Amitriptyline analogues are modern. Modern analogues of "amitriptyline", their comparison and reviews. Combination with other medications

Sooner or later, a modern person is faced with the need to purchase antidepressant drugs used in complex treatment for a depressed emotional state. Antidepressants are “called upon” to serve a person to elevate mood, create a positive emotional background, and ultimately.

When is a doctor's prescription required for antidepressants?

The dosage and daily regimen of medication is prescribed, of course, by the doctor. Only a qualified specialist will be able to assess the true state of your psyche, accurately calculate and schedule the dosage of medications. Compliance with the prescription when treating depression is one of the components of success in the fight against depression.

A prescription for purchasing antidepressant drugs is required only in the following cases:

• exacerbation of the disease;
• treatment of the most severe forms of depression;
• with an atypical form of the disease.

In this situation, the doctor prescribes monoamine oxidase inhibitors (MAOIs). These are potent antidepressant drugs that are used when other types are ineffective or have severe side effects.

The most effective in treating severe forms of depression are moclobemide, phenelzine, isocarboxazid and tranylcypromine.

Phenelzine, isocarboxazid and tranylcypromine are time-tested drugs, but have been used since the 50s of the 20th century and have many side effects. Moclobemide is a new generation medicine, with a faster effect and fewer associated negative reactions.

Mild antidepressants of a new generation. What's special?

A mild form of depression can be “corrected” with the help of drugs for which pharmacies do not require a prescription. New generation antidepressants, as a rule, do not cause as much harm to the body as drugs produced in the last century. Modern “over-the-counter” antidepressants are fundamentally different from heavy medications and drugs of the older generation.

Advantages of modern antidepressants:

1. faster effect on the body and elimination of depression;
2. fewer side effects;
3. possibility of simultaneous use with many other medications;
4. absence of significant addiction to the action of the drug.

Based on the effect the drugs have on a person’s mental state, antidepressants are distinguished between stimulating and sedative properties.

It is very important to accurately determine the nature of the disease and the subsequent correct choice of antidepressant medication (to stimulate or inhibit the central nervous system). The time and effectiveness of treatment largely depends on this.

List of mild antidepressants available without prescription (15 drugs)

Over-the-counter antidepressants are divided into different groups according to the degree and type of their effect. Let us list the main groups and the drugs included in them. Let's start the list by listing stimulant antidepressants.

1. Maprotiline

Drug name: Maprotiline.

Analogues: Ludiomil, Ladiomil, Flexyx.

Indications: endogenous, involutional, psychogenic and neurotic depression, exhaustion, somatogenic, latent, menopausal depression.

Action: reducing apathy, improving mood, relieving psychomotor retardation.

Side effects: headache, lethargy, drowsiness, hearing loss, hallucinations, tachycardia, arrhythmia, vomiting, nausea, dry mouth, urticaria, swelling, weight gain, sexual disorders, stomatitis.

Contraindications: epileptic disease, kidney disease, liver disease, pregnancy.

2. Prozac

Drug name: Prozac.

Analogues: Fluoxetine, Prodel, Profluzac, Fluval.

Indications: depression, bulimia nervosa, obsessive-compulsive disorder (obsessive thoughts and actions).

Action:

• relieves emotional overload and obsessive thoughts;
• will alleviate anorexia nervosa;
• eliminates premenstrual disorders;
• reduce anxiety and panic.

Side effects: at the beginning of treatment and when the dose is increased - anxiety, drowsiness, headache, nausea. Rarely – convulsions. Possible skin rashes, pain in muscles, joints, fever

Contraindications: hypersensitivity, pregnancy, lactation.

3. Paxil

Drug name: Paxil.

Analogues: Rexetine, Adepress, Actaparoxetine, Plizil, Paroxetine hydrochloride hemihydride, Sirestill.

Indications: depression of all types in adults and children 7-17 years old.

Action: in the first weeks of use, symptoms of depression decrease and suicidal thoughts are eliminated. Prevents relapses of depression.

Side effects: drowsiness, insomnia, loss of appetite, tachycardia, nausea, constipation, seizures, sweating.

Contraindications: hypersensitivity to paroxetine and the components of the drug. Pregnancy, lactation.

Drug name: Deprim.

Analogues: Gelarium hypericum, Doppel-Hertz Nervotonic.

