Amitriptyline, tablets 25 mg 50 pcs

Antidepressant from the group of tricyclic compounds, dibenzocycloheptadine derivative.
The mechanism of antidepressant action is associated with increased concentration of noradrenaline in synapses and/or serotonin in CNS due to inhibition of neuronal reuptake of these mediators. With long-term use, it reduces the functional activity of β-adrenoreceptors and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems that are disturbed in depressed states. In anxiety-depressive states it reduces anxiety, agitation and depressive manifestations.

Indications

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug-induced, with organic brain lesions, alcohol withdrawal), schizophrenic psychoses, mixed emotional disorders, behavior disorders (activity and attention), nocturnal enuresis (except for patients with bladder hypotonia), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical facial pain, postherpetic neuralgia, posttraumatic neuropathy, diabetic neuropathy, peripheral neuropathy), migraine prevention, gastric and duodenal ulcer.

Active ingredient

Amitriptyline

Composition

Interaction

Concomitant use with drugs that have CNS depressant effect, a significant increase in the CNS depressant effect, hypotensive effect, respiratory depression is possible.

Concomitant use with drugs that have anticholinergic activity, possible increase in anticholinergic effects.

Simultaneous use may increase the effect of sympathomimetic drugs on the cardiovascular system and increase the risk of cardiac arrhythmias, tachycardia, severe arterial hypertension.

Simultaneous use with antipsychotic agents (neuroleptics) mutually inhibits metabolism, thus reducing the threshold of seizure readiness.

Simultaneous use with antihypertensive agents (except for clonidine, guanethidine and their derivatives) may increase the antihypertensive effect and the risk of orthostatic hypotension.

Concomitant use with MAO inhibitors may cause hypertensive crisis; with clonidine, guanethidine – possible decrease of hypotensive action of clonidine or guanethidine; with barbiturates, carbamazepine – possible decrease of amitriptyline action due to its increased metabolism.

A case of serotonin syndrome during concomitant use with sertraline has been described.

Concomitant use with sucralfate decreases absorption of amitriptyline; with fluvoxamine – increased blood plasma concentration of amitriptyline and risk of toxic effects; with fluoxetine – increases the concentration of amitriptyline in blood plasma and develops toxic reactions due to inhibition of CYP2D6 isoenzyme under the influence of fluoxetine; with quinidine – may slow metabolism of amitriptyline; with cimetidine – may slow metabolism of amitriptyline, increase its concentration in blood plasma and development of toxic effects.

Simultaneous use with ethanol increases the effect of ethanol, especially during the first few days of therapy.

Directions for use

For oral administration, the initial dose is 25-50 mg at night. Then, within 5-6 days, the dose is increased individually to 150-200 mg/day (most of the dose is taken at night). If during the second week, there was no improvement, the daily dose is increased to 300 mg. If symptoms of depression disappear, the dose is reduced to 50-100 mg/day and the therapy is continued for at least 3 months. In elderly patients with mild impairment the dose is 30-100 mg/day, usually once a day at night, after achieving therapeutic effect, the minimum effective dose is transferred to 25-50 mg/day.

In nocturnal enuresis in children aged 6-10 years – 10-20 mg/day at night, in children aged 11-16 years – 25-50 mg/day.

In/m – the initial dose is 50-100 mg/day in 2-4 injections. If necessary, the dose may be gradually increased up to 300 mg/day, in exceptional cases – up to 400 mg/day.

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Special Instructions

Caution is used in CHD, arrhythmia, heart block, heart failure, myocardial infarction, arterial hypertension, stroke, chronic alcoholism, thyrotoxicosis, during therapy with thyroid drugs.

During the therapy with amitriptyline caution is required in case of sudden change to the upright position from lying or sitting position.

Withdrawal syndrome may occur in case of abrupt termination of therapy.

