Amitriptyline pills 25mg, 50pcs

Composition

of 1 tab. amitriptyline hydrochloride 28.3 mg, which corresponds to an amitriptyline content of 25 mg

Excipients: lactose monohydrate, corn starch, gelatin, calcium stearate, talc, colloidal silicon dioxide.

Shell composition:  simethicone SE-2, macrogol, Sepifilm 3048 yellow (Sepifilm 3048 Yellow) (hypromellose, microcrystalline cellulose, polyoxyl 40 stearate, titanium dioxide, quinoline yellow dye (E 104).

Pharmacological action

An antidepressant

Indications

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

As part of complex therapy, it is used for mixed emotional disorders, psychoses in schizophrenia, alcohol withdrawal, behavioral disorders (activity and attention), nocturnal enuresis in children (except for patients with hypotension of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraines, rheumatic diseases, atypical facial pain, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headaches, migraines (prevention), peptic ulcer of the stomach and duodenum 12.

Contraindications

• Hypersensitivity,
• the application together with MAO inhibitors and 2 weeks before treatment,
• myocardial infarction (acute and subacute periods),
• acute alcohol intoxication,
• acute intoxication hypnotic, analgesic and psychoactive drugs,
• angle-closure glaucoma,
• severe AV-and intraventricular conduction (blockade of the legs of bundle branch block, AV blockade of II degree),
• lactation,
• children up to age 6 years.

Due to the content of lactose monohydrate (milk sugar), the drug should not be taken by patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

With caution

, Amitriptyline should be used with caution in people with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, with suppression of bone marrow hematopoiesis, diseases of the cardiovascular system (CVS) (angina pectoris, arrhythmia, heart block, chronic heart failure, myocardial infarction, arterial hypertension), intraocular hypertension, stroke, decreased motor function of the gastrointestinal tract (GIT) (risk of paralytic intestinal obstruction), liver and/or kidney failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, hypotension of the bladder, during pregnancy (especially I trimester), in the elderly.

Side effects

Mainly associated with the holinoblocking effect of the drug: paresis of accommodation. Blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, urinary retention, fever. All these phenomena usually disappear after adaptation to the drug or reduction of doses. From the central nervous system:  headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremor, paresthesia, peripheral neuropathy, changes in the EEG. Rarely-extrapyramidal disorders, seizures, anxiety. From the cardiovascular system:  tachycardia, arrhythmia, conduction disorders, lability of blood pressure, expansion of the QRS complex on the 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, epigastric discomfort, gastralgia, increased activity of “hepatic” transaminases, rarely cholestatic jaundice, diarrhea. From the endocrine system:  breast enlargement 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, testicular edema. Allergic reactions:  skin rash, pruritus, photosensitivity, angioedema, urticaria. Other services:  agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, enlarged lymph nodes, increased body weight with prolonged use, sweating, pollakiuria. With prolonged treatment, especially in high doses, with abrupt discontinuation of treatment, withdrawal syndrome may develop: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with bright, unusual dreams, increased excitability.

Interaction

With the combined use of ethanol and drugs that depress the central nervous system (including other antidepressants, barbiturates, benzadiazepines and general anesthetics), a significant increase in the depressive effect on the central nervous system, respiratory depression and hypotensive effect is possible.

Increases sensitivity to drinks containing ethanol.

Increases the anticholinergic effect of drugs with anticholinergic activity (for example, phenothiazine derivatives, antiparkinsonian drugs, amantadine, atropine, biperiden, antihistamines), which increases the risk of side effects (from the central nervous system, vision, intestines and bladder). When combined with holinoblokatorami, phenothiazine derivatives and benzodiazepines-mutual strengthening of sedative and central holinoblokiruyushchy effects and increased risk of epileptic seizures (lowering the threshold of convulsive activity); phenothiazine derivatives, in addition, may increase the risk of neuroleptic malignant syndrome.

When combined with anticonvulsant drugs, it is possible to increase the depressing effect on the central nervous system, reduce the threshold of convulsive activity (when used in high doses) and reduce the effectiveness of the latter.

When combined with antihistamines, clonidine-increased depressive effect on the central nervous system; with atropine-increases the risk of paralytic intestinal obstruction; with drugs that cause extrapyramidal reactions-an increase in the severity and frequency of extrapyramidal effects.

Concomitant use of amitriptyline and indirect anticoagulants (coumarin or indadione derivatives) may increase the anticoagulant activity of the latter.

Amitriptyline may increase depression caused by glucocorticosteroids (corticosteroids).

Drugs for the treatment of thyrotoxicosis increase the risk of agranulocytosis.

Reduces the effectiveness of phenytoin and alpha-blockers.

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

Combined use with disulfiram and other acetaldehydrogenase inhibitors provokes delirium.

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

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

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

Antiarrhythmic drugs (such as quinidine) increase the risk of rhythm disorders (possibly slowing down the metabolism of amitriptyline).

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

Increases the effect of epinephrine, norepinephrine, isoprenaline, ephedrine, and phenylephrine on the cardiovascular system (including when these drugs are part of local anesthetics) and increases the risk of heart rhythm disorders, tachycardia, and severe arterial hypertension.

