Quetiapine Canon - Instructions For Use, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Quetiapine Canon

Quetiapine Canon: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Quetiapine Kanon

ATX code: N05AH04

Active ingredient: quetiapine (Quetiapine)

Producer: Kanonpharma production, CJSC (Russia)

Description and photo update: 2019-05-07

Prices in pharmacies: from 572 rubles.

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Quetiapine Canon is a neuroleptic (antipsychotic drug).

Release form and composition

Dosage form - tablets, film-coated: round biconvex, blue with a pearlescent sheen, the core in the cross section is almost white (in a cardboard box 3 or 6 blisters containing 10 tablets at a dosage of 25, 100, 200 or 300 mg; in cardboard box 2 or 4 blister packs containing 15 tablets at a dosage of 200 or 300 mg; in a cardboard box 1 or 2 blisters containing 30 tablets at a dosage of 25 or 100 mg. Each pack also contains instructions for the use of Quetiapine Canon) …

Composition of 1 tablet (dosage 25/100/200/300 mg):

• active substance: quetiapine in the form of quetiapine hemifumarate - 28.78 / 115.14 / 230.27 / 345.4 mg;
• auxiliary components: calcium hydrogen phosphate dihydrate - 46.4 / 32.94 / 33.39 / 41.64 mg; calcium stearate - 0.62 / 1.02 / 1.64 / 2.36 mg; magnesium stearate - 1 / 1.5 / 2/3 mg; microcrystalline cellulose - 32/24/25/32 mg; sodium carboxymethyl starch - 2 / 3.5 / 3.5 / 4.6 mg; pregelatinized corn starch - 6 / 16.9 / 17.2 / 20 mg; Hyprolose (hydroxypropylcellulose Klucel LF) - 3.2 / 5/7/11 mg;
• film coating: AquaPolish D blue [microcrystalline cellulose - 0.3 / 0.5 / 0.8 / 1.2 mg; glycerin (glycerol) - 0.15 / 0.25 / 0.4 / 0.6 mg; hydroxypropyl methylcellulose (hypromellose) - 1.5 / 2.5 / 4/6 mg; talc - 0.44 / 0.73 / 1.17 / 1.76 mg; indigo carmine dye - 0.07 / 0.12 / 0.19 / 0.28 mg; dye kandurin silver shine - 0.54 / 0.9 / 1.44 / 2.16 mg] - 3/5/8/12 mg.

Pharmacological properties

Pharmacodynamics

Quetiapine - the active substance of Quetiapine Canon, belongs to the group of atypical antipsychotics (neuroleptics). The effect of the drug is based on the interaction of the substance and its active metabolite N-desalkyl quetiapine (norkvetiapine) with a wide range of neurotransmitter receptors in the brain.

Quetiapine and N-dezalkyl quetiapine show a higher affinity for serotonin receptors (5HT ₂) compared to those for dopamine D ₁ and D ₂ receptors in the brain. It is generally accepted that this combination of receptor antagonism with greater selectivity for 5HT ₂ in comparison with D ₂ receptors determines the presence of clinical antipsychotic properties and the insignificant ability of quetiapine to lead to the development of EPE (extrapyramidal side effects) compared to typical drugs with antipsychotic action.

Also, quetiapine is characterized by a lack of affinity for the norepinephrine transporter and a low affinity for the 5HT ₂ -serotonin receptor, while its metabolite has a high affinity for both. In addition, both quetiapine and N-dezalkyl quetiapine have high affinity for histaminergic and adrenergic α ₁ receptors, and low affinity for adrenergic α ₂ receptors and serotonin 5HT _1A receptors.

Selective affinity for m-choline and benzodiazepine receptors was not revealed. Against the background of therapy, the activity of mesolimbic A ₁₀ -dopaminergic neurons decreases in comparison with A ₉ -nigrostrial neurons, which are involved in motor functions. The duration of communication with 5HT ₂ -serotonin and D ₂ -dopamine receptors is less than 12 hours. Quetiapine has no or low affinity for muscarinic receptors, while norkvetiapine has a high or moderate affinity for several muscarinic receptor subtypes.

Quetiapine exhibited antipsychotic activity in standard tests.

The specific contribution of norquetiapine to the pharmacological activity of the parent substance has not been established.

According to the results of a study of EPS (extrapyramidal symptoms) in animals, it was found that quetiapine in doses that effectively block D ₂ receptors causes mild catalepsy.

The substance is effective against the positive and negative symptoms of schizophrenia.

Quetiapine is effective as monotherapy for moderate to severe manic episodes. There are no data on the long-term use of Quetiapine Canon for the prevention of subsequent depressive and manic episodes. There is limited information on the use of quetiapine in combination with valproate seminatrium or lithium preparations for moderate to severe manic episodes, but overall this combination therapy was well tolerated.

