lorcaserin (Discontinued)

Brand and Other Names:Belviq, Belviq XR
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Dosing & Uses

AdultPediatric

FDA Safety Communication

February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer

For more information, see FDA Drug Safety Communication

Dosage Forms & Strengths

tablet: Schedule IV

  • 10mg

extended-release tablet: Schedule IV

  • 20mg

FDA Safety Communication

February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer

For more information, see FDA Drug Safety Communication

Health care professionals should stop prescribing and dispensing lorcaserin to patients

Contact patients currently taking lorcaserin, inform them of the increased occurrence of cancer seen in the clinical trial, and ask them to stop taking the medicine

Discuss alternative weight-loss medicines or strategies

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

Dravet Syndrome (Orphan)

Orphan designation for treatment of Dravet syndrome

Sponsor

  • Epygenix Therapeutics, Inc; 140 East Ridgewood Avenue, Suite 415 South Tower; Paramus, New Jersey 07652

Safety and efficacy not established

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Interactions

Interaction Checker

and lorcaserin

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse 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%)

            Postmarketing Reports

            Hypersensitivity

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            Warnings

            Contraindications

            Pregnancy

            Prior hypersensitivity reaction

            Cautions

            Monitor for serotonin syndrome or NMS-like reactions; discontinue therapy and any concomitant serotonergic and/or dopaminergic agents immediately if signs or symptoms arise

            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

            Priapism may occur; men with erections >4 hours should immediately discontinue therapy and seek emergency medical attention to avoid irreversible damage to erectile tissue; 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

            Neutropenia, leukopenia, lymphopenia, anemia and/or decreases in hematocrit and hemoglobin reported; consider monitoring CBC periodically during use

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            Pregnancy & Lactation

            Pregnancy

            Contraindicated during pregnancy, because weight loss offers no benefit to a pregnant woman and may result in fetal harm; limited data on lorcaserin use in pregnant women are not sufficient to determine drug-associated risk of major congenital malformations or miscarriage; appropriate weight gain based on pre-pregnancy weight is currently recommended for all pregnant women, including those who are already overweight or obese, due to the obligatory weight gain that occurs in maternal tissues during pregnancy; in rats, maternal exposure to lorcaserin in late pregnancy resulted in lower body weight in offspring which persisted to adulthood; advise pregnant women of potential risk to a fetus

            Lactation

            There are no data on presence of lorcaserin in human milk, effects on breastfed infant, or effects on milk production; because of potential for serious adverse reactions in breastfed infant, advise women receiving therapy that product is not recommended while breastfeeding

            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.

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            Pharmacology

            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%

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            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
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.