lorcaserin (Belviq, Belviq XR)
Classes: CNS Stimulants, Anorexiants; Serotonin 5-HT2C-Receptor Agonists
Dosing and uses of Belviq, Belviq XR (lorcaserin)
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