Quetiapine, when used at a dose of 300 and 600 mg, is effective in patients with moderate to severe bipolar I and II disorder. At the same time, the effectiveness of the substance from doses of 300 and 600 mg per day is comparable.

Quetiapine Canon is effective in the treatment of schizophrenia and mania when taken twice a day, despite the fact that the T _1/2 (half-life) of the parent substance is approximately 7 hours.

The duration of the effect of quetiapine on 5HT ₂ and D ₂ receptors is up to 12 hours.

The use of quetiapine with dose titration in the treatment of schizophrenia gives the frequency of EPS and concomitant therapy with m-anticholinergics comparable to that in the placebo group. In the case of the appointment of quetiapine in the range of fixed daily doses of 75–750 mg to patients with schizophrenia, an increase in the incidence of EPS and the need for concomitant use of m-anticholinergics was not observed.

The frequency of EPS and the concomitant use of m-anticholinergics when using quetiapine in a daily dose of up to 800 mg for the treatment of manic episodes of moderate to severe severity in the form of monotherapy or in combination with valproate seminodium or lithium preparations is comparable to that when taking placebo.

The drug does not cause a prolonged increase in the concentration of prolactin in the blood plasma. There were no differences in the concentration of prolactin with quetiapine or placebo in a fixed dose.

Pharmacokinetics

Quetiapine is well absorbed from the gastrointestinal tract when taken orally. Food has no significant effect on bioavailability.

The level of communication with plasma proteins is 83%. Pharmacokinetic parameters of quetiapine are linear, there is no difference between them in women and men.

The equilibrium molar concentration of the active metabolite of N-dealkyl quetiapine is 35% of that of quetiapine.

Metabolism occurs in the liver, while under the action of the isoenzyme CYP3A4, mediated by cytochrome P ₄₅₀, pharmacologically inactive metabolites are formed. Quetiapine and some of its metabolites have a weak inhibitory effect on the following isozymes of cytochrome P ₄₅₀ - CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, but only in concentrations that are 10-50 times higher than those arising at the usually used effective daily dose of 300-450 mg …

According to the results of drug interaction studies, it was found that in healthy volunteers, the combined use of 25 mg quetiapine with ketoconazole (one of the CYP3A4 inhibitors) causes an increase in the AUC (area under the concentration-time curve) of quetiapine by 5-8 times, therefore the combination of these drugs contraindicated.

The main metabolites in the blood plasma do not possess pronounced pharmacological activity.

Excretion is carried out: 73% - by the kidneys, 21% - through the intestines. Does not undergo metabolism and is excreted by the kidneys or with feces in unchanged form less than 5% of quetiapine. The half-life value (T _1/2) is 7 hours.

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

Against the background of severe renal failure (in patients with creatinine clearance less than 30 ml / min / 1.73 m ²), the mean plasma clearance of quetiapine decreases by about 25%, while the individual parameters are in the range of values that were found in healthy volunteers.

In liver failure (compensated alcoholic cirrhosis), the mean plasma clearance of quetiapine decreases by about 25%. Since the substance is actively metabolized in the liver, against the background of liver failure, the plasma concentration of quetiapine may increase, which requires a dose change.

Based on the research results, it can be assumed that with the simultaneous administration of quetiapine and other drugs, clinically pronounced inhibition of drug metabolism mediated by cytochrome P ₄₅₀ does not occur.

Indications for use

• schizophrenia (treatment);
• bipolar disorder (treatment);
• severe episodes of depression in the structure of bipolar disorder;
• severe and moderate manic episodes in the structure of bipolar disorder.

Contraindications

Absolute:

• combined use with inhibitors of cytochrome P ₄₅₀, including erythromycin, antifungal drugs of the azole group, nefazodone, clarithromycin, as well as HIV protease inhibitors;
• psychosis in patients over 65 with dementia;
• age up to 18 years;
• pregnancy and lactation;
• individual intolerance to the components of Quetiapine Canon, including hypersensitivity with congenital deficiency of specific disaccharidases or os-amylase.

Relative (Quetiapine Canon is prescribed under medical supervision):

• liver failure;
• cardiovascular and cerebrovascular diseases or other conditions that predispose to arterial hypotension;
• conditions accompanied by the risk of developing aspiration pneumonia and stroke;
• combined use with drugs that have a depressing effect on the central nervous system, or with alcohol;
• combination therapy with drugs that increase the QT interval (including with antipsychotics), especially in elderly patients, in patients with congenital prolongation of the QT interval, myocardial hypertrophy, congestive heart failure, hypomagnesemia or hypokalemia;
• aggravated history of epilepsy and epileptic seizures;
• dementia;
• diabetes;
• Parkinson's disease;
• elderly age.

