Index of drugs

Treatment of schizophrenia. Prevention of relapse in patients with stable schizophrenia using the preparation as a maintenance therapy. Treatment of moderate to severe manic episodes in the course of bipolar disorder. Treatment of episodes of severe depression in the course of bipolar disorder. Prevention of relapse in patients with bipolar disorder, in patients with manic or depressive episodes responding to Quetiapine treatment. Treatment of major depressive episodes in patients with severe depressive disorder, as adjunctive therapy, if the response to antidepressant monotherapy was less than optimal; before starting treatment, the safety profile of the medicine should be taken into account.

1 tabl about Release (XR) contains 200 mg, 300 mg or 400 mg quetiapine (as fumarate). The preparation contains lactose.

Atypical antipsychotic drug. Quetiapine and its active metabolite, norkwetiapine, interact with many neurotransmitter receptors. The antipsychotic effect is mainly due to the blocking of serotonin (5-HT) receptors in the brain₂) and Dopamine (D.₁ and D₂). In addition, norcorapine has a strong affinity for the norepinephrine transporter (NET). Quetiapine and norquetiapine also have a strong affinity for histamine and α receptors₁-adrenergic and lower affinity for α receptors₂-renergic and serotonin 5-HT₁. Affinity to muscarinic and benzodiazepine cholinergic receptors is negligible. After oral administration, quetiapine is well absorbed from the gastrointestinal tract. The maximum plasma concentration of quetiapine and norcoratapine is reached approximately 6 hours after application of the tablet. XR. The maximum molar concentration of the active metabolite, norkwetiapine, at steady-state is about 35% of the values ​​obtained for quetiapine. Food high in fat caused a statistically significant increase in C_max and AUC of quetiapine in sustained release form, by 50% and 20%, respectively. It can not be ruled out that the impact of high fat meals on the drug may be greater. A light meal had no significant effect on C_max or Quetiapine AUC. It is recommended that quetiapine in a prolonged release form be taken once a day without food. Quetiapine is approximately 83% bound to plasma proteins. It is extensively metabolised in the liver, mainly involving CYP3A4. Less than 5% of quetiapine is excreted unchanged with faeces and urine. About 73% of the metabolites of quetiapine are excreted in the urine, 21% in the faeces. T_0,5 quetiapine in the elimination phase is about 7 h, norewetiapine - 12 h.

Hypersensitivity to quetiapine or other components of the preparation. Do not use together with CYP3A4 inhibitors such as HIV protease inhibitors, azole antifungals, Erythromycin, Clarithromycin, nefazodone.

Quetiapine in children and adolescents is not recommended. Quetiapine is not approved for the treatment of elderly patients with psychotic symptoms in the course of dementia. The efficacy and safety of the medicine has not been studied in patients> 65 years with episodes of depression in the course of bipolar disorder. Long-term efficacy and safety of combination therapy (quetiapine - XR table together with antidepressant therapy) in patients with severe depressive disorder were not evaluated. Use with caution in patients with cardiovascular disease, cerebrovascular disease or other conditions predisposing to hypotension; with risk factors for stroke; with history of epilepsy; with diabetes or risk factors for developing diabetes (regularly monitor these patients for deterioration in blood Glucose control and weight control); with risk factors for neutropenia (with an earlier low white blood cell count and a history of drug-induced neutropenia); with hepatic impairment; in the elderly; in patients using medicines that strongly induce hepatic enzymes (these medicines significantly reduce the amount of quetiapine in the blood).Caution should be exercised in patients with cardiovascular disease or QT family history prolongation and if quetiapine is used concomitantly with other QT prolonging agents, especially in elderly patients, congenital long QT syndrome, congestive heart failure, hypertrophy of the muscle heart failure, hypokalaemia or hypomagnesaemia. Quenching disorders have been observed with quetiapine - caution should be used in patients at risk of aspiration pneumonia. Before and during treatment, all possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken. All patients treated with quetiapine should be monitored for signs of suicidal ideation and behavior (especially during early recovery, after dose adjustment, as well as after sudden withdrawal); this applies especially to patients under the age of 25 years and patients with a history of suicidal behavior or thoughts. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with major depressive disorder. All patients treated with quetiapine should be monitored for signs of hyperglycaemia (excessive thirst and hunger, polyuria and weakness). During treatment with Quetiapine, body weight and lipid profile should be monitored. If the risk profile of metabolic changes (changes in body weight, Glucose, lipids in the blood) deteriorates, the clinical guidelines should be followed and appropriate treatment should be given. If symptoms of hypotension occur during treatment with quetiapine, a dose reduction or slower titration should be considered. In patients with akathisia, increasing the dose of quetiapine may be harmful. If tardive dyskinesia occurs, consideration should be given to reducing the dose or stopping quetiapine treatment. Quetiapine treatment should be discontinued in case of symptoms of malignant neuroleptic syndrome. Drug discontinuation should be discontinued in patients with neutrophil counts <1 x 10⁹/ L; patients should be monitored for signs of infection, and neutrophil counts should be monitored until they exceed 1.5 x 10⁹/ L. Patients with depression in the course of bipolar disorder and patients with severe depressive episodes in severe depressive disorder in whom severe drowsiness occurs, may require more frequent visits during the first 2 weeks after the onset of sleepiness or until improvement; it may be necessary to consider discontinuation of treatment. Data on the use of quetiapine in combination with valproate or lithium in moderate to severe manic episodes are limited, although the combination therapy was well tolerated (from these data it appears that in the third week, the therapy has an additive effect). Due to the lactose content, the drug should not be used in patients with inherited galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

It can only be used during pregnancy if the benefits to the mother outweigh the risks to the fetus. There were withdrawal symptoms in newborns whose mothers took quetiapine during pregnancy. You should avoid breastfeeding while using quetiapine.

