Amitriptyline, tablets 25 mg 50 pcs

Enuresis, Migraine, Anxiety, Pain, Depression, Depressed mood

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug-induced, with organic brain lesions).

. As a part of complex therapy it is used for mixed emotional disorders, psychosis in schizophrenia, alcohol withdrawal, behavior disorders (activity and attention), nocturnal enuresis in children (except for patients with bladder hypotension), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pain in the face, postherpetic neuralgia, posttraumatic neuropathy, diabetic or others. peripheral neuropathy), headache, migraine (prevention), gastric and 12 duodenal ulcer.

Active ingredient

Composition

1 tablet of amitriptyline hydrochloride 28.3 mg, which corresponds to the content of amitriptyline 25 mg

Added substances: lactose monohydrate, corn starch, gelatin, calcium stearate, talcum, colloidal silicon dioxide.

The composition of the film: simethicone SE-2, macrogol, Sepifilm 3048 Yellow (hypromellose, microcrystalline cellulose, polyoxyl 40 stearate, titanium dioxide, quinoline dye (Quinolin Yellow) (E104).

How to take, the dosage

It is administered orally (during or after meals). The initial daily oral dose 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 obtained. The optimal daily therapeutic dose is 150-200 mg (the maximum portion of the dose is taken at night).
In severe depression, resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose (maximum dose for outpatients is 150 mg/day). In these cases, it is reasonable to start treatment with intramuscular or intravenous administration of the drug, using higher initial doses, accelerating dosage escalation under control of somatic condition. After obtaining a stable antidepressant effect in 2-4 weeks, the dose is gradually and slowly reduced to 50-100 mg/day and therapy is continued for at least 3 months. In case of signs of depression when the dose is reduced, it is necessary to return to the previous dose.
If the patient’s condition does not improve within 3-4 weeks of treatment, further therapy is inadvisable.

In elderly patients with mild disorders, in outpatient practice, doses are 25-50-100mg daily in divided doses or once daily at night.

In nocturnal enuresis in children aged 6-10 years – 10-20 mg/day at night, in age 11-16 years – 25-50 mg/day. (the dose should not exceed 2.5 mg/kg of child weight).

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

In severe depression, resistant to therapy: intramuscularly or intravenously (administer slowly!) administered at a dose of 10-20-30 mg up to 4 times a day, the dose should be increased gradually, the maximum daily dose of 150 mg; after 1-2 weeks the drug is transferred to oral administration.
Children over 12 years of age and the elderly are given lower doses and increased more slowly.
If the patient’s condition does not improve within 3-4 weeks of treatment, further therapy is not advisable.

Interaction

When using ethanol and CNS depressant drugs (including other antidepressants, barbiturates, benzadiazepines and general anesthetics) together, a significant increase in CNS depressant effect, respiratory depression and hypotensive effect are possible.

It increases sensitivity to beverages containing ethanol.

Enhances the anticholinergic activity of drugs with anticholinergic activity (e.g., phenothiazine derivatives, anti-Parkinsonian drugs, amantadine, atropine, biperidine, antihistamine drugs), which increases the risk of side effects (CNS, vision, bowel and bladder). When co-administration with choline blockers, phenothiazine derivatives and benzodiazepines – mutual enhancement of sedative and central choline blocking effects and increased risk of epileptic seizures (lower threshold of seizure activity); phenothiazine derivatives may also increase the risk of neuroleptic malignant syndrome.

When used concomitantly with anticonvulsants, increased CNS depression, decreased seizure threshold (when used in high doses) and decreased effectiveness of the latter may occur.

When used concomitantly with antihistamines, clonidine – increased CNS depression; with atropine – increased risk of paralytic ileus; with drugs causing extrapyramidal reactions – increased severity and frequency of extrapyramidal effects.

In concomitant use of amitriptyline and indirect anticoagulants (coumarin derivatives or indadeon) the anticoagulant activity of the latter may increase.

Amitriptyline may increase depression caused by glucocorticosteroids (GCS).

The drugs for the treatment of thyrotoxicosis increase the risk of agranulocytosis.

Decreases the effectiveness of phenytoin and alpha-adrenoblockers.

Microsomal oxidation inhibitors (cimetidine) prolong T1/2, increase the risk of toxic effects of amitriptyline (a 20-30% dose reduction may be required), microsomal liver enzyme inducers (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) decrease the plasma concentration and decrease the effectiveness of amitriptyline.

The co-administration with disulfiram and other acetaldehydrogenase inhibitors provokes delirium.

Fluoxetine and fluvoxamine increase the plasma concentration of amitriptyline (it may be necessary to reduce the dose of amitriptyline by 50%).

Estrogen-containing oral contraceptive drugs and estrogens may increase the bioavailability of amitriptyline.

In concomitant use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa – decrease the hypotensive effect of the latter; with cocaine – risk of cardiac arrhythmias.

The antiarrhythmic drugs (such as quinidine) increase the risk of arrhythmias (the metabolism of amitriptyline may be slowed).

Pimozide and probucol may exacerbate cardiac arrhythmias, which is manifested by prolongation of the Q-T interval on the ECG.

The effects of epinephrine, norepinephrine, isoprenaline, ephedrine, and phenylephrine on the SCS (including when these drugs are part of local anesthetics) and increase the risk of cardiac rhythm disturbances, tachycardia, and severe arterial hypertension.

The vasoconstrictor effect of alpha-adrenomimetics for intranasal administration or for use in ophthalmology (with significant systemic absorption) may increase when co-administered.

