lorcaserin (Rx)

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Brand and Other Names:Belviq, Belviq XR

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet: Schedule IV

  • 10mg

extended-release tablet: Schedule IV

  • 20mg
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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

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%)

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            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

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            Pregnancy & 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.

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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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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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