Seroquel Prolong, pills 200mg, 60pcs

Composition

1 tablet of prolonged action, film-coated, contains:

Active ingredient:

quetiapine (in the form of fumarate) 200 mg,

excipients:

lactose monohydrate;

MCC;

sodium citrate dihydrate;

hypromellose;

magnesium stearate,

shell composition:

hypromellose; macrogol 400; titanium dioxide E 171; iron oxide yellow dye E 172

Indications

Schizophrenia, including relapse prevention in stable patients; bipolar disorders, including:

• moderate and severe manic episodes in the structure of bipolar disorder;
• severe episodes of depression in the structure of bipolar disorder;
• prevention of relapses of bipolar disorders in patients with previous effective therapy with quetiapine manic or depressive episodes in the structure of bipolar disorder.

Contraindications

• hypersensitivity to any component of the drug Seroquel Prolong;
• lactase deficiency, glucose-galactose malabsorption and intolerance to galactose;
• simultaneous use with inhibitors of cytochrome P-450, such as antifungal azole group, erythromycin, clarithromycin and nefazodone, and protease inhibitors;
• the age of 18 years (despite the fact that the efficacy and safety of the drug Seroquel Prolong in children and adolescents aged 10-17 years were studied in clinical trials).

With caution:

• cardiovascular and cerebrovascular diseases or other conditions predisposing to hypotension;
• advanced age;
• liver failure;
• a history of convulsive seizures.

Side effects

The most common side effects of Seroquel Prolong are drowsiness, dizziness, dry mouth, mild asthenia, constipation, tachycardia, orthostatic hypotension, and dyspepsia.

Taking the drug Seroquel Prolong, as well as other antipsychotic drugs, may be accompanied by an increase in body weight, syncope, the development of neuroleptic malignant syndrome, leukopenia, neutropenia and peripheral edema.

The frequency of adverse reactions is given in the following gradation: very often – ≥1/10; often – ≥1/100, <1/10; infrequently – ≥1/1000, <1/100; rarely – ≥1/10000, <1/1000; very rarely —

Prolongation of the QT interval, ventricular arrhythmia, sudden death, cardiac arrest, and bidirectional ventricular tachycardia are considered side effects inherent in antipsychotics.

The incidence of EPS in short-term clinical trials for schizophrenia and mania in the structure of bipolar disorder was comparable in the quetiapine and placebo group (patients with schizophrenia: 7.8% in the quetiapine group and 8% in the placebo group; mania in the structure of bipolar disorder: 11.2% in the quetiapine group and 11.4% in the placebo group).

The incidence of EPS in short-term clinical trials for depression in the structure of bipolar disorder in the quetiapine group was 8.9%, in the placebo group-3.8%. At the same time, the frequency of individual EPS symptoms (such as akathisia, extrapyramidal disorders, tremor, dyskinesia, dystonia, anxiety, involuntary muscle contractions, psychomotor agitation, and muscle rigidity) was generally low and did not exceed 4% in each of the treatment groups. In long-term clinical trials of quetiapine in schizophrenia and bipolar disorder, the incidence of EPS was comparable in the quetiapine and placebo groups.

Against the background of quetiapine therapy, a small dose-dependent decrease in the concentration of thyroid hormones, in particular total thyroxine (T4) and free T4, may occur. The maximum decrease in total and free T4 was recorded at the 2nd and 4th weeks of therapy with Seroquel Prolong, without further decrease in the concentration of hormones during long-term treatment. In almost all cases, the concentration of total and free T4 returned to the initial level after discontinuation of therapy with Seroquel Prolong, regardless of the duration of treatment. A slight decrease in total triiodothyronine (T3) and reverse T3 was observed only when using high doses. The concentration of thyroxine-binding globulin (TSH) remained unchanged, and there was no increase in TSH concentration.

Interaction

Caution should be exercised when using Seroquel Prolong in combination with other drugs that affect the central nervous system, as well as with alcohol.