Quetiapine Canon, instructions for use: method and dosage

Quetiapine Canon is taken orally, regardless of food intake, 2 times a day.

Therapy should be prescribed by a physician experienced in the treatment of bipolar disorders.

The initial daily dose for the treatment of schizophrenia for the first four days is 50, 100, 200, 300 mg, respectively. Subsequently, the dose is titrated to an effective dose in the range of 300–450 mg.

Depending on the severity of the clinical effect and tolerability of Quetiapine Canon, the daily dose can vary from 150 to 750 mg (maximum).

In patients with moderate or severe manic episodes in the structure of bipolar disorder, the drug can be used as monotherapy or as an adjuvant treatment to stabilize mood. The initial daily dose for the first four days is 100, 200, 300, 400 mg, respectively. By the sixth day, it can be increased to 800 mg (the maximum increment is 200 mg per day).

In the future, the daily dose may be in the range of 200-800 mg (determined by the effect of the therapy and the tolerability of the drug). An effective dose is usually 400 to 800 mg (maximum) per day.

For the treatment of severe episodes of depression in patients with bipolar disorder, Quetiapine Canon is prescribed 1 time per day at night. The initial daily dose for the first four days is 50, 100, 200, 300 mg, respectively. In the future, the drug is recommended to be used at 300 mg per day. The maximum daily dose is 600 mg (no clinical improvement was found with the higher dose).

For elderly patients and patients with hepatic insufficiency, Quetiapine Canon is prescribed with caution, especially during dose selection. Therapy should be started with 25 mg per day. Then, daily (if necessary, taking into account the response to treatment and the tolerability of the drug, it can be slower), in increments of 25-50 mg, the dose is increased to an effective one. In older patients, it may be lower than in younger patients.

Side effects

During the use of Quetiapine Canon, as well as other antipsychotic drugs, the development of disorders such as fainting, neuroleptic malignant syndrome, neutropenia, leukopenia, peripheral edema is possible.

Most often (in more than 10% of cases), the following adverse reactions occur: withdrawal syndrome, dizziness, drowsiness, xerostomia, increased triglyceride concentration, increased total cholesterol concentration (mainly low density lipoprotein cholesterol), decreased concentration of high density lipoprotein cholesterol, weight gain, extrapyramidal symptoms, decreased hemoglobin concentration.

Possible side effects (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):

• immune system: infrequently - hypersensitivity reactions; very rarely - anaphylactic reactions ⁶;
• blood and lymphatic system: often - leukopenia ^{1, 25}, increased number of eosinophils ²⁴, decreased number of neutrophils ^{1, 22}; infrequently - a decrease in the number of platelets ¹⁴, thrombocytopenia; rarely - agranulocytosis ²⁷, with an unknown frequency - neutropenia ¹;
• metabolism and nutrition: very often - an increase in the serum concentration of triglycerides in the blood ^{1, 11}, an increase in the level of total cholesterol (mainly low-density lipoprotein cholesterol) ^{1, 12}, a decrease in the plasma concentration of high-density lipoprotein cholesterol in the blood ^{1, 18}, weight gain ⁹; often - increased appetite, hyperglycemia ^{1, 7}; infrequently - diabetes mellitus ^{1, 5, 6}, hyponatremia ²⁹;
• endocrine system: often - an increase in the serum concentration of prolactin in the blood ¹⁶, an increase in the plasma concentration of thyroid-stimulating hormone (TSH) ²⁰ in the blood, a decrease in the concentration of total triiodothyronine (T3) ²⁰, a decrease in the plasma concentration of total and free thyroxine (T4) ²⁰ in the blood; infrequently - a decrease in the concentration of free T3 in blood plasma ²⁰; very rarely - syndrome of inappropriate secretion of antidiuretic hormone;
• respiratory system: often - rhinitis, shortness of breath ¹⁹;
• nervous system: very often - headache, drowsiness ^{2, 17}, dizziness ^{1, 4, 17}; often - extrapyramidal symptoms ^{1, 13}, syncope ^{1, 4, 17}, dysarthria; infrequently - tardive dyskinesia ^{1, 6}, restless legs syndrome, convulsions ¹;
• digestive system: very often - xerostomia; often - vomiting ²¹, constipation, dyspepsia; infrequently - dysphagia ^{1, 8}; rarely - intestinal obstruction / ileus;
• psyche: often - suicidal thoughts and behavior ¹, nightmarish and unusual dreams; rarely - somnambulism and similar phenomena ¹⁷;
• cardiovascular system: often - palpitations ¹⁹, orthostatic hypotension ^{1, 4, 17}, tachycardia ^{1, 4}; infrequently - lengthening of the QT interval ^{1, l3, 30}, bradycardia ²⁶; rarely - venous thromboembolism ¹;
• organ of vision: often - blurred vision;
• kidneys and urinary tract: infrequently - urinary retention;
• liver and biliary tract: rarely - hepatitis ⁶, jaundice ⁶;
• skin and subcutaneous tissues: very rarely - Stevens-Johnson syndrome ⁶, angioedema ⁶;
• connective and musculoskeletal tissue: very rarely - rhabdomyolysis;
• instrumental and laboratory data: very often - a decrease in the concentration of high-density lipoprotein cholesterol ^{1, 18}, an increase in the concentration of triglycerides ^{1, 11}, an increase in total cholesterol (mainly low-density lipoprotein cholesterol) ^{1, 12}, weight gain ⁹, a decrease in the concentration of hemoglobin ²³; often - an increase in the activity of aspartate aminotransferase ³, a decrease in the number of neutrophils ^{1, 22}, an increase in the activity of alanine aminotransferase ³, an increase in the activity of gamma-glutamyl transpeptidase (GGT) ³, an increase in the number of eosinophils ²⁴, hyperglycemia ^{1, 7}, a decrease in the concentration of total and free T4 ²⁰, an increase in the concentration of prolactin in the blood serum ¹⁶, an increase in the concentration of TSH ²⁰, a decrease in the concentration of total T3 ²⁰; infrequently - thrombocytopenia ¹⁴, decreased concentration of free T3 ²⁰, prolongation of the QT interval ^{1, 13}; rarely - agranulocytosis ²⁷, increased activity of creatine phosphokinase ¹⁵;
• genitals and mammary gland: infrequently - sexual dysfunction; rarely - galactorrhea, priapism, menstrual disorders;
• pregnancy, postpartum and perinatal conditions: with unknown frequency - withdrawal syndrome in newborns ²⁸;
• general disorders: very often - withdrawal syndrome ^{1, 10}; often - peripheral edema, irritability, fever, mild asthenia; rarely - hypothermia, neuroleptic malignant syndrome ¹.

