Sertraline - instructions for use, dose, side effects, contraindications

The mechanism of antidepressant action is mainly associated with increased serotonergic activity in the CNS as a result of inhibition of serotonin reuptake by neurons of the brain. Along with antidepressant has sedative effect, does not affect peripheral innervation. Causes anorexia.

Pharmacokinetics:

Adsorption is slow, but stable, bioavailability increases when taken with food. Vd 20 l / kg. Relationship with plasma proteins 98%. Biotransformation in the liver (CYP2S19, 2D6) to form a metabolite of N-desmethylsertraline. Presystemic elimination. The half-life is 22-26 hours (sertraline), 62-104 h (N-desmethylsertraline). Cmax 5-8 h. Elimination with feces and urine in equal parts.

Indications:Treatment and prevention of depression of various etiologies (including accompanied by a sense of anxiety), obsessive-compulsive disorder, panic disorder (with agoraphobia or not), post-traumatic stress disorder.

ICD-10

V.F30-F39.F31.9 Bipolar affective disorder, unspecified

V.F30-F39.F31.8 Other bipolar affective disorders

V.F30-F39.F31.7 Bipolar affective disorder, current remission

V.F30-F39.F31.6 Bipolar affective disorder, current episode of mixed character

V.F30-F39.F31.5 Bipolar affective disorder, the current episode of severe depression with psychotic symptoms

V.F30-F39.F31.4 Bipolar affective disorder, the current episode of severe depression without psychotic symptoms

V.F30-F39.F31.3 Bipolar affective disorder, current episode of mild or moderate depression

V.F30-F39.F31.2 Bipolar affective disorder, the current episode of mania with psychotic symptoms

V.F30-F39.F31.1 Bipolar affective disorder, current episode of mania without psychotic symptoms

V.F30-F39.F31.0 Bipolar affective disorder, the current episode of hypomania

V.F30-F39.F31 Bipolar affective disorder

V.F90-F98.F92.0 Depressive behavior disorder

V.F40-F48.F41.2 Mixed anxiety and depressive disorder

V.F30-F39.F33.9 Recurrent depressive disorder, unspecified

V.F30-F39.F33.8 Other recurrent depressive disorders

V.F30-F39.F33.4 Recurrent depressive disorder, current state of remission

V.F30-F39.F33.3 Recurrent depressive disorder, a current episode of severe degree with psychotic symptoms

V.F30-F39.F33.2 Recurrent depressive disorder, current episode of severe degree without psychotic symptoms

V.F30-F39.F33.1 Recurrent depressive disorder, current episode of moderate degree

V.F30-F39.F33.0 Recurrent depressive disorder, current episode of mild

V.F30-F39.F33 Recurrent depressive disorder

V.F30-F39.F32.9 Depressive episode, unspecified

V.F30-F39.F32.8 Other depressive episodes

V.F30-F39.F32.3 Depressive episode of severe degree with psychotic symptoms

V.F30-F39.F32.2 Depressive episode of severe degree without psychotic symptoms

V.F30-F39.F32.1 Depressive episode of moderate degree

V.F30-F39.F32.0 Depressive episode of mild

V.F30-F39.F32 Depressive episode

V.F20-F29.F25.1 Schizoaffective disorder, depressive type

V.F20-F29.F20.4 Post-schizophrenic depression

Contraindications:

Hypersensitivity, simultaneous use of MAO inhibitors, tryptophan or fenfluramine, unstable epilepsy, children under 6 years.

Carefully:

Neurological disorders (including mental retardation), manic conditions, epilepsy, hepatic and / or renal failure, weight loss, children over 6 years of age.

Pregnancy and lactation:

Recommendation category FDA - C.

Adequate and well-controlled studies in humans and animals have not been conducted. The application is possible if the expected benefit for the mother exceeds the potential risk to the fetus. It is found in breast milk. For the duration of treatment, breastfeeding should be discontinued. Women of childbearing age who use sertraline, it is necessary to use reliable methods of contraception.

