Amitriptyline instructions for use, contraindications, side effects, reviews. What is dangerous amitriptyline Tablets amitriptyline side effects

Indications for the use of the tricyclic antidepressant Amitriptyline are depression, emotional disorders, behavioral disorders, schizophrenic psychosis, neurogenic pain syndrome, neurotic, organic brain damage.

Amitriptyline has an antidepressant, sedative effect by reducing the sensitivity of serotonin, beta-adrenergic receptors. It has an inhibitory effect on the processes in the brain.

The drug soothes pain, promotes scarring of tissues with stomach ulcers, reduces appetite. In the treatment of depression, the effect of the drug does not appear immediately. It takes on average up to 3 weeks for the results of the treatment to appear. Accordingly, the question arises: is it possible to take Amitriptyline with alcohol?

Properties

Tablets, pills are absorbed in the stomach, intestines. In the blood, the drug accumulates at a maximum concentration after 3-8 hours. The half-life is from 10 to 26 hours, metabolites of Amitriptyline are excreted within 18 to 44 hours.

Contraindications

Amitriptyline is contraindicated in the following diseases:

With caution, Amitriptyline is prescribed for epilepsy, high intraocular pressure, heart disease, arrhythmias.

Side effects are noted mainly from the side of the heart, nervous, vascular system, stomach.

When taking the drug observed:

• dizziness, drowsiness, tremor;
• confusion;
• noise in ears;
• nightmares;
• cardiopalmus;
• fainting;
• stomach pain, nausea, loss of appetite.

With an overdose of Amitriptyline, life-threatening conditions develop, convulsions, hallucinations, cardiac arrhythmia occur, psychosis, coma are possible.

On the video description of the drug Amitriptyline:

Interaction with alcohol

Amitriptyline enhances the effect of alcohol. The compatibility of these drugs causes a decrease in blood pressure, has an inhibitory effect on the respiratory center, and depresses the central nervous system.

Ethyl alcohol enhances the side effects of Amitriptyline. With simultaneous use, the risk of visual impairment, the appearance of hallucinations, and disorientation in the surrounding space increases.

Ethanol negatively affects the urinary system, causes significant difficulties with urination, provokes constipation, having a depressing effect on intestinal motility.

Ethanol and the drug negatively affect the liver, exhaust the possibilities of liver enzymes, and create conditions for the accumulation of metabolic products. Moreover, both ethanol and Amitriptyline metabolites are highly active.

So, acetaldehyde is a metabolite of alcohol, several times more toxic than ethyl alcohol itself. The activity of the metabolite of Amitriptyline, the compound nortriptyline, is also high. In addition, nortriptyline is excreted from the body for a longer time (up to 3 days).

The use of alcoholic beverages prolongs the half-life of the drug and its metabolites, which creates the risk of overdose, and the appearance of all the symptoms associated with an overdose in a more pronounced manifestation.

Possible consequences

Alcohol in combination with Amitriptyline:

• increases depression, causes a panic attack, psychosis;
• disrupts liver function, leads to cirrhosis;
• makes it difficult to excrete urine, contributes to kidney failure;
• causes a sharp decrease in blood pressure, a decrease in body temperature, to whom;
• can cause respiratory arrest and death.

Taking 5 g of Amitriptyline causes poisoning, and the lethal dose of the drug in the absence of alcohol in the blood is 12 g. Ethyl alcohol enhances the side effects of the antidepressant, which in an unpredictable way reduces the lethal dose of the drug.

The degree of intensification of the side effects of the drug depends on the condition of the patient's liver, the characteristics of his metabolism, the ability to utilize alcohol, antidepressant and their metabolites.

A person, simply out of ignorance, can exceed a lethal dose if he combines the medicine, even at the prescribed therapeutic dosage, with the use of alcoholic beverages.

Admission rules

Amitriptyline and its metabolites remain in the blood for a long time. It may take several days for the drug to be completely cleared from the body. You can drink alcohol after the last dose of an antidepressant no earlier than 3 days later.

But the tradition of wine drinking, unfortunately, is indestructible. They drink "for the company" even during treatment with antidepressants. Such extreme lovers should be aware of the danger of an overdose of the drug as a result of the intensifying effect of alcohol, take alcoholic beverages in the minimum dose.

You can resume the course of treatment after drinking alcohol no earlier than a day later. The most dangerous consequence of taking alcohol and Amitriptyline can be a severe coma.

And not always the doctors have time to save the victim. And the exit from a coma is accompanied by a deterioration in vision, a violation of cardiac activity, prolonged depression, which is very difficult to treat.

conclusions

Amitriptyline should not be combined with alcohol. Taking even small doses of alcohol-containing drinks can cause severe depression, cancel out the result of several weeks of treatment for depression, stomach ulcers, schizophrenic psychosis.

According to doctors, alcohol is contraindicated both in the treatment of Amitriptyline and in the diseases for which it is prescribed. Drinking alcohol just causes the disease for which antidepressants are prescribed. And it is unacceptable to combine the intake of a depressant, which is alcohol, with the antidepressant Amitriptyline.

Symptoms and dangerous consequences of an overdose of Amitriptyline

As with any medication, the dose may be exceeded during treatment with Amitriptyline, and then such unpleasant moments as the consequences of an overdose, symptoms of poisoning and, accordingly, the fight against them cannot be avoided.

What is Amitriptyline?

The antidepressant Amitriptyline is a "classic" drug for a wide range of ailments and disorders, with a wide range of indications, contraindications, and side effects.

The medicine is produced by pharmacists both in the form of tablets, capsules and dragees, and in the form of solutions for intramuscular injections.

The medicine has a pronounced effect:

This is due to its high antihistamine and anticholinergic activity, and the ease of the possibility of drug poisoning or accidental overdose is also due to this.

How does an overdose occur?

The area of ​​​​use of the drug is quite wide, if we summarize the indications for use, then a medicine is prescribed, mainly in the following cases:

1. depression.
2. Exacerbations of neurological disorders.
3. Behavioral disturbances and inadequacy of reactions.
4. Emotional disorders of mixed nature.
5. Children's enuresis and fears.
6. Nervous bulimia.
7. Chronic migraine.

It is recommended to take the drug, starting with the minimum dose - this is 50 mg per day, then, based on the body's reaction, the dosage is increased, slightly, but regularly - by 100 mg, not exceeding the allowable daily threshold of 300 mg. And at this stage of taking the medicine there is a significant risk of poisoning them.

signs

In the very first hours after taking an excessive amount of a tranquilizer, symptoms such as:

They are quickly replaced by:

At this stage, a person, as a rule, does not attach any importance to his symptoms, the idea that an overdose is possible does not even occur to him. They usually begin to worry only with the appearance of hallucinations, after which the following symptoms can be observed:

• dryness of all mucous membranes in the body;
• urinary retention;
• as opposed to urination - spontaneous relaxation and emptying of the intestine;
• a sharp increase in temperature;
• attacks of tachycardia;
• severe convulsions, in the form of seizures, resembling epilepsy.

After that, the depression of the central nervous system continues, with variable intensity for several hours. This is accompanied by the following symptoms:

• shortness of breath, shortness of breath - similar to asthma attacks;
• a sharp disturbance in the heart rhythm - pronounced fluttering of the ventricles, tachyarrhythmia;
• arterial hypotension.