Notes:

¹ Violations are described in the section Special instructions.

² The development of drowsiness is most often noted during the first two weeks of treatment; this disorder is usually resolved with continued administration of Quetiapine Canon.

³ An increase (more than 3 times in comparison with the upper limit of the norm when measured at any time) in the activity of alanine aminotransferase, aspartate aminotransferase and gamma-glutamyl transpeptidase in the blood serum may be asymptomatic. In most cases, this disorder is reversible and does not require discontinuation of therapy.

⁴ Reception of Quetiapine Canon, like other antipsychotic drugs with α ₁ -adrenoceptor blocking action, often leads to the development of orthostatic hypotension, which is accompanied by such disorders as dizziness, tachycardia, and sometimes fainting (especially at the beginning of treatment).

⁵ Decompensation of diabetes mellitus is observed in rare cases.

⁶ The incidence of this disorder was assessed based on the results of post-marketing surveillance.

⁷ The concentration of fasting blood glucose increases above 126 mg / dL (> 7.0 mmol / L) or blood glucose after a meal above 200 mg / dL (> 11.1 mmol / L), at least with a single determination.

⁸ An increase in the incidence of dysphagia while taking Quetiapine Canon in comparison with placebo was observed only in patients with depression in the structure of bipolar disorder.

⁹ Initial body weight increases by no less than 7%. Most often, this disorder occurs in adults at the beginning of therapy.

¹⁰ The development of the following symptoms was noted during short-term placebo-controlled clinical trials of quetiapine in monotherapy mode during the study of withdrawal syndrome: headache, insomnia, nausea, vomiting, diarrhea, irritability, dizziness. Withdrawal rates significantly decreased 7 days after treatment withdrawal.

¹¹ The concentration of triglycerides increases above 200 mg / dL (> 2.258 mmol / L) in patients over 18 years of age or above 150 mg / dL (> 1.694 mmol / L) in patients under 18 years of age, at least with a single determination.

¹² The concentration of total cholesterol increases above 240 mg / dL (> 6.2064 mmol / L) in patients over 18 years of age or above 200 mg / dL (> 5.172 mmol / L) in patients under 18 years of age, at least with a single determination.

¹³ Violations are described in detail in the Special instructions section.

^{14 The} number of platelets decreases below 100 × 10 ⁹ / l, at least with a single determination.

^{15 The} disorder, according to clinical studies, develops without association with neuroleptic malignant syndrome.

¹⁶ Prolactin concentration increases in patients over 18 years of age: in men, more than 20 μg / l (> 869.56 pmol / l); in women, more than 30 μg / L (> 1304.34 pmol / L).

¹⁷ This violation may result in falls.

