SERPANRAY

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SERPANRAY (SERPANRAY).

How it works

Serotonin-dopamine activity modulator; partial agonist at 5-HT1A and D2 receptors, antagonist at 5-HT2A receptors.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2D6; minor pathways include CYP1A2 and CYP2C19.
Excretion	Primarily hepatic metabolism via CYP1A2 and CYP3A4, with 18% excreted unchanged in urine and 26% in feces as metabolites.
Half-life	Terminal elimination half-life is approximately 62 hours following oral administration, allowing for once-daily dosing.
Protein binding	99.5% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Apparent Vd is 4.0 L/kg, indicating extensive tissue distribution beyond plasma volume.
Bioavailability	Oral bioavailability is 30–40% due to first-pass metabolism.
Onset of Action	Oral: Clinical effects (antipsychotic) typically begin within 1–2 hours after first dose, with peak effects at steady state (10–14 days).
Duration of Action	After single oral dose, antipsychotic effects persist for 24 hours due to long half-life. Steady-state maintained with once-daily dosing.

Classification & Brands

Dosing & administration

1.5 mg orally once daily at bedtime, titrated up to a maximum of 3 mg once daily.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min), use is not recommended due to lack of data.
Liver impairment	Child-Pugh Class A: No dosage adjustment. Child-Pugh Class B: Reduce dose to 1 mg once daily, may increase to 1.5 mg based on tolerability. Child-Pugh Class C: Use is not recommended.
Pediatric use	Not approved for pediatric patients below 18 years of age; no specific dosing guidelines available.
Geriatric use	Elderly patients may be more sensitive to sedative and orthostatic hypotensive effects. Initiate at 1 mg once daily, titrate cautiously. Maximum dose 1.5 mg once daily for patients >65 years.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SERPANRAY (SERPANRAY).

Breastfeeding	No data on presence in human milk, effects on breastfed infant, or milk production. M/P ratio unknown. Caution recommended; consider alternative agents.
Teratogenic Risk	First trimester: No adequate human data; animal studies not available. Risk cannot be excluded. Second/third trimester: No data; consider risks versus benefits. Pregnancy category N (not classified by FDA due to lack of data).
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. SERPANRAY is not approved for the treatment of dementia-related psychosis.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to SERPANRAY or any of its components; concomitant use with strong CYP3A4 inducers or inhibitors (due to potential for significant drug interactions); history of severe allergic reactions (e.g., anaphylaxis, angioedema) to SERPANRAY.

Clinical Precautions

Precautions

Cerebrovascular adverse events in elderly dementia patients; neuroleptic malignant syndrome; tardive dyskinesia; metabolic changes (hyperglycemia, dyslipidemia, weight gain); hyperprolactinemia; orthostatic hypotension; leukopenia/neutropenia/agranulocytosis; seizures; body temperature dysregulation; dysphagia; falls; cognitive and motor impairment; increased mortality in elderly with dementia.

Clinical Tips & Counseling

Drug interactions

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SERPANRAY

Clinical safety rating: caution

Comprehensive clinical and safety monograph for SERPANRAY (SERPANRAY).

How it works

Serotonin-dopamine activity modulator; partial agonist at 5-HT1A and D2 receptors, antagonist at 5-HT2A receptors.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2D6; minor pathways include CYP1A2 and CYP2C19.
Excretion	Primarily hepatic metabolism via CYP1A2 and CYP3A4, with 18% excreted unchanged in urine and 26% in feces as metabolites.
Half-life	Terminal elimination half-life is approximately 62 hours following oral administration, allowing for once-daily dosing.
Protein binding	99.5% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Apparent Vd is 4.0 L/kg, indicating extensive tissue distribution beyond plasma volume.
Bioavailability	Oral bioavailability is 30–40% due to first-pass metabolism.
Onset of Action	Oral: Clinical effects (antipsychotic) typically begin within 1–2 hours after first dose, with peak effects at steady state (10–14 days).
Duration of Action	After single oral dose, antipsychotic effects persist for 24 hours due to long half-life. Steady-state maintained with once-daily dosing.

Classification & Brands

Dosing & administration

1.5 mg orally once daily at bedtime, titrated up to a maximum of 3 mg once daily.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min), use is not recommended due to lack of data.
Liver impairment	Child-Pugh Class A: No dosage adjustment. Child-Pugh Class B: Reduce dose to 1 mg once daily, may increase to 1.5 mg based on tolerability. Child-Pugh Class C: Use is not recommended.
Pediatric use	Not approved for pediatric patients below 18 years of age; no specific dosing guidelines available.
Geriatric use	Elderly patients may be more sensitive to sedative and orthostatic hypotensive effects. Initiate at 1 mg once daily, titrate cautiously. Maximum dose 1.5 mg once daily for patients >65 years.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for SERPANRAY (SERPANRAY).

Breastfeeding	No data on presence in human milk, effects on breastfed infant, or milk production. M/P ratio unknown. Caution recommended; consider alternative agents.
Teratogenic Risk	First trimester: No adequate human data; animal studies not available. Risk cannot be excluded. Second/third trimester: No data; consider risks versus benefits. Pregnancy category N (not classified by FDA due to lack of data).
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. SERPANRAY is not approved for the treatment of dementia-related psychosis.