Quetiapine
Quetiapine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Quetiapine
ATX code: N05AH04
Active ingredient: quetiapine (quetiapine)
Manufacturer: Drug Technology (Russia), Kanonpharma production, CJSC (Russia), Severnaya Zvezda (Russia), VERTEX, JSC (Russia)
Description and photo update: 2018-21-11
Prices in pharmacies: from 572 rubles.
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Quetiapine is a drug with an antipsychotic effect.
Release form and composition
Dosage form - film-coated tablets: round biconvex, the core and shell of almost white or white color (in a cardboard box 1 glass, polyethylene or polymer can / bottle of 30, 60 or 90 pcs. Or 1-4, 6 blisters 10, 15, 20 or 30 pcs.).
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 hydrogen phosphate 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 an atypical antipsychotic drug. Shows a higher affinity for hydroxytryptamine (serotonin) receptors (5HT2) than for dopamine D1 and D2 receptors in the brain. It also has a more pronounced affinity for histamine and alpha1-adrenergic receptors and less for alpha2-adrenergic receptors.
No noticeable affinity of quetiapine for benzodiazepine and muscarinic receptors was found. Shows antipsychotic activity in standard tests.
Pharmacokinetics
When administered orally, quetiapine is well absorbed from the gastrointestinal tract and is actively metabolized in the liver. The main metabolites in plasma do not possess pronounced pharmacological activity.
Food intake has no 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.
There are no differences in pharmacokinetic parameters in women and men. Pharmacokinetics is linear.
In elderly patients, the average clearance of quetiapine is 30-50% less than in patients 18-65 years old.
In severe renal failure (creatinine clearance up to 30 ml / min / 1.73 m 2) and liver damage, the mean plasma clearance of quetiapine is approximately 25% less, but the interindividual clearance values are within the range that corresponds 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 in unchanged form). It has been established that CYP3A4 is a key isoenzyme of quetiapine metabolism.
In a study of the pharmacokinetic parameters of quetiapine in 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 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 there will be a clinically pronounced inhibition of cytochrome P450-mediated metabolism of other drugs.
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 that predispose to the development of arterial hypotension;
- burdened history of seizures;
- liver failure;
- elderly age;
- pregnancy.
Instructions for the use of Quetiapine: method and dosage
The tablets are intended for oral administration.
The recommended daily dose for 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 can 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 permissible 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 effective.
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 triglyceride concentration and blood cholesterol.
Therapy may be accompanied by the occurrence of moderate asthenia, dyspepsia and rhinitis, an increase in body weight (mainly in the first weeks of treatment). Quetiapine can cause dizziness, orthostatic hypotension, tachycardia, and, in some cases, fainting. Violations occur mainly in the initial period of dose selection.
The intake of Quetiapine is associated with a small dose-dependent decrease in the concentration of thyroid hormones, in particular, total and free T4. The maximum decrease in indicators is recorded at the second and fourth weeks of treatment. In the future, with prolonged use, a decrease in the concentration of hormones is not observed.
With prolonged therapy, there is a potential for tardive dyskinesia. With the development of symptoms of the disease, the dose should be reduced or the drug should be discontinued. With a sharp cancellation of Quetiapine in high doses, the following acute reactions (withdrawal syndrome) may develop: vomiting, nausea, 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 canceled 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, increasing the 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, decreased T4 concentration;
- allergic reactions: angioedema, eosinophilia, anaphylactic reactions, skin rash, Stevens-Johnson syndrome;
- others: galactorrhea, visual impairment (including blurred visual perception), 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 have been described, after which fatal consequences did not develop and complete recovery was observed. However, there is information about extremely rare cases of overdose, which led to coma and death.
Overdose symptoms may result from increased pharmacological effects of Quetiapine - drowsiness, excessive sedation, tachycardia, and lower blood pressure.
There is no specific antidote. Treatment is symptomatic. In cases of overdose, the following measures are shown: gastric lavage (after intubation, in cases where the patient is unconscious), taking laxatives and activated charcoal (with the aim of removing unabsorbed Quetiapine). The effectiveness of these measures has not been studied. Also, measures are 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 people). The relationship between taking the drug and an increase in QTc (corrected with respect to heart rate, the value of the QT interval) was not revealed. 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 psychoses associated with dementia. 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 / increase of symptoms of tardive dyskinesia is possible.
If neuroleptic malignant syndrome occurs, treatment should be canceled.
Quetiapine should be used with caution in combination with other drugs that depress the central nervous system, or alcohol.
Therapy in children, adolescents and patients under 24 years of age with depression and other mental disorders can lead to the appearance of suicidal thoughts / behavior. Before prescribing the drug for 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 and 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.
Application during pregnancy and lactation
- pregnancy: the drug can be used under medical supervision;
- lactation period: therapy is contraindicated.
Pediatric use
For patients under 18 years of age, Quetiapine therapy is contraindicated.
With impaired renal function
According to the instructions, Quetiapine should be administered with caution in patients with renal insufficiency in a reduced initial dose (25 mg per day).
For violations of liver function
The drug should be administered to patients with hepatic impairment with caution at a reduced initial dose (25 mg per day).
Use in the elderly
Quetiapine should be prescribed with caution in elderly patients at a reduced initial dose (25 mg per day).
Drug interactions
Possible interactions:
- antifungal agents of the azole group, clarithromycin, erythromycin, nefazodone (drugs with a potent 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: increasing the clearance of quetiapine;
- drugs that depress the central nervous system and ethanol: an increase in the likelihood of developing adverse reactions of quetiapine.
Analogs
The analogues of Quetiapine are Servitel, Quetipex, Ketiap, Ketilept, Quentiax, Viktoel, Seroquel, Kumenthal, Laquel, Nantarid, Gedonin.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Quetiapine
According to reviews, Quetiapine is an effective drug. Of the shortcomings, they usually indicate the appearance of drowsiness, which develops in varying degrees of severity.
Price for Quetiapine in pharmacies
The approximate price for Quetiapine 100 mg - 1140 rubles, 200 mg - 1161-2210 rubles, 300 mg - 1709-2757 rubles, 25 mg - 559-782 rubles (the price is indicated for a package of 60 tablets).
Quetiapine: prices in online pharmacies
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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!
