Amitriptyline treatment minimum doses. What does Amitriptyline help with? Amitriptyline and products based on it: indications, instructions, reviews

Dosage form: Film-coated tablets are blue, with a biconvex surface, scored on one side.

Before taking this medicine, read the entire leaflet carefully:

Do not throw away this leaflet. You may need to re-read it.

If you have any questions, ask your doctor or pharmacist.

This medicine must be prescribed to you by your doctor. Do not pass it on to others. It can harm them, even if their symptoms are the same as yours.

If any of the side effects become serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

What is Amitriptyline and what is it used for: Each Amitriptyline tablet contains the active substance - amitriptyline hydrochloride, 25 mg, and excipients: lactose, corn starch, dibasic calcium phosphate, gelatin, talc, magnesium stearate, colloidal anhydrous silicon dioxide, polyethylene glycol 6000, Opadry Blue (hydroxypropyl methylcellulose, titanium dioxide (E) 171), talc, polyethylene glycol, brilliant blue (E 133)).

Belongs to the group of antidepressants, has a sedative effect, improves mood, and helps eliminate bedwetting.

Amitriptyline is used in the following cases:

severe depression, especially with characteristic signs of anxiety, agitation and sleep disorders;

nocturnal enuresis in children in the absence of organic pathology.

Do not take Amitriptyline if:

hypersensitivity to amitriptyline or to any of the components of this drug;

angle-closure glaucoma;

disturbance of urodynamics due to prostatic hypertrophy or bladder atony;

recent myocardial infarction, cardiac conduction or rhythm disturbances, coronary artery insufficiency;

simultaneous use with MAO inhibitors, sultopride.

Before prescribing Amitriptyline, be sure to inform your doctor about the following changes in your health:

tendency to develop orthostatic hypotension and sedation during treatment with amitriptyline;

chronic constipation;

prostatic hyperplasia;

diseases of the cardiovascular system;

hypothyroidism, taking thyroid hormone medications;

liver or kidney failure.

When prescribing Amitriptyline, be sure to inform your doctor if you are taking any of the following medications:

Antihypertensives – for the treatment of hypertension;

Atropine and other atropine-like substances (sedative H1-histamine, antiparkinsonian, anticholinergic, antispasmodic atropine drugs, disopyramide, phenothiazine neuroleptics) - for the treatment of allergies, Parkinson's disease, eye diseases, mental disorders.

Central nervous system depressants (morphine derivatives - analgesics, antitussives; barbiturates, benzdiazepines; anxiolytics; sedative antidepressants (doxypine, miaserine, mirtazapine, trimipramine), neuroleptics; sedative H1-antihistamines; centrally acting antihypertensives; thalidomide) - for pain relief, treatment of cough, depression, allergies, hypertension.

Baclofen is a muscle relaxant.

Beta blockers (bisoprolol, carvedilol, metoprolol) – for the treatment of heart diseases.

Combinations of Amitriptyline with certain drugs are undesirable and require medical supervision and dose adjustment of drugs:

Medicines containing alcohol.

Clonidine, guanfacine - for the treatment of hypertension.

Selective MAO inhibitors (moclobemide, toloxatone) – for the treatment of depression.

Linezolid – for the treatment of infections.

Alpha and beta sympathomimetics (epinephrine, norepinephrine, adrenaline, norepinephrine, systemic dopamine for parenteral administration).

Antiepileptic drugs, incl. carbamazepine, valproic acid, valpromide - for the treatment of epilepsy.

Antidepressants - selective serotonin reuptake inhibitors (citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline).

Alpha and beta sympathomimetics (adrenaline, epinephrine as a local hemostatic and for subcutaneous/subbucal injections).

Phenothiazides (thioridazine) – for the treatment of mental disorders.

The combined use of Amitriptyline and the following medications is contraindicated:

Non-selective monoamine oxidase inhibitors (MAO) - for the treatment of depression, anxiety disorders and other diseases.

Sultopride – for the treatment of mental disorders.

Use of Amitriptyline during pregnancy and lactation:

Taking amitriptyline during pregnancy is possible under medical supervision only in cases where the expected benefit to the mother outweighs the possible risk to the fetus. If amitriptyline therapy is necessary to maintain maternal mental health, treatment with the drug at an effective dose can be continued throughout pregnancy. Newborns may experience some side effects that appear in the first days of life and, as a rule, are short-lived and mild. Be sure to warn your doctor about taking amitriptyline: observation and care of newborns is carried out taking into account the above effects.

Amitriptyline passes into breast milk. If treatment with the drug is necessary during lactation, breastfeeding must be interrupted.

The ability of Amitriptyline to influence the control of vehicles and other mechanisms: the drug may reduce the ability to drive a car and use other machinery, which must be taken into account.

The dose of the drug is determined by the doctor. Take during or after meals with water. To improve sleep, the drug can be taken in the evening. The dose is usually increased by taking the drug in the evening or before bed. For maintenance therapy, it can be taken once a day. The withdrawal of the drug is carried out gradually under the supervision of a doctor.

The mark on the tablet is intended solely to facilitate patient administration.

Depression. Treatment begins with low doses and is gradually increased under the close supervision of a physician to assess the effectiveness and tolerability of therapy.

Typically the dose is 75-150 mg per day, higher doses are used in hospital settings. The average daily dose in adults is usually 75 mg (25 mg 3 times a day). After 3 weeks of effective treatment, the daily dose can be revised individually.

In children, the effective daily dose is no more than 1 mg/kg body weight.

