(eye loe PER i done)
Schizophrenia: Treatment of adults with schizophrenia
Hypersensitivity to iloperidone (eg, anaphylaxis, angioedema) or any component of the formulation
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Iloperidone is not approved for the treatment of patients with dementia-related psychosis.
Schizophrenia: Oral: Initial: 1 mg twice daily; titrate to the recommended dosage range with dosage adjustments not to exceed 2 mg twice daily (4 mg daily) every 24 hours; recommended dosage range: 6 to 12 mg twice daily (maximum: 24 mg/day)
Note: Titrate dose to effect (to avoid orthostatic hypotensive effects); when reinitiating treatment after discontinuation (>3 days), follow initial titration schedule.
Dosage adjustment in patients receiving strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine, quinidine) or strong CYP3A4 inhibitors (eg, ketoconazole, clarithromycin): Decrease iloperidone dose by 50%; when CYP2D6 inhibitor or CYP3A4 inhibitor is discontinued, return to previous dose.
Dosage adjustment in poor metabolizers of CYP2D6: Decrease iloperidone dose by 50%.
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer 's labeling; however, renal impairment alone is unlikely to have a significant impact on the pharmacokinetics of iloperidone.
Mild impairment: No dosage adjustment necessary.
Moderate impairment: There are no specific dosage adjustments provided in the manufacturer 's labeling; however, dosage adjustment may be necessary; use with caution.
Severe hepatic impairment: Use is not recommended.
Administer with or without food.
Store at 25 ‚ °C (77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F). Protect from light and moisture.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Fanapt: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg
Fanapt Titration Pack: 1 mg (2s), 2 mg (2s), 4 mg (2s), and 6 mg (2s)
Abiraterone Acetate: May increase the serum concentration of CYP2D6 Substrates. Management: Avoid concurrent use of abiraterone with CYP2D6 substrates that have a narrow therapeutic index whenever possible. When concurrent use is not avoidable, monitor patients closely for signs/symptoms of toxicity. Consider therapy modification
Acetylcholinesterase Inhibitors (Central): May enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients. Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy
Amisulpride: Antipsychotic Agents may enhance the adverse/toxic effect of Amisulpride. Avoid combination
Amphetamines: Antipsychotic Agents may diminish the stimulatory effect of Amphetamines. Monitor therapy
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
Anti-Parkinson Agents (Dopamine Agonist): Antipsychotic Agents (Second Generation [Atypical]) may diminish the therapeutic effect of Anti-Parkinson Agents (Dopamine Agonist). Management: Consider using an alternative antipsychotic agent when possible in patients with Parkinson disease. If an atypical antipsychotic is necessary, consider using clozapine or quetiapine, which may convey the lowest interaction risk. Consider therapy modification
Asunaprevir: May increase the serum concentration of CYP2D6 Substrates. Consider therapy modification
Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification
Blood Pressure Lowering Agents: May enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy
CYP2D6 Inhibitors (Moderate): May decrease the metabolism of CYP2D6 Substrates. Monitor therapy
CYP2D6 Inhibitors (Strong): May increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. CYP2D6 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Management: Reduce iloperidone dose by half when administered with a strong CYP2D6 inhibitor. Consider therapy modification
CYP3A4 Inhibitors (Strong): May increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolites P88 and P95 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Iloperidone. Management: Reduce iloperidone dose by half when administered with a strong CYP3A4 inhibitor. Consider therapy modification
Dimethindene: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy
Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification
Highest Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of other Highest Risk QTc-Prolonging Agents. Avoid combination
HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification
Ivabradine: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination
Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy
Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Consider therapy modification
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification
Methylphenidate: Antipsychotic Agents may enhance the adverse/toxic effect of Methylphenidate. Methylphenidate may enhance the adverse/toxic effect of Antipsychotic Agents. Monitor therapy
Metoclopramide: May enhance the adverse/toxic effect of Antipsychotic Agents. Avoid combination
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy
MetyroSINE: May enhance the adverse/toxic effect of Antipsychotic Agents. Monitor therapy
MiFEPRIStone: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination
Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Moderate Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Monitor therapy
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Peginterferon Alfa-2b may increase the serum concentration of CYP2D6 Substrates. Monitor therapy
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification
Perhexiline: CYP2D6 Substrates may increase the serum concentration of Perhexiline. Perhexiline may increase the serum concentration of CYP2D6 Substrates. Monitor therapy
Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Avoid combination
