Amitriptyline - instructions for use, what helps, spectrum of application, rules for taking an antidepressant, analogues. Amitriptyline: review and experience of use How long can you take amitriptyline without a break

A classic and highly effective tricyclic antidepressant is Amitriptyline Nycomed. Reviews about him are usually positive. This medicine has a wide range of applications.

pharmachologic effect

The drug "Amitriptyline" is an antidepressant from a number of tricyclic compounds. It is a derivative of dibenzocycloheptadine. The action of amitriptyline is associated with the stimulation of serotonergic and adrenergic mechanisms of the brain by suppressing the reuptake of mediators. It gives a sedative effect, exhibits antihistamine and anticholinergic activity. The antidiuretic benefit in nighttime incontinence is achieved through anticholinergic activity. The drug has an analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system and the effect of tricyclic compounds on opioid endogenous systems.

Pharmacokinetics

It is believed that the drug "Amitriptyline" has good bioavailability. Reviews usually confirm this. The bioavailability of the drug is 31-61%. It binds to blood proteins by 82-96%. Metabolization is carried out with the formation of the metabolite nortriptyline (active). The half-life is 31-46 hours. The drug is excreted mainly through the kidneys.

Indications

The drug is used during the depressive phase of manic-depressive psychoses, various depressions (including children's), with mixed emotional disorders, with pathological behavioral disorders. In children's enuresis (with the exception of patients with hypotonic bladder pathology), the medicine "Amitriptyline" has proven itself quite well. Reviews about its action are good. The drug is also prescribed for bulimia nervosa and chronic pain syndromes. Also, this remedy is prescribed for the treatment of bulimic neurosis, psychogenic anorexia, with chronic neurogenic pain, in order to prevent migraine.

Dosing

Amitriptyline tablets are taken orally (without chewing) after meals. For adults, the initial dose is 25 mg 2 to 4 times a day. The maximum dosage for outpatient treatment is 150 mg per day, for inpatient treatment - 300 mg per day, and for the elderly 100 mg. The medication can be administered intravenously or intramuscularly at a dose of 20-40 mg four times a day. Over time, injections can be replaced by oral administration. Course - no more than 6 months. For children, the drug is prescribed as an antidepressant in dosages of 10-30 mg, for adolescents - 10 mg three times a day, for the treatment of enuresis in children over six years of age - 12-25 mg at night. The dosage should not exceed the proportion of 2.5 mg per 1 kg of body weight.

Side effects

As a rule, the medicine "Amitriptyline" is well tolerated. Feedback on the use is positive. However, various side effects are possible. CNS: disorientation, hallucinations, drowsiness, extrapyramidal disorders, fatigue, anxiety, trembling. Cardiovascular system: tachycardia, orthostatic hypotension, conduction disturbance. Gastrointestinal: cholestatic jaundice, vomiting, stomatitis. Reproductive system: delayed ejaculation, various disorders, changes in libido, decreased potency. Endocrine system: diabetes mellitus, glucosuria, hyperglycemia, decreased glucose tolerance, inadequate ADH secretion. Metabolism: weight gain. Allergic reactions: skin rashes, itching. Effects caused by anticholinergic activity: disturbances of accommodation, dry mouth, urinary retention, increased intraocular pressure, blurred vision, constipation. Side effects occur infrequently when taking the medication "Amitriptyline". Reviews about it are generally positive.

Contraindications

The drug should not be prescribed against the background of the following diseases: with angle-closure glaucoma, atony of the bladder, prostate hypertrophy, paralytic ileus, pyloric stenosis, epilepsy, early recovery period after a heart attack. The drug also can not be used simultaneously with MAO inhibitors. It is also contraindicated to use the drug for decompensated heart defects, blood diseases, glaucoma, severe liver and kidney diseases, stomach ulcers and hypersensitivity to the active substance and other components of the drug.

