Medicinal reference book geotar. Quetiapine is a leader in the treatment of bipolar disorder, depression and schizophrenia

Quetiapine: instructions for use and reviews

Latin name: Quetiapine

ATX Code: N05AH04

Active substance: quetiapine (quetiapine)

Producer: Technology of drugs (Russia), Canonpharma production, CJSC (Russia), North Star (Russia), VERTEKS, AO (Russia)

Description and photo update: 21.11.2018

Quetiapine is an antipsychotic drug.

Release form and composition

Dosage form - film-coated tablets: round biconvex, core and shell of almost white or white color (in a carton pack 1 glass, polyethylene or polymer jar / bottle of 30, 60 or 90 pieces or 1-4, 6 blister packs 10, 15, 20 or 30 pieces).

Composition of 1 tablet:

active substance: quetiapine (in the form of fumarate) - 25, 100, 150, 200 or 300 mg;
excipients (25/100/150/200/300 mg): microcrystalline cellulose - 8.718/34.87/0/69.74/104.61 mg; lactose monohydrate - 4.5/18/30/36/54 mg; sodium starch glycolate - 3.5/14/21/28/42 mg; povidone K-30 - 2/8/12/16/24 mg; talc - 1.25/5/0/10/15 mg; colloidal silicon dioxide - 0.75/3/0/6/9 mg; magnesium stearate - 0.5/2/0/4/6 mg; calcium hydrophosphate dihydrate - 0/0/46, 32/0/0 mg; potato starch - 0/0/15/0/0 mg; calcium stearate -0/0/3/0/0 mg;
film shell (25/100/200/300 mg): (hypromellose - 0.9 / 3.6 / 7.2 / 10.8 mg; talc - 0.3 / 1.2 / 2.4 / 3.6 mg; titanium dioxide - 0.165 / 0.66 / 1.32 / 1.98 mg; macrogol 4000 - 0.135 / 0.54 / 1.08 / 1.62 mg) or (dry mixture for film coating containing: hypromellose - 60%, talc - 20%, titanium dioxide - 11%, macrogol 4000 - 9%) - 1.5/6/12/18 mg;
film shell (150 mg): Aquarius Prime BAP21S010 white (hypromellose - 65%; titanium dioxide - 25%; macrogol - 10%) - 9 mg.

Pharmacological properties

Pharmacodynamics

Quetiapine is one of the atypical antipsychotics. Shows a higher affinity for hydroxytryptamine (serotonin) receptors (5HT2) than for dopamine receptors D1 and D2 of the brain. It also has a more pronounced affinity for histamine and alpha1-adrenergic receptors and less for alpha2-adrenergic receptors.

A noticeable affinity of quetiapine for benzodiazepine and muscarinic receptors was not found. In standard tests, it exhibits antipsychotic activity.

Pharmacokinetics

Quetiapine when administered orally is well absorbed from the gastrointestinal tract and is actively metabolized in the liver. The main metabolites in plasma do not have pronounced pharmacological activity.

Eating does not have a significant effect on the biological activity of the substance. T 1/2 (half-life) - approximately 7 hours. Approximately 83% of the substance binds to plasma proteins.

Differences in pharmacokinetic parameters in women and men are not observed. Pharmacokinetics is linear.

In elderly patients, the average clearance of quetiapine is less than in patients aged 18–65 years by 30–50%.

In severe renal insufficiency (creatinine clearance up to 30 ml / min / 1.73 m 2) and liver damage, the average plasma clearance of quetiapine is less than about 25%, but inter-individual clearance rates are within the range that correspond to healthy volunteers. About 21% is excreted in the feces, 73% in the urine. Less than 5% of the substance is not metabolized (excreted by the kidneys or with feces unchanged). It has been established that CYP3A4 is a key isoenzyme of quetiapine metabolism.

In a study of the pharmacokinetic parameters of quetiapine at various doses, it was found that its use before taking ketoconazole or simultaneously with it leads to an increase, on average, Cmax (maximum concentration of the substance) and AUC (area under the concentration-time curve) of quetiapine by 235% and 522% respectively. In addition, there is a decrease in the clearance of quetiapine, on average, by 84%. T 1/2 increases, but the time to reach Cmax does not change.

Quetiapine and some of its metabolites have a weak inhibitory activity against cytochrome P450 isoenzymes 1A2, 2C9, 2C19, 2D6 and ZA4, but only in cases where the concentration is 10-50 times higher than the usual therapeutic (300-450 mg per day).

It should not be expected that with the simultaneous use of quetiapine with other drugs, a clinically significant inhibition of cytochrome P450-mediated metabolism of other drugs will be observed.

Indications for use

acute and chronic psychoses, including schizophrenia;
manic episodes in the structure of bipolar disorder.

