Quetiapine Fumarate Powder
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General Information:Quetiapine Fumarate is an atypical antipsychotic medication used primarily for the treatment of schizophrenia, bipolar disorder, and major depressive disorder (as an adjunct therapy). It works by modulating neurotransmitters in the brain, particularly dopamine (D2) and serotonin (5-HT2A) receptors.
Chemical Properties:
Chemical Name: Quetiapine Fumarate
Molecular Formula: CHNOS (for the fumarate salt)
Molecular Weight: 883.1 g/mol
CAS Number: 111974-72-2
Appearance: White to off-white crystalline powder
Solubility: Slightly soluble in water, soluble in methanol and ethanol
Melting Point: 170180C
Mechanism of Action:Quetiapine acts as a dopamine and serotonin receptor antagonist, particularly affecting:
Dopamine D2 receptors Reduces psychotic symptoms by balancing dopamine activity.
Serotonin 5-HT2A receptors Helps with mood stabilization and cognitive function.
Histamine H1 and Alpha-1 receptors Causes sedation and helps with sleep disturbances.
Pharmacokinetics:
Absorption: Well absorbed orally, peak plasma levels in 1.5 hours.
Metabolism: Extensively metabolized in the liver (CYP3A4 enzyme).
Half-life: 67 hours (extended-release versions have longer half-life).
Excretion: Primarily via urine and feces.
Therapeutic Uses & Indications:
Schizophrenia (both acute and maintenance therapy)
Bipolar disorder (manic and depressive episodes)
Major Depressive Disorder (MDD) (adjunct therapy)
Generalized Anxiety Disorder (off-label use)
Insomnia (off-label, due to sedative effects)
Dosage & Administration:
Immediate-release formulations:
Schizophrenia/Bipolar: 25800 mg per day, divided into 2 doses.
Extended-release (XR) formulations:
Initial dose: 50300 mg per day, titrated as needed.
Maintenance dose: 400800 mg per day, once daily.
Administration:
Taken with or without food (XR should be taken without food for better absorption).
Side Effects:
Common: Drowsiness, dizziness, weight gain, dry mouth, constipation.
Serious: Increased risk of diabetes, metabolic syndrome, QT prolongation, neuroleptic malignant syndrome (NMS), tardive dyskinesia.
Black Box Warning: Increased mortality in elderly patients with dementia-related psychosis.
Precautions & Contraindications:
Contraindicated in:
Severe liver impairment
Known hypersensitivity to Quetiapine
Caution in:
Patients with diabetes, cardiovascular disease, or seizures
Pregnant and breastfeeding women (use only if benefits outweigh risks)
Drug Interactions:
CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): Increase quetiapine levels.
CYP3A4 inducers (e.g., rifampin, carbamazepine): Decrease quetiapine effectiveness.
CNS depressants (e.g., alcohol, benzodiazepines): Enhance sedation effects.
Storage & Stability:
Store at room temperature (1530C)
Protect from moisture and light
Keep in a tightly closed container
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