Trade Names:Seroquel- Tablets 25 mg- Tablets 50 mg- Tablets 100 mg- Tablets 200 mg- Tablets 300 mg- Tablets 400 mg
Trade Names:Seroquel XR- Tablets, ER 50 mg- Tablets, ER 150 mg- Tablets, ER 200 mg- Tablets, ER 300 mg- Tablets, ER 400 mg
Has antipsychotic effects, apparently caused by dopamine- and serotonin-receptor blockade in the CNS.
Rapid absorption. T max is 1.5 h (immediate-release) and 6 h (ER). Bioavailability is 100%. Food increases the immediate-release C max and AUC by 25% and 15%, respectively. High-fat meal increases the ER C max and AUC by as much as 52% and 22%, respectively; however, a light meal has no effect. Steady-state concentrations are expected within 2 days.
Widely distributed throughout the body. Vd is about 10 L/kg. It is 83% bound to plasma proteins.
Highly metabolized by the liver via CYP3A4 isoenzyme. Major metabolic pathways are sulfoxidation to the sulfoxide metabolite and oxidation to parent acid metabolite; both metabolites are inactive. Active metabolite is N-desalkyl quetiapine.
Mainly via hepatic metabolism; less than 1% excreted as unchanged drug. About 73% of dose recovered in urine and 20% in feces. The mean terminal half-life for immediate-release is 6 h, for ER is 7 h, and for N-desalkyl quetiapine is 9 to 12 h.
CrCl 10 to 30 mL/min had 25% lower Cl; dosage adjustment not needed.Hepatic Function Impairment
30% lower Cl; AUC and C max is 3-fold higher. Dosage adjustments may be needed.Elderly
Oral Cl reduced 40%. Dosage adjustments may be needed.
Treatment of schizophrenia ( Seroquel ); acute and maintenance treatment of schizophrenia ( Seroquel XR ); treatment of acute manic episodes associated with bipolar I disorder, as either monotherapy or adjunct therapy to lithium or divalproex; treatment of depressive episodes associated with bipolar I disorder; maintenance treatment of bipolar I disorder as adjunct therapy to lithium or divalproex.
Alcohol dependence; Tourette syndrome.
PO ( Seroquel ) 100 mg/day in 2 divided doses on day 1; increase to 400 mg/day on day 4 in increments of up to 100 mg/day in 2 divided doses. Further dosage adjustments of up to 800 mg/day by day 6 should be in increments of no more than 200 mg/day. Usual dosage ranges from 400 to 800 mg/day.Adults
PO ( Seroquel XR ) 300 mg on day 1 and 600 mg on day 2. Administer dose in the evening. Adjust dose between 400 and 800 mg beginning on day 3 depending on the response and tolerance of the patient.DepressionAdults
PO ( Seroquel ) Start with 50 mg once daily at bedtime. Increase to 100 mg on day 2, 200 mg on day 3, and 300 mg on day 4. If indicated, the dose may be increased to 400 mg on day 5 and 600 mg on day 8.Adults
PO ( Seroquel XR ) 50 mg on day 1; 100 mg on day 2; 200 mg on day 3; 300 mg on day 4. Administer in the evening.Maintenance in Bipolar I DisorderAdults
PO Generally, in the maintenance phase, patients are continued on the same dose on which they were stabilized during dose stabilization.SchizophreniaAdults
PO ( Seroquel ) 25 mg twice daily initially; may increase in increments of 25 to 50 mg 2 or 3 times daily on days 2 and 3 to target range of 300 to 400 mg/day by day 4. Increase dose every 2 days by 25 to 50 mg twice daily as indicated. Therapeutic dosage range is 150 to 750 mg/day. Dosages of more than 800 mg/day have not been evaluated in clinical trials.Adults
PO ( Seroquel XR ) Start with 300 mg once daily, preferably in the evening. Dose increases can be made at daily intervals in increments of up to 300 mg/day. Dosages above 800 mg/day have not been evaluated in clinical trials.Elderly/Hepatic Function ImpairmentAdults
PO ( Seroquel XR ) Start with 50 mg/day; increase in daily increments of 50 mg/day to an effective dose.Hepatic Function ImpairmentAdults
PO ( Seroquel ) Start with 25 mg/day; increase in daily increments of 25 to 50 mg/day to an effective dose.
Store at 59° to 86°F.
Possible additive CNS depressant effects; use with caution. Avoid alcohol.Antihypertensive agents
Hypotensive effects may be enhanced.Cimetidine
Quetiapine concentrations may be increased slightly; dosage adjustment does not appear to be needed.Divalproex
Quetiapine concentrations may be increased.Dopamine agonists (eg, pramipexole, ropinirole), levodopa
Quetiapine may antagonize therapeutic effects of dopamine agonists and levodopa.Dopamine/Epinephrine
Do not use dopamine, epinephrine, or other sympathomimetics with beta-agonist activity for the treatment of quetiapine-induced hypotension.Inducers of CYP3A (eg, barbiturates, carbamazepine, glucocorticoids, phenytoin, rifampin)
May decrease the effects of quetiapine; increased doses of quetiapine may be necessary to maintain control of psychotic symptoms. Quetiapine may increase the plasma concentrations of the active metabolite of carbamazepine, resulting in neurotoxicity.Inhibitors of CYP3A (eg, erythromycin, fluconazole, fluvoxamine, itraconazole, ketoconazole, protease inhibitors, voriconazole)
May increase the effects of quetiapine; use with caution.Lorazepam
Quetiapine increases the effects of lorazepam.Thioridazine
May decrease the effects of quetiapine.