Indications: chronic fatigue syndrome, depression, emotional exhaustion, decreased ability to work.

Action: increased performance, mental and physical activity, normalization of sleep.

Side effects: dry mouth, changes in the gastrointestinal tract, fatigue.

Contraindications: children under 6 years old. Individual intolerance. It should be taken with special caution during pregnancy and lactation.

Along with medications of chemical origin, herbal preparations can be taken to combat depression. Antidepressants of herbal etiology are herbal infusions that can be purchased at a pharmacy or prepared at home.

5. Leuzea extract

Drug name: Leuzea extract (Raponticum safflower).

Indications: as a complex therapy.

Action: general tonic effect, increased performance, improved mood, increased appetite .

Side effects: headache, irritability, increased blood pressure, allergic reaction, insomnia.

Contraindications: hypersensitivity, epilepsy, chronic sleep disorders, acute period of infectious diseases.

6. Ginseng tincture

Drug name: Ginseng tincture.

Indications: hypotension, increased fatigue, overwork.

Action: increased performance, decreased fatigue, increased blood pressure.

Side effects: insomnia, headache, diarrhea, nausea, nosebleeds.

Contraindications: hypertension, children under 16 years of age, hyperfunction of the thyroid gland.

7. Schisandra tincture

Drug name: Schisandra tincture.

Indications: hypotension, neurasthenia, depression.

Action: stimulating the central nervous system, increasing blood pressure, improving visual acuity.

Side effects: overexcitation of the central nervous and cardiovascular systems.

Contraindications: insomnia, high blood pressure, acute infectious diseases.

Let's take a closer look at the class of sedative antidepressants.

8. Azafen

Drug name: Azafen.

Indications: asthenodepressive syndrome, anxiety-depressive state, alcoholic depression, endogenous depression, exogenous depression, depressive states in chronic somatic diseases.

Action: elimination of anxiety and depression, manifestations of senile depression, smoothing out the negative state caused by long-term use of antipsychotics.

Side effects: nausea, vomiting, headache, dizziness.

Contraindications: hypersensitivity, myocardial infarction, coronary heart disease, diabetes mellitus, pregnancy, acute infectious diseases.

9. Persen

Drug name: Persen.

Indications: poor sleep, irritability, increased nervous excitability.

Action: sedative and antispasmodic effect.

Side effects: allergic reaction. With prolonged use - constipation.

Contraindications: hypersensitivity to the components of the drug, arterial hypotension. Children under 3 years old (tablets), children under 12 years old (capsules)

10. Mianserin

Drug name: Mianserin.

Indications: Depression of various origins.

Action: improved sleep, decreased nervous excitability.

Side effects: drowsiness, hypokinesia, convulsions.

Contraindications: manic syndrome, pregnancy, lactation, childhood (up to 18 years). Liver and kidney failure.

11. Amitriptyline

Drug name: Amitriptyline.

Indications: manic-depressive psychosis, bulimia nervosa, childhood enuresis.

Action: sedative effect, antidiuretic effect for bedwetting, analgesic effect.

Side effects: drowsiness, disorientation, excitability, hallucinations, fatigue, tachycardia, nausea, vomiting, weight gain.

Contraindications: epilepsy, intestinal obstruction, angle-closure glaucoma, pregnancy, breastfeeding.

12. Mirtazapine

Drug name: Mirtazapine.

Indications: depressive states, early awakening from sleep, loss of interest, anxious depression.

Action: restoring the ability to enjoy, adjusting sleep, eliminating suicidal thoughts.

Side effects: drowsiness, dizziness, unusual dreams, tachycardia, nausea, diarrhea, decreased libido, dry mouth, increased appetite.

Contraindications: hypersensitivity to the components of the drug, epilepsy, organic brain damage.

13. Novo-passit

Drug name: Novo-passit.

Indications: neurasthenia, “manager” syndrome, migraine, eczema of psychological etiology.

Action: sedative, relieving nervous excitability of the premenstrual and menopausal periods, eliminating anxiety.

Side effects: allergic reactions, dizziness, drowsiness, slight decrease in muscle tone.

Contraindications: hypersensitivity to the components of the drug, children (up to 12 years), alcoholism, epilepsy, diseases, brain injuries.

