From the author: Amitriptyline reviews forum. Instructions for use of the drug. Pharmacies. Added patient reviews from 2013 to 2019-2020. An essay in which the author shares his own experience of using good old Amitriptyline. In case of anxiety. For depression. For insomnia, BAR. In children. With enuresis. With pathological menopause. For OCD, stress, PTSD, pregnancy, breastfeeding. Price. Added reviews from patients who took Amitriptyline. Withdrawal syndrome. My comments on them—November, 2018. Help from a psychiatrist in Moscow. Search for an alternative to Amitriptyline. The other day (September 2013) I had a conversation with one “advanced” Internet user, and also my patient. The essence of the question: the doctor prescribes Amitriptyline to the patient, but he refuses. Because... I read “a lot of bad things” about this drug on the Internet: the drug is old, discontinued in other countries and only dense, backward Russia, in which, Unfortunately, the patient was born and uses this medicine for his offspring. When the doctor asked him to indicate the author of the “bad words about Amitriptyline,” the patient was unable to answer. The doctor’s subsequent dissuasions had no effect—this patient trusts the Internet (virtual guru) more than his attending physician. By the way, my patient (who visits the doctor only to write out a prescription for the next Internet-approved sleeping pill) has been for more than ten years unsuccessfully “treated” by the virtual community; and without any chance (in my opinion) of recovery. What real effect does Amitriptyline have? What can a patient hope for and what should he fear? 1) Amitriptyline (belonging to the group of tricyclic antidepressants) is indeed “older” than its fellow selective serotonin reuptake inhibitors (SSRIs). 2) The main advantage of Amitriptyline is that the sedative effect of the drug is realized immediately! No accumulation effect. What does this do in the clinic? The fact that Amitriptyline is able to stop a panic attack or anxiety syndrome is, as they say, “on the needle.” I have repeatedly observed this: today the patient is shaking with anxiety, and the next day, after taking the medicine for the first time, he is already a “living person” capable of adequately perceiving reality. Similarly, Amitriptyline is able to restore a person’s healthy sleep within a day (!). And the completely opposite effect is observed with SSRIs: in the first three to four days, anxiety only intensifies, sometimes reaching the level of a panic attack. My attempts to prescribe SSRIs at night, those that are marketed by manufacturers as “sedatives,” resulted in severe anxiety for the patient and worsening of his insomnia. The result of such prescriptions was the patient’s categorical refusal to be treated with a “sedative” drug from the SSRI group or to be treated by SUCH a doctor at all! 3) In outpatient practice, small dosages of the drug are usually prescribed. More often, “quarter” tablets (25 mg) four times a day. A short-acting drug. 4) Of the main disadvantages that led to the discontinuation of the drug, I will note the same pronounced sedative effect (disadvantages, as is known, are just a continuation of the advantages). Sedation, in particularly sensitive patients, caused daytime drowsiness, which was the reason for discontinuation of the drug. Another common side effect of Amitriptyline is dry mouth (dry mucous membranes). It must be said that these side effects are dose-dependent. Those. directly depend on the dosage of the drug: if you take small doses of the medicine, then side effects will not manifest themselves. 5) There are (as without them) contraindications to prescribing Amitriptyline. I won’t talk about them in detail, because... The doctor’s task is to take into account all possible contraindications when prescribing medicine (the patient does not need to think about this).-------------------------------------------------- -------------------------------------------------- ----------- The instructions for Amitriptyline are given below: International nonproprietary name: amitriptyline Chemical rational name: 5-(3-dimethylaminopropylidene)-10,11-dihydrodibenzocycloheptene. Composition: 1 tablet contains Active substance: amitriptyline hydrochloride 11.3 mg and 28.3 mg Excipients: propylene glycol, magnesium stearate, povidone, titanium dioxide, hypromellose, talc, microcrystalline cellulose, potato starch, lactose monohydrate. Dosage form: film-coated tablets Description: Round, biconvex tablets, white film-coated colors. Pharmacotherapeutic group: Antidepressant. ATC code: N06AA09 Pharmacological properties: 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 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 the effect on endogenous opioid systems. It has pronounced peripheral and central anticholinergic action due to 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 have a sedative and m-anticholinergic