Amitriptyline: indications for use, side effects

Compound

Amitriptyline dragees and tablets contain 10 or 25 mg of the active substance in the form of amitriptyline hydrochloride.
Additional substances in the tablets are: microcrystalline cellulose, talc, lactose monohydrate, silicon dioxide, magnesium stearate, pregelatinized starch.

Additional substances in the dragees are: magnesium stearate, potato starch, talc, polyvinylpyrrolidone, lactose monohydrate.

1 ml of solution contains 10 mg of active substance. Additional substances are: hydrochloric acid (sodium hydroxide), dextrose monohydrate, water for infusion, sodium chloride, benzethonium chloride.

"Amitriptyline": main characteristics

The main component of the drug is the substance of the same name, amitriptyline (for better absorption, it is presented in the form of hydrochloride). Available in 3 forms:

1. Tablets (each containing 10 mg or 25 mg of amitriptyline).
2. Dragee (same dosage).
3. Solution for injections (10 mg of amitriptyline per 1 ml volume).

According to its effects on the body, it is classified as a tricyclic antidepressant. Gives a sedative and thymoleptic effect, also acts as an analgesic (as an additional remedy).

Tablets, dragees and containers with solutions are dispensed only with a prescription. They are stored under normal room conditions (temperature no higher than 25 degrees, moderate humidity) within the general shelf life (3 years from the date of production).

Pharmacodynamics and pharmacokinetics

The drug reduces appetite, eliminates nighttime urinary incontinence, and has an antiserotonin effect. The drug has a strong central and peripheral anticholinergic effect.

The antidepressant effect is achieved by increasing the concentration of serotonin in the nervous system and norepinephrine in synapses. Long-term therapy leads to a decrease in the functional activity of serotonin and beta-adrenergic receptors in the brain. Amitriptyline reduces the severity of depressive symptoms, agitation, anxiety in anxiety-depressive conditions . By blocking H2-histamine receptors in the stomach wall (parietal cells), an antiulcer effect is provided. The medication is able to reduce body temperature and blood pressure during general anesthesia. The drug does not inhibit monoamine oxidases. The antidepressant effect appears after 3 weeks of therapy.

The maximum concentration of the substance in the blood occurs after a few hours, usually after 2-12. Excreted as metabolites in urine. Binds well to proteins.

Choosing an antidepressant based on effectiveness and tolerability

Summary

A classification of side effects of antidepressants is presented. Side effects may be toxic or neuronal. Neuronal side effects are divided into “non-therapeutic” (persistent or reversible) and “para-therapeutic” side effects. Seven categories of antidepressant tolerability have been defined. The lowest category VII included clomipramine, imipramine, maprotiline, agomelatine. Category VI includes amitriptyline, V - pipofezin, trazodone, mianserin and mirtazapine, IV - vortioxetine, III - venlafaxine and duloxetine, II - sertraline, paroxetine, citalopram, escitalopram, fluoxetine, fluvoxamine and milnacipran, I - pirlindole and moclobemide. Among the most effective antidepressants (amitriptyline, imipramine, venlafaxine in high daily doses), venlafaxine had the best tolerability category. This drug is the most effective and tolerable antidepressant. Other options for the practical use of classifications are discussed.

Summary

A classification of the side effects of antidepressants is presented. Side effects can be toxic or neuronal. Neuronal side effects are divided into “extratherapeutic” (persistent or reversible), as well as “paratherapeutic”. Seven antidepressant tolerance categories have been identified. The lowest category VII included clomipramine, imipramine, maprotiline, agomelatine. Amitriptyline belongs to the VI category, pipofezin, trazodone, mianserin and mirtazapine to the V category, vortioxetine belongs to the IV category, venlafaxine and duloxetine to the III category, sertraline, paroxetine, citalopram, escitalopram, fluoxetine, fluvoxamine and milnacipran to the II category, and pirlindole and moclobemide to the I category. Among the most effective antidepressants (amitriptyline, imipramine, venlafaxine in high daily doses), venlafaxine was in the best category of tolerance. This drug is the most effective and tolerable antidepressant. Other options for the practical use of classifications are discussed.

The previous article presented a description of the mechanism of action of various antidepressants (tricyclic - TcA, sertonin-modulating - SMA, tetracyclic - CtsA, reversible inhibitors of monoamine oxidase type "A" - OIMAO-A, selective serotonin reuptake inhibitors - SSRIs, selective serotonin and norepinephrine reuptake inhibitors – SNRIs, norepinephrine and selective serotonin – NaSSA, melatonergic – MeA, multimodal – MmA) (Table 1).

Table 1. Antidepressants known in Russia, their effect on neurons and the “formula” of the mechanism of action (1-4).

* - white color - the drug does not affect neurons, dark gray - a pronounced increase in activity, light gray - a moderate increase in activity, ** - in high doses, IOR - neurotransmitter reuptake inhibitors, SVRR - agents affecting regulatory receptors, OIMAO-A are reversible inhibitors of monoamine oxidase type “A”.

All these drugs, to varying degrees, contribute to the activation of serotonin (↑C or ↑c), norepinephrine (↑H or ↑n), dopamine (↑D or ↑d) or melatonin (↑M or ↑m) neurons, the “tone” of which decreases for depression. But the most pronounced effect on the vital activity of neurons is ↑SNd antidepressants: amitriptyline and imipramine (TcA), as well as venlafaxine (SNRI) in high daily doses. It is no coincidence that many experts consider them to be the most effective drugs for treating depression (5).

Of course, the choice of any antidepressant should be related not only to its therapeutic properties (efficacy), but also to side effects (tolerability). The vast majority of authors agree that tolerability is best with SSRIs and worse with TCAs (6–9), with other drugs falling in between (1). This assessment of the tolerability of antidepressants is correct, but is of a generalized nature. To clarify it, you should refer to data on the mechanisms of side effects.