These features are being replaced by:

Death occurs quickly, with common signs of such ailments as:

• cardiovascular insufficiency;
• asthmatic insufficiency of the respiratory system.

How to cure drug poisoning?

Excessive action of amitriptyline is also dangerous because there is no antidote for the drug. If there is a possibility of an overdose of the drug, then it is necessary to immediately call the doctors, and while they are traveling, provide first aid. It will consist in simple actions:

1. Gastric lavage if the medication was taken less than three hours ago.
2. Reception by the affected sorbent, it is best to double the dosage of activated charcoal.
3. Providing access to fresh air.
4. Conscious person support.

Arriving on a call, doctors, as a rule, immediately hospitalize the victim. In a hospital, treatment will begin with the fact that a person will be connected to cardiac monitoring in order to control:

• frequency and freedom of breathing;
• blood pressure indicators;
• the rhythm of heartbeats.

The following will also need to be monitored:

1. The level of electrolytes, their concentration in the blood of the victim.
2. Acid-alkaline state of the body.

Since no antidote or antidote for tranquilizer poisoning has been invented, and extracorporeal detoxification does not help, the following therapy is carried out:

• In case of interruptions in breathing - artificial ventilation of the lungs, if necessary - incubation of the trachea.
• In case of metabolic acidosis, droppers with solutions of sodium bicarbonate and sodium chloride are installed, if necessary, hyperventilation of the lungs is connected.
• Antiarrhythmic drugs are prescribed.
• In the case of heart failure, solutions of salts and colloids are administered intravenously, sometimes Dopamine infusion is done.
• If necessary, stop convulsions - Valium or Seduxen are prescribed.

Effects

Possible complications after poisoning with Amitriptyline include a number of pathologies. The consequences of an overdose can be divided into two types:

Early, that is, arising, as a rule, in the first year after an accident with a medicine, include:

• acute pneumonia with complications;
• hypocoagulation syndrome with significant bleeding, both internal and external;
• acute renal failure;
• liver disease and dysfunction.

• diseases of the nervous system and brain pathology;
• chronic uncontrolled spontaneous depression;
• organ failure in a chronic form - kidneys, liver, heart.

In the case of treatment with any tranquilizers and antidepressants, it is easier to avoid an overdose than to deal with its consequences. However, drug poisoning does not always occur due to an excessive dose, sometimes it is due to a person’s negligent attitude to their health and the use of alcohol in conjunction with medications.

Amitriptyline and alcohol

Alcohol and Amitriptyline are incompatible, their simultaneous use can lead to any completely unpredictable consequences, including sudden death.

This is due to the fact that both substances have the same effect on the body:

1. Inhibition of the functions of the central nervous system, their oppression.
2. Increase in blood pressure.
3. Disorientation.
4. Allergic reactions.

And a number of other indicators.

The combination of alcohol and an antidepressant does not just mutually increase their effect at times, it directly strikes at:

• Kidneys, which will manifest itself in the form of blackening of the tongue, nausea, stomatitis.
• The liver, forced to break down both alcohol and a tranquilizer, in response, it will manifest various types of toxicosis.
• A heart that can just stop at any moment.

With alcoholism, as a disease, this antidepressant is not prescribed under any circumstances if the period of sobriety of a person is less than six months. The state of internal organs is also taken into account.

Avoiding Amitriptyline poisoning is simple, just take it correctly - no more than 300 mg per day and do not mix with alcohol.

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For what purpose and when is amitriptyline prescribed?

Quite often, with depression, doctors prescribe amitriptyline to patients, the indications for the use of which are various psycho-emotional disorders. In our country, it was not customary to treat such conditions for a long time, but, according to recent studies, depression is a disease and it requires treatment.

It affects about 20% of the population of all developed countries of the modern world, which puts it on a par with such diseases as cardiovascular diseases and oncology. The main danger is that a person loses the taste for life, he is not interested in anything, no desires arise. And this disrupts the ability to work, affects the work of internal organs, relationships with loved ones. The disease in the initial stages is rarely manifested by disorders of the body systems, and the person does not consider it necessary to visit a specialist. And when it turns, depression is already severe and protracted.

What are the dangers of depression?

With the modern rhythm of life with many problems, difficult situations and instability, depression is increasingly being diagnosed by psychologists and psychiatrists. Usually this disease develops after a severe stressful situation, which was preceded by a long emotional overstrain: a serious illness of a loved one that ended in his death, a wave of layoffs at work and dismissal, long preparation for the exam and failure of one of them, etc.

Depression usually presents with the following symptoms:

• excitement and anxiety;
• constant anxiety;
• oppression;
• increased irritability;
• inability to concentrate;
• loss of interest in the environment.

In order to get rid of the disease, it is necessary to undergo a complex and rather long treatment, including taking various antidepressants, psychosocial therapy and attending special courses that increase emotional stability.

Drug therapy for depression

Treatment with drugs is reduced to taking various drugs that restore the mental and emotional state of a person - antidepressants. They have different mechanisms of action on the nervous system, which determines their belonging to one or another class of medicines. They are divided into the following classes:

More often than others, representatives of the first class of drugs are used in medicine, one of which is Amitriptyline Nycomed. In addition to depression, this drug has other indications for use.

In psychiatry, it is prescribed for a variety of diagnoses, even very severe ones. Amitriptyline Nycomed is effective for the treatment of depression of all types, including neurosis, which led to brain damage. Depression in alcohol dependence, which is reflected by anxiety, sleep disorders, restlessness.

Also, this drug is prescribed for urinary incontinence at night, various phobias, eating disorders (bulimia, anorexia), for the prevention of migraine. It is often included in complex therapy for diseases of the gastrointestinal tract (ulcers, gastritis, gastric bleeding), and can be prescribed for severe pain in cancer patients suffering from rheumatism and neuropathy.

The composition of the drug and its action

The drug is based on the active ingredient amitriptyline hydrochloride. The pharmacological action of Amitriptyline Nycomed is very wide, which leads to a wide range of its appointments. It has such effects as a pronounced sedative, hypnotic and antihistamine. In addition, Amitriptyline Nycomed relieves anxiety well, has an analgesic effect, slightly stimulates the nervous system, gives a feeling of energy and promotes the healing of ulcers on the mucous membranes of the stomach and intestines.

How to use Amitriptyline Nycomed?

The drug is available in two forms - uncoated tablets and intramuscular injections. With psychoemotional disorders of the mild type, Amitriptyline Nycomed is prescribed in tablet form in the most minimal doses. It is taken after meals, without chewing and drinking plenty of liquid.

The specialist prescribes a dose, it depends on the general condition of the patient, his age and the presence of concomitant diseases. On average, the therapeutic effect of the drug occurs after 3 weeks from the day you start taking it.

At the first stages of treatment and in not very severe conditions, the dosage is prescribed as minimal as possible. If there is no improvement, the frequency of administration or dose may increase. In severe emotional disorders or schizophrenia, Amitriptyline Nycomed can be prescribed in the form of injections, followed by a course of tablet treatment.