14. Hawthorn tincture

Drug name: Hawthorn tincture.

Indications: nervousness, cardiovascular diseases, menopause, high cholesterol.

Action: calming effect on the nervous system, normalization of heart activity, reduction of excitability during menopause.

Side effects: allergic reactions, itching, urticaria.

Contraindications: pregnancy, lactation period, individual intolerance, children under 12 years of age.

15. Valerian tincture

Drug name: Valerian tincture.

Indications: insomnia, migraine, hysteria, increased excitability, smooth muscle spasms.

Action: calming, antispasmodic, choleretic, normalizing effect for the gastrointestinal tract.

Side effects: decreased performance, drowsiness, depression.

Contraindications: individual intolerance.

Contraindications for over-the-counter antidepressants

Antidepressants sold without a prescription have a beneficial effect on the elimination of neurotic conditions of various etiologies. But this does not mean at all that you can take these drugs for a very long time and without negative consequences.

Many antidepressant medications that are freely available in pharmacies may have a number of contraindications.

These “prohibitions” apply to almost all antidepressants:

• individual intolerance to the components of the drug;
• pregnancy;
• breastfeeding period;
• children under 18 years of age.

It must be said that each drug with antidepressant action, along with the contraindications listed above, may also have its own, unique to this medicine.

If you are in doubt about whether or not to take antidepressants, watch a video that will enlighten you and destroy a number of myths about drugs of this kind:

Constant stressful situations and the very fast pace of modern life lead to many people becoming overly irritable, nervous, and susceptible to various types of phobias. Depressive conditions, unfortunately, have ceased to be something unique and isolated.

Nowadays, even young children are familiar with the term “depression.”

The chemical composition and clinical use of these drugs may vary. The search for new pharmacological compounds to combat depression in medical science does not stop.

The first medications to combat depression began to be prescribed to patients in the 50s of the 20th century. The drug iproniazid is at the origins of antidepressants. Currently, there are about 125 drugs with antidepressant effects in pharmacology. Be careful when choosing antidepressants!

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

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

Amitriptyline tablets - indications for use

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

Amitriptyline - side effects, contraindications and complications

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

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

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

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

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

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

Amitriptyline - reviews from patients and psychotherapists

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

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

Amitriptyline - analogues

Psychological exercises to combat depression and neurotic manifestations

I was prescribed Amitriptyline for depression, which became chronic and was accompanied not only by insomnia, but also by panic attacks. The drug had to be taken simultaneously with Phenibut, which eliminated the side effects of Amitriptyline. I did not observe any side effects during the entire treatment period, despite the fact that the therapy lasted three months. I would like to note that already... I was prescribed Amitriptyline for depression, which became chronic and was accompanied not only by insomnia, but also by panic attacks. The drug had to be taken simultaneously with Phenibut, which eliminated the side effects of Amitriptyline.
I did not observe any side effects during the entire treatment period, despite the fact that the therapy lasted three months. I would like to note that within a month my emotional state improved significantly, my sleep patterns even normalized, which had not happened for a very long time. The drug is very effective, but potent - it can lead to you sleeping for 12 hours at night. and then during the day it makes you sleepy.
To avoid drowsiness in the second and third months of treatment, I already took 1/4 of the dose of Amitriptyline, instead of 1/2. The condition was still good.

One tablet of amitriptyline made my eyes run wild in the morning, movement became simply impossible, everything was swimming before my eyes, terrible dizziness, nausea... use this drug with great caution

But amitriptyline helped me very well, seemingly without side effects, but when I tried Neurofulol. I felt at that moment that after all, this is an expensive medicine, it’s not for nothing that it’s expensive, it’s a completely different remedy, and the depression has passed, and there’s no addiction (I can not drink it for a week) And most importantly... But amitriptyline helped me very well, seemingly without side effects, but when I tried Neurofulol. I felt at that moment that after all, it’s an expensive medicine, it’s not for nothing that it’s expensive, it’s a completely different remedy, and the depression has passed, and there’s no addiction (I can not drink it for a week) And most importantly, I don’t have a headache, I don’t feel nauseous, I feel good, I’m cheerful I feel myself!

I took amitriptyline for depression for quite a long time, I thought that it would help, but I thought so in vain, I got tired of waiting and went to the doctor, he said that this drug was not for me. So you had to drink so much and wait to hear it (((Prescribed Neurofulol.

