Amitriptyline is a popular drug in psychiatry. It combines the antidepressant, hypnotic and anti-anxiety effects recommended by the World Health Organization. But, in addition to the therapeutic effect, many side effects of amitriptyline have been recorded, which requires a detailed study of this drug.
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Description of the dosage form, composition
Today, this tricyclic antidepressant is available in the form of a dragee with the amount of active substance - amitriptyline hydrochloride - from 10 to 75 mg. The tablets are packed in a plastic bottle, the coating is light pink. When breaking the dragee, the inner layer of a yellowish tint is visible. The drug also includes additional components - sucrose, lactose, calcium stearate, corn starch, gelatin, white opadra - the main component of the dense coating of Amitriptyline tablets.
The second possible form of release is capsules. The outer gelatin shell is reddish brown. Auxiliary components: shellac, talc, sucrose, titanium dioxide, povidone, stearic acid.
The last form, used mainly in acute manifestations of depressive disorders, is a solution (1%) in 2 ml ampoules. Externally completely transparent liquid without sediment or subsequent discoloration. Additional components: injection water, glucose. Amitriptyline injections can be administered intramuscularly, or drip therapy (intravenously) is used.
Side effects and contraindications of amitriptyline
The principle of action of amitriptyline is the reuptake of neurotransmitters such as dopamine, norepinephrine, mainly serotonin, which are responsible for a depressed person. This provides a calming, anti-anxiety, sedative effect. Along with this, amitriptyline exhibits anticholinergic activity, which is the reason for a large number of side effects.
To reduce the possible negative effect, at the beginning of therapy it is necessary to gradually increase the dose, and in the end, gradually abandon the drug.
The following symptoms are associated with anticholinergic effects:
- problems with urination, up to atony of the bladder;
- violation of visual function (blurry and defocused image near, photosensitivity);
- constipation, which without the necessary treatment develops into acute bowel obstruction or paralysis;
- dilated pupils, agitation, a feeling similar to intoxication, apathy (due to sedation, especially at high doses), lethargy;
- delirium (blurred consciousness, attention, perception, emotions) - mainly in elderly patients;
- anticholinergic syndrome is extremely rare.
Other side effects include the following conditions:
- disturbances in the perception of taste, dyspeptic disorders, constant hunger;
- allergy development;
- change in blood composition: thrombocytopenia (platelet deficiency), leukopenia (lack of white blood cells in plasma), eosinophilia (decreased concentration of eosinophils), hyponatremia (decrease in the number of Na ions), fluctuations in sugar level;
- lowering blood pressure, tachycardia, other heart rhythm disorders, orthostatic collapse (problems with blood flow to the brain when changing body position, darkening in the eyes, dizziness or loss of consciousness);
- disturbances in the liver;
- in gynecology - decreased libido, potency, anorgasmia, gynecomastia (hypertrophic enlargement of the mammary glands), galactorrhea (spontaneous leakage of milk from the breast), ejaculation disorders;
- in neurology - extrapyramidal syndromes (spontaneous involuntary contractions of individual muscles), ataxia (inconsistency in skeletal muscle tension), neuropathy (mainly peripheral, manifested as increased sensitivity of the limbs, tingling or numbness of the hands, feet), dysarthria (pronunciation problems due to pronunciation restrictions on the supply of a nerve impulse to the organs of speech);
- in psychiatry - mania, hypermania (typical for patients with thyroid dysfunction, affective or schizoaffective disorders), hallucinations, depersonalization.
In patients with epilepsy undergoing amitriptyline therapy, seizures from taking a small amount of an antidepressant can occur, which also applies to patients with craniocerebral injuries. In people without contraindications, convulsions appear when large doses are administered intravenously.
An important side effect is aggravation of suicidal tendencies with an increase in the initial dose. Because of this, it is recommended to start taking the drug in small quantities and only in the evening, gradually the dose can be increased by adding receptions in the morning and afternoon. In acute manifestations of suicidal ideation amid depression, treatment must begin in a hospital setting.
The likelihood of suicide increases in the presence of the following diseases:
- astheno-depressive syndrome;
- depression with self-incriminating acts;
- depersonalization.
Amitriptyline is able to affect the speed of reaction and perception, so during therapy it is not recommended to drive or perform complex work that requires significant concentration and is life threatening due to inattention.
The tool is contraindicated in such pathologies:
- cardiovascular diseases: severe hypertension, decompensated heart disease, recovery from a heart attack;
- ulcers of the intestine and stomach, pyloric stenosis (insufficient size of the hole between the stomach and duodenum);
- glaucoma;
- atony (paralysis) of the bladder or intestines;
- pregnancy;
- manic phase;
- age up to 12 years;
- dysfunction of the prostate gland.
Drug addiction
In some countries (for example, in Ukraine), amitriptyline is banned and listed as a substance. This is due to the fact that patients, having experienced a temporary retreat of the symptoms of depression, can independently increase the dose to obtain a permanent effect. Impact on the central nervous system (central nervous system), in which there is a feeling of relaxation, some "slowing down" of consciousness, lead to the fact that the patient can additionally drink a double or triple dose to cause a feeling of euphoria.
Some of the side effects are perceived as the first signs of drug addiction, but they are not: tremor of the palms (involuntary trembling), dilated pupils, irritability, temper, photosensitivity, intoxication.
