Amitriptyline Akos, solution for injection (ampoules). Amitriptyline solution for intravenous and intramuscular administration "Moscow endocrine plant" Amitriptyline 10 mg therapeutic dose

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This medicine has been prescribed for you personally and should not be given to others as it may harm them even if they have the same symptoms as you.

INSTRUCTIONS FOR THE MEDICAL USE OF THE MEDICINE AMITRIPTYLINE

Registration number: Р N002756/02-071114
Brand name: Amitriptyline
International non-proprietary name: Amitriptyline
Chemical name: 3-(10,11-Dihydro-5H-dibenzo-[a,d]-cyclohepten-5-ylidene)-N,N-dimethylpropan-1-amine hydrochloride
Dosage form: solution for intravenous and intramuscular administration

Compound
1 ml of solution contains:
Active substance:
amitriptyline hydrochloride - 11.31 mg,
equivalent to 10.0 mg amitriptyline
Excipients:
dextrose monohydrate
in terms of dextrose - 40.0 mg,
sodium chloride - 2.6 mg,
benzethonium chloride - 0.1 mg,
hydrochloric acid or sodium hydroxide - up to pH 4.0-6.0,
water for injection - up to 1 ml.

Description: Clear, colorless or slightly colored liquid.

Pharmacotherapeutic group: antidepressant

ATX code: N06AA09

Pharmacological properties

Amitriptyline is a tricyclic antidepressant with a sedative effect.
Pharmacodynamics
Amitriptyline equally inhibits the reuptake of norepinephrine and serotonin in the presynaptic nerve ending. The main metabolite of amitriptyline, nortriptyline, inhibits the reuptake of norepinephrine rather than serotonin more strongly. It has anticholinergic and H1-histamine activity. It has a powerful antidepressant, sedative and anxiolytic effect.
Pharmacokinetics
Suction
Amitriptyline has a high absorption. The time to reach the maximum concentration (Tcmax) after oral administration is 4-8 hours, Cmax is 0.04-0.16 μg / ml. The equilibrium concentration is reached approximately 1-2 weeks after the start of the course of treatment. Amitriptyline concentrations in tissues are higher than in plasma. The bioavailability of amitriptyline with various routes of administration is 33-62%, its active metabolite nortriptyline is 46-70%. Distribution volume (Vd) - 5-10 l/kg. Effective therapeutic concentrations of amitriptyline in the blood are 50-250 ng / ml, for nortriptyline (its active metabolite) - 50-150 ng / ml. Communication with plasma proteins - 92-96%. Amitriptyline passes through histohematological barriers, including the blood-brain barrier (including nortriptyline), penetrates the placental barrier, is excreted in breast milk at concentrations similar to plasma.
Metabolism
The metabolism of amitriptyline is carried out mainly due to demethylation (CYP2D6, CYP3A isoenzymes) and hydroxylation (CYP2D6 isoenzyme) followed by conjugation with glucuronic acid. Metabolism is characterized by significant genetic polymorphism. The main active metabolite is the secondary amine, nortriptyline. The metabolites cis- and trans-10-hydrosiamitriptyline and cis- and trans-10-hydroxynortriptyline are characterized by an activity profile similar to that of nortriptyline, although their action is much less pronounced. Demethylnortriptyline and amitriptyline-N-oxide are present in the blood plasma in negligible concentrations; the last metabolite is practically devoid of pharmacological activity. In comparison with amitriptyline, all metabolites have a significantly less pronounced m-anticholinergic effect.
The main factor determining the renal clearance, and, accordingly, the concentration in the blood plasma, is the rate of hydroxylation. A small proportion of people have genetically determined delayed hydroxylation.
breeding
The half-life (T1 / 2) from blood plasma is 10-28 hours for amitriptyline, for nortriptyline - 16-80 hours. The average total clearance of amitriptyline is 39.24 ± 10.18 l / h. Amitriptyline is excreted mainly by the kidneys and through the intestines in the form of metabolites. About 50% of the administered amitriptyline is excreted in the urine as 10-hydroxyamitriptyline and its glucuronic acid conjugate, about 27% is excreted as 10-hydroxy-nortriptyline, and less than 5% of amitriptyline is excreted as the parent substance and nortriptyline. Complete elimination of amitriptyline from the body occurs within 7 days.
Elderly patients
In elderly patients, there is an increase in the half-life and a decrease in the clearance of amitriptyline due to a decrease in the metabolic rate.
Patients with impaired liver function
Impaired liver function can lead to a slowdown in the metabolism of amitriptyline and an increase in its plasma concentrations.
Patients with impaired renal function
In patients with impaired renal function, the excretion of metabolites of amitriptyline and nortriptyline is slow, although the metabolism as such does not change. Due to its association with blood proteins, amitriptyline is not removed from the blood plasma by dialysis.

Indications for use

Endogenous depression and other depressive disorders.

Contraindications

Hypersensitivity, myocardial infarction (acute and subacute periods), arrhythmias, severe disorders of atrioventricular and intraventricular conduction (blockade of the bundle legs, atrioventricular block II degree), heart failure, acute alcohol intoxication, acute intoxication with hypnotics, analgesics and psychoactive drugs, angle-closure glaucoma, urinary retention, including with prostatic hyperplasia, paralytic ileus, pyloric stenosis, hypokalemia, concomitant use of drugs that prolong the QT interval or cause hypokalemia, lactation, children under 18 years of age.
Contraindicated simultaneous use with monoamine oxidase inhibitors (MAO) and their use within 14 days before and after the end of treatment.