Dosing and Administration:

Inside, the initial dose for adults and adolescents over 12 years is 25-50 mg once a day in the morning or evening; in the absence of effect, the dose gradually (within a few weeks) increases to a maximum daily dose of 200 mg (50 mg / week). The initial dose for children 6-12 years is 25 mg / day, followed by an increase to 50 mg / day.For children aged 12 to 17 years, the initial dose is 50 mg once a day in the morning or evening. If necessary, the daily dose can be gradually, not earlier than a week, increased from 50 mg to a maximum daily dose of 200 mg. To avoid an overdose, less weight in children should be taken into account compared with adults, and with a dose increase of more than 50 mg / day, careful monitoring of this category of patients is necessary and at the first signs of an overdose, the drug should be discontinued.

Side effects:

From the nervous system and sensory organs: drowsiness, dizziness, headache, insomnia, confusion, amnesia, ataxia, discoordination, hyper- and paresthesia, hyperkinesia, hypo- and dyskinesia, extrapyramidal disorders, convulsions, mydriasis, nystagmus, ptosis, hyporeflexia , aggressiveness, anxiety, psychosis, amnesia, apathy, depersonalization, emotional lability, euphoria, hallucinations, paranoid reactions, somnambulism.

From the cardiovascular system and blood (hematopoiesis, hemostasis): arterial hypertension or arterial hypotension, palpitation, chest pain, anemia; rarely - tachycardia, collapsoid states.

On the part of the digestive system: dry mouth, decreased appetite until anorexia (rarely - increased appetite, possibly as a consequence of eliminating depression), dyspeptic disorders (flatulence, nausea, vomiting, diarrhea or unstable stools, constipation), stomach cramps, pain in the stomach abdomen, pancreatitis, changes in hepatic tests, hepatitis, jaundice or liver failure, dysphagia, irritation of the mucous membrane of the gastrointestinal tract, glossitis, gingival hypertrophy, ulcerative stomatitis.

On the part of the respiratory system: a feeling of chest compression.

On the part of the genitourinary system: delayed ejaculation, decreased libido, erectile dysfunction, anorgasmia, menstrual irregularities, gynecomastia, priapism, dysuria, hyperprolactinaemia, galactorrhea.

Allergic reactions: redness of the skin, hives; swelling of the face or lips; skin rash, generalized itching, multi-form exudative erythema.

Others: swelling (including periorbital), arthralgia, lymphadenopathy, increased sweating, weight loss, withdrawal syndrome.

Overdose:

Symptoms: serotonin syndrome - nausea, vomiting, drowsiness, ECG changes, mydriasis, tachycardia, agitation, dizziness,anxiety, psychomotor agitation, diarrhea, increased sweating, myoclonus, and hyperreflexia.

Treatment: the appointment of activated charcoal, symptomatic therapy, maintenance of vital functions.

Interaction:

Concentrated oral preparations of sertraline contain 12% alcohol, concomitant with disulfiram the use is contraindicated.

Amitriptyline inhibits CYP2D6 and slows biotransformation, can increase plasma concentration, enhances (mutually) the effect; at a combined appointment it is necessary to lower the dose.

Against the background of sertraline (competing for communication sites with proteins), the plasma level of the free fraction of warfarin increases; can increase the effect.

Concentration of metoprolol (in combination vinpocetine + indapamide + metoprolol + enalapril) in the blood plasma can increase with simultaneous admission.

Together with diazepam increases the depression of the central nervous system.

With simultaneous application with lithium salts, tremor may be strengthened. With simultaneous use with desipramine, an increase in the concentration of desipramine in the blood plasma is possible; with cimetidine - a significant decrease in the clearance of sertraline.

Special instructions:

Use with caution in patients who have abused drugs or with drug dependence in history, with violations of the liver, kidneys, epileptic seizures, with insufficient body weight.

Do not use in patients undergoing electroshock therapy. The use of sertraline is possible no earlier than 14 days after the abolition of MAO inhibitors.

During the treatment period, do not drink alcohol.

Affects the ability to drive vehicles and control mechanisms. During the period of treatment, it is necessary to avoid activities requiring increased attention and high speed of psychomotor reactions.

Instructions

Sertraline (Sertralinum)