Contraindications

Absolute:

combined use with CYP3A4 inhibitors - clarithromycin, HIV protease inhibitors, erythromycin, azole antifungal drugs, nefazodone;
lactation period;
age up to 18 years;
individual intolerance to the components of the drug.

Relative (Quetiapine is prescribed under medical supervision):

cardiovascular and cerebrovascular diseases or other conditions predisposing to the development of arterial hypotension;
burdened history of convulsive seizures;
liver failure;
elderly age;
pregnancy.

Instructions for use Quetiapine: method and dosage

The tablets are intended for oral administration.

The recommended daily dose in the treatment of acute and chronic psychoses, including schizophrenia, from the first to the fourth day of therapy is 50, 100, 200 and 300 mg, respectively. In the future, the dose should be adjusted to clinically effective, which is usually in the range of 300-450 mg per day. Depending on individual tolerance and clinical effect, the daily dose may vary from 150 to 750 mg (maximum).

For the treatment of manic episodes in the structure of bipolar disorder, quetiapine can be used as a monotherapy drug or as part of adjuvant therapy to stabilize mood. From the first to the fourth day of therapy, the daily dose of Quetiapine is 100 mg, 200 mg, 300 mg and 400 mg, respectively. In the future, by the sixth day of admission, it is possible to increase the daily dose to 800 mg (the maximum allowable single increase in the daily dose is 200 mg).

The effective daily dose is usually 400-800 mg. Depending on individual tolerance and clinical effect, the daily dose may vary in the range of 200–800 mg (maximum).

The initial dose of Quetiapine in elderly patients, as well as in renal / hepatic insufficiency, is 25 mg per day. The dose should be increased daily by 25-50 mg until an effective one is achieved.

Side effects

Most often (in 6-17.5% of cases) while taking Quetiapine, the following disorders develop: dizziness, drowsiness, dyspepsia, constipation, tachycardia, orthostatic hypotension, dry mouth, increased activity of liver enzymes in the blood serum, plasma increase in triglycerides and blood cholesterol.

Therapy may be accompanied by the occurrence of moderate asthenia, dyspepsia and rhinitis, weight gain (mainly in the first weeks of treatment). Quetiapine can cause orthostatic hypotension accompanied by dizziness, tachycardia and, in some cases, syncope. Violations occur mainly in the initial period of dose selection.

Quetiapine is associated with a slight dose-dependent decrease in thyroid hormone concentrations, in particular total and free T4. The maximum decrease in indicators is recorded on the second and fourth weeks of treatment. In the future, with prolonged use, a decrease in the concentration of hormones is not observed.

With long-term therapy, there is a potential for the appearance of tardive dyskinesia. With the development of symptoms of the disease, the dose should be reduced or the use of the drug should be discontinued. With the abrupt cancellation of Quetiapine in high doses, the following acute reactions (withdrawal syndrome) may develop: vomiting, nausea, and in rare cases, insomnia.

During the use of the drug, psychotic symptoms may worsen and involuntary movement disorders appear, manifested in the form of dystonia, akathisia, dyskinesia (Quetiapine should be discontinued gradually).

Possible negative side reactions:

cardiovascular system: tachycardia, orthostatic hypotension, prolongation of the QT interval;
nervous system: tremor, asthenia, anxiety, drowsiness, dizziness, headache, hostility, agitation, insomnia, akathisia, convulsions, depression, paresthesia, restless legs syndrome, neuroleptic malignant syndrome (in the form of hyperthermia, muscle rigidity, changes in mental status, lability autonomic nervous system, increased activity of creatine phosphokinase);
respiratory system: rhinitis, pharyngitis;
digestive system: hepatitis, dryness of the oral mucosa, vomiting, nausea, abdominal pain, constipation / diarrhea, jaundice, increased activity of hepatic transaminases;
laboratory parameters: hyperglycemia, neutropenia, leukopenia, hypertriglyceridemia, hypercholesterolemia, decrease in T4 concentration;
allergic reactions: angioedema, eosinophilia, anaphylactic reactions, skin rash, Stevens-Johnson syndrome;
others: galactorrhea, visual impairment (including blurred vision), chest and lower back pain, low-grade fever, weight gain (mainly in the first weeks of taking Quetiapine), priapism, dry skin, myalgia, decompensation of existing diabetes mellitus.

Overdose

There are limited data on quetiapine overdose. Cases of taking more than 20,000 mg of the drug are described, after which fatal consequences did not develop and a complete recovery was observed. However, there are reports of extremely rare cases of overdose, which led to coma and death.

Overdose symptoms may be due to an increase in the pharmacological effects of Quetiapine - drowsiness, excessive sedation, tachycardia and lowering blood pressure.

