Index of drugs

Treatment of schizophrenia. Treatment of moderate to severe manic episodes associated with bipolar disorder. Treatment of depressive episodes in the course of bipolar disorder. Prevention of subsequent mania, depression and mixed episodes in patients who responded to Quetiapine treatment for these episodes.

1 tabl powl. contains 25 mg, 100 mg, 200 mg or 300 mg quetiapine (as fumarate); drug contains lactose.

Atypical antipsychotic drug. Quetiapine and its pharmacologically active metabolite, norkwetiapine, act on many receptors of neurotransmitters. 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 high 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. Quetiapine is well absorbed from the gastrointestinal tract (food does not affect its bioavailability). It binds to plasma proteins in 83%. It is extensively metabolised in the liver, mainly involving CYP3A4. Less than 5% of the drug 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 indicated for the treatment of elderly patients with psychosis associated with dementia. Use with caution in patients with cardiovascular disease, cerebrovascular disease or other conditions predisposing to hypotension; with risk factors for stroke; with history of epileptic seizures and those at whom the seizure threshold may be reduced (eg with Alzheimer's disease, over 65 years of age); with diabetes or risk factors for the development of diabetes (regularly monitor glycaemia); 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). As with other antipsychotics, caution should be exercised when prescribing quetiapine to patients with cardiovascular disease or a long history of QT. Similarly, caution is advised when quetiapine is combined with drugs known to prolong the QT interval, with neuroleptics (especially in the elderly), patients with congenital QT prolonged syndrome, congestive heart failure, hypertrophy, hypokalaemia and hypomagnesaemia, and patients with an extended QT interval in a family history. Quenching disorders have been observed with quetiapine - caution should be used in patients at risk of aspiration pneumonia. Before and during treatment with the preparation, all possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken. All patients treated with the product should be monitored for signs of suicidal ideation and behavior (especially in early recovery and after a change in the dose); this applies especially to patients under the age of 25 years and patients with a history of suicidal behavior or thoughts. During treatment with Quetiapine, the lipid profile should be monitored; changes in lipid levels should be treated if clinically significant. Patients should be monitored for hyperglycaemia.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. QUetiapine should be discontinued in patients with neutrophil counts <1x10⁹/ L; patients should be monitored for signs of infection, and neutrophil counts should be monitored until they exceed 1.5x10⁹/ L. Patients with bipolar depression who are experiencing drowsiness of severe intensity 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. Treatment with quetiapine was accompanied by orthostatic hypotension and associated dizziness (caution should be exercised due to the risk of falls, especially in elderly patients), akathisia development (symptoms are more likely in the first week of treatment, dose escalation may be detrimental) and weight gain (body weight should be monitored). Data on the use of quetiapine in combination with valproate or lithium in the treatment of moderate to severe symptoms of mania 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 preparation should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

During pregnancy, apply only if the benefits for the mother outweigh the potential risk to the fetus. Extrapyramidal disturbances and / or withdrawal symptoms were observed in newborns whose mothers used quetiapine during pregnancy (especially in the third trimester). Women taking the drug should not breastfeed.

Very common: pain and dizziness, drowsiness, dry mouth, withdrawal symptoms, increased triglycerides in the blood, increased total cholesterol (mainly LDL), lower HDL cholesterol, weight gain, and reduced hemoglobin. Common: leukopenia, hyperprolactinemia, decrease in total T concentration₄, decrease in free T concentration₄, decrease in total T concentration₃, increased TSH, increased appetite, increased blood sugar to hyperglycemic level, strange dreams and nightmares, suicidal thoughts and behaviors, syncope, extrapyramidal symptoms, dysarthria, blurred vision, tachycardia, palpitations, orthostatic hypotension, rhinitis, dyspnoea, constipation, dyspepsia, vomiting, elevated aminotransferases (ALAT, AST), elevated blood γ-glutamyltransferase levels, mild asthenia, peripheral edema, irritability, fever. Uncommon: thrombocytopenia, anemia, decreased number of platelets, hypersensitivity reactions, decreased free T concentration₃, hypothyroidism, hyponatremia, diabetes, convulsions, restless legs syndrome, tardive dyskinesia, QT prolongation, bradycardia, dysphagia, sexual dysfunction. Rarely: agranulocytosis, metabolic syndrome, somnambulism and related reactions, ie sleep and sleep related disorders, venous thromboembolism, pancreatitis, jaundice, hepatitis, priapism, galactorrhoea, breast edema, menstrual disorders, neuroleptic malignant syndrome , hypothermia, elevation of creatine phosphokinase. Very rare: anaphylactic reactions, inappropriate antidiuretic hormone secretion, angioneurotic edema, Stevens-Johnson syndrome, rhabdomyolysis. Not known: neutropenia, toxic epidermal necrolysis, erythema multiforme, withdrawal syndrome in the newborn. 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; often: irritability.

Orally. Adults.Treatment of schizophrenia: drug administered twice a day. 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, from day 4 the dose should be increased to an effective dose usually 300-450 mg per day.Depending on the clinical response and tolerability, the dose can be adjusted in the range of 150-750 mg per day.Treatment of manic episodes associated with bipolar disorder: drug administered twice a day. The total daily dose for the first 4 days of treatment is: 100 mg - day 1, 200 mg - day 2, 300 mg - day 3, 400 mg - day 4, then the dose may be increased by a maximum of 200 mg per day to 800 mg daily dose on day 6 of treatment. Depending on the clinical response and tolerability, the dose can be adjusted between 200-800 mg / day; the usual effective dose is 400-800 mg per day.Treatment of episodes of depression associated with bipolar disorder: drug 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. Depending on the patient's response to treatment, the dosage can be increased to 600 mg per day. The antidepressant efficacy of 300 mg and 600 mg per day has been demonstrated; however, no additional benefit was found with the 600 mg dose versus the 300 mg dose per day during short-term treatment.Prevention of subsequent episodes of mania, depression and mixed episodes in the course of bipolar disorders: patients who have responded clinically to quetiapine in the acute course of bipolar disorder should continue treatment with the same dose. The dose can be modified depending on the clinical response and tolerability of the patient, in the 300-800 mg range, administered twice daily. For maintenance therapy, the lowest effective dose should be used.Special groups of patients. In elderly patients, the starting dose is 25 mg per day, then the dose should be increased by 25 mg or 50 mg per day to an effective dose, which is usually lower than in younger patients. In patients over 65 years, plasma clearance of quetiapine may be reduced, in which case a dose adjustment may be necessary. The efficacy and safety of treatment has not been determined in patients> 65 years with depressive episodes in the course of bipolar disorder. As in the elderly, it is recommended that patients who are debilitated and prone to hypotensive reactions should be titrated up more slowly and with lower therapeutic doses. Patients with hepatic impairment may need to change their dosage, especially at the beginning of treatment; treatment should start with a daily dose of 25 mg and increase the daily dose by 25-50 mg to achieve a therapeutic dose. No dosage adjustment is necessary for patients with impaired renal function.
The drug can be taken with or without food.