Antidepressant Amitriptyline belongs to the group of indiscriminate inhibitors of neuronal uptake of monoamines. Amitriptyline has a pronounced thymoanaleptic and sedative effect.

Pharmacodynamics
The mechanism of the antidepressant action of amitriptyline is associated with the inhibition of the reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin in the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and in the periphery, has peripheral antihistamine (H1) and antiadrenergic properties. Also causes anti-neuralgic (central analgesic), antiulcer and anti-bulimic action, is effective for bedwetting. The antidepressant effect develops within 2-4 weeks. After the start of application.

Pharmacokinetics
The bioavailability of amitriptyline for various routes of administration is 30-60%, its active metabolite nortriptyline is 46-70%. The time to reach the maximum concentration (Tmax) after oral administration is 2.0-, 7.7 hours. The volume of distribution is 5-10 l / kg. Effective therapeutic blood concentrations of amitriptyline are 50-250 ng / ml, for nortriptyline (its active metabolite) 50-150 ng / ml. The maximum concentration in blood plasma (Cmax) is 0.04-0.16 μg / ml. Passes through the histohematological barriers, including the blood-brain barrier (including nortriptyline). Tissue concentrations of amitriptyline are higher than those in plasma. Communication with plasma proteins 92-96%. It is metabolized in the liver (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. Plasma half-life is 10 to 28 hours for amitriptyline and 16 to 80 hours for nortriptyline. Excreted by the kidneys - 80%, partly with bile. Complete elimination within 7-14 days. Amitriptyline crosses the placental barrier, is excreted in breast milk in concentrations similar to plasma concentrations.

Indications for use

A drug Amitriptyline apply strictly according to the doctor's prescription.
Depression of any etiology. It is especially effective for anxiety - depressive states, due to the severity of the sedative effect. Does not cause an exacerbation of productive symptoms (delirium, hallucinations), in contrast to antidepressants with a stimulating effect.
Mixed emotional and behavioral disorders, phobic disorders.
Infantile enuresis (excluding children with hypotonic bladder).
Psychogenic anorexia, bulimic neurosis.
Chronic neurogenic pain, for the prevention of migraine.

Mode of application

Amitriptyline tablets appoint inside (during or after meals).

Initial daily dose Amitriptyline when taken orally, it is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg, until the desired antidepressant effect is obtained. The optimal daily therapeutic dose is 150-200 mg (the maximum part of the dose is taken at night). In severe depression resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose. In these cases, it is advisable to start treatment with intramuscular or intravenous administration the drug, while using higher initial doses, accelerating the increase in dosages under the control of the somatic state.

After receiving a persistent antidepressant effect after 2-4 weeks, the dose is gradually and slowly reduced. If signs of depression appear with decreasing doses, it is necessary to return to the previous dose.

If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is inappropriate.

In elderly patients with mild disorders, in outpatient practice, the doses are 25-50-100 mg (max) in divided doses or once a day at night. For the prevention of migraine, chronic pain of a neurogenic nature (including prolonged headaches) from 12.5-25 mg to 100 mg / day. Interaction with other medicinal products Amitriptyline potentiates the depression of the central nervous system with the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, central and narcotic analgesics, anesthetics, alcohol.

Assign intramuscularly or intravenously. In severe depression resistant to therapy: intramuscularly or intravenously (inject slowly!) In a dose of 10-20-30 mg up to 4 times a day, the dose should be increased gradually, the maximum daily dose is 150 mg; after 1-2 weeks, they switch to taking the drug inside. Children over 12 years of age and the elderly are given lower doses and increase them more slowly.

When used together amitriptyline with antipsychotics, and / or anticholinergic drugs, a febrile temperature reaction, paralytic intestinal obstruction may occur. Amitriptyline potentiates the hypertensive effects of catecholamines, but inhibits the effects of drugs acting on the release of norepinephrine.

Amitriptyline can reduce the antihypertensive effect of sympatholytics (octadine, guanethidine and drugs with a similar mechanism of action).

With the simultaneous administration of amitriptyline and cimetidine, an increase in plasma concentration is possible amitriptyline.

Simultaneous reception amitriptyline with MAO inhibitors can be fatal. The break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days!

Side effects

Mainly associated with the anticholinergic action of the drug: accommodation paresis. Blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, urinary retention, fever. All these phenomena usually disappear after adaptation to the drug or dose reduction.
From the side of the central nervous system: headache, ataxia, increased fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremors, paresthesias, peripheral neuropathy, changes in EEG. Rarely extrapyramidal disorders, convulsions, anxiety. From the side of cardio-vascular system: tachycardia, arrhythmia, conduction disturbance, lability blood pressure, expansion of the QRS complex on the ECG (violation of intraventricular conduction), symptoms of heart failure, fainting. From the gastrointestinal tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disturbances, darkening of the tongue, discomfort in the epigastrium, gastralgia, increased activity of "hepatic" transaminases, rarely cholestatic jaundice, diarrhea. From the side endocrine system: an increase in the size of the mammary glands in men and women, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), changes in libido, potency. Rarely, hypo- or hyperglycemia, glucosuria, impaired glucose tolerance, testicular edema. Allergic reactions: skin rash, itching, photosensitivity, angioedema, urticaria. Others: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, increase lymph nodes, increase in body weight with long-term use, sweating, pollakiuria. With long-term treatment, especially in high doses, with an abrupt termination of treatment, the development of a withdrawal syndrome is possible: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with vivid, unusual dreams, increased excitability.