A minority of them are due to the toxic effect of antidepressants on the organs and tissues of patients. These “toxic” side effects are very dangerous (10). For example, while taking some TCAs (clomipramine, imipramine), as well as MeA (agomelaptine), drug-induced hepatitis is observed, which leads to the death of patients (10, 11). Maprotiline also has serious toxic side effects, causing agranulocytosis and leukopenia (12). Fortunately, toxic side effects are very rare and can be detected promptly by test results.

For example, when it was discovered that agomelatine causes severe and drug-induced hepatitis, detailed precautions were added to its instructions (11). They include a biochemical blood test, which is prescribed to all patients (without exception) before prescribing the drug, as well as while taking it. Similar analysis is required in patients receiving clomipramine and imipramine (13,14). However, when prescribing these antidepressants, biochemical analysis is required only for patients with existing liver diseases. Finally, regular general blood tests to detect agranulocytosis and leukopenia are also necessary during maprotiline treatment (12).

Obviously, the need for additional tests can significantly complicate the use of antidepressants. Fortunately, this is only required when using the medications listed. When prescribing other antidepressants, there is no need to resort to additional examinations. However, their tolerability may be impaired due to the drugs' adverse effects on neurons. As a result, “neural” side effects are formed, which, however, do not directly threaten the lives of patients and are easily diagnosed based on their complaints.

Some of the neuronal side effects are due to the effect of the antidepressant on histamine and acetylcholine neurons, which do not reduce their activity in the formation of mental disorders that are indications for the prescription of antidepressants (2,15). Accordingly, such pharmacological properties can be designated as “non-therapeutic” (extra, unrelated to the treatment process) side effects. They only increase the number of neuronal systems that the patient suffers. Most often, “non-medicinal” side effects are persistent. They may occur throughout the course of treatment, particularly when the antidepressant blocks excitatory receptors on histamine and acetylcholine neurons (15).

This mechanism of action, characteristic of neuroleptics rather than antidepressants, leads to a sharp drop in the activity (inhibition) of these nerve cells (↓G and ↓A) (1,2). Moreover, normal histamine and acetylcholine neurons cannot restore their functions, since there are no effective compensatory mechanisms for this. Accordingly, patients develop persistent mental and somatic symptoms, which seriously complicate treatment (Table 2).

Table 2. The main “non-therapeutic” side effects of antidepressants associated with the blockade of excitatory receptors on histamine and acetylcholine neurons (1,2)

Characterized by drowsiness, fatigue, deterioration of memory and attention. There are complaints of dry mouth, disturbances of accommodation and urination, constipation, pain in the eyes due to increased intraocular pressure, heart rhythm disturbances, increased appetite and weight gain.

There is, however, an antidepressant whose “non-medicinal” side effects are not persistent. This drug is vortioxetine. It does not inhibit histamine and acetylcholine neurons (due to blockade of excitatory receptors), but increases their “tone” due to its influence on regulatory receptors (16). On the one hand, this provides vortioxetine with a unique nature of “non-therapeutic” side effects. In particular, when taking this antidepressant, agitation, anger, “unusual” dreams, and insomnia may occur (Table 3).

Table 3. “Non-medicinal” side effects of vortioxetine (16,17).

Characterized by ketoacidosis, somatic complaints of dizziness, itching (including generalized), sweating, hot flashes, nausea, diarrhea, vomiting. On the other hand, these side effects are fundamentally reversible, since neurons have special mechanisms that are aimed at combating excessive activation. To do this, they can, for example, reduce the sensitivity of their regulatory receptors (a mechanism known as autoregulation). Therefore, “non-therapeutic” side effects of vortioxetine often reduce spontaneously in the first two weeks of treatment (16).

Moving now to the rest of the antidepressants, we point out that the vast majority of them do not have any “non-therapeutic” side effects that increase the number of affected neuronal systems (2). Many drugs do not affect histamine and acetylcholine neurons. Moreover, they increase the activity of only those neurons (serotonin, norepinephrine and dopamine) whose “tone” decreases in mental disorders that are indications for the prescription of antidepressants. However, even this feature cannot relieve antidepressants from “neural” side effects. The latter will arise due to the fact that within any affected neuronal system, the activity of only part of the nerve cells decreases, while the functions of the other part are not impaired. Antidepressants both activate “damaged” neurons and create therapeutic effects, and increase the “tone” of normally functioning nerve cells and cause side effects.

At the same time, the tolerability of antidepressants paradoxically turns out to be “hostage” to their therapeutic properties. The more effectively the drug activates the affected neurons, the more it affects similar nerve cells that are still functioning at the proper level. Therefore, it is advisable to designate the side effects under consideration as “paratherapeutic”. They are manifested by restlessness, restlessness, insomnia and anxiety (Table 4).

Table 4. Main “paramedical” side effects of antidepressants (15)

Somatic complaints are represented by sexual dysfunction, disruption of the digestive system and heart rhythm, and fluctuations in blood pressure. As a rule, “paratherapeutic” side effects are reversible. They may resolve on their own in the second or third week of treatment (18). This is due to the already noted above ability of “normal” neurons to quickly adapt to excessive activation, reducing their sensitivity to neurotransmitters (2)2.

The presented data on toxic and neuronal side effects can be used to classify antidepressants into seven tolerability categories, with the seventh being the worst and the first being the best (Table 5).

Table 5. Categories of tolerability of antidepressants, taking into account toxic and neuronal side effects.

Thus, antidepressants from the lowest category VII (clomipramine, imipramine, maprotiline, agomelatine) have toxic side effects that directly threaten the lives of patients. Moreover, when prescribing them, additional examination of patients is required. Problems with tolerability of other antidepressants are due to neuronal side effects. All of them are not fatal, and their identification usually does not require additional examination.

