Why is amitriptyline dangerous? The drug amitriptyline - instructions for use and interactions with other drugs Amitriptyline instructions for use side effects

Name:

Amitriptyline (Amitriptylinum)

Pharmacological
action:

Amitriptyline- tricyclic antidepressant from the group of non-selective inhibitors neuronal uptake of monoamines. It has a pronounced thymoanaleptic and sedative effect.

Pharmacodynamics
The mechanism of the antidepressant action of amitriptyline is associated with inhibition of the reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin into the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and in the periphery, and has peripheral antihistamine (H1) and antiadrenergic properties. It also causes antineuralgic (central analgesic), antiulcer and antibulemic effects, and is effective for bedwetting. The antidepressant effect develops within 2-4 weeks. After starting use.

Pharmacokinetics
The bioavailability of amitriptyline through various routes of administration is 30-60%, its active metabolite nortriptyline is 46-70%. Time to reach maximum concentration (Tmax) after oral administration is 2.0-7.7 hours. Volume of distribution is 5-10 l/kg. Effective therapeutic concentrations in the blood of amitriptyline are 50-250 ng/ml, for nortriptyline (its active metabolite) 50-150 ng/ml. Maximum concentration in blood plasma (Cmax) -0.04-0.16 mcg/ml. Passes through histohematic barriers, including the blood-brain barrier (including nortriptyline). Amitriptyline concentrations in tissues are higher than in plasma. Communication with plasma proteins is 92-96%. Metabolized in the liver (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. The plasma half-life ranges from 10 to 28 hours for amitriptyline and from 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 and is excreted into breast milk in concentrations similar to plasma concentrations.

Indications for
application:

Depression of any etiology. It is especially effective for anxiety and depression due to the severity of the sedative effect. Does not cause exacerbation of productive symptoms (delusions, hallucinations), unlike antidepressants with a stimulating effect.
- Neurogenic pain of a chronic nature.
- Mixed emotional and behavioral disorders, phobic disorders.
- Children's enuresis (except for children with a hypotonic bladder).
- Psychogenic anorexia, bulimic neurosis.

Mode of application:

Prescribed orally(during or after meals).

Initial daily dose 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 dose is taken at night). For severe depression resistant to therapy, the dose is increased to 300 mg or more, to the maximum tolerated dose. In these cases, it is advisable to begin treatment with intramuscular or intravenous administration of the drug, using higher initial doses, accelerating the increase in dosage under the control of the somatic condition.

After obtaining a stable antidepressant effect after 2-4 weeks, the dose is gradually and slowly reduced. If signs of depression appear when reducing doses, you should return to the previous dose.

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

In elderly patients for mild disorders, in outpatient practice, doses are 25-50-100 mg (max) in divided doses or 1 time per day at night. For the prevention of migraines, chronic neurogenic pain (including long-term headaches) from 12.5-25 mg to 100 mg/day. Interaction with other drugs Amitriptyline potentiates the inhibition of the central nervous system by the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, central and narcotic analgesics, anesthetics, alcohol.

Prescribed intramuscularly or intravenously. For severe depression resistant to therapy: intramuscularly or intravenously (administer slowly!) at 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 orally. Children over 12 years of age and the elderly are given lower doses and increased more slowly.

And/or anticholinergic drugs may cause febrile fever and paralytic ileus. Amitriptyline potentiates the hypertensive effects of catecholamines, but inhibits the effects of drugs affecting the release of norepinephrine.

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

When taking amitriptyline and cimetidine simultaneously increased plasma concentrations of amitriptyline are possible.

Concomitant use 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!

Side effects:

Caused by blockade of peripheral m-cholinergic receptors: dry mouth, urinary retention, constipation, intestinal obstruction, blurred vision, accommodation paresis, increased intraocular pressure, increased sweating.

From the nervous system and sensory organs: headache, dizziness, ataxia, increased fatigue, weakness, irritability, drowsiness, insomnia, nightmares, motor agitation, tremor, paresthesia, peripheral neuropathy, EEG changes, impaired concentration, dysarthria, confusion, hallucinations, tinnitus .

From the cardiovascular system: tachycardia, orthostatic hypotension, arrhythmia, blood pressure lability, widening of the QRS complex on the ECG (impaired intraventricular conduction), symptoms of heart failure, fainting, changes in the blood picture, incl. agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura.

