Index of drugs

Episodes of major depression. Prevention of recurrence of major depressive episodes. Panic disorder with accompanying (or not) agoraphobia. Obsessive-compulsive disorder (ZO-K) in adults and children and adolescents aged 6-17. Social anxiety disorder. Post-traumatic stress disorder (PTSD).

1 tabl powl. contains 50 mg or 100 mg of sertraline in the form of a hydrochloride.

Antidepressant - a strong, selective inhibitor of neuronal reuptake of serotonin. It has a very weak effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, it inhibits serotonin uptake in platelets. Sertraline does not increase catecholaminergic activity. It does not show affinity for muscarinic (cholinergic), serotonin, dopaminergic, adrenergic, histaminergic receptors, GABA receptors or benzodiazepine receptors. After an oral dose of 50-200 mg once daily for 14 days, the maximum plasma concentration occurred 4.5-8.4 h after daily administration. Plasma protein binding is approximately 98%. Sertraline undergoes extensive metabolism during the first pass through the liver. It is metabolised by many pathways, including CYP3A4, CYP2C19 and CYP2B6. Sertraline and its major metabolite, desmethylsertraline, are also substrates of P-glycoprotein underin vitro. Medium T_0,5 is about 26 hours (22-36 h). In the final phase of elimination, there is an approximate double accumulation to stationary steady state concentrations, which are achieved after 1 week of once daily dosing. T_0,5 N-desmethylsertraline remains in the range of 62-104 h. Both sertraline and N-desmethylsertraline are extensively metabolised and the resulting metabolites are excreted in the faeces and in the urine in equal amounts. Only a small amount (<0.2%) of unchanged sertraline is excreted in the urine.

Hypersensitivity to the active substance or to any of the excipients. Concomitant use of sertraline with irreversible MAO inhibitors is contraindicated due to the risk of serotonin syndrome, whose symptoms include: agitation, tremor and hyperthermia. Sertraline should not be started for at least 14 days after stopping treatment with an irreversible MAO inhibitor. Sertraline should be discontinued at least 7 days before treatment with an irreversible MAO inhibitor. The concurrent use of pimozide is contraindicated.

