| Identification | Back Directory | [Name]
Lorcaserin hydrochloride | [CAS]
846589-98-8 | [Synonyms]
LORCASERIN HCL
(R)-1H-3-BENZAZEPINE
Lorcaserin hydrochloride
R Lorcaserin hydrochloride
Lorcaserin Hydrochloride (>
Thiosildenafil Solution, 100ppm
Lorcaserin (hydrochloride) (CRM)
Lorcaserin Hydrochloride (>50% ee)
Green Card mianserin hydrochloride
lorcaserin hydrochloride (APD-356)
R-Lorcaserin hydrochloride USP/EP/BP
LORCASERIN HCL;APD-356;APD356;APD 356
Lorcaserin HCl , Lorcaserin Hydrochloride
Lorcaserin Hydrochloride Solution in Methanol, 1000 ug/ml
(1R)-8-chloro-1-Methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
(R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
(R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE
(R)-8-Chloro-1-Methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine hydrochloride
Lorcaserin hydrochloride, 98%, a selective full agonist of human 5-HT2C receptor
1H-3-Benzazepine,8-chloro-2,3,4,5-tetrahydro-1-Methyl-, hydrochloride (1:1), (1R)-
(R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE USP/EP/BP | [EINECS(EC#)]
1592732-453-0 | [Molecular Formula]
C11H15Cl2N | [MDL Number]
MFCD09833667 | [MOL File]
846589-98-8.mol | [Molecular Weight]
232.15 |
| Hazard Information | Back Directory | [Description]
In June 2012, the US FDA approved lorcaserin for chronic weight management
in adult patients who are characterized as overweight or obese and
have at least one comorbid, weight-related condition.
Lorcaserin (also known as APD356) is the first 5-HT2C agonist
approved for chronic weight management since the withdrawal of the
5-HT2C agonist fenfluramine in 1997 due to rare cases of cardiac valvulopathy. The serotonin receptor 5-HT2C is found primarily in the hypothalamus
and regulates appetite and feeding behavior. Safety issues with
fenfluramine were associated with poor selectivity for 5-HT2C versus
5HT2A and 5HT2B. Ring constraint afforded by the benzazepine in
lorcaserin improved selectivity for 5HT2C by over 2 log units. | [Originator]
Pharmaceuticals (United States) | [Uses]
Lorcaserin hydrochloride, a novel antiobesity drug, is a selective serotonin 5-HT2C receptor agonist, approved by FDA in 2012. | [Definition]
ChEBI: A hydrochloride obtained by reaction of lorcaserin with one equivalent of hydrochloric acid. Used as an anti-obesity drug. | [Brand name]
Belviq | [Side effects]
Lorcaserin hydrochloride (Belviq) is a serotonin 2C receptor agonist that causes weight loss by causing appetite suppression.It appears to have fewer adverse effects than orlistat,although long-term safety data are limited. The recommended dosage is 10mg twice daily. Lorcaserin should be discontinued if patients do not lose 5% of their body weight in 12 weeks. The efficacy of lorcaserin appears similar to that of orlistat (mean difference in weight loss between active and placebo-treated groups approximately 3-4 kg).Common side effects include nausea, headache,dizziness, nasopharyngitis, and fatigue. Lorcaserin may increasethe risk of symptomatic hypoglycemia in patients with type 2 diabetes on oral agents, necessitating a reduction in the dose of diabetes medications. Lorcaserin should not be used in individuals with creatinine clearance <30 mL/minute. It is contraindicated during pregnancy. In addition, lorcaserin should not be used with other serotonergic drugs (e.g., selective serotonin reuptake inhibitors,selective serotonin-norepinephrine reuptake inhibitors, bupropion[Wellbutrin], tricyclic antidepressants,and monamine oxidase inhibitors)because of the theoretical potential for serotonin syndrome.
https://www.accessdata.fda.gov
https://medlineplus.gov | [Drug interactions]
Belviq (lorcaserin hydrochloride) may interact with antidepressants, including selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors (MAOIs), triptans, bupropion, dextromethorphan, or St. John's Wort.
| [Precautions]
The precautions of BELVIQ (lorcaserin hydrochloride) tablets:
Serotonin Syndrome or Neuroleptic Malignant Syndrome (NMS)- like Reactions: The safety of coadministration with other serotonergic or antidopaminergic agents has not been established.
Valvular heart disease: If signs or symptoms develop, consider BELVIQ discontinuation and evaluate the patient for possible valvulopathy.
Cognitive Impairment: This may cause disturbances in attention or memory. Caution with the use of hazardous machinery when starting BELVIQ treatment.
Psychiatric Disorders, including euphoria and dissociation: Do not exceed the recommended dose of 10 mg twice daily.
Monitor for depression or suicidal thoughts. Discontinue if symptoms develop.
Use of Antidiabetic Medications: Weight loss may cause hypoglycemia. Monitor blood glucose. BELVIQ has not been studied in patients taking insulin.
Priapism: Patients should seek emergency treatment if an erection lasts >4 hours. Use BELVIQ with caution in patients predisposed to priapism. | [References]
[1] PAUL J. FLETCHER . Characterizing the effects of 5-HT2C receptor ligands on motor activity and feeding behaviour in 5-HT2C receptor knockout mice[J]. Neuropharmacology, 2009, 57 3: Pages 259-267. DOI: 10.1016/j.neuropharm.2009.05.011
[2] HARSHINI NEELAKANTAN. Lorcaserin Suppresses Oxycodone Self-Administration and Relapse Vulnerability in Rats[J]. ACS Chemical Neuroscience, 2017, 8 5: 1065-1073. DOI: 10.1021/acschemneuro.6b00413 |
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