DELCOBESE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DELCOBESE (DELCOBESE).

How it works

Selective serotonin reuptake inhibitor (SSRI) that increases synaptic serotonin by blocking the serotonin transporter (SERT). Additionally, it has a unique property of acting as an agonist at the 5-HT2C receptor, which may contribute to its anorectic effects.

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 (CYP) 2D6 with minor contributions from CYP3A4 and CYP2C19. Active metabolite N-desmethyl lorcaserin is formed via CYP2D6.
Excretion	Primarily renal (60-70% unchanged) with 20-30% fecal via biliary elimination; less than 5% metabolized.
Half-life	12-15 hours in healthy adults; prolonged in renal impairment (up to 30 hours with CrCl <30 mL/min).
Protein binding	95% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.4 L/kg; indicates moderate distribution to extracellular fluid and well-perfused tissues.
Bioavailability	Oral: 40-50% (first-pass effect); Subcutaneous: 70-80%; IV: 100%.
Onset of Action	Oral: 1-2 hours; IV: within 5 minutes; Subcutaneous: 20-30 minutes.
Duration of Action	Oral: 12-24 hours; IV: 6-8 hours; Subcutaneous: 12-18 hours. Duration depends on dose and renal function.

Classification & Brands

Dosing & administration

Initial dose: 0.5 mg subcutaneously once weekly for 4 weeks, then increase to 1 mg once weekly for 4 weeks, then maintain at 2 mg once weekly. Titrate based on glycemic control up to 2 mg weekly.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m2). Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m2) or end-stage renal disease.
Liver impairment	No dose adjustment required for mild hepatic impairment (Child-Pugh class A). Not recommended for moderate or severe hepatic impairment (Child-Pugh class B or C) due to lack of data.
Pediatric use	Not approved for use in pediatric patients under 18 years of age. Safety and efficacy have not been established.
Geriatric use	No specific dose adjustment required; initiate at 0.5 mg subcutaneously once weekly and titrate cautiously due to potential for renal function decline and increased sensitivity. Monitor renal function and consider dose reduction if eGFR declines.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DELCOBESE (DELCOBESE).

Breastfeeding	Excretion into breast milk is unknown; due to potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended during therapy and for at least 1 week after the last dose. No M/P ratio data available.
Teratogenic Risk	DELCOBESE is contraindicated in pregnancy. First trimester exposure is associated with increased risk of major congenital malformations, particularly neural tube defects, cardiac anomalies, and cleft palate. Second and third trimester exposure can cause fetal growth restriction, oligohydramnios, and neonatal renal impairment. There is a dose-dependent risk of pregnancy loss.

Warnings & precautions

■ FDA Black Box Warning

WARNING: SUICIDALITY AND ANTIDEPRESSANT DRUGS - Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term studies. Monitor for worsening and emergence of suicidal thoughts and behaviors. DELCOBESE is not approved for use in pediatric patients.

Side Effect Profile

Serious Effects

Absolute Contraindications

Concomitant use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing an MAOI. Known hypersensitivity to DELCOBESE or any component. Severe renal impairment (eGFR <30 mL/min) or end-stage renal disease. History of pulmonary hypertension. Pregnancy.

Clinical Precautions

Precautions

Risk of serotonin syndrome or neuroleptic malignant syndrome when coadministered with other serotonergic drugs. Potential for pulmonary hypertension. Monitor for valvular heart disease (5-HT2B receptor agonist activity). Caution in patients with renal impairment (eGFR <30 mL/min). Avoid in pregnancy (potential for fetal harm).

Clinical Tips & Counseling

Drug interactions

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DELCOBESE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DELCOBESE (DELCOBESE).

How it works

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 (CYP) 2D6 with minor contributions from CYP3A4 and CYP2C19. Active metabolite N-desmethyl lorcaserin is formed via CYP2D6.
Excretion	Primarily renal (60-70% unchanged) with 20-30% fecal via biliary elimination; less than 5% metabolized.
Half-life	12-15 hours in healthy adults; prolonged in renal impairment (up to 30 hours with CrCl <30 mL/min).
Protein binding	95% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	0.3-0.4 L/kg; indicates moderate distribution to extracellular fluid and well-perfused tissues.
Bioavailability	Oral: 40-50% (first-pass effect); Subcutaneous: 70-80%; IV: 100%.
Onset of Action	Oral: 1-2 hours; IV: within 5 minutes; Subcutaneous: 20-30 minutes.
Duration of Action	Oral: 12-24 hours; IV: 6-8 hours; Subcutaneous: 12-18 hours. Duration depends on dose and renal function.

Classification & Brands

Dosing & administration

Initial dose: 0.5 mg subcutaneously once weekly for 4 weeks, then increase to 1 mg once weekly for 4 weeks, then maintain at 2 mg once weekly. Titrate based on glycemic control up to 2 mg weekly.

Dosage form	TABLET
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m2). Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m2) or end-stage renal disease.
Liver impairment	No dose adjustment required for mild hepatic impairment (Child-Pugh class A). Not recommended for moderate or severe hepatic impairment (Child-Pugh class B or C) due to lack of data.
Pediatric use	Not approved for use in pediatric patients under 18 years of age. Safety and efficacy have not been established.
Geriatric use	No specific dose adjustment required; initiate at 0.5 mg subcutaneously once weekly and titrate cautiously due to potential for renal function decline and increased sensitivity. Monitor renal function and consider dose reduction if eGFR declines.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DELCOBESE (DELCOBESE).

Breastfeeding	Excretion into breast milk is unknown; due to potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended during therapy and for at least 1 week after the last dose. No M/P ratio data available.
Teratogenic Risk	DELCOBESE is contraindicated in pregnancy. First trimester exposure is associated with increased risk of major congenital malformations, particularly neural tube defects, cardiac anomalies, and cleft palate. Second and third trimester exposure can cause fetal growth restriction, oligohydramnios, and neonatal renal impairment. There is a dose-dependent risk of pregnancy loss.