Patients using SSRIs, including sertraline, have been reported to develop potentially life-threatening symptoms of the serotonin syndrome or neuroleptic malignant syndrome. The risk was greater when serotonergic drugs (including triptans) were used simultaneously with drugs that affect the metabolism of serotonin (including MAO inhibitor), antipsychotic drugs and other Dopamine antagonists. The patient should be monitored for symptoms of serotonin syndrome or neuroleptic malignant syndrome. Caution should be exercised when changing therapy with SSRIs, antidepressants and antiobsessives to sertraline, especially when changing from long-acting drugs such as fluoxetine. The concomitant use of sertraline with other drugs that enhance the effects of serotoninergic neurotransmission (eg tryptophan, fenfluramine or 5-HT agonists) or herbal remedies containing St John's wort requires caution; where possible, simultaneous use should be avoided. Due to the risk of prolongation of the QTc interval and ventricular tachycardiatorsade de pointes sertraline nordicides should be used with caution in patients with risk factors with risk factors for prolonging the QTc interval. Caution should be exercised in patients with a history of mania or hypomania, close medical monitoring is necessary. Sertraline should be discontinued if the patient goes into a manic phase. Patients with schizophrenia may experience worsening of psychotic symptoms. The use of sertraline in patients with unstable epilepsy should be avoided; patients with controlled epilepsy require close monitoring.Sertraline should be discontinued in any patient who develops seizures. Depression is associated with an increased risk of suicidal thoughts, self harm and suicide. This risk persists until significant improvement is achieved. The patient should be closely monitored until the appearance of improvement and in the early stages of recovery (increased risk of suicide). In patients treated for other psychiatric disorders, the same precautions should be taken as in patients with major depression. 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 suicide attempts and should be closely monitored during treatment, particularly in patients below 25 years of age. During treatment, especially at the beginning of therapy and when the dose is changed, patients should be closely monitored, particularly those at high risk. Sertraline should not be used to treat children and adolescents under 18 years of age, except in patients with obsessive-compulsive disorder aged 6-17. During clinical trials, suicidal behaviors (suicidal thoughts and attempts) and hostility (especially aggression, rebel behavior and anger) were more frequently observed in children and adolescents treated with antidepressants than in the placebo group. If, however, as a result of an existing clinical need, a decision to treat is made, the patient should be closely monitored for signs of suicidal symptoms. In addition, limited clinical data are available related to the safety of long-term use of sertraline in children and adolescents regarding growth, sexual maturation and cognitive development and behavioral development. In the post-marketing period, several cases of delayed growth and maturation were reported. Clinical significance and cause and effect relationship have not been fully elucidated. The doctor must monitor the health of children and adolescents treated for a long time in order to detect abnormal growth and development. Due to the risk of abnormal bleeding, caution is advised in patients taking SSRIs, especially when concomitant use of drugs that affect platelet function (eg anticoagulants, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, Acetylsalicylic acid and NSAIDs), as well as patients with a history of bleeding disorders. During the use of the preparation there is a risk of hyponatremia (may result from the syndrome of inappropriate secretion of antidiuretic hormone (SIADH)); cases of decrease in serum sodium below 110 mmol / l have been reported. Higher risk of hyponatraemia may be associated with elderly patients and patients taking diuretic or other medications that reduce fluid volume. In patients with symptomatic hyponatraemia, discontinuation of sertraline and appropriate medical management should be considered. In patients who develop symptoms of akathisia, increasing the dose may be harmful. Severe caution should be used when treating sertraline in patients with liver disease. In patients with impaired hepatic function, lower doses of sertraline should be considered or prolongation of the interval between consecutive doses should be considered. Sertralin should not be used in patients with severe hepatic impairment. In diabetic patients, treatment with SSRIs may affect glycemic control - adjustment of insulin dose and / or oral antidiabetic agents may be required. No clinical trials have been conducted to determine the risks or benefits of concomitant electroconvulsive therapy and sertraline. The use of sertraline with grapefruit juice is not recommended. SSRIs, including sertraline, can affect the size of the pupil, which results in its enlargement. Pupil dilation may cause narrowing of the angle of the eye, resulting in increased intraocular pressure and the development of glaucoma with a closed angle of perception, especially in patients with predisposing factors. Caution should be exercised when using sertraline in patients with closed-angle glaucoma or history of glaucoma.

There are no adequate controlled studies on the use of sertraline in pregnant women. However, the analysis of a significant amount of collected data does not indicate that sertraline caused congenital malformations. The results of epidemiological studies indicate that the use of SSRI in pregnant women, especially in the third trimester, may increase the risk of persistent pulmonary hypertension of the newborn (PPHN). Cases have been reported in which the use of sertraline during pregnancy caused symptoms (consistent with discontinuation symptoms) in some newborns whose mothers had been treated with sertraline. The use of sertraline is not recommended during pregnancy except when the clinical condition of the woman justifies the use of the drug and the potential benefits of treatment outweigh the potential risk. If the mother continues her treatment with sertraline later in pregnancy (especially in the third trimester), the newborn baby needs to be observed. In newborns whose mothers take sertraline later in pregnancy, the following symptoms may be observed: respiratory failure, cyanosis, apnea, seizures, fluctuations in body temperature, difficulty in taking food, vomiting, hypoglycaemia, increased muscle tone, decreased muscle tone, increased reflexes , muscle tremors, muscle cramps, irritability, hypothermia, constant crying, drowsiness and sleep disorders. These symptoms may be due to serotonergic effects or symptoms of withdrawal. In most cases, complications develop immediately or in a short time (less than 24 hours) after delivery. Small amounts of sertraline and its metabolite N-desmethylsertraline are excreted in breast milk. This medicine is not recommended for mothers who are breastfeeding, except when the doctor believes that the benefits of taking the medicine outweigh the risks. There have been reports indicating that the use of certain SSRIs in humans has a transient effect on sperm quality. No effects on human fertility have been observed so far.