I took the tablets as prescribed by a neurologist. There were no side effects. My sleep was restored, and most importantly, my arms don’t hurt at night. I sleep very well.

A very good remedy, not a hypnotic, not inhibitory like other sedatives. And you don’t need to drink them all the time, but only when there is a need for it. It relieves feelings of resentment, anxiety, etc. very well. I bought it back in 2000, 50 tablets per package and still... A very good remedy, not a hypnotic, not inhibitory like other sedatives. And you don’t need to drink them all the time, but only when there is a need for it. It relieves feelings of resentment, anxiety, etc. very well. I bought it back in 2000, 50 tablets per pack, and I still have it to this day. I only use it when I really need it. And there are no side effects and no need to invent them. Think better about what the side effect is.

Amitriptyline is a terrible drug. I experienced everything myself. People, it’s better to look for another drug, albeit more expensive, but safer. The doctor prescribed it for me for depression. Side effects began - everything was swimming in the eyes, I might not recognize my acquaintances on the street, terrible drowsiness and this is just a few of the described effects. It was like I was in some... Amitriptyline is a terrible drug. I experienced everything myself. People, it’s better to look for another drug, albeit more expensive, but safer.
The doctor prescribed it for me for depression. Side effects began - everything was swimming in the eyes, I might not recognize my acquaintances on the street, terrible drowsiness and this is just a few of the described effects. I was like in some kind of dream, everything was so colorful and bright. This is probably what drug addicts see when they take a dose. I'm afraid to imagine what I looked like from the outside. I decided to reduce the dosage, but the pain and all the other symptoms of depression returned.
In general, it was some kind of nightmare, it became even worse than before using Amitriptyline. And you need to quit it gradually, fortunately, the doctor suggested this to me. Otherwise I don’t know what would have happened. It is better not to take this remedy. Take care of your health!!!

Of course, everything is individual. It works well for one person, but for another, such side effects will appear that mother, don’t worry. But here you see, this is how I think. When doctors prescribe medications for treatment, they don’t know what hereditary diseases we have, for example, or maybe we ourselves don’t really know, maybe we... Of course, everything is individual. It works well for one person, but for another, such side effects will appear that mother, don’t worry. But here you see, this is how I think. When doctors prescribe medications for treatment, they don’t know what hereditary diseases we have, for example, or we ourselves may not really know, maybe this drug is not suitable for us due to contraindications. And to identify personal contraindications, you need to do a lot of tests. And when the doctor prescribes tests for us, we say - what a rip-off, just to prescribe unnecessary tests in order to rip off more money.
And then we start taking such tablets, capsules, etc. Here is the result. For some it’s ok, for others it’s bad. I went to see a therapist because of constant headaches. He referred me to a neurologist. The result is vegetative-vascular dystonia against the background of depressive exacerbation... You can imagine my shock when I heard such a diagnosis. Well, what should I do? They prescribed me a comprehensive treatment. One of the prescribed drugs was Amitriptyline. I read the instructions, it says to take it under the supervision of a doctor, which means that the drug is very serious. The price of Amitriptyline is about 10 hryvnia, so I bought it and started taking it as indicated in the prescription. After 2 days of taking the drug, I started having nightmares, to the point where I woke up from my own scream... I went again to the same neurologist, told about my abnormal sleep at night, to which he replied that this means you there is such a side effect, we will cancel it... What kind of PPC is this? Those. pills for depression, but for going crazy. Horror.

There are contraindications. Before starting use, consult your doctor.

Commercial names abroad (abroad) - Domical, Elatrolet, Elavil, Eliwel, Endep, Equilibrin, Laroxyl, Lentizol, Neurarmonil, Novoprotect, Saroten, Sarotex, Triptyl, Tryptanol, Tryptine, Tryptizol, Tryptomer, Uxen.

All drugs used in neurology and psychiatry.

You can ask a question or leave a review about the medicine (please, do not forget to indicate the name of the drug in the text of the message).