Carefully

Convulsive disorders, chronic alcoholism, prostatic hyperplasia, severe liver and cardiovascular diseases, bronchial asthma, manic-depressive psychosis (MDP) and epilepsy (see section "Special Instructions"), oppression of bone marrow hematopoiesis, hyperthyroidism, thyrotoxicosis, delay urination, hypotension of the bladder, angina pectoris, increased intraocular pressure, decreased motor function of the gastrointestinal tract (risk of paralytic ileus), schizophrenia (although there is usually no exacerbation of productive symptoms when taken), old age, pregnancy, breastfeeding.
If you have one of the listed diseases, be sure to consult your doctor before taking the drug.

Use during pregnancy and during breastfeeding

Use during pregnancy is not recommended.
If the drug is used by pregnant women, it is necessary to warn about the high risk of such use for the fetus, especially in the third trimester of pregnancy. The use of high doses of tricyclic antidepressants in the third trimester of pregnancy can lead to neurological disorders in the newborn. Cases of drowsiness have been reported in newborns whose mothers used nortriptyline (a metabolite of amitriptyline) during pregnancy, cases of urinary retention were noted.
Amitriptyline passes into breast milk. The ratio of concentrations of breast milk / plasma is 0.4-1.5 in a child who is breastfed.
When using amitriptyline, breastfeeding should be discontinued.
If this is not done, the child's condition should be monitored, especially during the first four weeks after birth.
A child who is breastfed may experience unwanted reactions (see section "Side effects").

Dosage and administration

Assign intramuscularly and intravenously.
Doses of the drug are selected individually depending on the age and condition of the patient.
For depression resistant to therapy: intramuscularly and intravenously (inject slowly!) administered 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 inside.
Elderly people are given lower doses and increase them more slowly.
If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is inappropriate.
Cancel
The drug should be discontinued gradually to avoid the development of "withdrawal" symptoms.
Symptoms of "cancellation": after prolonged use with a sharp cessation of administration, adverse reactions such as nausea, vomiting, diarrhea, headache, malaise, insomnia, unusual dreams, unusual arousal, irritability may occur; after prolonged use with gradual withdrawal - irritability, sleep disturbances, unusual dreams. These symptoms do not indicate the development of addiction to the drug.

Side effect

WHO classification of adverse reactions by frequency of development
Very common - 1/10 appointments (≥ 10%)
Frequent - 1/100 appointments (≥ 1%, but< 10 %)
Infrequent - 1/1000 appointments (≥ 0.1%, but< 1 %)
Rare - 1/10000 appointments (≥ 0.01%, but< 0,1 %)
Very rare - less than 1/10,000 appointments (< 0,01 %)
Blood and lymphatic system disorders: rarely - depression of bone marrow hematopoiesis, agranulocytosis, leukopenia, thrombocytopenia, eosinophilia.
Metabolic and nutritional disorders: very often - weight gain; rarely - weight loss, loss of appetite.
Mental disorders: often - confusion, decreased libido; infrequently - hypomania, mania, anxiety, insomnia, "nightmare" dreams; rarely - delirium (in elderly patients), hallucinations (in patients with schizophrenia).
Nervous system disorders: very often - drowsiness, tremor, dizziness, headaches; often - impaired concentration, dysgeusia, paresthesia, ataxia; infrequently - convulsions.
On the part of the organ of vision: very often - a violation of accommodation; often - mydriasis; infrequently - increased intraocular pressure.
On the part of the organ of hearing and labyrinth disorders: infrequently - tinnitus.
Cardiac disorders: very often - palpitations, tachycardia, orthostatic hypotension; often - atrioventricular blockade (AV blockade), blockade of the bundle branch of His, intracardiac conduction disturbances recorded only on the ECG, but not clinically manifested (an increase in the QT interval, an increase in the QRS complex); infrequently - arterial hypertension; rarely - arrhythmia.
From the gastrointestinal tract: very often - dry mouth, constipation, nausea; infrequently - diarrhea, vomiting, swelling of the tongue; rarely - an increase in the salivary glands, paralytic ileus.
On the part of the liver and biliary tract: rarely - jaundice, a violation of the indicators of the functional state of the liver, an increase in the activity of alkaline phosphatase (AP) of the blood and transaminases.
Skin and subcutaneous tissue disorders: very often - hyperhidrosis; infrequently - skin rash, urticaria, swelling of the face; rarely - alopecia, photosensitivity reactions.
Renal and urinary disorders: infrequently - urinary retention.
Violations of the genital organs and mammary gland: often - erectile dysfunction; rarely - gynecomastia.
General disorders and disorders at the injection site: often - fatigue; rarely - pyrexia.
Withdrawal symptoms: after prolonged use with abrupt discontinuation of use, adverse reactions such as nausea, vomiting, diarrhea, headache, malaise, insomnia, unusual dreams, unusual arousal, irritability may occur; after prolonged use with gradual withdrawal - irritability, sleep disturbances, unusual dreams. These symptoms do not indicate the development of addiction to the drug.
Some of the adverse reactions, such as headache, tremors, impaired concentration, constipation and decreased libido, may be manifestations of depression and disappear as the depression resolves.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Reactions to overdose in different patients vary significantly.
In adult patients, taking more than 500 mg causes moderate or severe intoxication.
The lethal dose of amitriptyline is 1200 mg.
Symptoms
Symptoms may develop slowly and imperceptibly, or abruptly and suddenly. During the first hours there is drowsiness or agitation, agitation and hallucinations.
Anticholinergic symptoms: mydriasis, tachycardia, urinary retention, dry mucous membranes, fever, slowed intestinal motility.
Neuropsychic signs: convulsions, sudden depression of the central nervous system (CNS), decreased level of consciousness up to coma, respiratory depression.
Cardiac symptoms: As signs of overdose increase, changes in the cardiovascular system increase. Arrhythmias (ventricular tachyarrhythmia, cardiac arrhythmias like Torsade de Pointes, ventricular fibrillation). The ECG is characterized by PR interval prolongation, QRS complex widening, QT interval prolongation, T wave simplification or inversion, ST segment depression, and intracardiac conduction block of varying degrees, which can progress to cardiac arrest, low blood pressure, heart failure, intraventricular block, frequent pulse.
The expansion of the QRS complex usually correlates with the severity of toxic effects due to acute overdose.
Heart failure, decreased blood pressure, cardiogenic shock. Metabolic acidosis, hypokalemia.
After awakening, confusion, agitation, hallucinations, ataxia are again possible.
Treatment: discontinuation of amitriptyline therapy, administration of physostigmine 1-3 mg every 1-2 hours IM or IV, fluid infusion, symptomatic therapy, maintenance of blood pressure and fluid and electrolyte balance. Showing monitoring of cardiovascular activity (ECG) for 5 days, tk. relapse can occur after 48 hours or later. Hemodialysis and forced diuresis, gastric lavage are ineffective.