There is no specific antidote. Treatment is symptomatic. In cases of overdose, the following measures are indicated: gastric lavage (after intubation, in cases where the patient is unconscious), taking laxatives and activated charcoal (in order to remove unabsorbed Quetiapine). The effectiveness of these measures has not been studied. Measures are also needed that are aimed at maintaining the function of the cardiovascular system, respiration, ensuring adequate ventilation and oxygenation. Medical supervision should be continued until complete recovery.

special instructions

Reception of Quetiapine can lead to the development of orthostatic hypotension, especially in the initial period of dose selection (in older patients, the disorder occurs more often than in young patients). The relationship between taking the drug and an increase in QTc (QT interval corrected for heart rate) has not been identified. However, when combined with drugs that prolong the QTc interval, care must be taken, especially in elderly patients. With a decrease in the number of neutrophils less than 1000 / μl, Quetiapine is canceled.

The drug is not intended for the treatment of dementia-related psychosis. In cases of development of symptoms of tardive dyskinesia, the dose of Quetiapine should be reduced. A complete gradual withdrawal of therapy is also possible. After discontinuation of the drug, the appearance / strengthening of symptoms of tardive dyskinesia is possible.

If neuroleptic malignant syndrome occurs, treatment should be discontinued.

Quetiapine should be used with caution in combination with other central nervous system depressants or alcohol.

Therapy in children, adolescents and patients under 24 years of age with depression and other mental disorders may cause suicidal thoughts / behavior. Before prescribing the drug to this age group of patients, it is necessary to correlate the expected benefit with the possible risk. All patients should be monitored for early detection of behavioral disturbances/changes, as well as suicidal tendencies.

Influence on the ability to drive vehicles and complex mechanisms

While taking Quetiapine, patients are advised to refuse to drive vehicles, which is associated with the likelihood of drowsiness.

Use during pregnancy and lactation

pregnancy: the drug can be used under medical supervision;
lactation period: therapy is contraindicated.

Application in childhood

Quetiapine therapy is contraindicated in patients under 18 years of age.

For impaired renal function

According to the instructions, Quetiapine should be used with caution in patients with renal insufficiency at a reduced initial dose (25 mg per day).

For impaired liver function

The drug in patients with hepatic insufficiency should be administered with caution at a reduced initial dose (25 mg per day).

Use in the elderly

Quetiapine should be used with caution in elderly patients at a reduced starting dose (25 mg daily).

drug interaction

Possible interactions:

azole antifungal agents, clarithromycin, erythromycin, nefazodone (drugs with a strong inhibitory effect on the CYP3A4 isoenzyme): an increase in the plasma concentration of quetiapine (the combination is not recommended);
carbamazepine: a decrease in the plasma concentration of quetiapine, as a result of which an increase in its dose may be required (depending on the clinical effect); the same changes are observed when combined with phenytoin; when canceling inducers of the liver enzyme system or replacing it with a drug that does not induce microsomal liver enzymes (in particular, valproic acid), the dose of quetiapine should be adjusted;
thioridazine: increased clearance of quetiapine;
drugs that depress the central nervous system and ethanol: an increase in the likelihood of adverse reactions to quetiapine.

Analogues

Quetiapine's analogues are Servitel, Kvetiteks, Ketiap, Ketilept, Kventiax, Victoel, Seroquel, Kumental, Lakvel, Nantarid, Gedonin.

Terms and conditions of storage

Store in a place protected from light and moisture, at temperatures up to 25 °C. Keep away from children.

Shelf life - 2 years.

pharmachologic effect

Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin (hydroxytryptamine) receptors (5HT2) than for dopamine D1 and D2 receptors in the brain. Quetiapine also has a more pronounced affinity for histamine and alpha 1 -adrenergic receptors and less for alpha 2 -adrenergic receptors. No significant affinity for quetiapine for muscarinic and benzodiazepine receptors was found. In standard tests, quetiapine exhibits antipsychotic activity.

Pharmacokinetics

When administered orally, quetiapine is well absorbed from the gastrointestinal tract and extensively metabolized in the liver. The main metabolites in plasma do not have a pronounced pharmacological activity.

Food intake does not significantly affect the bioavailability of quetiapine. T 1/2 is about 7 hours. Approximately 83% of quetiapine binds to plasma proteins.

The pharmacokinetics of quetiapine is linear, there are no differences in pharmacokinetic parameters in men and women.

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

The mean plasma clearance of quetiapine is less than approximately 25% in patients with severe renal insufficiency (creatinine clearance less than 30 ml / min / 1.73 m 2) and in patients with liver damage, but inter-individual clearance rates are in the range corresponding to healthy volunteers. Approximately 73% of quetiapine is excreted in the urine and 21% in the faeces. Less than 5% of quetiapine is not metabolized and is excreted unchanged by the kidneys or faeces. It has been established that CYP3A4 is a key isoenzyme of quetiapine metabolism mediated by cytochrome P450.