Treatment with antidepressants is symptomatic. The duration of treatment is about 6 months to prevent relapse.

Nocturnal enuresis in children. The doses of amitriptyline used for enuresis are lower than those used to treat depression. The daily dose for children aged 6 to 10 years with a body weight of 25 kg or more is 25 mg per day (1 tablet), from 11 to 16 years - 25 - 50 mg per day (1-2 tablets).

The drug is taken before bedtime. The duration of therapy is no more than 3 months.

Special categories of patients. In patients over the age of 65 years, the initial dose should be reduced (to 50% of the minimum). The daily dose can be divided into several doses or taken once before bedtime. If necessary, the dose is increased gradually, under close medical supervision due to the possibility of serious side effects in this category of patients (fainting, confusion). In case of impaired liver and kidney function, careful selection of an individual dose is recommended, which may be reduced compared to patients with normal function of these organs.

If you take a larger dose of Amitriptyline than your doctor recommends: If the number of tablets per day you take exceeds the number recommended by your doctor, or your child swallows the tablets, consult a doctor or call an ambulance immediately! Stop taking the medicine immediately! Symptoms of overdose are likely to include dry mouth, accommodation disorders, tachycardia, heart rhythm disturbances, decreased blood pressure, increased sweating, and urinary retention. Confusion and coma are possible. As first aid, carry out the following measures: gastric lavage, taking an activated carbon suspension, laxatives, maintaining body temperature, monitoring blood pressure, ECG.

If you forget to take your next dose of Amitriptyline: Take the tablet as soon as you remember, making sure there is time before taking the next dose. If there is little time before your next dose, take as directed by your doctor. Do not take a double dose if you miss the next dose!

Possible adverse reactions::

Amitriptyline may cause adverse reactions similar to those that occur with other tricyclic antidepressants. Some of the side effects listed below (headache, tremor, difficulty concentrating, constipation and decreased libido) may also be symptoms of depression and will subside as the depression resolves.

dry mouth, constipation, accommodation disorders, tachycardia, increased sweating, urinary retention;

orthostatic hypotension, decreased sexual function;

drowsiness or sedation, tremor, seizures in susceptible individuals, confusion, loss of consciousness, dysarthria;

risk of developing suicidal behavior/thoughts, mood changes with the onset of a manic episode, manifestations of anxiety;

weight gain;

• disturbance of conduction and heart rhythm (in high doses);

  breast enlargement, milk secretion from the mammary glands;

allergic skin reactions;

• an increase in the number of eosinophils, a decrease in the number of leukocytes and platelets in the blood.

Adverse reactions in elderly patients. In patients aged 50 years and older, an increased risk of bone fractures was found when taking selective serotonin reuptake inhibitors or tricyclic antidepressants. The mechanism of occurrence of this side effect is not clear.

Special precautions when taking Amitriptyline:

Depression is associated with an increased risk of developing suicidal behavior, self-aggression and suicide. Such a risk may exist until stable remission is achieved and may occur spontaneously throughout the course of therapy, especially in the early stages of remission or when the dosage is changed. When treating with antidepressants, it is necessary to carefully monitor your condition, especially at the beginning of therapy: changes in mood, behavior, clinical deterioration and/or the appearance of suicidal thoughts, the development of side effects. Ask your loved ones to help you assess your condition during treatment. If there is any change in condition or doubt in its assessment, please consult a doctor or tell your loved ones!

If insomnia or nervousness occurs at the beginning of treatment, it is recommended to consult a doctor to reduce the dose of the drug and carry out the necessary symptomatic treatment.

In patients suffering from manic-depressive disorders, the course of the disease may worsen. You should stop taking amitriptyline and consult your doctor for appropriate treatment.

In patients with epilepsy while taking amitriptyline, the seizure threshold may be reduced. If seizures develop, amitriptyline should be discontinued. Consult a doctor for appropriate treatment.

When you stop taking the drug, rare signs of withdrawal syndrome are observed (headache, malaise, nausea, anxiety, sleep disturbances), to prevent which a gradual (over several weeks) dose reduction with careful monitoring of the condition is necessary.

The drug is used with caution in elderly patients.

Due to the presence of lactose in the drug, the drug is contraindicated in persons with congenital galactosemia, impaired absorption of glucose and galactose, or lactose deficiency.

Storage conditions:

Store in a place protected from moisture and light at a temperature not exceeding 25C.

Keep out of the reach of children.

Package: 50 tablets in polymer jars or 10 tablets in a blister pack. One can or 5 blister packs together with an insert sheet are placed in a cardboard pack.

Best before date: 3 years.

Vacation conditions: By doctor's prescription

Manufacturer information:

Belarusian-Dutch joint venture limited liability company "Farmland", Republic of Belarus, Minsk region, Nesvizh, st. Leninskaya, 124, building 3

In this article you can read the instructions for use of the drug Amitriptyline. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Amitriptyline in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Amitriptyline analogues in the presence of existing structural analogues. Use for the treatment of depression, psychosis and schizophrenia in adults, children, as well as during pregnancy and lactation. Combination of the drug with alcohol.

Amitriptyline- antidepressant (tricyclic antidepressant). It also has some analgesic (of central origin), antiserotonin effect, helps eliminate bedwetting and reduces appetite.

It has a strong peripheral and central anticholinergic effect due to its high affinity for m-cholinergic receptors; strong sedative effect associated with affinity for H1-histamine receptors and alpha-adrenergic blocking effect.