¹⁸ The concentration of high-density lipoprotein cholesterol decreases: in men, less than 40 mg / dL (<1.03 mmol / L); in women, less than 50 mg / dL (<1.29 mmol / L).

¹⁹ These disorders were often observed against the background of dizziness, tachycardia, orthostatic hypotension and / or concomitant pathologies of the respiratory or cardiovascular systems.

²⁰ Side effect was documented based on potentially clinically significant deviations from the normal baseline, which were observed in all clinical trials. There is a change in the concentration of total T3 and T4, free T3 and T4 to values less than 80% of the lower limit of the norm (pmol / l) when measured at any time. The TSH concentration varied by more than 5 mIU / L when measured at any time.

²¹ Disorder reported on the basis of an increased incidence of vomiting in patients over 65 years of age.

²² The development of neutropenia was recorded during short-term clinical trials using quetiapine as monotherapy in patients with a neutrophil count above 1.5 × 10 ⁹ / L before the start of the course. At the same time, there were cases of development of neutropenia (the number of neutrophils below 1.5 × 10 ⁹ / L) in 1.9% of patients in the quetiapine group and in 1.5% in the placebo group. A decrease in the number of neutrophils in the range from> 0.5 × 10 ⁹ / L to <1.0 × 10 ⁹ / L was noted with a frequency of 0.2% in both the quetiapine and placebo groups. The number of neutrophils was below 0.5 × 10 ⁹ / L at least once determined in 0.21% of patients in the quetiapine group and 0% in the placebo group.

²³ The concentration of hemoglobin decreases in men below 13 g / dl, in women below 12 g / dl, this disorder was observed, at least with a single determination, in 11% of patients while receiving Quetiapine Canon in all clinical trials, including long-term treatment. In short-term placebo-controlled studies, a decrease in hemoglobin concentration in men below 13 g / dl and in women below 12 g / dl, at least with a single determination, was observed in 8.3% of patients in the quetiapine group compared with 6.2% in a group of patients taking a placebo.

^{24 The} impairment was confirmed by potentially clinically significant deviations from baseline normal levels noted in all clinical trials. The number of eosinophils rises above 1 × 10 ⁹ / L when measured at any time.

^{25 The} violation was confirmed by potentially clinically significant deviations from the baseline normal level, which were recorded in all clinical trials. The leukocyte count decreases below 3 x 10 ⁹ / L when measured at any time.

²⁶ Side effect may develop early in therapy and be accompanied by syncope and / or hypotension. Frequency estimates were based on reports of bradycardia and associated adverse events reported in all clinical trials of quetiapine.

^{27 The} violation was recorded based on the estimated frequency in patients participating in all clinical trials of the drug, who developed severe neutropenia (<0.5 × 10 ⁹ / L) in combination with infections.

²⁸ Violation is described in detail in the section "Use during pregnancy and lactation."

²⁹ There is a change in concentration from> 132 mmol / L to <132 mmol / L, at least with a single determination.

³⁰ The frequency of QTc interval change ranges from <450 msec to ≥ 450 msec with an increase of 30 msec or more. In placebo-controlled studies, the number of patients who experienced a clinically significant increase in the QTc interval was baseline in both the quetiapine and placebo groups. Ventricular arrhythmias, prolongation of the QT interval, bidirectional ventricular tachycardia, cardiac arrest, and sudden death are considered adverse reactions that are associated with antipsychotics.

Overdose

There are reports of death after taking 13,600 mg of quetiapine in a patient who participated in a clinical study. Also, a lethal outcome was recorded during a post-marketing study of Quetiapine Canon after taking a dose of 6000 mg. At the same time, there is data on the intake of quetiapine at a dose of 30,000 mg, which did not end with a lethal outcome.

In extremely rare cases, an overdose of quetiapine leads to an increase in the QT interval, coma, or death. In patients with a history of severe cardiovascular disease, the likelihood of adverse reactions in case of overdose may increase.

Symptoms noted in an overdose are manifested mainly by an increase in the known pharmacological effects of Quetiapine Canon, including drowsiness, sedation, lowering blood pressure and tachycardia. There are isolated reports of the development of the following symptoms: rhabdomyolysis, respiratory depression, urinary retention, confusion, delirium and agitation.

There is no specific antidote. In case of severe intoxication, it is necessary to remember the likelihood of an overdose of several drugs. Measures are recommended, the action of which is aimed at maintaining the cardiovascular system and respiratory function, ensuring adequate ventilation and oxygenation.

When refractory hypotension occurs, therapy is carried out by intravenous fluid and / or with the help of sympathomimetic drugs (epinephrine and dopamine are not prescribed, since against the background of blockade of α-adrenergic receptors with quetiapine, when β-adrenergic receptors are stimulated, hypotension may increase).