In a study of the pharmacokinetics of quetiapine at various doses, the use of quetiapine before taking ketoconazole or simultaneously with ketoconazole led to an increase, on average, C max and area under the concentration-time curve (AUC) of quetiapine by 235% and 522%, respectively, as well as to a decrease in the clearance of quetiapine, on average, by 84%. T 1/2 quetiapine increased, but T max did not change.

Quetiapine and some of its metabolites have weak inhibitory activity against cytochrome P450 isoenzymes 1A2, 2C9, 2C19, 2D6 and 3A4, but only at a concentration 10-50 times higher than the concentration observed at the commonly used effective dose of 300-450 mg / day.

Based on in vitro results, co-administration of quetiapine with other drugs should not be expected to result in clinically significant inhibition of cytochrome P450-mediated metabolism of other drugs.

Indications

- acute and chronic psychoses, including schizophrenia;

- manic episodes in the structure of bipolar disorder.

Dosing regimen

Adults:

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. Starting on day 4, the dose should be adjusted to a clinically effective dose, which is usually in the range of 300 to 450 mg/day. Depending on the clinical effect and individual tolerability, the dose may vary from 150 to 750 mg / day.

Treatment of manic episodes in the structure of bipolar disorder

Quetiapine is used as monotherapy or as adjuvant therapy for mood stabilization.

The 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. In the future, by the 6th day of therapy, the daily dose of the drug can be increased to 800 mg. An increase in the daily dose should not exceed 200 mg per day.

Depending on the clinical effect and individual tolerance, the dose may vary from 200 to 800 mg / day. Usually an effective dose is from 400 to 800 mg / day.

For treatment schizophrenia the maximum recommended daily dose of quetiapine is 750 mg, for the treatment of manic episodes in the structure of bipolar disorder, the maximum recommended daily dose of quetiapine is 800 mg / day.

In elderly patients

In patients with renal or hepatic insufficiency

Side effect

The most common adverse reactions associated with taking the drug: drowsiness (17.5%), dizziness (10%), constipation (9%), dyspepsia (6%), orthostatic hypotension and tachycardia (7%), dry mouth (7% ), an increase in the activity of "liver" enzymes in the blood serum (6%), an increase in the concentration of cholesterol and triglycerides in the blood plasma.

Taking quetiapine may be accompanied by the development of moderate asthenia, rhinitis and dyspepsia, weight gain (mainly in the first weeks of treatment). Quetiapine can cause orthostatic hypotension (accompanied by dizziness), tachycardia and, in some patients, syncope; these adverse reactions mainly occur in the initial period of dose selection (see section "Special Instructions"). Therapy with quetiapine is associated with a small dose-dependent decrease in the concentration of thyroid hormones, in particular, total T4 and free T4. The maximum decrease in total and free T4 was registered at the 2nd and 4th weeks of quetiapine therapy, without further decrease in hormone concentrations during long-term treatment. Subsequently, there were no signs of clinically significant changes in the concentration of thyroid-stimulating hormone.

With prolonged use of quetiapine, there is a potential for the development of tardive dyskinesia. If symptoms of tardive dyskinesia occur, the dose should be reduced or further treatment with quetiapine should be discontinued. With the abrupt cancellation of high doses of antipsychotic drugs, the following acute reactions (withdrawal syndrome) may occur: nausea, vomiting, and rarely, insomnia.

There may be cases of exacerbation of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia). In this connection, the abolition of the drug is recommended to be carried out gradually.

The following are the adverse reactions observed with the use of quetiapine and distributed by organs and systems:

From the side of the nervous system: drowsiness, dizziness, headache, anxiety, asthenia, hostility, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesia, neuroleptic malignant syndrome (hyperthermia, muscle rigidity, changes in mental status, lability of the autonomic nervous system, increased activity of creatine phosphokinase) , restless leg syndrome.

From the side of the cardiovascular system: orthostatic hypotension, tachycardia, prolongation of the QT interval.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, diarrhea or constipation, increased activity of "liver" transaminases, jaundice, hepatitis.

From the respiratory system: pharyngitis, rhinitis.

Allergic reactions: skin rash, eosinophilia, angioedema, Stevens-Johnson syndrome, anaphylactic reactions.

Laboratory indicators: leukopenia, neutropenia, hypercholesterolemia, hypertriglyceridemia, decreased T4 concentration (first 4 weeks), hyperglycemia.

Others: back pain, chest pain, low-grade fever, weight gain (mainly in the first weeks of treatment), myalgia, dry skin, visual impairment, incl. blurred vision, decompensation of existing diabetes mellitus, priapism, galactorrhea.