Pregnancy and lactation

The drug "Amitriptyline" should not be used during pregnancy, and especially in the 1-3 trimesters. The use of the drug is allowed only when absolutely necessary. The fact is that adequate clinical studies of the effect of the drug on the fetus and the mother's body have not been conducted. Therefore, it is not known how safe it is. In experimental studies, the drug gave a teratogenic effect in dosages much higher than normal.

special instructions

With great care, this drug is used for heart failure, arrhythmias, coronary artery disease. Abrupt discontinuation of medication can lead to the development of a withdrawal syndrome. This tool can be used no earlier than two weeks after taking MAO inhibitors. You can not use the drug simultaneously with sympathomimetic medications: with epinephrine, isoprenaline, ephedrine, phenylephrine, norepinephrine, phenylpropanolamine. With great care, this medicine is prescribed together with drugs that have an anticholinergic effect. Do not drink alcohol while taking the medication. Means "Amitriptyline" affects the ability to control mechanisms. During therapy, it is necessary to refrain from activities associated with a potential danger, requiring a good reaction rate and increased attention. This drug was included in the list of essential drugs. With an overdose of Amitriptyline, the following symptoms are observed: disorientation, drowsiness and confusion, fever, dysarthria, shortness of breath, dilated pupils, hallucinations, stupor, convulsions, arrhythmia, muscle rigidity, hypotension, respiratory depression, heart failure.

drug interaction

As a rule, with the simultaneous use of Amitriptyline with other drugs that have a depressant effect on the central nervous system, as well as with alcohol, an excessive increase in depression of the central nervous system is possible. The effect of alcohol is enhanced. In addition, hypotensive effects and respiratory depression may be observed. If you take the medicine together with other drugs that are characterized by anticholinergic activity, it is possible to increase the anticholinergic effect. Taking the drug "Amitriptyline" with symptomatic medications enhances their effect on the heart and the cardiovascular system as a whole. Because of this, the risk of developing various rhythm disturbances, arterial hypertension (severe forms), and tachycardia increases. Reception with guanethidine and clonidine reduces the hypotensive effect of these drugs. Use together with barbiturates: with quinidine - slowing down the metabolism of the drug "Amitriptyline", with carbozepine - a significant decrease in the effect of the drug due to a strong acceleration of its metabolism. Simultaneous use together with cimetidine also slows down the metabolism of Amitriptyline, and also increases its plasma concentration and increases the risk of toxic effects.

It is time to make a separate article about this drug. Moreover, I have something to say about him.

It is by far my favorite antidepressant. I endure it better than the others, my efficiency does not fall, there is no fog in my head. One minus is that at therapeutic doses (medium and high) it gives off weight. But let's talk about everything in more detail.

I first heard about amitriptyline from my not quite normal boyfriend, from whom a relative took it. He, in his usual manner to generalize everything, put him on a par with haloperidol, and this is a serious neuroleptic for completely psychos (schizophrenics, for example). So for me, amitriptyline has become associated with complete abnormality. Yes, and at the first appointment with the doctor, she told me something like “well, I can, of course, prescribe you cheap amitriptyline, then you won’t be able to walk later.” Yeah. I was doing great on amitriptyline. This is not as terrible a drug as they are trying to show us. By the way, I switched to him from the “ideal” cipralex, which could not completely remove my panic attacks.

What helps amitriptyline?

From depression, panic attacks, anxiety and so on. It belongs to a large group of tricyclic antidepressants that are quite potent, but only if the dosage is adequate. He is very fond of giving in hospitals, as he almost immediately gives an effect due to the fact that the anti-anxiety and hypnotic effects appear after the first dose. Antidepressant, on the other hand, develops gradually and can be counted on only after three weeks.

Amitriptyline is also often used for chronic pain. They even treat ulcers! True, treatment can be started only when the acute period has passed. I can also say with confidence that the drug is excellent at fighting pain in the intestines, especially if they are caused by such a nasty diagnosis as irritable bowel syndrome. Amitriptyline also helps with (it really helps, it's checked!). With all these sores, doses are usually taken smaller than for depression.

Manufacturer

Personally, I (and everyone else too) met with three different amitriptylines - Denmark (Amitriptyline Nycomed), Slovenia and Russia. Someone says that they don't feel the difference, someone claims that only Slovenian is good. From personal experience I can say that I like Amitriptyline Nycomed the most - now I drink just that. He acts more delicately, from him I did not notice the effect of the type of "fried with a dusty bag on the head." Of course, it is more expensive than domestic, but, people, it still costs 55 rubles for 50 tablets of 25 mg! It's practically free! By the way, some begin to doubt the drug with such a cost, but I tell you with all responsibility - do not hesitate! It works and how.