The cytochrome P450 isoenzyme (CYP) 3 A 4 is the main isoenzyme responsible for the metabolism of quetiapine, which is carried out through the cytochrome P450 system. In a study in healthy volunteers, co-use of quetiapine (at a dose of 25 mg) with ketoconazole, a CYP3A4 inhibitor, resulted in a 5-8-fold increase in quetiapine AUC.

Therefore, the combined use of quetiapine and cytochrome CYP3A4 inhibitors is contraindicated. During quetiapine therapy, it is not recommended to eat grapefruit juice.

In a pharmacokinetic study, the use of quetiapine in various dosages before or simultaneously with carbamazepine led to a significant increase in quetiapine Cl and, accordingly, a decrease in AUC, on average by 13%, compared with quetiapine without carbamazepine. In some patients, the decrease in AUC was even more pronounced. This interaction was accompanied by a decrease in the concentration of quetiapine in plasma and could reduce the effectiveness of therapy with Seroquel® Prolong. Co-use of quetiapine with phenytoin, another inducer of the liver microsomal system, was accompanied by an even more pronounced (approximately 450%) increase in quetiapine clearance. Application of Seroquel® Prolongation in patients receiving inducers of the liver enzyme system is possible only if the expected benefit of therapy with Seroquel® Prolong exceeds the risk associated with discontinuation of the drug — inducer of liver enzymes. Changes in the dose of drugs that induce microsomal enzymes should be gradual. If necessary, they can be replaced with drugs that do not induce microsomal enzymes (for example, valproic acid preparations).

The pharmacokinetics of quetiapine were not significantly affected by concomitant use of the antidepressant imipramine (a CYP2D6 inhibitor) or fluoxetine (a CYP3A4 and CYP2D6 inhibitor).

The pharmacokinetics of quetiapine do not change significantly when co — administered with the antipsychotic drugs risperidone or haloperidol. However, co-use of quetiapine and thioridazine resulted in an increase in quetiapine Cl by approximately 70%.

The pharmacokinetics of quetiapine do not significantly change with concomitant use of cimetidine.

Lorazepam clearance decreases by approximately 20% with a single dose of 2 mg lorazepam and 250 mg quetiapine 2 times a day.

The pharmacokinetics of lithium preparations do not change with simultaneous use of quetiapine. There were no clinically significant changes in the pharmacokinetics of valproic acid and quetiapine with the combined use of seminodium valproate and quetiapine.

Pharmacokinetic studies on the interaction of Seroquel Prolong with drugs used for cardiovascular diseases have not been conducted.

Caution should be exercised when using Seroquel Prolong in combination with drugs that can cause electrolyte imbalance and prolong the QT interval.

Quetiapine did not induce induction of hepatic enzyme systems involved in phenazone metabolism.

False-positive results of screening tests for methadone and tricyclic antidepressants by enzyme-linked immunosorbent assay were observed in patients taking quetiapine. To confirm the results of screening, it is recommended to conduct a chromatographic study.

How to take, course of use and dosage

Inside, swallowing whole (without dividing, chewing or breaking),1 time a day separately from food.

Adults

Treatment of schizophrenia, moderate and severe manic episodes in the structure of bipolar disorder

Seroquel Prolong should be taken at least 1 hour before meals.

The daily dose for the first 2 days of therapy is: day 1-300 mg, day 2-600 mg. The recommended daily dose is 600 mg, but if necessary, it can be increased to 800 mg / day. Depending on the clinical effect and individual patient tolerance, the dose may vary from 400 to 800 mg / day. Maintenance therapy for schizophrenia does not require dose adjustment after relief of exacerbation.