Very common: dizziness, drowsiness, headache, dry mouth, withdrawal symptoms (including insomnia, nausea, headache, diarrhea, vomiting, dizziness and irritability), increased triglycerides, increased total cholesterol (mainly fractions) LDL), low HDL cholesterol, decreased hemoglobin, weight gain. Common: leukopenia, hyperprolactinemia, increased appetite, unusual or unpleasant dreams, nightmares, suicidal ideation and behavior, syncope, extrapyramidal symptoms, dysarthria, tachycardia, blurred vision, orthostatic hypotension, rhinitis, constipation, indigestion, mild weakness, edema peripheral, irritability, increase in ALT and AST, reduction in neutrophil counts, increase in blood glucose up to hyperglycaemia.Uncommon: eosinophilia, thrombocytopenia, hypersensitivity reactions, hyponatremia, epileptic seizures, restless legs syndrome, tardive dyskinesia, dysphagia, sexual dysfunction, increased GGT activity, decreased platelet count, QT prolongation. Rare: venous thromboembolism, jaundice, hepatitis, priapism, galactorrhea, breast swelling, menstrual disorders, neuroleptic malignant syndrome, elevation of creatine phosphokinase. Very rare: anaphylactic reactions, abnormal secretion of the diuretic hormone, diabetes mellitus, angioedema, Stevens-Johnson syndrome, rhabdomyolysis. Frequency unknown: neutropenia. Quetiapine treatment is also associated with small dose-related decreases in thyroid hormone levels in the blood, mainly T4 and fT4. During treatment with neuroleptics, cases of prolongation of the QTc interval, atrial arrhythmias, sudden unexpected deaths, cardiac arrest, ventricular tachycardia were observed.torsade de pointes. Side effects that are more common in children and adolescents (10-17 years) than in adults and side effects that were not seen in adults: very common: increased appetite, increased prolactin, increased blood pressure, extrapyramidal symptoms; common: irritability - not recommended for use in children.

Orally. Adults.Treatment of schizophrenia. The product should be administered once a day. The daily dose is: 300 mg - day 1, 600 mg - day 2, the recommended daily dose is 600 mg, but in clinically justified cases the dose can be increased to 800 mg daily. Depending on the clinical response and tolerability, the dose can be adjusted between 400-800 mg / day. There is no need to change the dosage during maintenance therapy in schizophrenia.Treatment of manic episodes in the course of bipolar disorder. The product should be administered once a day. The daily dose is: 300 mg - day 1, 600 mg - day 2, the recommended daily dose is 600 mg, but in clinically justified cases the dose can be increased to 800 mg daily. Depending on the clinical response and tolerability, the dose can be adjusted between 400-800 mg / day.Treatment of depressive episodes in the course of affective disorder bipolar. The product should be administered once a day before bedtime. The total daily dose for the first 4 days of treatment is: 50 mg - day 1, 100 mg - day 2, 200 mg - day 3, 300 mg - day 4, the recommended daily dose is 300 mg. Some patients benefit from a 600 mg dose per day. Doses greater than 300 mg should be administered by a physician experienced in the treatment of bipolar disorder. In some patients who have problems tolerating the drug, a dose reduction of up to 200 mg per day may be considered.Prevention of relapse in bipolar disorder. In patients who have experienced a reaction to quetiapine for the treatment of an acute phase of bipolar disorder, quetiapine should be continued at the same dose to prevent recurrence of manic, mixed or depressive episodes. The dose can be modified depending on the clinical response and tolerability of the patient, in the range of 300-800 mg per day. For maintenance therapy, the lowest effective dose should be used.Supportive therapy in the treatment of severe depressive episode in depressive disorders. The product should be administered once a day before bedtime. The daily dose starting therapy is 50 mg - 1st and 2nd day, 150 mg - 3rd and 4th day. In short-term clinical trials, antidepressant effects were observed at doses of 150 and 300 mg per day in adjunctive therapy (with Amitriptyline, bupropion, citalopram, duloxetine, escitalopram, Fluoxetine, paroxetine, sertraline and venlafaxine) and 50 mg per day as monotherapy in short-term studies. There is an increased risk of side effects after using the drug at higher doses. Therefore, the lowest effective dose should be used, starting with 50 mg daily. The need to increase the dose from 150 to 300 mg per day should be based on an individual assessment of the patient's condition.Special groups of patients. Elderly patients: the initial daily dose is 50 mg, then the dose may be increased by 50 mg per day to the effective dose, depending on the clinical response and tolerability of the patient; in patients with severe depressive episodes in depressive disorders, the daily dose is 50 mg from 1 to 3.on day 4 and up to 150 mg on day 8 of the day, use the lowest effective dose if you need to increase the dose to 300 mg daily, do not take this dose before day 22 of treatment. . Patients with hepatic impairment: initially 50 mg, then the dose can be increased by 50 mg per day until the therapeutic dose is reached. Patients with impaired renal function: there is no need to change the dosage.Way of giving. Table. should be swallowed whole, not to be divided, chewed or crushed; take once a day, without food (at least 1 hour before meals).