There is also some physical dependence on the drug - when taken from 1 month, the body develops a persistent addiction to an antidepressant, and a sharp cessation of treatment can be reflected in the form of withdrawal. But this property is characteristic of many drugs, especially for drugs of a similar nature and other drugs, the course of treatment of which exceeds 3-5 months.
Possible effects of alcohol intake
The principle of action of amitriptyline and alcohol is partially similar - there is a "inhibition" of the central nervous system. But when used together, these substances increase the degree of exposure to the body. As a result, severe intoxication occurs against the background of severe side effects of an antidepressant or signs of an overdose.
The most common symptoms are severe abdominal pain, vomiting, stool disorders, stomatitis, and a change in taste perception.
The load on the heart increases due to serious violations of its rhythm, which, under the influence of elevated temperature, nervous excitement, can lead to a stroke or heart attack.
The liver wears out quickly - the main metabolic reactions occur in it, including the processing of alcohol toxins and medications. The risk of developing toxic necrosis is increased.
The kidneys excrete metabolites of amitriptyline and ethyl alcohol, which, in turn, also increases the load on them. Therefore, violations of the function of the excretory system, including the appearance of acute renal failure (acute renal failure), are possible.
Other symptoms include clouding of consciousness, disorientation, hallucinations, uneven breathing, increased sweating, rash, redness, or other allergic reactions.
In case of unintentional combination of Amitriptyline and ethyl alcohol, the patient must immediately rinse the stomach and take a means to remove toxins (the most common option is activated charcoal). Next - to carry out rehabilitation in a hospital under the guidance of an experienced specialist.
Contraindications during pregnancy and lactation
Amitriptyline is not prescribed during pregnancy due to the ability to influence the development of the fetus, except in situations where another alternative is not available. Studies have shown that a child after childbirth may experience pathological drowsiness, irritability, tearfulness, and sometimes there are problems with urination. This effect is due to exposure to one of the metabolites of the substance - nortriptyline.
During lactation, this antidepressant is also not prescribed, although there is no specific data on the harmful effects on the newborn during breastfeeding.No more than 2% of the daily dose taken by the mother can enter the body of the child, which can manifest as drowsiness. Therefore, treatment with Amitriptyline for lactation is not prohibited, but in this case it is recommended to carefully monitor the condition of the child, especially in the first 4 weeks of life.
Amitriptyline withdrawal syndrome
Cancellation syndrome is a pathological condition that occurs when a drug is abruptly abandoned, especially with prolonged use.
This is a body reaction to a support substance that can cause the following symptoms:
- dizziness, headache attacks, photosensitivity, tinnitus;
- insomnia, nightmares;
- dyspeptic disorders, decreased salivation;
- disturbances in the emotional state, panic;
- bradycardia (slow heart rate), tachycardia (increased heart rate).
Symptomatic therapy of withdrawal syndrome is recommended: taking sedatives, preferably on a plant basis, cleansing the body, restoring electrolyte balance, consulting a gastroenterologist to get rid of gastrointestinal tract disorders, taking antihypertensive drugs (to even out the heart rate), as additional strengthening procedures - physiotherapy, massage, oxygen therapy, etc. In cases of acute panic attacks, the occurrence of suicidal ideas will require a reception antipsychotics.
The best preventive action for Amitriptyline withdrawal syndrome is a gradual rejection of the drug, minimizing stress and other harmful factors for the patient’s health.
Instructions for use
The main principle on which the appointment of Amitriptyline is based is to gradually increase the daily dose of the drug to prevent the occurrence of side effects.
The initial dose is 50-75 mg of the active substance. Every day, it is recommended to add 25-50 mg. The standard dose at which the build-up is stopped is 150-250 mg (up to 300 mg if the patient has a severe form of depression).
Vulnerable groups of patients (elderly, adolescents, people undergoing primary treatment) and patients with mild depression may not increase the dose so quickly, for example, adding 25 mg to the previous amount every 2-3 days.
In the presence of diseases requiring a quick result, it is possible to start therapy with higher rates, for example, 100 mg of the substance per day, but treatment must be carried out in a hospital.
If tolerance of the drug allows, it is possible to prescribe 400-450 mg of amitriptyline, but only under the strict supervision of the attending physician.
It is recommended to increase the dose by taking it in the evening. The tablets are taken with meals, washed down with a sufficient amount of liquid, preferably plain water.
In severe depressive conditions, injections (intramuscularly) or drip (intravenously) are prescribed. Gradually replaced with tablets.
Patients after 55 and adolescents begin treatment with lower doses and increase them more slowly, with the exception of acute depressive disorders.
The effect of the drug is noticeable 2-4 weeks after reaching the "working" (150-200 mg) dose.
In order to avoid withdrawal syndrome, a gradual decrease in the amount of the drug taken is necessary at the same rate with which the increase took place.
The course of treatment is not recommended for longer than 6-8 months.
Amitriptyline is the most popular tricyclic antidepressant used to treat depressive disorders of varying severity. Despite the relatively easy perception of the drug by the body, there is a long list of contraindications and special instructions that must be taken into account when prescribing and taking the drug. And in no case should you self-medicate with the help of this variety of drugs.