It has the properties of a class IA antiarrhythmic drug; like quinidine in therapeutic doses, it slows down ventricular conduction (in overdose it can cause severe intraventricular block).

The mechanism of antidepressant action is associated with an increase in the concentration of norepinephrine and/or serotonin in the central nervous system (CNS) (decreasing their reabsorption).

The accumulation of these neurotransmitters occurs as a result of inhibition of their reuptake by the membranes of presynaptic neurons. With long-term use, it reduces the functional activity of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, and restores the balance of these systems, disturbed during depressive states. In anxiety-depressive conditions, it reduces anxiety, agitation and depressive symptoms.

The mechanism of antiulcer action is due to the ability to have a sedative and m-anticholinergic effect. Effectiveness for bedwetting appears to be due to anticholinergic activity leading to increased bladder distensibility, direct beta-adrenergic stimulation, alpha-adrenergic agonist activity leading to increased sphincter tone, and central blockade of serotonin uptake. It has a central analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and an effect on endogenous opioid systems.

The mechanism of action in bulimia nervosa is unclear (may be similar to that in depression). A clear effect of the drug on bulimia has been shown in patients both without depression and in its presence, while a decrease in bulimia can be observed without a concomitant weakening of depression itself.

During general anesthesia, it reduces blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).

The antidepressant effect develops within 2-3 weeks after the start of use.

Pharmacokinetics

Absorption is high. Passes (including nortriptyline, a metabolite of amitriptyline) through histohematic barriers, including the blood-brain barrier, placental barrier, and penetrates into breast milk. Excreted by the kidneys (mainly in the form of metabolites) - 80% in 2 weeks, partially with bile.

Indications

• depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, medicinal, 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 (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, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headaches, migraines (prevention), gastric and duodenal ulcers.

Release forms

Tablets 10 mg and 25 mg.

Dragee 25 mg.

Solution for intravenous and intramuscular administration (injections in injection ampoules).

Instructions for use and dosage

Administered orally, without chewing, immediately after meals (to reduce irritation of the gastric mucosa).

Adults

For adults with depression, the initial dose is 25-50 mg at night, then the dose can be gradually increased, taking into account the effectiveness and tolerability of the drug, to a maximum of 300 mg per day in 3 divided doses (the largest part of the dose is taken at night). When a therapeutic effect is achieved, the dose can be gradually reduced to the minimum effective, depending on the patient's condition. The duration of the course of treatment is determined by the patient’s condition, the effectiveness and tolerability of the therapy and can range from several months to 1 year, and if necessary, more. In old age with mild disorders, as well as with bulimia nervosa, as part of complex therapy for mixed emotional disorders and behavioral disorders, psychoses in schizophrenia and alcohol withdrawal, a dose of 25-100 mg per day (at night) is prescribed, after achieving a therapeutic effect, switch for the minimum effective dose - 10-50 mg per day.

For the prevention of migraines, with chronic pain syndrome of a neurogenic nature (including prolonged headaches), as well as in the complex therapy of gastric and duodenal ulcers - from 10-12.5-25 to 100 mg per day (maximum part of the dose taken at night).

Children

For children as an antidepressant: from 6 to 12 years old - 10-30 mg per day or 1-5 mg/kg per day in fractions, in adolescence - up to 100 mg per day.

For nocturnal enuresis in children 6-10 years old - 10-20 mg per day at night, 11-16 years old - up to 50 mg per day.

Side effect

• blurred vision;
• mydriasis;
• increased intraocular pressure (only in persons with a local anatomical predisposition - a narrow angle of the anterior chamber);
• drowsiness;
• fainting conditions;
• fatigue;
• irritability;
• anxiety;
• disorientation;
• hallucinations (especially in elderly patients and patients with Parkinson's disease);
• anxiety;
• mania;
• memory impairment;
• decreased ability to concentrate;
• insomnia;
• "nightmare" dreams;
• asthenia;
• headache;
• ataxia;
• increased frequency and intensification of epileptic seizures;
• changes in the electroencephalogram (EEG);
• tachycardia;
• feeling of heartbeat;
• dizziness;
• orthostatic hypotension;
• arrhythmia;
• lability of blood pressure (decrease or increase in blood pressure);
• dry mouth;
• constipation;
• nausea, vomiting;
• heartburn;
• gastralgia;
• increased appetite and body weight or decreased appetite and body weight;
• stomatitis;
• change in taste;
• diarrhea;
• darkening of the tongue;
• increase in size (swelling) of the testicles;
• gynecomastia;
• increase in the size of the mammary glands;
• galactorrhea;
• decreased or increased libido;
• decreased potency;
• skin rash;
• photosensitivity;
• angioedema;
• hives;
• hair loss;
• tinnitus;
• swelling;
• hyperpyrexia;
• swollen lymph nodes;
• urinary retention.

Contraindications

• hypersensitivity;
• use together with MAO inhibitors and 2 weeks before starting treatment;
• myocardial infarction (acute and subacute periods);
• acute alcohol intoxication;
• acute intoxication with sleeping pills, analgesics and psychoactive drugs;
• angle-closure glaucoma;
• severe disturbances of AV and intraventricular conduction (bundle branch block, AV block 2 degrees);
• lactation period;
• children under 6 years of age;
• galactose intolerance;
• lactase deficiency;
• glucose-galactose malabsorption.

Use during pregnancy and breastfeeding

In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Use in children

Contraindicated in children under 6 years of age.

In children, adolescents and young adults (under 24 years of age) 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 should be weighed against the benefits of their use

Special instructions

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

Caution is required when suddenly moving to a vertical position from a lying or sitting position.