Contraindications for use

Hypersensitivity to any of the components of the drug;

Concurrent use with CYP3A4 inhibitors such as HIV protease inhibitors, azole antifungals, erythromycin, clarithromycin, nefazodone;

Children's age up to 18 years;

lactation period.

Carefully use in patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension; in old age; with liver failure; convulsive seizures in history; pregnancy.

Use during pregnancy and lactation

Use with caution during pregnancy. Contraindicated during lactation.

Use in children

Contraindicated in children and adolescents under 18 years of age.

Overdose

Data on quetiapine overdose are limited. Cases of taking quetiapine at a dose exceeding 20 g are described without fatal consequences and with complete recovery, however, there are reports of extremely rare cases of overdose of quetiapine, leading to death or coma.

Symptoms may be due to an increase in the known pharmacological effects of the drug, such as drowsiness and excessive sedation, tachycardia and a decrease in blood pressure.

Treatment: There are no specific antidotes for quetiapine. In cases of overdose, gastric lavage (after intubation, if the patient is unconscious), administration of activated charcoal and laxatives to remove unabsorbed quetiapine is possible, however, the effectiveness of these measures has not been studied. Symptomatic therapy and measures aimed at maintaining the function of respiration, the cardiovascular system, ensuring adequate oxygenation and ventilation are shown. Medical control and observation should be continued until the patient has fully recovered.

drug interaction

With the simultaneous use of drugs that have a strong inhibitory effect on the CYP3A4 isoenzyme (such as antifungal agents of the azole group and erythromycin, clarithromycin, nefazodone), the plasma concentration of quetiapine increases, so their simultaneous administration with quetiapine is contraindicated. With the simultaneous use of quetiapine with drugs that induce the liver enzyme system, such as carbamazepine, a decrease in the plasma concentration of the drug is possible, which may require an increase in the dose of quetiapine, depending on the clinical effect. In a study of the pharmacokinetics of quetiapine at various doses, when it was used before or simultaneously with carbamazepine (an inducer of liver enzymes), it resulted in a significant increase in the clearance of quetiapine. This increase in quetiapine clearance reduced AUC by an average of 13% compared with quetiapine without carbamazepine. The simultaneous use of quetiapine with another inducer of microsomal liver enzymes, phenytoin, also led to an increase in the clearance of quetiapine. With the simultaneous use of quetiapine and phenytoin (or other inducers of liver enzymes, such as barbiturates, rifampicin), an increase in the dose of quetiapine may be required. It may also be necessary to reduce the dose of quetiapine when phenytoin or carbamazepine or another inducer of the liver enzyme system is canceled or replaced with a drug that does not induce microsomal liver enzymes (for example, valproic acid).

The pharmacokinetics of lithium preparations does not change with the simultaneous use of 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 used simultaneously with antipsychotic drugs - risperidone or haloperidol. However, the simultaneous administration of quetiapine and thioridazine led to an increase in the clearance of quetiapine. CYP3A4 is a key enzyme involved in the cytochrome P450-mediated metabolism of quetiapine. The pharmacokinetics of quetiapine does not change significantly with the simultaneous use of cimetidine, which is a P450 inhibitor.

The pharmacokinetics of quetiapine did not change significantly with the simultaneous use of imipramine (CYP2D6 inhibitor) or fluoxetine (CYP3A4 and CYP2D6 inhibitor). CNS depressants and ethanol increase the risk of side effects of quetiapine.

Terms and conditions of storage

Keep out of the reach of children, dry, dark place at a temperature not exceeding 25 °C.

Shelf life - 2 years.

Application for violations of liver function

In patients with liver failure it is recommended to start quetiapine therapy with 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is reached.

Application for violations of kidney function

In patients with renal insufficiency it is recommended to start quetiapine therapy with 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is reached.

Use in elderly patients

In elderly patients the initial dose of quetiapine 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.

special instructions

Quetiapine can cause orthostatic hypotension, especially during the initial dose selection period (in elderly patients it is more common than in young patients). There was no relationship between taking quetiapine and an increase in QTc-interval. However, when using quetiapine concomitantly with drugs that prolong the QTc interval, care must be taken, especially in the elderly. During treatment with a decrease in the number of neutrophils less than 1000 / µl, quetiapine should be discontinued.

With the development of orthostatic hypotension during treatment with the drug, it is necessary to reduce the dose or titrate doses more slowly. The drug is not indicated for the treatment of psychosis associated with dementia. In the event of the development of symptoms of tardive dyskinesia, the dose of the drug should be reduced or the drug should be gradually discontinued. Symptoms of tardive dyskinesia may worsen or even appear after discontinuation of the drug.

In the event of the development of a malignant neuroleptic syndrome, the drug must be discontinued.

