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The chemical composition of the drug Seroquel or Seroquel Prolong depends primarily on the form of release medicines A. One tablet of the above-mentioned drugs may contain 25, 50, 100, 150, 200, 300 or 400 mg. quetiapine (active substance).

The drug Seroquel also contains such auxiliary compounds as: calcium hydrogen phosphate, povidone, carboxymethyl starch, microcrystalline cellulose, lactose monohydrate, sodium carboxymethyl starch And Magnesium stearate .

The film coating of the tablets contains macrogol 400, titanium dioxide , and also hypromellose , and in some dosage forms the drug contains dyes, for example, yellow or red iron oxide.

In addition to the active compound, Seroquel Prolong contains quetiapine contains such auxiliary components as: lactose monohydrate, microcrystalline cellulose, sodium dihydrate, magnesium stearate , and also hypromellose . The film coating of the tablets contains titanium dioxide, macrogol, yellow or red iron oxide and hypromellose.

Release form

Covered film-coated Seroquel tablets differ not only in the amount of the medicinal compound they contain, but also in color. The manufacturer produces tablets pink color- 25 mg each. quetiapine (10 pieces in a blister, 3 or 6 blisters in a package), yellow - 100 mg each. quetiapine (10 pieces in a blister, 3,6 or 9 blisters in a package) and white - 200 mg each. quetiapine (10 pcs per blister, 3,6 or 9 blisters per package).

In addition, one package of a medicine may contain a combination different forms release of the drug, i.e. contains 6 tablets of 25 mg each, 3 tablets of 100 mg each. and 1 – 200 mg. An engraving is applied to one side of the tablets, which indicates the amount of the medicinal compound contained in one or another form of the drug - Seroquel 25, Seroquel WO and Seroquel 200.

The drug Seroquel Prolong is also available in tablet form. Depending on the shape medicinal release An oblong and biconvex tablet of this medicine, coated with a special film shell, can be engraved, which corresponds to the quantity quetiapine eg XR50, XR150, XR200, XR300 and XR400. As a rule, one blister contains 10 tablets of the drug, and one cardboard package contains 6 blisters.

Pharmacological action

Both drugs belong to antipsychotropic medications and have an effect on the body neuroleptic effect .

Pharmacodynamics and pharmacokinetics

Since both drugs belong to the group atypical antipsychotic drugs , they show affinity high degree in relation to serotonin receptors class 5HT2 , compared to brain dopamine receptors D1 and D2 . The drugs show similar properties in relation to adrenergic receptors And histamine receptors .

During scientific research the affinity of both drugs with benzodiazepine and cholinergic muscarinic receptors was not identified. When performing standard medical tests, drugs show their antipsychotic properties. Seroquel Prolong, like Seroquel, causes unexpressed catalepsy what entails blocking dopamine D2 receptors.

What happens next selective reduction in the activity of dopaminergic mesolimbic A10 neurons compared to those involved in motor functionnigrostriatal neurons . When using both drugs, blood levels do not increase prolactin. As a result of research, experts discovered the ability of these medications to combat symptoms and manifestations.

At orally drugs, the medicinal compounds included in their composition are quickly absorbed into stomach e, and then actively metabolized through liver . It is worth noting that on bioavailability of quetiapine are not affected by food, so both medications can be taken regardless of meals.

Both Seroquel Prolong and Seroquel are eliminated from the human body with feces , and also urine .

Indications for use

These drugs are indicated for:

• schizophrenia;
• chronic psychoses;
• manic states;
• bipolar disorders Oh.

Seroquel Prolong is also used for preventive purposes, for example, to prevent relapses of schizophrenic seizures at stable patients, and also bipolar disorders in patients who have previously successfully completed courses of treatment quetiapine . In addition, the drug is often included in complex treatment patients with suboptimal response to monotherapy using antidepressants .

Contraindications

Both drugs are contraindicated if patients have individual intolerance to certain components included in the chemical composition drugs, as well as lactase deficiency or when galactose intolerance , at malabsorption of glucose-galactose.

In addition, both medications are contraindicated in children under 18 years of age. Seroquel Prolong, like Seroquel, should be taken with extreme caution in elderly patients and people suffering from cerebrovascular and cardiovascular ailments or located towards hypotension , as well as those categories of patients whose medical history describes the risks of developing seizures, liver failure, aspiration pneumonia and .

Side effects of Seroquel

Among the most common side effects of Seroquel and Seroquel Prolong are the following:

• dispersion;
• dry mouth;
• orthostatic hypotension;
• increased levels of triglycerides, liver enzymes, and insulin in the blood.

Patients often gain weight in the first weeks of using medications. Quite rarely, however, when taking these medications, side effects may occur such as: convulsions, priapism, neuroleptic syndrome, dystonia, vegetative-vascular disorders, neutropenia, akathisia, and also leukopenia . With long-term use of drugs, it may develop tardive dyskinesia .

Instructions for use Seroquel Prolonga (Method and dosage)

Seroquel Prolong should be taken on an empty stomach; the tablets should not be chewed or broken. The dosage and duration of treatment with the drug depends on the type and severity of the disease, and, in addition, the health status of the patients should be taken into account. During treatment schizophrenia , and also bipolar disorders should be taken this medicine according to the following plan:

• 300 mg each. on the first day;
• 600 mg each. over the next two days.

