Fanapt

— THERAPEUTIC CATEGORIES —
  • Mood disorders
  • Psychosis

Fanapt Generic Name & Formulations

General Description

Iloperidone 1mg, 2mg, 4mg, 6mg, 8mg, 10mg, 12mg; tabs.

Pharmacological Class

Atypical antipsychotic.

How Supplied

Tabs—60; Titration pack—8 (2 x 1mg, 2 x 2mg, 2 x 4mg, 2 x 6mg)

Generic Availability

NO

Mechanism of Action

The mechanism of action of iloperidone in schizophrenia; is unknown. However the efficacy of iloperidone could be mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5-HT2) antagonism. Iloperidone forms an active metabolite, P88, that has an in vitro receptor binding profile similar to the parent drug.

Fanapt Indications

Indications

Acute treatment of manic or mixed episodes associated with bipolar I disorder.

Fanapt Dosage and Administration

Adult

Titrate slowly. ≥18yrs: Initially 1mg twice daily, then 3mg, 6mg, 9mg, and 12mg twice daily on Days 2, 3, 4, and 5 respectively, to reach 24mg/day dose. Reduce dose by ½ with concomitant strong CYP2D6/CYP3A4 inhibitors, or poor metabolizers of CYP2D6. Retitrate if therapy suspended >3 days.

Children

<18yrs: not established.

Fanapt Contraindications

Not Applicable

Fanapt Boxed Warnings

Boxed Warning

Increased mortality in elderly patients with dementia-related psychosis.

Fanapt Warnings/Precautions

Warnings/Precautions

Increased mortality in elderly patients with dementia-related psychosis (not approved use). Bradycardia, hypokalemia, hypomagnesemia, congenital QT prolongation, recent MI, uncompensated heart failure, arrhythmias: avoid (risk of torsades de pointes/ sudden death). Discontinue if persistent QTc measurements >500msec occur. Cardio- or cerebrovascular disease. Monitor electrolytes esp. K+, Mg++. Monitor for neuroleptic malignant syndrome (NMS); discontinue if suspected and treat appropriately. Consider discontinuing if tardive dyskinesia occurs; assess periodically the need for continued treatment. Moderate hepatic impairment. Severe hepatic impairment: not recommended. Diabetes or risk factors (obtain baseline fasting blood sugar). Dyslipidemia (obtain baseline fasting lipid profile). Monitor for blood glucose, lipid profile, weight changes. History of breast cancer or seizures. Orthostatic hypotension. Preexisting low WBC count or history of leukopenia/neutropenia: monitor CBC during 1st few months of therapy; discontinue if WBCs decline. If neutropenia develops, monitor for fever, signs/symptoms of infection; discontinue if severe neutropenia (absolute neutrophil count <1000/mm3) occurs. Exposure to extreme heat. Aspiration pneumonia risk. Dehydration. Perform fall risk assessments when initiating and recurrently on long-term therapy. Risk of intraoperative floppy iris syndrome (IFIS) during cataract or glaucoma surgery: not recommended. Write ℞ for the smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post delivery (due to exposure during 3rd-trimester pregnancy). Reevaluate periodically. Pregnancy. Nursing mothers: not recommended.

Fanapt Pharmacokinetics

Absorption

Time to peak plasma concentrations: within 2 to 4 hours. Relative bioavailability: 96%.

Distribution

Apparent volume of distribution: 1340 to 2800 L. 95% serum protein bound.

Metabolism

Hepatic (CYP2D6, CYP3A4). 

Elimination

Renal (58.2% for extensive metabolizers; 45.1% for poor metabolizers), fecal (19.9% for extensive metabolizers; 22.1% for poor metabolizers). Half-life: 18 hours (extensive metabolizers); 33 hours (poor metabolizers).

Fanapt Interactions

Interactions

Avoid other drugs that cause QT prolongation (eg, quinidine, procainamide, amiodarone, sotalol, chlorpromazine, thioridazine, gatifloxacin, moxifloxacin, pentamidine, levomethadyl acetate, methadone). May potentiate antihypertensives. Caution with alcohol, CNS depressants. Potentiated by inhibitors of CYP2D6 (eg, fluoxetine, paroxetine) or CYP3A4 (eg, clarithromycin, ketoconazole).

Fanapt Adverse Reactions

Adverse Reactions

Dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, increased weight; QT prolongation (discontinue if QTc >500msec persists), priapism, neuroleptic malignant syndrome, tardive dyskinesia, hyperglycemia, dyslipidemia, dysphagia, hyperprolactinemia, hypersensitivity reactions, intraoperative floppy iris syndrome (IFIS).