The duration of admission depends on the diagnosis of the patient and the severity of his illness, and the general therapeutic course is at least one month. The maximum course of taking an antidepressant should not exceed 12 months, because this can lead to severe and irreversible complications, the most severe of which is death.

Like any drug, Amitriptyline Nycomed has contraindications for use. It is not prescribed to patients after myocardial infarction and in the stage of exacerbation of cardiovascular diseases, if the patient is intoxicated, suffers from angle-closure glaucoma, intraventricular obstruction. Do not use Amitriptyline Nycomed in conjunction with sleeping pills, strong psychotropic drugs and analgesics. Do not prescribe this medicine to children and women during breastfeeding.

Amitriptyline - emergency or extreme case

Amitriptyline is a new generation of antidepressants. Producer Poland, Germany. Similar products with the same name are produced by many countries. Released by prescription. It has a pronounced sedative effect. It is prescribed for severe nervous disorders, irritability, aggressiveness, panic attacks, migraines. In special cases, it is prescribed for menopause with severe CNS disorders. The therapeutic effect develops 2 weeks after the start of treatment.

Release form

Produced in the form of dragees or tablets, solution for injection. The injections are administered intramuscularly. In this form, it is used in therapy within the walls of the hospital. At home, dragee is more often used.

The tablets are round yellow. The package contains 50 pieces. The active ingredient is amitriptyline hydrochloride. As additional components are used:

The shell of the tablets is resistant to the acidic environment of the digestive tract. Efficiency is not lost.

In the form of a solution for injection, it is available in transparent ampoules of 10 pieces per pack.

Store at a temperature not exceeding 25 degrees Celsius. Shelf life 3 years.

Indications for use

Climax negatively affects the entire body. The central nervous system is under special stress. In a mild form, a woman feels irritability, mood swings, feels a sense of self-pity. Tearfulness, anger, and other unpleasant states are observed. With a strong load on the CNR, more dangerous conditions can be observed: aggression, clouding of consciousness, panic attacks, fear, thoughts of death, and so on. Amitriptyline is prescribed by a doctor after a conversation with a woman, an examination. It is highly undesirable to start treatment on your own. The drug is very strong, if used improperly, causes severe side effects.

The indication for use is:

• persistent depression;
• neurosis;
• significant behavioral disorder;
• phobias;
• emotional disorders;
• anorexia;
• chronic pain syndrome on a nervous basis.

Prescribed to prevent migraine if there have been problems in the past in this part. A direct indication for treatment with Amitriptyline is a confirmed diagnosis:

Mild sleep disorders, mood swings Amitriptyline is not treated. To do this, use lighter means.

Contraindication

Amitriptyline is the strongest antidepressant that affects the functioning of the central nervous system. In this regard, there are a number of contraindications:

• myocardial infarction;
• pronounced drops in blood pressure;
• diseases of the liver, kidneys;
• diseases of the gastrointestinal tract;
• heart failure;
• atony of the bladder;
• individual intolerance to the components;
• parallel therapy with MAO inhibitors.

Caution should be given to women with:

• bronchial asthma;
• manic-depressive psychosis;
• with heart problems;
• schizophrenia;
• glaucoma;
• alcoholism;
• epilepsy;
• in violation of hematopoiesis.

In case of problems with the kidneys and liver, the doctor may decide on the advisability of treatment, but with a correction of the daily dose. In the future, the patient's condition is constantly monitored.

Terms of use

Dragee is swallowed whole during meals or after a meal. Wash down with a small amount of liquid. The optimal dose per day is 200 mg. Start taking the drug with 50-75 mg per day. Increase every day by 25 mg. The maximum dose is taken at bedtime. Reception is carried out 3-4 times a day. In severe depression, increase to 300 mg. The therapy is carried out under the supervision of doctors.

After achieving a stable therapeutic effect after 4 weeks, the dose is gradually reduced every day. If signs of disorder appear again, return to the previous dosage. In the absence of the desired effect for about 1 month, the therapy is canceled due to the lack of a proper result.

Elderly women after 65 years of age are prescribed pills in doses of 25, 50, 100 mg per day. Divided into several receptions or drink at night for 1 time. To prevent migraine, severe headache, take 100 mg per day.

Intramuscularly injected 10-30 mg slowly. The injection sites must be changed. Daily dose 150 mg. After 3 weeks of injections, you should switch to a dragee. Injections are administered during therapy within the walls of the hospital.

Concurrent use with drugs

Amitriptyline enhances the side effects of drugs:

• anticonvulsants;
• sedatives;
• neuroleptics;
• sleeping pills;
• means of anesthesia;
• other antidepressants;
• analgesics;
• alcohol.

Concurrent use with birth control pills enhances the activity of Amitriptyline. Its combined use with MAO inhibitors leads to death. The interval between treatments with these drugs should be at least 2 weeks.

Unwanted Effects

Causes a lot of side effects. Some of them do not require interruption of treatment, go away on their own after a few days. In some cases, the dose is adjusted. The situation is considered under control and quite normal.

• increased intracranial pressure;
• dry mouth;
• bowel problems;
• blurred vision;
• temperature rise;
• problems with urination.

A large list of side effects occurs from the side of the central nervous system, digestive, cardiovascular, endocrine. There is an allergic reaction on the skin. With prolonged therapy, there is an increase in body weight, increased sweating.

Side effects appear after the drug is discontinued. Especially if the doses were high.

special instructions

Therapy with Amitriptyline should be carried out according to the doctor's prescription, under his supervision. Periodically, it is necessary to undergo an examination, take tests. It is strictly forbidden to take alcohol during therapy. It is not recommended to drive a car, perform work that requires high accuracy, fast response. After the age of 65 years, the daily dose should not exceed 100 mg. At high doses, convulsive seizures are possible.

Overdose

Toxic symptoms are observed a few hours after taking the next dose.

• pupil dilation;
• apathy;
• loss of consciousness;
• decrease in body temperature;
• drowsiness;
• hallucinations;
• pressure reduction;
• disruption of the heart;
• convulsions;
• coma.

To eliminate the symptoms, it is necessary to perform gastric lavage, provide symptomatic treatment.

Effect on the body

Amitriptyline improves pathologically low mood, eliminates headaches, removes panic attacks, neurasthenia, neuroses, and normalizes sleep. A significant improvement is observed after 3 weeks of treatment. The analgesic effect is observed almost immediately. After internal administration of the tablet, a high concentration in the blood appears after 4 hours. The half-life is 25 hours. It is excreted mainly in the urine. The therapeutic effect lasts for a long time. A second course is prescribed according to indications not earlier than 1 month after the end of the previous one.

The cost of the drug

Amitriptyline is an affordable drug. You can buy it at any pharmacy with a prescription from a doctor. The cost depends on the location of the pharmacy, manufacturers.

• Tablets 25 mg, 50 pcs. - 26.50 rubles;
• Tablets 10 mg, 50 pcs. - 27.00 rubles;
• Tablets 20 mg, 50 pcs. - 46 rubles;
• Ampoules, 2 ml, 10 pcs. - 46 rubles.

Amitriptyline is produced by Denmark, Russia, Croatia, Poland, Germany, Czech Republic.

Analogues

Among similar products with an identical active ingredient, we can distinguish:

The question of replacing Amitriptyline with another similar drug should be discussed with the doctor.

