Trade names
Amizol. Amineurin. Amirol. Amiton. Amitriptyline. Amitriptyline hydrochloride. Apo-Amitriptyline. Probability Amitriptyline. Damilya maleinat. Novo-Triptin. Saroten. Saroten retard. Triptizol. Elivel.
Subgroup
Tricyclic antidepressant, a derivative dibenzotsiklogeptadina.
Action
* Antidepressive (developing within 2-3 weeks after starting treatment);
* Anxiolytic, sedative;
* Analgesic;
* Antidizuricheskoe (antidiureticheskoe);
* Antiholinergicheskoe (blocks m-choline receptors of central nervous system);
* Antihistaminic (gistaminovye blocks the receptors of central nervous system).
Mechanism of Action
Antidepressive effect of Amitriptyline is associated with adrenergic stimulation and serotoninergicheskih mechanisms in the brain by reverse neuronal capture of oppression mediators.
Antidiureticheskoe effect attributed antiholinergicheskoy activity.
Analgesic effect, which is associated with changes in the concentration monoanines in the central nervous system, especially serotonin, and the influence of Amitriptyline on the endogenous opioid system.
Pharmacokinetics
Rapidly and well absorbed from the ZHKT. Bioavailability Amitriptyline at different ways to the introduction of 30-61%, its metabolite - nortriptilina - 46-70%. The volume of distribution - 5-10 L / kg. Cmax in the blood after ingestion is achieved through 2,0-7,7 h. The therapeutic concentration in the blood for Amitriptyline - 50-250 ng / ml for nortriptilina - 50-150 ng / ml. Binding to plasma proteins was 82-96%.'s Easy to pass, as nortriptilin through gistogematicheskie barriers, including GEB, placental, penetrate into breast milk. T1 / 2 of 31-46 h.
Metabolized in the liver (demethylation, hydroxylation, N-oxidation) to form the active - nortriptilin, 10-hydroxy-Amitriptyline, and inactive metabolites. Derive mainly kidneys, mainly as metabolites, within a few days.
Indications
* Depressive syndrome (Depression: endogenous, involutional, reactive, neurotic, with organic brain damage, medical)
* Schizophrenic psychosis,
* Disturbing-depressive state of different genesis,
* Mixed emotional distress and breach of conduct,
* Psychogenic anorexia, bulimia;
* Night enuresis (excluding children with hypotonic bladder),
* Chronic pain syndrome.
Contraindications
* Hypersensitivity,
* Glaucoma,
* Hypertrophy of the prostate,
* Bladder atony,
* Paralytic ileus,
* Pilorostenoz,
* Epilepsy,
* The early recovery period after myocardial infarction,
* The use of MAO inhibitors in the preceding 2 weeks,
* Pregnancy, lactation,
* Children age (6 years).
Limitations to the use of
With careful use, with ischemic heart disease, arrhythmia, congestive heart failure.
Side Effects
From CNS: drowsiness, disorientation, excitation, hallucinations, ekstrapiramidnye disorders, dizziness, trembling, tremor, fatigue, rare - anxiety.
On the part of the cardiovascular system: tilt hypotension, tachycardia, hypertension, conduction, ECG changes (especially the QRS)
On the part of the digestive system: sour-bitter taste in the mouth, nausea, vomiting, stomatitis, rarely - cholestatic jaundice.
On the part of the reproductive system: potential violations, or delay ejaculation, reduction of potency, changes in libido.
From the Endocrine System: rare - hyperglycemia, glyukozuriya, violations of glucose tolerance, diabetes, syndrome of inappropriate secretion of ADG.
On the part of metabolism: an increase in body weight.
Allergic reactions: skin rash, itching.
Effects due to blockade of peripheral M-holinoretseptorov: dry mouth, disturbance of accommodation, poor vision, increased intraocular pressure, delayed urination, constipation, increased sweating.
Dependence syndrome and the abolition of
At the reception following the sudden cessation of long-term treatment may develop the syndrome cancel.
Interaction
With simultaneous application of Amitriptyline:
* With other drugs, have a depressing effect on the central nervous system, as well as the significant increase in ethanol may act on the central nervous system depressant, hypotensive action, oppression of breathing;
* With other drugs that have antiholinergicheskoy activity - strengthening antiholinergicheskih effects;
* A sympathomimetic means - may enhance their action on the cardiovascular system and increase the risk of heart rhythm irregularities, tachycardia, severe hypertension;
* With clonidine, guanetidinom - may reduce their antihypertensive effects;
* With barbiturates, carbamazepine - reducing the Amitriptyline because of its metabolism and reducing concentrations in the blood plasma;
* With quinidine - perhaps slowing metabolism Amitriptyline;
* With tsimetidinom - perhaps slowing metabolism Amitriptyline, increasing its concentration in blood plasma and the development of toxic effects.
Incompatible with MAO inhibitors.
Dosing and Administration in Adults
For admission into the starting dose is 25-50 mg per night (not razzhevyvaya, after meals). Then, within 5-6 days to increase the individual dose of 150-200 mg / day (most of the dose taken at night). If, during the second week did not come to improve, increasing the daily dose of 300 mg. With the disappearance of signs of depression, the dose is reduced to 50-100 mg / day and continue such therapy for at least 3 months.
V / m - initial dose of 50-100 mg / day in 2-4 introduction. If necessary, the dose can be gradually increased to 300 mg / day, in exceptional cases - up to 400 mg / day.
In old age, with light violations, which are treated with outpatient, dose is 50-100 mg / day, usually 1 time per day at night. The maximum dose for outpatient treatment - up to 150 mg / day in the hospital - up to 300 mg / d in elderly patients - up to 100 mg / day.
Dosing and Administration in pediatric practice
Children as antidepressant: 6 to 12 years - 10-30 mg or 1-5 mg / kg / d fractional, as a teenager - 10 mg 3 times a day (if necessary, up to 100 mg / day)
For the treatment of night enuresis for children under 6 years - 10 mg at night, 6-10 years - 10-20 mg / day, 11-16 years old - by 25-50 mg / day.
Pregnancy and lactation
Contraindicated in pregnancy, especially in I and III terms, except in cases of extreme necessity.
At the time of treatment should stop breastfeeding.
Adequate and well controlled clinical studies safety of Amitriptyline in pregnancy have been conducted.
In experimental studies Amitriptyline has teratogenic effects in doses many times the clinical dose.
Overdosage
Symptoms: hallucinations, convulsions, deliry, coma, cardiac conduction violation, extrasystoles, ventricular arrhythmia, hypothermia, etc.
Treatment: gastric lavage, receiving suspensions of activated charcoal, laxatives, maintaining body temperature, and monitoring functions of the cardiovascular system is not less than 5 days, with heavy holinoliticheskih symptoms (hypotension, arrhythmia, coma) - 0,5-2 g in fizostigmina / m or in / in. Hemodialysis and forced diuresis are not effective.
Cautions
Receive Amitriptyline is possible not earlier than 14 days after the lifting of MAO inhibitors.
Older children and recommended a reduced dose.
You should not assign manic patients and patients with suicidal tendencies.
It should not be used in conjunction with sympathomimetic means, including with epinephrine, ephedrine, izoprenalinom, norepinephrine, fenilefrinom, fenilpropanolaminom.
With caution used in conjunction with other drugs that provide antiholinergicheskoe operation.
During the reception of Amitriptyline is not allowed alcohol.
During the period of treatment should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