Contraindications

Heart failure in the stage of decompensation
Acute and recovery period of myocardial infarction
Violation of the conduction of the heart muscle
Severe arterial hypertension
Acute diseases liver and kidney with severe dysfunction
Peptic ulcer and 12 duodenal ulcer in the acute stage
Hypertrophy prostate
Atony of the bladder
Pyloric stenosis, paralytic intestinal obstruction
Concomitant treatment with MAO inhibitors (see Interaction)
Pregnancy, breastfeeding period
Childhood up to 6 years
Hypersensitivity to amitriptyline
Amitriptyline should be used with caution in persons suffering from alcoholism, with bronchial asthma, manic-depressive psychosis (MDP) and epilepsy (see Special instructions), with inhibition of bone marrow hematopoiesis, hyperthyroidism, angina pectoris and heart failure, angle-closure glaucoma, intraocular hypertension schizophrenia (although it usually does not exacerbate productive symptoms).

Overdose

Drowsiness, disorientation, confusion, dilated pupils, fever, shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle stiffness, supor, coma, vomiting, arrhythmia, arterial hypotension, heart failure, respiratory depression.
Relief measures: discontinuation of therapy amitriptyline, gastric lavage, fluid infusion, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Shown monitoring of cardiovascular activity (ECG) for 5 days, because relapse may occur 48 hours later or later. Hemodialysis and forced diuresis are not very effective.

Interaction with other medicinal products

Amitriptyline enhances the depressing effect on the central nervous system the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; shows synergism when interacting with other antidepressants. With the combined use of amitriptyline with antipsychotics, and / or anticholinergic drugs, a febrile temperature reaction, paralytic intestinal obstruction may occur. Amitriptyline potentiates the hypertensive effects of catecholamines and other adrenostimulants, which increases the risk of developing disorders heart rate, tachycardia, severe arterial hypertension but inhibits the effects of drugs acting on the release of norepinephrine. Amitriptyline can reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect of anticonvulsants. With the simultaneous use of amitriptyline and anticoagulants - coumarin or indandione derivatives, an increase in the anticoagulant activity of the latter is possible. With the simultaneous administration of amitriptyline and cimetidine, an increase in plasma concentration of amitriptyline with the possible development of toxic effects is possible.

Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduce plasma concentrations of amitriptyline. Amitriptyline enhances the action of antiparkinsonian drugs, and other drugs that cause extrapyramidal reactions. Quinidine slows down the metabolism of amitriptyline. Joint application amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors can provoke delirium. Oral contraceptives containing estrogen may increase the bioavailability of amitriptyline; pimozide and probucol may increase cardiac arrhythmias. Amitriptyline may increase glucocorticosteroid-induced depression; joint application with drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases. Simultaneous administration of amitriptyline with MAO inhibitors can be fatal. The break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days!

special instructions

Amitriptyline in doses higher than 150 mg / day, it reduces the threshold of seizure activity, therefore, the possibility of seizures in patients with a history of seizures, and in the category of patients who are predisposed to this due to age or injury, should be taken into account. Treatment with amitriptyline in old age should be closely monitored and, using minimal doses of the drug, increasing them gradually, in order to avoid the development of delirious disorders, hypomania and other complications. Patients with a depressive phase of the TIR can go into a manic stage. While taking amitriptyline, it is forbidden to drive vehicles, maintain mechanisms and other types of work that require increased concentration of attention, as well as drinking alcohol.

Release form

The following forms of release are possible:
Packing - 50 tablets, each of which contains 25 mg of active substance.
Packs of 20, 50 and 100 coated tablets.
2 ml in colorless glass ampoules. 5 ampoules are packed in a molded PVC container. 2 molded containers (10 ampoules), together with instructions for use, are placed in a cardboard box.
Solution for injection 10 mg / ml in 2 ml ampoules, 5 or 10 ampoules in a cardboard box; 5 ampoules in a blister, 1 or 2 blister packs in a cardboard box together with instructions for use.

Description of the solution

Transparent, colorless, free of mechanical impurities, may be slightly colored.

Storage conditions

At temperatures from 10 ° C to 25 ° C in a dry, dark place and out of the reach of children.

Shelf life - 2-3 years (depending on the form of release and manufacturer). Do not take after the expiration date printed on the package!

Terms of dispensing from pharmacies - by prescription.

Synonyms

Teperin, Triptisol, Adepril, Adepress, Atriptal, Damilen, Daprimen, Elatral, Lantrone, Laroxal, Novotriptin, Redomex, Saroten, Sarotex, Triptil, Triptanol, Elavil, Amiprin, Laroxil, Lentizol, Tripride-Proheptillin, Amitrophin , Amitriptyline Lechiva, Amitriptyline-Akos Amitriptylin-Slovakopharma

Composition

Amitriptyline tablets coated contain 0.0283 g (28.3 mg) amitriptyline hydrochloride, which corresponds to 0.025 g (25 mg) amitriptyline.

For 1 ml of solution for injection Amitriptyline hydrochloride 10 mg (in terms of amitriptyline)
Excipients: glucose, sodium chloride, benzethonium chloride, water for injection.

International name: 5- (3-dimethylaminopropylidene) -10,11-dihydrodibenzocycloheptene.

main parameters

Name:	AMITRIPTILINE
ATX code:	N06AA09 -

Dosage form"type =" checkbox ">

Dosage form

Film-coated tablets, 25mg

Composition

One tablet contains

active substance - amitriptyline 25 mg (in the form of amitriptyline hydrochloride 0.0283 g),

excipients: lactose monohydrate, corn starch, gelatin, calcium stearate, talc, silicon dioxide colloidal anhydride

shell composition: sepifilm 3048 yellow (hydroxypropyl methylcellulose, microcrystalline cellulose, polyoxyl 40 stearate, titanium dioxide E171, quinoline yellow E 104), silicone antifoam emulsion SE-2, macrogol 6000

Description

Film-coated tablets, yellow, round shape, with a biconvex surface

Pharmacotherapeutic group

Psychoanaleptics. Antidepressants.