Amitriptyline is produced in many countries. The buyer himself makes a choice in favor of one or the other. The price differs insignificantly. The main difference between the drug in manufacturing technology. The final choice is up to the buyer.

Reviews of women taking Amitriptyline

“They prescribed a drug for deep depression. I took it according to the instructions. At first there was a state of deep hibernation. Don't care at all. I just wanted to sleep. Apathy was present for a week, then hallucinations began to appear in broad daylight. Stopped taking it out of fear. Didn't go to the doctor. I did not notice any side effects after that, it even got better right away. My depression also disappeared, probably from fear. In general, the drug is terrible!

“Terrible side effects are not for me. I took 170 mg per day. Of the undesirable effects of dry mouth. Sleep didn't get better. I still woke up at 4 in the morning, I could not fall asleep. As a sleeping pill it does not work at all. I didn't have depression."

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She suffered from a terrible migraine. They prescribed me this drug. Initially, I was alarmed by the side effects, and what applies to antidepressants. Then the doctor explained that the migraine was due to the severe stiffness of the body. Amitriptyline relieves stress, allows the body to relax. I noticed results almost immediately. The migraine stopped tormenting after a week of taking it. She was still treated for 2 weeks. Within 1 year, the headache bothered slightly. The drug helps. Of the side effects, I had an unpleasant aftertaste in my mouth, my eyesight worsened during the treatment, then it recovered. Dreams were unusual, not always good. After cancellation, no unpleasant symptoms!

There was a terrible depression, I did not want to live. This drug was prescribed. I vaguely remember my first impressions. You just turn into a vegetable. Nothing to worry about, nothing to care about. Slept day, night, could not sleep off. A week later she began to revive. There was a mood, an interest in life. Slowly everything got better. I would like to note that the drug is very strong. It is better to fight ordinary depression by other means. Besides, you can't get carried away. Get used to it like a drug!

She suffered from chronic joint pain. The neurologist explained that my pain was imaginary, from nerves. Prescribed this drug. I took it according to the instructions. Frightening side effects. Pain relief almost immediately. Gradually, she stopped feeling pain. After 2 weeks I didn't feel it at all. Completed the course. Everything became good. Chronic pain that tormented me for 2 years disappeared in 1.5 months!

Amitriptyline

Release forms

Sale: prescription

Shelf life: 24 months.

Sale: prescription

Storage: 15-25C (room temperature)

Expiration date: 36 months.

Instructions for amitriptyline

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

Bioavailability of Amitriptyline is about 50%, half-life. Elimination from the body is carried out with urine. The drug is available in tablet and ampouled form. Begin pharmacotherapy with a dose of mg, the optimal time of admission is before bedtime. Gradually, during the week, the dose is increased by 3-4 times. In the absence of improvement in the second week, the daily dose is increased to 300 mg. Elimination of depressive manifestations is not a reason for refusing treatment: in this case, the dose is reduced to daily mg and pharmacotherapy is continued for at least another three months. In the elderly with a mild course of depression, the dose of the drug is set in the range from 30 to 100 mg per day, and when positive results are achieved, they switch to a maintenance daily dose of vmg. In the course of treatment, it is necessary to avoid situations that require a sharp rise from a sitting or lying position. It is not recommended to abruptly interrupt treatment: in this case, a withdrawal syndrome may develop. It is necessary to take the necessary precautions when using Amitriptyline in patients suffering from epilepsy, because. the drug in a daily dose of more than 150 mg reduces the convulsive threshold. When planning treatment, the possibility of suicide attempts in patients suffering from severe depression should be kept in mind. The combined use of Amitriptyline and electroconvulsive therapy is possible only under the condition of constant medical monitoring. In patients with a burdened history and the elderly, taking the drug can lead to the occurrence of pharmacological psychoses (after the cessation of drug therapy, such phenomena quickly disappear). Prolonged use of Amitriptyline may lead to the development of caries. The drug is not compatible with alcohol.

Reviews of doctors about amitriptyline

Amitriptyline belongs to the tricyclic antidepressants, the oldest antidepressant. Subjectively not suitable for all patients. Yes, it removes well the affect of melancholy, anxiety for 2-3 weeks of constant use. The best effect at stationary dosages and in a hospital. Well relieves anxiety, effective in the treatment of panic attacks.

Subjectively, some patients note drowsiness, according to patients, "stomps, sausages." Others take large doses and experience no side effects. It must be remembered that after 2 weeks of admission, some patients, more often men, may experience urinary retention.

Inexpensive effective antidepressant.

A good antidepressant with sufficient effect, time-tested, is available. It helps well in neurological practice in the treatment of chronic pain syndrome, mainly in peripheral neuropathies of various origins, postherpetic neuralgia, migraine.

There are side effects, mainly at the beginning of taking the drug, in the form of drowsiness, dizziness, dry mouth, changes in taste, sometimes feelings of anxiety, anxiety, as a result of which it is necessary to adjust the dosage at the beginning and at the end of taking the drug.

The drug of choice for patients with limited finances, but you have to put up with side effects.

Affordable, inexpensive antidepressant, on which sufficient experience has been collected. It has the widest spectrum of receptor activity.

Causes quite pronounced side effects: dry mouth, urinary retention, sedation. Not everyone is suitable for outpatient treatment. Not recommended for first line treatment of depression, as SSRIs don't work well after that.

An excellent analgesic for headaches (psychosomatic). And the antidepressant is just wonderful.

Disappeared from pharmacies at a dosage of 10 mg. Urinary retention is possible.

Far from golden, but certainly the standard of antidepressant therapy. It combines well with other drugs, suitable as an adjunct to therapy before the development of the effect of SSRIs and as a symptomatic agent.

At the present stage, the appointment of amitriptyline, in my opinion, is preferable in a specialized department, moreover, by injection - for the rapid relief of severe neurotic depression. Best of all - in / in the drip for 1 week, followed by the selection of a serotonergic antidepressant.

All known side effects, the most important of which are cystitis, prolactinemia, QT interval widening, weight gain.

Until now, almost the only drug that allows you to achieve an almost "instant" antidepressant effect.

The drug from the first generation of antidepressants belongs to the group of tricyclic antidepressants. Indispensable for a major depressive episode and anxiety-depressive symptoms. Minimum price.

Often side effects in the form of dryness, accommodation spasm, sphincter spasm and sexual dysfunction.

The drug is affordable and effective.

There are side effects that reduce the quality of life for people taking this drug. These include lethargy and the inability to engage in mental work, drive a car, as the reaction rate decreases sharply. In men suffering from prostatic hyperplasia, it can cause urinary retention.

For a long time of use in neurological practice, as an adjuvant for the treatment of dysfunctional back pain, Amitriptyline has shown itself to be quite effective when taken once a day for a short period.

Most side effects occur when the dosage of the drug is incorrectly selected and patients do not comply with the regimen.

Amitriptyline is very often prescribed in the wrong doses, for the wrong duration, and in the wrong combinations. The use of amitriptyline requires experience and skill. It would be worth forbidding to prescribe it to non-psychiatrists. I stopped prescribing it myself a long time ago. I think this is the prerogative of psychiatrists.

In outpatient practice, it is extremely difficult for working people to use it due to numerous side effects.