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

Prescribed no earlier than 14 days after discontinuation of MAO inhibitors, starting with small doses.

If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop.

Amitriptyline in doses above 150 mg per day reduces the threshold of convulsive activity (the risk of epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors predisposing to the occurrence of convulsive syndrome, for example, brain damage of any etiology, simultaneous use of antipsychotic drugs (neuroleptics) ), during the period of withdrawal from ethanol or withdrawal of medications with anticonvulsant properties, for example, benzodiazepines). Severe depression is characterized by a risk of suicidal actions, which can persist until significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or antipsychotic drugs and constant medical supervision (entrust trusted persons with the storage and dispensing of drugs) may be indicated. In children, adolescents and young adults (under 24 years of age) 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 should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. 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 (reducing the dose or discontinuing the drug and prescribing an antipsychotic drug is necessary). After relief of these conditions, if indicated, treatment in low doses can be resumed.

Due to 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 under the condition of careful medical supervision.

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

May cause paralytic ileus, primarily in patients with chronic constipation, the elderly, or those forced to bed rest.

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

Due to the anticholinergic effect, there may be a decrease in tear production 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 long-term use, an increase in the incidence of dental caries is observed. The need for riboflavin may be increased.

Animal reproduction studies have shown adverse effects on the fetus, and there are no adequate and well-controlled studies in pregnant women. In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Passes into breast milk and may cause drowsiness in nursing infants. 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 is gradually discontinued at least 7 weeks before the expected birth.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug interactions

When ethanol (alcohol) is used together with drugs that depress the central nervous system (including other antidepressants, barbiturates, benzadiazepines and general anesthetics), a significant increase in the depressant effect on the central nervous system, respiratory depression and hypotensive effect is possible. Increases sensitivity to drinks containing ethanol (alcohol).

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 used together with anticholinergic blockers, phenothiazine derivatives and benzodiazepines, there is a mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (lowering the threshold of convulsive activity); Phenothiazine derivatives may also increase the risk of neuroleptic malignant syndrome.

When used together with anticonvulsants, it is possible to enhance the inhibitory 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 used together with antihistamines, clonidine - increased inhibitory 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.

With the simultaneous use of amitriptyline and indirect anticoagulants (coumarin or indadione derivatives), the anticoagulant activity of the latter may increase. Amitriptyline may enhance depression caused by glucocorticosteroids (GCS). Medicines used to treat thyrotoxicosis increase the risk of developing agranulocytosis. Reduces the effectiveness of phenytoin and alpha-blockers.

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

Combined use with disulfiram and other acetaldehydrogenase inhibitors provokes delirium.

Fluoxetine and fluvoxamine increase plasma concentrations of amitriptyline (a 50% reduction in amitriptyline dose may be required).

With the simultaneous use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa - a decrease in the hypotensive effect of the latter; with cocaine - the risk of developing cardiac arrhythmias.

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

Pimozide and probucol may increase cardiac arrhythmias, which is manifested by prolongation of the QT interval on the ECG.

It enhances 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 developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.

When co-administered with alpha-adrenergic agonists for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictor effect of the latter may be enhanced.

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

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

When co-administered with other hematotoxic drugs, increased hematotoxicity is possible.

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

Analogues of the drug Amitriptyline

Structural analogues of the active substance:

• Amizol;
• Amirol;
• Amitriptyline Lechiva;
• Amitriptyline Nycomed;
• Amitriptyline-AKOS;
• Amitriptyline-Grindeks;
• Amitriptyline-LENS;
• Amitriptyline-Ferein;
• Amitriptyline hydrochloride;
• Apo-Amitriptyline;
• Vero-Amitriptyline;
• Saroten retard;
• Tryptisol;
• Elivel.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Amitriptyline is a classic tricyclic antidepressant. Due to the fact that it was one of the first to be synthesized, it is often called the “old antidepressant.” However, despite the emergence of a number of more modern drugs, treatment of depression with Amitriptyline is still carried out today. The main advantage of this drug is its pronounced dual action. The medicine is effective not only against depression, but is also widely used in the treatment of chronic pain. However, due to a fairly large number of contraindications, it cannot be considered universal.

The medicine should be taken orally after meals with plenty of water.

Amitriptyline is one of the most prominent representatives of the first generation of antidepressants. It has a direct effect on the nerve cells of the brain, allowing you to suppress anxiety and reduce the severity of depressive conditions.

Important! Unlike a number of analogues, Amitriptyline does not cause hallucinations, and therefore it is often prescribed for migraines and chronic headaches.

The medicine is available in tablet form and as a solution for injection. The tablets are small in size, round in shape and covered with a white coating. The solution appears as a clear liquid that is either colorless or faintly colored.

How does Amitriptyline work?

This drug has a pronounced sedative effect, which is why it is often used to treat depressive conditions. It helps reduce severe emotional arousal and anxiety. In addition, the drug has the following properties:

• antihistamine;
• thymoleptic;
• antiserotonin;
• analgesic;
• anxiolytic;
• antiulcer;
• M-anticholinergic.

Amitriptyline is also used to lower body temperature and blood pressure during general anesthesia.

The effect of taking the drug occurs no earlier than two weeks after the start of its use.

