Names and pronunciation
(ill-o-pehr′ih-dohn) Fanapt
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Drug reference
(ill-o-pehr′ih-dohn) Fanapt
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Func. class.: 2nd-generation atypical antipsychotic
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Chem. class.: Benzisoxazole derivative
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Do not confuse: Fanapt/Xanax
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ACTION: Unknown; may be mediated through both DOPamine type 2 (D2) and serotonin type 2 (5-HT2) antagonism, high receptor binding affinity for norepi- nephrine (alpha 1)
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USES: Schizophrenia
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CONTRAINDICATIONS: Breast- feeding, hypersensitivity Precautions: Pregnancy, children, geriatric patients, renal/hepatic disease, breast cancer, Parkinson’s disease, dementia with Lewy bodies, seizure dis- order, QT prolongation, bundle branch block, acute MI, ambient temperature increase, AV block, stroke, substance abuse, suicidal ideation, tardive dyski- nesia, torsades de pointes, blood dys- crasias, dysphagia
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Black Box Warning: Increased mortality in elderly patients with dementia-related psychosis; opioids Black Box Warning: Dementia-related psychosis: sudden death; not to be used in the elderly with dementia • Neuroleptic malignant syndrome: hy perthermia, increased CPK, altered mental status, muscle rigidity, seizures, diaphoresis; discontinue immediately, notify prescriber Black Box Warning: Opioids: Use only if alternative agents are not effective • Constipation, urinary retention daily; if these occur, increase bulk and water in diet • Weight gain, BMI, waist circumfer- ence, hyperglycemia, metabolic changes in diabetes • Supervised ambulation until patient is stabilized on medication; do not in- volve patient in strenuous exercise program because fainting is possible; patient should not stand still for long periods • Sips of water, candy, gum for dry mouth • Beers: avoid in older adults except for schizophrenia, bipolar disorder, or short-term use as an antiemetic during chemotherapy; increased risk of stroke • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; infant ex- posed to product during 3rd trimester may exhibit EPS; do not breastfeed, ex- cretion unknown Black Box Warning: Opioids: Teach patient/family/caregiver, to seek medical care immediately if dizziness, drowsi- ness, trouble breathing occur • To avoid OTC preparations (cough, hay fever, cold), herbals, supplements unless discussed by prescriber because serious product interactions may occur; to avoid use of alcohol because increased drowsiness may occur • To use gum, lozenges for dry mouth • To avoid hazardous activities if drowsy or dizziness occurs • To comply with product regimen, to take as prescribed, not to skip or double doses, if medication is missed for >3 days start as initial dose • To report impaired vision, tremors, muscle twitching • That follow-up exams will be needed • To use contraception; to inform prescriber if pregnancy is planned or suspected; if pregnant, should enroll in the Atypical Antipsychotic National Preg nancy Registry: 866-961-2388
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SIDE EFFECTS CNS: EPS, pseudoparkinsonism, akathisia, dystonia, tardive dyskinesia; drowsiness, seizures, neuroleptic malig nant syndrome, dizziness, delirium, depression, paranoia, fatigue, hostility, lethargy, restlessness, vertigo, tremor CV: Orthostatic hypotension, heart failure, AV block, QT prolongation, tachycardia EENT: Blurred vision, cataracts, nystag- mus, tinnitus, nasal congestion GI: Nausea, vomiting, anorexia, consti pation, jaundice, weight gain/loss, abdominal pain, stomatitis, xerostomia, dry mouth GU: Urinary retention/incontinence, priapism HEMA: Agranulocytosis, leukopenia, neutropenia MISC: , Decreased bone density hyperglycemia, dyslipidemia SYST: Anaphylaxis, angioedema
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INTERACTIONS Increase: sedation—other CNS depres- sants, alcohol, opioids Increase: iloperidone effect, decreased clearance—CYP2D6 (fluoxetine, parox- etine), CYP3A4 inhibitors (delavirdine, indinavir, isoniazid, itraconazole, dalfo- pristin, ritonavir, tipranavir); reduce dose Increase: QT prolongation—class IA/III antidysrhythmics, some phenothiazines, β-agonists, local anesthetics, tricyclics, haloperidol, methadone, chloroquine, clarithromycin, droperidol, erythromycin, pentamidine Decrease: iloperidone action—CYP2D6, CYP3A4 inducers (carBAMazepine, bar- biturates, phenytoins, rifAMPin) Drug/Lab Test Increase: prolactin levels, cholesterol, glucose, lipids, triglycerides Decrease: potassium
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TREATMENT OF OVERDOSE: Lavage if orally ingested; provide airway; do not induce vomiting
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DOSAGE AND ROUTES • Adult: PO 1 mg bid, may increase to target dose of 6-12 mg bid with daily dose adjustment of max 2 mg bid, titrate slowly; max 24 mg/day in 2 divided doses; reduce dose by 50% in patient who is a poor metabolizer of CYP2D6 or when used with strong CYP2D6/CYP3A4 inhibitors
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Available forms: Tabs 1, 2, 4, 6, 8, 10, 12 mg; titration pack
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Administer: • Use without regard to meals • Reduced dose in geriatric patients • Anticholinergic agent for EPS • Avoid use with CNS depressants • Store in tight, light-resistant container
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Assess: • AIMS assessment, lipid panel, blood glucose, CBC, glycosylated hemoglobin A1c, LFTs, neurologic function, preg- nancy test, serum creatinine, electrolytes, prolactin, thyroid function studies, weight • Affect, orientation, LOC, reflexes, gait, coordination, sleep-pattern disturbances • B/P standing and lying, pulse, respira- tions q4hr during initial treatment; estab- lish baseline before starting treatment; report drops of 30 mm Hg; watch for ECG changes; QT prolongation may occur; dizziness, faintness, palpitations, tachy- cardia on rising • Extrapyramidal symptoms, including akathisia, tardive dyskinesia (bizarre movements of the jaw, mouth, tongue, extremities), pseudoparkinsonism (ri- gidity, tremors, pill rolling, shuffling gait) • Check to see the patient swallows the medication I
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Evaluate: • Therapeutic response: decrease in emotional excitement, hallucinations, de- lusions, paranoia; reorganization of pat- terns of thought, speech
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That orthostatic hypotension may oc- cur; to rise from sitting or lying position gradually • To avoid hot tubs, hot showers, tub baths because hypotension may occur; that heat stroke may occur in hot weather; to take extra precautions to stay cool • To avoid abrupt withdrawal of product because extrapyramidal symptoms may result; that product should be withdrawn slowly; to review symptoms of neurolep- tic malignant syndrome
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PHARMACOKINETICS PO: Extensively metabolized by liver to major active metabolite by CYP2D6, CYP3A4; protein binding 95%; peak 2-4 hr; excreted in urine and feces; termi- nal half-life 18 hr in extensive metaboliz- ers; 33 hr in poor metabolizers
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• Adult: PO 1 mg bid, may increase to target dose of 6-12 mg bid with daily dose adjustment of max 2 mg bid, titrate slowly; max 24 mg/day in 2 divided doses; reduce dose by 50% in patient who is a poor metabolizer of CYP2D6 or when used with strong CYP2D6/CYP3A4 inhibitors
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