Adult Dosing & Uses
Dosing Forms & Strengths
tablets, immediate-release
- 25mg
- 50mg
- 100mg
- 200mg
- 300mg
- 400mg
tablets, extended-release
- 50mg
- 150mg
- 200mg
- 300mg
- 400mg
Schizophrenia
Immediate-release
- Day 1: 25 mg PO BID
- Days 2-3: Increase by daily increments of 25-50 mg divided BID/TID to range of 300-400 mg by Day 4
- Further adjustment can be made in increments of 25-50 mg BID in intervals not <2 days
- Dosage range: 150-750 mg/day
Extended-release
- Day 1: 300 mg PO qDay
- May increase dose by up to 300 mg/day in increments as little as 1-day intervals
- Schizophrenia maintenance (monotherapy): 400-800 mg/day
- Dosage range: 400-800 mg/day
Bipolar I Disorder, Mania
Monotherapy or as an adjunct to lithium or divalproex
Immediate-release
- Day 1: 50 mg PO BID
- Day 2: 100 mg PO BID
- Day 3: 150 mg PO BID
- Day 4: 200 mg PO BID
- Further dosage adjustments up to 800 mg/day by Day 6 should be in increments of no >200 mg/day
- Dosage range: 400-800 mg/day
Extended-release
- Day 1: 300 mg PO single dose
- Day 2: 600 mg PO single dose
- Maintenance (Day 3 onwards): between 400-800 mg PO qDay
- Dosage range: 400-800 mg/day
Bipolar Disorder, Depression
Administer either immediate- or extended-release qDay at bedtime; titrate upward over 4 days
Day 1: 50 mg PO qHS
Day 2: 100 mg PO qHS
Day 3: 200 mg PO qHS
Day 4 onwards: 300 mg PO qhs
Dosage range: 300 mg/day
Bipolar I Disorder, Maintenance
Adjunct to lithium or divalproex
Immediate-release: 400-800 mg/day PO divided BID
Extended-release: 400-800 mg PO qDay
Generally, in the maintenance phase, patients continued on the same dose on which they were stabilized
Major Depressive Disorder
Extended-release product used as adjunct to antidepressants
Days 1 and 2: 50 mg PO in evening
Days 3 and 4: May increase to 150 mg PO in evening
Dosage range: 150-300 mg/day
Geriatric Dosing
Not approved for dementia-related psychosis because of increased risk of cardiovascular or infectious related deaths (see Black Box Warnings)
Schizophrenia, Bipolar Disorder
- Immediate release: 50-200 mg PO qDay, may increase by 25-50 mg/day
- Extended release: 50 mg PO qDay, may increase by 50 mg/day
Psychosis, Agitation related to Alzheimer's Dementia (Off-label)
- 12.5-50 mg PO qDay initially; may gradually increase as tolerated; not to exceed 200-300 mg/day
Alcohol Dependence (Off-label)
25-50 mg PO qHS
Tourette Syndrome (Off-label)
50-600 mg/day for 12 weeks
Insomnia (Off-label)
Usually start 25 mg PO qHS
Other Information
Take preferably in evening without food or with light meal
Pediatric Dosing & Uses
Dosing Forms & Strengths
tablets, immediate-release
- 25mg
- 50mg
- 100mg
- 200mg
- 300mg
- 400mg
Schizophrenia
<13 years: Safety and efficacy not established
13-17 years (monotherapy, immediate-release)
- Day 1: 25 mg PO BID
- Day 2: 100 mg/day PO divided BID
- Day 3: 200 mg/day PO divided BID
- Day 4: 300 mg/day PO divided BID
- Day 5: 400 mg/day PO divided BID
- Further adjustments should be in increments not exceeding 100 mg/day within dosage range of 400-800 mg/day
- Based on response and tolerability, daily dose may be divided TID
Bipolar I Disorder, Mania
<10 years: Safety and efficacy not established
10-17 years (monotherapy, immediate-release)
- Day 1: 25 mg PO BID
- Day 2: 100 mg/day PO divided BID
- Day 3: 200 mg/day PO divided BID
- Day 4: 300 mg/day PO divided BID
- Day 5: 400 mg/day PO divided BID
- Further adjustments should be in increments not exceeding 100 mg/day within dosage range of 400-600 mg/day
- Based on response and tolerability, daily dose may be divided TID
Drug Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Dizziness
Dry mouth
Headache
Somnolence
1-10%
Abdominal pain
Constipation
Dyspepsia
Vomiting
Increased appetite
Weight gain
Agitation
Asthenia
Tremor
Back pain
Postural hypotension
Tachycardia
Fever
Pharyngitis
Rhinitis
Rash
Visual disturbances
Arthralgia
Frequency Not Defined
Hypercholesterolemia
Hypertriglyceridemia
Eye lens changes (rare)
Hyperglycemia
Hypothyroidism
Increased LFTs
Potential for new-onset diabetes
Postmarketing Reports
Elevated total cholesterol (predominantly LDL)
Somnambulism
Hypothermia
QT prolongation
Leukopenia
Neutropenia
Anaphylactic reaction
Galactorrhea
Agranulocytosis
Cardiomyopathy
Hyponatremia
Stevens - Johnson syndrome
Dyspnea
Palpitations
Contraindications & Cautions
Black Box Warnings
Elderly 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
Deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature
Not approved for the treatment of patients with dementia-related psychosis
Increased risk of suicidal thinking and behavior in children, adolescents and young adults taking antidepressants for major depressive disorder and other psychiatric disorders
Contraindications
Documented hypersensitivity
Cautions
Cardiovascular disease
Cerebrovascular disease
Hypotensive conditions
Breast cancer
History of seizure
Increased risk of hyperglycemia and diabetes; in some cases, hyperglycemia concomitant with use of atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death
Monitor blood glucose of high-risk patients
Risk of NMS and tardive dyskinesia
Clinical worsening of depression and suicide ideation may occur despite treatment
Hyperlipidemia
Weight gain
Orthostatic hypotension
Monitor for cataract
Increased blood pressure in children and adolescents
Leukopenia
Neutropenia
Agranulocytosis
Somnolence (especially with XR product)
Tardive dyskinesia syndrome may occur following discontinuation
Withdrawal symptoms may occur with abrupt discontinuation
False positive urine drug screens reported when using immunoassays for methadone or TCAs
FDA Warning regarding off-label use for dementia in elderly (see Black Box Warnings)
QT interval prolongation
- QT interval: Not associated with persistent increase in QT interval In trials, but QT effect was not systematically evaluated in a thorough QT study
- QT prolongation reported with acute overdose during postmarketing experience
- Avoid combination with other drugs known to prolong QTc or in patients with increased risk of QT prolongation
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: excreted in breast milk, breast feeding is not recommended
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
Mechanism of Action
Atypical antipsychotic related to clozapine
Reduces positive & negative symptoms of psychotic disorders via dopamine D2 & serotonin 5-HT2 antagonism
Also has alpha-blocking & antihistaminic activity
Absorption
Bioavailability: 100%
Peak Plasma Time: immediate-release 1.5 hr; extended-release 6 hr
Distribution
Protein Bound: 83%
Vd: 10±4 L/kg
Metabolism
Metabolism: hepatic CYP3A4
Elimination
Half-Life: 6 hr
Excretion: urine 73%; feces 20%
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