Preparations containing Amitriptyline (Amitriptyline, ATC code N06AA09):

Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Country, manufacturer	Price in Moscow, r	Offers in Moscow
Amitriptyline	tablets 25mg	50	Different	12- (average 60) -72	439↘
Amitriptyline-Nycomed	tablets 10mg	50	Denmark, Nycomed	42- (average 49) -54	241↘
Amitriptyline-Nycomed	tablets 25mg	50	Denmark, Nycomed	18- (average 53) -63	172↘
Rarely encountered and discontinued release forms (less than 100 offerings in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Country, manufacturer	Price in Moscow, r	Offers in Moscow
Amitriptyline-Grindeks	tablets 10mg	50	Latvia, Grindeks	18- (average 44) -54	25↘
Amitriptyline	solution for intramuscular injection 20 mg in 2 ml	10	Russia, Moscow Endocrine Plant	36- (average 50↘) -52	9↘
Amitriptyline	tablets 10mg	50	Russia, ALSI	17- (average 25) -53	57↘
Amitriptyline-Acos	injection solution 10mg/ml 2ml	10	Russia, Synthesis	7- (average 42) -54	6
Amitriptyline-Grindeks	tablets 25mg	50	Latvia, Grindeks	31- (average 53) -60	50↗
Amitriptyline-Ferein	tablets 0.025g	50	Russia, Bryntsalov-A	25- (average 31) -33	3
Apo-Amitriptyline	tablets 10mg	50	Canada, Apotex	No	No
Vero-Amitriptyline	tablets 25mg	50	Russia, Veropharm	25-31	2↘
Saroten retard	capsules 50 mg	30	Denmark, Lundbeck	25-31	2↘
Amizol (Amyzol)	tablets 25mg	50 and 100	Slovenia, Lek	No	No

Amitriptyline - instructions for use. The drug is a prescription, the information is intended only for healthcare professionals!

Clinical and pharmacological group:

Antidepressant.

pharmachologic effect

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

The mechanism of the antidepressant action of amitriptyline is associated with inhibition of the reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin into the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and in the periphery, and has peripheral antihistamine (H1) and antiadrenergic properties. It also causes antineuralgic (central analgesic), antiulcer and antibulimic effects, and is effective for bedwetting.

The antidepressant effect develops within 2-4 weeks after the start of use.

Pharmacokinetics

Absorption is high. The time to reach Cmax after oral administration is 4-8 hours. The bioavailability of amitriptyline is from 33 to 62%, its active metabolite nortriptyline is 46-70%. Vd - 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. Cmax in blood plasma is 0.04-0.16 mcg/ml.

Passes through histohematological 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.

T1/2 - from 10 to 28 hours for amitriptyline and from 16 to 80 hours for nortriptyline.

Excreted by the kidneys - 80%, partially with bile. Complete elimination occurs within 7-14 days.

Amitriptyline crosses the placental barrier and is excreted into breast milk in concentrations similar to plasma concentrations.

Indications for use of the drug AMITRIPTILINE tablets

• depression of any etiology (due to the severity of the sedative effect, it is especially effective for anxiety and depressive conditions);
• mixed emotional and behavioral disorders;
• phobic disorders;
• childhood enuresis (except for children with a hypotonic bladder);
• psychogenic anorexia, bulimic neurosis;
• chronic pain syndrome (neurogenic);
• migraine prevention.

Dosage regimen

Prescribed orally (during or after meals).

The initial daily dose when taken orally is 50-75 mg (25 mg in 2-3 doses), then the dose is gradually increased by 25-50 mg until the desired antidepressant effect is obtained. The optimal daily therapeutic dose is 150-200 mg (the maximum dose is taken at night). For severe depression that is resistant to therapy, the dose is increased to 300 mg or more, to the maximum tolerated dose (the maximum dose for outpatients is 150 mg per day). In these cases, it is advisable to begin treatment with intramuscular or intravenous administration of the drug, using higher initial doses, accelerating the increase in dosage under the control of the somatic condition.

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

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

In elderly patients with mild disorders, in outpatient practice, doses are 25-50-100 mg maximum, in divided doses or 1 time per day at night.

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

Side effect

Mainly associated with the anticholinergic effect of the drug: accommodation paresis, blurred vision, increased intraocular pressure, dry mouth, constipation, intestinal obstruction, urinary retention, increased body temperature. All these phenomena usually disappear after adaptation to the drug or dose reduction.