From the gastrointestinal tract: nausea, vomiting, heartburn, anorexia, discomfort in the epigastrium, gastralgia, increased activity of liver transaminases, stomatitis, taste disturbance, darkening of the tongue.

Metabolism: galactorrhea, changes in ADH secretion; rarely - hypo- or hyperglycemia, impaired glucose tolerance.

From the genitourinary system: changes in libido, potency, testicular swelling, glucosuria, pollakiuria.

Allergic reactions: skin rash, itching, angioedema, urticaria.

Others: increase in the size of the mammary glands in women and men, hair loss, enlarged lymph nodes, photosensitivity, weight gain (with long-term use), withdrawal syndrome: headache, nausea, vomiting, diarrhea, irritability, sleep disturbance with vivid, unusual dreams, increased excitability (after long-term treatment, especially in high doses, with abrupt cessation of the drug).

Contraindications:

Heart failure in the stage of decompensation.
- Acute and recovery period of myocardial infarction.
- Conduction disorders of the heart muscle.
- Severe arterial hypertension.
- Acute diseases of the liver and kidneys, with severe dysfunction.
- Blood diseases.
- Peptic ulcer of the stomach and duodenum in the acute stage.
- Prostate hypertrophy.
- Atony of the bladder.
- Pyloric stenosis, paralytic intestinal obstruction.
- Simultaneous treatment with MAO inhibitors (see Interaction).
- Pregnancy, breastfeeding period.
- Children under 6 years of age (for oral administration),
- Children under 12 years of age (for IM and IV administration),
- Hypersensitivity to amitriptyline.
Amitriptyline should be used with caution in persons suffering from alcoholism, bronchial asthma, manic-depressive psychosis (MDP) and epilepsy (see Special Instructions), suppression of bone marrow hematopoiesis, hyperthyroidism, angina pectoris and heart failure, angle-closure glaucoma, intraocular hypertension, schizophrenia (although when taking it there is usually no exacerbation of productive symptoms).

Interaction
other medicinal
by other means:

Amitriptyline enhances the inhibitory effect on the central nervous system the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; exhibits synergism when interacting with other antidepressants. When combined with amitriptyline and antipsychotics, and/or anticholinergic drugs, a febrile temperature reaction and paralytic intestinal obstruction may occur. Amitriptyline potentiates the hypertensive effects of catecholamines and other adrenergic stimulants, which increases the risk of developing heart rhythm disturbances, tachycardia, severe arterial hypertension, but inhibits the effects of drugs affecting the release of norepinephrine. Amitriptyline may reduce antihypertensive effects 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 - derivatives of coumarin or indanedione, an increase in the anticoagulant activity of the latter is possible. When taking amitriptyline and cimetidine simultaneously it is possible to increase the plasma concentration of amitriptyline with the possible development of toxic effects. Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduce plasma concentrations of amitriptyline. Amitriptyline enhances the effect of antiparkinsonian drugs and other drugs that cause extrapyramidal reactions. Quinidine slows down the metabolism of amitriptyline. Concomitant use of amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors may precipitate delirium. Estrogen-containing oral contraceptives may increase the bioavailability of amitriptyline; Pimozide and probucol may increase cardiac arrhythmias. Amitriptyline may enhance depression caused by glucocorticosteroids; combined use with drugs for the treatment of thyrotoxicosis increases the risk of developing agranulocytosis. Concomitant use 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!

Pregnancy:

Application of Amitriptyline contraindicated during pregnancy and lactation.

Overdose:

Symptoms: drowsiness, disorientation, confusion, dilated pupils, increased body temperature, shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle rigidity, suppuration, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression.
Treatment: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Monitoring of cardiovascular activity (ECG) is indicated for 5 days, because relapse may occur within 48 hours or later. Hemodialysis and forced diuresis are not very effective.

Release form:

Pills:
Packaging - 50 tablets, each containing 25 mg of active substance.
Packages of 20, 50 and 100 film-coated tablets.
2 ml in colorless glass ampoules. 5 ampoules are packed in a molded PVC container. 2 molded containers (10 ampoules) along with instructions for use are placed in a cardboard box.
Injection 10 mg/ml in ampoules of 2 ml, 5 or 10 ampoules per cardboard pack; 5 ampoules per blister pack, 1 or 2 blister packs per cardboard pack along with instructions for use.

