Active substanceAmitriptylineAmitriptyline
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  • Dosage form: & nbsppills
    Composition:

    Each tablet contains active substance amitriptyline hydrochloride 28.3 mg (in terms of amitriptyline 25 mg).

    Excipients: lactose monohydrate (sugar milk) - 50.0 mg, corn starch - 9.2 mg, povidone-K25 - 1.25 mg, microcrystalline cellulose - 10.25 mg, magnesium stearate - 1.0 mg.

    Description:

    Tablets are white or white with a cream shade of color with inclusions of beige color, flat-cylindrical, with a facet on both sides and risk from one side.

    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.

    Pharmacodynamics

    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, is 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 for 4-8 hours. Bioavailability of amitriptyline from 33 to 62%, its active metabolite nortriptyline - 46-70%. The volume of distribution is 5-10 l / kg. Effective therapeutic concentrations in the blood of amitriptyline are 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. The connection with plasma proteins is 92% 96%. Metabolised in the liver (by demethylation, hydroxylation) with formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites.

    The period of excretion from the blood plasma is from 10 to 28 hours for amitriptyline and from 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:

    Apply strictly according to the doctor's prescription.

    - Endogenous depression and other depressive disorders.

    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 severe 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 or in the previous 2 weeks treatment with MAO inhibitors.

    Pregnancy, the period of breastfeeding.

    Children under 6 years.

    Hypersensitivity to amitriptyline.

    Carefully:

    Amitriptyline should be used with caution in people with alcoholism, with bronchial asthma, manic-depressive psychosis (MDP) and epilepsy, with oppression of bone marrow hematopoiesis, hyperthyroidism, angina and heart failure, angle-closure glaucoma, intraocular hypertension, schizophrenia (although when taken usually there is no exacerbation of productive symptoms).

    Dosing and Administration:

    Assign inside (during or after eating).

    The initial daily intake for 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 l|50- 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 (maximum dose for outpatients is 150 mg / day). In these cases, treatment is advisable to start 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 condition. After receiving a persistent antidepressant effect in 2-4 weeks, the doses gradually and slowly reduce. 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 prevention of migraine, chronic pain of a neurogenic nature (including prolonged headaches) from 12.5-25 mg to 100 mg / day.

    Side effects:

    Side effects are mainly 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 central nervous system: headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, 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, violation conductivity, 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 sharp cessation of treatment, it is possible to develop a withdrawal syndrome: headache,nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with bright, unusual dreams, increased excitability.

    Overdose:

    Drowsiness, disorientation, confusion, dilated pupils, fever, dyspnea, dysarthria, agitation, hallucinations, convulsive seizures, muscle stiffness, coma, 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. The monitoring of cardiovascular activity (ECG) for 5 days, 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.

    In the joint use of amitriptyline with antipsychotics, and / or anticholinergic drugs, febrile temperature reaction, paralytic intestinal obstruction may occur.

    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 - derivatives of coumarin, an increase in anticoagulant activity of the latter.

    With the simultaneous administration of amitriptyline and cimetidine, plasma concentrations of amitriptyline may increase 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 may increase depression caused by glucocorticosteroids; joint use with drugs to treat thyrotoxicosis increases the risk of agranulocytosis.

    Simultaneous reception 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 of 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, driving of vehicles, maintenance of mechanisms and other types of work requiring increased concentration of attention, as well as alcohol intake are prohibited.
    Form release / dosage:

    Tablets 25 mg.

    Packaging:

    For 10, 20, 30, 40, 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 10, 20, 30, 40, 50, 60, 70, 80, 90 or 100 tablets in cans of polyethylene terephthalate.

    One jar or 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (pack) made of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005402/08
    Date of registration:14.07.2008 / 25.12.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.08.2017
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