None well documented.
Orthostatic/postural hypotension (7%); tachycardia (6%); hypotension, increased heart rate, syncope (less than 5%); palpitation (at least 1%); cardiomyopathy, myocarditis (postmarketing).
Somnolence/sedation (52%); headache (21%); agitation (20%); dizziness (18%); extrapyramidal effects (13%); asthenia, fatigue (10%); insomnia (9%); tremor (8%); dysarthria, lethargy (5%); anxiety (4%); akathisia, dystonia, postural dizziness, pyrexia, tardive dyskinesia, tremor (less than 5%); hypertonia (at least 1%); abnormal dreams and nightmares, restless leg syndrome.
Rash (4% to less than 5%); sweating (at least 1%); Stevens-Johnson syndrome (postmarketing).
Pharyngitis (6%); nasal congestion (5%); rhinitis (3%); amblyopia (2%); blurred vision, drooling (less than 5%).
Dry mouth (44%); constipation (10%); abdominal pain, dyspepsia (7%); vomiting (6%); dysphagia (less than 5%); gastroenteritis (2%); anorexia (at least 1%).
Leukopenia (at least 1%); agranulocytosis, decreased platelets (postmarketing).
Increased ALT (5%); increased AST (3%).
Increased triglycerides (23%); increased cholesterol (16%); increased GGT (1%); elevated serum creatine phosphokinase.
Weight gain (23%); hyperglycemia (11%); peripheral edema (at least 1%); hyponatremia, SIADH (postmarketing).
Back pain (5%); rhabdomyolysis (postmarketing).
Dyspnea, increased cough (at least 1%).
Increased appetite (12%); pain (7%); fever (2%); flu-like syndrome (at least 1%); hypersensitivity; NMS; anaphylactic reaction, galactorrhea (postmarketing).
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Over the course of a 10-wk controlled trial, the rate of death in drug-treated patients was about 4.5% compared with 2.6% in the placebo group. Although the causes of death were varied, most of the deaths appeared to be either CV (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Quetiapine is not approved for the treatment of patients with dementia-related psychosis.Suicidality
Compared with placebo, antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants for major depressive disorders and other psychiatric disorders. Appropriately monitor patients of all ages who are started on antidepressant therapy and observe them closely for clinical worsening, suicidality, or unusual changes in behavior. Advise families and caregivers of the need for close observation and communication with the prescriber. Quetiapine is not approved for use in children.
Monitor all patients for the emergence of agitation, irritability, clinical worsening, and other unusual changes in behavior, as well as the emergence of suicidality, especially during the initial few months of therapy or at times of dose changes. Monitor patients for symptoms of hyperglycemia. Perform fasting glucose testing in patients who develop hyperglycemia during treatment. Ensure that patients with risk factors for diabetes undergo fasting blood glucose testing at the start of therapy and periodically thereafter. Monitor patients with established diagnosis of diabetes mellitus regularly for worsening of glucose control. Perform eye exam at initiation of therapy to detect cataract formation and at 6-mo intervals during long-term treatment. Monitor patients for any unusual changes in behavior (eg, agitation, irritability). Monitor patients requiring antipsychotic drug treatment after recovery from NMS for recurrence of NMS if quetiapine therapy is reintroduced. Monitor WBC frequently during the first few months of therapy in patients with a preexisting low WBC or history of drug-induced leukopenia/neutropenia. Carefully monitor patients with neutropenia for fever or other symptoms or signs of infection.
Category C .
Safety and efficacy not established; not approved for use in children.
May be more susceptible to effects. Consider lower starting dose, slower titration, and careful monitoring. May be at increased risk of tardive dyskinesia, especially elderly women.
Dosage adjustment may be needed.
Consider lower starting dose, slower titration, and careful monitoring in debilitated patients and patients with predisposition to hypotensive reactions.
Antipsychotics can disrupt the body's ability to reduce core temperature.
Orthostatic hypotension may occur, especially during the initial dose-titration period. Use with caution in patients with known cardiovascular disease (eg, conduction abnormalities, heart failure, history of MI, ischemic heart disease), cerebrovascular disease, or condition that would predispose patients to hypotension (eg, dehydration, hypovolemia, treatment with antihypertensive medications).
Lens changes have been observed in patients during long-term treatment.
Mental and/or physical abilities may be impaired, especially during the first few days of therapy.
Antipsychotics have been associated with esophageal dysmotility and aspiration. Use with caution in patients at risk for aspiration pneumonia.
Agranulocytosis (including fatal cases), leukopenia, and neutropenia have been reported during postmarketing experience.
Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, may occur.
Increased cholesterol and/or triglycerides may occur.
Patients treated with antipsychotic agents often have elevation in prolactin levels.
Has occurred with antipsychotics and is potentially fatal.
Has been reported.
Use with caution in patients with a history of seizures or with conditions that potentially lower the seizure threshold (eg, Alzheimer dementia).
Closely supervise high-risk patients; prescribe small quantities.
A potentially irreversible syndrome of involuntary body and facial movements may occur.
Asymptomatic, transient, and reversible elevations in serum transaminases (mainly ALT) may occur.
Acute withdrawal symptoms, including nausea, vomiting, and insomnia, have been reported rarely after abrupt cessation of therapy. Gradual withdrawal is advised.
Coma, death, drowsiness, first-degree heart block, hypokalemia, hypotension, QTc prolongation, sedation, tachycardia.
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