Description of the solution:
Transparent, colorless, free of mechanical inclusions, may be slightly colored.

Storage conditions:

At a temperature of 10 °C to 25 °C in a dry place, protected from light and out of reach of children.

Best before date- 2-3 years (depending on the form of release and manufacturer). Do not take after the expiration date indicated on the package!

Conditions for dispensing from pharmacies - by doctor's prescription.

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

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

Drug: AMITRIPTYLINE

Active substance of the drug: amitriptyline
ATX encoding: N06AA09
KFG: Antidepressant
Registration number: P No. 015860/01
Registration date: 07.22.04
Owner reg. cert.: ZENTIVA a.s. (Czech Republic)

Amitriptyline release form, drug packaging and composition.

The solution for intramuscular administration is transparent, colorless, and does not contain mechanical inclusions.
1 ml
1 amp.
amitriptyline hydrochloride
10 mg
20 mg

Excipients: dextrose, water for injection.

2 ml - ampoules (5) - molded containers (2) - cardboard packs.

Yellow film-coated tablets, round, biconvex; 2 layers are visible on the cross section.
1 tab.
amitriptyline hydrochloride
25 mg

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

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

10 pieces. - blisters (2) - cardboard packs.
10 pieces. - blisters (5) - cardboard packs.
10 pieces. - blisters (10) - cardboard packs.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All information provided is provided for information only about the drug; you should consult your doctor about the possibility of use.

Pharmacological action Amitriptyline

An antidepressant from the group of tricyclic compounds, a derivative of dibenzocycloheptadine.

The mechanism of antidepressant action is associated with an increase in the concentration of norepinephrine in synapses and/or serotonin in the central nervous system due to inhibition of the reverse neuronal uptake of these mediators. With long-term use, it reduces the functional activity of adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, and restores the balance of these systems, disturbed during depressive states. In anxiety-depressive conditions, it reduces anxiety, agitation and depressive symptoms.

It also has some analgesic effect, which is believed to be associated with changes in the concentrations of monoamines in the central nervous system, especially serotonin, and effects on endogenous opioid systems.

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

It has an antiulcer effect, the mechanism of which is due to the ability to block histamine H2 receptors in the parietal cells of the stomach, as well as to have a sedative and anticholinergic effect (for gastric and duodenal ulcers, it reduces pain and helps accelerate ulcer healing).

Efficacy for bedwetting is apparently due to anticholinergic activity, leading to an increase in the ability of the bladder to stretch, direct -adrenergic stimulation, and the activity of -adrenergic receptor agonists, accompanied by an increase in sphincter tone and central blockade of serotonin uptake.

The mechanism of therapeutic action for bulimia nervosa has not been established (possibly similar to that for depression). Amitriptyline has been shown to be clearly effective against bulimia in patients both without and with depression, while a decrease in bulimia can be observed without a concomitant decrease in depression itself.

During general anesthesia it reduces blood pressure and body temperature. Does not inhibit MAO.

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

Pharmacokinetics of the drug.

The bioavailability of amitriptyline is 30-60%. Plasma protein binding 82-96%. Vd - 5-10 l/kg. Metabolized to form the active metabolite nortriptyline.

T1/2 - 31-46 hours. Excreted mainly by the kidneys.

Indications for use:

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug-induced, with organic brain damage, alcohol withdrawal), schizophrenic psychoses, mixed emotional disorders, behavioral (activity) disorders and attention), nocturnal enuresis (except for patients with bladder hypotension), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical pain in the face, post-herpetic neuralgia, post-traumatic neuropathy, diabetic neuropathy, peripheral neuropathy), migraine prevention, peptic ulcer of the stomach and duodenum.

Dosage and method of administration of the drug.

For oral administration, the initial dose is 25-50 mg at night. Then, over 5-6 days, the dose is individually increased to 150-200 mg/day (most of the dose is taken at night). If there is no improvement during the second week, the daily dose is increased to 300 mg. When signs of depression disappear, the dose is reduced to 50-100 mg/day and therapy is continued for at least 3 months. In elderly patients with mild disorders, the dose is 30-100 mg/day, usually 1 time/day at night; after achieving a therapeutic effect, they switch to the minimum effective dose - 25-50 mg/day.