Interaction with other drugs

Simultaneous administration of amitriptyline and MAO inhibitors can cause serotonin syndrome (possible agitation, confusion, tremor, myoclonus, hyperthermia).
Amitriptyline may be prescribed 14 days after discontinuation of treatment with irreversible MAOIs and at least 1 day after discontinuation of therapy with the reversible MAOA inhibitor moclobemide. MAO inhibitors can be prescribed 14 days after the end of taking amitriptyline.
Amitriptyline may increase the effects of alcohol, barbiturates and other CNS depressants.
Since tricyclic antidepressants, including amitriptyline, can enhance the effect of anticholinergic drugs on the organs of vision, central nervous system, intestines and bladder, their simultaneous use should be avoided due to the risk of developing paralytic ileus, hyperpyrexia.
When taking tricyclic antidepressants in combination with anticholinergics or antipsychotics, especially in hot weather, hyperpyrexia may develop.
Amitriptyline may enhance the effect of epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine and phenylpropanolamine on the cardiovascular system; therefore, anesthetics, decongestants and other preparations containing these substances should not be used simultaneously with amitriptyline.
May reduce the antihypertensive effect of guanethidine, betanidine, reserpine, clonidine and methyldopa. With the simultaneous use of tricyclic antidepressants, it is necessary to adjust antihypertensive therapy.
When combined with antihistamine drugs, it is possible to increase the inhibitory effect on the central nervous system; with drugs that cause extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.
Simultaneous use of amitriptyline and drugs that lengthen the QT interval (antiarrhythmics (quinidine), antihistamines (astemizole and terfenadine), some antipsychotics (cisapride, halofantrine and sotalol, especially pimozide and sertindole)), increases the risk of developing ventricular arrhythmia.
Antifungal drugs, for example, fluconazole, terbinafine - increase the level of concentration of tricyclic antidepressants in serum and, accordingly, their toxicity. Possible fainting and the development of paroxysms of ventricular tachycardia (Torsade de Pointes).
Barbiturates and other enzyme inducers, such as rifampicin and carbamazepine, etc., can increase the metabolism of tricyclic antidepressants, and as a result, reduce the concentration of tricyclic antidepressants in blood plasma and reduce their effectiveness.
With simultaneous use with cimetidine, methylphenidate and calcium channel blockers, it is possible to slow down the metabolism of amitriptyline, increase its concentration in the blood plasma and develop toxic effects.
When co-administered with antipsychotics, it should be borne in mind that tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism, lowering the seizure threshold.
With the simultaneous use of amitriptyline and indirect anticoagulants (coumarin or indandione derivatives), an increase in the anticoagulant activity of the latter is possible.
Amitriptyline may exacerbate depression caused by glucocorticoid drugs (GCS).
When used together with anticonvulsant drugs, it is possible to increase the inhibitory effect on the central nervous system, lower the threshold for convulsive activity (when used in high doses) and reduce the effectiveness of the latter.
Simultaneous administration with drugs for the treatment of thyrotoxicosis increases the risk of developing agranulocytosis.
Due to the risk of arrhythmias, special care should be taken when prescribing amitriptyline to patients with hyperthyroidism or to patients receiving thyroid medications.
Fluoxetine and fluvoxamine may increase plasma concentrations of amitriptyline (may require dose reduction of amitriptyline).
When used together with anticholinergics, phenothiazines and benzodiazepines, mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (reducing the threshold of convulsive activity) are possible.
Estrogen-containing oral contraceptives and estrogens may increase the bioavailability of amitriptyline. Dosage reduction of either estrogen or amitriptyline may be necessary to restore efficacy or reduce toxicity. However, drug withdrawal may be required.
Co-administration with disulfiram and other acetaldehyde rogenase inhibitors may increase the risk of developing psychotic conditions and confusion.
When using amitriptyline together with phenytoin, the metabolism of the latter is inhibited, and the risk of its toxic effect (ataxia, hyperreflexia, nystagmus, tremor) increases. When starting the use of amitriptyline in patients receiving phenytoin, the concentration of the latter in the blood plasma should be monitored due to an increased risk of inhibition of its metabolism. At the same time, the therapeutic effect of amitriptyline should be monitored, because. you may need to increase its dose.
Hypericum perforatum preparations reduce the maximum plasma concentration of amitriptyline by approximately 20% due to activation of the hepatic metabolism of amitriptyline by the CYP3A4 isoenzyme. Which increases the risk of serotonin syndrome. This combination can be used with a dose adjustment of amitriptyline, depending on the results of measuring its concentration in blood plasma.
With the simultaneous use of valproic acid, the clearance of amitriptyline from the blood plasma decreases, which can lead to an increase in the concentration of amitriptyline and its metabolite, nortriptyline. Serum concentrations of amitriptyline and nortriptyline should be monitored when amitriptyline and valproic acid are co-administered. Dose reduction of amitriptyline may be required.
With the simultaneous use of amitriptyline in a high dose and lithium preparations for more than six months, the development of seizures and cardiovascular complications is possible. It is also possible the occurrence of signs of a neurotoxic effect in the form of tremor, memory impairment, distractibility, disorganization of thinking, even with a normal concentration of lithium in the blood and moderate doses of amitriptyline.

