Index of drugs

Treatment of schizophrenia. Treatment of moderate to severe manic episodes. Quetiapine has not been shown to prevent recurrent episodes of mania or depression.

1 tabl powl. contains 25 mg, 100 mg, 150 mg, 200 mg or 300 mg of quetiapine (as fumarate).

Quetiapine is an atypical antipsychotic drug. Quetiapine and its pharmacologically active metabolite - N-desalkylketiapine 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, N-desalkylketiapine has a strong affinity for the norepinephrine transporter (NET). Quetiapine and N-desalkylketiapine 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 the bioavailability of the drug). 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 approximately 7 h, N-dealkylquintiapine - 12 h.

Hypersensitivity to the components of the preparation. Do not use concurrently with cytochrome P450 3A4 inhibitors, such as HIV protease inhibitors, azole antifungals, Erythromycin, Clarithromycin or nefazodone.

The efficacy and safety of quetiapine in children and adolescents has not been established. Use with caution in patients with cardiovascular disease, cerebrovascular disease or other conditions predisposing to hypotension, risk factors for stroke, patients with history of seizures, diabetes or risk factors for diabetes (glycemic control), with liver function, in the elderly and in patients using medicines that strongly induce hepatic enzymes (these medicines significantly reduce the concentration of quetiapine in the blood). Caution should be exercised when quetiapine is used concomitantly with other drugs that prolong the QTc interval, especially in elderly patients, patients with prolonged QT interval, family history of QT prolongation, congestive heart failure, hypertrophy, hypokalaemia or hypomagnesaemia. Quetiapine should not be used in patients with psychosis associated with dementia. Data on the use of quetiapine in combination with divalapioate or lithium in moderate to severe manic episodes are limited, although the combination therapy was well tolerated. In case of symptoms of malignant neuroleptic syndrome, treatment with quetiapine should be discontinued. If tardive dyskinesia occurs, consideration should be given to reducing the dose or stopping quetiapine treatment. In patients with neutrophil count less than 1 x 10⁹/ l, quetiapine should be discontinued; patients should be monitored for signs of infection, and neutrophil counts should be monitored until they exceed 1.5 x 10⁹/ L. The preparation contains lactose and should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose, it also contains sunset yellow, which may cause allergic reactions.

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. The use is not recommended during breastfeeding.

Very common: pain and dizziness, drowsiness, increased triglycerides and total blood cholesterol.Common: leukopenia, syncope, tachycardia, orthostatic hypotension, rhinitis, dry mouth, constipation, indigestion, weakness, peripheral edema, weight gain, ALT and AST elevation, decreased neutrophil count, increased blood Glucose levels above normal . Uncommon: eosinophilia, hypersensitivity reactions, epileptic seizures, restless leg syndrome, increased gamma-GT activity. Rare: jaundice, priapism, neuroleptic malignant syndrome. Very rare: anaphylactic reaction, diabetes or exacerbation of symptoms of pre-existing diabetes, tardive dyskinesia, hepatitis, angioneurotic edema, Stevens-Johnson syndrome. In addition, neutropenia, QT prolongation, ventricular arrhythmia,torsade de pointes, cardiac arrest and cases of sudden, unexplained death. Treatment with quetiapine is associated with a small dose-related decrease in thyroid hormone levels, mainly T4 and fT4 and, at higher doses, a reduction in T3 and rT3 in the blood. In clinical trials, an increased risk of adverse cerebrovascular events has been observed in dementia patients using atypical antipsychotics. After the sudden discontinuation of Quetiapine, withdrawal symptoms (including nausea, headache and dizziness, diarrhea, irritability, vomiting, insomnia) have been reported very commonly.

Orally. Adults.Schizophrenia. The 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 the 4th day, the daily dose is usually 300-450 mg. The dose can be adjusted between 150-750 mg daily, depending on the patient's response to the medicine.Manic episodes associated with bipolar disorder. The 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. The dose can then be increased by a maximum of 200 mg daily to a daily dose of 800 mg on the 6th day of treatment. Depending on the patient's response and tolerability, the daily dose in maintenance treatment may be 200-800 mg per day. The usual recommended dose is 400-800 mg per day.
In patients with hepatic impairment, it is recommended to start treatment with a dose of 25 mg daily and increase daily by 25-50 mg until an effective therapeutic dose is reached. In elderly patients, it may be necessary to increase the dose more slowly and lower the daily therapeutic dose than in younger patients. There is no need to change the dosage in patients with impaired renal function.
The preparation should be taken twice a day, regardless of the meal.