Absorption: Well absorbed after oral administration.
Distribution: Widely distributed.
Metabolism/Excretion: Extensively metabolized by the liver (mostly by P450 CYP3A4 enyzme system) to norquetiapine (active metabolite with anticholinergic properties); <1% excreted unchanged in the urine.
Half-life: 6 hr.
CV: ↑BP (children), palpitations, peripheral edema, postural hypotension.
Derm: ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME, sweating.
EENT: ear pain, rhinitis, pharyngitis.
Endo: weight gain, hyperglycemia, hyperlipidemia, hyperprolactinemia, hypertriglyceridemia, hypothyroidism.
GI: GI OBSTRUCTION, PANCREATITIS, anorexia, constipation, dry mouth, dyspepsia.
GU: ↓fertility (females).
Hemat: AGRANULOCYTOSIS, ↓ hemoglobin, leukopenia, neutropenia.
MS: rhabdomyolysis.
Neuro: NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, dizziness, cognitive impairment, extrapyramidal symptoms, sedation, tardive dyskinesia.
Resp: cough, dyspnea.
Misc: flu-like syndrome.
Schizophrenia
- PO (Adults): Immediate-release — 25 mg twice daily on Day 1, ↑ by 25–50 mg 2–3 times daily on Days 2 and 3, up to 300–400 mg/day in 2–3 divided doses by Day 4 (not to exceed 800 mg/day); Extended-release — 300 mg once daily, ↑ by 300 mg/day (not to exceed 800 mg/day); elderly patients or patients with hepatic impairment should be started on immediate-release product and converted to extended-release product once effective dose is reached.
- PO (Children 13–17 yr): Immediate-release — 25 mg twice daily on Day 1, ↑ to 50 mg twice daily on Day 2, then ↑ to 100 mg twice daily on Day 3, then ↑ to 150 mg twice daily on Day 4, then ↑ to 200 mg twice daily on Day 5; may then ↑ by no more than 100 mg/day (not to exceed 800 mg/day).
Acute Manic Episodes Associated with Bipolar I Disorder
- PO (Adults): Immediate-release — 50 mg twice daily on Day 1, then ↑ to 100 mg twice daily on Day 2, then ↑ to 150 mg twice daily on Day 3, then ↑ to 200 mg twice daily on Day 4; may then ↑ by no more than 200 mg/day up to 400 mg twice daily on Day 6 if needed; Extended-release — 300 mg once daily on Day 1, then 600 mg once daily on Day 2, then 400–800 mg once daily starting on Day 3.
- PO (Children 10–17 yr): Immediate-release — 25 mg twice daily on Day 1, then ↑ to 50 mg twice daily on Day 2, then ↑ to 100 mg twice daily on Day 3, then ↑ to 150 mg twice daily on Day 4, then ↑ to 200 mg twice daily on Day 5; may then ↑ by no more than 100 mg/day (not to exceed 600 mg/day).
Acute Depressive Episodes Associated with Bipolar Disorder
- PO (Adults): Immediate-release or extended-release — 50 mg once daily at bedtime on Day 1, then ↑ to 100 mg daily at bedtime on Day 2, then ↑ to 200 mg daily at bedtime on Day 3, then ↑ to 300 mg daily at bedtime thereafter.
Maintenance Treatment of Bipolar I Disorder
- PO (Adults): Continue at the dose required to maintain symptom remission (usual dosage: 400–800 mg/day given as once daily dose [extended-release] or in two divided doses [immediate-release]).
- PO (Children 10–17 yr): Continue at the lowest dose required to maintain symptom remission.
Depression
- PO (Adults): Extended-release — 50 mg once daily on Days 1 and 2, then ↑ to 150 mg once daily starting on Day 3 (not to exceed 300 mg/day).
Therapeutic Classification: antipsychotics
1 wk off, follow initial titration schedule.
24 yr.