How Effective Is Quetiapine for Bipolar?

Quetiapine fumarate tablets, this product is used to treat schizophrenia and treat manic episodes of bipolar disorder.

Drug Name: Quetiapine fumarate tablets
Drug type: Occupational injury medical insurance

Hanyu Pinyin: Fu Ma Suan Kui Liu Ping Pian
Use classification: Other antipsychotics

Caution of quetiapine fumarate tablets

Elderly patients with dementia-related psychosis are at risk of increased mortality when treated with antipsychotics. In 17 placebo-controlled trials completed by such patients (with a modest course of about 10 weeks), the risk of death from atypical antipsychotics is 1.6-1.7 times that of placebo. In a typical 10-week controlled clinical study, the mortality rate was 4.5% in the drug-treated group and 2.6% in the placebo control group. Although the causes of death vary, most die from cardiovascular disease (such as heart failure, sudden death) or infection (such as pneumonia). Observational studies suggest that, similar to atypical antipsychotics, traditional antipsychotics may also increase mortality. It is unclear to what extent the increase in mortality in these observational studies is due to antipsychotics or some patient characteristics. This product (quetiapine fumarate) is not approved for the treatment of dementia-related psychosis.

Quetiapine fumarate tablets ingredients

The main ingredient of this product is quetiapine fumarate. Its chemical name is 11- {4- [2- (2-hydroxyethoxy) ethyl-1-piperazinyl]} diphenylhydrazone (b, f) (1,4) thiazeptofumarate (2: 1)
Chemical Structure:

http://x1.webres.medlive.cn/drugref/ChemPreparationDetail/201306191533330485.jpg

Molecular formula: (C ₂₁ H ₂₅ N ₃ O ₂ S ₂ · C ₄ H ₄ O ₄
Molecular weight: 883.08

Quetiapine fumarate tablet properties

25mg, 0.1g, 0.2g are biconvex circular film-coated tablets, 25mg is pink, 0.1g is yellow, 0.2g is white; 0.3g is a capsule-shaped white film-coated tablet, all of which appear white after removing the film coating.

Indications of quetiapine fumarate tablets

This product is used to treat schizophrenia and treat manic episodes of bipolar disorder.

Specifications of quetiapine fumarate tablets

(1) 25mg (2) 0.1g (3) 0.2g (4) 0.3g (based on C ₂₁ H ₂₅ N ₃ O ₂ S)

Dosage and dosage of quetiapine fumarate tablets

oral. Take 2 times a day before or after meals.
adult:
1. For the treatment of schizophrenia:
The total daily dose at the beginning of treatment was: 50 mg on the first day, 100 mg on the second day, 200 mg on the third day, and 300 mg on the fourth day.
After the fourth day, the dose will be gradually increased to the effective dose range, usually 300-450 mg per day. The dose can be adjusted to 150-750 mg per day based on the patient's clinical response and tolerability.
2. Manic episodes used to treat bipolar disorder:
When used as a monotherapy or as an adjuvant therapy for mood stabilizers, the total daily dose at the beginning of treatment is 100 mg on the first day, 200 mg on the second day, 300 mg on the third day, and 400 mg on the fourth day. By the sixth day, the dose can be further adjusted to 800 mg per day, but the daily dose increase cannot exceed 200 mg.
The dose can be adjusted to 200-800mg per day according to the clinical response and tolerability of the patient, and the commonly used effective dose range is 400-800mg per day.
Elderly patients:
As with other antipsychotic drugs, this product is used with caution in elderly patients, especially when starting medication. The starting dose for elderly patients should be 25 mg daily. Subsequently, the effective dose is increased daily in the range of 25-50 mg, but the effective dose may be lower than that of young patients.
Patients with kidney and liver damage:
The clearance rate after oral quetiapine decreases in patients with kidney and liver damage by about 25%. Quetiapine is extensively metabolized in the liver and should be used with caution in patients with liver damage.
For patients with kidney or liver damage, the starting dose of this product should be 25 mg daily. It is then increased daily to an effective dose in the range of 25-50 mg.
Or as directed by your doctor.