Treatment of episodes of depression in the structure of bipolar disorder

Seroquel Prolong should be taken before bedtime. The daily dose for the first 4 days of therapy is: day 1-50 mg, day 2-100 mg, day 3-200 mg, day 4-300 mg. The recommended daily dose is 300 mg. Depending on the clinical effect and individual patient tolerance, the dose can be increased to 600 mg. The advantage of using the drug Seroquel Prolong in a daily dose of 600 mg compared to 300 mg was not revealed. Seroquel Prolong in a dose exceeding 300 mg should be prescribed by a doctor who has experience in the treatment of bipolar disorders.

Prevention of recurrent bipolar disorders in patients with previous effective therapy with quetiapine manic or depressive episodes in the structure of bipolar disorder

To prevent relapses of manic, depressive, and mixed episodes in bipolar disorders, patients who respond positively to treatment with Seroquel Prolong should continue therapy at the same daily dose as at the beginning of therapy. Seroquel Prolong should be taken before bedtime. Depending on the clinical effect and individual patient tolerance, the dose may vary from 300 to 800 mg / day. For maintenance therapy, it is recommended to use the minimum effective dose of Seroquel Prolong.

Transfer from taking Seroquel to taking Seroquel Prolong

For the convenience of admission, patients currently receiving fractional therapy with Seroquel can be transferred to taking Seroquel Prolong 1 time per day at a dose equivalent to the total daily dose of Seroquel. In some cases, you may need to adjust the dose.

Elderly patients

As with other antipsychotic agents, Seroquel Prolong should be used with caution in elderly patients, especially at the beginning of therapy. Selection of the effective dose of Seroquel Prolong in the elderly may be slower, and the daily therapeutic dose is lower than in young patients. The mean plasma Cl of quetiapine in elderly patients is 30-50% lower than in younger patients. In elderly patients, the initial dose of Seroquel Prolong is 50 mg / day. The dose can be increased by 50 mg per day until an effective dose is achieved, depending on the clinical response and tolerability of the drug by the individual patient.

Patients with renal insufficiency

No dose adjustment is required in patients with renal insufficiency.

Patients with hepatic insufficiency

Quetiapine is extensively metabolized in the liver. Therefore, caution should be exercised when using Seroquel Prolong in patients with hepatic insufficiency, especially at the beginning of therapy. It is recommended to start therapy with Seroquel Prolong at a dose of 50 mg / day and increase the dose daily by 50 mg until the effective dose is reached.

Overdose

Symptoms. A fatal outcome was reported with 13.6 g of quetiapine in a patient participating in a clinical study, as well as a fatal outcome after taking 6 g of quetiapine in a post-marketing study of the drug. At the same time, a case of taking quetiapine in a dose exceeding 30 g, without a fatal outcome, is described.

Extremely rare cases of quetiapine overdose have been reported, resulting in increased QT interval, death, or coma.

In patients with a history of severe cardiovascular disease, the risk of side effects from overdose may increase.

The symptoms reported in overdose were mainly due to an increase in the known pharmacological effects of the drug, such as drowsiness and sedation, tachycardia and a decrease in blood pressure.

Treatment.There are no specific antidotes to quetiapine. In cases of severe intoxication, you should be aware of the possibility of overdosing on several medications. It is recommended to carry out measures aimed at maintaining the function of respiration and the cardiovascular system, ensuring adequate oxygenation and ventilation. Gastric lavage (after intubation, if the patient is unconscious) and the use of activated charcoal and laxatives may contribute to the elimination of unabsorbed quetiapine, but the effectiveness of these measures has not been studied.

Close medical monitoring should continue until the patient’s condition improves.

Special instructions

Drowsiness

Somnolence and associated symptoms, such as sedation, may occur during therapy with Seroquel Prolong. In clinical studies involving patients with depression in the structure of bipolar disorder, drowsiness usually developed during the first three days of therapy. The severity of this side effect was generally minor or moderate. If severe drowsiness develops, patients with depression in the structure of bipolar disorder may need more frequent visits to the doctor within 2 weeks from the onset of drowsiness or until the severity of symptoms decreases. In some cases, it may be necessary to stop therapy with Seroquel Prolong.