Gastric lavage (if the patient is unconscious, then after intubation), the use of activated charcoal and drugs with a laxative effect can contribute to the elimination of unabsorbed substances. However, the effectiveness of these measures has not been studied. Until the patient's condition improves, close medical supervision should be established for him.

special instructions

Quetiapine Canon is not prescribed for children under 18 years of age, since there is not enough data on the use of the drug in this age group of patients. According to the results of clinical studies, some adverse reactions in children and adolescents were observed more often than in adult patients. These include a runny nose, vomiting, increased appetite, an increase in serum prolactin concentration in the blood, fainting. In this group of patients, there may be a change in the function of the thyroid gland, as well as an increase in blood pressure, which does not occur in adult patients.

In placebo-controlled studies, the incidence of EPS when using Quetiapine Canon in patients under 18 years of age with schizophrenia and mania in the structure of bipolar disorder was higher than with placebo.

Several placebo-controlled studies have confirmed that the use of atypical antipsychotic drugs in elderly patients with psychoses associated with dementia increases the risk of cerebrovascular complications by about 3 times (the exact mechanism has not been studied). A similar risk cannot be excluded for other antipsychotic drugs or other drug groups. In patients at risk of developing a stroke, Quetiapine Canon should be used with caution.

In bipolar disorder, depression is associated with an increased risk of suicidal ideation, suicide, and self-harm. The increased risk persists until severe remission occurs. It should be borne in mind that the period from the beginning of treatment to the improvement of the patient's condition can be from several weeks, in connection with which, until this moment, careful medical control should be established for the patient's condition.

According to generally accepted clinical experience, the likelihood of suicide may increase in the early stages of remission. Any cases of clinical deterioration, suicidal thoughts or behavior, or unusual changes in behavior should be reported to the doctor immediately.

Based on clinical studies, in patients with depression associated with bipolar disorder, the likelihood of developing events associated with suicide is 3% for quetiapine and 0% for placebo in patients 18-24 years old; 1.8% and 1.8% for patients over 25 years old, respectively.

Other psychiatric disorders for which Quetiapine Canon is prescribed are also associated with an increased likelihood of suicidal events. These conditions can be comorbid with a depressive episode. Therefore, the precautions described for the treatment of patients with a depressive episode should be applied to patients with other mental disorders as well. In the event of an abrupt discontinuation of the drug, it is necessary to take into account the potential risk of occurrence of events associated with suicide.

Patients with a history of suicidal events, as well as patients who clearly express suicidal thoughts before starting therapy, are considered to be at increased risk of suicidal intentions and suicidal attempts, and their condition should be carefully monitored. According to data from short-term placebo-controlled studies, in all age groups and for all indications, the frequency of events that are associated with suicide for quetiapine and placebo is 0.8%. Monitoring for changes in behavior and suicidal tendencies, especially in the first months of therapy and when changing the dose of Quetiapine Canon, should be established for all patients who are prescribed therapy.

During the period of taking Quetiapine Canon, drowsiness and associated symptoms, including sedation, may develop. When conducting clinical studies with the participation of patients with depression in the structure of bipolar disorder, the development of drowsiness was usually noted in the first three days of therapy. The severity of this disorder is usually mild or moderate. Patients with depression in the structure of bipolar disorder, in the case of severe drowsiness, may require more frequent medical consultation within two weeks from the onset of this disorder or until its severity decreases. Sometimes therapy has to be canceled.

Since during treatment, orthostatic hypotension and dizziness may develop (as a rule, at the beginning of the use of Quetiapine Canon when selecting a dose), patients, especially the elderly, are advised to be careful to avoid accidental falls and injuries. This precaution also applies to patients with cerebrovascular and cardiovascular diseases, and other conditions that predispose to hypotension. With the development of orthostatic hypotension, the dose may be reduced or a slower titration will be required.

In patients with depression in the structure of bipolar disorder during therapy with Quetiapine Canon for depressive episodes, there was an increase in the incidence of EPS in comparison with placebo.

It should be borne in mind that taking Quetiapine Canon can cause tardive dyskinesia. It manifests itself in involuntary violent movements and can be irreversible. When symptoms of tardive dyskinesia appear, a dose reduction or gradual withdrawal of the drug is recommended. The symptoms of this disease may worsen or even occur after the cancellation of Quetiapine Canon.

During therapy, akathisia may occur. Its characteristic features are an unpleasant feeling of restlessness and the need to move, which is expressed as the inability of the patient to stand or sit without movement. With the development of these disorders, the dose of Quetiapine Canon should not be increased.