During the treatment period depressive states Seroquel Prolong is taken according to the following regimen:

• 50 mg each. on the first day;
• 100 mg each. on the second day;
• then 200 mg. during the third day;
• then 300 mg. throughout the fourth day.

The recommended daily dosage of the drug is 300 mg. may be increased to 600 mg. By medical indications and in case of normal tolerability of the drug by patients. For preventive purposes, Seroquel Prolong is taken at night within a dose range of 300-800 mg.

Included complex therapy at suboptimal response patients for treatment antidepressants The drug is taken at 50 mg. the first two days, and then 150 mg. for another four days.

In accordance with the instructions for Seroquel, the drug is taken twice a day. The medication regimen, as well as the duration of the course of treatment, depends on the type of disease and the patient’s health condition.

During treatment schizophrenia, and also psychoses the drug is taken:

• 50 mg each. on the first day;
• 100 mg each. on the second day;
• 200 mg each. on the third day;
• 300 mg each. on the fourth day.

During treatment biopolar disorders , as well as manic-depressive states, Seroquel is taken according to the following scheme:

• 100 mg each. on the first day;
• 200 mg each. on the second day;
• 300 mg each. on the third day;
• 400 mg each. on the last fourth day.

Gradually, the therapeutic dose of the drug is increased and by the sixth day it can reach 800 mg.

Overdose

It is worth noting that if the recommendations for taking both medications are followed, cases of drug overdose are quite rare. However, in some cases, the consequences of an overdose were so incompatible with the lives of patients that they led to death or

If daily doses of drugs are exceeded, symptoms such as: drowsiness, decreased blood pressure, excessive sedation , and, in addition, in severe intoxication be carried out symptomatic treatment, as well as activities aimed at maintaining cardiovascular and respiratory systems human body.

Interaction

Increased concentration quetiapine , and, consequently, an increase in the effectiveness of both drugs may occur when taking Seroquel Prolong and Seroquel with antibiotics belonging to the group macrolides , and also with azole antifungals . Drug dosage adjustments may also be necessary if simultaneous use preparations with medicinal products containing phenytoin or called induce liver enzymes , For example,

Pharmacological action
Seroquel is an atypical antipsychotic drug. Seroquel contains the active ingredient quetiapine - medicinal substance, interacting with a number of neurotransmitter receptors. Quetiapine and its active metabolite interact with dopamine D1 and D2 receptors, serotonin 5HT2 receptors, and also have an affinity for the norepinephrine transporter.
The drug also has high affinity for histaminergic and alpha1-adrenergic receptors, as well as some affinity for alpha2-adrenergic receptors.
There is no significant effect of quetiapine on cholinergic muscarinic or benzodiazepine receptors.
Quetiapine is active in antipsychotic tests. The drug blocks the action of dopamine agonists (the effect has been proven behaviorally and electrophysiologically). Seroquel is effective in treating positive and negative symptoms schizophrenia.
When using doses that effectively block D2 receptors, quetiapine causes only mild catalepsy without significant extrapyramidal symptoms (in 3 placebo-controlled studies, the frequency of extrapyramidal symptoms with quetiapine and placebo was on average the same (excluding a study that used doses of 75-750 mg/day). day)).
Seroquel does not cause a significant and lasting increase in prolactin levels.
When using the drug Seroquel as monotherapy or in combination with other drugs, effectiveness has been demonstrated in manic symptoms in patients with bipolar disorders (using doses ranging from 400 to 800 mg per day).
During the research, it was revealed increased risk deaths in elderly patients with dementia prescribed quetiapine for psychosis (5.5% with quetiapine and 3.3% with placebo). The causes of death were different and characteristic of this population, a direct connection between taking the drug Seroquel and fatal has not been established, but the prescription of quetiapine to such patients should be carried out under the close supervision of a physician.
When taken orally, quetiapine is well absorbed from the intestine and is actively metabolized in the liver (with the participation of the cytochrome P450 system). About 83% of the dose taken is bound to plasma proteins.
The half-life of quetiapine is 7 hours, that of its active metabolite is 12 hours.
IN clinical studies The effectiveness of taking Seroquel twice a day has been proven (which is confirmed by the results of studies using positron emission tomography regarding the load of D2 and 5HT2 receptors).
Within therapeutic doses, the pharmacokinetics of Seroquel are linear. There are no differences between the pharmacokinetics of quetiapine in women and men.
On average, the clearance of quetiapine in elderly patients is 30-50% lower than in young and mature age. Also, a decrease in the clearance of quetiapine is observed in patients with impaired renal function (by an average of 25%) and liver.
About 5% of the dose taken is excreted unchanged. 73% of metabolites are excreted by the kidneys, 21% by the intestines.
Quetiapine in vitro slightly reduces the activity of cytochrome P450 enzymes 1A2, 2D6, 2C9, 3A4 and 2C19 (at doses 5-50 times higher than therapeutic).

Indications for use
Seroquel is used in the treatment of patients with schizophrenia.
Seroquel is also prescribed to patients with manic episodes associated with bipolar disorder.