Dosage

Amitriptyline is available in two dosages - 10 and 25 mg. The minimum therapeutic dose is 75 mg per day. The antidepressant effect of the drug is revealed at a dosage of at least 150 mg per day - these are 6 tablets of 25 mg. They can be distributed like this - 2-2-2 (morning-afternoon-evening), 3-3 (morning-evening), 1-1-4 (morning-afternoon-night). The instruction allows you to drink most of the dose at night, since the drug has quite severe side effects (especially at the beginning of the intake), but then he drank and lay down, fell asleep, did not feel anything.

I must say right away that doctors outside hospitals avoid prescribing normal doses of amitriptyline. I don't know why - they are afraid, perhaps, that the patient will not reach them later, will fall down somewhere along the road? The last time, when I said that I usually drink three tablets a day (that is, those same 75 mg), they asked me - “isn't it a lot?”. This speaks well of the professionalism of doctors in psychiatric clinics, since lower dosages simply will not have the desired effect. Or do they just hope that with a small dosage the patient will receive an anti-anxiety effect, and more is not needed?

In small doses, according to both patients and researchers, only sedative and hypnotic effects predominate. I use it regularly and it usually takes me two weeks on 50mg to bounce back. But if you need a serious effect, then you can’t do without serious doses.

You should start taking the minimum dosage, because if you immediately drink a 25 mg tablet, you will be knocked out so that you will not want to continue later. Half, and that one - for the night. Add half every 3-4 days until you reach 75 mg per day. Sit on such a dose, let the body get used to it. Then you can add one tablet a week to the desired dosage - let me remind you, it should be no less than 100-150 mg. Once you reach the desired dose, you can count 3 weeks. There is no desired effect - raise more. At home, I do not recommend drinking more than 150 mg, so if you decide to do this, then either consult your doctor or go to the hospital.

Why do I paint the initial and further dosages in this way? Because although amitriptyline is a well-studied drug, many doctors make quite gross mistakes. Either large doses are immediately prescribed, or initially they do not want to go even to the minimum therapeutic dose. But, in any case, I always recommend that you coordinate all changes in dosages with your doctor, and if you do something on your own, then only at your own peril and risk.

And remember that we will take beta-blockers (such as, for example,) significantly increase the concentration of amitriptyline in the blood, so the dosage should be minimal (best of all, two times lower than required).

Duration of admission

You need to drink amitriptyline in the right dosage for six months (counting from the complete disappearance of symptoms). Then you can reduce the dosage - very, very gradually, half a week, otherwise it will cover the withdrawal syndrome. He is not as strong with him as with the same paxil, but for some he can deliver inexpressible sensations. I always lowered smoothly, so I didn’t feel anything like that.

When you reduce to 2-3 tablets per day, sit on this dose longer, do not reduce to the end. This is a maintenance dose, it can be taken for a year or several years. If you do not pass, then you may have to drink this dose for the rest of your life. My depression usually returns in about a month if I took the pills for a long time, and after two weeks if the course was short. Therefore, it is best not to decrease to zero, to leave the minimum dose. I now have one tablet a day, so far enough.

Side effects

Ooooh, this is just a huge field for writing the Talmuds. You will have side effects from any antidepressant, but some call amitriptyline just a brutal drug in this regard. Well, it's really not that scary. So what can you have?

Dry mouth. This is the first thing even a doctor will tell you. Some say that even speaking is difficult, the tongue does not turn in the mouth. I didn't even have it on high doses. I don't know what's wrong with me.

Tachycardia. The resting pulse can be up to 120 beats per minute. In my first course, I was afraid of this side effect, but gradually everything calmed down. The maximum can be 90-100 strokes. By the way, in general, amitriptyline is considered cardiotoxic, that is, it can start to act up the heart. But this applies only to high doses and a long time of admission. But, in any case, once every six months it is better to do an ECG.

pupil dilation. Everyone close to you may take you for a drug addict (wear dark glasses, ha ha!). But gradually it will pass. Personally, I didn't have that.

Constipation. This can be a real problem if you do not immediately grab this side by the tail. If you have a penchant for this business, then it is best to start eating more fiber. And if this does not help, then there is an excellent drug duphalac, which can be drunk for a long time.

Weakness, lethargy. Probably will be at the beginning of the reception. We take the main dose at night and wait for the body to adapt. Gradually everything will pass.

Decline in cognitive abilities. The kettle stops cooking. The same happens at the beginning of treatment. Personally, he always cooks for me, but not everyone is like me. This must be endured. Naturally, you should not start taking amitriptyline before important exams or projects, otherwise you will fill up everything.

