Active substanceAmitriptylineAmitriptyline
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  • Dosage form: & nbspcoated tablets
    Composition:

    One tablet contains:

    Active substance: amitriptyline hydrochloride - 0.025 g.

    Excipients: sugar, milk or granule 70, cellulose microcrystalline or vigapur 102, corn pregelatinized corn starch, copolyvidone, silicon dioxide colloid (aerosil), calcium stearate, hydroxypropylcellulose, polyethylene glycol 4000, titanium dioxide, talc, or film-forming system EasyCoat, consisting of hydroxypropylmethylcellulose, polyethylene glycol 6000, copolyvidone (plastzona), talc, titanium dioxide and azorubin.

    Description:

    The tablets covered with a cover of pink color, round biconcave form. A slight unevenness of the coating is allowed.

    Pharmacotherapeutic group:Antidepressant
    ATX: & nbsp

    N.06.A.A.09   Amitriptyline

    Pharmacodynamics:

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

    The mechanism of antidepressant action of amitriptyline is associated with inhibition of reverse neuronal seizure of catecholamines (noradrenaline, dopamine) and serotonin in the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and periphery, has peripheral antihistamine (H1) and antiadrenergic properties.Also causes antinevralgic (central analgesic), antiulcer and anti-bulimic action, effective for bedwetting. Antidepressant effect develops within 2-4 weeks. after the beginning of the application.

    Pharmacokinetics:

    Absorption is high. The time to reach the maximum concentration (Tmah) after ingestion of 4-8 hours h. Bioavailability of amitriptyline from 33 to 62%, its active metabolite nortriptyline - 46-70%. The volume of distribution is 5-10 l / kg. Effective therapeutic concentration in the blood of amitriptyline is 50-250 ng / ml, for nortriptyline (its active metabolite) 50-150 ng / ml. The maximum concentration in the blood plasma (Cmax) 0.04-0.16 μg / ml. Passes through the histohematological barriers, including the blood-brain barrier (including nortriptyline).

    The concentrations of amitriptyline in tissues are higher than in plasma. Relationship with plasma proteins 92 - 96%. Metabolised in the liver (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites.

    The half-life of plasma from 10 to 28 hours for amitriptyline and 16 to 80 hours for nortriptyline. It is allocated by the kidneys - 80%, partially with bile. Complete excretion within 7-14 days.

    Amitriptyline penetrates the placental barrier, is excreted in breast milk in concentrations similar to plasma.

    Indications:

    Depression of any etiology. Due to the severity of the sedative effect is especially effective in anxiety - depressive states.

    Mixed emotional disorders and behavioral disorders; phobic disorders.

    Children's enuresis (except for children with hypotonic urinary bladder).

    Psychogenic anorexia, bulimic neurosis.

    Chronic pain syndrome (neurogenic nature), prevention of migraine.

    Contraindications:

    Heart failure in the stage of decompensation.

    Acute and recovery period of myocardial infarction.

    Violations of the conduction of the heart muscle.

    Severe arterial hypertension.

    Acute liver and kidney disease with marked impairment of functions.

    Stomach ulcer and 12 duodenal ulcer in the stage of exacerbation.

    Hypertrophy of the prostate.

    Atony of the bladder.

    Pylorosthenosis, paralytic obstruction of the intestine.

    Simultaneous treatment with MAO inhibitors (see Interaction).

    Pregnancy, the period of breastfeeding.

    Children under 6 years.

    Hypersensitivity to amitriptyline.

    Carefully:

    Amitriptyline should be used with caution in patients suffering from alcoholism, people with asthma, manic-depressive psychosis (MDP) and epilepsy (see. Special instructions), with inhibition of bone marrow hematopoiesis, hyperthyroidism, angina and heart failure, angle-closure glaucoma, ocular hypertension, schizophrenia ( although it usually does not exacerbate productive symptoms during its administration).

    Dosing and Administration:

    Assign inside (during or after eating).

    The initial daily intake with oral administration is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg until the desired antidepressant effect is achieved. The optimal daily therapeutic dose is 150-200 mg (the maximum part of the dose is taken at night). In severe depression, resistant to therapy, the dose is increased to 300 mg or more, to the maximum tolerated dose (the maximum dose for outpatient of patients - 150 mg / day). In these cases, treatment is advisable to begin with intramuscular or intravenous administration of the drug, while using higher initial doses, accelerating the build-up of dosages under the control of the somatic state.

    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 to the 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 25-50-100 mg maximum, in divided doses or once a day at night.

    When enuresis, children older than 6 years 12.5-25 mg before bed (dose should not exceed 2.5 mg / kg of body weight of the child).

    For the prevention of migraine, chronic pain of a neurogenic nature (including prolonged headaches) from 12.5-25 mg to 100 mg / day.

