Adult Dosing & Uses
Dosing Forms & Strengths
capsules
- 20mg
- 40mg
- 60mg
- 80mg
powder for injection
- 20mg/mL
oral suspension
- 10mg/mL
Schizophrenia
Initial: 20 mg BID with food, may increase q2d PRN; not to exceed 80 mg BID
Maintenance: Periodically assess need for maintenance; no added benefit shown in clinical trials with doses above 20 mg BID
Acute Agitation With Schizophrenia
IM: 10 mg IM q2hr, or 20 mg IM q4hr; not to exceed 40 mg qD for up to 3 days (switch to oral if continuing)
Bipolar I Disorder
Acute treatment of manic or mixed episodes
- Initial: 40 mg PO BID PO with food
- Titration: On day 2, may increase dose if needed to 60-80 mg PO BID
- Adjust dose according to tolerance and efficacy within range of 40-80 mg BID
Maintenance
- Indicated for maintenance therapy as an adjunct to lithium or valproate
- Continue at same dose which patient was initially stabilized within range of 40-80 mg PO BID with food
- Periodically reassess need for maintenance treatment
Pediatric Dosing & Uses
Safety and efficacy not established
Drug Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Somnolence (11-15%)
1-10%
Respiratory disorders
Nausea
Constipation
Dyspepsia
Dizziness
EPS
Rash
Tachycardia
Orthostatic hypotension
Diarrhea
Anorexia
Myalgia
Rhinitis
Cough
<1%
Syncope
Seizures
Frequency Not Defined
QT interval prolongation
Neuroleptic malignant syndrome
Hyperprolactinemia
Contraindications & Cautions
Black Box Warnings
Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature.
This drug is not approved for the treatment of patients with dementia-related psychosis.
Contraindications
Documented hypersensitivity
Any drugs or conditions that prolong QT interval
Cautions
Prolongs QT/QTc (caution in patients with known risk factors eg, hypomagnesemia, hypokalemia); caution in seizure disorders; may cause hypotension, extrapyramidal symptoms, and somnolence; hyperglycemia may occur and in some cases be extreme, resulting in ketoacidosis, hyperosmolar coma, or death
Monitor blood glucose of high-risk pts
FDA Warning regarding off-label use for dementia in elderly
Leukopenia/neutropenia and agranulocytosis reported; possible risk factors for leukopenia/neutropenia include pre-existing low white blood cell count (WBC) and history of drug-induced leukopenia/neutropenia ( if history of clinically significant low WBC or drug-induced leukopenia/neutropenia, monitor complete blood count (CBC) frequently during first few months of therapy; discontinue drug at first sign of a clinically significant decline <1000/mm3 in WBC in absence of other causative factors and continue monitoring WBC until recovery)
Pregnancy & Lactation
Pregnancy Category: C
Neonates exposed to antipsychotic drugs during the 3rd trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery
These complications vary in severity; in some cases, symptoms have been self-limited, while in other cases neonates have required intensive care unit support and prolonged hospitalization
Lactation: unknown; avoid
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Half-Life: 7 hr (PO), 2-5 hr (IM)
Peak Plasma Time: 6-8 hr (PO), 60 min (IM)
Bioavailability: 60% (PO), 100% (IM)
Protein Bound: 99%
Vd: 1.5 L/kg
Metabolism: liver
Total Body Clearance: 7.5 mL/min/kg
Excretion
Urine: 20%
Feces: 66%
Mechanism of Action
Antagonist at dopamine (D2), serotonin (5HT1D, 5HT2A) receptors
Agonist at serotonin 5HT1A receptor
Also has alpha-blocking & antihistaminic activity