Patients with cardiovascular diseases

Caution should be exercised when prescribing Seroquel Prolong to patients with cardiovascular and cerebrovascular diseases and other conditions predisposing to hypotension. Orthostatic hypotension may occur during therapy with Seroquel Prolong, especially during titration of the dose at the beginning of therapy. If orthostatic hypotension occurs, it may be necessary to reduce the dose or titrate it more slowly.

Dysphagia and aspiration were observed during therapy with Seroquel Prolong. A causal relationship between the occurrence of aspiration pneumonia and taking the drug Seroquel Prolong has not been established. However, caution should be exercised when prescribing the drug to patients at risk of aspiration pneumonia.

Convulsive seizures

There was no difference in the incidence of seizures in patients taking quetiapine or placebo. However, as with other antipsychotic drugs, caution is recommended when treating patients with a history of seizures.

Extrapyramidal symptoms

There was an increase in the incidence of EPS in adult patients with depression in the structure of bipolar disorder when taking quetiapine for depressive episodes compared to placebo. However, when quetiapine was used in patients with schizophrenia and mania, there was no increase in the incidence of EPS in the structure of bipolar disorder compared to placebo.

Tardive dyskinesia

If symptoms of tardive dyskinesia develop, it is recommended to reduce the dose of the drug or gradually cancel it. Symptoms of tardive dyskinesia may worsen or even occur after discontinuation of the drug.

Neuroleptic malignant syndrome

Neuroleptic malignant syndrome may develop while taking antipsychotic medications, including quetiapine. Clinical manifestations of the syndrome include hyperthermia, altered mental status, muscle rigidity, lability of the autonomic nervous system, and increased creatine phosphokinase activity. In such cases, it is necessary to stop taking the drug Seroquel Prolong and conduct appropriate treatment.

Severe neutropenia

In clinical studies of quetiapine, cases of severe neutropenia (neutrophil count) were infrequently reported. Most cases of severe neutropenia occurred several months after the start of quetiapine therapy. No dose-dependent effect was detected. Leukopenia and / or neutropenia resolved after quetiapine therapy was discontinued. A possible risk factor for neutropenia is a previous low white blood cell count and a history of drug-induced neutropenia. In patients with neutrophil counts The patient should be monitored for possible symptoms of infection and the neutrophil count should be monitored (up to 1.5·109/l).

Interaction with other medicinal products

The use of Seroquel Prolong in combination with powerful inducers of the liver enzyme system, such as carbamazepine and phenytoin, helps to reduce the concentration of quetiapine in plasma and may reduce the effectiveness of therapy with Seroquel Prolong.

use of Seroquel Prolong to patients receiving inducers of the liver enzyme system is possible only if the expected benefit of therapy with Seroquel Prolong exceeds the risk associated with discontinuation of the drug — inducer of liver enzymes. Changes in the dose of drugs that are inducers of microsomal enzymes should be gradual. If necessary, they can be replaced with drugs that do not induce microsomal enzymes (for example, valproic acid preparations).

Hyperglycemia

While taking quetiapine, hyperglycemia or exacerbation of diabetes mellitus may develop in patients with a history of diabetes mellitus. Clinical monitoring of patients with diabetes mellitus and patients with risk factors for developing diabetes mellitus is recommended.

Lipid concentration

While taking quetiapine, it is possible to increase the concentration of triglycerides and cholesterol and reduce the concentration of HDL.

Prolongation of the QT interval

There was no correlation between quetiapine intake and a persistent increase in the absolute value of the QT interval. However, prolongation of the QT interval was observed with an overdose of the drug. Caution should be exercised when prescribing quetiapine, as well as other antipsychotic drugs, to patients with cardiovascular diseases and previously observed prolongation of the QT interval. Caution should also be exercised when prescribing quetiapine concomitantly with drugs that prolong the QT interval_withother neuroleptics, especially in the elderly, patients with congenital QT prolongation syndrome, chronic heart failure, myocardial hypertrophy, hypokalemia or hypomagnesemia.

