Dosing & Uses
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February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer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February 13, 2020: FDA requests lorcaserin be withdrawn from the market owing to a potential risk of cancer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
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

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 topical
cocaine topical 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 (82)
- 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.
- dextroamphetamine transdermal
lorcaserin, dextroamphetamine transdermal. Either increases effects of the other by serotonin levels. Modify Therapy/Monitor Closely. Initiate with lower doses and monitor for signs and symptoms of serotonin syndrome, particularly during initiation or dosage increase. If serotonin syndrome occurs, discontinue dextroamphetamine transdermal and concomitant serotonergic drug(s).
lorcaserin will increase the level or effect of dextroamphetamine transdermal by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Initiate with lower doses and monitor patients for signs and symptoms of serotonin syndrome, particularly during dextroamphetamine initiation and after a dosage increase. If serotonin syndrome occurs, discontinue dextroamphetamine transdermal and CYP2D6 inhibitor. - 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.
- gepirone
gepirone and lorcaserin both increase serotonin levels. Use Caution/Monitor. Monitor for symptoms of serotonin syndrome when gepirone is used gepirone with other drugs that may affect the serotonergic neurotransmitter systems. If serotonin syndrome occurs, consider discontinue gepirone and/or concomitant serotonergic drug.
- 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)
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
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
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.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%
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