Very common: insomnia (19%), dizziness (11%), drowsiness (13%), headache (21%), diarrhea (18%), nausea (24%), dry mouth (14%), ejaculation disorders (14%), fatigue (10%). Common: pharyngitis, decreased appetite, increased hunger, depression, depersonalization, nightmares, anxiety, agitation, nervousness, decreased libido, bruxism, paresthesia, tremor, hypertonia, taste disorders, concentration disorders, visual disturbances, tinnitus, palpitations, hot flushes, yawning, abdominal pain, vomiting, constipation, dyspepsia, flatulence, rash, excessive sweating, joint pain, muscle pain, erectile dysfunction, chest pain, malaise. Uncommon: upper respiratory tract infections, rhinitis, hypersensitivity, hypothyroidism, hallucinations, euphoria, apathy, thinking disorders, seizures, involuntary muscle contractions, coordination disorders, hyperkinesia, amnesia, hypoaesthesia, speech disorders, locomotive dizziness, fainting , migraine, mydriasis, earache, tachycardia, hypertension, flushing, bronchospasm, shortness of breath, nosebleeds, oesophagitis, dysphagia, haemorrhagic tumors, salivary glands, tongue disorders, belching, swelling periorbital, face edema, purpura, baldness, cold sweats, dry skin, urticaria, pruritis, arthritis and bones, muscle weakness, backache, muscle tics, nocturia, urinary retention, polyuria, pollakiuria, urinary disorders, urinary incontinence, vaginal bleeding, dysfunction sexual dysfunction, sexual dysfunction in women, irregular menstruation, peripheral edema, chills, fever, asthenia, thirst, increased ALT, AST, weight loss, weight gain. Rarely: diverticulitis, gastroenteritis, otitis media, cancer, lymphadenopathy, anaphylactoid reactions, diabetes mellitus, hypercholesterolemia, hypoglycaemia, conversion disorders, drug addiction, psychotic disorders, paranoia, suicidal ideation, suicide behavior, cougarettes, premature ejaculation, coma, choreoathetosis, dyskinesia, hyperaesthesia, impaired sensation, glaucoma, impaired tear secretion, loss of visual field, double vision, photophobia, bleeding into the anterior chamber of the eye, myocardial infarction,bradycardia, cardiac disorders, peripheral ischaemia, hematuria, laryngeal spasm, hyperventilation, hypoxia, larynx, dysphonia, hiccups, tarry stools, presence of fresh blood in the stool, oral mucositis, tongue ulcer, tooth disorder, tongue inflammation, mouth ulcer , liver dysfunction, dermatitis, dermatitis, follicular rash, abnormal hair structure, abnormal skin smell, bone disorders, oliguria, delayed urination, menorrhagia, atrophic vulvovaginitis, glans and foreskin inflammation, vaginal discharge, painful penile erection, galactorrhea, hernia, fibrosis at the injection site, reduced drug tolerance, gait disturbances, sperm abnormalities, increased cholesterol, injuries, vasodilation. Not known: leukopenia, thrombocytopenia, allergy, hyperprolactinemia, hypersecretion hormone hyperactivity disorder (ADH), hyponatremia, hyperglycemia, sleep disturbances, movement disorders (including extrapyramidal disorders such as hyperkinesia, hypertonia, grinding of teeth and gait disturbances), symptoms subjects and subjects associated with serotonin syndrome or neuroleptic malignant syndrome, e.g. agitation, confusion, profuse sweating, diarrhea, fever, hypertension, stiffness, tachycardia (in some cases this was associated with the simultaneous use of serotonergic drugs), akathisia and psychomotor restlessness , cerebral vasospasm (including transient cerebrovascular spasm and Call-Fleming syndrome), abnormal vision, uneven pupils, QTc prolongation of ventricular tachycardia (torsade de pointes), abnormal bleeding (nosebleeds, from the gastrointestinal tract), interstitial pneumonitis, pancreatitis, severe liver disease (including hepatitis, jaundice and hepatic failure), severe side effects from the skin (e.g. Stevens-Johnson syndrome and epidermal necrolysis), angioneurotic edema, hypersensitivity to light, skin reactions, muscle spasms, gynecomastia, abnormal laboratory tests, and platelet dysfunction. Elderly patients may be more at risk of clinically significant hyponatraemia. Epidemiological studies conducted mainly among patients over 50 years have shown an increased risk of bone fractures in patients taking SSRIs and tricyclic antidepressants. In pediatric patients, the general adverse reaction profile was generally similar to that seen in studies involving adults. The following adverse reactions were observed in controlled studies: very common: headache (22%), insomnia (21%), diarrhea (11%), and nausea (15%); common: chest pain, mania, fever, vomiting, anorexia, emotional lability, aggression, agitation, nervousness, attention disorders, dizziness, hyperkinesia, migraine, drowsiness, tremors, blurred vision, dry mouth, indigestion, nightmares , fatigue, incontinence, rash, acne, nosebleed, bloating; uncommon: prolongation of the ECG QT interval, suicide attempts, convulsions, extrapyramidal disorder, paraesthesia, depression, hallucinations, purpura, hyperventilation, anemia, liver dysfunction, elevated ALT, cystitis, herpes, external otitis, earache, aches and pains eyesight, mydriasis, malaise, hematuria, pustular rash, rhinitis, injuries, weight loss, muscle cramps, abnormal dreams, apathy, proteinuria, pollakiuria, polyuria, breast pain, menstrual disorders, alopecia, dermatitis, skin disorders, abnormal skin smell, hives, bruxism, hot flushes. Not known: incontinence. Withdrawal of sertraline (especially sudden) often results in withdrawal symptoms. The most frequently reported reactions are: dizziness, sensory disturbances (including paraesthesia), sleep disorders (including insomnia and intense dreams), agitation or anxiety, nausea and / or vomiting, muscle twitching and headaches.