Monoamine reuptake inhibitors are non-selective. Amitriptilline.

ATX code N06AA09

Pharmacological properties"type =" checkbox ">

Pharmacological properties

Pharmacokinetics

Amitriptyline is almost completely absorbed from the digestive tract, the maximum concentration is reached within 4-8 hours, about 95% binds to plasma proteins. It is metabolized mainly to desmethylamitriptyline (nortriptyline is the main active metabolite). The biological half-life ranges from 10 to 28 hours, for nortriptyline - from 16 to 80 hours. In older patients, there is a predisposition to more high concentrations in plasma and a longer half-life than in young people. Amitriptyline is excreted mainly through the kidneys in the form of several metabolites, both free and conjugated, less than 5% is excreted unchanged. A certain amount of the drug is excreted in the feces.

Amitriptyline crosses the placental barrier and also enters breast milk.

Pharmacodynamics

Amitriptyline is a tricyclic antidepressant from the group of indiscriminate inhibitors of neuronal monoamine uptake. It has a pronounced thymoleptic effect, like imipramine, but its sedative and sedative effect is more pronounced. The mechanism of the antidepressant action of amitriptyline is associated with the inhibition of the reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin in the central nervous system. Amitriptyline is an antagonist of muscarinocholinergic receptors in the central nervous system and in the periphery, has antihistamine (H1) and a1-adrenolytic properties. Consequently, it causes anti-neuralgic (central analgesic), anti-ulcer and anti-bulimic action. It helps to reduce the tone of the smooth muscles of the bladder, increase the capacity and, on the contrary, increases the tone of the bladder sphincter. This explains its effectiveness in the treatment of bedwetting.

Indications for use

Mild, moderate, and severe depressive phases with or without psychotic features in all types of mood disorders such as bipolar disorder, recurrent depressive disorder, and organic affective disorder

Depressive schizoaffective disorder; depression associated with schizophrenia (against the background of constant treatment with antipsychotics)

Depressions previously defined as reactive and neurotic depressions: dysthymia, mixed anxiety-depressive disorder, depressive disorders that emerged as a reaction to severe stress or are a manifestation of adjustment disorder

Depression during treatment with reserpine, inorganic (i.e. primary) enuresis without hypotonic bladder, inorganic encopresis (fecal incontinence), anorexia nervosa, and irritable bowel syndrome

It is used for long-term treatment of pain in complex therapy

Method of administration and dosage

The drug is intended for use in adults, the actual dose is selected individually for each patient, and this dosage should be strictly adhered to.

The initial dose is usually 25-50 mg, taken at bedtime, then the doses are gradually increased depending on tolerance over 5-6 days to 150-200 mg daily, with the maximum daily dose taken before bed. If the patient's condition does not improve during the second week of therapy, the dose is increased to 300 mg per day. This dose is then gradually reduced as the symptoms of depression disappear; reduced doses of 50-100 mg per day are usually taken for 3 months.

Elderly patients

Elderly patients or patients with mild depressive syndrome receiving outpatient treatment are given lower doses of 50-100 mg as one daily dose at bedtime. Therapeutic effect usually appears 7-10 days after starting treatment. Amitriptyline therapy can be considered ineffective only if there is no improvement in the patient's condition after 3 weeks of treatment.

The onset of antidepressant action can be accelerated when amitriptyline is taken together with nortriptyline. In most cases, treatment with amitriptyline for more than 6-8 months is ineffective. Lithium preparations are more suitable to prevent the expected phase of intermittent depression. For this purpose, amitriptyline can be prescribed only to those patients for whom the use of lithium preparations is contraindicated.

Side effects

The expected frequency of undesirable effects is 16 - 20%, while they are most often found in the elderly and children under 5 years of age.

Frequency of occurrence adverse reactions assessed as follows: "very often" (> 1/10), "often" (from ≥ 1/100 to< 1/10), «нечасто» (от >1/1000 to< 1/100), «редко» (от >1/10000 to< 1/1000), «очень редко» (< 1/10000), «частота не известна» (нельзя установить исходя из имеющихся данных).

Often

Vertigo

Tachycardia, arrhythmia (extrasystole, palpitations, impaired cardiac conduction)

Orthostatic hypotension - hyperhidrosis

Fatigue

Disorientation, agitation, psychosis, hallucinations

Drowsiness, tremors

Disturbance of accommodation, blurred vision

Dry mouth, taste disturbances (bitter and sour taste in the mouth), constipation

Delayed urination, delayed onset of urination at the start of treatment

Changes in libido, potency

Violation of hematopoiesis

Extrapyramidal disorders (tardive dyskinesia, slurred speech, low seizure threshold)

Worsening of existing heart failure

Paralytic ileus

Jaundice

Skin reactions

Gynecomastia, galactorrhea

Very rarely

Atrial fibrillation, ventricular fibrillation, cardiac arrest

Increased activity of transaminases

Frequency not known

Hyperglycemia

In exceptional cases, transient delusional states and paranoid states, accompanied by hallucinations, are observed, especially in elderly people with organic cerebral syndrome after abrupt cessation of high doses of the drug.

There have been reports of cases of suicidal thoughts or behavior during or after discontinuation of amitriptyline treatment.

Group effects

Epidemiological studies conducted mainly in patients over 50 years of age and above show an increased risk of bone fractures in patients receiving selective inhibitors serotonin reuptake and tricyclic antidepressants. The mechanism leading to this risk is not clear.

