Rexulti Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mechanism of Action
Rexulti Indications
Indications
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.
Rexulti Dosage and Administration
Adult
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
Rexulti Contraindications
Not Applicable
Rexulti Boxed Warnings
Boxed Warning
Rexulti Warnings/Precautions
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 Pharmacokinetics
Absorption
-
Peak plasma concentration occurred within 4 hours after administration.
-
Absolute oral bioavailability: 95%.
-
Steady-state concentrations were attained within 10 to 12 days of dosing.
Distribution
-
Volume of distribution after IV administration: 1.56 ± 0.42 L/kg.
-
>99% plasma protein bound.
Elimination
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Rexulti Interactions
Interactions
Rexulti Adverse Reactions
Adverse Reactions
Rexulti Clinical Trials
See Literature
Rexulti Note
Not Applicable
Rexulti Patient Counseling
See Literature
Rexulti Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mechanism of Action
Rexulti Indications
Indications
Rexulti Dosage and Administration
Adult
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 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
Rexulti Contraindications
Not Applicable
Rexulti Boxed Warnings
Boxed Warning
Rexulti Warnings/Precautions
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 Pharmacokinetics
Absorption
-
Peak plasma concentration occurred within 4 hours after administration.
-
Absolute oral bioavailability: 95%.
-
Steady-state concentrations were attained within 10 to 12 days of dosing.
Distribution
-
Volume of distribution after IV administration: 1.56 ± 0.42 L/kg.
-
>99% plasma protein bound.
Elimination
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Rexulti Interactions
Interactions
Rexulti Adverse Reactions
Adverse Reactions
Rexulti Clinical Trials
See Literature
Rexulti Note
Not Applicable
Rexulti Patient Counseling
See Literature
Rexulti Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mechanism of Action
Rexulti Indications
Indications
Rexulti Dosage and Administration
Adult
>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
<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.
Rexulti Contraindications
Not Applicable
Rexulti Boxed Warnings
Boxed Warning
Rexulti Warnings/Precautions
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 Pharmacokinetics
Absorption
-
Peak plasma concentration occurred within 4 hours after administration.
-
Absolute oral bioavailability: 95%.
-
Steady-state concentrations were attained within 10 to 12 days of dosing.
Distribution
-
Volume of distribution after IV administration: 1.56 ± 0.42 L/kg.
-
>99% plasma protein bound.
Elimination
-
Fecal (46%), renal (25%).
-
Half-life: 91 hours.
Rexulti Interactions
Interactions
Rexulti Adverse Reactions
Adverse Reactions
Rexulti Clinical Trials
See Literature
Rexulti Note
Not Applicable
Rexulti Patient Counseling
See Literature