Piribedil [INT]: Antipsychotic Agents may diminish the therapeutic effect of Piribedil [INT]. Piribedil [INT] may diminish the therapeutic effect of Antipsychotic Agents. Management: Use of piribedil with antiemetic neuroleptics is contraindicated, and use with antipsychotic neuroleptics, except for clozapine, is not recommended. Avoid combination
QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying): May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification
Quinagolide: Antipsychotic Agents may diminish the therapeutic effect of Quinagolide. Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy
Serotonin Modulators: May enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Exceptions: Nicergoline. Monitor therapy
Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification
Sulpiride: Antipsychotic Agents may enhance the adverse/toxic effect of Sulpiride. Avoid combination
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification
Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification
Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Vinflunine: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification
Mental status; vital signs (as clinically indicated); blood pressure (baseline; repeat 3 months after antipsychotic initiation, then yearly); ECG (as clinically indicated); weight, height, BMI, waist circumference (baseline; repeat at 4, 8, and 12 weeks after initiating or changing therapy, then quarterly; consider switching to a different antipsychotic for a weight gain ≥5% of initial weight); CBC (as clinically indicated; monitor frequently during the first few months of therapy in patients with preexisting low WBC or history of drug-induced leukopenia/neutropenia); electrolytes (annually and as clinically indicated; perform baseline serum potassium and magnesium with periodic monitoring in patients at risk for significant electrolyte disturbances); liver function (annually and as clinically indicated); personal and family history of obesity, diabetes, dyslipidemia, hypertension, or cardiovascular disease (baseline; repeat annually); fasting plasma glucose level/HbA1c (baseline; repeat 3 months after starting antipsychotic, then yearly); fasting lipid panel (baseline; repeat 3 months after initiation of antipsychotic; if LDL level is normal, repeat at 2- to 5-year intervals or more frequently if clinical indicated); changes in menstruation, libido, development of galactorrhea, erectile and ejaculatory function (at each visit for the first 12 weeks after the antipsychotic is initiated or until the dose is stable, then yearly); abnormal involuntary movements or parkinsonian signs (baseline; repeat weekly until dose stabilized for at least 2 weeks after introduction and for 2 weeks after any significant dose increase); tardive dyskinesia (every 12 months; high-risk patients every 6 months); ocular examination (yearly in patients >40 years; every 2 years in younger patients) (ADA, 2004; Lehman, 2004; Marder, 2004).
>10%:
Cardiovascular: Tachycardia (3% to 12%; dose-related)
Central nervous system: Dizziness (10% to 20%; dose-related), drowsiness (9% to 15%)
1% to 10%:
Cardiovascular: Orthostatic hypotension (3% to 5%), hypotension ( ≤3%; dose-related), palpitations ( ≥1%)
Central nervous system: Fatigue (4% to 6%), extrapyramidal reaction (4% to 5%), lethargy (1% to 3%), akathisia (2%), aggressive behavior ( ≥1%), delusions ( ≥1%), restlessness ( ≥1%)
Dermatologic: Skin rash (2% to 3%)
Endocrine & metabolic: Weight gain (1% to 9%; dose-related), weight loss ( ≥1%)
Gastrointestinal: Nausea ( ≤10%), xerostomia (8% to 10%), diarrhea (5% to 7%), abdominal distress ( ≤3%; dose-related)
Genitourinary: Ejaculation failure (2%), erectile dysfunction ( ≥1%), urinary incontinence ( ≥1%)
Neuromuscular & skeletal: Arthralgia (3%), tremor (3%), muscle rigidity (1% to 3%; dose-related), dyskinesia (<2%), muscle spasm ( ≥1%), myalgia ( ≥1%)
Ophthalmic: Blurred vision ( ≤3%), conjunctivitis ( ≥1%)
Respiratory: Nasal congestion (5% to 8%), nasopharyngitis ( ≤4%), upper respiratory tract infection (2% to 3%), dyspnea (2%)
<1% (Limited to important or life-threatening): Abnormal gait, acute renal failure, amenorrhea, amnesia, anemia, anorgasmia, aphthous stomatitis, asthma, blepharitis, bradykinesia, bulimia nervosa, cardiac arrhythmia, cardiac failure, cataract, catatonia, cholelithiasis, confusion, decreased hematocrit, decreased hemoglobin, decreased libido, dehydration, delirium, dry nose, duodenal ulcer, dystonia, dysuria, edema, emotional lability, epistaxis, eyelid edema, fecal incontinence, first degree atrioventricular block, fluid retention, gastritis, gastroesophageal reflux disease, gynecomastia, hiatal hernia, hostility, hyperacidity, hyperemia, hypermenorrhea, hyperthermia, hypokalemia, hypothyroidism, impulse control disorder, increased appetite, increased neutrophils, increased thirst, leukopenia, major depressive disorder, mania, mastalgia, menstrual disease, nephrolithiasis, nystagmus, obsessive-compulsive disorder, oral mucosa ulcer, panic attack, paresthesia, paranoia, Parkinson disease, pollakiuria, polydipsia (psychogenic), postmenopausal bleeding, prolonged Q-T interval on ECG, prostatitis, pruritus, psychomotor agitation, restless leg syndrome, retrograde ejaculation, rhinorrhea, salivation, sinus congestion, sleep apnea, stomatitis, swelling of eye, testicular pain, tinnitus, torticollis, urinary retention, urticaria, uterine hemorrhage, vertigo, xerophthalmia
Higher (2-fold) and more variable free drug exposure to the active metabolite P88 in patients with moderate hepatic impairment.