Indications and contraindications

The advisability of taking this drug arises in the following cases:

1. The patient was diagnosed with severe depression. Symptoms of sleep disturbance, emotional overexcitation and anxiety are observed. We can talk about depression caused by mental trauma, alcoholism or organic brain damage.
2. Disorders of mental activity that occur against the background of the development of schizophrenia. Amitriptyline is often used in the treatment of depressive conditions in schizophrenic patients.
3. Mixed emotional disturbances. If the complication of the patient’s mental state was caused by several factors, then this remedy also helps to stabilize the patient’s well-being.
4. Attention disorders, the patient’s inability to carry out any active activity.
5. Bulimia, which is of a nervous nature.
6. Nocturnal enuresis.
7. Chronic pain observed in cancer patients, rheumatic diseases and migraines. Amitriptyline is also prescribed to patients with postherpetic neuralgia, atypical pain in the heart area and neuropathies of various origins.
8. Peptic ulcer of the duodenum and stomach.

This drug has a fairly wide list of contraindications, and therefore its use should be carried out exclusively under the supervision of a doctor.

Taking Amitriptyline is prohibited if you have the following diseases and conditions:

1. Myocardial infarction, which is in an acute form or subacute period of development.
2. Serious problems in the functioning of the heart muscle. We are talking about intraventricular conduction disorders, atrioventricular blockades, etc. The drug should be used with caution in patients with coronary heart disease and arrhythmias.
3. Acute alcohol intoxication.
4. Thyroid diseases.
5. Angle-closure glaucoma.
6. Pregnancy. Prescribing this drug during the 1st and 3rd trimesters is strictly prohibited. In case of emergency, Amitriptyline is taken under medical supervision.
7. Breast-feeding. If Amitriptyline therapy is absolutely necessary, breastfeeding should be discontinued.
8. The presence of acute intoxication with hypnotics, analgesics and psychoactive drugs.

Amitriptyline is not prescribed to children under 6 years of age.

Side effects

When taking the drug, tachycardia and heart rhythm disturbances may occur.

When taking this drug, it is necessary to take into account a number of possible side effects, which manifest themselves as follows:

1. Confusion, weakness and dizziness, fainting.
2. Heart rhythm disturbances, tachycardia.
3. Urinary retention, constipation, development of paralytic intestinal obstruction.
4. Minor weight gain.

Due to the large number of side effects, many doctors use inappropriately low dosages of Amitriptyline in treatment, which results in a significant reduction in the effectiveness of treatment.

In case of overdose, this drug can lead to the development of severe poisoning. Therefore, it is often acquired by people with suicidal tendencies. The doctor’s task in this case is to timely recognize such a patient and prevent death.

The effect of Amitriptyline in the treatment of depressive conditions

This drug can treat the following disorders:

• depression;
• nocturnal bulimia;
• worry and anxiety;
• mental disorders, etc.

To assess the effectiveness of this drug in the fight against depression, one should consider the mechanism of its effect on the body. With the development of depression, a sharp decrease in norepinephrine and serotonin is observed in the patient’s body. This happens because they begin to flow to the brain cells.

The high effectiveness of Amitriptyline in the treatment of depression lies in improving the patient’s mood due to the release of norepinephrine and serotonin from the brain structures. As a result, symptoms of depression are alleviated. If the absorption of neurotransmitters in cells occurs repeatedly, then this no longer affects a person’s mood.

Method of use for depression

The daily dose should be gradually reduced if a positive effect is obtained

Amitriptyline should be taken only if prescribed by a doctor. In most cases, the dosage is calculated individually, taking into account the severity of the disease.

The medicine should be taken orally after meals with plenty of water. Chewing the tablets is prohibited, as this may irritate the stomach walls.

Let's look at how to take Amitriptyline for depression:

1. The initial daily dose is considered to be 50-75 mg. Thus, the drug is taken one tablet (25 mg), twice or thrice a day. A course of treatment of depression with Amitriptyline is carried out until the patient's condition stabilizes.
2. The optimal dose of the drug is 175-200 mg. Moreover, most of this dose is taken at night.
3. If we are talking about the development of severe depression that is not responsive to therapy, then the daily dose can be increased to 300 mg. In some cases, it is possible to take a larger dose of the substance, which is calculated individually for each patient.

In the latter case, the drug is administered by injection. In this case, the initial doses are higher than usual, and their increase occurs at a faster rate. In this case, constant monitoring of the patient’s somatic condition is necessary.

The daily dose should be gradually reduced when a pronounced effect is obtained. If a resumption of depression is observed, it is necessary to return to the original dosage.

If no changes in the patient’s condition are observed in the fourth week of treatment, then further therapy is considered inappropriate. In this case, the doctor prescribes another drug.

Interaction with other drugs

When using Amitriptyline, you should take into account the peculiarities of its interaction with other drugs:

1. Barbiturates, antidepressants and other drugs that depress the central nervous system. When taken simultaneously with Amitriptyline, an increased inhibitory effect on the central nervous system, a hypotensive effect, and depression of respiratory function are observed.
2. Clonidine, antihistamines. The effect is similar to that described above.
3. Phenothiazines, Atropine, antiparkinsonian drugs, antihistamines. An increase in anticholinergic effect is observed, side effects from the bladder, intestines, visual organs and the central nervous system are possible. Paralytic type intestinal obstruction may develop.
4. Anticonvulsants. There is an increase in central nervous system depression and a decrease in the effectiveness of these drugs.
5. Phentothiazines, anticholinergics, benzodiazepines. There is a high risk of developing epileptic seizures, and the patient may develop neuroleptic-type malignant syndrome.
6. Guanethidine, Clonidine, Mutildopa, Reserpine, Betanidine. When taken simultaneously with Amitriptyline, the hypotensive effect of these drugs is reduced.
7. Thyroid hormones. There is a mutual enhancement of both the therapeutic effect and the toxic effect on the patient’s body.
8. Probucol, Pimozide. Severe cardiac arrhythmia may occur.