special instructions

Tricyclic antidepressants should not be prescribed to children and adolescents under the age of 18 due to insufficient data on the efficacy and safety of drugs in this group of patients.
Amitriptyline at doses above 150 mg / day reduces the threshold for seizure activity, so the possibility of seizure disorders in patients with a history of seizures, and with brain damage of any etiology, simultaneous use of antipsychotics, during the period of refusal of ethanol or withdrawal of drugs that have anticonvulsant properties (benzodiazepines).
Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of violations or changes in behavior, as well as suicidal tendencies.
The use of anesthetics during the course of treatment with tri- and tetracyclic antidepressants may increase the risk of arrhythmias and lower blood pressure. If possible, amitriptyline should be discontinued a few days before surgery. If emergency surgery is required, the anesthesiologist should be advised that the patient is being treated with amitriptyline.
Dry mouth and decreased tear production may occur with a relative increase in the amount of mucus in the lacrimal fluid, which can lead to damage to the corneal epithelium in contact lens wearers.

Influence on the ability to drive vehicles and mechanisms

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

Release form
Solution for intravenous and intramuscular administration of 10 mg / ml in ampoules of 2 ml.
5 ampoules in a blister pack made of PVC film and printed lacquered aluminum foil, or flexible packaging based on aluminum foil, or without foil.
1 or 2 blister packs with instructions for use, a knife or an ampoule scarifier in a pack of cardboard.
20, 50 or 100 blisters with foil with 10, 25 or 50 instructions for use, knives or ampoule scarifiers in cardboard boxes or corrugated cardboard boxes (for a hospital).
When packing ampoules with notches, rings or break points, ampoule knives or scarifiers are not inserted.

Amitriptyline is an antidepressant with a pronounced sedative, antibulemic and antiulcer effect. Instructions for use recommend taking tablets and dragees 10 mg and 25 mg, injections in ampoules for depression, psychosis, alcoholism.

Release form and composition

Amitriptyline is produced in the form:

1. Tablets 10 mg and 25 mg.
2. Dragee 25 mg.
3. Solution for intravenous and intramuscular administration (injections in ampoules for injection).

Dragees and tablets Amitriptyline contain 10 or 25 mg of the active substance in the form of amitriptyline hydrochloride.

1 ml of solution contains 10 mg of the active substance.

pharmachologic effect

The drug Amitriptyline has a pronounced sedative (sedative), thymoanaleptic (the ability to suppress depression) and anxiolytic (the ability to suppress anxiety and fear) action. The agent does not cause an exacerbation of productive symptoms: hallucinations or delusions. The drug is well absorbed in the gastrointestinal tract. The binding of amitriptyline to blood proteins reaches 90-95%.

What helps Amitriptyline?

According to the instructions, Amitriptyline is prescribed for the treatment of depressive conditions of an involutionary, reactive, endogenous, drug nature, as well as depression on the background of alcohol abuse, organic brain damage, accompanied by sleep disorders, agitation, anxiety.

Indications for the use of the drug are:

• Nervous bulimia.
• Behavioral disorders.
• Emotional mixed disorders.
• Chronic pain (migraine, atypical facial pain, pain in cancer patients, post-traumatic and diabetic neuropathy, rheumatic pain, postherpetic neuralgia).
• Nocturnal enuresis (in addition, which is caused by low bladder tone).
• schizophrenic psychoses.

The drug is also used for peptic ulcers of the gastrointestinal tract, to relieve headaches and prevent migraines.

Instructions for use

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

adults

For adults with depression, the initial dose is 25-50 mg at night, then gradually the dose can be increased, taking into account the effectiveness and tolerability of the drug, up to a maximum of 300 mg per day in 3 doses (the largest part of the dose is taken at night).

When a therapeutic effect is achieved, the dose can be gradually reduced to the minimum effective, depending on the patient's condition. The duration of the course of treatment is determined by the patient's condition, the effectiveness and tolerability of the therapy and can range from several months to 1 year, and if necessary, more.

In old age, with mild disorders, as well as with bulimia nervosa, as part of complex therapy for mixed emotional disorders and behavioral disorders, psychosis, schizophrenia and alcohol withdrawal, they are prescribed at a dose of 25-100 mg per day (at night), after reaching a therapeutic effect, they switch at the minimum effective dose - 10-50 mg per day.

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

Children

Children are prescribed as an antidepressant: from 6 to 12 years - 10-30 mg per day or 1-5 mg / kg per day fractionally, in adolescence - up to 100 mg per day. With nocturnal enuresis in children 6-10 years old - 10-20 mg per day at night, 11-16 years old - up to 50 mg per day.