Weight gain. This is the main side effect of amitriptyline for me! I usually gain from 10 to 25 kg per course, and this is a lot! My doctor tried to put me on a diet that banned almost everything. It didn’t work, there were breakdowns, and because of them, I scored even more than I could. So now I just “surrender to the waves” and eat. But at the same time I try to walk and play sports to minimize the harm.

Amitriptyline and anesthesia

The instructions for the drug say that if you are taking it, then you need to inform the doctor who is going to give you anesthesia - both local and general (for example, it can be a dentist). But in practice, you will get a puzzled face and complete ignorance of what amitriptyline is and how dangerous it can be during anesthesia. I was very interested in this issue and this is what I found out. If you are taking medium or high doses of amitriptyline, it is best to avoid anesthesia altogether at this point. If without it in any way, then this should be the minimum possible dose of anesthetic for a short time. It is best to do everything in the clinic, where there is everything you need in case you pass out. And in general it is better if the clinic is not too far from the hospital. Scary? That's me too. So it is best not to mix amitriptyline with anesthesia. Well, at low doses you can, of course, but also with caution.

9022 0

Amitriptylme
Antidepressants (tricyclic compounds)

Release form

Mechanism of action

Amitriptyline has sedative properties.

Main Effects

Pharmacokinetics

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

Indications

Dosage and administration

For the prevention of migraine, with chronic pain of a neurogenic nature (including with prolonged headaches) - from 12.5-25 to 100 mg per day (the maximum part of the dose is taken at night).

Contraindications

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

Precautions, therapy control

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

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

Parenteral use should be carried out only in a hospital, under the supervision of a physician, with bed rest in the first days of therapy. Care should be taken when abruptly moving to an upright position from a lying or sitting position.

During the treatment period, the use of ethanol is unacceptable.

Assign amitriptyline not earlier than 14 days after the abolition of monoamine oxidase inhibitors. It should be borne in mind that the therapeutic activity and severity of adverse reactions of amitriptyline are influenced by drugs of many pharmacological groups (see "Interaction").

With a sudden discontinuation after prolonged treatment, the development of a "cancellation" syndrome is possible.

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

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

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

Anticholinergic action leads to a decrease in the secretion of saliva, dryness in the oral cavity. With prolonged use, there is an increase in the incidence of dental caries. There is a decrease in lacrimation and a relative increase in the amount of mucus in the composition of the lacrimal fluid, which can lead to damage to the corneal epithelium in patients using contact lenses.

The need for riboflavin may increase.

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

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

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

Side effects

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

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

■ tachycardia;
■ heartbeat;
■ dizziness;
■ orthostatic hypotension;
■ nonspecific changes in the electrocardiogram (S-T interval or T wave) in patients who do not have heart disease; arrhythmia; lability of blood pressure; violation of intra-ventricular conduction (expansion of the QRS complex, changes in the P-Q interval, blockade of the legs of the bundle of His).

From the digestive system:
■ nausea.

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

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

From the reproductive system:
■ increase in size (edema) of the testicles;
■ gynecomastia;
■ an increase in the size of the mammary glands;
■ disturbance or delay in ejaculation;
■ decrease or increase in libido;
■ reduced potency.

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

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

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

Local reactions (with a / in the introduction):
■ thrombophlebitis;
■ lymphangitis;
■ burning sensation;
■ skin reactions.

Overdose

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

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

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

Treatment: gastric lavage, administration of activated charcoal, laxatives (oral overdose); symptomatic and supportive therapy; with severe symptoms due to blockade of cholinergic receptors, the introduction of cholinesterase inhibitors (the use of physostigmine is not recommended due to an increased risk of seizures); maintenance of body temperature, blood pressure and water and electrolyte balance.

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

Interaction

Synonyms

G.M. Barer, E.V. Zoryan

With a calming effect. Synthesized in the 1960s, it has become the gold standard in the treatment of depression.

Reviews of patients who have taken Amitriptyline throughout its existence have singled out the drug as a reliable and one of the most inexpensive remedies for anxiety disorders, agitated conditions, sleep disorders, and various types of depression.

The classic tricyclic antidepressant has a wide range of indications, primarily affecting depressive states of various nature: endogenous, neurological, involutional, reactive, drug-induced. The drug is effective for organic changes in brain tissue, alcohol withdrawal syndrome.