effect (for peptic ulcers stomach and duodenum reduces pain, helps accelerate the healing of ulcers). The effectiveness of bedwetting is apparently due to anticholinergic activity, leading to an increase in the ability of the bladder to stretch, direct β-adrenergic stimulation, and the activity of α-adrenergic receptor agonists, 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 weakening of the depression itself. During general anesthesia, it reduces blood pressure and body temperature. Does not inhibit MAO. Pharmacodynamics: The mechanism of the antidepressant action of amitriptyline is associated with inhibition of the reverse neuronal uptake of catecholamines (norepinephrine, dopamine and serotonin) into the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and periphery, and is therefore one of the most potent tricyclic antidepressants in this regard. It also has antihistamine and antiadrenergic properties. Pharmacokinetics: When administered orally, amitriptyline reaches peak plasma concentrations within 4-8 hours. Its bioavailability ranges from 33 to 62%. Because amitriptyline slows gastrointestinal transit time, absorption may be delayed, especially in overdose. When administered intramuscularly, peak plasma concentrations are higher and reached earlier. Effective blood concentrations of amitriptyline and nortriptyline (its active metabolite) average from 120 to 240 ng/ml. Concentrationamitriptyline in tissues is higher than in plasma, where 92% is associated with proteins. Metabolized in the liver, the plasma half-life is 10 to 28 hours for amitriptyline and 16 to 80 hours for nortriptyline. It is excreted mainly in urine. Complete elimination within 7 days. Amitriptyline crosses the placental barrier and is excreted in breast milk in concentrations similar to plasma concentrations. Indications for use: Use strictly as prescribed by a doctor. Depression of any etiology. It is especially effective for anxiety and depression due to the severity of the sedative effect. Does not cause exacerbation of productive symptoms (delusions, hallucinations), unlike antidepressants with a stimulating effect. Mixed emotional disorders and behavioral disorders, phobic disorders. Childhood enuresis (except for children with a hypotonic bladder). Psychogenic anorexia, bulimic neurosis. Neurogenic pain of chronic nature, for the prevention of migraine. Contraindications: Decompensated heart defects. Acute and recovery period of myocardial infarction. Cardiac muscle conduction disorders. Stage 3 hypertension. Acute liver and kidney diseases, with severe dysfunction. Blood diseases. Peptic ulcer of the stomach and duodenum in the acute stage. Glaucoma. Prostate hypertrophy. Atony of the bladder. Pyloric stenosis, paralytic ileus. Simultaneous treatment with MAO inhibitors. Pregnancy, breastfeeding. Children under 6 years of age (injectable forms up to 12 years of age). Hypersensitivity to amitriptyline. With caution: chronic alcoholism, bronchial asthma, manic-depressive psychosis, cardiovascular diseases (angina pectoris, arrhythmia, heart block, CHF, myocardial infarction, arterial hypertension), stroke, liver and/or kidney failure, thyrotoxicosis, urinary retention, bladder hypotension , schizophrenia (possible activation of psychosis), epilepsy, old age. Method of administration and doses: Prescribed orally (during or after meals), intramuscularly or intravenously. 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 achieved. 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/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 dosages under the control of the somatic condition (on average 10-30 mg up to 4 times a day, but not more than 150 mg /day). After obtaining a persistent 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 (max) in divided doses or 1 time per day at night. Children as an antidepressant: 6-12 years old, orally 10-30 mg (1-5 mg/kg) per day in 2 divided doses; over 12 years of age (12-18 years), orally 10 mg 3 times a day and 20 mg at bedtime, if necessary, and taking into account tolerance, the dose is increased to 100 mg per day in divided doses or once before bedtime. For the prevention of migraines, chronic neurogenic pain (including long-term headaches) from 12.5-25 mg to 100 mg/day. Interaction with other drugs: Amitriptyline potentiates the inhibition of the central nervous system by the following drugs: antipsychotics, sedatives and hypnotics, anticonvulsants, central and narcotic analgesics, drugs for generalanesthesia, alcohol. When combined with amitriptyline and antipsychotics and/or anticholinergic drugs, a febrile temperature reaction and paralytic intestinal obstruction may occur. Amitriptyline potentiates the hypertensive effects of catecholamines, but inhibits the effects of drugs affecting the release of norepinephrine. Amitriptyline may reduce the antihypertensive effect of sympatholytics (octadine, guanethidine and