In co-administration with thyroid hormones – mutual enhancement of therapeutic effects and toxic effects (include cardiac arrhythmias and stimulating effects on the CNS).

M-cholinoblockers and antipsychotic drugs (neuroleptics) increase the risk of hyperpyrexia (especially in hot weather).

The co-administration with other hematotoxic drugs may increase hematotoxicity.

Incompatible with MAO inhibitors (increased frequency of periods of hyperpyrexia, severe seizures, hypertensive crises and patient death are possible).

Special Instructions

Before treatment it is necessary to control BP (in patients with low or labile BP it may decrease even more); during treatment – control of peripheral blood (in some cases agranulocytosis may develop, therefore it is recommended to monitor the blood picture, especially with fever, flu-like symptoms and angina), during long-term therapy – control of CSS and liver functions. The elderly and patients with diseases of the cardiovascular system should have control of heart rate (HR), BP, ECG. ECG may show clinically insignificant changes (smoothed T wave, depressed S-T segment, widened QRS complex).

Precaution should be exercised when suddenly going upright from lying or sitting position.

Ethanol should be avoided during treatment.

Prescribe at least 14 days after withdrawal of MAOI inhibitors, starting with low doses.

The development of withdrawal syndrome may occur if the drug is stopped suddenly after long-term treatment.

Amitriptyline in doses above 150 mg/day lowers the seizure threshold (the risk of epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other predisposing conditions. other factors predisposing to the development of a seizure syndrome, such as brain damage of any etiology, concurrent use of antipsychotic drugs (neuroleptics), withdrawal from ethanol, or withdrawal of drugs with anticonvulsant properties, such as benzodiazepines.)

The risk of suicidal behavior is inherent in severe depression and may persist until substantial remission is achieved. Because of this, a combination of benzodiazepine or neuroleptic medications may be indicated at the beginning of treatment and constant physician supervision (entrusting trusted persons to store and dispense medications).

In children, adolescents and young adults (younger than 24 years) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients the risk of suicide and the benefit of their use should be correlated. In short-term studies, the risk of suicide did not increase in people over 24 years of age, and slightly decreased in people over 65 years of age. All patients should be monitored during antidepressant treatment for early detection of suicidal tendencies.

In patients with cyclic affective disorder during the depressive phase, manic or hypomanic states may develop during therapy (dose reduction or drug withdrawal and administration of antipsychotic medication is necessary). After these states have subsided, if indicated, treatment at low doses may be resumed.

Because of possible cardiotoxic effects, caution is required when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.

In combination with electroconvulsive therapy, it is prescribed only with close medical supervision.

In predisposed patients and elderly patients, it may provoke the development of drug-induced psychosis, mainly at night (after withdrawal of the drug goes away within a few days).

May cause paralytic ileus, mainly in chronically constipated, elderly patients or in patients who are forced to remain in bed.

The anesthesiologist should be advised before general or local anesthesia that the patient is taking amitriptyline.

The anticholinergic effects may decrease tear production and increase the relative amount of mucus in the lacrimal fluid, which can lead to corneal epithelial damage in patients who wear contact lenses.

An increase in the incidence of dental caries has been observed with long-term use. There may be an increased need for riboflavin.

Animal reproduction studies have shown adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not been conducted. In pregnant women, the drug should be used only if the estimated benefit to the mother exceeds the potential risk to the fetus.

It penetrates into the breast milk and may cause somnolence in infants.

In order to avoid the development of “withdrawal” syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, high or low blood pressure, tremor or spastic phenomena) amitriptyline administration should be gradually stopped at least 7 weeks before the expected delivery.

Children are more susceptible to acute overdose, which should be considered dangerous and potentially fatal to them.

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

Side effects

Mainly related to the cholin-blocking effect of the drug: accommodation paresis. Blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, urinary retention, increased body temperature. All these phenomena usually disappear after adaptation to the drug or dose reduction.
CNS disorders: headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, concentration disorders, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremor, paresthesias, peripheral neuropathy, EEG changes. Rarely-extrapyramidal disorders, seizures, anxiety.
Cardiovascular system: tachycardia, arrhythmia, conduction disorders, blood pressure fluctuations, QRS complex dilation on ECG (intraventricular conduction disorders), symptoms of heart failure, syncope.
Gastrointestinal tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disorders, darkened tongue, discomfort in the epigastrium, gastralgia, increased liver transaminases activity, rarely cholestatic jaundice, diarrhea.
Endocrine system disorders: increase in breast size in men and women, galactorrhea, altered secretion of antidiuretic hormone (ADH), altered libido and potency. Rarely, hypo- or hyperglycemia, glucosuria, impaired glucose tolerance, testicular edema. Allergic reactions: skin rash, itching, photosensitization, angioedema, urticaria.
Other: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, enlarged lymph nodes, weight gain during long-term use, sweating, pollakiuria. With long-term treatment, especially in high doses, abrupt discontinuation of treatment may lead to withdrawal syndrome: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disorders with vivid, unusual dreams, increased excitability.

Overdose

Symptoms:drowsiness, disorientation, confusion, dilated pupils, increased body temperature, dyspnea, dysarthria, agitation, hallucinations, seizures, muscle rigidity, suppuration, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression.
Treatment:Cessation of amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of BP and water-electrolyte balance. Cardiovascular monitoring (ECG) for 5 days is indicated, as relapse may occur after 48 hours or later. Hemodialysis and forced diuresis are of little use.