Analogs

Taken orally immediately after meals (irritates the gastric mucosa), with a small amount of water

If it is impossible to prescribe Amitriptyline to the patient, the doctor may prescribe one of the following analogues:

• Saroten;
• Anafranil;
• Doxepin;
• Novo-Triptin;
• Melipramine.

It should be understood that each of the above drugs has its own side effects and contraindications that should be taken into account when using these drugs.

Amitriptyline is an effective drug whose action is aimed at combating depression. It is depression that often provokes insomnia. If you choose the right dosage, you can cope with chronic insomnia.

Description of the drug

Amitriptyline is an antidepressant drug characterized by analgesic, sedative, anxiolytic, and antiserotonin actions. After taking it, appetite decreases significantly.

This is a remedy against depression. Reduces anxiety, severe emotional arousal, and depressive symptoms. The mechanism of action against depression is due to an increase in the amount of nonadrenaline in synapses.

The effect of the drug begins a couple of weeks after it enters the body. It has an antihistamine, sedative, antiulcer, and M-anticholinergic effect. When performing anesthesia, it lowers blood pressure.

Release form and composition

Amitriptyline is produced in the form of tablets for oral use and as a solution for injection. Available at the pharmacy only with a prescription. The active substance is amitriptyline hydrochloride.

Manufacturers

Manufacturers of Amitriptyline for insomnia:

• Moscow Endocrine Plant;
• Alsi Pharma;
• OZONE;
• DalkhimPharm;
• Zio-Health;
• GreenDex;
• ZENTIVA Czech Republic;
• Synthesis Russia;
• Bryntsalov-A.

Indications for use

Amitriptyline for sleep is indicated in the following cases:

• insomnia;
• bulimia nervosa;
• depression;
• headaches.

Against the background of constant depression and nervousness, insomnia appears.

Contraindications and special instructions

Amitriptyline is contraindicated in:

• hypersensitivity to the components in the composition;
• acute alcohol poisoning;
• angle-closure glaucoma;
• myocardial infarction;
• acute poisoning with sleeping pills.

Since the composition contains lactose monohydrate, it cannot be used in the treatment of people who have a lack of lactose and lactase intolerance. Prescribe therapy with extreme caution to patients suffering from alcoholism, increased intraocular pressure, thyrotoxicosis, hypotension of the bladder, decreased motor function of the intestines and stomach, liver or kidney failure, and bipolar disorders.

Side effects

When taking the medication, some experience a jump in intraocular pressure, vision problems, confusion, constipation, tachycardia, mydriasis, and paralytic ileus.

Acute overdose of the drug entails hallucinations, shortness of breath, increased sweating, ataxia, anxiety, and drowsiness. To combat the symptoms, gastric lavage is performed and symptomatic treatment is prescribed.

Benefits and harms from use

The benefits of Amitriptyline are significant, since the completed course of therapy allows you to cope with depression, anxiety, fears, aggressiveness, and excitability. All of these conditions have an impact on sleep. Due to depression, its quality changes significantly. The drug allows you to normalize sleep, establish a routine, and reduce the number of awakenings. After therapy, the person begins to feel much better.

Negative aspects include the presence of contraindications, as well as possible adverse reactions. Treatment is carried out with special care in elderly patients.

Instructions for use and dosage

Children from 6 to 12 years old take 1 tablet once a day. If necessary, the frequency of application can be increased up to 2 times. The place has the condition of the baby and the symptoms that appear. The maximum daily dosage is 75 mg.

Adults and children over 12 years of age are advised to take 2 tablets three times a day. The doctor can increase the frequency up to 4 times. The maximum daily dose is 350 mg. Both children and adults should take the product during meals or after. Treatment of insomnia should begin with minimal doses.

Attention! You must take the medicine regularly, otherwise there will be no result.

If the product is purchased in the form of a solution, then children over 12 and adults are prescribed 10-30 mg of the drug 2-4 times a day. The maximum permissible dose is 150 mg per day. The drug is administered intramuscularly slowly.

In old age, the drug is used very carefully. At this age, for mild sleep disturbances, 10-50 mg per day is indicated. Taking medication can trigger the onset of drug-induced psychosis, especially at night.

Pregnant women should take the drug only if the expected benefit outweighs the possible risk to the child. The substance passes into breast milk and may therefore cause drowsiness in infants. During treatment it is necessary to discontinue breastfeeding.

Analogs, substitutes and generics

Amitriptyle, as a sleeping pill, has many analogues. The best are:

• Saroten;
• Elivel;
• Amirol;
• Amizol;
• Damilena maleinate.

But only a doctor should select an analogue.

9022 0

Amitriptylme
Antidepressants (tricyclics)

Release form

Dragee 25 mg
Caps. 50 mg
R-r d/in. 20 mg/2 ml
Table 5 mg, 10 mg
Tablet, p.o., 10 mg, 25 mg

Mechanism of action

The mechanism of the antidepressant action of amitriptyline is associated with the inhibition of the reverse neuronal uptake of neurotransmitters by the presynaptic membranes of nerve endings, which increases the concentration of adrenaline and serotonin in the synaptic cleft and activates postsynaptic impulses. With long-term use, amitriptyline normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed in depressive states. In addition, amitriptyline blocks histamine and M-cholinergic receptors. The high affinity for M-cholinergic receptors determines both the central and strong peripheral cholinergic blocking effects of amitriptyline.