drugs with a similar mechanism of action). When taking amitriptyline and cimetidine simultaneously, the plasma concentration of amitriptyline may increase. Concomitant use of amitriptyline with MAO inhibitors can be fatal. The break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days! Pimozide and probucol can increase cardiac arrhythmias, which is manifested by prolongation of the P-T interval on the ECG. It enhances the effect of epinephrine, norepinephrine, isoprenatine, ephedrine and phenylephrine on the cardiovascular system (including when these drugs are part of local anesthetics) and increases the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension. Parenteral use is possible only in a hospital setting, under the supervision of a physician, with bed rest in the first days of therapy. Caution is required when suddenly moving to a vertical position from a lying or sitting position. During the treatment period, the use of ethanol should be avoided. Prescribed no earlier than 14 days after discontinuation of MAO inhibitors. starting with small doses. If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop. Amitriptyline in doses above 150 mg/day reduces the threshold of convulsive 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 convulsive syndrome, for example, brain damage of any etiology, simultaneous use of antipsychotic drugs (neuroleptics) , during the period of refusal of ethanol or withdrawal of drugs with anticonvulsant properties, such as benzodiazepines). Severe depression is characterized by a risk of suicidal actions, which can persist until 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 (entrusting the storage and dispensing of drugs to trusted persons) may be indicated. In patients with cyclical affective disorders, manic or hypomanic symptoms may develop during the depressive phase during therapy. Special instructions: Before starting treatment, blood pressure monitoring is necessary (in patients with low or labile blood pressure, it may decrease even more); during the treatment period - 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, development of flu-like symptoms and sore throat), during long-term therapy - control of the functions of the cardiovascular system and liver. In the elderly and patients with cardiovascular diseases, monitoring of heart rate, blood pressure, and ECG is indicated. Clinically insignificant changes may appear on the ECG (smoothing of the T wave, depression of the ST segment, widening of the QRS complex). Caution is required when suddenly moving to a vertical position from a lying or sitting position. During the treatment period, the use of ethanol should be avoided. If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop. Severe depression is characterized by a risk of suicidal actions, which can persist until 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 (entrusting the storage and dispensing of drugs to trusted persons) may be indicated. In combination with electroconvulsive therapy, it is prescribed only under the condition of careful medical supervision. (BeforeWhen performing general or local anesthesia, the anesthesiologist should be warned that the patient is taking amitriptyline.) Due to the anticholinergic effect, there may be a decrease in tear production and a relative increase in the amount of mucus in the tear fluid, which can lead to damage to the corneal epithelium in patients using contact lenses. With long-term use, an increase in the incidence of dental caries is observed. The need for riboflavin may be increased. Side effects: Mainly associated with the anticholinergic effect of the drug, disturbance of accommodation, increased intraocular pressure, dry mouth, stool retention, intestinal obstruction, urinary retention, increased body temperature, drowsiness. All these phenomena usually disappear after adaptation to the drug or dose reduction. From the cardiovascular system: tachycardia, arrhythmias, orthostatic arterial hypotension. From the gastrointestinal tract: nausea, vomiting, anorexia, stomatitis, taste disturbances, discomfort in the epigastrium, rarely liver dysfunction. From the endocrine system: gynecomastia, galactorrhea, changes in ADH secretion, decreased libido, potency. Other: agranulocytosis and other blood changes, skin rash, hair loss, swollen lymph nodes, weight gain with long-term use. Amitriptyline in doses above 150 mg/day reduces the threshold for seizure activity, so the risk of seizures should be taken into account in patients with a history of seizures, and in those patients who are predisposed to this due to age or injury. Treatment with amitriptyline in old age should be carried out under careful somatic control and with the use of minimal doses of the drug, increasing them gradually, in order to avoid the development of delirious disorders, hypomania and other complications. Patients with the depressive phase of MDP may progress to