For nocturnal enuresis in children aged 6-10 years - 10-20 mg/day at night, in children aged 11-16 years - 25-50 mg/day.

IM - the initial dose is 50-100 mg/day in 2-4 injections. If necessary, the dose can be gradually increased to 300 mg/day, in exceptional cases - up to 400 mg/day.

Side effects of Amitriptyline:

From the central nervous system and peripheral nervous system: drowsiness, asthenia, fainting, anxiety, disorientation, agitation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, motor restlessness, manic state, hypomanic state, aggressiveness, disturbance memory, depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of symptoms of psychosis, headache, myoclonus, dysarthria, tremor (especially of the hands, head, tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus , ataxia, extrapyramidal syndrome, increased frequency and intensification of epileptic seizures, changes in the EEG.

From the cardiovascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific changes on the ECG (ST interval or T wave), arrhythmia, blood pressure lability, intraventricular conduction disturbances (widening of the QRS complex, changes in the PQ interval, bundle branch block ).

From the digestive system: nausea, heartburn, vomiting, gastralgia, increased or decreased appetite (increased or decreased body weight), stomatitis, change in taste, diarrhea, darkening of the tongue; rarely - liver dysfunction, cholestatic jaundice, hepatitis

From the endocrine system: testicular swelling, gynecomastia, breast enlargement, galactorrhea, changes in libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inadequate ADH secretion.

From the hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.

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

Effects due to anticholinergic activity: dry mouth, tachycardia, accommodation disturbances, blurred vision, mydriasis, increased intraocular pressure (only in individuals with a narrow anterior chamber angle), constipation, paralytic ileus, urinary retention, decreased sweating, confusion, delirium or hallucinations.

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

Contraindications to the drug:

Acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute intoxication with hypnotics, analgesics and psychotropic drugs, closed-angle glaucoma, severe disturbances of AV and intraventricular conduction (bundle branch block, AV block of the second degree), lactation period, children up to 6 years of age (for oral administration), children up to 12 years of age (for intramuscular and intravenous administration), simultaneous treatment with MAO inhibitors and a period of 2 weeks before the start of their use, hypersensitivity to amitriptyline.

Use during pregnancy and lactation.

Amitriptyline should not be used during pregnancy, especially in the first and third trimesters, unless absolutely necessary. Adequate and strictly controlled clinical studies of the safety of amitriptyline during pregnancy have not been conducted.

Excreted in breast milk and may cause drowsiness in nursing infants.

Amitriptyline should be gradually discontinued at least 7 weeks before the expected birth to avoid withdrawal syndrome in the newborn.

In experimental studies, amitriptyline had a teratogenic effect.

Special instructions for the use of Amitriptyline.

Use with caution for ischemic heart disease, arrhythmia, heart block, heart failure, myocardial infarction, arterial hypertension, stroke, chronic alcoholism, thyrotoxicosis, and during therapy with thyroid drugs.

During amitriptyline therapy, caution is required when abruptly moving to a vertical position from a “lying” or “sitting” position.

If you stop taking it abruptly, withdrawal syndrome may develop.

Amitriptyline in doses of more than 150 mg/day reduces the seizure threshold; the risk of developing epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors that increase the risk of developing convulsive syndrome (including brain damage of any etiology, simultaneous use of antipsychotic drugs, during the period of ethanol withdrawal or drug withdrawal, having anticonvulsant activity).

It should be taken into account that patients with depression may experience suicide attempts.

Should only be used in combination with electroconvulsive therapy under close medical supervision.

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

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

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

With long-term use, an increase in the incidence of caries is observed. The need for riboflavin may increase.

Amitriptyline can be used no earlier than 14 days after discontinuation of MAO inhibitors.

Should not be used simultaneously with adrenergic and sympathomimetics, incl. with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.

Use with caution simultaneously with other drugs that have anticholinergic effects.

Avoid drinking alcohol while taking amitriptyline.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, you should refrain from potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Interaction of Amitriptyline with other drugs.

When used simultaneously with drugs that have a depressant effect on the central nervous system, a significant increase in the inhibitory effect on the central nervous system, hypotensive effect, and respiratory depression is possible.

When used simultaneously with drugs that have anticholinergic activity, the anticholinergic effects may be enhanced.