Given that quetiapine mainly affects the central nervous system, the drug should be used with caution in combination with other drugs that depress the central nervous system, or alcohol. In children, adolescents, and young people (under 24 years of age) with depression and other psychiatric disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing Quetiapine or any other antidepressants in children, adolescents and young people (under 24 years of age), the risk of suicide should be correlated with the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, and slightly decreased in people over 65 years of age. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of violations or changes in behavior, as well as suicidal tendencies.

Influence on the ability to drive vehicles and control mechanisms

Quetiapine can cause drowsiness, therefore, during the period of treatment, patients are advised to refrain from driving vehicles and engaging in activities that require increased concentration and speed of psychomotor reactions.

1 tablet contains: quetiapine (as fumarate) 25 mg.

Excipients: microcrystalline cellulose 60 mg, lactose monohydrate 44 mg, povidone 9 mg, croscarmellose sodium 10.5 mg, magnesium stearate 1.5 mg.
Beige-yellow to beige film-coated tablets, round, biconvex. White or almost white in cross section.

pharmachologic effect

Antipsychotic drug (neuroleptic). Shows a 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? 1 receptors and less pronounced - for? 2 receptors. It has no affinity for m-cholinergic receptors and benzodiazepine receptors.
Quetiapine at a dose that effectively blocks dopamine D2 receptors causes only mild catalepsy. Selectively reduces the activity of mesolimbic A10-dopamine neurons compared to A9-nigrostriatal neurons involved in motor function.
Does not cause a long-term increase in prolactin levels.
In accordance with the results of positron emission tomography, the effect of quetiapine on serotonin 5HT2- and dopamine D2-receptors lasts up to 12 hours.

Indications for use

Acute and chronic psychoses (including schizophrenia).

Mode of application

When used in adults, the initial dose is 50 mg / day, for elderly patients - 25 mg / day. Then the dose is gradually increased according to the scheme. Depending on the clinical effect and individual sensitivity, an effective therapeutic dose may be 150-750 mg / day.
In patients with impaired liver and / or kidney function, the initial dose is 25 mg / day. The daily dose increase should be 25-50 mg until the optimal effect is achieved.

Interaction

With simultaneous use with ketoconazole, erythromycin, it is theoretically possible to increase the concentration of quetiapine in the blood plasma and the development of side effects.
With simultaneous use with phenytoin, carbamazepine, barbiturates, rifampicin, the clearance of quetiapine increases, and its concentration in the blood plasma decreases.
With simultaneous use with thioridazine, an increase in the clearance of quetiapine is possible.

Side effect

From the side of the central nervous system:
- headache, drowsiness, dizziness, anxiety;
- rarely - NMS.
From the side of the cardiovascular system: orthostatic hypotension, tachycardia, arterial hypertension.
From the digestive system: constipation, dry mouth, dyspepsia, diarrhea, transient increase in liver enzymes (ALT, AST, GGT), abdominal pain.
From the side of the hematopoietic organs:
- asymptomatic leukopenia and / or neutropenia;
- rarely - eosinophilia.
From the musculoskeletal system: myalgia.
From the respiratory system: rhinitis.
Dermatological reactions: skin rash, dry skin.
On the part of the organ of hearing: pain in the ear.
From the genitourinary system: urinary tract infections.
On the part of metabolism: a slight increase in cholesterol and triglycerides in the blood.
From the endocrine system: a slight dose-dependent reversible decrease in the level of thyroid hormones (in particular, total and free T4).
Other: asthenia, back pain, weight gain, fever, chest pain.

Contraindications

Hypersensitivity to quetiapine.

Use during pregnancy and lactation
During pregnancy and lactation, use is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus. It is not known whether quetiapine is excreted in breast milk. If necessary, use during lactation, breastfeeding should be discontinued.
In experimental studies on animals, no mutagenic and clastogenic effects of quetiapine were detected. There was no effect of quetiapine on fertility (decrease in male fertility, pseudo-pregnancy, an increase in the period between two estrus, an increase in the precoital interval and a decrease in the frequency of pregnancy), however, the data obtained cannot be directly transferred to humans, because. there are specific differences in the hormonal control of reproduction.

Use in elderly patients
Use with caution in the elderly, especially when taking drugs that prolong the QT interval.