From the central nervous system and peripheral nervous system: headache, ataxia, increased fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, disorientation, tremor , paresthesia, peripheral neuropathy, EEG changes; rarely - extrapyramidal disorders, seizures, anxiety.

From the cardiovascular system: tachycardia, arrhythmia, conduction disturbances, blood pressure lability, widening of the QRS complex on the ECG (intraventricular conduction disturbance), symptoms of heart failure, fainting.

From the digestive system: nausea, vomiting, heartburn, anorexia, stomatitis, taste disturbances, darkening of the tongue, discomfort in the epigastrium, gastralgia, increased activity of liver transaminases, rarely - cholestatic jaundice, diarrhea.

From the endocrine system: an increase in the size of the mammary glands in men and women, galactorrhea, changes in the secretion of antidiuretic hormone, changes in libido, potency; rarely - hypo- or hyperglycemia, glucosuria, impaired glucose tolerance, testicular swelling.

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

Other: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other blood changes, hair loss, swollen lymph nodes, weight gain with long-term use, sweating, pollakiuria.

With long-term treatment, especially in high doses, with abrupt cessation of treatment, withdrawal syndrome may develop: headache, nausea, vomiting, diarrhea, as well as irritability, sleep disturbance with vivid, unusual dreams, increased excitability.

Contraindications to the use of the drug AMITRIPTILINE tablets

• heart failure in the stage of decompensation;
• acute and recovery period of myocardial infarction;
• conduction disorders of the heart muscle;
• severe arterial hypertension;
• acute diseases of the liver and kidneys with severe dysfunction;
• peptic ulcer of the stomach and duodenum in the acute stage;
• prostatic hypertrophy;
• bladder atony;
• pyloric stenosis, paralytic ileus;
• simultaneous treatment with MAO inhibitors;
• pregnancy, breastfeeding period;
• children under 6 years of age;
• hypersensitivity to amitriptyline.

With caution: use in persons suffering from alcoholism, bronchial asthma, manic-depressive psychosis and epilepsy, suppression of bone marrow hematopoiesis, hyperthyroidism, angina pectoris and heart failure, angle-closure glaucoma, intraocular hypertension, schizophrenia (although when taking it there is usually no exacerbation of productive symptoms).

Use of the drug AMITRIPTILINE tablets during pregnancy and breastfeeding

Contraindication: pregnancy, breastfeeding period.

Use for liver dysfunction

The use of the drug is contraindicated in acute liver diseases with severe dysfunction.

Use for renal impairment

The use of the drug is contraindicated in acute kidney diseases with severe dysfunction.

Use in elderly patients

In elderly patients with mild disorders, in outpatient practice, doses are 25-50-100 mg maximum, in divided doses or 1 time per night.

Use in children

Contraindication: children under 6 years of age.

For enuresis, children over 6 years old - 12.5-25 mg at bedtime (the dose should not exceed 2.5 mg/kg of the child’s body weight).

special instructions

Amitriptyline in doses above 150 mg per day lowers the threshold for seizure activity, so the possibility of seizures should be considered in patients with a history of seizures and in patients who are predisposed to them due to age or injury.

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

Patients with the depressive phase of manic-depressive psychosis may progress to the manic phase.

While taking amitriptyline, drinking alcohol is prohibited.

Impact on the ability to drive vehicles and operate machinery

While taking amitriptyline, driving vehicles, servicing machinery and other types of work that require increased concentration are prohibited.

Overdose

Symptoms: drowsiness, disorientation, confusion, depression of consciousness up to coma, dilated pupils, increased body temperature, shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle rigidity, vomiting, arrhythmia, arterial hypotension, heart failure, respiratory depression.

Treatment: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Monitoring of cardiovascular activity (ECG) is indicated for 5 days, because relapse may occur within 48 hours or later.

Hemodialysis and forced diuresis are not very effective.

Drug interactions

Amitriptyline enhances the inhibitory effect on the central nervous system of the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; exhibits synergism when interacting with other antidepressants.

When amitriptyline is used together with neuroleptics and/or anticholinergic drugs, a febrile temperature reaction and paralytic intestinal obstruction may occur.

Amitriptyline potentiates the hypertensive effects of catecholamines and other adrenergic stimulants, which increases the risk of developing cardiac arrhythmias, tachycardia, and severe arterial hypertension, but inhibits the effects of drugs that affect the release of norepinephrine.