Contraindications

Side effects

The instruction warns that when taking the drug Amitriptyline, the following side effects are possible:

• rash and other allergic reactions;
• from the side of the central nervous system: dizziness, drowsiness, tremor;
• on the part of the gastrointestinal tract: a violation of taste, dry mouth, constipation, intestinal obstruction, stomatitis, nausea, vomiting, the development of anorexia, in rare cases, violations of the liver;
• increased intraocular pressure, disturbances of accommodation, urinary retention, increased body temperature;
• from the endocrine system: decreased libido and potency, changes in ADH secretion, gynecomastia;
• disorders in the work of the cardiovascular system: tachycardia, increased blood pressure, orthostatic hypotension, etc.

Children, during 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. Penetrates into breast milk and may cause drowsiness in infants.

To avoid the development of the "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 discontinued at least 7 weeks before the expected birth.

In children, adolescents and young patients (under 24 years of age) with depression and other psychiatric disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and may provoke suicidal behavior. Therefore, when prescribing Amitriptyline, it is recommended that the potential benefit of treatment be carefully weighed against the risk of suicide.

special instructions

Long-term use of the drug can lead to weight gain. The drug is prescribed with caution to people with manic-depressive psychosis, as there is a risk of the disease moving into the manic stage.

The use of Amitriptyline with a daily dose above 150 mg leads to a decrease in the seizure threshold. Therefore, patients with a history of seizures, as well as those patients in whom they may occur due to age or injuries, must take into account the risk of seizures.

drug interaction

The hypotensive effect, respiratory depression, depressant effect on the nervous system is observed with the joint appointment of drugs that depress the central nervous system: general anesthetics, benzodiazepines, barbiturates, antidepressants and others.

The drug enhances the severity of the anticholinergic effect when taking amantadine, antihistamines, biperidene, atropine, antiparkinsonian drugs, phenothiazine. The drug enhances the anticoagulant activity of indadione, coumarin derivatives, indirect anticoagulants.

There is a decrease in the effectiveness of alpha-blockers, phenytoin. Fluvoxamine, fluoxetine increase the concentration of the drug in the blood. The risk of developing epileptic seizures increases, as well as the central anticholinergic and sedative effects in combination with benzodiazepines, phenothiazines, anticholinergics.

Simultaneous administration of methyldopa, reserpine, betanidine, guanethidine, clonidine reduces the severity of their hypotensive effect. When taking cocaine, an arrhythmia develops. Delirium develops when taking inhibitors of acetaldehyde, disulfiram.

Amitriptyline enhances the effect on the cardiovascular system of phenylephrine, norepinephrine, epinephrine, isoprenaline. The risk of hyperpyrexia increases when taking antipsychotics, m-anticholinergics.

Amitriptyline's analogs

According to the structure, analogues are determined:

1. Elivel.
2. Apo-amitriptyline.
3. Amitriptyline Lechiva (Nycomed; -AKOS; -Grindeks; -LENS; -Ferein).
4. Vero-Amitriptyline.
5. Amirol.
6. Saroten retard.
7. Amitriptyline hydrochloride.
8. Triptizol.
9. Amizol.

Holiday conditions and price

The average price of Amitriptyline (tablets 10 mg No. 50) in Moscow is 26 rubles. It is released from pharmacies by prescription.

The drug must be stored in a dry place, out of the reach of children, at a temperature of 15-25 ° C. Shelf life 4 years.

Post Views: 451

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

The drug is presented in the form of tablets for oral administration and a solution for intramuscular injection. The active substance is amitriptyline.

Amitriptyline is a tricyclic antidepressant that works by inhibiting the reuptake of dopamine, norepinephrine, and serotonin. Against the background of long-term use of the drug, it restores the balance of systems disturbed by depressive states. The drug has a pronounced sedative effect, as well as antihistamine and antibulimic effects.

The use of the drug Amitriptyline during the treatment of depressive-anxiety disorders helps to reduce agitation, anxiety and depressive manifestations. The use of the drug also contributes to the provision of a moderate analgesic effect due to the effect on the receptors of the central nervous system.

Amitriptyline has antiulcer, sedative and m-anticholinergic effects, which contributes to the provision of analgesic effects and accelerates the healing process of ulcers. Amitriptyline increases the ability of the bladder to stretch, increases the tone of the sphincter. This makes it possible to use drugs during the treatment of bedwetting. Against the background of general anesthesia, amitriptyline can reduce body temperature and blood pressure.

The antidepressant effect of the drug develops within 14-21 days after the start of use.

The excretion of the active component is carried out by the kidneys. The period of complete elimination takes 1-2 weeks. The substance can cross the placenta and be excreted in breast milk.

Indications and contraindications

Indications for the use of Amitriptyline are:

Amitriptyline can also be used to prevent migraine attacks.

Contraindications

Amitriptyline is contraindicated for use in the event of the development of such conditions:

• heart failure (in the stage of decompensation);
• acute heart attack and recovery period after a similar condition;
• with violations of the conduction of the heart muscles;
• individual intolerance to the active substance;
• with a pronounced increase in blood pressure;
• with severe violations of the functioning of the liver and urinary system;
• exacerbations of peptic ulcer of the stomach and duodenum;
• the drug is not used in the treatment of pregnant and lactating women, as well as patients under 6 years of age.

Simultaneous use with MAO inhibitors is strictly contraindicated in patients with atony of the bladder, intestinal obstruction and prostatic hypertrophy.

The drug is used with extreme caution in the treatment of people with a history of alcoholism, bronchial asthma, a tendency to manic-depressive psychosis, epilepsy, hyperthyroidism, angina pectoris, heart failure, angle-closure glaucoma, intraocular hypertension, schizophrenia.