Directions for use
Seroquel is taken orally. The tablets can be taken with or without food. sufficient quantity drinking water. It is recommended to divide the daily dose into 2 doses with an interval of 12 hours. The duration of treatment, the dose of quetiapine and the dosage regimen are determined by the doctor.
For schizophrenia, quetiapine is usually prescribed at 50 mg per day (first day of treatment), 100 mg quetiapine (second day of treatment), 200 mg (third day of treatment) and 300 mg (fourth day of treatment). After the fourth day, the dose is selected individually, taking into account the tolerability and effectiveness of the Seroquel drug.
The average therapeutic dose for schizophrenia is 300-450 mg of quetiapine per day (dose range from 150 mg to 750 mg of quetiapine per day).
For manic episodes due to bipolar disorders, 100 mg of quetiapine per day is prescribed at the beginning of therapy. The dose is increased by 100 mg daily for 4 days. If the daily dose of 400 mg is ineffective, it can be gradually increased to 800 mg per day (the dose should not be increased by more than 200 mg at a time).
Elderly patients should prescribe Seroquel with caution. The starting dose for patients over 65 years of age is 25 mg quetiapine per day.
For patients with impaired renal and liver function, quetiapine is prescribed at an initial dose of 25 mg per day. In such patients, the dose should not be increased by more than 25 mg at a time.
Discontinuation of the drug Seroquel should be carried out by gradually reducing the dose (over at least 2 weeks). If you abruptly stop taking Seroquel, you may develop a severe withdrawal syndrome (which is accompanied by vomiting, insomnia, dystonia, dyskinesia and akathisia).

Side effects
The most common undesirable effects when taking Seroquel are tachycardia, stool disorders, dizziness, drowsiness, dry mouth, dyspepsia, asthenia and orthostatic hypotension.
Same as when using others antipsychotics while taking the drug Seroquel, the development of neuroleptic malignant syndrome, neutropenia, leukopenia, syncope and peripheral edema is possible.
In addition, in in rare cases During treatment with Seroquel, patients experienced the following adverse events:
From the outside nervous system: headache, decreased visual acuity, extrapyramidal symptoms, loss of consciousness, convulsions, dysarthria, restless legs syndrome, dyskinesia.
From the outside laboratory parameters: increased transaminase levels, hyperglycemia, decreased neutrophil count, thrombocytopenia, eosinophilia, hypertriglyceridemia, increased gamma-GT levels, hypercholesterolemia, increased creatine phosphokinase levels.
Allergic reactions: rhinitis, urticaria, angioedema, anaphylactic shock, Stevens-Johnson syndrome.
Others: changes in body weight, dysphagia, hepatitis, priapism, jaundice.
Drowsiness usually develops in the first days of therapy and disappears after several weeks of regular use of quetiapine.
Leukopenia and neutropenia, which develop during therapy with Seroquel, are reversible and go away on their own after discontinuation of the drug.
During development unwanted effects It is necessary to consult a doctor as soon as possible, as some side effects require discontinuation of quetiapine.

Contraindications
Seroquel is contraindicated in patients with intolerance to quetiapine and other components of the drug.
Seroquel should not be prescribed to patients receiving azole-containing HIV protease inhibitors. antifungal agents, as well as nefazodone, erythromycin and clarithromycin (due to possible reduction quetiapine concentrations).
Seroquel is not used in pediatrics.
Seroquel should be prescribed with caution to patients suffering from diseases cardiovascular system, as well as cerebrovascular disorders with a risk of hypotension.
Elderly patients who receive medicines, potentially prolonging the QT interval, Seroquel is prescribed with caution.
Quetiapine is prescribed with caution in the presence of risk factors for stroke, as well as in those with a tendency to convulsive syndrome, a decrease in the number of leukocytes and neutropenia associated with taking medications (including when indicating a history of these conditions).
Seroquel is used with caution in patients with diabetes mellitus and risk factors for developing diabetes mellitus(during the period of therapy, regular monitoring of plasma glucose levels is necessary).
Seroquel is not the drug of choice for the treatment of psychosis associated with dementia.
While taking quetiapine, it is not recommended to drive unsafe machinery or a car (due to high risk development of drowsiness).

Pregnancy
There is no information on the use of Seroquel in pregnant women. It is possible to prescribe quetiapine to pregnant women only for health reasons and under the strict supervision of a doctor.
About the possibility of penetration active component There is no data on the drug Seroquel in breast milk. If it is necessary to use quetiapine during lactation, the issue of stopping breastfeeding should be decided.

Drug interactions
Ethyl alcohol and drugs that affect the central nervous system should not be used simultaneously with Seroquel.
There is a decrease in the clearance of quetiapine when combined with thioridazine.
Carbamazepine and other hepatic enzyme inducers, when used in combination with Seroquel, may lead to a decrease in plasma concentrations of quetiapine. It is recommended to monitor the level of quetiapine and, if necessary, adjust the dose while taking it with liver enzyme inducers (you should not take high doses of Seroquel for a long time; the maximum daily dose for the treatment of schizophrenia is 750 mg of quetiapine, for the treatment of bipolar disorders - 800 mg).

Overdose
Information on quetiapine overdose is limited. A case of taking more than 20 g of quetiapine without fatal consequences is described. Upon admission high doses of the drug Seroquel, patients experienced the development of sedation, drowsiness, arterial hypotension, reflex tachycardia, prolongation Q-T interval and coma.
A specific antidote for Seroquel is unknown. In case of severe intoxication, carry out intensive care, intubation and artificial respiration. If necessary, treatment is carried out aimed at eliminating the symptoms of quetiapine overdose.
It is necessary to monitor the patient's condition after taking high doses of Seroquel.