Adverse reactions of quetiapine fumarate tablets

The following table lists the incidence of adverse reactions (ADRs) during the treatment of this product.

1. Triacylglycerol 200mg / dL (> 2.258 mmol / L) occurred at least once.
2. Cholesterol 240mg / dL (> 6.2064 mmol / L) occurred at least once.
3. Like other antipsychotic drugs, this product may also cause weight gain, which mainly occurs in the first few weeks of treatment.
4. Fasting blood glucose 7.0 mmot / L or non-fasting blood glucose 11.1 mmol / L occurred at least once.
5. The calculation of the incidence of these adverse reactions is only based on post-marketing data.
6. Platelet count 100x10 ⁹ / L at least once
7. Only in clinical trials of bipolar depression, the incidence of dysphagia caused by this product was higher than placebo.
8. According to reports of adverse events in clinical trials, elevated serum creatine phosphatase was not associated with neuroleptic malignant syndrome.
9. It is very rare that diabetic patients cause exacerbations of diabetes during treatment with quetiapine.
Neutropenia: In placebo-controlled monotherapy treatment of patients with baseline neutrophils> 1.5 = 10 ⁹ L, in patients treated with this product. At least one occurrence of neutrophils (<1.5x10 ⁹ > 1.5x10 ⁹ L) occurred in patients treated with this product at least once with a neutrophil count <0.5x10 ⁹ / L of 0.21% in the placebo group Is O%. Patients treated with this product at least once had a neutrophil count of 0.5x10 ⁹ / l and <1.OxlO ⁹ / L (0.75% vs. 0.11% in the placebo group).
Extrapyramidal symptoms: In short-term, placebo-controlled clinical trials in patients with schizophrenia and bipolar mania, the incidence of extrapyramidal symptoms is similar to placebo (schizophrenia: 7.8% for this product and placebo for 8.0%; bipolar mania: this product is 11.2%, placebo is 11.4%).
In the use of antipsychotics, reports of prolonged QT, ventricular arrhythmias, unexplained sudden death, cardiac arrest, and apical torsional ventricular tachycardia have been reported very rarely and are considered to be similar drugs (see Warnings).
Thyroid level: Treatment with this product may be accompanied by a slight, dose-related decrease in thyroid hormone levels, especially total T4 and free T4. The decline in total T4 and free T4 was most significant in the second to fourth weeks of quetiapine treatment, and there was no further decline during long-term treatment. Almost all patients could recover their effects on total T4 and free T4 after quitting quetiapine And, regardless of the course of treatment, only a small decrease in total T3 and anti-T3 was observed at high doses. TBG levels have not changed, and there is generally no corresponding increase in TSH, which indicates that this product will not cause clinically significant hypothyroidism.
There have been reports of jaundice in the application of this product.

