Lorcaserin hydrochloride Chemical Properties

solubility 

Soluble in DMSO > 10 mM

form 

Powder

Stability:

Hygroscopic

Lorcaserin hydrochloride Usage And Synthesis

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-HT_2C agonist approved for chronic weight management since the withdrawal of the 5-HT_2C agonist fenfluramine in 1997 due to rare cases of cardiac valvulopathy. The serotonin receptor 5-HT_2C is found primarily in the hypothalamus and regulates appetite and feeding behavior. Safety issues with fenfluramine were associated with poor selectivity for 5-HT_2C versus 5HT_2A and 5HT_2B. Ring constraint afforded by the benzazepine in lorcaserin improved selectivity for 5HT_2C by over 2 log units.

Description

Lorcaserin (hydrochloride) (CRM) (Item No. 19247) is a certified reference material categorized as an anorectic. It also decreases oxycodone intake and has positive effects on self-administration and relapse vulnerability in the rat. Lorcaserin is regulated as a Schedule IV compound in the United States. This product is intended for research and forensic applications.

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.

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