An interesting effect when combined with other drugs, but the main thing is its effectiveness, and, of course, price and quality.

Of the side effects, the main disadvantage is dry mouth, increased appetite and drowsiness, sometimes disorientation, muscle rigidity, in particular the bladder, sometimes with an overdose of vomiting, arrhythmia, arterial hypotension, heart failure, respiratory depression. But if taken correctly and carefully, then disadvantages can be avoided.

Amitriptyline is the gold standard for tricyclic antidepressants.

The drug is old, rather well studied, used for various neurological and mental disorders, as well as in the treatment of persistent pain syndromes in combination with analgesics (for example, in cancer patients).

Many side effects, not designed for long-term use.

Main advantage: efficiency at low cost. These two facts allow amitriptyline to remain in medical practice, despite frequent side effects. "Cheap and cheerful."

"Good old" antidepressant. One of the first. Well studied. Until now, it “does its job” well in a narrow range of clinical situations: 1) severe endogenous depression with severe anxiety, agitation, suicidal tendencies; 2) post-psychotic (post-schizophrenic) depressions with the threat of exacerbation, failure of remission; 3) therapy of anxious depressions in the structure of chronic endogenous psychoses, especially in those cases when insurance against exacerbation of the course of the endogenous process is needed; 4) depressive phases in the structure of bipolar affective disorder with the threat of phase inversion (usually in the absence of proper normothymic therapy).

It is well known - cardiotoxic, extremely pronounced anticholinergic side effects - dry mouth, nausea, constipation, etc. Strong sedation, sexual dysfunction, metabolic syndrome.

In the presence of new generation antidepressants, these are not “cons”, these are the features of tricyclic antidepressants, just like with MAO inhibitors, everything was even an order of magnitude more complicated.

An excellent choice for patients in a difficult financial situation. It can be used for sleep disorders, anxiety depression, persistent hypochondria in various combinations, depressive symptoms within illnesses with severe psychotic symptoms. Speed ​​is good.

Side effects are terrible dryness, dizziness, drowsiness that disappears from the beginning, tachycardia, problems with urinary retention in both men and women. Be careful with the elderly.

A powerful drug, in which side effects are often ahead of the curative ones.

Amitriptyline is a tricyclic antidepressant that I prescribe to my patients with endogenous depression of varying severity. The drug has a good antidepressant effect, but sometimes it takes a long time to wait for the effect. Alas, this drug is not without side effects, which often force patients to refuse this drug.

Gross formula

Pharmacological group of the substance Amitriptyline

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Amitriptyline

Tricyclic antidepressant. Amitriptyline hydrochloride is a white, odorless crystalline powder, easily soluble in water, ethanol, chloroform. Molecular weight 313.87.

Pharmacology

It inhibits the reuptake of neurotransmitters (norepinephrine, serotonin) by presynaptic nerve endings of neurons, causes the accumulation of monoamines in the synaptic cleft and enhances postsynaptic impulses. With prolonged use, it reduces the functional activity (desensitization) of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed during depressive states. Blocks m-holino- and histamine receptors of the central nervous system.

When taken orally, it is quickly and well absorbed from the gastrointestinal tract. The bioavailability of amitriptyline with different routes of administration is 30-60%, its metabolite - nortriptyline - 46-70%. Cmax in the blood after oral administration is reached after 2.0-7.7 hours. Therapeutic blood concentrations for amitriptyline are 50-250 ng / ml, for nortriptyline - 50-150 ng / ml. Binding to blood proteins is 95%. Easily passes, like nortriptyline, through histohematic barriers, including the BBB, placental, penetrates into breast milk. T 1 / 2 is 10-26 hours, for nortriptyline - 18-44 hours. In the liver, it undergoes biotransformation (demethylation, hydroxylation, N-oxidation) and forms active - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. It is excreted by the kidneys (mainly in the form of metabolites) within a few days.

In anxiety-depressive conditions, it reduces anxiety, agitation and depressive manifestations. Antidepressant action develops within 2-3 weeks after the start of treatment. With a sudden discontinuation after prolonged treatment, withdrawal syndrome may develop.

The use of the substance Amitriptyline

Depression of various etiologies (especially with severe anxiety and agitation), incl. endogenous, involutional, reactive, neurotic, with organic brain damage, drug-induced; schizophrenic psychoses, mixed emotional disorders, behavioral disorders, bulimia nervosa, childhood enuresis (except for children with hypotension of the bladder), chronic pain syndrome (neurogenic in nature), migraine prophylaxis.

Contraindications

Hypersensitivity, the use of MAO inhibitors in the previous 2 weeks, myocardial infarction (acute and recovery periods), heart failure in the stage of decompensation, impaired intracardiac conduction, severe arterial hypertension, benign prostatic hyperplasia, bladder atony, paralytic ileus, pyloric stenosis, peptic ulcer stomach and duodenum in the acute stage, acute diseases of the liver and / or kidneys with a pronounced violation of their function, blood diseases, children under 6 years of age (for injection forms - up to 12 years).

Application restrictions

Epilepsy, ischemic heart disease, arrhythmia, heart failure, angle-closure glaucoma, intraocular hypertension, hyperthyroidism.

Use during pregnancy and lactation

Contraindicated in pregnancy.

At the time of treatment should stop breastfeeding.

Side effects of Amitriptyline

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

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

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

From the digestive tract: nausea, vomiting, heartburn, anorexia, epigastric discomfort, gastralgia, increased activity of hepatic transaminases, stomatitis, taste disturbance, darkening of the tongue.

From the side of metabolism: galactorrhea, changes in ADH secretion; rarely - hypo- or hyperglycemia, impaired glucose tolerance.

From the genitourinary system: change in libido, potency, testicular edema, glucosuria, pollakiuria.

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

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

Interaction

Incompatible with MAO inhibitors. Enhances the inhibitory effect on the central nervous system of neuroleptics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; shows synergism when interacting with other antidepressants. When combined with neuroleptics and / or anticholinergic drugs, it is possible to develop a febrile temperature reaction, paralytic ileus. Potentiates the hypertensive effects of catecholamines and other adrenostimulants, which increases the risk of developing cardiac arrhythmias, tachycardia, and severe arterial hypertension. May reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect of anticonvulsants. With simultaneous use with anticoagulants - coumarin or indandione derivatives - an increase in the anticoagulant activity of the latter is possible. Cimetidine increases the plasma concentration of amitriptyline with the possible development of toxic effects, inducers of microsomal liver enzymes (barbiturates, carbamazepine) - reduce. Quinidine slows down the metabolism of amitriptyline, estrogen-containing oral contraceptives may increase bioavailability. Co-administration with disulfiram and other acetaldehyde dehydrogenase inhibitors may cause delirium. Probucol may exacerbate cardiac arrhythmias. Amitriptyline may exacerbate glucocorticoid-induced depression. When used together with drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases. With caution combine amitriptyline with digitalis preparations and baclofen.

Overdose

Symptoms: hallucinations, convulsions, delirium, coma, cardiac conduction disturbance, extrasystole, ventricular arrhythmia, hypothermia.