With simultaneous use, it is possible to enhance the effect of sympathomimetic drugs on the cardiovascular system and increase the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.

When used simultaneously with antipsychotics (neuroleptics), metabolism is mutually inhibited, and the threshold for convulsive readiness decreases.

When used simultaneously with antihypertensive drugs (with the exception of clonidine, guanethidine and their derivatives), the antihypertensive effect and the risk of developing orthostatic hypotension may be increased.

When used simultaneously with MAO inhibitors, a hypertensive crisis may develop; with clonidine, guanethidine - the hypotensive effect of clonidine or guanethidine may be reduced; with barbiturates, carbamazepine - the effect of amitriptyline may be reduced due to an increase in its metabolism.

A case of the development of serotonin syndrome with simultaneous use with sertraline has been described.

When used simultaneously with sucralfate, the absorption of amitriptyline decreases; with fluvoxamine - the concentration of amitriptyline in the blood plasma and the risk of developing toxic effects increases; with fluoxetine - the concentration of amitriptyline in the blood plasma increases and toxic reactions develop due to inhibition of the CYP2D6 isoenzyme under the influence of fluoxetine; with quinidine - the metabolism of amitriptyline may be slowed down; with cimetidine - it is possible to slow down the metabolism of amitriptyline, increase its concentration in the blood plasma and develop toxic effects.

When used simultaneously with ethanol, the effect of ethanol is enhanced, especially during the first few days of therapy.

"Amitriptyline" is widely used by medical psychotherapists and psychiatrists to eliminate symptoms of depression, insomnia, anxiety and fear.
The drug amitriptyline, in addition to its antidepressant effect (unlike antidepressants SSRIs - Selective Serotonin Reuptake Inhibitors) is a non-selective inhibitor of monoamine uptake (serotonin, dopamine, norepinephrine...), and additionally has a calming, anti-anxiety and hypnotic effect.

Thus, amitriptyline tablets will help you relieve some depressive and neurotic symptoms, but they are unlikely to cure the disease itself, its source.
To find out more, including about analogues of this drug, read the article to the end.

Amitriptyline tablets - indications for use

Indications for the use of Amitriptyline, in addition to depression, neurotic manifestations, fears and phobias, insomnia and anxiety, are neurotic personality disorders such as anorexia, bulimia, neurogenic pain, migraine and even enuresis in children.
Only your attending physician can prescribe the drug and dose. Don’t experiment on your health, don’t play psychotherapist - consult a specialist on Skype.

Amitriptyline - side effects, contraindications and complications

The side effects of amitriptyline are wide and varied. This antidepressant drug has many contraindications and complications, especially if the medication is taken incorrectly and unsupervised by a doctor.

Side effects when taking amitriptyline are more pronounced and more dangerous than other tricyclic antidepressants. Unlike selective antidepressants (SSRIs), this medicine is much less tolerated by patients.

The main side effects and effects of amitriptyline:
dry mouth, difficulty focusing vision, constipation, even intestinal obstruction, difficulty urinating, hand tremors, drowsiness, lethargy, dizziness, apathy and passivity, weakness, decreased blood pressure, tachycardia, fainting, convulsions, decreased libido and potency, etc.

Complications associated with taking amitriptyline:
At large doses there is a possibility of death. In severely depressed patients, amitriptyline may provoke suicidal thoughts, possibly leading to actual behavior. Also, some neurotic disorders may develop: hypochondria, depersonalization, asthenia...

Amitriptyline contraindications:
Amitriptyline should not be used in a state of intoxication, with coronary heart disease, with myocardial infarction, arrhythmia, with atony of the bladder, intestinal obstruction, diseases of the prostate, thyroid gland, or during pregnancy.

While taking this medicine, you should never drive a car or use other machinery, or go to work where increased attention and reactions are required.

Amitriptyline - reviews from patients and psychotherapists

Reviews from patients taking amitriptyline who suffer from depression and other psychological and emotional personality disorders are almost unambiguous - the drug helps relieve some symptoms and improve the overall psycho-emotional state, but only while the patient is taking these pills. Because amitriptyline does not cure the disease itself, so when the dose is reduced or completely discontinued, which, by the way, cannot be done abruptly, the symptoms return.