Quetiapine fumarate tablets contraindications

Patients who are allergic to any of the ingredients in this product.
caveat
1. Elderly people with dementia-related psychosis < br This product has not been approved to treat patients with dementia-related psychosis.
In randomized placebo-controlled clinical trials of atypical antipsychotics in patients with dementia, the risk of cerebrovascular adverse events has increased approximately three-fold. The mechanism for this increased risk has not yet been clarified. This risk cannot be ruled out for other antipsychotics or other patients.
This product should be used with caution in patients with risk factors for stroke.
2. Suicide / Suicidal Thoughts or Clinical Deterioration Depression in bipolar disorder is associated with an increased risk of suicidal thoughts, self-harm, and suicide (suicide-related events), and the risk will continue until the condition is reduced. Because the condition may not improve for weeks or longer after the start of treatment, the patient should be closely monitored until the condition improves. Common clinical experience suggests that the risk of suicide may increase during the early stages of recovery.
In clinical trials of patients with major depressive episodes of bipolar disorder, suicide was observed in young adult patients under 25 years of age compared with the placebo group (3.0% and 0%) in the quetiapine group Increased risk of related events.
3. Nerve blocker malignant syndrome < br br Antipsychotic drugs (including this product) treatment will be accompanied by a nerve blocker malignant syndrome. Clinical manifestations include high fever, altered mental state, muscle rigidity, autonomic dysfunction, and increased creatine phosphokinase activity. If this happens, this product should be discontinued and given appropriate treatment.
4. Tardive dyskinesia Like other antipsychotic drugs, long-term treatment with this product may also cause tardive dyskinesia. If there are signs and symptoms of tardive dyskinesia, the dose of this product should be reduced or discontinued.
5. Cardiovascular disease < br This product should be used with caution in patients with known cardiovascular disease, cerebrovascular disease, or other patients with a tendency to hypotension.
Like other antipsychotic drugs with alpha1 adrenergic blocking effects, this product may cause orthostatic hypotension (with dizziness), tachycardia, and syncope in some patients; these events mostly occur at the initial dose Increase period. Orthostatic hypotension is more common in older patients than in younger patients.
6. QT interval extension <br br In clinical trials and in accordance with the instructions, the use of quetiapine does not accompany the permanent extension of the absolute QT interval. However, in the case of overdose (see [Drug Overdose]), a prolonged QT interval was observed. As with other antipsychotics, this product should be used with caution in patients with cardiovascular disease or a family history of prolonged QT interval. Furthermore, caution should be exercised with other drugs known to prolong the QT interval and with neuroleptics. Especially for elderly patients, patients with prolonged QT syndrome, patients with congestive heart failure, patients with cardiac hypertrophy, patients with hypokalemia or patients with hypomagnesemia (see [Drug Interactions]).
7. Severe neutropenia < br In clinical trials, severe neutropenia (number of neutrophils <0.5 × 10 ⁹ / L is not commonly reported. Most neutrophils The reduction occurred within months of starting quetiapine. There was no significant dose relationship. Risk factors that could cause neutropenia include low baseline white blood cell count and a history of neutropenia caused by the drug. Neutrophil count This product should be discontinued in patients <1.0 × 10 ⁹ / L. Patients should be observed for signs, symptoms, and neutrophil counts (until they exceed 1.5 × 10 ⁹ / L).
8. Epilepsy < br In clinically controlled trials, the incidence of epilepsy in patients taking this product was not different from patients taking placebo. As with other antipsychotics, care should be taken when this product is used to treat patients with a history of epilepsy.
9. Drowsiness < br The treatment of this product is related to drowsiness and related symptoms (such as sedation), usually in the first two weeks of treatment, and usually can be eliminated after continuous administration.