Other indications for the appointment of Amitriptyline:

Amitriptyline is prescribed for the prevention of migraine attacks, as well as for chronic pain that is difficult to stop:

• rheumatic;
• diabetic;
• oncological;
• postherpetic;
• post-traumatic.

The drug is included in the complex therapy of stomach and intestinal ulcers, used for cyclic vomiting syndrome, chronic fatigue syndrome and irritable bowel syndrome, as well as a number of painful pathologies of the urogenital area in men and women.

Compound

The main active ingredient of the drug - amitriptyline hydrochloride - white powder is odorless, soluble in water, ethanol, chloroform. Refers to psychopharmacological substances from the group of classic tricyclic antidepressants. Amitriptyline in the human body reveals sedative, thymoleptic, analgesic effects.

The substance has a powerful anticholinergic effect, due to the ability to block cholinergic receptors. The sedative effect is due to affinity for H1-histamine receptors. At the same time, amitriptyline exhibits the properties of an alpha-adenoblocker.

Additional components of the drug in tablets: cellulose (microcrystalline), talc, lactose, magnesium stearate, starch (gelatinized), silicon dioxide, quinoline dye (yellow). Auxiliary ingredients provide the shape and consistency of the tablet form of the drug and stabilize the main substance.

1 ml of Amitriptyline injection solution contains 10 mg of the active substance. Auxiliary ingredients of the liquid form of the drug: water, caustic soda, sodium chloride, benzethonium chloride.

In what form is it issued

Amitriptyline is available in tablets, dragees, and IM solution.

Amitriptyline tablets are round, biconvex, film-coated, yellow in color.

Pharmadynamics

The antidepressant effect of Amitriptyline is provided by the normalization of the amount of serotonin and the retention of norepinephrine by blocking their reabsorption. Long-term use of the drug leads to a decrease in the activity of serotonin, beta-adrenergic receptors, ensures the normal transmission of nerve impulses, and restores balance in the nervous system.

Amitriptyline reviews of patients taking the drug are characterized as a quick way to reduce agitation, lethargy, stop panic attacks, normalize mood and sleep. The antidepressant effect is noted within 3 weeks after the start of administration.

The blocking effect of a tricyclic antidepressant on histamine receptors provides a sedative and hypnotic effect to the drug. This property in the early stages of treatment is considered a positive quality, and in long-term therapy is referred to as undesirable side effects.

The antiulcer effect of Amitriptyline is due to the sedative and anticholinergic effect on the gastrointestinal tract receptors.

Efficiency in enuresis is provided by an increase in the muscle tone of the sphincter and relaxation of the bladder (which increases its ability to stretch), as well as the muscles of the prostate gland. The analgesic effect is associated with an effect on opiate receptors and the concentration of monoamine neurotransmitters (especially serotonin) in the central nervous system.

The mechanism of action in eating disorders of a nervous nature is not fully understood, but is similar to the action in depression. The effect of Amitriptyline in bulimia in patients with depression and in its absence is noted. Moreover, the correction of eating behavior and neurological symptoms can occur independently of each other.

Pharmacokinetics

Amitriptyline is highly absorbed, its bioavailability reaches 60%, and some active metabolites - 70%. The peak concentration of the active substance in the blood is reached 2-7 hours after a single dose. With intramuscular injection, the maximum concentration in the blood is higher and is reached faster.

Amitriptyline crosses the blood-brain, histohematogenous and placental barriers, is found in breast milk at concentrations close to plasma. Metabolism of the drug takes place in the liver cells with a significant "first pass effect" and the formation of active and inactive metabolites.

The elimination half-life of Amitriptyline can take 28 hours, but on average does not exceed 10 hours. Nortriptyline, as the most important metabolite, is found in the blood for up to 7 days. Complete elimination takes 14 days.

Application

Amitriptyline reviews of patients taking the drug are recommended to be taken strictly in accordance with the instructions: without chewing, during or immediately after a meal, drinking tablets with plenty of liquid.

So you can significantly reduce the risk of irritation of the gastric mucosa. Different conditions require treatment for different durations. Courses shorter than 30 days are ineffective, most often antidepressant therapy lasts from several months to several years.

Blood pressure is monitored before starting therapy. During treatment, the blood picture is monitored. Mandatory laboratory monitoring of the condition for any increase in temperature, sore throat, flu-like condition. Long courses of therapy are carried out with regular monitoring of the functions of the cardiovascular system (hereinafter referred to as CCC) and the liver.

