sense organs: diplopia, nystagmus.

    Dermatological reactions: transient alopecia, itching.

    urinary system: urinary incontinence or retention, impaired renal function.

    Reproductive system: dysmenorrhea, decreased libido.

    Allergic reactions, phlebitis at the injection site.

    Overdose:

    Drowsiness, impaired coordination, confusion, oppression of reflexes, coma.

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

    Interaction:

    Reduce the systemic effect of clonazepam when administered inducers of the isoenzyme CYP3A4: carbamazepine, rifampicin, phenytoin.

    Increase the half-life of clonazepam: itraconazole, saquinavir, erythromycin, fluconazole.

    Strengthens the effects of neuroleptics, tranquilizers, sleeping pills, anticonvulsants, analgesics and anesthetics.

    With the simultaneous use of blockers of β-adrenoreceptors, calcium channel blockers, diuretics, ACE inhibitors, levodopa, magnesium sulfate and nitrates, the hypotensive effect is enhanced.

    Incompatible with alcohol.

    Special instructions:

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    The drug is addictive, the withdrawal is gradual.

    Instructions
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