Contraindications

Hypersensitivity to the active and auxiliary components of the drug (see section "Composition")

Acute intoxication with drugs that inhibit the central nervous system

Alcohol poisoning

Acute delirium

Glaucoma

Paralytic intestinal obstruction (due to the anticholinergic effect of amitriptyline)

Epilepsy

Pyloric stenosis

Concomitant therapy with MAO inhibitors (MAO inhibitors must be excluded from the intake at least 14 days before starting treatment with amitriptyline)

Children and adolescents up to 18 years old

Pregnancy and lactation

Cardiac ischemia

Heart failure

Abnormal heart rhythm

Hypertrophy of the prostate

Retention of urine

Drug interactions"type =" checkbox ">

Drug interactions

Amitriptyline enhances the anticholinergic effect of drugs used to treat Parkinson's disease, phenothiazine derivatives, thiazide diuretics and vasodilators.

Amitriptyline enhances the effects on central system narcotic analgesics and barbiturates.

Amitriptyline impairs the reaction to disulfiram.

Amitriptyline potentiates the effect of alcohol (mainly vegetative disorders and poor health can occur), enhances the symptom-mimetic and psychostimulatory effects.

Concomitant use with other serotonergic active substances (such as selective serotonin reuptake inhibitors (SSRIs), selective serotonin-norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors, lithium preparations, tryptan, tramadol, linezolid, L-tryaptophan drugs Hypericum perforatum) can lead to the development of serotonin syndrome. Amitriptyline therapy in combination with any of these substances must be carried out under the close supervision of a physician. In any case, the administration of irreversible monoamine oxidase inhibitors should be discontinued at least 14 days before starting amitriptyline therapy.

Amitriptyline may increase the effectiveness of some antiarrhythmic drugs used to treat type 1 and 3 arrhythmias.

Substances that alkalinize urine and methylphenidate enhance the effect of amitriptyline.

Amitriptyline reduces the antihypertensive effect of reserpine and guanethidine, reduces the activity of anticonvulsants.

Urine alkalizing drugs methylphenidate increase the effectiveness of amitriptyline.

The induction of enzyme synthesis caused by the intake of barbiturates leads to a decrease in the level of amitriptyline to the level of one twentieth part.

special instructions

The use of amitriptyline is not recommended for the following conditions, or the risk / benefit ratio should be carefully weighed: ischemic disease heart failure, heart failure, prostatic hypertrophy, urinary retention, any condition associated with tachycardia or heart rhythm disturbances.
It is prohibited to use alcoholic beverages while taking amitriptyline!
During the period of taking amitriptyline, it is recommended to periodically monitor: blood pressure control, electrocardiogram (ECG), blood tests, liver function tests, electroencephalography (EEG) may be used

Amitriptyline in doses above 150 mg / day lowers the threshold of seizure activity, therefore, the possibility of seizures in patients who are predisposed to this due to age or injury should be considered.

Amitriptyline should be used with caution in persons suffering from alcoholism, bronchial asthma, inhibition of bone marrow hematopoiesis, hyperthyroidism, schizophrenia (although when taken, there is usually no exacerbation of productive symptoms).

Treatment with amitriptyline in old age should be closely monitored, using minimal doses of the drug and gradually increasing them, in order to avoid the development of delirious disorders, hypomania and other complications.

Patients with a depressive phase of manic-depressive syndrome can go into a manic phase.

Suicidal attempts / suicidal thoughts

Depression is associated with an increased risk of suicidal ideation and attempted suicide. The risk exists until a stable remission occurs. Improvement may not be observed during the first weeks of treatment or more, so patients should be monitored by a physician until signs of improvement appear. According to the general clinical experience, the risk of suicide increases by initial stage recovery period.

Other mental conditions for which amitriptyline is prescribed may also be associated with an increased risk of suicide. Therefore, during the treatment of patients with other mental disorders the same precautions should be followed as with major depressive disorders, namely, patients should be under close medical supervision.

Patients with a history of attempted suicide or high degree the likelihood of suicidal thoughts before starting the use of amitriptyline, during the period of treatment should be closely monitored, as they have a greater risk of suicidal thoughts or attempts at suicide. In adult patients with mental disorders, the risk of suicidal behavior is increased with antidepressants compared with placebo in patients under 25 years of age.

Patients (and their caregivers) should be warned of the need for monitoring and possible clinical deterioration, and if they develop suicidal behavior or thoughts, or unusual changes in behavior, seek immediate medical attention.

Hyperglycemia / Diabetes

Epidemiological studies have revealed the existence of an increased risk of developing diabetes mellitus in depressed patients who received tricyclic antidepressants. It is necessary to carefully monitor blood glucose levels in patients with diagnosed diabetes mellitus or with risk factors for the development of diabetes mellitus, who begin therapy with amitriptyline.

Serotonin Syndrome

Serotonin syndrome can develop if tricyclic antidepressants are used concurrently with other serotonergic active substances (see the section on drug interactions). Serotonin syndrome, which is caused by excess serotonin, can be fatal and includes following symptoms:

Neuromuscular agitation (muscle twitching, hyperreflexia, myoclonus, muscle stiffness);

Vegetative changes (hyperthermia, tachycardia, changes in blood pressure, sweating, tremors, hyperemia, dilated pupils, diarrhea);

The change mental state(anxiety, agitation, confusion, coma).

Therapy, in which serotonergic active substances are combined with amitriptyline, must be carried out under the close supervision of a physician. If serotonin syndrome develops, therapy with amitriptyline should be discontinued.

Due to the presence of lactose in the composition, the drug is not recommended for patients with hereditary lactose intolerance, deficiency of the enzyme Lapp-lactase, malabsorption of glucose-galactose.