It is considered inappropriate to use the drug for more than 30 days, without a visible improvement in the condition.

For children under 18

The drug is approved for the treatment of children with some restrictions:

• contraindicated in patients under 6 years of age;
• from enuresis for children from 6 to 10 years old, no more than 20 mg of the drug at bedtime is prescribed daily;
• from 10 to 16 years, the amount is calculated from the ratio of 5 mg of the substance per 1 kg of weight, but not exceeding 50 mg per day;
• for disorders of attention, behavior, hyperactivity, anxiety, depression, phobias in children under 12 years old, from 10 to 30 mg / day is prescribed. or calculate the daily dose depending on the weight (1-5 mg/kg). Take fractionally up to 3 times a day;
• for adolescents, the dose of Amitriptyline is allowed to be increased to 100 mg / day.

A feature of the action of an antidepressant on children with mental illness and depression is an increase in suicidal tendencies. The appointment is carried out taking into account the risk of suicide, commensurate with the possible harm and benefit of therapy.

For adults

The first dose of Amitriptyline for depression is produced in a small dose. In accordance with age, weight and severity of the condition, 25 or 50 mg of the drug is prescribed once a night.

In the next 6 days, gradually raise the dose to the prescribed one (from 150 to 200 mg), dividing it into three doses. If there is no significant positive dynamics in 15 days, the daily rate is raised to 300 mg. Therapy is carried out without changes until the symptoms disappear, and then the dosage is reduced.

Features of the use of Amitriptyline:

With persistent, chronic pain of any origin, in order to prevent migraine attacks, in the treatment of gastric and duodenal ulcers, half the dosage is prescribed from 10 to 25 mg, not more than 100 mg per day, with most of the dose consumed before bedtime.

Acute conditions with alcohol withdrawal, psychosis with schizophrenia are stopped with a daily dose of 100 mg taken at night. The duration of further therapy is determined by the attending physician.

For pregnant

Since the active substance easily penetrates into all body fluids, the use of Amitriptyline during pregnancy is undesirable. The remedy is prescribed in extreme cases, if the potential benefit far outweighs the possible harm to the fetus.

Amitriptyline, according to reviews of patients who took the drug during breastfeeding, causes intestinal colic, shortness of breath, excessive drowsiness, tremors and spasms in infants. That's why during lactation and feeding, tricyclic antidepressants are prohibited.

With an urgent need to take the drug during pregnancy, it is gradually excluded 6-7 weeks before the expected date of birth. Otherwise, newborns may experience a “withdrawal syndrome”.

For the elderly

Amitriptyline is used with caution in older patients. Elderly patients are more likely to detect adverse reactions to therapy in the form of drug-induced psychosis, nighttime anxiety. When the drug is discontinued, side effects disappear on their own in a few days.

For mild behavioral disorders, attention disorders, depression in the elderly, Amitriptyline is prescribed depending on the severity of the deviation, age and concomitant diseases. Tablets are taken daily at night in a dosage of 25 to 100 mg. After achieving the effect, the daily rate is reduced to 10-50 mg.

With concomitant diseases of the cardiovascular system during the entire period of therapy, it is necessary to control blood pressure, pulse, and regularly conduct an ECG.

Contraindications

The drug has a powerful effect, therefore, it has strict contraindications for admission and a number of relative restrictions.

Amitriptyline therapy is absolutely contraindicated in such conditions:

Since lactose monohydrate is present in the tablets, the drug is prohibited for use with galactose intolerance, malabsorption of carbohydrates in the intestine (malabsorption), and lactase deficiency.

With caution and under constant medical supervision, Amitriptyline is used for such disorders:

• any diseases of the cardiovascular system;
• insufficiency of hematopoiesis;
• renal/liver failure;
• increased intraocular pressure;
• violation of intestinal motility and patency;
• decreased bladder tone and urinary retention;
• prostate adenoma (BPH);
• bronchial asthma;
• thyrotoxicosis;
• stroke.

Amitriptyline reviews of patients taking the drug are described as a drug that requires special monitoring in the treatment of schizophrenia and bipolar disorder due to the possible spontaneous activation of psychosis. With epilepsy, convulsive syndrome is aggravated.