Amitriptyline has sedative properties.

Main effects

■ The psychotropic effect develops within 2-3 weeks after the start of use: in anxiety-depressive conditions, anxiety, agitation and depressive symptoms decrease.
■ The effectiveness of drugs for bedwetting is obviously associated primarily with peripheral anticholinergic activity.
■ Amitriptyline has a central analgesic effect, which is believed to be due to changes in the concentration of monoamines in the central nervous system (especially serotonin) and effects on endogenous opioid systems. Potentiates the effect of opioid analgesics.
■ During general anesthesia, amitriptyline reduces blood pressure and body temperature.
■ Reduces the secretion of the salivary glands.
■ A clear effect of drugs has been shown in patients with bulimia, both without and with depression.

Pharmacokinetics

Absorption is high. The bioavailability of amitriptyline through various routes of administration is 30-60%, its main metabolite, nortriptyline, is 46-70%. Connection with plasma proteins is up to - 96%, the maximum plasma concentration of 0.04-0.16 mcg/ml is achieved 2.0-7.7 hours after oral administration. At equal doses, when taking capsules, the maximum concentration is lower than when using tablets, which causes less cardiotoxic effect. Volume of distribution - 5-10 l/kg. Therapeutic blood concentrations for amitriptyline are 50-250 ng/ml, for nortriptyline - 50-150 ng/ml. Both compounds easily pass through histohematic barriers, including the blood-brain and placental barriers, and penetrate into breast milk.

Amitriptyline is metabolized in the liver with the participation of the enzyme system of cytochromes CYP2C19, CYP2D6, undergoes the processes of demethylation, hydroxylation and N-oxidation, with the formation of active metabolites (nortriptyline, 10-hydroxy-amitriptyline) and inactive compounds. Has a “first pass” effect through the liver. Within 2 weeks, 80% of the administered dose is excreted mainly in the form of metabolites by the kidneys, partially in the feces. T1/2 of amitriptyline - 10-26 hours, nortriptyline - 18-44 hours.

Indications

■ Amitriptyline is effective in patients with chronic pain (especially chronic neurogenic pain: postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathies).
■ Headache and migraine (prevention).
■ Depression, especially with anxiety, agitation and sleep disorders of various natures (endogenous, involutional, reactive, neurotic, medicinal, with organic brain damage, with alcohol withdrawal), the depressive phase of manic-depressive psychosis, schizophrenic psychoses, mixed emotional disorders.

Directions for use and doses

Amitriptyline is prescribed orally, intramuscularly and intravenously.

For the prevention of migraines, for chronic pain of a neurogenic nature (including long-term headaches) - from 12.5-25 to 100 mg per day (the maximum dose is taken at night).

Contraindications

■ Hypersensitivity.
■ Angle-closure glaucoma.
■ Epilepsy.
■ Prostatic hyperplasia.
■ Atony of the bladder.
■ Paralytic ileus, pyloric stenosis.
■ History of myocardial infarction.
■ Combined use with MAO inhibitors.
■ Pregnancy.
■ Lactation period.
■ Children under 6 years of age (for injection forms - 12 years).

Restrictions on use:
■ coronary heart disease due to tachycardia;
■ arterial hypertension;
■ peptic ulcer of the stomach and duodenum;
■ anxiety-paranoid syndrome with depression (due to the risk of suicide).

Cautions, therapy monitoring

Before starting treatment, it is necessary to determine blood pressure (in patients with low or labile blood pressure, it may decrease even more).

During treatment, the peripheral blood picture should be monitored (in some cases, agranulocytosis may develop); during long-term therapy, monitoring the functional state of the liver.

In elderly people and in patients with cardiovascular diseases, monitoring of heart rate (HR), blood pressure, and electrocardiography readings is indicated. Clinically insignificant changes may appear on the electrocardiogram (smoothing of the T wave, depression of the S-T segment, widening of the QRS complex).

Parenteral use should be carried out only in a hospital setting, under the supervision of a physician, with bed rest in the first days of therapy. Caution should be exercised when suddenly moving to a vertical position from a lying or sitting position.

During the treatment period, ethanol consumption is unacceptable.

Amitriptyline is prescribed no earlier than 14 days after discontinuation of monoamine oxidase inhibitors. It should be taken into account that the therapeutic activity and severity of adverse reactions of amitriptyline are influenced by drugs of many pharmacological groups (see “Interaction”).

If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop.

In predisposed patients and elderly patients, amitriptyline can provoke the development of drug-induced psychoses, mainly at night (after drug withdrawal, they subside within a few days).

Amitriptyline can cause paralytic ileus, mainly in patients with chronic constipation, in the elderly or in patients forced to remain in bed.

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

The anticholinergic effect leads to a decrease in salivary secretion and dry mouth. With long-term use, an increase in the incidence of dental caries is observed. There is a decrease in tear production 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.

The need for riboflavin may increase.

Amitriptyline passes into breast milk and may cause drowsiness in nursing infants.

Children are more sensitive to acute overdose, which is dangerous and potentially fatal for them.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Prescribe with caution when:
■ chronic alcoholism;
■ bronchial asthma;
■ inhibition of bone marrow hematopoiesis;
■ stroke;
■ schizophrenia (possible activation of psychosis);
■ liver and/or kidney failure;
■ thyrotoxicosis.