the manic phase. Anticholinergic effects: blurred vision, paralysis of accommodation, mydriasis, increased intraocular pressure (only in those with a local anatomical predisposition - a narrow anterior chamber angle), tachycardia, dry mouth, confusion, delirium or hallucinations, constipation, paralytic ileus, difficulty urinating , decreased sweating. From the nervous system: drowsiness, asthenia, fainting, anxiety, disorientation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, agitation, motor restlessness, manic state, hypomanic state, aggressiveness, memory impairment, depersonalization , increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, asthenia; activation of symptoms of psychosis; headache, myoclonus; dysarthria, tremor of small muscles, especially the arms, hands, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus; ataxia, extrapyramidal syndrome, increased frequency and intensification of epileptic seizures; changes on the EEG. From the cardiovascular system: tachycardia, palpitations, dizziness, orthostatic hypotension, nonspecific changes on the ECG (ST interval or T wave) in patients who do not suffer from heart disease; arrhythmia, blood pressure lability (decrease or increase in blood pressure), intraventricular conduction disturbances (widening of the QRS complex, changes in the PQ interval, bundle branch block). From the digestive system: nausea, rarely - hepatitis (including impaired liver function and cholestatic jaundice), heartburn, vomiting, change in taste, diarrhea, darkening of the tongue. From the endocrine system: increase in size (swelling) of the testicles, gynecomastia; increase in the size of the mammary glands, galactorrhea; decreased or increased libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inappropriate ADH secretion. From the hematopoietic organs: agranulocytosis, leukopenia, thrombocytopenia, purpura.eosinophilia. Allergic reactions: skin rash, skin itching, urticaria, photosensitivity, swelling of the face and tongue. Other: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urinary retention, pollakiuria, hypoproteinemia. Withdrawal symptoms: in case of sudden withdrawal after long-term treatment - nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual agitation; with gradual withdrawal after long-term treatment - irritability, restlessness. sleep disorders. unusual dreams. The connection with taking the drug has not been established: lupus-like syndrome (migratory arthritis, the appearance of antinuclear antibodies and positive rheumatoid factor), liver dysfunction, ageusia, gastralgia, increased appetite and body weight or decreased appetite and body weight, stomatitis. Driving is prohibited while taking amitriptyline. servicing mechanisms and other types of work that require increased concentration. Overdose: Drowsiness, disorientation, confusion, dilated pupils, increased body temperature, shortness of breath, dysarthria, agitation, hallucinations, seizures, muscle rigidity, suppuration, coma, vomiting, arrhythmia, hypotension, heart failure, respiratory depression. Helpful measures: discontinuation of amitriptyline therapy, gastric lavage, fluid infusion, administration of physostigmine 1-3 mg every 1/2-2 hours IM or IV (for children, administration of physostigmine begins with 0.5 mg, then the dose is repeated with 5- minute interval to determine the minimum effective dose, but not more than 2 mg), physostigmine should be used only in patients in a coma, with respiratory depression, epileptic seizures, severe hypotension and severe cardiac arrhythmia; symptomatic therapy, maintaining 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. Release form: 50 tablets in a dark glass bottle, sealed with a polypropylene screw cap, under which there is a gasket with a tear ring, ensuring control of the first opening. Part of the label is attached to the bottle with a special adhesive tape, which allows the label to be lifted. Instructions for use are made in the form of a folding sheet placed under the movable part of the label. Storage conditions: List B. Store at a temperature of 15° -25°C, out of the reach of children. Shelf life: 5 years. Do not use after the expiration date indicated on the packaging! Conditions for dispensing from pharmacies According to a doctor's prescription. -------------------------------------------------- -------------------------------------------------- -------------November, 2018: I will comment on the patient’s review and questions on the forum: “..., A year ago I went to see a psychiatrist because of depression. At that time it manifested itself in a depressed mood, apathy and problems with sleep. The psychiatrist hardly spoke to me. He listened to my complaints and prescribed Amitriptyline. After a while, I began to have problems with concentration and thinking, my sleep improved slightly, although I also fell asleep poorly and woke up exhausted, but slept for 6 hours. -8 hours. Two months ago I stopped taking antidepressants, but I didn’t think better. Today I went to the psychiatrist again. I complained about problems with attention, thinking, and absent-mindedness. He prescribed Amitriptyline again, but he changed the regimen. Questions two. 1. above the problem be a consequence of treatment with Amitriptyline? 