Concerns related to adverse effects:
- Altered cardiac conduction: May alter cardiac conduction and prolong the QTc interval; life-threatening arrhythmias have occurred with therapeutic doses of antipsychotics. Risks may be increased by conditions or concomitant medications which cause bradycardia, hypokalemia, and/or hypomagnesemia. Avoid use in combination with QTc-prolonging drugs. Avoid use in patients with congenital long QT syndrome, history of cardiac arrhythmia, recent MI, and/or uncompensated heart failure. Use caution in combination with drugs that inhibit iloperidone metabolism. Discontinue in patients found to have persistent QTc intervals >500 msec. Patients with symptoms of dizziness, palpitations, or syncope should receive further cardiac evaluation.
- Blood dyscrasias: Leukopenia, neutropenia, and agranulocytosis (sometimes fatal) have been reported in clinical trials and postmarketing reports with antipsychotic use; presence of risk factors (eg, pre-existing low WBC or history of drug-induced leuko-/neutropenia) should prompt periodic blood count assessment. Discontinue therapy at first signs of blood dyscrasias or if absolute neutrophil count <1,000/mm3.
- Cerebrovascular effects: An increased incidence of cerebrovascular effects (eg, transient ischemic attack, stroke), including fatalities, has been reported in placebo-controlled trials of antipsychotics for the unapproved use in elderly patients with dementia-related psychosis.
- CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).
- Dyslipidemia: Undesirable alterations in lipids has been reported with atypical antipsychotics. Use with caution in patients with a pre-existing abnormal lipid profile.
- Esophageal dysmotility/aspiration: Antipsychotic use has been associated with esophageal dysmotility and aspiration; use with caution in patients at risk of aspiration pneumonia (eg, Alzheimer disease).
- Extrapyramidal symptoms (EPS): May cause EPS, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is generally much lower relative to typical/conventional antipsychotics). Risk of dystonia (and probably other EPS) may be greater with increased doses, use of conventional antipsychotics, males, and younger patients. Risk of tardive dyskinesia and potential for irreversibility may be increased in elderly patients (particularly women), prolonged therapy, and higher total cumulative dose; antipsychotics may also mask signs/symptoms of tardive dyskinesia. Consider therapy discontinuation with signs/symptoms of tardive dyskinesia.
- Hyperglycemia: Atypical antipsychotics have been associated with development of hyperglycemia; in some cases, may be extreme and associated with ketoacidosis, hyperosmolar coma, or death. Use with caution in patients with diabetes or other disorders of glucose regulation; monitor for worsening of glucose control.
- Hyperprolactinemia: Use is associated with increased prolactin levels; clinical significance of hyperprolactinemia in patients with breast cancer or other prolactin-dependent tumors is unknown.
- Hypersensitivity: Hypersensitivity reactions, including anaphylaxis, angioedema, throat tightness, oropharyngeal swelling, swelling of the face, lips, mouth and tongue, rash, pruritus, and urticaria, have been reported.
- Neuroleptic malignant syndrome (NMS): Use may be associated with NMS; monitor for mental status changes, fever, muscle rigidity and/or autonomic instability; risk may be increased in patients with Parkinson disease or Lewy body dementia. (McKeith 2002)
- Orthostatic hypotension: May cause orthostatic hypotension associated with dizziness, tachycardia, and syncope; use with caution in patients with known cardiovascular disease (heart failure, history of myocardial infarction or ischemia, conduction abnormalities), cerebrovascular disease, or conditions that predispose the patient to hypotension (dehydration, hypovolemia, and treatment with antihypertensive medications).
- Priapism: Rare cases of priapism have been reported.
- Suicidal ideation: The possibility of a suicide attempt is inherent in psychotic illness; use with caution in high-risk patients during initiation of therapy. Prescribe the smallest quantity consistent with good patient care.
