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Amitriptyline (Amitriptylinum, Amitriptylini) - tricyclic antidepressant group of non-selective inhibitors of neuronal uptake of monoamines. It possesses strong timoanalepticheskim and sedative effect.
The mechanism of antidepressant action of amitriptyline is associated with inhibition of reverse neuronal uptake of catecholamines (norepinephrine, dopamine) and serotonin in the central nervous system.
Amitriptyline is an antagonist of muscarinic cholinergic receptors in the CNS and in the periphery, has a peripheral antihistamine (H1) and antiadrenergic properties. Also of antinevralgicheskoe (central analgesic), anti-ulcer and antibulemicheskoe action effective for bedwetting.
The antidepressant effect develops within 2-4 weeks. after the start of application.
Amitriptyline should be used with caution in patients suffering from alcoholism persons with asthma, manic-depressive psychosis (MDP) and epilepsy (see. Special instructions), the oppression of bone marrow hematopoiesis, hyperthyroidism, angina and heart failure, angle-closure glaucoma, ocular hypertension, schizophrenia (although it usually happens reception exacerbation productive symptoms).
Amitriptyline in doses above 150 mg / day reduces the threshold for seizure activity, therefore it is necessary to take into account the possibility of seizures in patients with such a history, and that category of patients who are predisposed to it due to age or injury. amitriptyline in treatment of the elderly should take place under the close supervision and with the use of minimal doses, increasing them gradually in order to avoid the development of delirium disorders, hypomania, and other complications. Patients with depressive phase TIR can go to the manic phase. While receiving amitriptyline prohibited from driving vehicles sredst, machinery maintenance and other work requiring high concentration, and alcohol intake.
Assign inside (during or after eating). The initial daily dose ingestion of 50-75 mg (25 mg in 2-3 hours), and then gradually increase the dose of 25-50 mg, to obtain the desired anti-depressive effect. The optimum daily therapeutic dose is 150-200 mg (the maximum of the dose taken at night).
In severe depression resistant to treatment, increase the dose to 300 mg or more, up to the maximum tolerated dose (maximum dose for outpatients 150 mg / day). In these cases it is advisable to start treatment with intramuscular or intravenous injection, applying the higher initial dose, dose escalating accelerating under the control of the medical condition. Upon receipt of proof of antidepressant effect in 2-4 weeks the dose gradually and slowly reduced to 50-100 mg / day and continue treatment for at least 3 months. In the case of depression symptoms at lower doses need to go back to the previous dose.
If the patient's condition does not improve within 3-4 weeks of treatment, further treatment is not practical.
Mostly associated with anticholinergic effect of the drug: paresis of accommodation. Blurred vision, increased intraocular pressure, dry mouth, constipation, ileus, urinary retention, increase in body temperature. These effects usually disappear after adaptation to the drug or dose reduction.
CNS: headache, ataxia, fatigue, weakness, irritability, dizziness, tinnitus, drowsiness or insomnia, impaired concentration, nightmares, dysarthria, confusion, hallucinations, motor agitation, confusion, tremor, paresthesia, peripheral neuropathy, changes in the EEG. Rarely, extrapyramidal disorders, convulsions, anxiety.
Cardio-vascular system: tachycardia, arrhythmias, conduction disturbances, labile blood pressure, expansion of the QRS complex on the ECG (violation of intraventricular conduction), symptoms of heart failure, syncope.
On the part of the digestive tract: nausea, vomiting, heartburn, anorexia, stomatitis, taste disturbances, dark tongue, epigastric discomfort, gastralgia, increased activity of "liver" transaminases, rarely cholestatic jaundice, diarrhea.
From endocrine system: an increase in the size of the mammary glands in men and women, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), changes in libido, potency. Rare hypo- or hyperglycemia, glycosuria, glucose intolerance, swelling of the testicles. Allergic reactions: skin rash, pruritus, photosensitivity, angioedema, urticaria.
Other: agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura and other changes in the blood, hair loss, swollen lymph nodes, weight gain during prolonged use, sweating, pollakiuria. With prolonged treatment, especially in high doses, the sudden cessation of treatment may develop withdrawal symptoms: headache, nausea, vomiting, diarrhea, and irritability, sleep disturbance with bright, unusual dreams, irritability.
Amitriptyline dampening effect on the central nervous system following medicines: antipsychotics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; exhibits synergism when interacting with other antidepressants. In a joint application with amitriptyline neuroleptics, and / or anticholinergic drugs can cause febrile temperature reaction, paralytic ileus. Amitriptyline potentiates the hypertensive effects of catecholamines and other agonists that increases the risk of cardiac arrhythmias, tachycardia, severe hypertension, but inhibits the effects of drugs acting on the release of noradrenaline. 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 simultaneous use of amitriptyline and anticoagulants - coumarin derivatives or indandiona may increase the anticoagulant activity of the latter. At the same time taking amitriptyline and cimetidine may increase the plasma concentrations of amitriptyline with the possible development of toxic effects. Inductors of microsomal liver enzymes (barbiturates, carbamazepine) reduces plasma concentrations of amitriptyline. Amitriptyline increases the effects of anti-funds and other drugs that cause extrapyramidal reactions. Quinidine slows the metabolism of amitriptyline. The combined use of amitriptyline with disulfiram and other inhibitors of acetaldehyde dehydrogenase can cause delirium. Estrogensoderjath oral contraceptives may increase the bioavailability of amitriptyline; pimozide probucol and can enhance cardiac arrhythmias. Amitriptyline may enhance the depression caused by corticosteroids; concomitant use with medicinal products for the treatment of hyperthyroidism increases the risk of agranulocytosis. Simultaneous treatment with MAO inhibitors amitriptyline can be fatal. Break in treatment between receiving MAO inhibitors and tricyclic antidepressants should not be less than 14 days!
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