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February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer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February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer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

Next:

Interactions

Interaction Checker

and lorcaserin

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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             activity indicator 

            Contraindicated (1)

            • eliglustat

              lorcaserin increases levels of eliglustat by affecting hepatic enzyme CYP2D6 metabolism. Contraindicated. If coadministered with strong or moderate CYP2D6 inhibitors, reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive and intermediate metabolizers; eliglustat is contraindiated if strong or moderate CYP2D6 inhibitors are given concomitantly with strong or moderate CYP3A inhibitors.

            Serious - Use Alternative (55)

            • almotriptan

              almotriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • amitriptyline

              amitriptyline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • bupropion

              bupropion and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • buspirone

              buspirone and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • citalopram

              citalopram and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • clomipramine

              clomipramine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • cocaine

              cocaine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • desipramine

              desipramine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • desvenlafaxine

              desvenlafaxine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • dextroamphetamine

              dextroamphetamine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • dextromethorphan

              dextromethorphan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • doxepin

              doxepin and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • duloxetine

              duloxetine and lorcaserin both increase sedation. Avoid or Use Alternate Drug.

            • eletriptan

              eletriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • escitalopram

              escitalopram and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • fluoxetine

              fluoxetine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • fluvoxamine

              fluvoxamine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • frovatriptan

              frovatriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • imipramine

              imipramine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • iobenguane I 131

              lorcaserin will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.

            • isocarboxazid

              isocarboxazid and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • isoniazid

              isoniazid and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • L-tryptophan

              L-tryptophan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • levomilnacipran

              levomilnacipran and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • linezolid

              linezolid and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • lisdexamfetamine

              lisdexamfetamine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • lithium

              lithium and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • meperidine

              meperidine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • methamphetamine

              methamphetamine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • metoclopramide intranasal

              lorcaserin will increase the level or effect of metoclopramide intranasal by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Concurrent use of metoclopramide intranasal and strong CYP2D6 inhibitors is not recommended since the metoclopramide intranasal dose cannot be adjusted.

            • milnacipran

              milnacipran and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • mirtazapine

              mirtazapine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • naratriptan

              naratriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • nefazodone

              nefazodone and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • nortriptyline

              nortriptyline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • paroxetine

              paroxetine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • perphenazine

              perphenazine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • phenelzine

              phenelzine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • protriptyline

              protriptyline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • rasagiline

              rasagiline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • rizatriptan

              rizatriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • selegiline

              selegiline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • selegiline transdermal

              selegiline transdermal and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • sertraline

              sertraline and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • St John's Wort

              St John's Wort and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • sumatriptan

              sumatriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • sumatriptan intranasal

              sumatriptan intranasal and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • tramadol

              tramadol and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • tranylcypromine

              tranylcypromine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • trazodone

              trazodone and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • venlafaxine

              venlafaxine and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • vilazodone

              vilazodone and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • vortioxetine

              lorcaserin increases levels of vortioxetine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Decrease vortioxetine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • ziprasidone

              ziprasidone and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            • zolmitriptan

              zolmitriptan and lorcaserin both increase serotonin levels. Avoid or Use Alternate Drug.

            Monitor Closely (80)

            • amitriptyline

              lorcaserin will increase the level or effect of amitriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • amoxapine

              lorcaserin will increase the level or effect of amoxapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • aripiprazole

              lorcaserin will increase the level or effect of aripiprazole by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, aripiprazole. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • asenapine

              lorcaserin, asenapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • atomoxetine

              lorcaserin will increase the level or effect of atomoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • benzhydrocodone/acetaminophen

              benzhydrocodone/acetaminophen, lorcaserin. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.

            • betaxolol

              lorcaserin will increase the level or effect of betaxolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • brexpiprazole

              lorcaserin will increase the level or effect of brexpiprazole by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Administer half of the usual brexpiprazole dose when coadministered with strong CYP2D6 inhibitors. If also administered with a strong/moderate CYP3A4 inhibitor, administer a quarter of brexpiprazole dose. NOTE: In MDD clinical trials, brexpiprazole dosage was not adjusted for strong CYP2D6 inhibitors (eg, paroxetine, fluoxetine); thus, CYP considerations are already factored into general dosing recommendations and brexpiprazole may be administered without dosage adjustment in patients with MDD.

            • captopril

              lorcaserin will increase the level or effect of captopril by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • cariprazine

              lorcaserin, cariprazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • carvedilol

              lorcaserin will increase the level or effect of carvedilol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • chloroquine

              lorcaserin will increase the level or effect of chloroquine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • chlorpromazine

              lorcaserin will increase the level or effect of chlorpromazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • cinacalcet

              lorcaserin will increase the level or effect of cinacalcet by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • citalopram

              lorcaserin will increase the level or effect of citalopram by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • clomipramine

              lorcaserin will increase the level or effect of clomipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • clozapine

              lorcaserin, clozapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • codeine

              lorcaserin will increase the level or effect of codeine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Prevents conversion of codeine to its active metabolite morphine.

            • desipramine

              lorcaserin will increase the level or effect of desipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • deutetrabenazine

              lorcaserin will increase the level or effect of deutetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Strong CYP2D6 inhibitors increase the systemic exposure to the active dihydro-metabolites of deutetrabenazine by approximately 3-fold. Do not exceed 18 mg/dose and 36 mg/day of deutetrabenazine if coadministered with strong CYP2D6 inhibitors.