When co-administered with alpha-adrenomimetics for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictive effect of the latter may increase.

When taken together with thyroid hormones, there is a mutual enhancement of the therapeutic effect and toxic effect (including cardiac arrhythmias and a stimulating effect on the central nervous system).

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

When co-administered with other hematotoxic drugs, it is possible to increase hematotoxicity.

Incompatible with MAO inhibitors (may increase the frequency of periods of hyperpyrexia, severe seizures, hypertensive crises and death of the patient).

How to take it, course of administration and dosage

Assign inside (during or after a meal). The initial daily dose when taken orally 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 part of the dose is taken at night). For severe depressionpatients who are resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose (the maximum dose for outpatient patients is 150 mg/day). In these cases, it is advisable to start treatment with intramuscular or intravenous use of the drug, using higher initial doses, accelerating the increase in dosages under the control of the somatic state. After receiving a persistent antidepressant effect after 2-4 weeks, the dose is gradually and slowly reduced to 50-100 mg / day and continue therapy for at least 3 months. In case of signs of depression when reducing the dose, 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, doses are 25-50-100 mg per day in divided doses or 1 time per day at night.

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

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

For severe depressionthat is resistant to therapy: intramuscularly or intravenously (administered slowly!) enter a dose of 10-20-30 mg up to 4 times a day, increasing the dose should be carried out gradually, the maximum daily dose is 150 mg; after 1-2 weeks, switch to taking the drug inside. Children over 12 years of age and the elderly are given lower doses and increase them more slowly. If the patient’s condition does not improve within 3-4 weeks of treatment, then further therapy is impractical.

Overdose

Symptoms: drowsiness, disorientation, confusion, dilated pupils, fever, dyspnea, dysarthria, agitation, hallucinations, seizures, muscle stiffness, constipation, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression. Treatment: 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 indicated, since relapse can occur in 48 hours or later. Hemodialysis and forced diuresis are not very effective.

Special instructions

Before starting treatment, blood pressure monitoring is necessary (in patients with low or labile blood pressure, it may decrease even more); during treatment, peripheral blood monitoring (in some cases, agranulocytosis may develop, and therefore it is recommended to monitor the blood picture, especially with an increase in body temperature, the development of flu-like symptoms and angina), with long-term therapy – monitoring of CVD and liver functions. In the elderly and patients with cardiovascular diseases, monitoring of heart rate (HR), blood pressure, and ECG is indicated. On the ECG, clinically insignificant changes may occur (smoothing of the T wave, depression of the S-T segment, expansion of the QRS complex).

Caution should be taken when suddenly moving to the vertical position from the “lying” or “sitting” position.

During the treatment period, the use of ethanol should be excluded.

Assign no earlier than 14 days after the withdrawal of MAO inhibitors, starting with small doses.

If you suddenly stop taking medication after prolonged treatment, you may develop a “withdrawal”syndrome.

Amitriptyline in doses above 150 mg/day lowers the threshold of convulsive activity (note the risk of epileptic seizures in susceptible patients, as well as in the presence of others predisposing to seizures factors, such as brain injury of any etiology, concomitant use of antipsychotic drugs (neuroleptics), in the period of refusal or cancellation of ethanol drugs possessing anticonvulsant properties, such as benzodiazepines).

Severe depressions are characterized by the risk of suicidal actions, which may persist until significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or neuroleptic drugs and constant medical monitoring (entrust trusted persons with the storage and delivery of drugs) may be indicated.

In children, adolescents, and young adults (under 24 years of age) with depression, etc. antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing amitriptyline or any other drugs. antidepressants in this category of patients should be correlated with the risk of suicide and the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, and in people over 65 years of age it decreased slightly. During treatment with antidepressants, all patients should be monitored for early detection of suicidal tendencies.

In patients with cyclic affective disorders during the depressive phase, manic or hypomanic states may develop during therapy (it is necessary to reduce the dose or cancel the drug and prescribe an antipsychotic drug). After stopping these conditions, if there are indications, treatment in low doses can be resumed.

Due to possible cardiotoxic effects, caution should be exercised when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.

In combination with electroconvulsive therapy, it is prescribed only under the condition of careful medical supervision.

In predisposed patients and elderly patients, it can provoke the development of drug psychoses, mainly at night (after discontinuation of the drug, they pass within a few days).

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

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

Due to the anticholinergic effect, it is possible to reduce lacrimation and a relative increase in the amount of mucus in the tear fluid, which can lead to damage to the corneal epithelium in patients using contact lenses.

With prolonged use, there is an increase in the frequency of dental caries. The need for riboflavin may be increased.

Animal reproduction studies have shown an adverse effect on the fetus, and no adequate and strictly controlled studies have been conducted in pregnant women. In pregnant women, the drug should only be used if the intended benefit to the mother exceeds the potential risk to the fetus.

Penetrates into breast milk and may cause drowsiness in infants.

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

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

During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a dry place, protected from light, out of reach of children, at a temperature of 15 to 25 about C.

Shelf

life is 3 years.

Active ingredient

Amitriptyline

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 6 years of age

Indications

Migraine, Enuresis, Depression