Pregnancy

The use of amitriptyline is not recommended during pregnancy, especially in the first trimester. Application is possible only after careful comparison of benefits and risks. To date, no phenomena have been reported about the development of developmental anomalies when taking therapeutic doses of amitriptyline.

Lactation period

It is not recommended to use the drug during breastfeeding, since the active substance penetrates in small quantities into breast milk. If the prescription of the drug is inevitable during the period breastfeeding, it is recommended to stop feeding.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Do not drive while taking amitriptyline Vehicle, maintenance of mechanisms, high-rise and other types of work requiring increased concentration of attention.

Overdose

Symptoms: agitation, psychomotor agitation with pronounced antimuscarinic effects, such as dry mouth, dilated pupils, tachycardia, urinary retention, enteral hypotension.

With more severe intoxication, the following symptoms are observed: loss of consciousness, convulsions, myoclonus, hyperreflexity, arterial hypotension, depression of respiratory and cardiac activity with life-threatening arrhythmias, which may recur after recovery. Overdose can be fatal.

Treatment: symptomatic and supportive therapy. Monitoring is necessary: ​​ECG recording and blood pressure control.

In case of severe intoxication, intravenously inject 1-3 mg of physostigmine salicylate. Since physostigmine salicylate is rapidly metabolized, the drug is injected repeatedly in the event of any of the sedentary life-threatening complications (arrhythmias, convulsions, deep coma). In connection with toxic effect physostigmine salicylate, after its administration, it is necessary to monitor the patient's clinical condition.

Storage conditions

Store in a dry, dark place at a temperature of 15 - 25 ° C.

Keep out of the reach of children!

Storage period

Conditions of dispensing from pharmacies

On prescription

Manufacturer

Saneka Pharmaceuticals as, Slovak Republic

Amitriptyline is a drug from the group of antidepressants that is used in the treatment of depressive conditions, mixed emotional and phobic disorders.

It has a pronounced thymoanaleptic and sedative effect. These are some of the strongest drugs at a fairly reasonable price. But to date, the opinions of experts about the possibility of recommending this remedy in the first line of therapy are divided.

In this article, we will consider why doctors prescribe Amitriptyline, including instructions for use, analogues and prices for this drug in pharmacies. The real REVIEWS of people who have already used Amitriptyline can be read in the comments.

Composition and form of release

The drug is available in the form of tablets, pills and solution.

• 1 tablet contains amitriptyline hydrochloride in terms of amitriptyline-25 mg;
• excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hypromellose, magnesium stearate, aerosil, macrogol 6000, titanium dioxide, talc, tween-80, acid red 2 C.

Clinical and pharmacological group: antidepressant.

Amitriptyline: indications for use

Amitriptyline is a drug commonly used in the treatment of the following psychopathological conditions and disorders:

1. All types of schizophrenia.
2. Inorganic psychoses of unspecified etiology and genesis.
3. Depressive manifestations of all types.
4. Recurrent depressive disorder.
5. Bulimia of nervous genesis.
6. Emotional intermittent personality disorder.
7. Disorders of behavior and social adaptation.
8. Inorganic enuresis.
9. Migraine.
10. Persistent pain resistant to therapy.

There are positive reviews about Amitriptyline used for peptic ulcer Gastrointestinal tract, to relieve headaches, prevent migraines.

pharmachologic effect

The drug belongs to the group of tricyclic antidepressants. In addition to the pronounced sedative effect, Amitriptyline has the following number of therapeutic effects:

• Anesthetic effect (associated with a decrease in serotonin concentration);
• Blocking acetylcholine receptors in the central and peripheral nervous system;
• Antiulcer effect (associated with blocking histamine receptors in the digestive system);
• An increase in the tone of the sphincter of the bladder and an increase in its ability to stretch (associated with blocking the receptors of serotonin and acetylcholine).

The therapeutic effect of the drug develops 2-3 weeks after the start of treatment.

Instructions for use

According to the instructions for use, the medicine is taken orally immediately after a meal, without chewing, which ensures the least irritation of the stomach walls.

1. The initial daily dose for oral administration is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg, until the desired antidepressant effect is obtained.
2. The optimal daily therapeutic dose is 150-200 mg (the maximum part of the dose is taken at night).
3. In severe depression resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose.
4. In these cases, it is advisable to start treatment with intramuscular or intravenous administration of the drug, while using higher initial doses, accelerating the increase in dosages under the control of the somatic condition.

After receiving a persistent antidepressant effect after 2-4 weeks, the dose is gradually and slowly reduced. If signs of depression appear with decreasing doses, it is necessary to return to the previous dose.

If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is inappropriate.

Contraindications

You can not use the drug in such cases:

• individual hypersensitivity reactions;
• myocardial infarction (even during the recovery period);
• heart failure or intracardiac conduction disorder;
• atony of the bladder;
• high blood pressure;
• hyperplasia of the prostate gland;
• intestinal obstruction;
• disturbances in the work of the liver and kidneys;
• exacerbations of stomach or duodenal ulcers;
• under 6 years of age.

Relative contraindications requiring additional examination of the patient and consultation with a doctor are:

• epilepsy;
• arrhythmia;
• hyperthyroidism,
• ischemic disease;
• glaucoma.

Side effects

The use of Amitriptyline can cause blurred vision, urination, dry mouth, increased intraocular pressure, increased body temperature, constipation, intestinal obstruction.

• Judging by the reviews about Amitriptyline, all these side effects disappear after a decrease in the prescribed doses or after the patient gets used to the drug.

