Quetiapine, 100 mg 60 pcs

Pharmacotherapeutic group

Antipsychotic (neuroleptic)

ATX code
N05AH04

Pharmacological action

Quetiapine is an atypical antipsychotic. Quetiapine and its active metabolite N-dezalkylquetiapine (norquetiapine) interact with a wide range of brain neutrotransmitter receptors. Quetiapine and N-desalkylquetiapine exhibit high affinity for 5HT2 – serotonin receptors and D1 and D2 – dopamine receptors, which accounts for the main clinical antipsychotic properties of the drug and low incidence of extrapyramidal side effects.

Quetiapine has no affinity for the noradrenaline transporter and low affinity for 5NT1A , whereas N-dezalkylquetiapine has high affinity for both. Inhibition of the noradrenaline transporter and partial agonism to 5NT1A-serotonin receptors by the metabolite may account for the antidepressant effects of the drug. Quetiapine and N-desalkylquetiapine have high affinity for histamine and α1-adrenoceptors and moderate affinity for α2-adrenoceptors.

Quetiapine shows no appreciable affinity for muscarinic receptors, whereas its metabolite N-dezalkylquetiapine shows moderate to high affinity for several muscarinic receptor subtypes. In standard tests in animals, quetiapine exhibits antipsychotic activity. The specific contribution of the metabolite N-dezalkylquetiapine to the pharmacological activity of quetiapine has not been established.

The results of a study of extrapyramidal symptoms (EPS) in animals revealed that quetiapine causes mild catalepsy at a dose that effectively blocks D2 – dopamine receptors. Quetiapine causes a selective decrease in the activity of mesolimbic A10- dopaminergic neurons compared to the A9- nigrostriatal neurons involved in motor function. The incidence of EPS and concomitant use of M-cholinoblockers was comparable to that of placebo when quetiapine was administered with dose titration in schizophrenia. The drug is well tolerated when taken at recommended doses, including in elderly patients. In placebo-controlled studies in elderly patients with dementia, the incidence of cerebrovascular complications when using quetiapine was not higher than in the placebo group.

The drug is effective against both positive and negative symptoms of schizophrenia. Quetiapine is effective as monotherapy for manic episodes of moderate to severe severity. There are no data on long-term use of the drug for prevention of subsequent manic and depressive episodes. There are limited data on the use of quetiapine in combination with valproate or lithium drugs for moderate to severe manic episodes, but the combination was generally well tolerated and the incidence of EPS and concomitant use of M-choline blockers was comparable to that of placebo. Quetiapine is effective at doses of 300 mg and 600 mg in patients with bipolar disorder types I and II of moderate to severe severity. At the same time, the effectiveness of the drug in doses of 300 mg and 600 mg is comparable. Quetiapine is effective in patients with schizophrenia and mania when taken twice daily, despite a half-life of approximately 7 hours. The effects of quetiapine on 5NT2 and D2 receptors last up to 12 hours after taking the drug. In a clinical study in patients with depressive episodes in the structure of bipolar disorder type I and II, the use of quetiapine at a dose of 300 mg per day was more effective compared to placebo in reducing the total score on the MADRS (Montgomery-Asberg Depression Rating Scale. Montgomery-Asberg Depression Rating Scale).

In 4 additional 8-week clinical trials of quetiapine in patients with moderate to severe depressive episodes of bipolar disorder, quetiapine at 300 mg and 600 mg doses was more effective than placebo: mean improvement in MADRS scores and improvement in overall MADRS scores (at least 50%) over baseline values. In a short-term (9-week) study in patients without dementia aged 66 to 89 years with major depressive disorder, quetiapine at doses ranging from 50 mg to 300 mg (the dose was adjusted for clinical response; the average daily dose was 160 mg) reduced depression symptoms compared with placebo. The incidence of EPS and weight gain in stable patients with schizophrenia did not increase with long-term therapy with the drug. In studies of major depressive disorder according to DSM-IV (Diagnostic and Statistical Manual of Mental Disorders (4th ed.)) criteria, no increased risk of suicidal behavior or suicidal ideation was observed when taking the drug compared to placebo. There were no differences in the incidence of extrapyramidal symptoms and concomitant use of anticholinergic medications when using quetiapine at 75-750 mg daily compared to placebo.

Quetiapine does not cause prolonged increases in plasma prolactin concentrations. No differences in prolactin concentrations have been found when using quetiapine or placebo at fixed dose. When quetiapine was used in doses up to 800 mg/day to treat moderate to severe manic episodes both in monotherapy and in combination with lithium or valproate seminary, the incidence of EPS and concomitant use of M-choline blockers was comparable to that with placebo.