Neuronal side effects are divided into “non-therapeutic” and “para-therapeutic” side effects. The first, as already mentioned above, are associated with “additional” dysfunction of histamine and acetylcholine neurons, which do not reduce their activity in mental disorders that are indications for the prescription of antidepressants. Accordingly, “non-therapeutic” side effects that expand the range of affected neuronal systems determine whether drugs belong to lower tolerability categories (VI, V and IV). In particular, amitriptyline promotes a persistent decrease in the activity of histamine and acetylcholine neurons and is therefore classified as tolerability category VI. “Non-therapeutic” side effects of antidepressants classified as category V are more limited. After all, pipofezin, trazodone, mianserin and mirtazapine contribute to a persistent decrease in the activity of only histamine neurons. Vortioxetine is classified into the next higher tolerability category IV. This antidepressant has the ability to increase the activity of histamine and acetylcholine neurons. However, the associated side effects are often reversible.

The highest tolerability categories I – III include antidepressants that act only on serotonin, norepinephrine and dopamine neurons, which suffer in mental disorders that are indications for prescribing drugs. These drugs are characterized by “paratherapeutic” side effects that do not increase the number of affected neuronal systems (Table 5). They arise due to the activation of part of the serotonin, norepinephrine and dopamine neurons, which still maintain normal “tone” (2). At the same time, the severity of “paratherapeutic” side effects depends, first of all, on the ability of the antidepressant to affect serotonin and norepinephrine nerve cells, since they all have a weak effect on dopamine nerve cells (Table 1).

Accordingly, tolerability category III includes antidepressants that simultaneously effectively activate serotonin and norepinephrine neurons. These drugs are venlafaxine and duloxetine (Tables 1 and 5). The first of them, depending on the dose, is a ↑SN- or ↑SNd-antidepressant. As for duloxetine, it has the properties of a ↑CH drug. Category II includes antidepressants that promote pronounced activation of only serotonin or only norepinephrine neurons (Tables 1 and 5). These include all ↑C-antidepressants (sertraline, paroxetine, citalopram, escitalopram, fluoxetine, fluvoxamine), as well as the ↑sND antidepressant – milnacipran. Finally, the highest category I of tolerability is possessed by drugs that are not capable of strongly activating serotonin and norepinephrine neurons (Tables 1 and 5). These are two ↑SND antidepressants - pirlindole and moclobemide.

In conclusion, it should be noted that the presented classification of antidepressants by tolerability does not pretend to be comprehensive. However, it provides clear criteria for assessing the main side effects, which allow different drugs to be compared with each other. This seems to be especially significant in a situation where there are no clear recommendations for taking into account side effects when prescribing antidepressants. For example, a generalized formula is currently used in various publications and instructions. It is recommended that an antidepressant be used “only after a careful assessment of the expected benefits versus risks in patients” (11). But the results of such a “careful assessment” are usually in favor of prescribing the drug.

In particular, about agomelatine they write that if all the requirements of the instructions for prescribing an antidepressant are met, then the risk of developing drug-induced hepatitis becomes minimal (19). At the same time, the unique mechanism of action attributed to agomelatine allows us to state that the benefits of prescribing an antidepressant are much greater than the certain inconveniences that are associated with its hepatotoxicity (19). Meanwhile, the uniqueness of the mechanism of action of agomelatine comes down to the possibility of influencing the neurons of the suprachiasmatic nucleus, the neurotransmitter of which is melatonin. And this effect is not at all required for the treatment of depression, since any antidepressant that activates serotonin and norepinephrine neurons can compensate for the deficiency of melatonin activity (20).

The “careful assessment” recommendations presented here are not the only example of facile judgments regarding the tolerability of antidepressants. Some authors believe that side effects are poorly related to the mechanism of action of the drugs. It is argued that side effects are nonspecific, probabilistic and therefore almost unpredictable (18). Other authors are at least looking for the reasons for the formation of side effects in order to take them into account when prescribing antidepressants. Unfortunately, they find these reasons not in the mechanisms of action of the drugs, but in the characteristics of depression, public opinion or the psychology of the patient.

Thus, it is reported that even with the use of any “most easily tolerated drugs in 80% of patients with mild to moderate depression” (21), heterogeneous adverse events are observed. They most often occur in dysthymia, early depressive states, with anxiety and somatic symptoms (21, 22), in people over 45 years of age, with high body weight deficiency (22), and a history of negative placebo reactions (23). It is reported that poor tolerability of antidepressants is associated with patients’ high demands on quality of life (24) and their concerns about social maladjustment (25). An initially negative attitude towards psychiatry on the part of public opinion, the patient’s low awareness of his own illness and the therapy recommended by the doctor, unsatisfactory experience of previous treatment, etc. also contribute to the problem. (22, 26).

The speculative nature of such constructions is obvious. To refute them, it is enough to say that the side effects of drugs, according to the WHO definition, are caused by their pharmacological properties (37). It is difficult to imagine that inhibition of histamine and acetylcholine neurons arises due to the patient’s high demands on quality of life, excessive activation of serotonin, norepinephrine and dopamine neurons due to negative attitudes towards psychiatry from public opinion, and drug-induced hepatitis due to concerns about social maladjustment.

Thus, the presented classification of antidepressants according to tolerability categories allows us to return the study of side effects to the mainstream of biological psychiatry. In addition, this classification is easy to use in practical medicine. In particular, the lower the category of tolerability of an antidepressant, the greater the need for a special justification for its prescription (efficacy, positive experience of treatment in the past, the patient’s desire, etc.). In turn, the appearance of such a detailed justification in the medical history will allow one to avoid many problems (psychological, social and other) that arise during the treatment process between the doctor and his patient.

Using the presented classification, it is easy to resolve the issue of choosing the most effective and tolerable antidepressant. This requires only comparing the tolerability categories of the most effective drugs: amitriptyline (TcA), imipramine (TcA) and venlafaxine (SNRI) (5). The first of them (amitriptyline) belongs to category VI of tolerability (Table 5). The side effects of the second antidepressant (imipramine) are even more serious. This drug belongs to category VII of tolerability. As for venlafaxine, the side effects of this antidepressant are much weaker, and this drug belongs to category III of tolerability. Thus, venlafaxine, when used in high doses, is the most effective and tolerable drug in the treatment of depression.