In addition, after treatment, weakness, ataxia, tachycardia, nausea, heartburn, stomatitis, vomiting, anorexia, discoloration of the tongue, epigastric discomfort, fatigue, insomnia, dizziness, nightmares, confusion, irritability, tremors, motor agitation, hallucinations may occur. , drowsiness, impaired attention, paresthesia, convulsions, arrhythmia, increased activity of liver enzymes, diarrhea, jaundice, galactorrhea, changes in potency, libido, testicular edema, urticaria, itching, purpura, hair loss, enlarged lymph nodes.

Pregnancy and lactation

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

It passes into breast milk and may cause drowsiness in nursing infants. In order to avoid the development of withdrawal syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increased or decreased blood pressure, tremors or spastic phenomena), amitriptyline is gradually canceled at least 7 weeks before the expected birth.

Analogs

Amitriptyline - INN (i.e. international non-proprietary name). To patented products containing Amitriptyline as active substance, include:

• Saroten Retard,
• Elivel,
• Damile Maleinat,
• Amitriptyline-Grindeks,
• Vero-Amitriptyline,
• Amitriptyline Nikomend.

Attention: the use of analogs must be agreed with the attending physician.

Amitriptyline is a popular drug in psychiatry. It combines antidepressant, hypnotic and anti-anxiety effects, recommended by the World Health Organization. But, in addition to the therapeutic effect, many side effects amitriptyline, which requires a detailed study of this drug.

Today, this tricyclic antidepressant is available in the form of pills with an amount of active substance - amitriptyline hydrochloride - from 10 to 75 mg. The tablets are packed in a plastic bottle with a light pink coating. When dragees are broken, an inner layer of a yellowish tint is visible. The drug also includes additional components - sucrose, lactose, calcium stearate, corn starch, gelatin, white opadry - the main component of the dense coating of Amitriptyline tablets.

The second possible form of release is capsules. The outer gelatinous shell is red-brown in color. Auxiliary components: shellac, talc, sucrose, titanium dioxide, povidone, stearic acid.

The latter form, used mainly for acute manifestations depressive disorders, - solution (1%) in ampoules of 2 ml. Outwardly absolutely transparent liquid without sediment or subsequent discoloration. Additional components: injection water, glucose. Amitriptyline injections can be given intramuscularly, or drip therapy (intravenous) is used.

Side effects and contraindications of Amitriptyline

The principle of action of amitriptyline is the reuptake of such neurotransmitters as dopamine, norepinephrine, mainly serotonin, which are responsible for the depression in humans. It provides a soothing, anti-anxiety, sedative effect. Along with this, amitriptyline exhibits anticholinergic activity, which is the cause of a large number of side effects.

To reduce the possible negative effect, at the beginning of therapy, it is necessary to gradually increase the dose, and at the end, consistently refuse the drug.

There are the following symptoms associated with anticholinergic effects:

• problems with urination, up to bladder atony;
• violation of visual function (blurry and defocused near image, photosensitivity);
• constipation, which, without the necessary therapy, develops into acute intestinal obstruction or paralysis;
• dilated pupils, agitation, feeling similar to drunkenness, apathy (due to sedation, especially at high doses), lethargy;
• delirium (clouding of consciousness, attention, perception, emotions) - mainly in elderly patients;
• anticholinergic syndrome is extremely rare.

Other side effects include the following conditions:

• disturbances in the perception of taste, dyspeptic disorders, constant hunger;
• the development of allergies;
• changes in blood composition: thrombocytopenia (platelet deficiency), leukopenia (lack of leukocytes in plasma), eosinophilia (decrease in the concentration of eosinophils), hyponatremia (decrease in the number of Na ions), fluctuations in sugar levels;
• low blood pressure, tachycardia, other heart rhythm disorders, orthostatic collapse (problems with blood flow to the brain when changing body position, darkening in the eyes, dizziness or loss of consciousness);
• violations in the liver;
• in gynecology - decreased libido, potency, anorgasmia, gynecomastia (hypertrophic enlargement of the mammary glands), galactorrhea (spontaneous flow of milk from the breast), ejaculation disorders;
• in neurology - extrapyramidal syndromes (spontaneous involuntary contractions of individual muscles), ataxia (inconsistency in the tension of skeletal muscles), neuropathy (mainly peripheral, manifests itself as increased sensitivity of the extremities, tingling sensation or numbness of the hands, feet), dysarthria (pronunciation problems due to admission restrictions nerve impulse to the organs of speech);
• in psychiatry - mania, hypermania (typical for patients with dysfunction thyroid gland, affective or schizoaffective disorders), hallucinations, depersonalization.

Patients with epilepsy on therapy with Amitriptyline may experience seizures from taking a small amount of an antidepressant, as also patients with traumatic brain injury. In people without contraindications, convulsions appear when large doses are administered intravenously.

An important side effect is the aggravation of suicidal tendencies with an increase in the initial dose. Because of this, it is recommended to start taking the drug in small amounts and only in the evening, gradually the dose can be increased by adding doses in the morning and afternoon. In acute manifestations of suicidal ideation against the background of depression, treatment should be started in a hospital setting.

The likelihood of suicide increases with the following diseases:

• asthenic-depressive syndrome;
• depression with acts of self-blame;
• depersonalization.

Amitriptyline can affect the speed of reaction and perception, therefore, during therapy, it is not recommended to drive or perform difficult work that requires significant concentration and is life-threatening due to inattention.

The remedy is contraindicated in such pathologies:

• cardiovascular diseases: severe hypertension, decompensated heart disease, recovery from a heart attack;
• ulcers of the intestine and stomach, pyloric stenosis (insufficient size of the opening between the stomach and duodenum);
• glaucoma;
• atony (paralysis) of the bladder or intestines;
• pregnancy;
• manic phase;
• age up to 12 years;
• dysfunction of the prostate gland.

