Treatment of depression symptoms, especially those in which the patient requires tranquility.
Composition:
1 tabl powl. contains 10 mg or 25 mg of Amitriptyline hydrochloride.
Action:
A tricyclic antidepressant. The exact mechanism of action of the drug is unknown. It is probably related to the intensity of synaptic transmission within the brain's adrenergic and serotoninergic neurons as a result of suppression of reabsorption and inactivation of noradrenaline and serotonin in the endings of these neurons, which leads to increased concentration of these neurotransmitters in the inter-synaptic space. The sedative effect of amitriptyline is probably due to its antihistamine properties. Following oral administration, amitriptyline is well absorbed from the gastrointestinal tract, reaching a maximum blood concentration of about 2-12 hours after administration (the presence of food does not affect absorption). Bioavailability is 30-60% and is associated with a significant first pass effect of the liver. In about 92-95%, the drug binds to plasma proteins (mainly to all-1-glycoproteins). Metabolized in the liver, the main active metabolite is nortriptyline, whose maximum concentration in the blood occurs within 8-24 h after drug administration. In about 7-10% of the population there is a genetic defect consisting in the weakening of CYP2D6 activity - in these patients a significant (even 8-fold) increase in AUC is observed. The drug is mainly excreted in the urine. T0,5 amitriptyline in the blood is 10-50 h (average about 19 h), and its active metabolite - nortriptyline - 20-100 h. The drug penetrates the blood-brain barrier, the placenta and into breast milk.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients or to benzodiazepines. Fresh myocardial infarction, atrioventricular conduction abnormalities, arrhythmia, angina pectoris. Manic arousal condition. Severe hepatic failure. Porphyria. Use during treatment and within 2 weeks after discontinuing MAO inhibitors. Breastfeeding period. Children and youth under 16 years.
Precautions:
Depression is associated with an increased risk of suicidal thoughts, self-mutilation and suicide. This risk persists until full remission is achieved. Patients should be closely monitored until improvement occurs and at an early stage of recovery (increased risk of suicide). Patients with a history of suicide-related events or patients exhibiting a significant degree of suicidal ideation prior to commencement of treatment are considered to be at increased risk of suicidal thoughts or attempts and should be closely monitored during treatment, particularly in patients below 25 years of age. During treatment, especially at the beginning and in the case of dose changes, patients should be closely monitored, particularly those at high risk. Patients with bipolar disorder may experience an increase in manic phase when treated with amitriptyline. In patients with schizophrenia, symptoms of this disease may become more severe; it is also possible that paranoid symptoms increase. Due to its cholinolytic effect, amitriptyline should be used with caution in patients with prostatic hyperplasia (the possibility of increased difficulty in passing urine), in patients with closed-angle glaucoma (possible increase in intraocular pressure) and in patients with a slow gastrointestinal passage. Patients with epilepsy may get worse during epilepsy; use of amitriptyline in this group of patients may require an increase in the amount of antiepileptic medication being taken. When high doses are used, cardiac arrhythmias, tachycardia and a significant reduction in blood pressure may occur; in patients with heart disease, similar disorders may occur after the usual doses. The preparation should be used with caution in patients with hepatic impairment.The effect of amitriptyline is more strongly expressed in patients with hyperthyroidism and in patients treated with thyroid hormones - the preparation is used with caution in these patients by adjusting the individual doses. In patients who are to undergo surgery, amitriptyline should be discontinued a few days before surgery. If the procedure has to be carried out suddenly, please inform your anesthetist if you are taking amitriptyline. During treatment with Amitriptyline, electroconvulsive therapy is not recommended. Special care should be taken and risk-related benefits should be considered when amitriptyline is used in patients with alcoholism (possibility of increased inhibition of o.u.n. activity); with blood disorders (the possibility of aggravation of these disorders); with asthma (the possibility of worsening asthma); with urinary retention.
Pregnancy and lactation:
Amitriptyline is not recommended in pregnant women, especially in the first and third trimester, due to the lack of sufficient clinical data on safety during this period. The preparation can be used during pregnancy only in cases when the benefit for the mother outweighs the potential risk to the fetus. The use of the drug during breast-feeding is contraindicated.
Side effects:
Frequency unknown: decreased salivation and associated dry mouth, increased teeth caries, constipation, paralytic ileus, nausea, vomiting, epigastric pain, stomatitis, dark tongue, unpleasant feeling (metallic or acidic) taste in the mouth, loose stools, swollen salivary glands, excessive sweating, alopecia, skin eruptions, urticaria, photodermatosis, accommodation disorders, mydriasis, increased intraocular pressure, visual disturbances, difficulty urinating (especially in men), frequent urge for urine, increase or decrease in blood pressure, increase or decrease in serum Glucose, weight loss or weight gain, changes in EEG, orthostatic hypotension, tachycardia, palpitations, myocardial infarction, arrhythmia, atrial conduction disorders, ischemic stroke, concentration disorders, drowsiness, psychomotor agitation, numbness, tingling sensations and limb paresthesia, peripheral neuropathy, ataxia, muscular tremor, generalized seizures, coma, involuntary and tardive dyskinesias, speech disorders, headache and dizziness, confusion disorientation, hallucinations, mild manic status, insomnia, anxiety, anxiety, nightmares, tinnitus, tiredness, weakness, swelling of face and tongue, bone marrow failure (manifested by agranulocytosis, leukopenia, eosinophilia, thrombocytopenia and hemorrhagic purpura), hepatitis, cholestatic jaundice, swollen testicles, gynecomastia, menstrual disorders, breast engorgement and milkweed in women, weakness or increased sex drive, impotence, disorders of antidiuretic hormone secretion (Schwartz-Bartter syndrome), insufficient or excessive appetite. Epidemiological studies, mainly in patients aged 50 and older, have shown an increased risk of bone fractures in patients treated with selective serotonin reuptake inhibitors and tricyclic antidepressants; the mechanism that increases this risk is unknown. In elderly patients, the risk of adverse reactions associated with the cholinolytic properties is increased. There have been reports of cases of suicidal thoughts and behavior during treatment with amitriptyline and also shortly after its discontinuation. Abrupt discontinuation of treatment, especially after prolonged use, may cause withdrawal symptoms: insomnia, irritability, nausea, headache and excessive sweating; in individual cases, the appearance of symptoms of hypomania or mania was observed in the first week after discontinuation of treatment.
Dosage:
Orally. Adults and adolescents over 16 years of age: treatment should be initiated at a dose of 50-100 mg / day, given as a single dose or as divided doses per night. The doses should then be increased gradually until efficacy is obtained; the maximum dose used in outpatient treatment is 200 mg / day. After clinical improvement, the dose should be gradually reduced to the lowest effective maintenance dose (usually 50-100 mg / day).The preparation is used in divided doses (2-4 times a day) or in a single dose, given due to the sedative-hypnotic effect usually in the evening (50-100 mg per night).Special groups of patients. In patients over 65 years of age, the treatment should start at a dose of 25-75 mg / day. Doses should be increased with caution and under strict medical supervision. The therapeutic effect can be obtained in this group of patients after doses lower by half than those used in younger age groups. The drug is not recommended for use in children and adolescents under 16 years due to the lack of sufficient data on efficacy and safety.Method of administration. The drug can be taken regardless of meals. If the dose to be used in a patient requires the need to divide the coated tablets, the use of 10 mg tablets should be considered. In order to reduce the likelihood of relapse, the recommended treatment period is 3 to 6 months.