2. Is there any point in contacting another psychiatrist? Maybe with similar symptoms you need to contact a neurologist? ... "(end of quote). 1) Of course, it is necessary to study the patient's case in detail in order to treat him effectively. 2) My opinion is that changing the Amitriptyline dosage regimen will not give the patient anything. 3) The sedative effect of Amitriptyline will further increase The patient's problems with concentration and other cognitive difficulties 4) Indeed, not clear.prognosis for this therapy—what exactly does the attending physician want to achieve? Spontaneous remission? Lifelong drug remission? 5) I believe this is the case when the medical homeopathic method can serve as the method of choice! By ensuring detailed attention to the patient's symptoms and selection of the most appropriate homeopathic medicine. 6) “Neurologist”—a specialist in working with sectional material; pathologist. The medical specialty is called “neurologist.” Neurologists do not have proper qualifications in psychiatry and psychopharmacotherapy!************** **************************************** ********************************* Question from a patient taking Amitriptyline; 2019 Psychiatric workshop. “Are feelings dulled? taking antidepressants? Can taking amitriptyline, for example, dull feelings such as pain or, conversely, happiness? Today I read an article about how antidepressants can block emotional attraction to the opposite sex. Is this so?" Of course! Any therapy with psychotropic drugs, including Amitriptyline, is primarily sedative and suppressive in nature. The main target: anxiety and depression. But other human emotions also come under “heavy artillery fire”! Hence the slang expression among patients : “I was like a vegetable.” Psychiatric workshop. Case from the forum, December, 2019. “I, too, have had migraines all my life, I’ve been on anticonvulsants and Teraligen for a year now. Plus now Mexidol, sermion. I take half a tablet of amitriptyline at night. Triptans cannot be taken with antidepressants. Have they been canceled for you completely? I’m already going to Botox, I’m tired of taking so many pills. The blockade of the trigeminal nerve was done according to compulsory medical insurance, but it did not help." Such a difficult situation. On the one hand, suppression of the symptom, on the other hand, a sharp increase in the drug disease with a combination of suppressive drugs! Will botulinum toxin have an effect?! It’s difficult to say: it will be better, it will be worse, no effect .Eco-friendly option: homeopathic treatment from a doctor. Continuation of the workshop. Review-commentary from open sources; 2020; according to the manner of presentation, “Hello! Amitriptyline is a good, proven pain reliever for chronic headache. It is taken 10–25 mg 1–3 times a day. But, unfortunately, you are already on a very high dose. A side effect of high doses can also be headache. On the contrary, have you tried reducing the dose? Amitriptyline can be supplemented with Fluoxetine, Duloxetine, Gabapentin, Neurontin. The doctor usually prescribes his favorite one. But do not forget about the cross-effects of side effects from these drugs. What will work for you is, unfortunately, determined by trial and error. Try it with your doctor. Have you considered physical therapy? It helps well as a distraction." My comment. 1) CGTH is a chronic tension headache. I've never heard of "acute tension headache." Funny. The usual diagnosis is tension headache; that's all. 2) "The doctor usually prescribes his beloved." - That’s what I’m writing about: an allopathic doctor has a “favorite remedy” that he will prescribe for me, you, him, her, everyone. What kind of “personalized medicine” is there?! Sad.3) Really , the more drugs, the more possible combinations of toxic effects and the less control of treatment. And of course, what kind of evidence-based medicine can we talk about in this case - if the combinations are activated arbitrarily and do not use monotherapy. 4) Physiotherapy as a distracting remedy!! ! Horrible! Obviously the doctor is not familiar with the targets of physiotherapy and its capabilities ********************************. **************************************** ************** Conclusion: The tricyclic antidepressant Amitriptyline is included in the Unified Register of Medicines approved for use in the Russian Federation. Accordingly, the use of Amitriptyline is legal and recommended. Therefore, all the talk about “good and bad antidepressants” is just rumors and fiction. It's another matter if.