Overdose

Symptoms of exceeding individually effective doses of Amitriptyline from various organs and systems:

1. CNS: hallucinations, stupor, anxiety, disorientation, muscle rigidity, pathological involuntary movements, epileptic syndrome.
2. CCC: hypotension, cardiac arrhythmias, A-B blockade, acute heart failure, shock, cardiac arrest.
3. Others: gagging, cyanosis of the skin, shortness of breath, hyperthermia, dilated pupils, sweating, decreased urine output, anuria.

Symptoms begin within 4 hours of taking a high dose of an antidepressant, peak within 24 hours, and may last up to 6 days. At the first signs of an overdose, urgent hospitalization is indicated.

Treatment consists in washing the stomach, taking sorbents, and eliminating symptoms. Relief of severe conditions produced in the intensive care unit. Hemodialysis and diuresis are ineffective. The patient's condition is monitored for at least 5 days. Relapses are possible after 48 hours, sometimes later.

Side effects

Amitriptyline reviews of patients taking the drug are described as a powerful antidepressant with a lot of undesirable side effects. The main unpleasant consequence of taking an antidepressant is called severe dry mouth., which is especially undesirable for elderly patients with urinary and kidney problems.

Patients are also often disturbed by drowsiness during the day, fatigue, emotional "deafness", disorientation, which are characteristic of all sedative antidepressants.

Other, more serious side effects from taking Amitriptyline occur less frequently, often have a dose-dependent nature, or appear in courses longer than 2 months.

Side effects of the drug:

• blurred vision, dilated pupils, tachycardia, delirium and hallucinations, intestinal obstruction, urination disorders;
• fainting, irritability, mania, anxiety, tremor of various muscle groups, their twitching or paralysis, nightmares, memory impairment and inability to concentrate;
• tachycardia, "strong heartbeat", hypotension, changes in the cardiogram in patients without heart pathologies, uncontrolled jumps in blood pressure, blockade of cardiac conduction;
• change in taste, malfunctioning of the liver, hepatitis, jaundice, nausea, heartburn, diarrhea, vomiting, uncontrolled change in appetite (increase or disappearance), weight gain or loss associated with these effects;

The endocrine system may respond to the course of treatment with such manifestations: swelling of the testicles, enlargement of the mammary glands, decreased libido or its significant increase, problems with potency.

Symptoms of abrupt discontinuation of therapy (withdrawal syndrome):

Of the allergic side effects noted: rash, swelling, itching, sensitivity of the skin and eyes to the sun. Among the atypical phenomena during treatment with Amitriptyline are tinnitus, swollen lymph nodes, hair loss, frequent urination, fever.

drug interaction

Co-administration of Amitriptyline with any alcohol-containing drinks depresses the central nervous system, significantly reduces pressure, and depresses the respiratory center. The body's sensitivity to alcohol during treatment increases.

The drug is absolutely incompatible with MAO inhibitor drugs, causing hyperpyrexia, uncontrolled increase in blood pressure, severe convulsions, up to death.

Interaction with groups of drugs and individual drugs:

1. With anticholinergic drugs (antiparkinsonian, antihistamines, atropine, amantadine) - the risk of all side effects increases.
2. With anticholinergics (benzodiazepine, phenothiazine) - mutual enhancement of action, increased convulsive and neuroleptic malignant syndromes.
3. With anticonvulsants - reduced efficiency, CNS depression, convulsions.
4. With indirect anticoagulants - increased blood thinning action.
5. With cimetidine, fluoxetine and fluvoxamine, the half-life is prolonged, the risk of intoxication with amitriptyline increases (the dose should be reduced by 20-50%).
6. With oral contraceptives, nicotine, barbiturates, phenytoin, carbamazepine, plasma concentrations decrease with a decrease in the effectiveness of Amitriptyline. Estrogen-containing drugs increase the bioavailability of the antidepressant.
7. With inhibitors of acetaldehyde (for example, disulfiram) - provokes clouding of consciousness to coma (delirium).
8. With benatidine, guanethidine, clonidine, reserpine and methyldopa, amitriptyline reduces their hypotensive effect.
9. Antiarrhythmic drugs (eg, quinidine) taken together with amitriptyline have the opposite effect, disrupting the heart rhythm.

Amitriptyline reduces the effectiveness of alpha-blockers, phenytoin, and may aggravate the course of depression that occurs during treatment with glucocorticosteroids. Drugs for the treatment of thyrotoxicosis increase the risk of agranulocytosis.

