lorcaserin (Belviq, Belviq XR)

Dosing and uses of Belviq, Belviq XR (lorcaserin)

• Adult
• Pediatric

 

Adult dosage forms and strengths

tablet: Schedule IV

• 10mg

extended-release tablet: Schedule IV

• 20mg

 

Obesity

Indicated as an adjunct to a reduced-calorie diet and exercise for chronic weight management with initial BMI ≥30 kg/m² (obese) or ≥27 kg/m² (overweight) with 1 weight-related comorbid condition (eg, hypertension, dyslipidemia, type 2 diabetes mellitus)

Tablets: 10 mg PO q12hr, Or

Extended-release tablets: 20 mg PO qDay

 

Dosage modifications

Renal impairment

• Mild (CrCl >50 mL/min): No dosage adjustment required
• Moderate (CrCl 30-50 mL/min): Use caution
• Severe (CrCl <30 mL/min) or ESRD: Not recommended

Hepatic impairment

• Mild-to-moderate (Child-Pugh score 5-9): No dosage adjustment required
• Severe (Child-Pugh score >9): Use caution

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Belviq, Belviq XR (lorcaserin) adverse (side) effects

>10%

Headache (16.8%)

Upper respiratory tract infection (13.7%)

Nasopharyngitis (13%)

 

1-10%

Dizziness (8.5%)

Nausea (8.3%)

Fatigue (7.2%)

Diarrhea (6.5%)

Urinary tract infection (6.5%)

Back pain (6.3%)

Constipation (5.8%)

Dry mouth (5.3%)

Vomiting (3.8%)

Rash (2.1%)

Musculoskeletal pain (2%)

 

Warnings

Contraindications

Pregnancy

Prior hypersensitivity reaction

 

Cautions

Monitor for serotonin syndrome or NMS-like reactions

Studies suggest possibility of regurgitant valvular heart disease (not likely); monitor if patient has congestive heart failure

Advise patient to take caution when operating hazardous machinery Monitor for worsening of depression, suicidal thoughts or behavior, or any other unusual changes in mood or behavior

Monitor for hypoglycemia with type 2 diabetes mellitus; if hypoglycemia occurs while on therapy; adjust antidiabetic drug regimen

Caution in men with predisposed conditions to priapism (eg sickle cell anemia, multiple myeloma, or leukemia) or anatomical deformation of the penis

Caution with bradycardia or a history of heart block

May cause decrease in white blood cell count and other hematological changes; consider periodic monitoring of CBC

Moderately elevates prolactin levels; obtain prolactin levels if hyperprolactinemia symptoms (eg, gynecomastia) occur

May cause pulmonary hypertension (insufficient data)

May cause confusion, somnolence, fatigue and cognitive impairment; use caution when operating heavy machinery or tasks that require mental alertness

Use in patients with severe hepatic impairment not studied; use caution

Use not recommended in patients with severe renal impairment or end stage renal disease;use caution in moderate renal impairment

 

Pregnancy and lactation

Pregnancy category: X

Lactation: Unknown whether distributed in breast milk; may increase prolactin and result in increased breast milk production

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Belviq, Belviq XR (lorcaserin)

Mechanism of action

Exact mechanism of action unknown

Thought to decrease food consumption and promote satiety by selectively activates 5-HT2C receptors on anorexigenic pro-opiomelanocortin neurons located in the hypothalamus

 

Absorption

Bioavailability: Undetermined

Peak Plasma Time: 1.5-2 hr (delayed by 1 hr when administered with food, but not clinically significant)

Peak Plasma Concentration: Increased ~9% with food

AUC: Increased ~5% with food

 

Distribution

Protein Bound: 70%

Distributed into CSF and CNs

 

Metabolism

Metabolized by liver by multiple pathways (extensive)

Metabolites: lorcaserin sulfamate is the major circulating metabolite (Cmax exceeds lorcaserin by 1- to 5-fold); N-carbamoyl glucuronide lorcaserin is the major urinary metabolite

Principal metabolites exert no pharmacological activity at serotonin receptors

 

Elimination

Half-life: 11 hr

Excretion: Urine 92.3% (mostly as metabolites), feces 2.2%

 

Administration

Oral Administration

May take with or without food

Discontinue if 5% weight loss not achieved by week 12

Do not exceed recommended dose

Extended-release tablets

• Swallow whole; do not chew, crush, or divide