Amitriptyline in doses over 150 mg/day lowers the seizure threshold; the risk of epileptic seizures in predisposed patients as well as in the presence of other factors that increase the risk of seizure syndrome (including brain damage of any etiology, concurrent use of antipsychotic drugs, during ethanol withdrawal or withdrawal of drugs with anticonvulsant activity) should be considered.

It should be noted that in patients with depression suicidal attempts are possible.

In combination with electroconvulsive therapy should be used only under close medical supervision.

In predisposed patients and elderly patients may provoke the development of drug psychosis, mainly at night (after discontinuation of the drug passes within a few days).

May cause paralytic intestinal obstruction, mainly in patients with chronic constipation, the elderly or in patients forced to observe bed rest.

Before general or local anesthesia, the anesthesiologist should be advised that the patient is taking amitriptyline.

An increased incidence of dental caries has been observed with prolonged use. There may be an increased need for riboflavin.

Amitriptyline can be used no earlier than 14 days after withdrawal of MAO inhibitors.

Should not be used simultaneously with adreno- and sympathomimetics, including epinephrine.

Do not use simultaneously with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.

Caution should be exercised when using simultaneously with other drugs with anticholinergic effect.

Do not drink alcohol while taking amitriptyline.

Effect on the ability to drive vehicles and operate mechanisms

During the treatment it is necessary to refrain from potentially dangerous activities requiring increased attention and quick psychomotor reactions.

Contraindications

Acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute intoxication with sleeping pills, analgesic and psychotropic drugs, closed-angle glaucoma, severe AV and intraventricular conduction disorders (Gis bundle branch block, AV-blockade of II degree), lactation, children under 6 years of age (for oral administration), children under 12 years of age (for IV and IV administration), concomitant treatment with MAO inhibitors and 2 weeks before their administration, hypersensitivity to amitriptyline.

Side effects

CNS and peripheral nervous system disorders: somnolence, asthenia, fainting, anxiety, disorientation, agitation, hallucinations (especially in elderly patients and patients with Parkinson’s disease), anxiety, motor anxiety, manic state, hypomanic state, aggressiveness, memory disturbance, depersonalization, worsening depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of psychosis symptoms, headache, myoclonus, dysarthria, tremor (especially of hands, head, tongue), peripheral neuropathy (paresthesias), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, increased frequency and intensity of seizures, changes on EEG.

Cardiovascular system: orthostatic hypotension, tachycardia, conduction disorders, dizziness, nonspecific changes on ECG (ST interval or T-wave), arrhythmia, labile BP, intraventricular conduction disorders (QRS dilation, changes of PQ interval, Gis bundle block).

The digestive system: nausea, heartburn, vomiting, gastralgia, increased or decreased appetite (weight gain or loss), stomatitis, change in taste, diarrhea, darkened tongue, rarely – liver function abnormalities, cholestatic jaundice, hepatitis.

Endocrine system: testicular edema, gynecomastia, increased mammary glands, galactorrhea, decreased libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), inadequate ADH secretion syndrome.

Blood system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.

Allergic reactions: skin rash, skin itching, urticaria, photosensitization, swollen face and tongue.

Effects due to anticholinergic activity: dry mouth, tachycardia, accommodation disorders, blurred vision, mydriasis, increased intraocular pressure (only in persons with narrow anterior chamber angle), constipation, paralytic obstruction, urinary retention, decreased sweating, confusion, delirium or hallucinations.

Other: hair loss, tinnitus, edema, hyperpyrexia, enlarged lymph nodes, pollakiuria, hypoproteinemia.

Overdose

Symptoms: drowsiness, disorientation, confusion, depression of consciousness up to coma, dilated pupils, increased body temperature, shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle rigidity, vomiting, arrhythmia, arterial hypotension, heart failure, respiratory depression.

Treatment: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of BP and water-electrolyte balance. Monitoring of cardiovascular activity (ECG) for 5 days is indicated, as relapse may occur after 48 hours or later.

Hemodialysis and forced diuresis are of little effect.