Release form
Film-coated tablets, Seroquel, 10 pieces in blister packs, 6 blister packs are placed in a cardboard pack.

Storage conditions
Seroquel should be kept away from direct sun rays at a temperature not exceeding 30 degrees Celsius.
The shelf life of Seroquel is 3 years.

Compound
1 tablet of Seroquel 25 contains:
Quetiapine fumarate (equivalent to quetiapine) – 25 mg;

1 tablet of Seroquel 100 contains:
Quetiapine fumarate (equivalent to quetiapine) – 100 mg;
Additional ingredients including milk sugar.

1 tablet of Seroquel 200 contains:
Quetiapine fumarate (equivalent to quetiapine) – 200 mg;
Additional ingredients including milk sugar.

Pharmacological group
Medicines acting primarily on the central nervous system
Psychotropic drugs
Antipsychotic, neuroleptic drugs

Active ingredient: Quetiapine

Instructions:

Clinical and pharmacological group

02.001 (Antipsychotic drug (neuroleptic))

Release form, composition and packaging

Pink, round, biconvex, film-coated tablets with "SEROQUEL 25" engraved on one side.

Shell composition: yellow iron oxide dye, titanium dioxide, hypromellose, macrogol 400.

Film-coated tablets white, round, biconvex, with "SEROQUEL 200" engraved on one side.

	1 tab.
quetiapine fumarate	230.26 mg,
which corresponds to the content of quetiapine	200 mg

Excipients: povidone, calcium hydrogen phosphate, microcrystalline cellulose, sodium carboxymethyl starch, lactose monohydrate, magnesium stearate.

Shell composition: titanium dioxide, hypromellose, macrogol 400.

10 pcs. - blisters (6) - cardboard packs.

Pharmacological action

Antipsychotic drug (neuroleptic). Shows higher affinity for serotonin 5HT2 receptors (compared to dopamine D1 and D2 receptors) in the brain. It also has a high affinity for histamine and α1-adrenergic receptors and is less active towards α2-adrenergic receptors. It has no affinity for m-cholinergic receptors and benzodiazepine receptors.

Showed antipsychotic activity in standard tests.

Results from studies of extrapyramidal symptoms in animals revealed that quetiapine causes only mild catalepsy when exposed to a dose that effectively blocks dopamine D2 receptors. Quetiapine selectively reduces the activity of mesolimbic A10-dopaminergic neurons compared to A9-nigrostriatal neurons involved in motor function.

Clinical studies (using quetiapine in doses of 75-750 mg/day) did not reveal differences between quetiapine and placebo in the incidence of extrapyramidal symptoms and concomitant use of anticholinergic drugs.

Seroquel does not cause a long-term increase in plasma prolactin levels. Multiple fixed-dose studies have shown no difference in prolactin levels between quetiapine and placebo.

In clinical studies, Seroquel has been shown to be effective in treating positive and negative symptoms of schizophrenia.

The effect of quetiapine on 5HT2 and D2 receptors lasts up to 12 hours after taking the drug.

Pharmacokinetics

Suction

At oral administration Quetiapine is well absorbed from the gastrointestinal tract.

Food intake does not significantly affect the bioavailability of quetiapine.

Distribution

Quetiapine is approximately 83% bound to plasma proteins.

The pharmacokinetics of quetiapine is linear, and no difference is observed between men and women.

Metabolism

Actively metabolized in the liver.

It has been established that the key enzyme in the metabolism of quetiapine is the CYP3A4 isoenzyme.

The main plasma metabolites do not have pronounced pharmacological activity.

Removal

T1/2 is approximately 7 hours. Less than 5% of quetiapine is not metabolized and is excreted unchanged by the kidneys or feces. Approximately 73% of quetiapine is excreted by the kidneys and 21% in the feces.

Pharmacokinetics in special clinical situations

The average clearance of quetiapine in elderly patients is 30-50% less than that observed in patients aged 18 to 65 years.

The average plasma clearance of quetiapine was approximately 25% less in patients with severe renal impairment (creatinine clearance less than 30 ml/min/1.73 m2) and in patients with liver damage (alcoholic cirrhosis in the compensation stage), but individual clearance levels were within the range , corresponding to healthy people.

In a study of the pharmacokinetics of quetiapine, when used at various doses, administering quetiapine before taking ketoconazole or concomitantly with ketoconazole resulted in an average increase in Cmax and AUC of quetiapine by 235% and 522%, respectively, as well as a decrease in quetiapine clearance by an average of 84%. T1/2 of quetiapine increased, but the average time to reach Cmax did not change.

Quetiapine and some of its metabolites have weak inhibitory activity against the isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, but only at concentrations 10-50 times higher than the concentrations observed at the commonly used effective dosage of 300-450 mg / day.

Based on in vitro results, coadministration of quetiapine with other drugs should not be expected to result in clinically significant inhibition of CYP-mediated metabolism of other drugs.

Dosage

Seroquel should be taken 2 times a day, regardless of meals.

For adults for the treatment of acute and chronic psychoses, including schizophrenia, the daily dose for the first 4 days of therapy is: 1st day - 50 mg, 2nd day - 100 mg, 3rd day - 200 mg, 4th day - 300 mg.

Depending on clinical effect and individual patient tolerance, the dose can vary from 150 mg to 750 mg/day. The maximum daily dose is 750 mg.