    Side effects:

    Basically, they are associated with the anticholinergic action of the drug: paresis of accommodation, blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, delayed urination, fever. All these phenomena usually pass after adaptation to the drug or reduce doses.

    From the side of the central nervous system: headache, ataxia, fatigue, weakness, irritability, dizziness,noise in the ears, drowsiness or insomnia, impaired concentration, nightmarish dreams, dysarthria, confusion, hallucinations, motor excitement, disorientation, tremor, paresthesia, peripheral neuropathy, changes on the EEG. Rarely, extrapyramidal disorders, convulsions, anxiety.

    From the side of the cardiovascular system: tachycardia, arrhythmia, conduction disorders, lability of arterial pressure, expansion of the complex QRS on ECG (violation of intraventricular conduction), symptoms of heart failure, fainting.

    From the gastrointestinal tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disorders, darkening of the tongue, a feeling of discomfort in the epigastrium, gastralgia, increased activity of "liver" transaminases, rarely cholestatic jaundice, diarrhea.

    From the endocrine system: increase in breast size in men and women, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), changes in libido, potency. Rarely - hypo- or hyperglycemia, glucosuria, impaired glucose tolerance, edema of the testicles.

    Allergic reactions: skin rash, itching, photosensitivity, angioedema, hives.

    Other: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, enlarged lymph nodes, weight gain with prolonged use, sweating, pollakiuria.

    With long-term treatment, especially in high doses, with a sudden cessation of treatment, it is possible to develop withdrawal syndrome: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with bright, unusual dreams, increased excitability.

    Overdose:

    Drowsiness, disorientation, confusion, depression of consciousness down to coma, pupil dilatation, fever, dyspnea, dysarthria, agitation, hallucinations, convulsive attacks, muscle rigidity, vomiting, arrhythmia, arterial hypotension, heart failure, respiratory depression.

    Measures of assistance: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Monitoring of cardiovascular activity (ECG) for 5 days is shown, since relapse can occur after 48 hours and later. Hemodialysis and forced diuresis are of little effect.

    Interaction:

    Amitriptyline strengthens the depressing effect on the central nervous system following drugs: neuroleptics, sedatives and hypnotics, anticonvulsant drugs, analgesics, funds for anesthesia, alcohol; shows synergism when interacting with other antidepressants.

    With the combined use of amitriptyline with neuroleptics, and / or anticholinergic drugs, a febrile temperature reaction may occur, paralytic intestinal obstruction.

    Amitriptyline potentiates the hypertensive effects of catecholamines and other adrenostimulants, which increases the risk of heart rhythm disturbances, tachycardia, severe arterial hypertension, but inhibits the effects of drugs that affect the release of norepinephrine.

    Amitriptyline may reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect of anticonvulsants.

    With the simultaneous use of amitriptyline and anticoagulants - coumarin derivatives, an increase in anticoagulant activity of the latter is possible.

    With the simultaneous administration of amitriptyline and cimetidine, an increase in plasma concentration of amitriptyline is possible with the possible development of toxic effects.

    Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduce the plasma concentrations of amitriptyline.

    Amitriptyline increases the effect of antiparkinsonian drugs and other drugs that cause extrapyramidal reactions.

    Quinidine slows the metabolism of amitriptyline.

    The combined use of amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors can trigger delirium.

    Estrogen-containing oral contraceptives can increase the bioavailability of amitriptyline; pimozide and probucol may increase cardiac arrhythmias. Amitriptyline can enhance depression caused by glucocorticosteroids; when combined with drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases.

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

    Special instructions:

    Amitriptyline in doses above 150 mg / day reduces the threshold of convulsive activity, therefore, one should consider the possibility of occurrence of convulsive seizures in patients with those with anamnesis and in the category of patients who are predisposed to it because of age or trauma.

    Treatment with amitriptyline in old age should be carefully controlled, with minimum doses of the drug and gradually increased, in order to avoid the development of delirious disorders, hypomania and other complications.

    Patients with a depressive TIR phase can go into a manic stage.

    Effect on the ability to drive transp. cf. and fur:

    During the reception of amitriptyline, it is forbidden to drive vehicles, service mechanisms and other types of work requiring increased concentration of attention, as well as alcohol intake.

    Form release / dosage:

    The coated tablets are 0.025 g.

    Packaging:For 10 tablets in a planar cell package. 5 contour mesh packages in a cardboard bundle together with instructions for medical use.
    Storage conditions:

    List B. In a dry, protected from light, out of reach of children, at a temperature of no higher than 25 ° C.

    Shelf life:2 years.The drug should not be taken after the expiry date indicated on the package!
    Terms of leave from pharmacies:On prescription
    Registration number:P N003295 / 01
    Date of registration:09.02.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.08.2017
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