Amitriptyline + Chlordiazepoxide (Amitriptylinum + Chlordiazepoxydum)

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

Anxiolytics

Antidepressants

Included in the formulation
  • Amide
    pills inwards 
    San Pharmaceutical Industries Co., Ltd.     India
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.06.C.A.01   Amitriptyline in combination with psycholeptics

    Pharmacodynamics:

    Amitriptyline is a tricyclic antidepressant from a group of indiscriminate inhibitors of neuronal capture of monoamines. It has a timoanaleptic and sedative effect.

    Chlordiazepoxide is a tranquilizer from the benzodiazepine group. Has a tranquilizing, anxiolytic, central muscle relaxant effect.

    The mechanism of action of the drug to the end has not been studied, probably based on the simultaneous effect of the tranquilizer of chlordiazepoxide on the limbic system responsible for the emotional state, and the antidepressant amitriptyline - on the synthesis of noradrenaline and serotonin in the synapses of neurons of the central nervous system.

    Pharmacokinetics:

    When administered orally, Cmax in plasma is reached within 4-8 hours. Because the amitriptyline slows transit time in the digestive tract, absorption can be slowed, especially when overdose. Amitriptyline binds to plasma proteins by 94%; T1 / 2 - about 20 hours. Chlordiazepoxide associated with plasma proteins by 96%; T1 / 2 - about 10 hours.Both components are metabolized in the liver. T1 / 2 active metabolite of amitriptyline (noratriptilina) is 30 h. T1 / 2active metabolite of chlordiazepoxide (desmethyl-chlordiazepoxide) is 1-4 days.

    The drug penetrates the placental barrier and is excreted in breast milk.

    Indications:

    Depression of various genesis, in the structure of which there is an anxiety syndrome of varying severity.

    ICD-10

    V.F30-F39.F31   Bipolar affective disorder

    V.F30-F39.F32   Depressive episode

    V.F30-F39.F33   Recurrent depressive disorder

    V.F40-F48.F41.2   Mixed anxiety and depressive disorder

    Contraindications:

    Decompensated heart disease; acute and recovery period of myocardial infarction; conduction disorders of the heart muscle; Stage III hypertension; acute liver and kidney disease with marked impairment of functions; blood diseases; hyperthyroidism and concurrent treatment with thyrotropic drugs; peptic ulcer of stomach and duodenal stage of exacerbation; glaucoma; hypertrophy of the prostate; atony of the bladder; pyloric stenosis, paralytic intestinal obstruction; simultaneous treatmentMAO inhibitors; marked myasthenia gravis; pregnancy; lactation period; childhood; hypersensitivity to any of the components of the drug. With caution - Simultaneous administration of the drug with MAO inhibitors can lead to death. A break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days.

    Carefully:

    Simultaneous administration of the drug with MAO inhibitors can lead to death. A break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days.

    Pregnancy and lactation:

    Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Assign inside (after eating), the dose of the drug is set individually.

    The initial daily dose is 1 tab. 2-3 times / day. If necessary, the dose of the drug can be increased to 6 tablets. (with the maximum content of active substances) / day. (for 2-3 sessions).

    After obtaining a persistent antidepressant effect, after 2-4 weeks the doses gradually and slowly decrease. In case of signs of depression with decreasing doses, it is necessary to return tothe previous dose.

    If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is impractical.

    In elderly patients with mild disorders, in outpatient practice, the doses are 12.5 / 5 mg; 25/5 mg or 25/10 mg usually 1 time / day at night.

    Side effects:

    From the cardiovascular system: tachycardia, orthostatic arterial hypotension or increased blood pressure, impaired conduction of the heart muscle; described individual cases of stroke and myocardial infarction.

    On the part of the digestive system: nausea, vomiting, anorexia, stomatitis, impaired taste, black staining of the tongue, a feeling of discomfort in epigastrium, diarrhea, rarely a violation of liver function.

    On the part of the endocrine system: gynecomastia, galactorrhea, changes in the secretion of antidiuretic hormone, decreased libido, potency.

    Other: oppression of bone marrow function, skin rash, hair loss, enlarged lymph nodes, weight gain with prolonged use.

    Overdose:

    Symptoms: drowsiness, disorientation, confusion, dysarthria, agitation, hallucinations, numbness of limbs, convulsive seizures, rigidity of muscles, stupor, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression.

    Treatment: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, detoxification, administration of physostigmine 1-3 mg every 1 / 2-2 hours IM or IV, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Long-term observation is shown, because relapse symptoms of intoxication may occur after 48 h.

    Interaction:

    Active components of the drug potentiate CNS depression by the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsant drugs, central and opioid analgesics, anesthetics, alcohol. When combined with neuroleptics, and / or anticholinergic drugs, a febrile temperature reaction may occur, paralytic intestinal obstruction.

    Active components of the drug potentiate the hypertensive effects of catecholamines, but inhibit the effects of drugs acting on the release of norepinephrine (turoamine).

    Active components included in the drug can block the antihypertensive effect of guanethidine and drugs with a similar mechanism of action.

    With the simultaneous administration of the drug and cimetidine, an increase in plasma concentration of amitriptyline is possible.

    Special instructions:

    Treatment in old age should be under close supervision and with the use of minimal doses of the drug, increasing them gradually, in order to avoid the development of delirious disorders, hypomania and other complications.

    Patients with a depressive phase of manic-depressive psychosis can go into a manic stage.

    During the reception of amitriptyline, driving of vehicles, maintenance of mechanisms and other types of work requiring increased concentration of attention is prohibited.

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