Drug dependence

In some countries (for example, in Ukraine), Amitriptyline is banned and included in the list of narcotic substances. This is due to the fact that patients, feeling a temporary receding of the symptoms of depression, can independently increase the dose to obtain a permanent effect. The impact on the central nervous system (central nervous system), in which there is a feeling of relaxation, some "inhibition" of consciousness, lead to the fact that in addition the patient can drink a double or triple dose to induce a feeling of euphoria.

Some of the side effects are perceived as the first signs of drug addiction, but they are not: palmar tremors (involuntary tremors), dilated pupils, irritability, irascibility, photosensitivity, intoxication.

There is also some physical dependence on the drug - when taken from 1 month, the body develops a persistent addiction to the antidepressant, and an abrupt cessation of treatment may be reflected in the form of a withdrawal syndrome. But this property is typical for many drugs, especially for drugs of a similar nature and other drugs, the course of treatment for which exceeds 3-5 months.

Possible consequences of taking with alcohol

The principle of action of amitriptyline and alcohol are partially similar - there is a "inhibition" of the central nervous system. But when used together, these substances increase the degree of effect on the body. As a result, severe intoxication occurs against the background of severe side effects of the antidepressant or signs of an overdose.

The most common symptoms are severe abdominal pain, vomiting, stool disturbances, stomatitis, and changes in taste perception.

The load on the heart increases due to serious disturbances in its rhythm, which under the influence elevated temperature, nervous overexcitation, can lead to stroke or heart attack.

The liver wears out quickly - basic metabolic reactions take place in it, including the processing of toxins from alcohol and medicines. The risk of developing toxic necrosis increases.

The kidneys excrete the metabolites of Amitriptyline and ethyl alcohol which, in turn, also increases the load on them. Therefore, dysfunctions of the excretory system are possible, including the appearance of acute renal failure (acute renal failure).

Other symptoms include blurred consciousness, disorientation, hallucinations, uneven breathing, increased sweating, rash, redness, or other allergic reactions.

In the case of an unintentional combination of Amitriptyline and ethyl alcohol, the patient must immediately rinse the stomach and take a means to remove toxins (the most common option is activated carbon). Further - to carry out rehabilitation in a hospital under the guidance of an experienced specialist.

Contraindications during pregnancy and lactation

Amitriptyline is not prescribed during pregnancy because of its potential to influence fetal development, except in situations where no other alternative is available. Studies have shown that a child after childbirth may experience pathological drowsiness, irritability, tearfulness, and sometimes problems with urination. This effect is due to the effect of one of the metabolites of the substance - nortriptyline.

During lactation, this antidepressant is also not prescribed, although there is no specific data on the detrimental effect on the newborn with breastfeeding... No more than 2% of the daily dose taken by the mother can enter the child's body, which can manifest itself as drowsiness. Therefore, treatment with Amitriptyline during lactation is not prohibited, but in this case it is recommended to carefully monitor the child's condition, especially in the first 4 weeks of life.

Amitriptyline withdrawal syndrome

Withdrawal syndrome is a pathological condition that occurs when a drug is abruptly abandoned, especially with prolonged use.

This is the body's response to a supportive agent and can cause the following symptoms:

• dizziness, headache attacks, photosensitivity, tinnitus;
• insomnia, nightmares;
• dyspeptic disorders, decreased salivation;
• emotional disturbances, panic;
• bradycardia (slowing the heart rate), tachycardia (increased heart rate).

Symptomatic therapy of withdrawal syndrome is recommended: sedatives, preferably on a plant basis, cleansing the body, restoring the electrolyte balance, consultation with a gastroenterologist to get rid of gastrointestinal disorders, the possible intake of antihypertensive drugs (to equalize the heart rate), as additional strengthening procedures - physiotherapy, massage, oxygen therapy, etc. the appearance of acute panic attacks, the emergence of suicidal ideas will require the use of antipsychotics.

The best preventive action for Amitriptyline withdrawal syndrome is to gradually withdraw from the drug, minimize stress and other detrimental factors for the patient's health.

Instructions for use

The main principle on which the appointment of Amitriptyline is based is a gradual increase in the daily dose of the drug to prevent the appearance of side effects.

The initial dose is 50-75 mg of the active substance. It is recommended to add 25-50 mg every day. The standard dose at which the buildup stops is 150-250 mg (up to 300 mg if the patient has a severe form of depression).

Vulnerable patient groups (elderly, adolescents, people who are primary care) and patients with mild depression may not increase the dose as quickly, for example, adding 25 mg to the previous amount every 2-3 days.

In the presence of diseases requiring a quick result, it is possible to start therapy with more high performance, for example, 100 mg of a substance per day, but the treatment must necessarily be carried out in a hospital setting.

If the tolerability of the drug allows, it is possible to prescribe 400-450 mg of Amitriptyline, but only under the strict supervision of the attending physician.

In severe depressive conditions, injections (intramuscularly) or drip (intravenous) are prescribed. Gradually replaced with tablets.

Patients over 55 and adolescents start treatment with lower doses and increase them more slowly, with the exception of acute depressive disorders.

The effect of the drug is noticeable 2-4 weeks after reaching the "working" (150-200 mg) dose.

In order to avoid withdrawal syndrome, it is necessary to gradually decrease the amount of the drug taken at the same rate as the increase.

Amitriptyline is the most popular tricyclic antidepressant used to treat depressive disorders of varying severity. Despite the relatively easy perception of the drug by the body, there is a long list of contraindications and special instructions, which must be taken into account when prescribing and taking funds. And in no case should you self-medicate with this type of drugs.