. In two short-term (6-week) studies of combination therapy of a depressive episode with quetiapine at a dose of 150 mg/day and 300 mg/day with amitriptyline, bupropion, cipopram, duloxetine,escitalopram fluoxetine, paroxetine, sertraline, or venlafaxine in patients with suboptimal response to antidepressant monotherapy showed improvement in depression symptoms on the Montgomery-Asberg Depression Rating Scale (MADRS). Montgomery-Asberg Depression Rating Scale) (rms change of 2-3.3 points) compared to antidepressant monotherapy.

Indications

– schizophrenia.

– manic episodes in the structure of bipolar disorder.

– depressive episodes of moderate to severe severity in the structure of bipolar disorder.

Quetiapine is not indicated for prevention of manic and depressive episodes.

Active ingredient

Composition

Microcrystalline cellulose – 34.870 mg,

Lactose monohydrate – 18.000 mg,

sodium carboxymethyl starch (sodium starch glycolate, type A) – 14.000 mg,

povidone K-30 – 8,000 mg,

talk – 5,000 mg,

colloidal silicon dioxide – 3,000 mg,

magnesium stearate – 2,000 mg;

coating:

[hypromellose – 3,600 mg, talc – 1,200 mg, titanium dioxide – 0,660 mg, macrogol 4000 (polyethylene glycol 4000) – 0,540 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] – 6,000 mg.

How to take, the dosage

Overly, 2-3 times a day, regardless of meals There are different patterns of administration of the drug, the physician should give clear instructions to the patient on the dosing regimen.

Adults

Acute and chronic psychoses including schizophrenia.

The drug is prescribed 2 times daily. The total daily dose for the first 4 days of therapy is 50 mg (day 1), 100 mg (day 2), 200 mg (day 3), 300 mg (day 4). Beginning on day 4, the dose should be adjusted to an effective dosage, usually between 300 and 450 mg/day. Subsequently, if a dose adjustment is necessary, it is recommended that the daily dose be increased by 50-100 mg at 2-day intervals. Depending on clinical effect and individual tolerance of the drug, the dose may vary from 150 to 750 mg/day. The maximum daily dose of quetiapine is 750 mg.

Treatment of manic episodes in the structure of bipolar disorder.

Quetiapine is used as monotherapy or in combination with drugs with normotensive effects. The drug is prescribed 2 times a day. The daily dose for the first 4 days of therapy is: 100 mg (day 1), 200 mg (day 2), 300 mg (day 3), 400 mg (day 4). Further, by the 6th day of therapy, the daily dose of the drug can be increased to 800 mg. The daily dose should not be increased faster than 200 mg per day. The daily dose is divided into two doses. Depending on the clinical effect and individual tolerance of the patient, the dose may vary from 200 to 800 mg/day. Usually the effective dose is 400 to 800 mg/day. The maximum daily dose of quetiapine is 800 mg.

Treatment of moderate to severe depressive episodes in the structure of bipolar disorder.

Quetiapine is prescribed once daily at bedtime. The daily dose for the first 4 days of therapy is: Day 1 – 50 mg, Day 2 – 100 mg, Day 3 – 200 mg, Day 4 – 300 mg. The recommended dose is 300 mg/day. Maximum daily dose is 600 mg. The antidepressant effect of quetiapine has been confirmed when used in doses of 300 and 600 mg per day. In short-term therapy, the efficacy of quetiapine in doses of 300 and 600 mg was comparable.

Elderly patients

In elderly patients, the starting dose of the drug 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 lower than in younger patients. In elderly patients, quetiapine (as well as other neuroleptics) should be taken with caution, especially at the beginning of therapy. The selection of an effective dose in such patients may be slower, and the daily therapeutic dose is lower than in younger patients. The average plasma clearance of quetiapine is 30-50% lower in elderly patients compared to younger patients. In addition, patients in this group have more frequent liver, kidney, nervous system and cardiovascular disease, and concomitant treatment is more common.

Patients with renal failure

Dose adjustment is not required. Patients with hepatic impairment Quetiapine is extensively metabolized in the liver. Therefore, caution should be exercised when using the drug in patients with hepatic impairment, especially at the beginning of therapy. It is recommended to start quetiapine therapy with a dose of 25 mg/day and increase the dose daily by 25-50 mg until therapeutic effect is achieved. Maintenance therapy To maintain remission, it is advisable to use the lowest dose. Patients should be evaluated periodically to determine the need for maintenance therapy. Resumption of interrupted treatment in patients who have previously received quetiapine. If therapy is resumed less than 1 week after quetiapine withdrawal, the drug may be continued at a dose adequate for maintenance therapy. When resuming therapy in patients who have not received quetiapine for more than 1 week, initial dose selection rules should be followed and an effective dose should be established until the patient’s clinical response.

Contraindications

– hypersensitivity to any component;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

– concomitant use with cytochrome P450 isoenzyme inhibitors, including antifungal agents – azole derivatives, erythromycin, clarithromycin, nefazodone, HIV protease inhibitors (see “Interaction with other drugs”). section “Interaction with other medicinal products”).

Psychosis and elderly patients with dementia.

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