Venlafaxine is well known in our country under the trade name Velaxin (Egis). This drug has been studied in leading scientific organizations conducting advanced research in the field of psychiatry. Among them are the Federal State Budgetary Institutions “State Scientific Center for Social and Forensic Psychiatry named after V.P. Serbsky" and "Moscow Research Institute of Psychiatry" of the Russian Ministry of Health, St. Petersburg Research Institute named after. V.M. Bekhterev (28,29). Long-acting capsules (Velaxin retard) are also well known (30), with the use of which there is a significant reduction in the frequency of such side effects of the drug as nausea (31). In addition, the study of Velaxin was successfully carried out not only in psychiatry, but also in neurology (32).

A video by M.Yu. Drobizhev on the same topic can be viewed at the link: https://www.youtube.com/watch?v=SwtO_bC_838&t=11s

Bibliography

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M.Yu. Drobizhev , Doctor of Medical Sciences, Head of the educational department of the Training Center of the Association of Medical and Pharmaceutical Universities of Russia. Contact Information -

E.Yu. Antokhin , Candidate of Medical Sciences, Associate Professor, Head of the Department of Clinical Psychology and Psychotherapy of the Orenburg State Medical University of the Russian Ministry of Health.

R.I. Palaeva is an assistant at the Department of Clinical Psychology and Psychotherapy at the Orenburg State Medical University of the Russian Ministry of Health.

S. V. Kikta , Candidate of Medical Sciences, Head. Department of the Federal State Budgetary Institution "Polyclinic No. 3" of the Administration of the President of the Russian Federation, Moscow

1 There are probably side effects due to excessive activation of melatonin nerve cells. However, they are not yet described even in the instructions for agomelatine, a melatonergic drug that has a direct effect on them (11).

2 Theoretically, “para-therapeutic” side effects can be observed even against the background of “non-therapeutic” side effects. After all, any antidepressant activates serotonin, norepinephrine or dopamine neurons to varying degrees. However, the drugs are dominated by “non-therapeutic” side effects, if only because they are most often persistent. At the same time, “paratherapeutic” side effects are always reversible. In addition, not all antidepressants that have “non-therapeutic” side effects are capable of seriously activating serotonin, norepinephrine and dopamine neurons.

Indications for use of Amitriptyline

What are tablets and solution usually prescribed for?

The drug is indicated:

• for depression (agitation, anxiety, sleep disturbances, alcohol withdrawal, organic brain damage, neurotic withdrawal);
• for behavioral disorders, mixed emotional disorders, nocturnal enuresis , chronic pain syndrome (for cancer pathology, postherpetic neuralgia );
• for bulimia nervosa ;
• for migraine (for prevention);
• for ulcerative lesions of the digestive system .

Indications for the use of Amitriptyline in tablets and in other forms of release are the same.

Indications for use

"Amitriptyline" is prescribed by a doctor in the presence of depressive conditions associated with the following manifestations:

• sleep disorders;
• agitation (restlessness);
• high level of anxiety;
• withdrawal syndrome in alcoholism;
• nocturnal enuresis;
• emotional instability;
• organic lesions of brain tissue.

The product is also used to treat such pathologies;

• nocturnal enuresis;
• postherpetic neuralgia;
• severe pain;
• migraine;
• bulimia nervosa;
• ulcers of the digestive system.

Contraindications

According to the annotation, the medicine is not used:

• for myocardial infarction ;
• intolerance to the main component;
• for angle-closure glaucoma ;
• acute intoxication with psychoactive, analgesic, hypnotics;
• for acute alcohol intoxication;
• during breastfeeding;
• severe disturbances of intraventricular conduction and antioventricular conduction;
• with pathology of the cardiovascular system;
• with suppression of bone marrow hematopoiesis;
• manic-depressive psychoses;
• bronchial asthma;
• chronic alcoholism;
• decreased motor function of the digestive system;
• stroke;
• liver and kidney pathologies;
• intraocular hypertension;
• urinary retention;
• prostatic hyperplasia;
• with hypotension of the bladder;
• thyrotoxicosis;
• pregnancy.

For epilepsy , Amitriptyline is prescribed with caution.

Side effects of Amitriptyline

Nervous system: agitation, hallucinations, disorientation , fainting, asthenia, drowsiness, anxiety, hypomanic state, increased depression, depersonalization , motor restlessness, increased epileptic seizures, extrapyramidal syndrome , ataxia, myoclonus, paresthesia in the form of peripheral neuropathy, tremor of small muscles, headache.

Anticholinergic effects: increased intraocular pressure, blurred vision, mydriasis, dry mouth, tachycardia , difficulty urinating, paralytic ileus, delirium, confusion, decreased sweating.

Cardiovascular system: instability of blood pressure, intraventricular conduction disorders , arrhythmia, orthostatic hypotension , dizziness, palpitations, tachycardia.

Digestive tract: darkening of the tongue, diarrhea, changes in taste perception, vomiting, heartburn , gastralgia, hepatitis, cholestatic jaundice.

Endocrine system: galactorrhea, hyperglycemia , decreased potency or increased libido, increased size of the mammary glands, gynecomastia , testicular swelling, syndrome of inappropriate ADH secretion, hyponatremia. Hypoproteinemia , pollakiuria, urinary retention, enlarged lymph nodes, hyperpyrexia, swelling, tinnitus, and hair loss are also noted

When discontinuing the drug, unusual agitation, sleep disturbances, malaise, headache, diarrhea, nausea, unusual dreams, restlessness, and irritability are noted. When administered intravenously, a burning sensation, lymphangitis , thrombophlebitis , and an allergic response .

Reviews of the side effects of Amitriptyline are quite frequent. When using the drug, addiction may also occur.

Amitriptyline (Amixid, Sarotene)

Clinical and pharmacological group

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 (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.

Contraindications

Hypersensitivity, use in conjunction with MAO inhibitors and 2 weeks before treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotics, analgesics and psychoactive drugs, angle-closure glaucoma, severe AV and intraventricular conduction disorders (branch block His bundle, AV block II stage), lactation period, children under 6 years of age.