10. Acute withdrawal drug < br In the clinical trials of acute placebo-controlled monotherapy to evaluate symptoms of withdrawal, the most common withdrawal symptoms observed were: insomnia, nausea, headache, diarrhea, vomiting, dizziness And irritable. The incidence of these reactions decreased significantly after one week of discontinuation. Following the sudden discontinuation of high-dose quetiapine, in addition to the acute withdrawal, psychiatric symptoms may recur, and involuntary dyskinesias (such as inactivity, dystonia, and dyskinesia) have been reported. Therefore, it is recommended that this product be gradually withdrawn within at least one to two weeks.
11. Effect on the liver < br Some patients taking this product have observed asymptomatic elevated serum aminotransferase (ALT, AST) or -GT levels. If jaundice occurs, discontinue use of this product.
12. Hyperglycemia < br There are reports of hyperglycemia and exacerbation of pre-existing diabetes. Proper clinical monitoring is recommended when diabetic patients and people at high risk of diabetes take this product.
13. Lipids < br In clinical trials using this product, triglycerides and cholesterol were observed to increase (see [Adverse Reactions]). Elevation of lipids should be properly controlled.
14. Weight gain < br Cases of weight gain have been found in clinical trials. Patients treated with this product should monitor their weight regularly.
Clinical studies have observed that some patients have experienced deterioration in body weight, blood glucose, or lipid metabolism parameters. Changes in these parameters should be handled as appropriate in the clinic.
15. Cataracts Long-term treatment studies in dogs have shown that quetiapine can cause cataracts. Lens changes have also been found in long-term treatment of adults, children, and adolescents, but it is not clear whether there is a causal relationship with quetiapine. The possibility of lens changes cannot be ruled out at this time. Therefore, it is recommended that the lens be inspected by slit lamp or other suitable and sensitive methods every 6 months at the beginning of treatment or short-term and long-term treatment after the start of treatment, and early detection of cataracts.
16. Hyperprolactinemia < br In clinical trials, the incidence of prolactin levels in the treatment group and placebo treatment group increased to clinically significant values of 3.6% (158/4416) and 2.6%, respectively. (51/1968). Like other drugs that antagonize the dopamine D2 receptor, quetiapine can increase prolactin levels in some patients and is sustainable during long-term treatment. Regardless of the cause, hyperprolactinemia can inhibit the hypothalamus and reduce pituitary gonadotropin secretion. This in turn can inhibit reproductive system function by damaging gonad steroid production in male and female patients. There are reports of galactorrhea, amenorrhea, gynecomastia, and male fistula in patients taking prolactin-raising compounds. Long-term hyperprolactinemia, if coexisted with hypogonadism, can lead to decreased bone mineral density in men and women.
17. Abnormal penile erection <br A report of abnormal penile erection has been received in 1 patient before using this product. Although it is not clear whether there is a causal relationship with this product, other drugs with alpha-adrenergic blocking effects are known to induce abnormal penile erections, so this product is also considered to have this possibility. Severe penile erections require surgical intervention.
18. Temperature regulation < br Antipsychotic drugs can disrupt the body's ability to reduce core body temperature, but this product has not been reported. This product should be given appropriate care in patients who may increase core body temperature (such as excessive exercise, exposure to extreme heat, combined use of anticholinergic drugs, or dehydration).
19. Swallowing difficulties < br Esophageal motor dysfunction and aspiration are considered to be related to the use of antipsychotics. Aspiration pneumonia is a common cause of morbidity and mortality in elderly patients, especially those with advanced Alzheimer's dementia. This product and other antipsychotics should be used with caution in patients at risk for aspiration pneumonia.