Amitriptyline may reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect of anticonvulsants.

With the simultaneous use of amitriptyline and anticoagulants - coumarin derivatives, it is possible to increase the anticoagulant activity of the latter.

When taking amitriptyline and cimetidine simultaneously, it is possible to increase the plasma concentration of amitriptyline with the possible development of toxic effects.

Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduce plasma concentrations of amitriptyline.

Amitriptyline enhances the effect of antiparkinsonian drugs and other drugs that cause extrapyramidal reactions. Quinidine slows down the metabolism of amitriptyline. Concomitant use of amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors may precipitate delirium.

Pimozide and probucol may increase cardiac arrhythmias.

Amitriptyline may enhance depression caused by corticosteroids.

When used together with drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases.

Concomitant use of amitriptyline with MAO inhibitors can be fatal. The treatment break between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days.

Conditions for dispensing from pharmacies

On prescription.

Storage conditions and periods

At a temperature of 15 to 25°C in a dry place, protected from light and out of reach of children. Shelf life - 4 years.

Amitriptyline is a classic tricyclic antidepressant. Suppresses 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 (eliminating anxiety) 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) opiateergic systems. The pronounced ability to bind to m-cholinergic receptors determines the powerful anticholinergic effect of Amitriptyline, and its ability to interact with histamine H1 receptors and block alpha-adrenergic receptors causes a sedative effect. It has an antiulcer effect, reduces the severity of pain in stomach and duodenal ulcers, and ensures rapid scarring of the ulcer. The above-mentioned anticholinergic activity of Amitriptyline, 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 transmitter serotonin by central neuronal synapses. Amitriptyline reduces bulimia nervosa both with and without comorbid depression. The antidepressant effect of the drug begins to clearly manifest itself 2-3 weeks after the start of drug therapy.

The bioavailability of Amitriptyline is about 50%, the half-life is 30-45 hours. Elimination from the body occurs through urine. The drug is available in tablet and ampoule form. Pharmacotherapy is started with a dose of 25-50 mg, the optimal time of administration is before bedtime. Gradually over the course of a week the dose is increased by 3-4 times. If there is no improvement in the condition in the second week, the daily dose is raised to 300 mg. Elimination of depressive symptoms is not a reason to refuse treatment: in this case, the dose is reduced to daily 50-100 mg and pharmacotherapy is continued for at least another three months. In elderly people with mild 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 move on to a maintenance daily dose of 250-50 mg. During treatment, it is necessary to avoid situations that require sudden standing up from a sitting or lying position. It is not recommended to abruptly interrupt treatment: in this case, 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 over 150 mg reduces the seizure threshold. When planning treatment, one should be aware of possible suicide attempts in patients suffering from severe depression. The combined use of Amitriptyline and electroconvulsive therapy is possible only with constant medical monitoring. In patients with a complicated medical history and the elderly, taking the drug can lead to the occurrence of pharmacological psychoses (after stopping drug therapy, such phenomena quickly disappear). Long-term use of Amitriptyline can lead to the development of caries. The drug is not compatible with alcohol.

Pharmacology

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

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

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

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

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

Efficacy for bedwetting appears to be due to anticholinergic activity leading to increased bladder distensibility, direct β-adrenergic stimulation, and α-adrenergic agonist activity accompanied by increased sphincter tone and central blockade of serotonin uptake.

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

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

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

Pharmacokinetics

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

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

Release form

10 pieces. - contour cell packaging (5) - cardboard packs.
50 pcs. - polymer jars (1) - cardboard packs.

Dosage

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

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

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

Interaction

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

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

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

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

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

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

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

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

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

Side effects

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

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

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

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

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

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

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

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

Indications

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

Contraindications

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

Features of application

Use during pregnancy and breastfeeding

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

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

In experimental studies, amitriptyline had a teratogenic effect.

Contraindicated during lactation. Excreted in breast milk and may cause drowsiness in nursing infants.

Use in children

Contraindication: children under 6 years of age (for oral administration), children under 12 years of age (for intramuscular and intravenous administration).

special instructions

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

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

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

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

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

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

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

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

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

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

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

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

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

Avoid drinking alcohol while taking amitriptyline.

Impact on the ability to drive vehicles and operate machinery

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