The drug is incompatible with epinephrine, norepinephrine, ephedrine, phenylephrine, pimozide, probucol, thyroid hormones, causing severe arrhythmias, tachycardia, hypertensive crisis. With anticholinergics and antipsychotics, there is a risk of excessive fever (above +41.5 ° C).

Terms and conditions of storage

• The drug should be stored in its original packaging, in a dry, dark place. The temperature should not exceed +25°C. Keep away from children.
• If properly stored, Amitriptyline retains its medicinal properties for 3 years. After this time, the drug is prohibited to use.
• The drug is dispensed by prescription.

Terms of dispensing from pharmacies

The drug can be purchased only on prescription. The prescription for the medicine remains at the pharmacy. A form certified by a doctor is kept for 3 months to control sales.

Analogues

Amitriptyline reviews of patients taking the drug are characterized as a reliable means of emergency care in acute conditions and long-term therapy of chronic pathologies. But the sheer number of side effects and the unpredictability of individual responses to tricyclic antidepressants often forces a replacement for this available drug.

Main analogues:

1. Saroten- drug-analogue of Amitriptyline on the active substance. Produced by foreign pharmaceutical companies and has a milder effect on the body. All indications for the appointment of Amitriptyline are valid in the case of the use of Saroten, but adverse reactions to it occur much less frequently. Dosages and contraindications for drugs are similar.
2. Novo-tryptin (Damilen)- a structural analogue of Amitriptyline, whose action is based on the same active substance. The drug is produced in Russia and Canada. All appointments of Amitripsin are valid for Novo-trypsin, and side effects are manifested to a lesser extent. Often a remedy is prescribed for the treatment of children, elderly patients, if necessary, use during pregnancy (only from the II trimester).
3. Anafranil- a substance also from the group of tricyclic antidepressants. Effective in anxiety disorders, panic attacks, depression, mental and motor retardation. The drug has much fewer contraindications: lactation period, post-infarction condition, allergy to components, age up to 5 years. The most serious side effects are tachycardia, hypertension, rash and itching.
4. Doxepin- a drug for the treatment of depression, manic-depressive psychosis, hypochondria, anxiety. It is a "light version" of Amitripsilin, differing from it structurally only by one extra oxygen atom. The drug works well in stopping panic attacks and treating sleep disorders. Unlike Amitriptyline, it has greater antihistamine activity, but less psychoanaleptic properties.
5. Melipramine. The active substance of the drug - imipramine hydrochloride - one of the first tricyclic antidepressants. Assign a remedy for the same indications, including enuresis and chronic pain. The drug has a great stimulating effect, in contrast to the sedative effect of Amitriptyline, so it is used in the morning. In some patients, Melipramine does not cause any side effects, otherwise the reactions of antidepressants are similar.

Amitriptyline has earned positive reviews from patients who have taken the drug for many years for its rapid action and availability. There are no analogues of the drug without side effects yet, therefore, despite complex drug interactions and an abundance of possible unpleasant consequences, it continues to be prescribed and used for many diseases.

Article formatting: Vladimir the Great

Video about Amitriptyline

Doctor about Amitriptyline:

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

Pharmacodynamics
The mechanism of the antidepressant action of amitriptyline is associated with 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.

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

Indications for use

Mode of application

Initial daily dose Amitriptyline when taken orally, it is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg, until the desired antidepressant effect is obtained. The optimal daily therapeutic dose is 150-200 mg (the maximum part of the dose is taken at night). In severe depression resistant to therapy, the dose is increased to 300 mg or more, up to the maximum tolerated dose. In these cases, it is advisable to start treatment with intramuscular or intravenous administration 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. In the event of signs of depression with a decrease in doses, it is necessary to return to the previous dose.

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

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

Assign intramuscularly or intravenously. In severe depression resistant to therapy: intramuscularly or intravenously (inject slowly!) 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 years of age and the elderly are given lower doses and increase them more slowly.

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

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

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

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

Side effects

Contraindications

Overdose

Interaction with other drugs

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. Joint application amitriptyline with disulfiram and other inhibitors of acetaldehyde dehydrogenase can provoke 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!

special instructions

Release form

Solution Description

Storage conditions

Shelf life - 2-3 years (depending on the form of release and manufacturer). Do not take after the expiry date stated on the packaging!

Conditions for dispensing from pharmacies - by prescription.

Synonyms

Compound

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

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

main parameters