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The site provides background information for informational purposes only. Diagnosis and treatment of diseases must be carried out under the supervision of a specialist. All drugs have contraindications. A specialist consultation is required!

In most cases medicinal product under the name amitriptyline is well tolerated by patients, but only if all available precautions are followed. In addition, using this medication, the patient is obliged to both warn and correct certain side effects... Since this pharmaceutical agent has a sedative effect, it does not affect the quality and duration of sleep. Considering given fact, this drug can be taken even before bedtime.

The greatest number of side effects occurs mainly due to the rather powerful anticholinergic properties. These side effects include both dilated pupils and blurred vision, dryness in oral cavity as well as constipation and intestinal obstruction. In the case of the use of this medication in overestimated dosages, the patient may experience a delay, as well as difficulty in the urination process. There are also cases when patients have complete atony of the bladder. When taking overdosages of this drug, even hand tremors may occur. It is quite possible that you develop feelings of intoxication, apathy, as well as excessive drowsiness, dizziness and lethargy.

Since amitriptyline is also characterized by alpha-adrenolytic action, against the background of the use of this medication, the patient may develop orthostatic hypotension, accompanied by collaptoid conditions, weakness, fainting, and tachycardia. Paresthesia is also often noted. In addition, allergic reactions very often occur.

One of the most dangerous side effects of a course of therapy given drug it is considered to be a violation of the heart rhythm. In the event of such disorders, it is very important to reduce the total dosage of amitriptyline as soon as possible. Immediately, let us draw the attention of readers to the fact that during the treatment with this medication, the patient may also have seizures, which, with all their appearance will resemble seizures of epilepsy. In such cases, in addition to amitriptyline, patients are also prescribed anticonvulsant medications. Especially often convulsive states develop in patients who have any trauma or damage to the brain or skull.

If the patient has schizophrenia or major depression, the use of this pharmaceutical product may lead to the development of hypomania, mania or dysphoric-irritable state. For such patients, amitriptyline is most often replaced with other suitable medications, along with which they can also be prescribed antipsychotics, normotimics, hormonal agents, and so on. In all cases, it all depends on the general state of health, as well as the diagnosis. In conclusion, we note that any changes in your health due to the use of amitriptyline should be urgently discussed with a specialist. Otherwise, complications can be very serious and sometimes even life-threatening.

Before use, you must consult a specialist.

Reviews

It helps me to live very well.

The first time the doctor prescribed me for cervical osteochondrosis, my head ached terribly that I could not sleep, I drank 1/4 for 3 hours before bedtime. I slept soundly, and walked very calmly and contentedly, then increased the dose to 1 tablet. I drank for a month, there were no addictions, I stopped. Then I drink not as intended. They are very soothing, and when nervous breakdowns I increase the dose to 3 tablets. Their parishes distract from problems, and life is beautiful. True, inhibition of thinking and speech is observed, and vision deteriorates.

I drink these pills for the third day, one pill each in the morning, as the doctor said, I slept all day yesterday.

This drug caused my husband's death. The doctor prescribed 3 tablets a day to his 66-year-old husband, who is undergoing rehabilitation. Three days later, he felt really bad, read the contraindications and canceled it herself, since the doctor was on vacation. After another 10 days, the husband died suddenly. Autopsy showed neither a secondary stroke, nor myocardial infarction, nor the presence of blood clots

I have been taking amitriptyline for a year with the minimum dosage, i.e. 10mg. 1 tablet at night. I sleep well, in the morning and in the afternoon there is no sleepiness. And dreams are just wonderful. I took a break for 1 month. No addictions or withdrawal symptoms. In general, as a good sleeping pill acts gently. The main thing is the dosage.

Tell me, is it generally from a migraine or an antidiprisant, the doctor told me to drink it from a migraine? I do not suffer from depression and do not suffer from neurosis. Does the doctor say this for a migraine?

I was diagnosed with deep depression! And they prescribed me half a pill for the night of amitriptyline! The third day I drink in the morning, everything is fine, but starting from two o'clock the whole body begins to pound, especially the head, face, and hands! I think to stop taking this device! Or is it an addictive organism?

I was given droppers with amitriptyline. relieves anxiety and irritability. But it gives lethargy and drowsiness.

I drank amitriptyline many times due to neurosis, it helps me well, the only thing I always take is imported, our pharmacy does not inspire confidence.

Diagnosed with depression and anxiety disorder, I drink the third week, the sensations are strange, but it helps from anxiety, distracts from depression with its effects))) as if constant drunkenness, the first three days I slept without getting up, my vision deteriorates, the appetite for some reason appeared on the contrary, although it is written that it usually decreases, tremor hands, dreams are vivid and meaningful))

Amitriptyline was prescribed to me for the first week 1/2, the second 1 tablet at night, the third week at lunchtime 1 and at night 2 tablets. The first week I got used to the drug, the second week it became easier, in the third week before lunch I was drowsy. Further general state in addition to drowsiness, it worsened, lethargy and delayed reaction appeared ... and I decided to take only 1 tablet at night. I take it for about 5 months and the doctor prescribed it for 6 months. Today I have an unpleasant sensation in the mouth in the morning, i.e. bitterness, dryness and heartburn. I think that I will no longer take amitriptyline ...

I was prescribed amitriptyline only once, but I was unable to complete the full course of therapy with this drug. The thing is that this medication caused my heart rhythm disturbances. As soon as I noticed this, I immediately called my doctor, who replaced this drug another pharmaceutical agent. It seems to me that I myself am to blame for what happened, since I did not quite clearly follow the dosages prescribed for me. Since then, I have been paying special attention to all medicines.