Another disorder that can occur during therapy is neuroleptic malignant syndrome. Its main clinical manifestations include hyperthermia, muscle rigidity, altered mental status, increased creatine phosphokinase activity, and lability of the autonomic nervous system. In such cases, Quetiapine Canon is canceled and appropriate symptomatic therapy is prescribed.

In short-term, placebo-controlled clinical trials using quetiapine as monotherapy, cases of severe neutropenia (neutrophil count below 0.5 × 10 ⁹/ l) in the absence of infection. There are reports of agranulocytosis (severe neutropenia associated with infections) in patients who received quetiapine as part of a clinical trial (rarely), as well as during post-marketing use (including with a fatal outcome). Severe neutropenia most often occurred several months after the start of Quetiapine Canon. The dose-dependent effect was not revealed. After discontinuation of therapy, leukopenia and / or neutropenia resolved. For neutropenia, a prior low leukocyte count and a history of drug-induced neutropenia are considered a possible risk factor. Agranulocytosis also occurred in patients without risk factors. In patients with infection or unexplained fever, the likelihood of neutropenia should be considered.especially in the absence of obvious predisposing factors. These cases should be managed according to clinical guidelines. If the neutrophil count becomes less than 1.0 x 10⁹ / l, Quetiapine Canon is canceled. The patient's condition should be monitored (in order to identify possible signs of infection), control of the level of neutrophils is required (up to exceeding the level of 1.5 × 10 ⁹ / l).

While taking Quetiapine Canon, an increase in body weight is noted. In this case, clinical observation of patients is recommended in accordance with the accepted standards of therapy.

Despite the fact that the causal relationship of Quetiapine Canon with the development of myocarditis and cardiomyopathy has not been identified, if these diseases are suspected, the appropriateness of taking the drug should be assessed.

Patients with a history of diabetes mellitus may develop hyperglycemia or an exacerbation of diabetes mellitus during the treatment period (in some cases, with the development of ketoacidosis or coma, including with a fatal outcome). It is recommended to monitor the condition in order to identify possible symptoms of hyperglycemia, which include polydipsia (pathologically increased thirst), polyuria (an increase in the amount of urine excreted), weakness and increased appetite. To identify a possible deterioration in glycemic control, it is recommended to establish monitoring of patients with diabetes mellitus and patients with risk factors for its development. It is necessary to regularly monitor the weight of patients.

In some patients, against the background of an increase in body weight, an increase in the concentration of lipids and glucose in the blood, a deterioration of the metabolic profile is possible, which requires appropriate medical supervision.

Before and during treatment with Quetiapine Canon, it is necessary to assess the risk factors for the development of venous thromboembolism and take preventive measures.

With the development of jaundice, therapy is stopped.

The relationship between the reception of Quetiapine Canon and a persistent increase in the absolute value of the QT interval has not been identified. However, lengthening of the QT interval was recorded with drug overdose. Prescribing the drug requires caution in patients with diseases of the cardiovascular system and a previously recorded lengthening of the QT interval. Caution is also required when prescribing Quetiapine Canon in combination with drugs that prolong the QT interval, other antipsychotics, especially in elderly patients, patients with congenital lengthening of the QT interval, myocardial hypertrophy, chronic heart failure, hypomagnesemia or hypokalemia.

In case of abrupt withdrawal of Quetiapine Canon, withdrawal syndrome may develop, which is manifested by nausea, vomiting, insomnia, headache, dizziness and irritability. The development of this disorder should be taken into account and the drug should be withdrawn gradually over at least 1-2 weeks.

Dysphagia and aspiration have been reported with quetiapine therapy. Despite the fact that a causal relationship has not been confirmed, caution should be exercised when prescribing Quetiapine Canon to patients at risk of developing aspiration pneumonia.

Constipation is one of the risk factors for bowel obstruction. Against the background of the use of the drug, cases of constipation and intestinal obstruction, including episodes that were fatal, were observed in patients at high risk of intestinal obstruction (including those receiving multiple concomitant drugs aimed at reducing intestinal motility, even in the absence of complaints of constipation).

During clinical trials and post-marketing observation, cases of pancreatitis have been reported (with the administration of Quetiapine Canon, a causal relationship has not been proven). In post-marketing reports, it was recorded that many patients had risk factors for pancreatitis, including alcohol consumption, increased triglyceride concentrations, cholelithiasis.

Information on the combined use of Quetiapine Canon with lithium or divalproate in the treatment of acute manic episodes of mild to moderate severity is limited. There was a good tolerance of this combination and an additive effect in the third week of treatment.

The long-term efficacy and safety of Quetiapine Canon as an adjunctive treatment for major depressive disorder has not been studied, but the efficacy / safety profile has been studied with monotherapy.

