Amitriptyline-Ferein - instructions for use, dose, side effects, contraindications

Each tablet, coated with a shell, contains: active ingredient - amitriptyline hydrochloride-0.01 g (10 mg) or 0.025 (25 mg) and Excipients: in the core - microcrystalline cellulose, croscarmellose sodium, aerosil, magnesium stearate; in the shell: hydroxypropylmethylcellulose, polyethylene glycol - 6000, titanium dioxide, indigocarmine for a dosage of 0.01 g (10 mg) or hydroxypropylmethylcellulose, polyethylene glycol-6000, titanium dioxide, tropeoline O-for a dosage of 0.025 (25 mg).

Description:

Tablets coated with a blue coating (for a dosage of 0.01 g) or yellow (for a dosage of 0.025 g) of color. Two layers are visible on the cross-section.

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.A.09 Amitriptyline

Pharmacodynamics:

Amitriptyline is a tricyclic antidepressant from a group of indiscriminate inhibitors of neuronal capture of monoamines. Has a pronounced timoanaleptic and sedative effect.

Pharmacodynamics

The mechanism of antidepressant action of amitriptyline is associated with inhibition of reverse neuronal seizure of catecholamines (norepinephrine, dopamine) in the central nervous system. Amitriptyline is an antagonist of muscarinic cholinergic receptors in the central nervous system and periphery. It also has peripheral antihistamine (H1) and antiadrenergic properties.

Pharmacokinetics:

Absorption is high.With oral administration of amitriptyline, the maximum plasma concentrations are reached within 4-8 hours. Its bioavailability is 33 to 62%. Time to reach the maximum concentration (Cmah) after intake of 2.0-7.7 hours. The volume of distribution is 5-10 l / kg. Effective therapeutic concentrations in the blood of amitriptyline are 50-250 ng / ml, for nortriptyline (its active metabolite) 50-150 ng / ml. Passes through the blood-brain barrier (including nortriptyline).

The concentrations of amitriptyline in tissues are higher than in plasma. Relationship with plasma proteins 92 - 96%.

Metabolised in the liver (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites.

The half-life of plasma from 10 to 28 hours for amitriptyline and 16 to 80 hours for nortriptyline. It is allocated, mainly, with urine. Complete excretion within 7 days. Amitriptyline penetrates the placental barrier, is excreted in breast milk in concentrations similar to plasma.

Indications:

Depression of any etiology. Due to the severity of the sedative effect is especially effective in anxiety - depressive states.

Mixed emotional disorders and behavioral disorders, phobic disorders.

Children's enuresis (except for children with hypotonic urinary bladder).

Psychogenic anorexia, bulimic neurosis.

Neurogenic pain of a chronic nature, for the prevention of migraine.

Contraindications:

Heart failure in the stage of decompensation.

Acute and recovery period of myocardial infarction.

Violations of the conduction of the heart muscle.

Severe arterial hypertension.

Acute liver and kidney disease, with severe impairment of functions.

Diseases of the blood.

Stomach ulcer and 12 duodenal ulcer in the stage of exacerbation.

Hypertrophy of the prostate.

Atony of the bladder.

Pylorosthenosis, paralytic obstruction of the intestine.

Simultaneous treatment with MAO inhibitors (see Interaction).

Pregnancy, the period of breastfeeding.

Children under 6 years.

Hypersensitivity to Amitriptyline.

Carefully:

Amitriptyline should be used with caution in people suffering from alcoholism, with bronchial asthma, manic-depressive psychosis (MDP) and epilepsy (see.Special instructions), oppression of bone marrow hematopoiesis, hyperthyroidism, angina pectoris and heart failure, as well as with angle-closure glaucoma and intraocular hypertension.

Dosing and Administration:

Assign inside (during or after eating).

The initial daily intake with oral administration 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 part of the dose is taken at night). In severe depression, resistant to therapy, the dose is increased to 300 mg or more, to the maximum tolerated dose (maximum dose for outpatients is 150 mg / day). In these cases, treatment is advisable to start with intramuscular or intravenous administration of the drug, while using higher initial doses, accelerating the build-up of dosages under the control of the somatic condition.

After obtaining a persistent antidepressant effect, after 2-4 weeks the doses gradually and slowly decrease. In case of signs of depression with decreasing doses, it is necessary to return to the previous dose.

If the patient's condition does not improve within 3-4 weeks of treatment, then further therapy is impractical.

In elderly patients with mild disorders, in outpatient practice, the doses are 25-50-100 mg - maximum, in divided doses or 1 time per day at night.

When enuresis, children older than 6 years 12.5-25 mg before bed (dose should not exceed 2.5 mg / kg of the child's weight).

For the prevention of migraine, chronic pain of a neurogenic nature (including prolonged headaches) from 12.5-25 mg to 100 mg / day.