Adverse reactions

Against the background of the use of Amitriptyline, the likelihood of developing disorders of the digestive, endocrine and cardiovascular systems, as well as the central nervous system increases: headache, fatigue, heart rhythm disturbances, nausea, vomiting. It is also possible to develop allergic manifestations, with prolonged treatment, hair may fall out and body weight increases.

If the patient took the drug for a long time and abruptly canceled its use, then a withdrawal syndrome may develop in the form of vomiting, intestinal upset, headache, irritability, and sleep disturbances.

Mode of application

Amitriptyline tablets should be taken orally, during or after a meal. The exact initial and daily dose is determined by the doctor, taking into account the indications for admission, the effectiveness of the drug and its tolerability. It is recommended to use the maximum part of the dose at bedtime.

In severe cases, therapy begins with intramuscular administration of the drug with a gradual transition to taking tablets.

After a stable antidepressant effect is achieved, after 15-30 days the dose is gradually reduced. If the manifestations of a depressive state resume against the background of a decrease in the dosage, one should return to the previous, effective dose.

If the dosage recommended by the doctor is not observed, an overdose may develop, which manifests itself in the form of confusion, dilated pupils, fever and drowsiness, shortness of breath, seizures, vomiting, arrhythmia, pressure reduction, heart failure, respiratory depression.

As a therapy, the drug Amitriptyline is immediately stopped. You should also wash the stomach, pick up funds for symptomatic treatment. In this case, it is necessary to carefully monitor the functioning of the cardiovascular system due to the risk of relapse over the next 2 days after an overdose.

Drug Interactions

Amitriptyline may increase the inhibitory effect on the central nervous system when interacting with such groups of drugs:

When combined with drugs from the group of neuroleptics, it is possible to develop a temperature reaction and paralytic ileus.

When used together with anticonvulsants, as well as guanethidine, their action may be weakened.

With the simultaneous use of Amitriptyline increases the activity of anticoagulants. When combined with cimetidine, the concentration of amitriptyline in the blood plasma may increase, which increases the risk of its toxic effects on the body. The combination with carbamazepine and barbiturates leads to a decrease in the concentration of amitriptyline.

When combined with estrogen-based contraceptive pills, the bioavailability of amitriptyline increases. Amitriptyline may contribute to an increase in depression provoked by glucocorticosteroids.

When combined with drugs from the group of MAO inhibitors, the risk of death increases. The interval between the use of Amitriptyline (as well as other drugs in this group) and drugs from the group of MAO inhibitors should be at least 14 days.

The use of Amitriptyline during the treatment of patients of older age groups should be carried out under the constant supervision of a physician. The drug is recommended to be used in the minimum effective dose.

Against the background of taking Amitriptyline during the treatment of depression, in no case should you drink alcohol.

The use of amitriptyline at certain doses may lower the threshold for seizure activity. It is necessary to be aware of the likelihood of seizures in people with a history of such a condition, as well as in patients predisposed to seizures.

Patients with depressive phases of manic-depressive psychosis are likely to go into the manic stage. Against the background of taking Amitriptyline, you should refuse to drive a car and other modes of transport, as well as perform work that requires increased attention.

Amitriptyline should be stored in compliance with the temperature regime: no more than 25 degrees in a dark place, protected from children and direct sunlight. Amitriptyline is dispensed in pharmacies upon presentation of a prescription from the attending physician.

Analogues, cost

The cost of the drug Amitriptyline is formed depending on the manufacturer:

• tablets 25 mg, 50 pcs. (Ozon, Russia) - 25-35 rubles;
• tab. 10 mg, 50 pcs. (Nycomed, Denmark) - 45-55 rubles;
• tab. 25 mg, 50 pcs. (Grindeks, Latvia) - 55-65 rubles;
• tab. 25 mg, 50 pcs. (Zentiva, Czech Republic) - 65-70 rubles.

Analogues of the drug Amitriptyline are: Amirol, Amizol, Tryptisol, Elivel, Saroten. The selection of a replacement is recommended to be carried out by prior agreement with the doctor.

Latin name

Release form

coated tablets

1 tablet contains amitriptyline hydrochloride (in terms of amitriptyline) 10 mg

Package

pharmachologic effect

Amitriptyline is a tricyclic antidepressant from the group of non-selective inhibitors of neuronal monoamine reuptake. It has a pronounced thymoanaleptic and sedative effect.
The mechanism of the antidepressant action of amitriptyline is associated with 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 CNS and in the periphery, has peripheral antihistamine (H1) and antiadrenergic properties. It also causes an anti-neuralgic (central analgesic), antiulcer and antibulemic effect, and is effective for bedwetting.
Antidepressant action develops within 2-4 weeks. after the start of application.

Indications

Depression of any etiology. It is especially effective in anxiety-depressive states, due to the severity of the sedative effect. It does not exacerbate 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 (with the exception of children with hypotonic bladder).
- Psychogenic anorexia, bulimic neurosis.

Contraindications

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

Dosage and administration

Assign inside (during or after a meal). 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. 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 (maximum dose for outpatients 150 mg / day). 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 obtaining a stable antidepressant effect after 2-4 weeks, the doses are gradually and slowly reduced to 50-100 mg / day and continue therapy for at least 3 months. In the event of signs of depression with a decrease in doses, it is necessary to return to the previous dose.

Elderly patients with mild disorders

In outpatient practice, doses are 25-50-100 mg per day in divided doses or once a day at night.

For nocturnal enuresis

in children aged 6-10 years

10-20 mg/day at night

aged 11-16 years

25-50 mg / day. (the dose should not exceed 2.5 mg/kg of the child's weight).