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

Carefully. Amitriptyline should be used with caution in persons with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, 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 ileus), liver and/or renal failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, hypotension bladder, during pregnancy (especially the first trimester), in old age.

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 gradually the dose can be increased taking into account the effectiveness and tolerability of the drug to a maximum of 300 mg/day. in 3 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, psychosis with schizophrenia and alcohol withdrawal, a dose of 25-100 mg/day is prescribed. (at night), after achieving a therapeutic effect, switch to the minimum effective dose - 10-50 mg/day.

For the prevention of migraine, for 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/day. (the maximum dose is taken at night).

Children

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

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

Side effects

Associated with the anticholinergic effect of the drug: blurred vision, paralysis of accommodation, mydriasis, increased intraocular pressure (only in persons with a local anatomical predisposition - a narrow anterior chamber angle), tachycardia, dry mouth, confusion (delirium or hallucinations), constipation, paralytic intestinal tract obstruction, difficulty urinating.

From the central nervous system: drowsiness, fainting, fatigue, irritability, anxiety, disorientation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, psychomotor agitation, mania, hypomania, memory impairment, decreased ability to concentrate, insomnia, nightmares, asthenia; headache; dysarthria, tremor of small muscles, especially the arms, hands, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus; ataxia, extrapyramidal syndrome, increased frequency and intensification of epileptic seizures; changes in the electroencephalogram (EEG).

From the cardiovascular system: tachycardia, palpitations, dizziness, orthostatic hypotension, nonspecific changes in the electrocardiogram (ECG) (S-T interval or T wave) in patients without heart disease; arrhythmia, blood pressure lability (decrease or increase in blood pressure), intraventricular conduction disturbances (widening of the QRS complex, changes in the PQ interval, bundle branch block).

From the gastrointestinal tract: nausea, heartburn, gastralgia, hepatitis (including impaired liver function and cholestatic jaundice), vomiting, increased appetite and body weight or decreased appetite and body weight, stomatitis, changes in taste, diarrhea, darkening of the tongue.

From the endocrine system: increase in size (swelling) of the testicles, gynecomastia; increase in the size of the mammary glands, galactorrhea; decreased or increased libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inappropriate secretion of antidiuretic hormone (ADH). Allergic reactions: skin rash, itching, photosensitivity, angioedema, urticaria.

Other: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urinary retention, pollakiuria.

With long-term treatment, especially in high doses, if it is abruptly stopped, withdrawal syndrome may develop: nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual agitation; with gradual withdrawal after long-term treatment - irritability, motor restlessness, sleep disturbances, unusual dreams.

The connection with taking the drug has not been established: lupus-like syndrome (migratory arthritis, the appearance of antinuclear antibodies and positive rheumatoid factor), impaired liver function, ageusia.

Overdose

Symptoms

.

From the central nervous system: drowsiness, stupor, coma, ataxia, hallucinations, anxiety, psychomotor agitation, decreased ability to concentrate, disorientation, confusion, dysarthria, hyperreflexia, muscle rigidity, choreoathetosis, epileptic syndrome.

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

Other: respiratory depression, shortness of breath, cyanosis, vomiting, hyperthermia, mydriasis, increased sweating, oliguria or anuria.

Symptoms 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.

Treatment: for oral administration: gastric lavage, intake of activated charcoal; symptomatic and supportive therapy; for severe anticholinergic effects (lowering blood pressure, arrhythmia, coma, myoclonic epileptic seizures) - administration of cholinesterase inhibitors (the use of physostigmine is not recommended due to the increased risk of seizures); maintaining blood pressure and water-electrolyte balance. Monitoring of cardiovascular functions (including ECG) for 5 days (relapse may occur after 48 hours or later), anticonvulsant therapy, artificial pulmonary ventilation (ALV) and other resuscitation measures are indicated. Hemodialysis and forced diuresis are ineffective.

Drug interactions

When ethanol 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.

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).

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

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).

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 ST 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, it is possible that withdrawal syndrome may develop 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 childbirth

Use in childhood

Contraindicated for 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 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

For impaired renal function

Use with caution in case of renal failure.

For liver dysfunction

Use with caution in case of liver failure.

Use in old age

Use with caution in elderly people.

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

Conditions
for dispensing from pharmacies
The drug is dispensed with a prescription.

Storage conditions and periods

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Release form, composition and packaging

Pills

from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer; Light marbling is allowed.

Excipients:

microcrystalline cellulose - 40 mg, lactose monohydrate (milk sugar) - 40 mg, pregelatinized starch - 25.88 mg, colloidal silicon dioxide (aerosil) - 400 mcg, talc - 1.2 mg, magnesium stearate - 1.2 mg.

10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — contour cell packaging (2) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.

Pills

from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer and a notch; Light marbling is allowed.

Excipients:

microcrystalline cellulose - 100 mg, lactose monohydrate (milk sugar) - 100 mg, pregelatinized starch - 64.7 mg, colloidal silicon dioxide (aerosil) - 1 mg, talc - 3 mg, magnesium stearate - 3 mg.

10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — contour cell packaging (2) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs.

Amitriptyline, instructions for use (Method and dosage)

The medicine is taken orally immediately after eating, without chewing, which ensures the least irritation of the stomach walls. The initial dosage is 25-50 mg at night for adults. Within 5 days, the amount of the drug is increased to 200 mg per day in 3 doses. If there is no effect within 2 weeks, the dose is increased to 300 mg.

Solutions are administered slowly intravenously and intramuscularly, 20-40 mg 4 times a day with a gradual transition to oral administration. The course of therapy is no more than 8 months. For prolonged headaches, for migraines, chronic pain syndrome of neurogenic origin, for migraines, 12.5-100 mg per day is prescribed.

Instructions for use of Amitriptyline Nycomed are similar. Before use, be sure to familiarize yourself with the contraindications for the drug.