To treat manic episodes in bipolar disorder, quetiapine is used as monotherapy or as adjuvant therapy to stabilize mood.

Daily dose for the first 4 days of therapy is: 1st day - 100 mg, 2nd day - 200 mg, 3rd day - 300 mg, 4th day - 400 mg. Subsequently, by the 6th day of therapy, the daily dose of the drug can be increased to 800 mg. The increase in the daily dose should not exceed 200 mg/day.

Depending on the clinical effect and individual tolerance, the dose can vary from 200 mg to 800 mg/day. Typically, the effective dose is from 400 mg to 800 mg/day. The maximum daily dose is 800 mg.

For the treatment of depressive episodes in the structure of bipolar disorder, Seroquel is prescribed once a day at night. The recommended dose is 300 mg. The daily dose for the first 4 days of therapy is: 1st day - 50 mg, 2nd day - 100 mg, 3rd day - 200 mg, 4th day - 300 mg. The maximum daily dose is 600 mg. No clinical improvement was noted when the dose was increased to more than 600 mg.

In elderly patients, the initial dose is 25 mg/day. The dose should be increased daily by 25-50 mg until an effective dose is reached, which is likely to be less than in younger patients.

In patients with renal or liver failure It is recommended to start therapy with Seroquel at 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is achieved.

The safety and effectiveness of quetiapine have not been studied in children and adolescents.

Overdose

Data on overdose with Seroquel are limited. Cases of taking Seroquel in doses exceeding 20 g have been described, without fatal consequences and with full restoration, however, there are reports of extremely rare cases of overdose with Seroquel, leading to death or coma.

Symptoms: The symptoms noted were mainly due to an increase in known pharmacological effects drug, such as drowsiness and excessive sedation, tachycardia and decreased blood pressure.

Treatment: There are no specific antidotes to quetiapine. In cases of serious intoxication, consideration should be given to symptomatic therapy and it is recommended to carry out measures aimed at maintaining respiratory function, the cardiovascular system, ensuring adequate oxygenation and ventilation. Medical control and observation should be continued until full recovery patient.

Drug interactions

With the simultaneous administration of drugs that have a strong inhibitory effect on the CYP3A4 isoenzyme (such as antifungals of the azole group and macrolide antibiotics), plasma concentrations of quetiapine may increase. In such cases, more low doses Seroquel. Particular attention should be paid to elderly and debilitated patients. It is necessary to assess the risk-benefit ratio individually for each patient.

Co-administration of Seroquel with drugs that induce the liver enzyme system, such as carbamazepine, may reduce the plasma concentration of the drug, which may require an increase in the dose of Seroquel, depending on the clinical effect. In a study of the pharmacokinetics of quetiapine when used in different doses, when administered before or simultaneously with carbamazepine (an inducer of liver enzymes), a significant increase in the clearance of quetiapine is possible. This increase in quetiapine clearance decreased AUC by an average of 13% compared with quetiapine without carbamazepine.

The simultaneous administration of Seroquel with another inducer of microsomal liver enzymes (phenytoin) also led to an increase in the clearance of quetiapine. When quetiapine is co-administered with phenytoin (or other hepatic enzyme inducers such as barbiturates, rifampicin), an increase in the dose of quetiapine may be required. It may also be necessary to reduce the dose of Seroquel when discontinuing phenytoin or carbamazepine or another liver enzyme inducer or replacing it with a drug that does not induce liver microsomal enzymes (for example, sodium valproate).

The pharmacokinetics of lithium preparations does not change with the simultaneous administration of Seroquel.

Not noted clinically significant changes pharmacokinetics of valproic acid and quetiapine when administered together with divalproex sodium (sodium valproate and valproic acid in a 1:1 molar ratio) and quetiapine (quetiapine).

Quetiapine did not cause induction of hepatic enzyme systems involved in the metabolism of antipyrine.

The pharmacokinetics of quetiapine does not change significantly when administered concomitantly with the antipsychotic drugs risperidone or haloperidol. However simultaneous administration Seroquel and thioridazine increased the clearance of quetiapine.

The CYP3A4 isoenzyme is a key enzyme involved in the cytochrome P450-mediated metabolism of quetiapine. The pharmacokinetics of quetiapine does not change significantly with simultaneous use of cimetidine, which is an inhibitor of cytochrome P450.

The pharmacokinetics of quetiapine did not change significantly with simultaneous administration of the antidepressant imipramine (CYP2D6 inhibitor) or fluoxetine (CYP3A4 and CYP2D6 inhibitor). However, caution is recommended during the simultaneous use of Seroquel and the systemic use of strong inhibitors of the CYP3A4 isoenzyme (such as azole antifungals and macrolide antibiotics).

CNS depressants and ethanol increase the risk of developing side effects Seroquel.

Use during pregnancy and lactation

The safety and effectiveness of quetiapine in pregnant women have not been established. Therefore, Seroquel can be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus.

The extent to which quetiapine is excreted in human milk is unknown. Women should be advised not to breastfeed while taking Seroquel.

Side effects

From the central nervous system and peripheral nervous system: often - drowsiness (17.5%), dizziness (10%); rarely - malignant neuroleptic syndrome (hyperthermia, impaired consciousness, muscle rigidity, vegetative-vascular disorders, increased concentration of CPK); very rarely - convulsions. At long-term use There is a potential for development of tardive dyskinesia with Seroquel. If symptoms of tardive dyskinesia occur, the dose should be reduced or discontinued. further treatment Seroquel.