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

In severe depression resistant to therapy: intramuscularly or intravenously (inject slowly!) administered 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 inside.

Children over 12 and the elderly

Enter lower doses and increase them more slowly.
If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is inappropriate.

Side effects

Mainly associated with anticholinergic action of the drug: paresis of accommodation. Blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, urinary retention, fever. All these phenomena usually disappear after adaptation to the drug or dose reduction.
From the side of the central nervous system: headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremor, paresthesia, peripheral neuropathy, EEG changes. Rare extrapyramidal disorders, convulsions, anxiety.
From the side of the cardiovascular system: tachycardia, arrhythmia, conduction disturbance, blood pressure lability, expansion of the QRS complex on the ECG (impaired intraventricular conduction), symptoms of heart failure, fainting.
From the digestive tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disturbances, darkening of the tongue, epigastric discomfort, gastralgia, increased activity of "liver" transaminases, rarely cholestatic jaundice, diarrhea.
From the 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, swollen lymph nodes, weight gain with prolonged use, sweating, pollakiuria. With prolonged treatment, especially at high doses, with a sharp cessation of treatment, withdrawal syndrome may develop: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with vivid, unusual dreams, and irritability.

special instructions

Amitriptyline at doses above 150 mg / day reduces the threshold for seizure activity, so the possibility of seizures should be considered in patients with a history of seizures, and in those patients who are predisposed to this due to age or injury. Treatment with amitriptyline in the elderly should be carefully monitored and, with the use of 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 MDP may go into the 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.

drug interaction

Amitriptyline enhances the inhibitory effect on the central nervous system of the following drugs: neuroleptics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; shows synergism when interacting with other antidepressants. With the combined use of amitriptyline with neuroleptics, and / or anticholinergic drugs, a febrile temperature reaction, paralytic ileus may occur. Amitriptyline potentiates the hypertensive effects of catecholamines and other adrenostimulants, which increases the risk of developing cardiac arrhythmias, tachycardia, severe arterial hypertension, but inhibits the effects of drugs that affect the release of norepinephrine. Amitriptyline may 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 the plasma concentration of amitriptyline is possible with the possible development of toxic effects. Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduces 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. Co-administration of amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors may cause delirium. Estrogen-containing oral contraceptives may increase the bioavailability of amitriptyline; pimozide and probucol may exacerbate cardiac arrhythmias. Amitriptyline may increase depression caused by glucocorticosteroids; combined use with drugs for the treatment of thyrotoxicosis increases the risk of developing agranulocytosis. 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!

Amitriptyline is a synthetic drug that is used in medicine to treat various forms of neurosis. Assign for mild, moderate, severe depression, diagnosing nervous, phobic disorders. The drug belongs to the category of tricyclic antidepressants.

Description of the drug

Amitriptyline is a highly effective agent with a pronounced sedative, antiserotinous effect, thymoanaleptic, anxiolytic properties. Belongs to the group of non-selective inhibitors of neuronal uptake of monoamines. The antidepressant is produced by many pharmaceutical companies. Also known under the following trade names: Amirol, Triptizol, Elivel, Amizol.

Amitriptyline is available in pharmacies only by prescription.

Amitriptyline is available in the form of tablets or dragees for oral administration (by mouth), as well as in the form of a white crystalline powder or sterile injection (for intramuscular injection).

The main active substance, regardless of the form of release of the antidepressant, is amitriptyline hydrochloride. The tablets contain 10 and 25 mg of the active ingredient (in one pill) and 20 mg of amitriptyline in each 2 ml ampoule of the injection solution.

The composition includes excipients that differ from manufacturer to manufacturer, namely: glucose, water in injections, and in pills - starch, MCC, lactose monohydrate, talc, starch, polyvinylpyrrolidone, magnesium stearate.

Store the medicine in a dry, cool place protected from direct sunlight at a temperature of 6 to 24 degrees Celsius. The expiration date from the date of issue is three years.

Pharmacodynamics and mechanism of action

Amitriptyline, instructions for use indicates that this drug has a pronounced peripheral and central anticholinergic effect, due to its high affinity for m-cholinergic receptors.

The antidepressant effect of this drug is due to the suppression of neuronal reuptake of serotonin, norepinephrine, dopamine by the membranes of presynaptic neurons. An increase in the number of neurotransmitters improves the psychological, emotional state.

Amitriptyline reduces the severity of depressive manifestations, agitation, eliminates the feeling of anxiety in mild to moderate anxiety-depressive conditions.

The antidepressant has a sedative, alpha-adrenergic blocking effect. It has the properties of class-A antiarrhythmic drugs. In the recommended therapeutic dosages, it inhibits and slows down ventricular conduction, but in case of an overdose, the drug can cause severe intraventricular blockade.

Important! It should be noted that the intake of pharmacological drugs of this group has the so-called "antidepressive threshold", which is manifested by the individual perception of the body. Therefore, the doctor selects a dosage that will reduce the capture of neurotransmitters by 5-10 times, individually for each patient.

Otherwise, the antidepressant effect will not be achieved and side effects may occur.

Tricyclic antidepressant has a sedative, thymoleptic effect. It also has a sedative, antibulimic, antihistamine, anticholinergic effect. With prolonged use of the drug, the balance of systems disturbed due to depressive states is restored.

The drug Amitriptyline has an additional analgesic effect of central origin. Due to the blocking of H2-histamine receptors in the parietal cells (ventricular walls), an antiulcer effect is provided. In addition, the drug lowers body temperature, blood pressure during general anesthesia.