- Temperature regulation: Impaired core body temperature regulation may occur; caution with strenuous exercise, heat exposure, dehydration, and concomitant medication possessing anticholinergic effects.
- Weight gain: Significant weight gain has been observed with antipsychotic therapy; incidence varies with product. Monitor waist circumference and BMI.
Disease-related concerns:
- Dementia: [US Boxed Warning]: Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Most deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Iloperidone is not approved for the treatment of dementia-related psychosis.
- Hepatic impairment: Use is not recommended in patients with severe hepatic impairment; use caution and consider dosage reduction in patients with moderate hepatic impairment.
- Seizures: Use with caution in patients at risk of seizures, including those with a history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Elderly patients may be at increased risk of seizures due to an increased prevalence of predisposing factors.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- CYP2D6 poor metabolizers: Use with caution in patients known to be poor metabolizers of CYP2D6; dosage adjustment recommended.
- Elderly: Use caution in older adults due to increased sensitivity to adverse effects (eg, tardive dyskinesia and seizures).
Adverse events have been observed in animal reproduction studies. Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (extrapyramidal symptoms [EPS]) and/or withdrawal symptoms in newborns following delivery. Symptoms in the newborn may include agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnolence, and tremor; these effects may be self-limiting or require hospitalization. Iloperidone may cause hyperprolactinemia, which may decrease reproductive function in both males and females.
The ACOG recommends that therapy during pregnancy be individualized; treatment with psychiatric medications during pregnancy should incorporate the clinical expertise of the mental health clinician, obstetrician, primary healthcare provider, and pediatrician. Safety data related to atypical antipsychotics during pregnancy is limited and routine use is not recommended. However, if a woman is inadvertently exposed to an atypical antipsychotic while pregnant, continuing therapy may be preferable to switching to a typical antipsychotic that the fetus has not yet been exposed to; consider risk:benefit (ACOG, 2008).
Healthcare providers are encouraged to enroll women 18 to 45 years of age exposed to iloperidone during pregnancy in the Atypical Antipsychotics Pregnancy Registry (1-866-961-2388 or http://www.womensmentalhealth.org/pregnancyregistry).
Iloperidone is a piperidinyl-benzisoxazole atypical antipsychotic with mixed D2/5-HT2 antagonist activity. It exhibits high affinity for 5-HT2A, NEα1, D2, and D3 receptors, low to moderate affinity for D1, D4, H1, 5-HT1A, 5-HT6, and 5-HT7 receptors, and no affinity for muscarinic receptors. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects (Huttunen 1995). Iloperidone 's low affinity for histamine H1 receptors may decrease the risk for weight gain and somnolence while its affinity for NEα1/α2C may improve cognitive function but increase the risk for orthostasis (Arif 2011, Huttunen 1995, Nasrallah 2008).
Well absorbed
Vd: 1,340 to 2,800 L
Hepatic via carbonyl reduction, hydroxylation (CYP2D6) and O-demethylation (CYP3A4); forms active metabolites (P88 and P95)
Active metabolites (P88 and P95): Urine (58% extensive metabolizers, 45% poor metabolizers); feces (20% extensive metabolizers, 22% poor metabolizers) (Sheehan 2010)
Iloperidone: <1% recovered unchanged in urine and feces (Sheehan 2010)
Plasma: 2 to 4 hours
Extensive metabolizers: Iloperidone: 18 hours; P88: 26 hours; P95: 23 hours
Poor metabolizers: Iloperidone: 33 hours; P88: 37 hours; P95: 31 hours
~97% iloperidone; ~92% active metabolites (P88 and P95)
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience nausea, weight gain, dry mouth, fatigue, loss of strength and energy, rhinitis, or diarrhea. Have patient report immediately to prescriber signs of infection, signs of neuroleptic malignant syndrome (fever, muscle cramps or stiffness, dizziness, very bad headache, confusion, change in thinking, fast heartbeat, abnormal heartbeat, or sweating a lot), signs of high blood sugar (confusion, feeling sleepy, more thirst, hunger, passing urine more often, flushing, fast breathing, or breath that smells like fruit), suicidal ideation, tachycardia, arrhythmia, severe dizziness, passing out, behavioral changes, mood changes, tremors, difficulty moving, rigidity, urinary retention, change in amount of urine passed, dysphagia, seizures, shortness of breath, enlarged breasts, sexual dysfunction, nipple discharge, amenorrhea, priapism, or signs of tardive dyskinesia (unable to control body movements; tongue, face, mouth, or jaw sticking out; mouth puckering; and puffing cheeks) (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.