Amitriptyline

Amitriptyline is a classic tricyclic antidepressant. Suppresses the reuptake of norepinephrine and serotonin by presynaptic neurons, which leads to an increase in the concentration of these mediators and the development of an antidepressant effect. With regular use, it suppresses the activity of cerebral beta-adrenergic receptors and serotonin receptors, normalizes the propagation of nerve impulses through these receptors, eliminates the imbalance of these systems caused by depression, exhibits an anxiolytic (eliminating anxiety) effect, reduces agitation (emotional overexcitation) and manifestations of depression. It has a mild analgesic effect, which, according to scientists, is due to fluctuations in the level of monoamines (primarily the neurotransmitter serotonin) in the central nervous system and the effect on the body’s own (internal) opiateergic systems. The pronounced ability to bind to m-cholinergic receptors determines the powerful anticholinergic effect of Amitriptyline, and its ability to interact with histamine H1 receptors and block alpha-adrenergic receptors causes a sedative effect. It has an antiulcer effect, reduces the severity of pain in stomach and duodenal ulcers, and ensures rapid scarring of the ulcer. The above-mentioned anticholinergic activity of Amitriptyline, which increases the elasticity of the bladder walls and their ability to stretch, makes it effective in the treatment of enuresis. This property of the drug is reinforced by direct beta-adrenergic stimulation and blocking the uptake of the transmitter serotonin by central neuronal synapses. Amitriptyline reduces bulimia nervosa both with and without comorbid depression. The antidepressant effect of the drug begins to clearly manifest itself 2-3 weeks after the start of drug therapy.

The bioavailability of Amitriptyline is about 50%, the half-life is 30-45 hours. Elimination from the body occurs through urine. The drug is available in tablet and ampoule form. Pharmacotherapy is started with a dose of 25-50 mg, the optimal time of administration is before bedtime. Gradually over the course of a week the dose is increased by 3-4 times. If there is no improvement in the condition in the second week, the daily dose is raised to 300 mg. Elimination of depressive symptoms is not a reason to refuse treatment: in this case, the dose is reduced to daily 50-100 mg and pharmacotherapy is continued for at least another three months. In elderly people with mild depression, the dose of the drug is set in the range from 30 to 100 mg per day, and when positive results are achieved, they move on to a maintenance daily dose of 250-50 mg. During treatment, it is necessary to avoid situations that require sudden standing up from a sitting or lying position. It is not recommended to abruptly interrupt treatment: in this case, withdrawal syndrome may develop. It is necessary to take the necessary precautions when using Amitriptyline in patients suffering from epilepsy, because the drug in a daily dose of over 150 mg reduces the seizure threshold. When planning treatment, one should be aware of possible suicide attempts in patients suffering from severe depression. The combined use of Amitriptyline and electroconvulsive therapy is possible only with constant medical monitoring. In patients with a complicated medical history and the elderly, taking the drug can lead to the occurrence of pharmacological psychoses (after stopping drug therapy, such phenomena quickly disappear). Long-term use of Amitriptyline can lead to the development of caries. The drug is not compatible with alcohol.

Overdose

Manifestations from the nervous system: coma, stupor, increased drowsiness, anxiety, hallucinations, ataxia, epileptic syndrome, choreoathetosis, hyperreflexia, dysarthria, muscle tissue rigidity, confusion, disorientation, impaired concentration, psychomotor agitation.

Manifestations of an overdose of Amitriptyline from the cardiovascular system: disturbance of intracardiac conduction, arrhythmia, tachycardia, drop in blood pressure, shock, heart failure, rarely - cardiac arrest.

Anuria , oliguria, increased sweating, hyperthermia , vomiting, shortness of breath, depression of the respiratory system, and cyanosis are also noted Possible drug poisoning.

To avoid the negative consequences of an overdose, emergency gastric lavage and administration of cholinesterase inhibitors are required in case of severe anticholinergic manifestations. It is also required to maintain water and electrolyte balance, blood pressure levels, control over the functioning of the cardiovascular system, and carry out resuscitation and anticonvulsant measures if necessary. Forced diuresis, as well as hemodialysis, have not proven effective in treating an overdose of Amitriptyline.

Interaction

A hypotensive effect, respiratory depression , and a depressant effect on the nervous system are observed with the joint prescription of medications that depress the central nervous system: general anesthetics, benzodiazepines, barbiturates, antidepressants and others.

The drug enhances the severity of the anticholinergic effect when taking amantadine , antihistamines, biperiden , atropine , antiparkinsonian drugs, phenothiazine .

The drug enhances the anticoagulant activity of indadione , coumarin derivatives, and indirect anticoagulants. There is a decrease in the effectiveness of alpha-blockers and phenytoin .

Fluvoxamine , Fluoxetine increase the concentration of the drug in the blood. The risk of developing epileptic seizures increases, and the central anticholinergic and sedative effects also increase when combined with benzodiazepines, phenothiazines, and anticholinergics.

Simultaneous use of methyldopa , reserpine , betanidine , guanethidine , clonidine reduces the severity of their hypotensive effect.

Delirium develops when taking acetaldehydrogenase , Disulfiram . phenylephrine , norepinephrine , epinephrine , and isoprenaline on the cardiovascular system . The risk of hyperpyrexia increases when taking antipsychotics and m-anticholinergics.

Amitriptyline

Concomitant use of amitriptyline and MAO inhibitors can cause serotonin syndrome (agitation, confusion, tremor, myoclonus, hyperthermia are possible).

Amitriptyline can be prescribed 14 days after stopping treatment with irreversible MAO inhibitors and at least 1 day after stopping therapy with the reversible MAO type A inhibitor, moclobemide. MAO inhibitors can be prescribed 14 days after stopping amitriptyline.

Amitriptyline may enhance the effects of alcohol, barbiturates and other CNS depressants.

Since tricyclic antidepressants, including amitriptyline, can enhance the effect of anticholinergic drugs on the organs of vision, central nervous system, intestines and bladder, their simultaneous use should be avoided due to the risk of developing paralytic ileus and hyperpyrexia.

When taking tricyclic antidepressants in combination with anticholinergic drugs or antipsychotics, especially in hot weather, hyperpyrexia may develop.