Precautions for quetiapine fumarate tablets

1. Lactose < br This product contains lactose. Patients with rare hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this product.
2. Impact on driving and operating the machine Due to this product may cause drowsiness. Patients who operate dangerous machines, including driving vehicles, should therefore be reminded.

Quetiapine fumarate tablets for pregnant and lactating women

The efficacy and safety of this product in human pregnancy have not been confirmed (see [Pharmacology and Toxicology] for animal reproductive toxicity information). Therefore, this product can only be used in pregnant patients under the circumstances of potential risks.
The excretion of quetiapine in human milk is unknown. Nursing women who take this product should advise that they discontinue breastfeeding while taking the drug.

Quetiapine fumarate tablets for children

The safety and effectiveness of this product for children and adolescents have not been evaluated.

Quetiapine fumarate tablets for elderly

For details, please refer to [Usage and Dosage].

Drug interactions of quetiapine fumarate tablets

1. Since quetiapine mainly has the role of the central nervous system, this product should be used with caution when it is used with other drugs or alcoholic beverages acting on the central nervous system.
2. The combination of this product with lithium salt preparation will not affect the pharmacokinetics of lithium.
3. When this product is used in combination with valproic acid hemi-sodium, the pharmacokinetics of valproic acid and quetiapine will not change clinically. (Semi-sodium valproate is a stable complex with sodium valproate and valproic acid in a molar ratio of 1: 1).
4. The combination of antipsychotic drugs risperidone or haloperidol does not significantly change the pharmacokinetics of quetiapine. However, when this product is combined with thioridazine, the clearance rate of quetiapine of this product will be increased.
5. Quetiapine does not induce liver enzyme systems related to antipyrine metabolism. However, in a multi-dose clinical trial, patients were evaluated for the pharmacokinetics of quetiapine before or during treatment with carbamazepine, a known inducer of liver enzymes. The results showed that carbamazepine combined significantly increased the clearance of quetiapine. This increase reduced the systemic absorption level (based on AUC) of quetiapine by 13% compared to when taken alone; however, a more significant effect was observed in some patients, namely lower plasma concentrations, so for each patient Higher doses of this product should be considered based on clinical response. It should be noted that the maximum recommended daily dose of this product for the treatment of schizophrenia is 750mg / day, and the maximum recommended daily dose for the treatment of manic episodes of bipolar disorder is 800mg / day. Individual patients have carefully evaluated the risks and benefits before considering continued use of higher doses.
6. The combination of phenytoin with another microsomal enzyme inducer can also increase the clearance of quetiapine. If quetiapine is combined with phenytoin or other liver enzyme inducers (such as barbiturates, rifampicin), in order to maintain the effect of antipsychotic symptoms, the dose of this product should be increased. If phenytoin or carbamazepine or other liver enzyme inducers are discontinued and replaced with a non-inducing agent (such as sodium valproate), the dose of this product needs to be reduced.
7. In cytochrome P450, the main enzyme that mediates quetiapine metabolism is CYP3A4. Combination with cimetidine (a known P450 enzyme inhibitor) does not alter the pharmacokinetics of quetiapine. Combination with the antidepressant imipramine (a known inhibitor of CYP2D6) or fluoxetine (a known inhibitor of CYP3A4 and CYP2D6) does not significantly change the pharmacokinetics of quetiapine. However, caution should be exercised if this product is combined with strong inhibitors of CYP3A4 (such as azole antifungals, macrolide antibiotics, or protease inhibitors) (see [Pharmacokinetics]).
8. Caution should be exercised when combining this product with drugs that can cause electrolyte imbalance or prolonged QT _C interval.

Quetiapine fumarate tablets overdose

In clinical trials, there have been reports of death after acute overdose of 13.6 g of this product. In the post-marketing experience, there have been reports of death after taking 6g of this product alone. However, there are also reports of survival after acute overdose of 30 g of this product.
In post-marketing experience, very rare reports of quetiapine overdose alone leading to death or coma or prolonged QT.
In general, the symptoms and signs reported in the overdose of this product are enhancements of the known pharmacological effects of the drug, namely drowsiness and sedation, tachycardia and hypotension.
Patients with severe cardiovascular disease have an increased risk of overdose (see [Caution] Cardiovascular Disease)
Treatment: Quetiapine has no specific antidote. Patients with severe poisoning should consider the possibility of involving multiple drugs and recommend active monitoring measures, including opening a good airway, ensuring adequate oxygen and ventilation, and monitoring and maintaining cardiovascular function. Although it has not been studied how to prevent absorption when the drug is overdose, gastric lavage can be performed in severe poisoning, if possible, within 1 hour after ingestion. Consideration should be given to using activated carbon.
Close medical monitoring and monitoring should be taken until the patient recovers.