Side effects

Anticholinergic cholinergic blocking effects:
■ dry mouth;
■ blurred vision;
■ paralysis of accommodation;
■ mydriasis;
■ increased intraocular pressure (only in persons with a local anatomical predisposition - a narrow angle of the anterior chamber);
■ tachycardia;
■ confusion;
■ delirium or hallucinations;
■ constipation, paralytic intestinal obstruction;
■ difficulty urinating;
■ decreased sweating.

From the nervous system:
■ drowsiness;
■ asthenia;
■ fainting;
■ anxiety;
■ disorientation;
■ hallucinations (especially in elderly patients and patients with Parkinson's disease);
■ anxiety;
■ excitement;
■ motor restlessness;
■ manic state, hypomanic state;
■ aggressiveness;
■ memory impairment, depersonalization;
■ increased depression;

■ insomnia, “nightmare” dreams;
■ yawning;
■ asthenia;
■ activation of symptoms of psychosis;
■ headache;
■ myoclonus;
■ dysarthria;
■ tremors of small muscles, especially the arms, hands, head and tongue;
■ peripheral neuropathy (paresthesia);
■ myasthenia gravis;
■ ataxia;
■ extrapyramidal syndrome;
■ increased frequency and intensification of convulsive seizures;
■ changes in the electroencephalogram.

■ tachycardia;
■ heartbeat;
■ dizziness;
■ orthostatic hypotension;
■ nonspecific changes in the electrocardiogram (S-T interval or T wave) in patients who do not suffer from heart disease; arrhythmia; blood pressure lability; intraventricular conduction disturbance (widening of the QRS complex, changes in the P-Q interval, bundle branch block).

From the digestive system:
■ nausea.

Rarely:
■ darkening of the tongue;
■ increased appetite and body weight or decreased appetite and body weight;
■ stomatitis, change in taste (sour-bitter taste in the mouth);
■ hepatitis (including liver dysfunction and cholestatic jaundice);
■ heartburn;
■ vomiting;
■ gastralgia;
■ diarrhea.

From the endocrine system:
■ hypo- or hyperglycemia;
■ impaired glucose tolerance;
■ diabetes mellitus;
■ hyponatremia (decreased vasopressin production);
■ syndrome of inappropriate secretion of antidiuretic hormone.

From the reproductive system:
■ increase in size (swelling) of the testicles;
■ gynecomastia;
■ increase in the size of the mammary glands;
■ disturbances or delay in ejaculation;
■ decrease or increase in libido;
■ decreased potency.

From the blood system:
■ agranulocytosis;
■ leukopenia;
■ thrombocytopenia;
■ purpura;
■ eosinophilia.

Allergic reactions:
■ skin rash;
■ itching of the skin;
■ urticaria;
■ photosensitivity;
■ swelling of the face and tongue.

Other effects:
■ hair loss;
■ tinnitus;
■ swelling;
■ hyperpyrexia;
■ enlarged lymph nodes;
■ urinary retention;
■ pollakiuria;
■ hypoproteinemia.

Local reactions (with intravenous administration):
■ thrombophlebitis;
■ lymphangitis;
■ burning sensation;
■ skin reactions.

Overdose

Symptoms: effects develop 4 hours after an overdose, reach a maximum after 24 hours and last 4-6 days. If an overdose is suspected, especially in children, the patient should be hospitalized.

From the side of the central nervous system:
■ drowsiness;
■ stupor;
■ coma;
■ ataxia;
■ hallucinations;
■ anxiety;
■ psychomotor agitation;
■ decreased ability to concentrate;
■ disorientation;
■ confusion;
■ dysarthria;
■ hyperreflexia;
■ muscle rigidity;
■ choreoathetosis;
■ seizures.

From the cardiovascular system:
■ decrease in blood pressure;
■ tachycardia;
■ arrhythmia;
■ violation of intracardiac conduction;
■ changes in the electrocardiogram (especially QRS) characteristic of intoxication with tricyclic antidepressants;
■ shock, heart failure; in very rare cases - cardiac arrest.

Others:
■ respiratory depression;
■ shortness of breath;
■ cyanosis;
■ vomiting;
■ mydriasis;
■ increased sweating;
■ oliguria or anuria.

Treatment: gastric lavage, administration of activated carbon, laxatives (overdose when taken orally); symptomatic and supportive therapy; for severe symptoms caused by blockade of cholinergic receptors, administration of cholinesterase inhibitors (the use of physostigmine is not recommended due to the increased risk of seizures); maintaining body temperature, blood pressure and water-electrolyte balance.

Monitoring the functions of the cardiovascular system for 5 days (relapse may occur after 48 hours or later), anticonvulsant therapy, artificial ventilation and other resuscitation measures are indicated. Hemodialysis and forced diuresis are ineffective.

Interaction

Synonyms

Amizol (Slovenia), Amirol (Cyprus), Adepren (Bulgaria), Amineurin (Germany), Amiton (India), Amitriptyline (Germany, Indonesia, Poland, Slovak Republic, France, Czech Republic), Amitriptyline Lechiva (Czech Republic), Amitriptyline Nycomed (Norway), Amitriptyline-AKOS (Russia), Amitriptyline-Grindeks (Latvia), Amitriptyline-LENS (Russia), Amitriptyline-Slovakofarm (Slovak Republic), Amitriptyline-Ferein (Russia), Apo-Amitriptyline (Canada), Vero- Amitriptyline (Russia), Novo-Triptin (Canada), Sarotene (Denmark), Sarotene retard (Denmark), Triptisol (India), Elivel (India)

G.M. Barer, E.V. Zoryan