Amitriptyline may enhance the cardiovascular effects of epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine and phenylpropanolamine; therefore, anesthetics, decongestants and other drugs containing these substances should not be used simultaneously with amitriptyline.

May reduce the antihypertensive effect of guanethidine, betanidine, reserpine, clonidine and methyldopa.

When taking tricyclic antidepressants simultaneously, it is necessary to adjust antihypertensive therapy.

When used together with antihistamines (clonidine), the inhibitory effect on the central nervous system may be enhanced; with drugs that cause extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.

Concomitant use of amitriptyline and drugs that prolong the QT interval (antiarrhythmics (quinidine), antihistamines (astemizole and terfenadine), some antipsychotics (cisapride, halofantrine and sotalol, especially pimozide and sertindole)) increases the risk of developing ventricular arrhythmia.

Antifungal drugs, for example, fluconazole, terbinafine, increase the concentration of tricyclic antidepressants in the blood serum and, accordingly, their toxicity.

Possible fainting and the development of paroxysms of ventricular tachycardia ( Torsade de Pointes

).

Barbiturates and other enzyme inducers, such as rifampicin and carbamazepine, can increase the metabolism of tricyclic antidepressants, and as a result, reduce the concentration of tricyclic antidepressants in the blood plasma and reduce their effectiveness.

When amitriptyline is used together with phenytoin, the metabolism of the latter is inhibited, and the risk of its toxic effects (ataxia, hyperreflexia, nystagmus, tremor) increases.

When starting the use of amitriptyline in patients receiving phenytoin, the concentration of the latter in the blood plasma should be monitored due to an increased risk of inhibition of its metabolism. At the same time, the therapeutic effect of amitriptyline should be monitored, because your dose may need to be increased.

Preparations of St. John's wort reduce the AUC0-12 hours and the maximum concentration of amitriptyline in the blood plasma by approximately 20% due to the activation of the hepatic metabolism of amitriptyline by the CYP3A4 isoenzyme.

This combination can be used with amitriptyline dose adjustment depending on the results of measuring its concentration in the blood plasma.

With simultaneous use of valproic acid, the clearance of amitriptyline from blood plasma decreases, which can lead to an increase in the concentration of amitriptyline and its metabolite, nortriptyline. When co-administering amitriptyline and valproic acid, serum concentrations of amitriptyline and nortriptyline should be monitored. Amitriptyline dose reduction may be required.

When used simultaneously with cimetidine, methylphenidate and calcium channel blockers, it is possible to slow down the metabolism of amitriptyline, increase its concentration in the blood plasma and develop toxic effects.

When co-prescribed with antipsychotics, it should be taken into account that tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism, reducing the threshold for convulsive readiness.

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 glucocorticoids (GCS).

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.

Concomitant use with drugs for the treatment of thyrotoxicosis increases the risk of developing agranulocytosis.

Due to the risk of arrhythmias, special caution must be exercised when prescribing amitriptyline to patients with hyperthyroidism or patients receiving thyroid medications.

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

When used together with anticholinergic blockers, phenothiazines and benzodiazepines, a mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (lowering the threshold of convulsive activity) is possible.

Estrogen-containing oral contraceptives and estrogens may increase the bioavailability of amitriptyline. A dose reduction of either estrogen or amitriptyline may be necessary to restore efficacy or reduce toxicity. However, discontinuation of estrogen-containing oral contraceptives may be necessary. In this case, it is necessary to discuss the possibilities of contraception with your gynecologist.

Concomitant use with disulfiram and other acetaldehydrogenase inhibitors may increase the risk of developing psychotic conditions and confusion.

With the simultaneous use of amitriptyline in a high dose and lithium preparations for more than six months, the development of seizures and cardiovascular complications is possible. It is also possible that signs of a neurotoxic effect may occur in the form of tremor, memory impairment, distractibility, disorganization of thinking, even with normal lithium concentrations in the blood and average doses of amitriptyline.

special instructions

Before carrying out therapy, monitoring blood pressure levels is mandatory.

Parenteral Amitriptyline is administered exclusively under the supervision of a physician in a hospital setting. In the first days of treatment it is necessary to observe bed rest. A complete abstinence from ethanol intake is required.

Abrupt refusal of therapy can cause withdrawal syndrome.

The drug at a dose of more than 150 mg per day leads to a decrease in the threshold of convulsive activity, which is important to consider in the development of epileptic seizures in patients with a predisposition.

It is possible to develop hypomanic or manic states in persons with cyclical, affective disorders during the depressive phase.

If necessary, treatment is resumed with small doses after relief of these conditions.

thyrotoxicosis when treating individuals taking thyroid hormone medications due to the possible risk of cardiotoxic effects.

The medication can provoke the development of paralytic intestinal obstruction in elderly people, as well as those prone to chronic constipation.

It is imperative to warn anesthesiologists about taking Amitriptyline before performing local or general anesthesia.

Long-term therapy provokes the development of caries .

riboflavin may increase .

Amitriptyline passes into breast milk and causes increased drowsiness in infants.

The medication affects driving.

How to take Amitriptyline

Amitriptyline should be taken exactly as prescribed by your doctor. If you have any doubts, you should consult your doctor or pharmacist.

Not all dosage regimens are possible with different dosage forms and doses of the drug.

The appropriate dosage form and dose of the drug should be selected for the starting and subsequent increasing doses.

Depression

Adults:

The recommended starting dose is 25 mg twice daily. Depending on the clinical effect, the dose may be increased to 150 mg/day, divided into two doses.

Elderly patients (over 65 years of age) and patients with cardiovascular diseases

The recommended starting dose is 10-25 mg per day. Depending on the clinical effect, the dose may be increased to 100 mg/day, divided into two doses. If you take 100 mg to 150 mg of the drug, you may need to consult your doctor more often.

Use in children and adolescents

Amitriptyline is not recommended for use in children and adolescents for the treatment of depression. For more information see section 2.

tension headaches and migraine prevention

Your doctor will choose the right dose based on your symptoms and your body's response to treatment.

Adults:

The recommended starting dose is 10-25 mg in the evening.