Influence on the ability to drive vehicles and complex mechanisms

During the period of taking Quetiapine Canon until the individual tolerance of therapy is determined, it is recommended to refrain from potentially hazardous activities, including driving motor vehicles.

Application during pregnancy and lactation

Quetiapine Canon is not prescribed during pregnancy / lactation.

In pregnant women, the safety and effectiveness of quetiapine has not been established. Based on the available data, it is impossible to draw a definite conclusion about the toxicity in the first trimester of quetiapine pregnancy. However, in animal studies, it was found that the drug has reproductive toxicity. Newborns exposed to neuroleptics (including quetiapine) during the third trimester are at risk of developing adverse reactions, including withdrawal symptoms and / or extrapyramidal events. The duration and severity of these and similar reactions after birth may vary. There are several reports of the development of disorders such as agitation, hypertension, hypotension, tremors, drowsiness, respiratory distress syndrome of the newborn and eating disorder.

The degree of penetration of quetiapine into breast milk is unknown, therefore, if it is necessary to take Quetiapine Canon, breastfeeding should be discontinued.

Pediatric use

For patients under 18 years of age, the drug is not prescribed.

Despite the fact that the efficacy and safety of Quetiapine Canon in children and adolescents have been studied in clinical trials, there are insufficient data.

With impaired renal function

Patients with renal insufficiency of any severity do not need to adjust the quetiapine dosage regimen.

For violations of liver function

Quetiapine Canon for liver failure should be used under medical supervision.

Use in the elderly

For the treatment of psychosis in patients over 65 years of age with dementia, the drug is contraindicated.

When prescribing Quetiapine Canon, elderly patients should be careful.

Drug interactions

• inhibitors of HIV proteases, ketoconazole, clarithromycin, erythromycin and other inhibitors of the isoenzyme CYP3A4: the combination is contraindicated, since in this case there is a significant increase in the AUC of quetiapine;
• drugs that affect the central nervous system, alcohol: when used together, their sedative effect may increase, so the combination requires caution;
• inducers of microsomal liver enzymes (for example, phenytoin): there is a significant increase in the clearance of quetiapine; first it is necessary to assess the expected benefit of therapy with Quetiapine Canon and the risk of withdrawal of the drug-inducer of liver microsomal enzymes. The dose of these drugs should be changed gradually. If necessary, they can be replaced with drugs that do not induce liver microsomal enzymes (in particular, valproic acid preparations);
• dopamine agonists and / or drugs with antiparkinsonian action: these drugs have an antagonistic effect against quetiapine; with combined use, there is a significant increase in the clearance of quetiapine and, accordingly, a decrease in the AUC value, this leads to a decrease in plasma concentration and reduces the effectiveness of Quetiapine Canon;
• lorazepam: its clearance may decrease;
• antipsychotic drugs: when combined with risperidone, haloperidol, the pharmacokinetics of quetiapine does not undergo significant changes, however, when taken simultaneously with thioridazine, a significant increase in quetiapine clearance is noted;
• drugs that can lead to an electrolyte imbalance and prolongation of the QT interval: when combined use, caution should be exercised;
• grapefruit juice: simultaneous use with quetiapine is not recommended;
• lithium preparations: their pharmacokinetics does not change, however, when used simultaneously in adult patients with an acute manic episode, there is a higher incidence of side effects associated with EPS (especially tremor), weight gain and drowsiness.

In patients taking Quetiapine Canon, false-positive results of screening tests for the detection of tricyclic antidepressants and methadone by enzyme immunoassay were noted. In order to confirm the screening results, a chromatographic research method is recommended.

Analogs

Quetiapine Canon analogs are Quetiapine, Ketiap, Ketilept, Nantarid, Quetitex, Laquel, Quentiax, Kumenthal, Gedonin, Quetiapin, Viktoel.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Contoured cell packaging must be stored in a cardboard box. Keep out of the reach of children.

Shelf life is 4 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Quetiapine Canon

Reviews of Quetiapine Canon are few. Most often they can be found on forums where people who take drugs for mental disorders communicate. In general, in terms of effectiveness and portability, Quetiapine Canon is practically not distinguished from analogues.

Price for Quetiapine Canon in pharmacies

The approximate price for Quetiapine Canon for 60 tablets per package depends on the dosage: 25 mg tablets - 684 rubles; tablets 100 mg - 1550 rubles; tablets 200 mg - 2280 rubles; tablets 300 mg - 2788 rubles.

Quetiapine Canon: prices in online pharmacies

Drug name Price Pharmacy

Quetiapine Canon 25 mg film-coated tablets 60 pcs. 572 r Buy

Quetiapine Canon 300 mg film-coated tablets 60 pcs. 2274 RUB Buy

Quetiapine Canon Prolong 150 mg film-coated tablets of prolonged action 60 pcs. 3248 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!