Fanapt Clinical Trials

See Literature

Fanapt Note

Not Applicable

Fanapt Patient Counseling

See Literature

Fanapt Generic Name & Formulations

General Description

Iloperidone 1mg, 2mg, 4mg, 6mg, 8mg, 10mg, 12mg; tabs.

Pharmacological Class

Atypical antipsychotic.

How Supplied

Tabs—60; Titration pack—8 (2 x 1mg, 2 x 2mg, 2 x 4mg, 2 x 6mg)

Generic Availability

NO

Mechanism of Action

The mechanism of action of iloperidone in schizophrenia; is unknown. However the efficacy of iloperidone could be mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5-HT2) antagonism. Iloperidone forms an active metabolite, P88, that has an in vitro receptor binding profile similar to the parent drug.

Fanapt Indications

Indications

Schizophrenia.

Fanapt Dosage and Administration

Adult

Titrate slowly. ≥18yrs: Initially 1mg twice daily, then 2mg, 4mg, 6mg, 8mg, 10mg, and 12mg twice daily on Days 2, 3, 4, 5, 6, and 7 respectively, to reach the 12mg/day to 24mg/day dose range. Reduce dose by ½ with concomitant strong CYP2D6/CYP3A4 inhibitors, or poor metabolizers of CYP2D6. Retitrate if therapy suspended >3 days.

Children

<18yrs: not established.

Fanapt Contraindications

Not Applicable

Fanapt Boxed Warnings

Boxed Warning

Increased mortality in elderly patients with dementia-related psychosis.

Fanapt Warnings/Precautions

Warnings/Precautions

Increased mortality in elderly patients with dementia-related psychosis (not approved use). Bradycardia, hypokalemia, hypomagnesemia, congenital QT prolongation, recent MI, uncompensated heart failure, arrhythmias: avoid (risk of torsades de pointes/ sudden death). Discontinue if persistent QTc measurements >500msec occur. Cardio- or cerebrovascular disease. Monitor electrolytes esp. K+, Mg++. Monitor for neuroleptic malignant syndrome (NMS); discontinue if suspected and treat appropriately. Consider discontinuing if tardive dyskinesia occurs; assess periodically the need for continued treatment. Moderate hepatic impairment. Severe hepatic impairment: not recommended. Diabetes or risk factors (obtain baseline fasting blood sugar). Dyslipidemia (obtain baseline fasting lipid profile). Monitor for blood glucose, lipid profile, weight changes. History of breast cancer or seizures. Orthostatic hypotension. Preexisting low WBC count or history of leukopenia/neutropenia: monitor CBC during 1st few months of therapy; discontinue if WBCs decline. If neutropenia develops, monitor for fever, signs/symptoms of infection; discontinue if severe neutropenia (absolute neutrophil count <1000/mm3) occurs. Exposure to extreme heat. Aspiration pneumonia risk. Dehydration. Perform fall risk assessments when initiating and recurrently on long-term therapy. Risk of intraoperative floppy iris syndrome (IFIS) during cataract or glaucoma surgery: not recommended. Write ℞ for the smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post delivery (due to exposure during 3rd-trimester pregnancy). Reevaluate periodically. Pregnancy. Nursing mothers: not recommended.

Fanapt Pharmacokinetics

Absorption

Time to peak plasma concentrations: within 2 to 4 hours. Relative bioavailability: 96%.

Distribution

Apparent volume of distribution: 1340 to 2800 L. 95% serum protein bound.

Metabolism

Hepatic (CYP2D6, CYP3A4). 

Elimination

Renal (58.2% for extensive metabolizers; 45.1% for poor metabolizers), fecal (19.9% for extensive metabolizers; 22.1% for poor metabolizers). Half-life: 18 hours (extensive metabolizers); 33 hours (poor metabolizers).

Fanapt Interactions

Interactions

Avoid other drugs that cause QT prolongation (eg, quinidine, procainamide, amiodarone, sotalol, chlorpromazine, thioridazine, gatifloxacin, moxifloxacin, pentamidine, levomethadyl acetate, methadone). May potentiate antihypertensives. Caution with alcohol, CNS depressants. Potentiated by inhibitors of CYP2D6 (eg, fluoxetine, paroxetine) or CYP3A4 (eg, clarithromycin, ketoconazole).

Fanapt Adverse Reactions

Adverse Reactions

Dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, increased weight; QT prolongation (discontinue if QTc >500msec persists), priapism, neuroleptic malignant syndrome, tardive dyskinesia, hyperglycemia, dyslipidemia, dysphagia, hyperprolactinemia, hypersensitivity reactions, intraoperative floppy iris syndrome (IFIS).

Fanapt Clinical Trials

See Literature

Fanapt Note

Not Applicable

Fanapt Patient Counseling

See Literature

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