The recommended daily dose is 25-75 mg.

Depending on the clinical effect, the dose may be gradually increased. If you take more than 100 mg/day, you may need to consult your doctor more often. Your doctor will advise you to take the drug once a day or divide the dose into two doses.

Elderly patients (over 65 years of age) and patients with cardiovascular diseases

The recommended starting dose is 10-25 mg in the evening.

Depending on the clinical effect of the drug, the dose may be gradually increased.

If you take more than 75 mg/day, you may need to consult your doctor more often.

Use in children and adolescents

Amitriptyline is not recommended for use by children and adolescents for the treatment of neuropathic pain, chronic tension-type headaches, and for the prevention of migraine. For more information, see the section What you need to know before using Amitriptyline.

Bed-wetting

Use in children and adolescents

Recommended dose for children:

• Children under 6 years of age: See section “Do not take Amitriptyline tablets”
• Children from 6 to 10 years: 10-20 mg per day. In this age group, appropriate release forms are used.
• Children 11 years and older: 25-50 mg.

The dose should be increased gradually.

You should take the drug 1 or one and a half hours before bedtime.

Before starting treatment, your doctor may perform an ECG to determine if there are signs of a heartbeat abnormality.

Your doctor will re-evaluate your condition after 3 months of treatment and perform a repeat ECG if necessary.

Do not stop taking the drug without consulting your doctor.

Special patient groups

Patients with liver disease or known to be "poor metabolizers" are usually prescribed lower doses.

Your doctor may take blood samples to determine your amitriptyline level (see What you need to know before you use Amitriptyline).

How and when to take Amitriptyline

The drug should be taken during or after meals.

The tablets should be swallowed whole with water. The tablets should not be chewed.

Treatment period

You should not change the dose of the drug or stop taking the drug without consulting your doctor.

Depression

As with other medications used to treat depression, it may take several weeks before you feel any improvement in your condition.

When treating depression, the duration of treatment is individual and is usually at least 6 months. The duration of treatment is determined by your attending physician.

Continue taking Amitriptyline for as long as prescribed by your doctor. The disease can persist for a long time. If you stop treatment too early, your symptoms may return.

tension headaches and migraine prevention

It may take several weeks for your condition to improve.

Consult your doctor about the duration of treatment and continue taking the drug until your doctor stops it.

Bed-wetting

Your doctor will determine the need to continue treatment after 3 months of taking the drug.

If you take more Amitriptyline than recommended

If you take more Amitriptyline than prescribed by your doctor, you should immediately contact your doctor or the nearest hospital emergency room, even if you do not experience any discomfort or symptoms of poisoning. Take the medicine package with you if you are going to the doctor or hospital.

Overdose symptoms include:

• dilated pupils
• fast or irregular heartbeat
• difficulty urinating
• dry mouth or tongue
• intestinal obstruction
• seizures
• fever
• anxiety
• confusion
• hallucinations
• involuntary movements
• low blood pressure, weak pulse, pallor
• difficulty breathing
• bluish skin
• decreased heart rate
• drowsiness
• loss of consciousness
• coma
• various heart diseases, such as cardiac conduction block, heart failure, hypotension, cardiogenic shock, metabolic acidosis, hypokalemia.

If you forget to take Amitriptyline

Take your next dose at your usual time. Do not take a double dose of the drug to compensate for the missed dose.

If you stop taking Amitriptyline

Your doctor will decide when and how to stop treatment to avoid unwanted symptoms that may occur if the drug is suddenly stopped (for example, headache, feeling unwell, insomnia and irritability).

If you have additional questions about the use of the drug, contact your doctor or pharmacist.

Amitriptyline analogues

Level 4 ATC code matches:
Doxepin

Ladisan

Ludiomil

Melipramine

Anafranil

Analogues of the drug are:

• Saroten
• Amitriptyline hydrochloride

Amitriptyline price, where to buy

The price of Amitriptyline in 25 mg tablets in Russia is about 30-40 rubles for 50 pieces.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Amitriptyline solution for intravenous and intramuscular administration.
  10 mg/ml 2 ml 10 pcs. Federal State Unitary Enterprise Moscow Endocrine Plant 49 rub. order
• Amitriptyline tablets 25 mg 50 pcs. OzonOzon LLC

  57 RUR order

• Amitriptyline tab. 25mg No. 50Ozon LLC

  69 RUR order

Pharmacy Dialogue

• Amitriptyline (25 mg tablet No. 50) Ozone LLC

  60 rub. order

• Amitriptyline (amp. 10 mg/ml 2 ml No. 10) Moscow Endocrine Plant

  53 RUR order

• Amitriptyline (25 mg tablet No. 50) Ozone LLC

  58 RUR order

• Amitriptyline (25 mg tablet No. 50) Moscow Endocrine Plant

  30 rub. order

• Amitriptyline (25 mg tablet No. 50) DHF JSC

  62 RUR order

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Pharmacy24

• Amitriptyline 25 mg No. 50 tablets PrAT “Technolog”, Uman, Cherkasy region, Ukraine
  20 UAH. order
• Amitriptyline 25 mg N25 tablets TOV Doslidniy, Ukraine/TOV FC Zdorovya, Ukraine

  13 UAH order

PaniPharmacy

• Amitriptyline tablets Amitriptyline h/x tablets. w/o 0.025g No. 50 control. cell unitary enterprise Ukraine, OZ GNTsLS LLC

  23 UAH order

• Amitriptyline ampoule Amitriptyline liquid solution d/in. 10mg/ml amp. 2ml No. 10 Ukraine, Health of the people LLC

  89 UAH order

• Amitriptyline tablets Amitriptyline h/x tablets. 0.025g No. 25 Ukraine, OZ GNTsLS LLC

  15 UAH order

• Amitriptyline liquid solution d/in. 1% amp. 2ml No. 10 Ukraine, OZ GNTsLS

  87 UAH order

• Amitriptyline tablets Amitriptyline h/x tablets. 0.025g No. 50 Ukraine, Health of the people LLC

  21 UAH order

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