Rexulti

Brexpiprazole

Schizophrenia in adults. Adjunctive treatment of major depressive disorder (MDD) in adults w/ inadequate response to prior antidepressant treatments during the current episode.

Schizophrenia Recommended starting dose: 1 mg once daily on days 1-4. Dose can be titrated to 2 mg once daily on days 5-7, then to 4 mg on day 8. Max: 4 mg once daily. Patients w/ moderate to severe hepatic impairment (Child-Pugh score ≥7); moderate, severe or end-stage renal impairment (CrCl <60 mL/min) Max recommended dose: 3 mg once daily. Adjunctive treatment in MDD Recommended starting dose: 0.5 or 1 mg once daily. Dose can be titrated at wkly intervals to 1 mg once daily, then up to recommended target dose 2 mg once daily. Max: 2 mg once daily. Patients w/ moderate to severe hepatic impairment (Child-Pugh score ≥7); moderate, severe or end-stage renal impairment (CrCl <60 mL/min) Max recommended dose: 1.25 mg once daily.

May be taken with or without food.

Hypersensitivity.

Post-marketing reports of serious hypersensitivity reactions. Not indicated for patients w/ dementia. Increased mortality in elderly patients w/ dementia. Closely monitor patients for signs of suicidal ideation & behavior; impulse-control disorders/compulsive behaviors. Disruption of body's ability to reduce core body temp; orthostatic hypotension; QTc prolongation; hyperglycemia & DM; metabolic changes including wt gain; dyslipidemia; elevated prolactin levels; leukopenia/neutropenia, agranulocytosis; VTE; NMS; tardive dyskinesia. Closely observe patients for signs of Rexulti misuse or abuse. Caution in patients w/ history of seizures or w/ conditions that lower the seizure threshold. Patients at risk for aspiration pneumonia. Potential for cognitive & motor impairment. Monitor fasting lipid profile, blood glucose & wt gain at baseline & periodically during treatment. Frequently monitor CBC in patients w/ pre-existing low WBC or history of drug-induced leukopenia/neutropenia during the 1st few mth of therapy; discontinue at the 1st sign of clinically significant decline in WBC or severe neutropenia (ANC <1x10⁹/L). May cause somnolence, postural hypotension, motor & sensory instability which may lead to falls & consequently, fractures or other injuries. Rare cases of priapism w/ antipsychotic use. Patients w/ rare hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Pregnancy. Women receiving Rexulti should not breastfeed. Not recommended in ped patients <18 yr. Elderly >65 yr. CYP2D6 poor metabolizers.

Diarrhoea, dry mouth; increased wt; back pain; akathisia, tremor, dizziness; restlessness. Schizophrenia: Dyspepsia, upper abdominal pain; increased blood creatine phosphokinase; pain in extremity, myalgia; sedation; rash. MDD: Blurred vision; constipation, flatulence; fatigue, asthenia; nasopharyngitis; decreased blood cortisol, increased blood prolactin; increased appetite; headache, somnolence; insomnia, anxiety, irritability.

Increased AUC w/ strong CYP3A4 inhibitors (ketoconazole); strong CYP2D6 inhibitors (quinidine, paroxetine, fluoxetine). Decreased AUC & C_max w/ strong CYP3A4 inducers (eg, rifampicin). Caution in combination w/ drugs known to cause QT-prolongation or electrolyte disturbances. Avoid combination w/ alcohol or other CNS drugs w/ overlapping undesirable effects eg, sedation.

Antipsychotics

N05AX16 - brexpiprazole ; Belongs to the class of other antipsychotics.

P₁S₁S₃