Treatment: gastric lavage, activated charcoal suspension, laxatives, fluid infusion, symptomatic therapy, maintaining body temperature, monitoring the function of the cardiovascular system for at least 5 days, because recurrence of violations can occur after 48 hours or later. Hemodialysis and forced diuresis are ineffective.

Routes of administration

Inside, in / m.

Amitriptyline Substance Precautions

Reception of amitriptyline is possible no earlier than 14 days after the abolition of MAO inhibitors. Reduced doses are recommended for elderly patients and children. Should not be given to patients with mania. Due to the possibility of suicidal attempts in patients with depression, regular monitoring of patients is necessary, especially in the first weeks of treatment, as well as administration in the minimum required doses to reduce the risk of overdose. If there is no improvement in the patient's condition within 3-4 weeks, it is necessary to reconsider the tactics of treatment. During treatment, you should avoid drinking alcohol, as well as abandon activities that require increased attention and speed of reactions.

In life, various troubles happen that bring serious harm to the well-being and nervous system of a person. To cope with stress, emotional experiences or illnesses, doctors prescribe the use of special drugs -.

But, like other medicines, they can not only heal, but also be harmful, so before using it, you must definitely read the instructions and pay attention to existing contraindications and possible side effects. One of the most popular and effective drugs of this group is Amitriptyline.

Amitriptyline is an antidepressant with sedative, antiulcer, and antibulimic effects. Its main active ingredient is amitriptyline hydrochloride. Excipients are lactose monohydrate, calcium stearate, colloidal silicon dioxide, gelatin, corn starch and talc.

The drug is available in the form of a solution and tablets of a round shape, convex on both sides, yellow, film-coated.

The action of the drug is based on the suppression of neuronal reuptake of dopamine, norepinephrine and serotonin. The drug has a central analgesic, anti-bulimic and anti-ulcer effect, helps in the elimination of nocturnal enuresis - urinary incontinence.

As an antidepressant, it fully manifests its effect after 2-4 weeks of regular use of the drug.

When prescribing, the doctor must take into account the possible side effects of Amitriptyline, so trying to be treated with the drug on your own can be risky.

Appointment and use of the drug

The scope of the drug is quite wide, since it is able to treat not only depressive conditions of a different nature, but also ulcerative lesions of various organs of the gastrointestinal tract, headaches, and is also used as a prophylactic against migraines.

The main indications for the appointment of Amitriptyline are the following conditions or diseases:

• Psychosis on the background of schizophrenia.
• Mixed emotional disorders.
• Nervous form of bulimia.
• Behavioral disorders.
• Bedwetting (in cases where enuresis is provoked by a weak muscle tone of the bladder).
• Pain of a chronic type (atypical pain in the face, rheumatic pain and suffering in cancer patients, diabetic and post-traumatic neuropathy, neuralgia after herpes).

The drug showed itself well with increased excitability, nervousness, sleep disorders in patients with alcoholism.

Medication rules:

• When using the drug, the dosage increases gradually, starting from 25-50 mg per day for adults. Take the tablets at night, drinking them with water and not chewing. During the week, the dosage may increase to reach 150-200 mg per day. This dose should be divided into three doses.
• You can raise the dosage up to 300 mg per day if the body does not respond positively to taking the drug. This can be done after consultation with the attending physician, taking into account the possible side effects of Amitriptyline. After a decrease or complete disappearance of depressive symptoms, the dosage is reduced to 50-100 mg of the drug during the day.
• Treatment is considered ineffective and subject to cancellation if the patient does not feel improvement after using the drug for a month or 2 weeks in a row.
• For older patients with minor health problems, the drug is usually prescribed at a dose of 30 to 100 mg per day. When the patient's condition returns to normal, they switch to a reduced dosage in the range of 25–50 mg of the drug.
• In the prevention of migraines and the treatment of chronic headaches, as well as other manifestations of neurological pain, the patient is prescribed Amitriptyline at a dosage of 12.5 mg to 100 mg daily.
• In depressive conditions in children aged 6 to 12 years, children are prescribed the drug at a dosage of 10–30 mg per day, or they are calculated according to the formula 1–5 mg per kilogram of weight. The medicine is divided into several doses.
• With bedwetting in children aged 6-10 years, the drug is given at night, 10-20 mg per day, adolescents from 11 to 16 years old in this situation receive 25-50 mg of Amitriptyline per 24 hours.
• With intravenous infusions or intramuscular injections, the agent must be administered slowly, 4 times a day, the dose is 20-40 mg. The duration of treatment is from six months to 8 months.

Who and when is Amitriptyline contraindicated?

The drug has the following contraindications:

• Hypersensitivity to amitriptyline hydrochloride or other components of the drug.
• Children's age up to 6 years.
• Pregnancy.
• breastfeeding period.
• High scores.
• Problems with the cardiovascular system (disturbances in myocardial conduction).
• Bladder atony.
• Diseases of the liver and kidneys in the acute stage.
• Prostate hypertrophy.
• Intestinal obstruction of paralytic nature.

The presence in the anamnesis of these contraindications makes it impossible to use Amitriptyline.

What side effects can it cause?

When prescribing the drug, the doctor always focuses on the potential side effects of Amitriptyline and asks the patient to be more attentive to possible manifestations of the reaction. When the following symptoms appear, most often they simply reduce the dosage to gradually get used to the patient or cancel the drug if they feel too unwell.

The most common side effects are urination disorders, the appearance of dry mouth, some decrease in vision, an increase in intraocular pressure, constipation, intestinal obstruction of a functional type, hyperthermia - an increase in body temperature.

In addition to these adverse reactions, the patient may complain of the following conditions:

• Increased fatigue, weakness.
• Sleepy state.
• Confused consciousness.
• Increased irritability.
• Nightmares.
• Insomnia.
• hallucinations.
• Distractedness, impaired attention.
• Trembling of limbs.
• Disorder of coordination of movements (ataxia).
• Feeling of crawling, tingling, sensory disturbances (paresthesia).
• Hair loss.
• Itching of the skin and mucous membranes.
• Hives.
• Purpura (small hemorrhages in the skin and mucous membranes).
• Enlarged lymph nodes.
• The secretion of milk from the mammary glands in non-lactating and non-pregnant women, as well as in men - galactorrhea.
• Potency disorders.
• Swelling of the testicles.
• Decreased or increased sexual desire.
• Diarrhea.
• Jaundice.
• Increased activity of liver enzymes.
• Nausea, vomiting.
• Pain and discomfort in the epigastric region.
• Anorexia.
• Changing the color of the tongue.
• Stomatitis.

Such a significant number of potential side effects means that the patient needs to be closely monitored for changes in their condition, especially when increasing the dosage of the drug. All negative manifestations should be reported to the attending physician in order to make a decision to reduce the dosage or to cancel the drug and switch to another drug.

Signs and dangers of overdose

When taking Amitriptyline, there is a risk of overdose, but its manifestations are related to the amount of the drug taken and may manifest differently in patients of different age, gender and health status.

It is believed that taking the drug more than 500 mg in adult patients leads to the appearance of signs of moderate or severe levels. A dose of 1200 mg or more is lethal. In children, extremely serious conditions and death can be caused by a much smaller amount of medicine.

Patients may respond differently to high doses of the drug. In some, the symptoms increase slowly, gradually, while others react immediately and violently.