            • doxepin

              lorcaserin will increase the level or effect of doxepin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • doxepin cream

              lorcaserin will increase the level or effect of doxepin cream by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • doxorubicin

              lorcaserin will increase the level or effect of doxorubicin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • doxorubicin liposomal

              lorcaserin will increase the level or effect of doxorubicin liposomal by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • duloxetine

              lorcaserin will increase the level or effect of duloxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • eluxadoline

              lorcaserin increases levels of eluxadoline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP2D6 inhibitors.

            • epinephrine inhaled

              lorcaserin, epinephrine inhaled. Either increases effects of the other by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.

            • flecainide

              lorcaserin will increase the level or effect of flecainide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • fluoxetine

              lorcaserin will increase the level or effect of fluoxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • fluphenazine

              lorcaserin will increase the level or effect of fluphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, fluphenazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • fluvoxamine

              lorcaserin will increase the level or effect of fluvoxamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • haloperidol

              lorcaserin will increase the level or effect of haloperidol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, haloperidol. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • hydrocodone

              hydrocodone, lorcaserin. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.

            • iloperidone

              lorcaserin will increase the level or effect of iloperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, iloperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • imipramine

              lorcaserin will increase the level or effect of imipramine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • lofexidine

              lorcaserin will increase the level or effect of lofexidine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Concomitant use of lofexidine with strong CYP2D6 inhibitors may increase lofexidine plasma levels. Monitor for symptoms of orthostasis and bradycardia if coadministered with a CYP2D6 inhibitor. Consider lofexidine dose reduction.

            • loxapine

              lorcaserin, loxapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • loxapine inhaled

              lorcaserin, loxapine inhaled. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • lurasidone

              lorcaserin, lurasidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • maprotiline

              lorcaserin will increase the level or effect of maprotiline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • metaxalone

              lorcaserin will increase the level or effect of metaxalone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • methamphetamine

              lorcaserin will increase the level or effect of methamphetamine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • metoprolol

              lorcaserin will increase the level or effect of metoprolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • mirtazapine

              lorcaserin will increase the level or effect of mirtazapine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • molindone

              lorcaserin, molindone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • nebivolol

              lorcaserin will increase the level or effect of nebivolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • nefazodone

              lorcaserin will increase the level or effect of nefazodone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • nortriptyline

              lorcaserin will increase the level or effect of nortriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • olanzapine

              lorcaserin, olanzapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • oliceridine

              lorcaserin will increase the level or effect of oliceridine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If concomitant use is necessary, may require less frequent oliceridine dosing. Closely monitor for respiratory depression and sedation and titrate subsequent doses accordingly. If inhibitor is discontinued, consider increase oliceridine dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal.

            • paliperidone

              lorcaserin, paliperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • paroxetine

              lorcaserin will increase the level or effect of paroxetine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • perphenazine

              lorcaserin will increase the level or effect of perphenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, perphenazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • pimavanserin

              lorcaserin, pimavanserin. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • pimozide

              lorcaserin, pimozide. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • pindolol

              lorcaserin will increase the level or effect of pindolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • pitolisant

              lorcaserin will increase the level or effect of pitolisant by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. If coadministered with strong CYP2D6 inhibitors, initiate pitolisant at 8.9 mg/day and increase after 7 days to maximum of 17.8 mg/day. For patients currently taking pitolisant, reduce pitolisant dose by half upon initiating strong CYP2D6 inhibitors.

            • procainamide

              lorcaserin will increase the level or effect of procainamide by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • promethazine

              lorcaserin will increase the level or effect of promethazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • propafenone

              lorcaserin will increase the level or effect of propafenone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • propranolol

              lorcaserin will increase the level or effect of propranolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • protriptyline

              lorcaserin will increase the level or effect of protriptyline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • quetiapine

              lorcaserin, quetiapine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • risperidone

              lorcaserin will increase the level or effect of risperidone by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

              lorcaserin, risperidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • ritonavir

              lorcaserin will increase the level or effect of ritonavir by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • sertraline

              lorcaserin will increase the level or effect of sertraline by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • sufentanil SL

              sufentanil SL, lorcaserin. Either increases effects of the other by serotonin levels. Use Caution/Monitor. Coadministration of drugs that affect the serotonergic neurotransmitter system may result in serotonin syndrome. If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment.

            • tamoxifen

              lorcaserin will decrease the level or effect of tamoxifen by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • tamsulosin

              lorcaserin increases levels of tamsulosin by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • thioridazine

              lorcaserin will increase the level or effect of thioridazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • thiothixene

              lorcaserin, thiothixene. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • timolol

              lorcaserin will increase the level or effect of timolol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • timolol ophthalmic

              lorcaserin will increase the level or effect of timolol ophthalmic by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • tolterodine

              lorcaserin will increase the level or effect of tolterodine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • tramadol

              lorcaserin will increase the level or effect of tramadol by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • trifluoperazine

              lorcaserin, trifluoperazine. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            • trimipramine

              lorcaserin will increase the level or effect of trimipramine by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.

            • valbenazine

              lorcaserin will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.

            • venlafaxine

              lorcaserin will increase the level or effect of venlafaxine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor.

            • ziprasidone

              lorcaserin, ziprasidone. unspecified interaction mechanism. Use Caution/Monitor. Serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotics may enhance serotonergic effect of serotonin modulators, which may result in serotonin syndrome. Monitor for evidence of serotonin toxicity (eg, mental status changes, autonomic instability, and neuromuscular hyperactivity) or neuroleptic malignant syndrome (eg, hyperthermia, muscle rigidity, autonomic dysfunction).

            Minor (0)

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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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              Images

              No images available for this drug.
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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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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.