Dosing and uses of Fanapt (iloperidone)
Adult dosage forms and strengths
tablet
- 1mg
- 2mg
- 4mg
- 6mg
- 8mg
- 10mg
- 12mg
Schizophrenia
Day 1: 1 mg PO q12hr; increase qDay to effective dose of 6-12 mg PO q12hr
Day 2: 2 mg PO q12hr, THEN increase qDay by 2 mg/day to effective dose of 6-12 mg PO q12hr; not to exceed 24 mg/day
Must gradually increase dose to avoid orthostatic hypotension
Dosage modifications
Coadministration with strong CYP2D6 or CYP3A4 inhibitors: Decrease iloperidone dose by 50%
Poor CYP2D6 metabolizers: Decrease iloperidone dose by 50%
Renal impairment: Unlikely to have a significant impact since <1% of drug is excreted unchanged in urine
Hepatic impairment
- Mild: No dosage adjustment required
- Moderate: Caution advised
- Severe: Use not recommended
Pediatric dosage forms and strengths
Safety and efficacy not established
Fanapt (iloperidone) adverse (side) effects
>10%
Dizziness (20%)
Dry mouth (15%)
Nausea (10%)
Somnolence (10%)
Tachycardia (12%)
1-10% (selected)
Diarrhea
Ejaculation failure
Myalgia
Nasal congestion
Orthostatic hypotension
Palpitations
Urinary incontinence
Weight gain
<1% (selected)
Amenorrhea
Edema
Hypothyroidism
Frequency not defined (selected)
Priapism
Postmarketing Reports
Retrograde ejaculation
Hypersensitivity reactions (including anaphylaxis; angioedema; throat tightness; oropharyngeal swelling; swelling of the face, lips, mouth, and tongue; urticaria; rash; and pruritus)
Warnings
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
Hypersensitivity; anaphylaxis, angioedema, and other hypersensitivity reactions reported
Cautions
Prolongs QT interval; caution with other drugs/conditions that increase QTc
Not recommended in hepatic impairment
Risk of neuroleptic malignant syndrome and extrapyramidal symptoms
May cause anticholinergic side effects (eg., confusion, agitation)
Blood dyscrasias (leukopenia, neutropenia, agranulocytosis) may occur
Orthostatic hypotension may occur
Cases of priapism reported
Motor and cognitive impairment may occur; use caution when operating heavy machinery
Use caution in patients with history of seizures or with conditions that lower seizure threshold
Monitor closely patients at high risk of committing suicide
Hyperprolactinemia may occur; gynecomastia and galactorrhea reported
Antipsychotic agents may disrupt body temperature regulation and may cause esophageal dysmotility and aspiration; use caution
Metabolic changes
- Atypical antipsychotics have been associated with metabolic changes that may increase cardiovascular/cerebrovascular risk including hyperglycemia, dyslipidemia, and body weight gain
- 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
- Possibility of weight gain
Pregnancy and 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: not known if excreted in breast milk, do not nurse
Pregnancy categories
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 of Fanapt (iloperidone)
Mechanism of action
May act by antagonizing a combination of dopamine type 2 (D2) and serotonin type 2 (5-HT2) receptors.
Alpha blocker
Absorption
Bioavailability 96%
Peak Plasma Time: 2-4 hr
Distribution
Protein Bound: 95%
Vd: 1340-2800 L
Metabolism
Metabolized by CYP2D6 and CYP3A4
Elimination
Excretion: Urine (45-58%), feces (20-22%)