The following manifestations of overdose are mainly noted:

1. Convulsions, seizures, loss of consciousness, which can turn into a coma, severe depression of the central nervous system, impaired functioning of the respiratory center.
2. Increased body temperature, drying of the mucous membranes, urinary retention, tachycardia (rapid heartbeat), dilated pupils (mydriasis), problems with intestinal motility (slowdown).
3. With a significant overdose, the patient has an increasing pulse rate, pressure may drop, intraventricular blockade, cardiac arrest may develop.

More information about antidepressants can be found in the video:

If symptoms of an overdose are present, Amitriptyline should be discontinued and appropriate measures taken. Physostigmine is administered intramuscularly or intravenously at a dosage of 1–3 mg every one to two hours.

It is necessary to introduce solutions to maintain electrolyte balance, equalize blood pressure indicators, and eliminate other symptoms of overdose. The patient remains under medical supervision for at least 5 days, it is necessary to monitor cardiac activity, as unexpected deviations are possible, since there is a risk of manifestation of intoxication and disruption of the heart within 2 days after an overdose.

Interaction with other drugs

When treating with the drug, it is necessary to take into account not only the side effects of Amitriptyline, but also its possible interactions with other drugs. This drug when taking MAO inhibitors can cause the so-called serotonin syndrome. At the same time, do not prescribe decongestants, painkillers and other drugs containing epinephrine, ephedrine and related substances.

Simultaneous use with antihistamines can enhance their action, which leads to the suppression of the normal functioning of the central nervous system. When using Amitriptyline, even without other drugs, it is not recommended to drive vehicles and use complex and dangerous devices and devices.

Co-administration of neuroleptics, antiarrhythmic drugs, antihistamines with Amitriptyline can provoke ventricular arrhythmia. Tachycardia can be provoked by the use of antifungal agents.

Barbiturates can cause a decrease in the effectiveness of the drug.

There are quite a few different dangerous combinations of Amitriptyline with other drugs, which only once again emphasizes the exceptional danger of self-administration of such a complex drug. When talking with a doctor, it is imperative to fully list all the medicines that are taken by the patient and can enter into a negative reaction with the antidepressant.

Antidepressant

Active substance

Amitriptyline (amitriptyline)

Release form, composition and packaging

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

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

Tablets from white to white with a slightly yellowish tint, flat-cylindrical shape, with a chamfer and a risk; light marbling is allowed.

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

10 pieces. - cellular contour packings (1) - packs of cardboard.
10 pieces. - cellular contour packings (2) - packs of cardboard.
10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - cellular contour packings (4) - packs of cardboard.
10 pieces. - cellular contour packings (5) - packs of cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.

pharmachologic effect

Antidepressant (tricyclic antidepressant). It also has some analgesic (of central origin), antiserotonin effect, helps to eliminate bedwetting and reduces appetite.

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

It has the properties of a class IA antiarrhythmic drug, like quinidine in therapeutic doses, slows down ventricular conduction (with an overdose, it can cause severe intraventricular blockade).

The mechanism of antidepressant action is associated with an increase in the concentration and / or serotonin in the central nervous system (CNS) (decrease in their reabsorption).

The accumulation of these neurotransmitters occurs as a result of inhibition of their reuptake by the membranes of presynaptic neurons. With prolonged use, it reduces the functional activity of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed during depressive states. In anxiety-depressive conditions, it reduces anxiety, agitation and depressive manifestations.

The mechanism of antiulcer action is due to the ability to have a sedative and m-anticholinergic effect. Efficacy in bedwetting appears to be due to anticholinergic activity resulting in increased bladder distensibility, direct beta-adrenergic stimulation, alpha-adrenergic agonist activity with increased sphincter tone, and central reuptake blockade. It has a central analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and the effect on endogenous opioid systems.

The mechanism of action in bulimia nervosa is unclear (may be similar to that in depression). A clear effect of the drug on bulimia in patients both without depression and in its presence is shown, while a decrease in bulimia can be observed without a concomitant weakening of the depression itself.

During general anesthesia, it lowers blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).

Antidepressant action develops within 2-3 weeks after the start of use.

Pharmacokinetics

Absorption is high.

The bioavailability of amitriptyline is 30-60%, its active metabolite nortriptyline is 46-70%. The time to reach C max after ingestion is 2.0-7.7 hours. V d 5-10 l / kg. Effective therapeutic blood concentrations for amitriptyline are 50-250 ng/ml, for nortriptyline 50-150 ng/ml.

Cmax 0.04-0.16 µg/ml. Passes (including nortriptyline) through histohematic barriers, including the blood-brain barrier, placental barrier, penetrates into breast milk. Communication with proteins - 96%.

Metabolized in the liver with the participation of isoenzymes CYP2C19, CYP2D6, has the effect of "first pass" (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. T 1/2 from blood plasma - 10-26 hours for amitriptyline and 18-44 hours for nortriptyline. Excreted by the kidneys (mainly in the form of metabolites) - 80% in 2 weeks, partly with bile.

Indications

Depression (especially with anxiety, agitation and sleep disturbances, including in childhood, endogenous, involutional, reactive, neurotic, drug, with organic brain damage).

As part of complex therapy, it is used for mixed emotional disorders, psychosis in schizophrenia, alcohol withdrawal, behavioral disorders (activity and attention), nocturnal enuresis (with the exception of patients with hypotension of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical pain in the face, postherpetic neuralgia, posttraumatic neuropathy, diabetic or other peripheral neuropathy), headache, migraine (prevention), peptic ulcer of the stomach and duodenum.

Contraindications

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

Carefully. Amitriptyline should be used with caution in people with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, depression of bone marrow hematopoiesis, diseases of the cardiovascular system (CVS) (angina pectoris, arrhythmia, heart block, chronic insufficiency, myocardial infarction, arterial hypertension), intraocular hypertension, stroke, decreased motor function of the gastrointestinal tract (GIT) (risk of paralytic ileus), liver and / or kidney failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, urinary hypotension bladder, during pregnancy (especially the first trimester), in old age.

Dosage

Assign inside, without chewing, immediately after eating (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 / 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 in schizophrenia and alcohol withdrawal, a dose of 25-100 mg / day is prescribed. (at night), after achieving a therapeutic effect, they switch to the minimum effective dose - 10-50 mg / 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 / day. (the maximum part of the dose is taken at night).

Children

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

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

Side effects

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

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

From the CCC: tachycardia, palpitations, dizziness, orthostatic hypotension, non-specific changes in the electrocardiogram (ECG) (S-T interval or T wave) in patients without heart disease; arrhythmia, lability of blood pressure (decrease or increase in blood pressure), impaired intraventricular conduction (expansion of the QRS complex, changes in the P-Q interval, blockade of the legs of the His bundle).

From the gastrointestinal tract: nausea, heartburn, gastralgia, hepatitis (including liver dysfunction and cholestatic jaundice), vomiting, increase in appetite and body weight or decrease in appetite and body weight, stomatitis, change in taste, diarrhea, darkening of the tongue.

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

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

With prolonged treatment, especially at high doses, with its abrupt cessation, it is possible development of withdrawal syndrome: nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual agitation; with gradual cancellation after long-term treatment - irritability, restlessness, sleep disturbances, unusual dreams.