The maximum concentration of the drug in the bloodstream occurs after 3-12 hours. It is metabolized in the liver, where it forms active and inactive metabolites. It is excreted from the body with urine. complete elimination takes one to two weeks.

The antidepressant effect is noted approximately three to four weeks after the start of the drug.

Indications for use

Antidepressant, the frequency of administration, the duration of the course is prescribed by the attending physician on an individual basis.

Indications:

• depressive-anxious states of various etiologies (endogenous, reactive);
• depression of moderate, mild, severe form;
• emotional disorders accompanied by behavioral disorders;
• sleep disorders (insomnia);
• schizophrenic psychoses;
• chronic neurogenic pain:
• phobias, panic attacks;
• bulimic neurosis, psychogenic anorexia.

The antidepressant Amitriptyline is also used in pediatrics in the treatment of nocturnal enuresis in children, which are also caused by weakness of the bladder sphincter.

An antidepressant relieves headaches caused by migraines. The drug is prescribed in the treatment of gastrointestinal ulcers, in the treatment of alcohol, drug addiction.

Instructions for use

According to the instructions, amitriptyline tablets should be taken after meals or during meals. Dragee without chewing, you need to drink plenty of water.

The initial daily dose of the drug is 50-75 mg, divided into two or three doses. Gradually increase the dosage to 150-200 mg per day to achieve the best effect. Sometimes the intake is adjusted to bring the intake to 300 mg or more (up to the maximum tolerated dose). In this case, the daily dose is divided into three doses, with the use of most of the drug at bedtime.

Important! You need to increase the dosage of any antidepressants gradually.

After 15-30 days after reaching the desired pronounced therapeutic therapeutic effect, the dosage is gradually reduced. After improvement of the condition, the minimum daily dose may be 25-50 mg.
But a sharp decrease is unacceptable, since a withdrawal syndrome may develop.

In the treatment of childhood enuresis, amitriptyline is prescribed 10-25 mg at bedtime. The dose is calculated individually based on the recommendation of taking 2.5 mg per kg of the child's weight. In childhood depression, 1.5 mg per kg of body weight is prescribed.

Contraindications for use

Amitriptyline has many contraindications, so carefully read the annotation to the medication before use.

Contraindications:

• myocardial infarction;
• chronic heart failure;
• violation of the conduction of the heart muscle;
• chronic liver pathology, renal failure;
• exacerbation of peptic ulcer;
• blood diseases;
• prostate hypertrophy;
• pregnancy, lactation;
• disorders in the functioning of the urinary system.

Amitriptyline is strictly prohibited for use in children under six years of age. With caution, an antidepressant is used for secondary glaucoma, bronchial asthma, epilepsy, intraocular hypertension, manic-depressive psychosis, oppression of bone marrow hematopoiesis, urinary retention, thyrotoxicosis.

Do not prescribe the drug to patients who have individual intolerance to the constituent components of the drug.

Side effects

If there are no contraindications to taking amitriptyline, hypersensitivity of the body, if the dosage is observed, side effects rarely occur. Excessive abuse, non-compliance with the dose can provoke poisoning, intoxication, a number of side effects.

In case of overdose note:

• dizziness;
• nausea, diarrhea, vomiting, heartburn;
• instability of blood pressure;
• allergic manifestations, itching, skin rash;
• decreased libido;
• epileptic seizures, convulsions, spasms;
• violation of coordination of movements, disorientation in space;
• tinnitus, severe headaches;
• angioedema;
• decreased visual function;
• gastralgia;
• constipation, intestinal obstruction;
• difficulty urinating;
• dry mouth;
• darkening of the tongue;
• increased excitability, irritability;
• anemic mucous;
• change in the circulatory formula;
• increased intraocular pressure;
• enlarged lymph nodes;
• change in taste sensations.

Patients may experience nightmares, hallucinations, sleep disturbance. The heartbeat becomes more frequent (tachycardia, arrhythmia), sweating increases, the general temperature rises. A coma may occur.

In case of overdose symptoms, consult a doctor immediately. Emergency medical attention is required to avoid severe complications. In case of individual intolerance, the course of treatment with amitriptyline is stopped. Patients are prescribed another antidepressant.

Before carrying out therapy, it is imperative to control the level of blood pressure. Parenteral Amitriptyline is used only under medical supervision in a hospital setting. In the first days of treatment, patients are advised to stay in bed.

Compatibility with other drugs

The antidepressant Amitriptyline enhances the inhibitory effect on the central nervous system when interacting with hypnotics, sedatives, anticonvulsants, analgesics, and premedication agents.

The drug is not combined with alcohol, drugs, increasing their toxic effects on the body. For the duration of the entire period of treatment, the use of any alcoholic beverages is strictly prohibited, since it can lead to very serious consequences, functional failures and disorders in the body. If you take alcohol and the drug at the same time, the heart rhythm is disturbed, pressure rises, and paralytic ileus occurs.

With the simultaneous use of amitriptyline with neuroleptics, it is possible to increase the overall temperature, the development of paralytic intestinal obstruction.

In combination with anticonvulsant drugs, guanethidine, their therapeutic effect may be weakened. With the simultaneous use of Amitriptyline increases the activity of anticoagulants. In combination with cimetidine, the concentration of amitriptyline in the bloodstream increases, which increases its toxic effect on the body as a whole.

The combination of amitriptyline with carbamazepine, barbiturates reduces the concentration of the antidepressant. When used with oral contraceptives based on estrogen, the bioavailability of the tranquilizer increases.

Amitriptyline can also increase depression caused by glucocorticosteroids.