Pharmacology and toxicology of quetiapine fumarate tablets

Pharmacological action Mechanism of action Oquinapine is a new type of atypical antipsychotic. Quetiapine and its metabolite N-dehydroquinidine in human plasma can interact with a variety of neurotransmitter receptors. In the brain, quetiapine and N-dehydroquinolidine have affinity for serotonin (5-HT ₂ ) receptors and dopamine D ₁ and dopamine D ₂ receptors. In the brain, quetiapine has a higher affinity for serotonin (5-HT ₂ ) receptors than dopamine D ₁ and dopamine D ₂ receptors N-dehydroquinolidine has noradrenaline transporter (NET) High affinity. Quetiapine and N-dehydroquinetine also have a high affinity for histamine and adrenergic l receptors, but have low affinity for adrenergic 2 receptors and serotonin (5-HT1) receptors. Quetiapine has essentially no affinity for cholinergic muscarinic receptors or benzodiazepine receptors.
2. Non-clinical efficacy quetiapine is positive for antipsychotic drug activity tests such as conditional avoidance reflex. It can also block the effects of dopamine antagonists, both in behavioral and electrophysiological tests, and can increase the concentration of dopamine metabolites, a neurochemical indicator of D ₂ receptor blockade.
The probability of the occurrence of EPS predicted by animal test results shows that the dose of quetiapine that effectively blocks dopamine D ₂ receptors results in only mild tonicity: quetiapine selectively reduces Al0 dopaminergic neurons in the limbic system of the midbrain. Discharges have a weak effect on nigrostriatal A9 neurons related to motor function: In allergic monkeys, quetiapine shows only a slight dystonia-causing effect.
The strength of N-dehydroquinolidine metabolite on the pharmacological action of this product in human body is not clear.
3 Clinical efficacy <br Results of three placebo-controlled clinical trials, including a trial of quetiapine at a dose of 75-750mg per day, showed that the incidence of EPS caused by quetiapine is similar to the incidence of EPS in the placebo group. There was no difference in the incidence of anticholinergic EPS.
In four controlled clinical trials, this product (maximum dose to 800 mg) was evaluated as a monotherapy and adjuvant lithium or valproic acid sodium in the treatment of bipolar affective manic episodes. This product was compared with a placebo. There were no differences in the incidence of EPS and the combined use of anticholinergic drugs.
Quetiapine does not produce persistent prolactin elevation. The results of a multiple fixed-dose clinical trial showed that there were no differences in the levels of prolactin between the different quetiapine dose groups and between placebo groups.
Clinical trials have shown that quetiapine is effective in treating both positive and negative symptoms of schizophrenia. One trial with chlorpromazine and two with haloperidol showed that the short-term efficacy of quetiapine is comparable to that of the control drug.
Clinical trials have shown that this product is effective in reducing manic symptoms in patients with bipolar disorder, either as monotherapy or as adjuvant therapy. For those who responded, the average median dose in the last week was about 600 mg, and about 85% of those who responded ranged from 400 to 800 mg per day.
Toxicological research Acute toxicity Quathiopine has low acute toxicity. The typical antipsychotic effects of mice and rats following oral (500 mg / kg) or intraperitoneal injection (100 mg / kg) include reduced activity, drooping of the upper eyelid, loss of righting reflex, drooling, and convulsions.
2. Repeated administration toxicity < br Repeated use of quetiapine in rats, dogs, and monkeys shows the expected antipsychotic-like central nervous system effects (such as sedation at low doses, tremor at high doses, convulsions, or weakness) .
Hyperprolactinemia caused by the antagonism of quetiapine or its metabolites on the dopamine D2 receptor varies among animals of different breeds, but is most prominent in rats, in a 12-month continuous study A series of effects were found, including hyperplasia of the mammary glands, increased weight of the pituitary, decreased weight of the uterus, and accelerated female development.
The reversible morphological and functional effects on the liver consistent with liver enzyme induction are seen in mice, rats, and monkeys.
Thyroid cell proliferation and corresponding changes in plasma thyroid hormone levels can be seen in rats and monkeys.
Pigmentation of several tissues, especially the thyroid, does not accompany any morphological function.
Transient heart rate increases have occurred in dogs, but without accompanying effects on blood pressure.
Post-triangular cataracts were found after 6 months of administration to dogs at 100 mg / kg daily, which is consistent with the inhibition of crystal cholesterol biosynthesis. No cataract was found in cynomolgus monkeys or rodents administered at doses up to 225 mg / kg daily. No corneal turbidity associated with the drug was detected in human clinical research monitoring.
No neutropenia or agranulocytosis was found in all toxicity studies.
3. Carcinogenicity <br In rat studies (daily doses of 0, 20, 75, and 250 mg / kg), it was found that the incidence of breast cancer in female rats increased in various dose groups, followed by a long-term high Prolactinemia.
In male rats (250 mg / kg daily) and mice (250 and 750 mg / kg daily), the incidence of benign adenoma-like changes in thyroid vesicle cells increased. This is consistent with known rodent-specific results due to increased clearance of thyroid hormone by the liver.
4. Reproductive toxicity < br The effects associated with increased prolactin levels (slightly reduced male fertility and pseudopregnancy, prolonged estrus, prolonged precopulation interval, and decreased chance of conception) can be seen in rats, but This has no direct relevance to humans because hormonal control of reproductive processes is different between different species. Quetiapine has no teratogenic effect.
5. Genotoxicity Genetic toxicology studies have shown that quetiapine has no mutagenic and fragmentation effects.

