Alzheimer's dementia:
Indications for: REXULTI
Agitation associated with dementia due to Alzheimer disease.
Limitations of Use:
Not indicated as an as needed (“prn”) treatment for agitation associated with dementia due to Alzheimer disease.
Adult Dosage:
Initially 0.5mg once daily on Days 1–7; titrate to 1mg once daily on Days 8–14, then to 2mg once daily on Day 15; target dose 2mg/day; max 3mg/day after at least 14 days based on clinical response and tolerability. Moderate to severe hepatic impairment (Child-Pugh ≥7), or renal impairment (CrCl <60mL/min): max 2mg/day. CYP2D6 poor metabolizers: give ½ of usual dose; and if taking with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP2D6 or strong CYP3A4 inhibitors: give ½ of usual dose. Concomitant moderate/strong CYP2D6 with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP3A4 inducers: double usual dose over 1–2 weeks.
Children Dosage:
Not established.
Boxed Warning:
Increased mortality in elderly patients with dementia-related psychosis. Suicidal thoughts and behaviors.
REXULTI Warnings/Precautions:
Elderly with dementia-related psychosis without agitation associated with dementia due to Alzheimer disease (not approved use); increased risk of death or cerebrovascular events (eg, stroke, TIA). Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults; monitor closely for worsening or unusual changes in all patients. Cardio- or cerebrovascular disease. Discontinue immediately if neuroleptic malignant syndrome is suspected; treat appropriately and monitor. Tardive dyskinesia. Pre-existing low WBC or ANC or history of leukopenia/neutropenia; monitor CBCs during 1st few months of treatment; discontinue if WBCs decline. Monitor for hyperglycemia/diabetes, dyslipidemia, weight gain. Risk of hypotension, syncope, or aspiration. Pathological gambling and other compulsive behaviors: consider dose reduction or discontinuation if develops. History of seizures or conditions that lower the seizure threshold. Strenuous exercise. Exposure to extreme heat. Dehydration. Hypovolemia. Perform fall risk assessments when initiating and recurrently on long-term therapy. CYP2D6 poor metabolizers. Renal or moderate to severe hepatic impairment. Write ℞ for smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post-delivery (due to exposure during 3rd-trimester pregnancy). Pregnancy. Nursing mothers.
REXULTI Classification:
Atypical antipsychotic.
REXULTI Interactions:
See Adults. May be potentiated by strong CYP3A4 inhibitors (eg, itraconazole, clarithromycin, ketoconazole) or strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine, quinidine). May be antagonized by strong CYP3A4 inducers (eg, rifampin, St. John’s wort). Potentiates antihypertensives. Caution with drugs that interfere with temperature regulation (eg, anticholinergics).
Adverse Reactions:
Weight gain, akathisia, headache, somnolence, tremor, nasopharyngitis, fatigue, increased appetite, dizziness, anxiety, restlessness.
Drug Elimination:
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
Mood disorders:
Indications for: REXULTI
Adjunct therapy for major depressive disorder (MDD).
Adult Dosage:
Initially 0.5mg or 1mg once daily; titrate weekly up to target dose of 2mg/day; max 3mg/day. Moderate to severe hepatic impairment (Child-Pugh ≥7), or renal impairment (CrCl <60mL/min): max 2mg/day. CYP2D6 poor metabolizers: give ½ of usual dose; and if taking with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP2D6 or strong CYP3A4 inhibitors: give ½ of usual dose. Concomitant moderate/strong CYP2D6 with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP3A4 inducers: double usual dose over 1–2 weeks.
Children Dosage:
Not established.
Boxed Warning:
Increased mortality in elderly patients with dementia-related psychosis. Suicidal thoughts and behaviors.
REXULTI Warnings/Precautions:
Elderly with dementia-related psychosis without agitation associated with dementia due to Alzheimer disease (not approved use); increased risk of death or cerebrovascular events (eg, stroke, TIA). Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults; monitor closely for worsening or unusual changes in all patients. Cardio- or cerebrovascular disease. Discontinue immediately if neuroleptic malignant syndrome is suspected; treat appropriately and monitor. Tardive dyskinesia. Pre-existing low WBC or ANC or history of leukopenia/neutropenia; monitor CBCs during 1st few months of treatment; discontinue if WBCs decline. Monitor for hyperglycemia/diabetes, dyslipidemia, weight gain. Risk of hypotension, syncope, or aspiration. Pathological gambling and other compulsive behaviors: consider dose reduction or discontinuation if develops. History of seizures or conditions that lower the seizure threshold. Strenuous exercise. Exposure to extreme heat. Dehydration. Hypovolemia. Perform fall risk assessments when initiating and recurrently on long-term therapy. CYP2D6 poor metabolizers. Renal or moderate to severe hepatic impairment. Write ℞ for smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post-delivery (due to exposure during 3rd-trimester pregnancy). Pregnancy. Nursing mothers.