Overdose

Cases of overdose in the treatment of Quetiapine develop quite rarely. In this case, the development of drowsiness, excessive sedation, tachycardia and a decrease in blood pressure is possible.
Overdose treatment includes gastric lavage, activated charcoal, or laxatives that can clear unabsorbed quetiapine.
Symptomatic treatment and activities that support respiratory function, cardiovascular function, and ensure adequate oxygenation and ventilation are also recommended. Medical monitoring is necessary until the patient is completely healthy.

special instructions

Use with caution in patients with cardiovascular diseases and other conditions associated with the risk of arterial hypotension, especially at the beginning of treatment and in the elderly; with indications of a history of seizures.
Quetiapine undergoes active metabolism in the liver. In patients with impaired liver and kidney function, the clearance of quetiapine is reduced by approximately 25%. Therefore, quetiapine should be used with caution in patients with hepatic and/or renal impairment.
Use with caution simultaneously with drugs that prolong the QT interval (especially in the elderly); with drugs that have a depressing effect on the central nervous system, as well as with ethanol; with potential inhibitors of the CYP3A4 isoenzyme (including ketoconazole, erythromycin).
If NMS develops during treatment, quetiapine should be discontinued and appropriate treatment instituted.
With prolonged use, there is a possibility of developing tardive dyskinesia. In such cases, it is necessary to reduce the dose of quetiapine or cancel it.
Use with caution in combination with other drugs that affect the activity of the central nervous system, as well as with ethanol.
In experimental studies, when studying the carcinogenicity of quetiapine, an increase in the incidence of mammary adenocarcinomas in rats (at doses of 20, 75 and 250 mg / kg / day) was noted, which is associated with prolonged hyperprolactinemia.
In male rats (250 mg/kg/day) and mice (250 and 750 mg/kg/day), there was an increase in the incidence of benign adenomas from thyroid follicular cells, which was associated with a known rodent-specific mechanism for increasing the hepatic clearance of thyroxine.
Influence on the ability to drive vehicles and control mechanisms
Quetiapine can cause drowsiness, so patients are not recommended to perform work related to the need for concentration of attention and a high speed of psychomotor reactions (including driving vehicles).

Quetiapine is a drug from the group of neuroleptics, the drug has an antipsychotic effect on the body.

What is the composition and form of release of the antipsychotic "Quetiapine"?

The pharmaceutical industry produces the drug in tablets, where the active substance is quetiapine, its dosage can be in the following quantities: 200 mg, 100 mg, 150 and 25 milligrams. Auxiliary components are also present in the medication.

The tablets are packaged in contour packs, on the box with the medicine you can see the expiration date, which is equal to two years, after this time it is necessary to refrain from the subsequent use of the medication. An antipsychotic drug is sold after presenting the appropriate prescription to the pharmacist.

What is the effect of Quetiapine?

The drug Quetiapine has an antipsychotic effect, the active substance of the drug shows affinity for serotonin receptors to a greater extent than for dopamine receptors in the brain. When taken orally, it is quite well absorbed from the digestive tract. Metabolized in the liver.

The half-life is seven hours. Approximately 83 percent of quetiapine is protein bound. Up to 73% is excreted in the urine, a smaller part is excreted in the stool.

What are the indications for Quetiapine?

Quetiapine is indicated for use in the following conditions:

With schizophrenia;
Assign pills for psychosis, both chronic and acute;

In addition, the antipsychotic is effective in the manic episodes that are characteristic of bipolar disorder.

What are the contraindications for Quetiapine?

The neuroleptic Quetiapine instructions for use do not prescribe in the following situations:

With increased sensitivity to the components of the drug;
Up to 18 years, the remedy is contraindicated;
You can not simultaneously take an antipsychotic with CYP3A4 inhibitors, erythromycin, clarithromycin, as well as with nefazodone;
Do not use medication for lactation.

With caution, the neuroleptic is used during pregnancy, with cardiovascular pathology, with some cerebrovascular diseases, in the elderly, as well as in the presence of seizures, in addition, with liver failure.

What are the uses and dosages of Quetiapine tablets?

The drug should be used as directed by a specialist. Usually, with psychosis, including also schizophrenia, the patient is prescribed medication for the first four days in the following dosages: 50, 100, 200 and 300 milligrams. Then the dose can be in the range from 300 to 450 mg, if necessary, it is increased to 750 mg / day.

Overdose from Quetiapine

In extremely rare cases, a patient's death has been reported in case of poisoning with Quetiapine. And we are on www.! Usually, the following symptoms are characteristic of an overdose: drowsiness occurs, excessive sedation is characteristic, tachycardia is noted, in addition, a change in pressure develops, in particular, it decreases.

In such a situation, it is important to start early gastric lavage in order to prevent the absorption of the active substance of the drug in a timely manner. Then you should give the patient activated charcoal in the amount of several tablets.

If the patient is unconscious, tracheal intubation is performed, in addition, laxatives are administered, and symptomatic therapy is also indicated.

What are the side effects of Quetiapine?

The drug Quetiapine can lead to the development of the following side effects: changes occur from the nervous system, they are manifested by drowsiness, dizziness, headache, anxiety, hostile mood, agitation, insomnia, tremor, convulsions, depression are not excluded, in addition, paresthesia.