From the outside digestive system: often - constipation (9%), dyspepsia (6%), dry mouth (7%); an increase in the activity of liver enzymes (ALT, AST, GGT) in the blood serum (6%), as well as an increase in the concentration of cholesterol and triglycerides (with treatment with Seroquel, these changes were usually reversible).

From the cardiovascular system: often - orthostatic hypotension (accompanied by dizziness), tachycardia (7%), fainting; these adverse reactions mainly found in initial period dose selection.

From the hematopoietic system: rarely - leukopenia and/or neutropenia. There were no cases of severe neutropenia or agranulocytosis in patients taking Seroquel. When using Seroquel in clinical practice leukopenia and/or neutropenia resolved after discontinuation of the drug. Possible factors Risks for the development of leukopenia and/or neutropenia include a decrease in the number of leukocytes before the start of therapy or a history of leukopenia and/or neutropenia caused by taking medications.

From the outside endocrine system: Seroquel therapy is associated with a small dose-dependent decrease in hormone levels thyroid gland, in particular, total T4 and free T4. The maximum decrease in total and free T4 was recorded on the 2nd and 4th weeks of quetiapine therapy without a further decrease in hormone concentrations during long-term treatment. There were no further signs of clinically significant changes in thyroid-stimulating hormone concentrations. In almost all cases, the concentration of total and free T4 returned to baseline after cessation of quetiapine therapy, regardless of the duration of treatment.

Allergic reactions: rarely - eosinophilia, allergic reactions, including angioedema.

Other: rarely - peripheral edema, moderate asthenia, rhinitis, weight gain (mainly in the first weeks of treatment); very rarely - priapism.

Seroquel may cause prolongation of the QTc interval, the relationship between the use of Seroquel and constant increase No QTc detected.

The following frequently occurring (1/100) side effects were also reported: increased blood pressure, palpitations, dysarthria, pharyngitis, cough, anorexia, increased sweating. Cause-and-effect data side effects with taking Seroquel has not been established.

Storage conditions and periods

The drug should be stored out of the reach of children at temperatures below 30°C. Shelf life - 3 years.

Indications

- treatment of acute and chronic psychoses, including schizophrenia;

— treatment of manic episodes in the structure of bipolar disorder;

- treatment of depressive episodes of moderate to severe severity in the structure of bipolar disorder (for 8 weeks).

Contraindications

— joint use with cytochrome P450 inhibitors ( antifungal drugs azole groups, erythromycin, clarithromycin, nefazodone, protease inhibitors);

— increased sensitivity to any of the components of the drug.

Special instructions

Caution should be exercised when prescribing Seroquel to patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, as well as elderly patients, with liver failure, seizures in the anamnesis.

Seroquel may cause orthostatic hypotension, especially during the initial dose titration period (more common in older patients than in younger patients).

With abrupt withdrawal of high doses of antipsychotic drugs, the following acute reactions (withdrawal syndrome) may be observed: nausea, vomiting; rarely - insomnia.

Cases of exacerbation have been reported psychotic symptoms and the appearance of involuntary movement disorders(akathisia, dystonia, dyskinesia). Therefore, it is recommended to discontinue the drug gradually.

The occurrence of NMS may be associated with ongoing antipsychotic treatment. Clinical manifestation of the syndrome includes: hyperthermia, altered mental status, muscle rigidity, instability of the autonomic nervous system, increased CPK levels. In such cases, Seroquel should be discontinued and appropriate treatment administered.

There were no differences in the incidence of seizures in patients taking quetiapine or placebo. However, caution is recommended when treating patients with a history of seizures.

There was no relationship between quetiapine and an increase in the QTc interval. However, when prescribing quetiapine concomitantly with drugs that prolong the QTc interval, caution must be exercised, especially in the elderly.

Given that quetiapine primarily affects the central nervous system, quetiapine should be used with caution in combination with other drugs that have a central depressant effect or alcohol.

Impact on the ability to drive vehicles and operate machinery

Seroquel may cause drowsiness, so patients are not recommended to work with dangerous mechanisms, incl. Driving a car or other moving vehicles is not recommended.

Use for renal impairment

Use for liver dysfunction

In patients with liver failure, it is recommended to begin therapy with Seroquel at 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is achieved.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Registration numbers

. tab., cover film-coated, 200 mg: 60 pcs. P N013468/01 (2021-11-08 - 0000-00-00)
. tab., cover film-coated, 25 mg: 60 pcs. P N013468/01 (2021-11-08 - 0000-00-00)
. tab., cover film-coated, 100 mg: 60 pcs. P N013468/01 (2021-11-08 - 0000-00-00)

Neuroses, mental and personality disorders that lead to a weakening of the nervous system are disorders that many of us often have to deal with.

The drug Seroquel helps eliminate the symptoms of depression, manic episodes, and also normalizes general condition psyche.

Release forms and components

The drug is available in tablet form. They may differ in color and may also contain different quantities active component.

In pharmacies, the medicine can be found in the following forms:

1. Pink pills with dosage active substance 25 mg. They are contained in blisters of 10 pieces. One cardboard pack can contain 3 or 6 blisters.
2. Pills yellow with a dosage of 100 mg. Placed in blisters of 10 pieces, of which there can be 3, 6 or 9 pieces in one pack.
3. The tablets have a white structure with a dosage level of the active component of 200 mg. The tablets are packaged in blisters, each containing 10 tablets. One pack of cardboard material contains 3, 6 or 9 blisters.