Side effects:

Mainly associated with the anticholinergic action of the drug: blurred vision, paresis of accommodation, increased intraocular pressure, dry mouth, stool retention, intestinal obstruction, urinary retention, fever. All these phenomena usually pass after adaptation to the drug or reduce doses.

From the side of the central nervous system: increased fatigue, irritability, dizziness, drowsiness, confusion, hallucinations, motor excitement, disorientation, tremor, ataxia, insomnia, nightmares, headache, peripheral neuropathy, EEG changes.Rarely - extrapyramidal disorders, increased anxiety.

From the side of the cardiovascular system: tachycardia, conduction disorders, orthostatic arterial hypotension, expansion of the complex QRS on ECG, symptoms of heart failure.

From the gastrointestinal tract: nausea, vomiting, anorexia, stomatitis, impaired taste, darkening of the tongue, a feeling of discomfort in the epigastrium, increased activity of "liver" transaminases, rarely cholestatic jaundice.

From the endocrine system: gynecomastia, galactorrhea, changes in the secretion of antidiuretic hormone (ADH), decreased libido, potency. Rarely - hyperglycemia, glucosuria, impaired glucose tolerance.

Allergic reactions: skin rash, itching, photosensitivity, angioedema. Other: agranulocytosis and other blood changes, hair loss, enlarged lymph nodes, weight gain with prolonged use, sweating, pollakiuria.

With prolonged treatment, especially in high doses, with a sharp cessation of treatment, it is possible to develop a withdrawal syndrome: headache, nausea, vomiting, etc.

Overdose:

Drowsiness, disorientation, confusion, mydriasis, fever, dyspnea, dysarthria, agitation, hallucinations, seizures, muscle stiffness, supor, coma, vomiting, arrhythmia, hypotension, cardiac failure, respiratory depression.

Measures of assistance: discontinuation of Amitriptyline therapy, gastric lavage, fluid infusion, symptomatic therapy, maintenance of blood pressure and water-electrolyte balance. Monitoring of cardiovascular activity (ECG) for 5 days is shown, since relapse can occur after 48 hours and later. Hemodialysis and forced diuresis are of little effect.

Interaction:

Amitriptyline increase CNS depression following medicines: antipsychotics, sedatives and hypnotics, anticonvulsants, central and narcotic analgesics, anesthetics, alcohol.

With the combined use of Amitriptyline with neuroleptics, and / or anticholinergic drugs, a febrile temperature reaction may occur, paralytic intestinal obstruction.

Amitriptyline potentiates the hypertensive effects of catecholamines, but inhibits the effects of drugs acting on the release of norepinephrine.

Amitriptyline may reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action.

With the simultaneous use of Amitriptyline and anticoagulants - derivatives of coumarin, an increase in anticoagulant activity of the latter is possible.

With the simultaneous administration of amitriptyline and cimetidine, an increase in the concentration in the plasma of Amitriptyline is possible with the possible development of toxic effects. Inducers of microsomal liver enzymes (barbiturates, carbamazepine) reduce the plasma concentrations of Amitriptyline.

Amitriptyline increases the effect of antiparkinsonian drugs.

Quinidine slows the metabolism of Amitriptyline.

The combined use of amitriptyline with disulfiram and other acetaldehyde dehydrogenase inhibitors can trigger delirium.

Simultaneous reception of Amitriptyline with MAO inhibitors can lead to death. A break in treatment between taking MAO inhibitors and tricyclic antidepressants should be at least 14 days!

Special instructions:

Amitriptyline in doses above 150 mg / day reduces the threshold of convulsive activity, therefore, one should consider the possibility of occurrence of convulsive seizures in patients with those in the anamnesis,and in the category of patients who are predisposed to this because of age or trauma.

Treatment with amitriptyline in old age should be under careful physical 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 a depressive TIR phase can go into a manic stage.

Effect on the ability to drive transp. cf. and fur:

During reception of Amitriptyline it is forbidden to drive vehicles, service mechanisms and other types of work that require increased concentration of attention, as well as alcohol intake.

Form release / dosage:

The coated tablets 10 mg, 25 mg.

Packaging:10, 20 tablets in a contour cell package; 1, 2, 3, 4, 5 contour packs in a pack, 40,50 tablets in cans of orange glass or jars and vials of glass for medicines; 40, 50, 60, 100 tablets in plastic containers, 1 can, a bottle, a plastic container in a pack.

Storage conditions:

List B. In a dry, protected from light, out of reach of children at a temperature of 15 ° to 30 ° C.

Shelf life:

5 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002069 / 01-2003

Date of registration:08.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp13.09.2017

Illustrated instructions

Instructions

Amitriptyline-Ferein (Amitriptyline-Ferein)