Orally.Adults. Initial treatment. Depression and ZO-K: treatment should start at 50 mg daily. Panic disorder, PTSD and social anxiety disorder: treatment should start with a dose of 25 mg per day. After 1 week, the dose should be increased to 50 mg once a day.This dosing regimen has been shown to reduce the frequency of adverse reactions characteristic of the initial phase of panic disorder.Increasing the dose. Depression, ZO-K, panic disorder, social anxiety disorder and PTSD: patients not responding to 50 mg may need to be increased. Dose changes should be made at intervals of at least 1 week, each time by 50 mg, up to a maximum dose of 200 mg per day. Because of T_0,5 sertraline in the elimination phase (24 h), the dosage should not be changed more often than once a week. The onset of therapeutic action can take place within 7 days. In order to achieve a therapeutic effect, especially in the treatment of patients with ZO-K, a longer treatment period is necessary.Maintenance treatmentThe dosage should be maintained at the lowest effective dose level and then adjusted depending on the patient's response to treatment. Depression: long-term treatment may also be necessary to prevent the recurrence of major depressive episodes. In most cases, the dose recommended for preventing relapse of episodes of depression is the same as the dose used to treat the current episode. Patients with depression should be treated long enough for at least 6 months to ensure that the symptoms of the disease have disappeared. Panic attack and ZO-K: the need to continue treatment should be regularly assessed because the ability to prevent relapse has not been proven in these disorders.Children and adolescents with obsessive-compulsive disorders. Age 13-17: initial dose 50 mg once a day. Age 6-12 years: starting dose of 25 mg once a day. After 1 week, the dose may be increased to 50 mg once a day. If there is no expected response to treatment, the dosage can be further increased by 50 mg / day, depending on the need, within a few weeks. The maximum daily dose is 200 mg. When increasing the dose above 50 mg, it should be taken into account that children usually have a lower body weight than adults. Do not change the dosage more often than once a week. The effectiveness of sertraline in cases of major depression in children has not been demonstrated. In elderly patients, the dose should be carefully selected. In patients with impaired hepatic function, lower doses should be used or longer between doses, the drug should not be used in case of severe hepatic impairment. There is no need to change the dosage in patients with renal insufficiency.
The preparation should be administered once a day, in the morning or evening, with or without food.