The manufacturer also offers for purchase the drug Seroquel Prolong with increased amount active substance quetiapine fumarate (460 mg).

Quetiapine Fumarate Formula

There are drug packages on sale that contain combinations of tablets. For example, they may contain 6 tablets of 25 mg, 3 tablets of 100 mg and one tablet of 200 mg.

On one side of the tablet there must be an engraving that reflects the dosage level of the main component - Seroquel 25, Seroquel WO and Seroquel 200.

The main substance of the drug is quetiapine. Additional elements include:

• calcium hydrogen phosphate;
• lactose monohydrate;
• MCC, povidone;
• magnesium stearate;
• Macragol 400; hypromellose;
• titanium dioxide;
• carboxymethyl starch;
• sodium carboxymethyl starch;
• dyes and others.

Pharmacological properties

Seroquel is part of the group (antipsychotics), and refers to drugs that have an antipsychotic drug effect.

The active substance of the drug, quetiapine, interacts with neurotransmitter-type receptors in the brain.

The main substance of the drug has an increased similarity to serotonin receptors of the 5HT2 class compared to dopamine receptors of the brain D1 and D2. The medicine has similar qualities with adrenergic receptors and histamine receptors.

During standard studies, the drug showed antipsychotic activity. When used, unexpressed symptoms may develop. As a result, dopamine D2 receptors are blocked.

During clinical examinations It has been found that Seroquel may cause increased efficiency during therapeutic therapy positive and negative symptoms schizophrenic condition.

At internal use the main element quetiapine has high absorption internally gastrointestinal tract. Eating does not affect the bioavailability of the main element.

About 83% of the main constituent element binds to blood plasma proteins. The main metabolism occurs in the liver.

It is eliminated from the body within 14 hours. Almost 73% of the drug is excreted in the urine through the kidneys, almost 21% is excreted in the feces.

Indications and contraindications for use

You should not use the medication if you have the following conditions:

• in the presence of individual intolerance to the elements contained in the medication;
• It is not advisable to use in the presence of lactase deficiency and galactose intolerance;
• cannot be used by adolescents under 18 years of age;
• It is not advisable for women to use during pregnancy;
• during lactation.

Course of administration and dosage

The medication is used twice a day. Its use does not depend on food intake. The dosage level and duration of treatment therapy depend on the severity of the disease and should be determined by the attending physician.

During schizophrenic conditions and bipolar disorder, the medication should be used as follows:

• during the first day you need to use up to 300 mg of the active substance;
• over the next two days you need to take 600 mg.

The dose of 600 mg per day can be increased to 800 mg. But only if it is really necessary and supported by the attending physician.

During depression, the medication is used as follows:

• on the first day you need to take 50 mg;
• the next day the dose is increased to 100 mg;
• on the third day the dosage is increased to 200 mg;
• on the fourth day take 300 mg active ingredient.

If such a need suddenly arises, the optimal dose of 300 mg can be increased to 600 mg. But it should be increased only if it is really necessary.

For psychosis, the dosage of the drug per day can range from 150 mg and reach up to 750 mg.

During bipolar disorders manic phase It is recommended to use the medication as follows:

• during the first day it is recommended to take 100 mg;
• on the second day it is indicated to use 200 mg;
• during the third day, 300 mg is taken;
• 400 mg of the active ingredient for the fourth day.

In the subsequent period, the dosage of the medication is increased; already on the sixth day it should be 600 mg. Increasing the dose is recommended only if necessary. Usually the dose is set and increased by the doctor and only if the patient has normal tolerance to the drug.

Taking medication during pregnancy and breastfeeding

Since the effect of the drug when used during pregnancy has not been fully studied, it is not recommended for pregnant women to use it. The components of the medicine may have harmful effects on the child.

However, in some cases, the medicine may be prescribed in cases where the expected positive effect for the mother will be higher than expected harmful influence per child.

You should not use the medicine during lactation, as the components are excreted along with breast milk. It is best to stop breastfeeding at the time of treatment with the drug.

Overdose and side effects

If during use you strictly follow all recommendations and do not exceed the established dosages, then the symptoms of an overdose appear quite rarely. When using the drug in high doses, the following side symptoms may occur:

If such undesirable effects occur, symptomatic treatment should be carried out.

Some unpleasant side effects may occur when using the medicine. Among the frequent unpleasant symptoms The following conditions are noted:

• the appearance of dizziness;
• dispersion may be observed;
• problems with stool - constipation or diarrhea;
• the appearance of tachycardia;
• increased dryness in the mouth;
• the occurrence of orthostatic hypotension;
• in the blood composition there may be an increase in the level of triglycerides, liver enzymes, and insulin.

Sometimes neutropenia and leukopenia may appear.

Practical application experience

Review by a practitioner and reviews of those taking Seroquel.

Doctor Review

Seroquel is an antipsychotic drug that can quickly restore mental state, normalize the nervous system.

The use of the medicine is indicated during various mental disorders, manic states, schizophrenia, bipolar disorders, depression.

Typically, this drug is taken only under the supervision of a doctor and according to necessary scheme reception. For each condition there must be a specific regimen and dose. It is imperative that when using the drug, all dosages must be strictly observed, this will prevent the appearance of unpleasant symptoms of an overdose.