Sometimes taking the antipsychotic drug Quetiapine can cause the development of neuroleptic syndrome, which is always malignant. In particular, in this condition, the patient will feel an increase in temperature, muscle rigidity will join, a change in the so-called mental status is characteristic, in addition, the lability of the nervous system and other manifestations.

In addition to the listed side effects, one can note: pharyngitis, the development of orthostatic hypotension, rhinitis, tachycardia, a change in the ECG in the form of a prolongation of the Q-T interval, allergic reactions up to an anaphylactic state, in addition, skin rash, itching, myalgia, as well as blurred visual perception.

Among other manifestations, the following symptoms can be noted: dryness of the oral mucosa, nausea, vomiting, some pain in the abdomen is characteristic, in addition, intestinal motility is disturbed, which is expressed by loose stools or, conversely, constipation. Laboratory parameters also undergo changes: leukopenia, neutropenia, hypercholesterolemia, hypertriglyceridemia, and hyperglycemia occur.

special instructions

With the development of orthostatic hypotension in a patient, it is recommended to reduce the dose of neuroleptic to the minimum. If neuroleptic malignant syndrome occurs, the antipsychotic should be discontinued. During treatment, it is contraindicated to drink alcohol.

How to replace Quetiapine, what analogues?

The drug Quetiapine Stada, Viktoel, Kventiax, Quetiapine, Hedonin, Ketilept, Kutipin, in addition, Seroquel, Seroquel Prolong, Quetiapine hemifumarate, Quetitex, Ketiap, Quetiapine fumarate, Servitel, as well as Laquel medication are analogues.

Conclusion

Be healthy!

Tatyana, www.site
Google

- Dear our readers! Please highlight the found typo and press Ctrl+Enter. Let us know what's wrong.
- Please leave your comment below! We ask you! We need to know your opinion! Thank you! Thank you!

tab., cover film coat, 25 mg: 30 or 60 pcs. Reg. No.: LSR-008008/10

Clinico-pharmacological group:

Antipsychotic drug (neuroleptic)

Release form, composition and packaging

10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - cellular contour packings (6) - packs of cardboard.

Description of the active ingredients of the drug Quetiapine»

pharmachologic effect

Indications

- acute and chronic psychoses, including schizophrenia;

- manic episodes in the structure of bipolar disorder.

Dosing regimen

Adults:

Acute and chronic psychoses, including schizophrenia

Treatment of manic episodes in the structure of bipolar disorder

Quetiapine is used as monotherapy or as adjuvant therapy for mood stabilization.

Depending on the clinical effect and individual tolerance, the dose may vary from 200 to 800 mg / day. Usually an effective dose is from 400 to 800 mg / day.

In elderly patients

In patients with renal or hepatic insufficiency

Side effect

The following are the adverse reactions observed with the use of quetiapine and distributed by organs and systems:

From the side of the cardiovascular system: orthostatic hypotension, tachycardia, prolongation of the QT interval.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, diarrhea or constipation, increased activity of "liver" transaminases, jaundice, hepatitis.

From the respiratory system: pharyngitis, rhinitis.

Allergic reactions: skin rash, eosinophilia, angioedema, Stevens-Johnson syndrome, anaphylactic reactions.

Laboratory indicators: leukopenia, neutropenia, hypercholesterolemia, hypertriglyceridemia, decreased T4 concentration (first 4 weeks), hyperglycemia.

Contraindications

Hypersensitivity to any of the components of the drug;

Concurrent use with CYP3A4 inhibitors such as HIV protease inhibitors, azole antifungals, erythromycin, clarithromycin, nefazodone;

Children's age up to 18 years;

lactation period.

Pregnancy and lactation

Use with caution during pregnancy. Contraindicated during lactation.

Application for violations of liver function

In patients with liver failure it is recommended to start quetiapine therapy with 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is reached.

Application for violations of kidney function

In patients with renal insufficiency it is recommended to start quetiapine therapy with 25 mg/day. It is recommended to increase the dose daily by 25-50 mg until an effective dose is reached.

Use in the elderly

Application for children

Contraindicated in children and adolescents under 18 years of age.

special instructions

In the event of the development of a malignant neuroleptic syndrome, the drug must be discontinued.

Influence on the ability to drive vehicles and control mechanisms

Overdose

Symptoms may be due to an increase in the known pharmacological effects of the drug, such as drowsiness and excessive sedation, tachycardia and a decrease in blood pressure.

drug interaction

Terms and conditions of storage

Keep out of the reach of children, dry, dark place at a temperature not exceeding 25 °C.

Shelf life - 2 years.

drug interaction

The pharmacokinetics of lithium preparations does not change with the simultaneous use of quetiapine.