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

Overdose

Symptoms.

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

From the CCC: decrease in blood pressure, tachycardia, arrhythmia, impaired intracardiac conduction, ECG changes (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, hyperthermia, mydriasis, increased sweating, oliguria or anuria.

Symptoms develop 4 hours after an overdose, reach a maximum after 24 hours and last 4-6 days. If an overdose is suspected, especially in children, the patient should be hospitalized.

Treatment: when taken orally: gastric lavage, activated charcoal; symptomatic and supportive therapy; with severe anticholinergic effects (lowering blood pressure, arrhythmia, coma, myoclonic epileptic seizures) - the introduction of cholinesterase inhibitors (the use of physostigmine is not recommended due to an increased risk of seizures); maintenance of blood pressure and water and electrolyte balance. Showing the control of CCC functions (including ECG) for 5 days (relapse may occur after 48 hours and later), anticonvulsant therapy, artificial lung ventilation (ALV), and other resuscitation measures. Hemodialysis and forced diuresis are ineffective.

drug interaction

With the combined use of ethanol and drugs that depress the central nervous system (including other antidepressants, barbiturates, benzodiazepines and general anesthetics), a significant increase in the inhibitory effect on the central nervous system, respiratory depression and hypotensive effect is possible. Increases sensitivity to drinks containing ethanol.

Increases the anticholinergic effect of drugs with anticholinergic activity (for example, phenothiazine derivatives, antiparkinsonian drugs, amantadine, biperidene, antihistamine drugs), which increases the risk of side effects (from the CNS, vision, intestines and bladder). When used together with anticholinergics, phenothiazine derivatives and benzodiazepines - mutual enhancement of sedative and central anticholinergic effects and increased risk of epileptic seizures (lowering the threshold of convulsive activity); phenothiazine derivatives, in addition, may increase the risk of neuroleptic malignant syndrome.

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.

When combined with antihistamine drugs, clonidine - increased inhibitory effect on the central nervous system; with atropine - increases the risk of paralytic ileus; with drugs that cause extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.

With the simultaneous use of amitriptyline and indirect (coumarin or indadione derivatives), an increase in the anticoagulant activity of the latter is possible. Amitriptyline may increase depression caused by glucocorticosteroids (GCS). Medicines for the treatment of thyrotoxicosis increase the risk of developing agranulocytosis. Reduces the effectiveness of phenytoin and alpha-blockers.

Inhibitors of microsomal oxidation (cimetidine) lengthen T 1/2, increase the risk of developing toxic effects of amitriptyline (a dose reduction of 20-30% may be required), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce plasma concentration and reduce the effectiveness of amitriptyline.

Combined use with disulfiram and other inhibitors of acetaldehyderogenase provokes delirium.

Fluoxetine and fluvoxamine increase plasma concentrations of amitriptyline (a dose reduction of amitriptyline by 50% may be required).

With the simultaneous use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa, a decrease in the hypotensive effect of the latter; with cocaine - the risk of developing cardiac arrhythmias.

Antiarrhythmic drugs (such as quinidine) increase the risk of developing rhythm disturbances (possibly slowing down the metabolism of amitriptyline).

Pimozide and probucol can increase cardiac arrhythmias, which is manifested in the prolongation of the Q-T interval on the ECG.

Enhances the effect of epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine on the CCC (including when these drugs are part of local anesthetics) and increases the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.

When co-administered with alpha-agonists for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictive effect of the latter may be enhanced.

When taken together with thyroid hormones - mutual enhancement of the therapeutic effect and toxic effects (include cardiac arrhythmias and a stimulating effect on the central nervous system).

M-anticholinergics and antipsychotic drugs (neuroleptics) increase the risk of developing hyperpyrexia (especially in hot weather).

When co-administered with other hematotoxic drugs, hematotoxicity may increase.

Incompatible with MAO inhibitors (possible increase in the frequency of periods of hyperpyrexia, severe convulsions, hypertensive crises and death of the patient).

special instructions

Before starting treatment, control of blood pressure is necessary (in patients with low or labile blood pressure, it may decrease even more); during the period of treatment - control of peripheral blood (in some cases, agranulocytosis may develop, and therefore it is recommended to monitor the blood picture, especially with an increase in body temperature, the development of flu-like symptoms and tonsillitis), with long-term therapy - control of CCC and liver functions. In the elderly and patients with cardiovascular disease, monitoring of heart rate, blood pressure, ECG is indicated. Clinically insignificant changes may appear on the ECG (smoothing of the T wave, depression of the S-T segment, expansion of the QRS complex).

Care must be taken when abruptly moving to a vertical position from a lying or sitting position.

During the period of treatment, the use of ethanol should be excluded.

Assign no earlier than 14 days after the abolition of MAO inhibitors, starting with small doses.

With a sudden cessation of administration after long-term treatment, the development of a "withdrawal" syndrome is possible.

Amitriptyline in doses above 150 mg / day. reduces the threshold for seizure activity (the risk of epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors predisposing to the occurrence of a convulsive syndrome, for example, brain damage of any etiology, the simultaneous use of antipsychotic drugs (neuroleptics), during the period of refusal of ethanol or discontinuation of drugs with anticonvulsant properties, such as benzodiazepines). Severe depressions are characterized by the risk of suicidal actions, which may persist until a significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or antipsychotic drugs and constant medical supervision (entrust trusted persons with the storage and issuance of drugs) may be indicated. In children, adolescents, and young people (under 24 years of age) with depression and other psychiatric disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients, the risk of suicide should be correlated with the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, and slightly decreased in people over 65 years of age. During treatment with antidepressants, all patients should be monitored for early detection of suicidal tendencies.

In patients with cyclic affective disorders during the depressive phase during therapy, manic or hypomanic states may develop (dose reduction or withdrawal of the drug and the appointment of an antipsychotic drug are necessary). After the relief of these conditions, if there are indications, treatment at low doses can be resumed.

Due to possible cardiotoxic effects, caution is required when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.

In combination with electroconvulsive therapy, it is prescribed only under the condition of careful medical supervision.

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

May cause paralytic ileus, mainly in patients with chronic constipation, 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.

Due to the anticholinergic effect, a decrease in lacrimation and a relative increase in the amount of mucus in the composition of the lacrimal fluid are possible, which can lead to damage to the corneal epithelium in patients using contact lenses.

With prolonged use, there is an increase in the incidence of dental caries. The need for riboflavin may be increased.

Animal reproduction studies have shown adverse effects on the fetus, and there are no adequate and well-controlled studies in pregnant women. In pregnant women, the drug should be used only if the intended benefit to the mother outweighs the potential risk to the fetus.

Children are more sensitive to acute overdose, which should be considered dangerous and potentially fatal for 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.

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 withdrawn at least 7 weeks before the expected birth.

Application in childhood

Contraindicated in children under 6 years of age.

In children, adolescents, and young people (under 24 years of age) with depression and other psychiatric disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients, the risk of suicide should be correlated with the benefits of their use.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

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

Shelf life - 3 years. Do not use after the expiration date.

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 it on a par with haloperidol, and this is a serious antipsychotic 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.