Reviews of amitriptyline from medical psychotherapists are mixed, but many of them prescribe this drug, especially in free clinics.
Non-medical psychotherapists, for the most part, have a negative attitude towards long-term use of this antidepressant. They suggest taking amitriptyline tablets in crisis situations, but in the future they prefer to treat the disease itself with various psychotherapeutic methods and techniques, without drugs.

Amitriptyline - analogues

If you want to get rid of depression, neuroses, anxiety and fears, then here you will really get help without amitriptyline and side effects.

Amitriptyline dragees and tablets contain 10 or 25 mg of the active substance in the form 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.

Release form

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

pharmachologic effect

Tricyclic antidepressant . Has a sedative, thymoleptic effect. It has an additional analgesic effect of central origin.

Pharmacodynamics and pharmacokinetics

MNN: Amitriptyline.

The drug reduces appetite, eliminates nighttime urinary incontinence, and has antiserotonin action. The drug has a strong central and peripheral anticholinergic effect. 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 during anxiety and depression . By blocking H2-histamine receptors in the stomach wall (parietal cells), an antiulcer effect is provided. The medication is able to reduce body temperature, the level 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.

Indications for use of Amitriptyline

What are tablets and solution usually prescribed for?

The drug is indicated for depression (agitation, anxiety, sleep disorders, alcohol withdrawal, with organic brain lesions, neurotic withdrawal), with behavioral disorders, mixed emotional disorders, nocturnal enuresis , chronic pain syndrome (with cancer, with postherpetic neuralgia ), for bulimia nervosa, for migraine (for prevention), for. Indications for the use of Amitriptyline in tablets and in other forms of release are the same.

Contraindications

According to the annotation, the medicine is not used if the main component is intolerant, if angle-closure glaucoma , acute intoxication with psychoactive, analgesic, hypnotics, and acute alcohol intoxication. The medication is contraindicated in breastfeeding, severe intraventricular conduction disorders, and antioventricular conduction disorders. With pathology of the cardiovascular system, with suppression of bone marrow hematopoiesis, manic-depressive psychoses , chronic alcoholism, decreased motor function of the digestive system, stroke, liver and kidney pathology, intraocular hypertension , urinary retention, prostatic hyperplasia, bladder hypotension, thyrotoxicosis, pregnancy, epilepsy Amitriptyline is prescribed with caution.

Side effects of Amitriptyline

Nervous system: agitation, hallucinations, 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, headaches.

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

The 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, 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. Also noted hypoproteinemia , pollakiuria, urinary retention, enlarged lymph nodes, hyperpyrexia, swelling, tinnitus, hair loss.

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

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

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.

Overdose

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

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

Also noted are oliguria, increased sweating, hyperthermia , vomiting, shortness of breath, depression of the respiratory system, cyanosis. 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

Hypotensive effect respiratory depression , a depressant effect on the nervous system is observed with the joint prescription of medications that depress the functioning of the central nervous system: general anesthetics, benzodiazepines, barbiturates, antidepressants and others. The drug increases the severity of the anticholinergic effect when taken , antihistamines , biperiden, atropine, antiparkinsonian drugs, phenothiazine. The drug enhances the anticoagulant activity of indadione, coumarin derivatives, and indirect anticoagulants. There is a decrease in efficiency alpha blockers , phenytoin. , 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 methyldopa , betanidine, guanethidine, reduces the severity of their hypotensive effect. When taking cocaine, arrhythmia develops. Delirium develops when taking acetaldehydrogenase inhibitors. Amitriptyline enhances the effects on the cardiovascular system , norepinephrine, , isoprenaline. The risk of hyperpyrexia increases when taking antipsychotics and m-anticholinergics.

Terms of sale

Prescription or not? The medicine is not sold without a prescription.

Storage conditions

In a dry, dark place, out of reach of children, at a temperature of no more than 25 degrees Celsius.

Best before date

No more than 3 years.

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, bed rest must be observed. 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 when developing epileptic seizures in patients with a predisposition. Possible development of 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. Caution should be exercised 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 development. The need for riboflavin may increase. Amitriptyline passes into breast milk and causes increased drowsiness in infants. The medication affects driving.

The medicine is described in Wikipedia.

Amitriptyline and alcohol

Amitriptyline analogues

Level 4 ATX code matches:

Analogues of the drug are: Saroten And Amitriptyline Hydrochloride .