REXULTI Classification:
Atypical antipsychotic.
REXULTI Interactions:
See Adults. May be potentiated by strong CYP3A4 inhibitors (eg, itraconazole, clarithromycin, ketoconazole) or strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine, quinidine). May be antagonized by strong CYP3A4 inducers (eg, rifampin, St. John’s wort). Potentiates antihypertensives. Caution with drugs that interfere with temperature regulation (eg, anticholinergics).
Adverse Reactions:
Weight gain, akathisia, headache, somnolence, tremor, nasopharyngitis, fatigue, increased appetite, dizziness, anxiety, restlessness.
Drug Elimination:
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
Psychosis:
Indications for: REXULTI
Schizophrenia.
Adult Dosage:
>17yrs: Initially 1mg once daily on Days 1–4; titrate to 2mg once daily on Day 5–7, then to 4mg once daily on Day 8; target dose 2–4mg/day; max 4mg/day. Moderate to severe hepatic impairment (Child-Pugh ≥7), or renal impairment (CrCl <60mL/min): max 3mg/day. CYP2D6 poor metabolizers: give ½ of usual dose; and if taking with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP2D6 or strong CYP3A4 inhibitors: give ½ of usual dose. Concomitant moderate/strong CYP2D6 with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP3A4 inducers: double usual dose over 1–2 weeks.
Children Dosage:
<13yrs: not established. 13–17yrs: Initially 0.5mg once daily on Days 1–4; titrate to 1mg once daily on Day 5–7, then to 2mg once daily on Day 8; target dose 2–4mg/day; max 4mg/day. Moderate to severe hepatic impairment (Child-Pugh ≥7), or renal impairment (CrCl <60mL/min): max 3mg/day. CYP2D6 poor metabolizers: give ½ of usual dose; and if taking with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP2D6 or strong CYP3A4 inhibitors: give ½ of usual dose. Concomitant moderate/strong CYP2D6 with moderate/strong CYP3A4 inhibitors: give ¼ of usual dose. Concomitant strong CYP3A4 inducers: double usual dose over 1–2 weeks.
Boxed Warning:
Increased mortality in elderly patients with dementia-related psychosis. Suicidal thoughts and behaviors.
REXULTI Warnings/Precautions:
Elderly with dementia-related psychosis without agitation associated with dementia due to Alzheimer disease (not approved use); increased risk of death or cerebrovascular events (eg, stroke, TIA). Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults; monitor closely for worsening or unusual changes in all patients. Cardio- or cerebrovascular disease. Discontinue immediately if neuroleptic malignant syndrome is suspected; treat appropriately and monitor. Tardive dyskinesia. Pre-existing low WBC or ANC or history of leukopenia/neutropenia; monitor CBCs during 1st few months of treatment; discontinue if WBCs decline. Monitor for hyperglycemia/diabetes, dyslipidemia, weight gain. Risk of hypotension, syncope, or aspiration. Pathological gambling and other compulsive behaviors: consider dose reduction or discontinuation if develops. History of seizures or conditions that lower the seizure threshold. Strenuous exercise. Exposure to extreme heat. Dehydration. Hypovolemia. Perform fall risk assessments when initiating and recurrently on long-term therapy. CYP2D6 poor metabolizers. Renal or moderate to severe hepatic impairment. Write ℞ for smallest practical amount. Neonates: risk of extrapyramidal and/or withdrawal symptoms post-delivery (due to exposure during 3rd-trimester pregnancy). Pregnancy. Nursing mothers.
REXULTI Classification:
Atypical antipsychotic.
REXULTI Interactions:
See Adults. May be potentiated by strong CYP3A4 inhibitors (eg, itraconazole, clarithromycin, ketoconazole) or strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine, quinidine). May be antagonized by strong CYP3A4 inducers (eg, rifampin, St. John’s wort). Potentiates antihypertensives. Caution with drugs that interfere with temperature regulation (eg, anticholinergics).
Adverse Reactions:
Weight gain, akathisia, headache, somnolence, tremor, nasopharyngitis, fatigue, increased appetite, dizziness, anxiety, restlessness.
Drug Elimination:
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Generic Drug Availability:
NO
How Supplied:
Tabs—30