Pharmacokinetics of quetiapine fumarate tablets

Quetiapine is well absorbed and completely metabolized after oral administration. Eating has no significant effect on the bioavailability of quetiapine. Quetiapine has a plasma protein binding rate of 83%. The steady-state peak concentration of the active metabolite N-dehydroquinolidine is 35% of quetiapine. The elimination half-lives of quetiapine and N-dehydroquinidine are about 7 and 12 hours, respectively.
Clinical trials have confirmed that quetiapine is effective when administered twice daily. Data from positron emission tomography (PET) studies have further confirmed that the drug's placeholder effect on 5-HT2 and D2 receptors can last 12 hours after administration.
The pharmacokinetics of quetiapine and N-dehydroquinetine are linear and there is no gender difference. The average clearance rate of quetiapine in the elderly is 30-50% lower than that of adults 18-65 years old.
In patients with severe renal impairment (creatinine clearance below 30ml / min / 73m ² ) and liver impairment (stable alcoholic cirrhosis), the average plasma clearance of quetiapine can be reduced by about 25%, but the individual-clearance value They are all within the normal population. In urine, the average molar ratio of free quetiapine and human plasma active metabolite N-dehydroquinolidine is less than 5%.
The metabolism of quetiapine is relatively complete. The prototype compounds in urine or feces after taking radiolabeled quetiapine account for less than 5% of the unchanged drug-related substances. About 73% of the radioactive material is excreted from urine and 21% is excreted from feces.
In vitro studies confirmed that the main metabolic enzyme of quetiapine is CYP3A4 of the cytochrome P450 enzyme system. N-dealkylated quetiapine is mainly formed and eliminated by CYP3A4.
In a multi-dose clinical trial, the pharmacokinetics of quetiapine in healthy volunteers before or during ketoconazole treatment was evaluated. The results showed that the combined use of ketoconazole resulted in an increase in the average Cmax and AUC of quetiapine of 235% and 522%, respectively, and a corresponding decrease in the average oral clearance of 84%. The average half-life of quetiapine increased from 2.6 hours to 6.8 hours, but the average tmax did not change.
Diquetiapine and its several metabolites (including N-dehydroquinolidine) are weak inhibitors of the cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6 and 3A4, but only above 300-800mg / day Occurrence of CYP inhibition was observed only at concentrations of 5-50 times the human effective dose range. Based on the results of these in vitro studies, quetiapine combined with other drugs is not likely to cause clinically significant cytochrome P450 enzyme-related drug inhibitory effects.

Storage of quetiapine fumarate tablets

Store tightly below 30 ° C.

Packaging of quetiapine fumarate tablets

Aluminum-plastic packaging, 20 pieces / box.

Validity of quetiapine fumarate tablets

36 months

Executive standard of quetiapine fumarate tablets

Import drug registration standards:
25mg, O.lg, 0.2g: JX19990170
0.3g: JX20040104

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