One of the first antidepressant drugs is Amitriptyline, the side effects of which are known not only to specialists, but also to those patients who have resorted to this method of treatment. Despite this, this drug is now widely used for problems such as emotional disorders and other diseases, which will be described below.

Despite the presence of a considerable number of side effects of Amitriptyline, this drug is quite well tolerated by most patients, provided that all required precautions are strictly followed.

Amitriptyline is prescribed for depression of various origins, mixed emotional disorders, behavioral disorders, phobias, psychogenic anorexia or bulimia, and migraine. The use of this medicine in the treatment of children from enuresis (urinary incontinence) is allowed.

This drug is an antidepressant that belongs to the group of tricyclic compounds. Its work is to prevent the secondary uptake of those substances that transmit nerve impulses in neurons (norepinephrine, acetylcholine, serotonin, dopamine), so their number in the brain increases. It is with an excess of the above substances that most of the side effects from the drug are associated.

In order for the patient to avoid unpleasant effects as much as possible when taking the drug, it is necessary to take into account all the features of its mechanism of action before using the drug. This can only be done by a specialist, so do not start taking an antidepressant without consulting your doctor. Side effects due to acetylcholine suppression. Acetylcholine, as a substance that transmits nerve impulses, is responsible for causing some physiological effects. The anticholinergic effect, that is, the cessation of the action of the substance, may have the opposite effect. Usually, the consequences appear already at the first stage of treatment with Amitriptyline. And here we can name the following side effects:

1. The iris of the eye does not contract, so the pupil stops responding to light and stops at the dilated stage. This makes vision blurry. Possible increase in intraocular pressure.
2. Decreased saliva production, dry mouth.
3. Suppression of the intestinal motor muscles, which leads to constipation and, less commonly, intestinal obstruction.
4. Suppression of motor function of the urinary tract. Hence the urinary retention.
5. Increased body temperature.

Side effects affecting the nervous systems

Since Amitriptyline is a drug that has a psychotropic effect, patients may experience certain side effects in the central and peripheral nervous systems:

1. General weakness, high fatigue.
2. Poor sleep, nightmares, difficulty falling asleep.
3. Migraine.
4. Dizziness.
5. Increased irritability, anxiety.
6. Ataxia is one of the motor disorders and a similar disorder of motor coordination.
7. Decreased concentration, difficulty pronouncing individual sounds or even words.
8. Sensory impairment.
9. Confusion and disorientation in the area are less common; hallucinations may be a possible side effect.
10. Cramps.

Side effects regarding other organs and systems

If Amitriptyline is prescribed, the instructions for use of the drug are signed by the doctor. In the area of ​​the circulatory system, changes may be observed such as increased heart rate or simply a disturbance in its rhythm, surges in blood pressure, signs of heart failure, and short-term loss of consciousness.

As for the blood condition, there may be changes in sugar levels, as well as a decrease in the total number of white blood cells and platelets. The second leads to decreased immunity and increased bleeding.

From the gastrointestinal tract, reactions to Amitriptyline include nausea and vomiting, heartburn, stomatitis, changes in taste, abdominal pain, constipation or diarrhea (may occur one after the other). Possible liver dysfunction. While taking Amitriptyline, hormonal disturbances may occur, manifested in breast enlargement in both men and women; discharge from the mammary glands; sexual dysfunction.

Other side effects include varying degrees of hair loss, weight changes - often upward, as well as profuse sweating, various allergic reactions, such as rashes, discharge on the skin.

Amitriptyline: instructions for use

Amitriptyline is prescribed for oral use immediately after meals. It is not advisable to chew the tablet to ensure minimal irritation of the stomach walls. The first dosage is 25-50 mg and is taken by an adult patient at bedtime. Over the course of five days, it is necessary to increase the dose to 200 mg per day in three doses. If the effect does not occur within two weeks, the dose may be increased by another 100 mg.

If Amitriptyline is prescribed in the form of a solution, it should be administered both intravenously (slowly) and intramuscularly. The dosage is 20-40 mg four times a day with a gradual transition to the oral route of taking the drug.

The course of treatment with Amitriptyline should not exceed eight months.

If after three to four weeks no changes are observed, then continuing treatment with the drug is not advisable and can lead to negative consequences and a deterioration in the condition of the patient taking the drug.