Psychotherapist

Patients' opinions

For a long time I fell into severe depression, could not sleep or work normally. As a result, I had to see a doctor, who, after an examination, prescribed Seroquel tablets, plus wrote a regimen for use.

Of course, when I read the instructions, I was immediately overcome with fear, there were so many side effects, but I still decided to start taking it. At first I noticed constant drowsiness and dizziness. But after a week everything went away.

But this medicine helped me think normally, sleep, all the symptoms of depression disappeared, and most importantly, joy and the desire to live appeared.

Elena, 45 years old

The doctor prescribed Seroquel for my husband to take. He had severe psychosis and depression. At that moment I didn’t care anymore, I was looking for any remedy that could restore my husband’s psyche, because living with him was very difficult.

I thought that this drug would have a bad effect on him, because there were too many side effects. But I noticed only two problems - with stool and dizziness. After just 6 months of taking it, my husband felt much better. Now he is a cheerful and happy person!

Lyudmila, 38 years old

Buying medicines and analogues

A package of tablets with a dosage of 25 mg and a quantity of 60 tablets costs about 1800-1900 rubles, the price of a package of Seroquel tablets with a dosage of 200 mg and a quantity of 60 tablets costs about 5800-5900 rubles, the following drug analogs are also available for purchase:

Film-coated tablets - 1 tablet:

quetiapine (in the form of fumarate) - 25/100/200 mg;
• excipients: povidone; dibasic calcium phosphate dihydrate; MCC; starch (sodium glycolate); lactose monohydrate; magnesium stearate;
• shell composition: red iron oxide (25 mg tablets); iron oxide yellow (25 and 100 mg tablets); titanium dioxide; hydroxypropyl methylcellulose; polyethylene glycol 400.

There are 10 pcs in a blister; in a cardboard pack there are 3 or 6 blisters (25 mg tablets); or in a cardboard pack of 3, 6 or 9 blisters (tablets 100 and 200 mg); or in a cardboard pack 1 blister (6 tablets of 25 mg, 3 tablets of 100 mg and 1 tablet of 200 mg).

Description of the dosage form

Tablet 25 mg: round, 6 mm in diameter, peach-colored, biconvex, film-coated.

Tablet 100 mg: round, 8.5 mm in diameter, yellow, biconvex, film-coated.

Tablet 200 mg: round, 11 mm in diameter, white, biconvex, film-coated.

Pharmacological action

Antipsychotic.

It has a higher affinity for serotonin 5HT2 receptors compared to dopamine D1 and D2 receptors in the brain, as well as a high affinity for histamine and alpha1 adrenergic receptors.

Pharmacokinetics

83% bound to plasma proteins. T1/2 - about 7 hours. Excreted in urine (73%) and feces (21%) in the form of inactive metabolites. Biotransformed with the participation of cytochrome P450.

Indications for use: Seroquel

Acute and chronic psychoses, including schizophrenia.

Contraindications to the use of Seroquel

Hypersensitivity.

Seroquel Use during pregnancy and children

Possibly if the expected effect of therapy exceeds the potential risk to the fetus. Breastfeeding should be stopped during treatment.

Seroquel Side Effects

From the cardiovascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, hypertension, tachycardia, leukopenia.

From the nervous system and sensory organs: drowsiness, dizziness, anxiety, rarely - neuroleptic malignant syndrome.

Metabolic: increased levels of cholesterol, serum triglycerides, ALT and AST, changes in the level of liver enzymes.

From the gastrointestinal tract: dry mouth, diarrhea or constipation, dyspepsia.

From the outside skin: rash, dry skin.

Others: pain syndrome(abdominal, headache, lower back, muscle pain, chest, ear), asthenia, rhinitis, infections urinary tract, fever, weight gain.

Drug interactions

The effect is weakened by inducers of microsomal liver enzymes (phenytoin, carbamazepine, barbiturates, rifampicin) and thioridazine (increases Cl).

Seroquel dosage

Orally, regardless of meals, 2 times a day.

Adults. The daily dose for the first 4 days of therapy is: on the first day - 50 mg, on the second day - 100 mg, on the third day - 200 mg, on the 4th day - 300 mg. Beginning on day 4, the dose should be titrated to the usually effective dosage, ranging from 300 to 450 mg/day. Depending on the clinical effect and individual patient tolerance, the dose can vary from 150 to 750 mg/day.

Elderly. Like other antipsychotic drugs, Seroquel should be used with caution in the elderly, especially during the initial period of therapy. In elderly patients, the initial dose of quetiapine should be 25 mg per day. The dose should be increased daily by 25 to 50 mg until an effective dose is reached, which is likely to be less than in younger patients.

The safety and effectiveness of quetiapine have not been studied in children and adolescents.

In patients with impaired liver and kidney function, Seroquel therapy should begin with a dose of 25 mg/day. The dose should be increased daily by 25–50 mg until an effective dose is reached.

Overdose

Symptoms: drowsiness, sedative effect, tachycardia, hypotension.

Treatment: symptomatic; restoration and control of patency of the upper respiratory tract, ensuring adequate oxygenation and ventilation, monitoring and maintaining the activity of the cardiovascular system.

Precautions

Caution should be exercised when combining with other drugs that have central activity, with alcohol, as well as when combined with potential biotransformation inhibitors - ketoconazole, erythromycin, etc.