Acute reactions associated with drug withdrawal

When quetiapine is abruptly discontinued, the following acute reactions may occur (withdrawal syndrome): — nausea, vomiting, insomnia, headache, dizziness and irritability. Therefore, it is recommended to cancel the drug gradually, for at least one or two weeks.

Elderly patients with dementia

Seroquel Prolong is not indicated for the treatment of dementia-related psychoses.

Some atypical antipsychotics in randomized placebo-controlled trials increased the risk of developing cerebrovascular complications in patients with dementia by about 3 times. The mechanism of this increased risk has not been studied. A similar risk of increasing the frequency of cerebrovascular complications cannot be excluded for other antipsychotic drugs or other groups of patients. Seroquel Prolong should be used with caution in patients at risk of stroke.

An analysis of the use of atypical antipsychotics for the treatment of dementia-related psychoses in elderly patients revealed an increase in mortality in the group of patients treated with this group, compared with the placebo group. Two 10-week placebo-controlled trials of quetiapine in a similar group of patients (n=710; mean age: 83 years; age range: 56-99 years) showed that the mortality rate in the quetiapine group was 5.5%, in the placebo group — 3.2%. The causes of deaths reported in these patients were consistent with those expected for this population. There was no causal relationship between quetiapine treatment and the risk of increased mortality in elderly patients with dementia.

Suicide / suicidal thoughts or clinical deterioration

Depression is associated with an increased risk of suicidal thoughts, self-harm, and suicide (suicide-related events). This risk persists until the onset of severe remission. Due to the fact that it may take several weeks or more for the patient’s condition to improve from the start of treatment, patients should be closely monitored until improvement occurs. According to generally accepted clinical experience, the risk of suicide may increase in the early stages of remission.

Other psychiatric disorders for which quetiapine is prescribed are also associated with an increased risk of suicide-related events. In addition, such conditions may be comorbid with a depressive episode. Thus, the precautions used in the treatment of patients with a depressive episode should also be taken in the treatment of patients with other mental disorders.

Patients with a history of suicidal events, as well as patients who clearly express suicidal thoughts before starting therapy, are at an increased risk of suicidal intentions and suicide attempts and should be carefully monitored during treatment.

According to short-term placebo-controlled studies, for all indications and in all age groups, the incidence of suicide-related events was 0.9% for both quetiapine (61/6270) and placebo (27/3047).

In these studies, in patients with schizophrenia, the risk of suicide events was 1.4% (3/212) for quetiapine and 1.6% (1/62) for placebo in patients aged 18-24 years; 0.8% (13/1663) for quetiapine and 1.1% (5/463) for patients over 25 years; 1.4% (2/147) for quetiapine and 1.3% (1/75) for placebo in patients under 18 years.

In patients with mania in bipolar disorder, the risk of developing suicide-related events was 0% (0/67) for quetiapine and 0% (1/57) for placebo in patients aged 18-24 years; 1.2% (6/496) for quetiapine and 1.2% (6/503) for placebo in patients over 25 years; 1% (2/193) for quetiapine and 0% (0/90) for placebo in patients under 18 years of age (see “Special instructions”).

In depressed patients with bipolar disorder, the risk of suicide events was 3% (7/233) for quetiapine and 0% (0/120) for placebo in patients aged 18-24 years; 1.8% (19/1616) for quetiapine and 1.8% (11/622) for placebo in patients over 25 years. Studies involving patients with depression in bipolar disorder under the age of 18 years have not been conducted.

Seroquel Prolong can cause drowsiness, so during the treatment period, patients are not recommended to work with dangerous mechanisms, including driving vehicles.

Form of production

Film-coated long-acting tablets

Storage conditions

At a temperature not exceeding 30 °C.

Shelf life

3 years

Active ingredient

Quetiapine

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets