quetiapine | Quentiax tablets 100 mg, 60 pcs.
Special Price
$37.83
Regular Price
$47.00
In stock
SKU
BID465237
release form
tablets, coated
tablets, coated
release form
tablets, coated
Packing
60 pcs.
Pharmacological action
Quentiax is an antipsychotic drug (antipsychotic).
Pharmacodynamics
Mechanism of Action
Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin receptors (5HT2) than for brain dopamine D1 and D2 receptors. Quetiapine has an affinity for histamine and alpha-1 receptors, and less affinity for alpha-2 receptors. No significant affinity of quetiapine for cholinergic muscarinic and benzodiazepine receptors was found. In standard tests, quetiapine exhibits antipsychotic activity.
Pharmacodynamic effects of
Extrapyramidal symptoms (EPS) in animals have shown that quetiapine causes mild catalepsy at a dose that effectively blocks dopamine D2 receptors. Quetiapine causes a selective decrease in the activity of mesolimbic A10-dopaminergic neurons, in comparison with A9-nigrostriate neurons involved in motor functions.
Clinical efficacy of
There were no differences between the use of quetiapine (at a dose of 75-750 mg / day) and placebo in the incidence of extrapyramidal symptoms and the concomitant use of anticholinergics. - Does not cause a prolonged increase in plasma prolactin concentration.
Quetiapine has long supported clinical improvement in those patients who developed a positive effect at the very beginning of treatment.
The duration of exposure to quetiapine on 5HT2 receptors - serotonin and D2-dopamine receptors is less than 12 hours after taking the drug.
Pharmacokinetics
Absorption - high, food intake does not affect bioavailability. Communication with plasma proteins - 83%.
The pharmacokinetics of quetiapine is linear and does not differ in men and women.
Actively metabolized in the liver with the formation of pharmacologically inactive metabolites under the influence of the enzyme CYP3A4 cytochrome P450. Quetiapine and some of its metabolites are weak inhibitors of the isoenzymes 1A2, 2C9, 2C19, 2D6 and ZA4 of human cytochrome P450, but only in concentrations at least 10-50 times higher than the concentration of the drug when used in the effective dose range from 300 to 450 mg / day
Based on in vitro results, it should not be expected that concomitant administration of quetiapine with other drugs will lead to a clinically pronounced inhibition of cytochrome P450 mediated metabolism of other drugs. The half-life (T ) Is approximately 7 hours.
Excreted by the kidneys approximately 73% and through the intestines - 21%. Less than 5% of quetiapine is not metabolized and excreted unchanged. The average clearance of quetiapine in elderly patients is 30-50% less than in patients aged 18 to 65 years. The average clearance of plasma quetiapine in patients with severe renal failure (creatinine clearance less than 30 ml / min / 1.73 m3) is reduced by approximately 25% and in patients with liver damage (stable alcoholic cirrhosis).
Contraindications
Hypersensitivity to quetiapine or other components of the drug Quentiax
Breastfeeding period
Children and adolescents under 18 years of age (efficacy and safety not established).
Caution: patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increase in the QT interval on the electrocardiogram (ECG) or in the presence of conditions that can potentially cause an increase in the QT interval (concomitant use of drugs that extend the QT interval, congestive heart insufficiency, hypokalemia, hypomagnesemia), advanced age, liver failure, epilepsy, history of seizures, pregnancy.
Use during pregnancy and lactation
Safety and efficacy of quetiapine in pregnant women have not been established. Therefore, during pregnancy, quetiapine can only be used if the expected benefit justifies the potential risk. The degree of excretion of quetiapine with mother's milk has not been established. Women should be advised to avoid breastfeeding while taking quetiapine.
Special instructions
The following acute reactions (“withdrawal syndrome”) - nausea, vomiting, rarely insomnia, may occur with abrupt cancellation of high doses of antipsychotic drugs. Cases have been reported. exacerbation of psychotic symptoms and the appearance of involuntary motor disorders (akathisia, dystonia, dyskinesia). In this connection, drug withdrawal is recommended to be carried out gradually.
When prescribing quetiapine simultaneously with drugs that extend the QT interval, caution must be exercised, especially in the elderly. With congestive heart failure, with hypokalemia and hypomagnesemia.
Given that quetiapine affects the central nervous system, the drug should be used with caution in combination with other drugs that have a depressing effect on the central nervous system. It is recommended to refrain from drinking alcohol.
If symptoms of tardive dyskinesia appear, reduce the dose or stop using quetiapine.
Convulsive seizures
In controlled clinical trials, there was no difference in the frequency of seizures between quetiapine and placebo. However, as with other antipsychotic drugs, caution is advised in treating patients with a history of seizures.
Malignant antipsychotic syndrome
Malignant antipsychotic syndrome may be associated with ongoing antipsychotic treatment. Clinical manifestations of the syndrome include: hyperthermia, altered mental status, muscle rigidity, instability of the autonomic nervous system, and an increase in the level of creatine phosphokinase. With the development of this syndrome, quetiapine should be withdrawn and appropriate treatment should be carried out.
Effect on the ability to drive a car and other mechanical means: during treatment with quetiapine, caution is advised when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 tablet contains: active substance: quetiapine fumarate 100 mg
excipients: lactose monohydrate, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, povidone, sodium carboxymethyl starch (type A),
Side effects
From the hemopoietic organs and lymphatic system: often - leukopenia infrequently - eosinophilia very rarely - neutropenia.
Disorders of metabolism and nutrition: often - increase in body weight (mainly in the first weeks of treatment) is very rare - hyperglycemia or decompensation of diabetes mellitus.
From the central and peripheral nervous system: very often - dizziness, drowsiness, headache often - syncopal conditions infrequently - anxiety, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesia very rarely: tardive dyskinesia.
From the cardiovascular system: often - tachycardia, orthostatic arterial hypotension, prolongation of the QT interval on the ECG. On the part of the respiratory system: rhinitis, pharyngitis.
From the gastrointestinal tract: often - dry mouth, constipation, diarrhea, dyspepsia rarely - jaundice, nausea, vomiting, abdominal pain is very rare - hepatitis.
Allergic reactions: infrequently - skin rash, hypersensitivity reactions very rarely - angioedema, Stevens-Johnson syndrome.
From the reproductive system and mammary glands: rarely - priapism (painful erection).
Other: often - peripheral edema, asthenia rarely - lower back pain, chest pain, low-grade fever, myalgia, dry skin, impaired vision, antipsychotic malignant syndrome (hyperthermia, impaired consciousness, muscle rigidity, vegetative - vascular disorders, an increase in the concentration of creatine phosphokinase).
Laboratory indicators: often - an increase in serum transaminases (ACT or ALT) is infrequent - an increase in serum GGT and triglycerides (not on an empty stomach), hypercholesterolemia is a decrease in the level of thyroid hormones: total T4 and free T4 (in the first 4 weeks), and same - general TK and reverse TK (only when taking high doses of quetiapine).
Drug interaction
Quetiapine does not induce the induction of liver enzyme systems involved in the metabolism of phenazone and lithium.
Concomitant administration of quetiapine with drugs that potentially inhibit liver enzymes, such as carbamazepine or phenytoin, as well as barbiturates, rifampicin, a decrease in plasma concentrations of quetiapine may be necessary, which may require an increase in the dose of Quentiax, depending on the clinical effect. This should also be considered when discontinuing phenytoin or carbamazepine, or another inducer of the liver enzyme system, or when replacing it with a drug that does not induce microsomal liver enzymes (for example, valproic acid).
main enzyme, responsible for the metabolism of quetiapine by cytochrome P450, is CYP3A4. The pharmacokinetics of quetiapine does not change with the simultaneous use of cimetidine (an inhibitor of P450) or fluoxetine (an inhibitor of CYP3A4 and CYP2D6), an antidepressant of imipramine (an inhibitor of CYP2D6).
Caution is recommended when using quetiapine and systemic use of CYP3A4 inhibitors (antifungal agents of the azole group and macrolide antibiotics), as plasma concentrations of quetiapine may increase. Therefore, lower doses of quetiapine should be used. Particular attention should be paid to elderly and debilitated patients. The pharmacokinetics of quetiapine did not change significantly with simultaneous administration with antipsychotic drugs - risperidone or haloperidone. However, concomitant use of quetiapine with thioridazine increased the clearance of quetiapine.
Medications that inhibit the central nervous system (CNS) and ethanol increase the risk of side effects.
Overdose
Quetiapine overdose is limited. Cases of quetiapine in excess of 30 g have been described. In most patients, no side effects were noted, and in cases of their development, the side effects occurred independently. A case of fatal outcome with 13.6 grams of quetiapine was reported. Extremely rare cases of quetiapine overdose have been reported leading to QT prolongation, coma, or death. In patients with a history of severe cardiovascular disease, the risk of side effects in overdose may increase.
Symptoms: excessive sedation, drowsiness, tachycardia, decreased blood pressure.
Treatment: symptomatic measures aimed at maintaining respiratory function, cardiovascular system, adequate oxygenation and ventilation. There are no specific antidotes.
Storage conditions
At a temperature not exceeding 30 РC.
Shelf life
2 years.
Deystvuyushtee substance
Quetiapine
Dosage form
tablets
Possible product names
QUENTIAX 0.1 N60 TABLE P / FILM / SHELL
Quentiax 100mg Tab. p / pl / rev X60 (R)
Quentiax 100mg No. 60
Quentiaks tab po 100mg x 60
QUENTIAX TAB. P.P.O. 100MG No. 60
KRKA d.d. Novo mesto AO, Slovenia
tablets, coated
Packing
60 pcs.
Pharmacological action
Quentiax is an antipsychotic drug (antipsychotic).
Pharmacodynamics
Mechanism of Action
Quetiapine is an atypical antipsychotic drug that exhibits a higher affinity for serotonin receptors (5HT2) than for brain dopamine D1 and D2 receptors. Quetiapine has an affinity for histamine and alpha-1 receptors, and less affinity for alpha-2 receptors. No significant affinity of quetiapine for cholinergic muscarinic and benzodiazepine receptors was found. In standard tests, quetiapine exhibits antipsychotic activity.
Pharmacodynamic effects of
Extrapyramidal symptoms (EPS) in animals have shown that quetiapine causes mild catalepsy at a dose that effectively blocks dopamine D2 receptors. Quetiapine causes a selective decrease in the activity of mesolimbic A10-dopaminergic neurons, in comparison with A9-nigrostriate neurons involved in motor functions.
Clinical efficacy of
There were no differences between the use of quetiapine (at a dose of 75-750 mg / day) and placebo in the incidence of extrapyramidal symptoms and the concomitant use of anticholinergics. - Does not cause a prolonged increase in plasma prolactin concentration.
Quetiapine has long supported clinical improvement in those patients who developed a positive effect at the very beginning of treatment.
The duration of exposure to quetiapine on 5HT2 receptors - serotonin and D2-dopamine receptors is less than 12 hours after taking the drug.
Pharmacokinetics
Absorption - high, food intake does not affect bioavailability. Communication with plasma proteins - 83%.
The pharmacokinetics of quetiapine is linear and does not differ in men and women.
Actively metabolized in the liver with the formation of pharmacologically inactive metabolites under the influence of the enzyme CYP3A4 cytochrome P450. Quetiapine and some of its metabolites are weak inhibitors of the isoenzymes 1A2, 2C9, 2C19, 2D6 and ZA4 of human cytochrome P450, but only in concentrations at least 10-50 times higher than the concentration of the drug when used in the effective dose range from 300 to 450 mg / day
Based on in vitro results, it should not be expected that concomitant administration of quetiapine with other drugs will lead to a clinically pronounced inhibition of cytochrome P450 mediated metabolism of other drugs. The half-life (T ) Is approximately 7 hours.
Excreted by the kidneys approximately 73% and through the intestines - 21%. Less than 5% of quetiapine is not metabolized and excreted unchanged. The average clearance of quetiapine in elderly patients is 30-50% less than in patients aged 18 to 65 years. The average clearance of plasma quetiapine in patients with severe renal failure (creatinine clearance less than 30 ml / min / 1.73 m3) is reduced by approximately 25% and in patients with liver damage (stable alcoholic cirrhosis).
Contraindications
Hypersensitivity to quetiapine or other components of the drug Quentiax
Breastfeeding period
Children and adolescents under 18 years of age (efficacy and safety not established).
Caution: patients with cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increase in the QT interval on the electrocardiogram (ECG) or in the presence of conditions that can potentially cause an increase in the QT interval (concomitant use of drugs that extend the QT interval, congestive heart insufficiency, hypokalemia, hypomagnesemia), advanced age, liver failure, epilepsy, history of seizures, pregnancy.
Use during pregnancy and lactation
Safety and efficacy of quetiapine in pregnant women have not been established. Therefore, during pregnancy, quetiapine can only be used if the expected benefit justifies the potential risk. The degree of excretion of quetiapine with mother's milk has not been established. Women should be advised to avoid breastfeeding while taking quetiapine.
Special instructions
The following acute reactions (“withdrawal syndrome”) - nausea, vomiting, rarely insomnia, may occur with abrupt cancellation of high doses of antipsychotic drugs. Cases have been reported. exacerbation of psychotic symptoms and the appearance of involuntary motor disorders (akathisia, dystonia, dyskinesia). In this connection, drug withdrawal is recommended to be carried out gradually.
When prescribing quetiapine simultaneously with drugs that extend the QT interval, caution must be exercised, especially in the elderly. With congestive heart failure, with hypokalemia and hypomagnesemia.
Given that quetiapine affects the central nervous system, the drug should be used with caution in combination with other drugs that have a depressing effect on the central nervous system. It is recommended to refrain from drinking alcohol.
If symptoms of tardive dyskinesia appear, reduce the dose or stop using quetiapine.
Convulsive seizures
In controlled clinical trials, there was no difference in the frequency of seizures between quetiapine and placebo. However, as with other antipsychotic drugs, caution is advised in treating patients with a history of seizures.
Malignant antipsychotic syndrome
Malignant antipsychotic syndrome may be associated with ongoing antipsychotic treatment. Clinical manifestations of the syndrome include: hyperthermia, altered mental status, muscle rigidity, instability of the autonomic nervous system, and an increase in the level of creatine phosphokinase. With the development of this syndrome, quetiapine should be withdrawn and appropriate treatment should be carried out.
Effect on the ability to drive a car and other mechanical means: during treatment with quetiapine, caution is advised when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 tablet contains: active substance: quetiapine fumarate 100 mg
excipients: lactose monohydrate, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, povidone, sodium carboxymethyl starch (type A),
Side effects
From the hemopoietic organs and lymphatic system: often - leukopenia infrequently - eosinophilia very rarely - neutropenia.
Disorders of metabolism and nutrition: often - increase in body weight (mainly in the first weeks of treatment) is very rare - hyperglycemia or decompensation of diabetes mellitus.
From the central and peripheral nervous system: very often - dizziness, drowsiness, headache often - syncopal conditions infrequently - anxiety, agitation, insomnia, akathisia, tremor, convulsions, depression, paresthesia very rarely: tardive dyskinesia.
From the cardiovascular system: often - tachycardia, orthostatic arterial hypotension, prolongation of the QT interval on the ECG. On the part of the respiratory system: rhinitis, pharyngitis.
From the gastrointestinal tract: often - dry mouth, constipation, diarrhea, dyspepsia rarely - jaundice, nausea, vomiting, abdominal pain is very rare - hepatitis.
Allergic reactions: infrequently - skin rash, hypersensitivity reactions very rarely - angioedema, Stevens-Johnson syndrome.
From the reproductive system and mammary glands: rarely - priapism (painful erection).
Other: often - peripheral edema, asthenia rarely - lower back pain, chest pain, low-grade fever, myalgia, dry skin, impaired vision, antipsychotic malignant syndrome (hyperthermia, impaired consciousness, muscle rigidity, vegetative - vascular disorders, an increase in the concentration of creatine phosphokinase).
Laboratory indicators: often - an increase in serum transaminases (ACT or ALT) is infrequent - an increase in serum GGT and triglycerides (not on an empty stomach), hypercholesterolemia is a decrease in the level of thyroid hormones: total T4 and free T4 (in the first 4 weeks), and same - general TK and reverse TK (only when taking high doses of quetiapine).
Drug interaction
Quetiapine does not induce the induction of liver enzyme systems involved in the metabolism of phenazone and lithium.
Concomitant administration of quetiapine with drugs that potentially inhibit liver enzymes, such as carbamazepine or phenytoin, as well as barbiturates, rifampicin, a decrease in plasma concentrations of quetiapine may be necessary, which may require an increase in the dose of Quentiax, depending on the clinical effect. This should also be considered when discontinuing phenytoin or carbamazepine, or another inducer of the liver enzyme system, or when replacing it with a drug that does not induce microsomal liver enzymes (for example, valproic acid).
main enzyme, responsible for the metabolism of quetiapine by cytochrome P450, is CYP3A4. The pharmacokinetics of quetiapine does not change with the simultaneous use of cimetidine (an inhibitor of P450) or fluoxetine (an inhibitor of CYP3A4 and CYP2D6), an antidepressant of imipramine (an inhibitor of CYP2D6).
Caution is recommended when using quetiapine and systemic use of CYP3A4 inhibitors (antifungal agents of the azole group and macrolide antibiotics), as plasma concentrations of quetiapine may increase. Therefore, lower doses of quetiapine should be used. Particular attention should be paid to elderly and debilitated patients. The pharmacokinetics of quetiapine did not change significantly with simultaneous administration with antipsychotic drugs - risperidone or haloperidone. However, concomitant use of quetiapine with thioridazine increased the clearance of quetiapine.
Medications that inhibit the central nervous system (CNS) and ethanol increase the risk of side effects.
Overdose
Quetiapine overdose is limited. Cases of quetiapine in excess of 30 g have been described. In most patients, no side effects were noted, and in cases of their development, the side effects occurred independently. A case of fatal outcome with 13.6 grams of quetiapine was reported. Extremely rare cases of quetiapine overdose have been reported leading to QT prolongation, coma, or death. In patients with a history of severe cardiovascular disease, the risk of side effects in overdose may increase.
Symptoms: excessive sedation, drowsiness, tachycardia, decreased blood pressure.
Treatment: symptomatic measures aimed at maintaining respiratory function, cardiovascular system, adequate oxygenation and ventilation. There are no specific antidotes.
Storage conditions
At a temperature not exceeding 30 РC.
Shelf life
2 years.
Deystvuyushtee substance
Quetiapine
Dosage form
tablets
Possible product names
QUENTIAX 0.1 N60 TABLE P / FILM / SHELL
Quentiax 100mg Tab. p / pl / rev X60 (R)
Quentiax 100mg No. 60
Quentiaks tab po 100mg x 60
QUENTIAX TAB. P.P.O. 100MG No. 60
KRKA d.d. Novo mesto AO, Slovenia
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