Chlordiazepoxide (Chlordiazepoxydum)

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

Anxiolytics

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    Tallinn Pharmaceutical Factory     Estonia
    • АТХ:

    N.05.B.A.02   Chlordiazepoxide

    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 is associated with oppression of epileptogenic activity due to 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 0.5-4 hours. The connection with plasma proteins is 96%. Deposited in adipose tissue. Penetrates through the blood-brain and placental barrier, enters the breast milk.

    Metabolism in the liver with the formation of 4 active metabolites with periods of semi-elimination: oxazepam 5-15 hours, desmethylchlorodiazepoxide 8-24 hours, demoxepam - 14-95 hours, desmethyldiazepam - 40-250 hours.

    Elimination 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 for relief of withdrawal syndrome with chronic alcoholism, substance abuse, and addiction, as well as for the treatment of diseases manifested by increased muscle tone: epilepsy, schizophrenia, with psychopathic agitation, specific personality disorders, insomnia.

    ICD-10

    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.F41.2   Mixed anxiety and depressive disorder

    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

    XIV.N80-N98.N94.3   Premenstrual tension syndrome

    XIV.N80-N98.N95.1   Menopause and menopause in women

    XVIII.R00-R09.R07.2   Pain in the region of the heart

    XVIII.R25-R29.R25.2   Cramp and spasm

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    XVIII.R40-R46.R45.4   Irritability and anger

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

    XXI.Z100.Z100 *   CLASS XXII Surgical Practice

    V.F90-F98.F90   Hyperkinetic disorders

    Contraindications:

    Hepatic and renal failure, angle-closure glaucoma, myasthenia gravis, pregnancy and lactation, children's age up to 4 years, individual intolerance.

    Carefully:

    Kidney and liver diseases, chronic respiratory failure, sleep apnea syndrome.

    Pregnancy and lactation:

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

    Dosing and Administration:

    Use in children

    Inside, the daily dose in 3-4 reception:

    4-7 years: 5-10 mg;

    8-14 years: 10-20 mg;

    15-18 years: 20-30 mg.

    Adults

    Inside, 5-10 mg 2-4 times a day. When insomnia - for 10-20 mg for 2 hours before bedtime.

    The highest daily dose: 40 mg.

    The highest single dose: 20 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.

    Hemopoietic system: neutropenia.

    The cardiovascular system: bradycardia, hypotension.

    Digestive system: nausea, constipation, dry mouth.

    Sense organs: nystagmus, diplopia.

    Reproductive system: menstrual irregularities, 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 chlordiazepoxide.

    Disrupts the metabolism of phenytoin.

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

    Incompatible with alcohol.

    Special instructions:

    Monitoring of the picture of peripheral blood and liver function.

    When treating with chlordiazepoxide, 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.

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