Lorcaserin HCL powder (846589-98-8)

Lorcaserin HCL powder is a selective serotonin 2C agonist labeled for chronic weight managementin adults who are obese (body mass index [BMI] ≥ 30 kg per m2) or who are overweight (BMI ≥ 27 kg per m2) with at least one weight-related comorbidity. Similar to other weight-loss medications, Lorcaserin HCL should be used in conjunction with diet and exercise. It suppresses appetite by activating the 5-HT2C receptors, which are types of serotonin receptors in a region of the brain (hypothalamus) that controls appetite. Lorcaserinaffects chemical signals in the brain that control appetite. Lorcaserin HCL works by helping you feel full with smaller meals. it is used together with diet and exercise to treat obesity.

Lorcaserin HCL powder is sometimes used to treat obesity that may be related to diabetes, highcholesterol, or high blood pressure. However, Lorcaserin HCL will not treat any underlyinghealth condition (such as heart disease, diabetes, high blood pressure).

Obesity is the second most common preventable cause of death, second only to tobaccouse. Evidence suggests that weight reduction substantially lowers the risk of related comorbidities and fosters their therapeutic. In June 2012, the US FDA approved lorcaserin forchronic 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. It plays a big role in helping people lose weight in health and safety.

Lorcaserin hydrochloride powder works by controlling appetite — specifically by activatingbrain receptors for serotonin, a neurotransmitter that triggers feelings of satiety and satisfaction. Intake of food is controlled by satiety center, located in ventromedial nucleus of hypothalamus and hunger center present in lateral hypothalamus. Various inputs from higher centers and gastrointestinal tracts converge in arcuate nucleus, where two types of neurons controlling food intake is present. Firstly, food intake stimulatory group producing agouti-related protein and neuropeptide Y; and secondly, food intake inhibitory group containing cocaine and amphetamine regulated transcript (CART) and pro-opiomelanocortin (POMC) neurons. POMC contains 5-HT 2C receptors, which when activated releases alpha-melanocyte-stimulating hormone (alfa-MSH).Both inhibitory and stimulatory neurons further projects paraventricular nucleus in the hypothalamus.Paraventricular nucleus contains melanocyte 4 receptors (MC4R) that inhibits appetiteIn therapeutic doses lorcaserin acts as a selective 5-HT 2C agonist on POMC neurons, which in turn causes release of alfa MSH. Further alfa MSH acts on MC4R in paraventricular nucleus in the hypothalamus, leading to decrease in appetite. In supratherapeutic doses, lorcaserin also acts on 5-HT 2B and 5-HT 2A receptors.

♦Treat obesity.

♦Treat obesity that may be related to diabetes, high cholesterol, or high blood pressure.

Initial studies demonstrate that lorcaserin HCL powder is safe when taken at the recommended dosage of 10 mg twice daily. Because serotonin agonists such as lorcaserin can cause serotonin syndrome, the manufacturer recommends that patients taking other serotonergic drugs such as antidepressants avoid coadministration of lorcaserin. Valvulopathy, a risk with previous weight-loss drugs, has notbeen demonstrated with lorcaserin; however, the medication has not beenevaluated in patients with significant valvulopathy or congestive heart failure. Itslong-term effects are unclear because it has not been studied for a period longer than two years.

Psychiatric symptoms including euphoria, hallucination, and dissociation rarely occur with recommended dosages, but these have occurred in 19% of patients taking 40 to 60 mg daily.1 Physical dependence has not been observed with lorcaserin HCL, although psychic dependence is possible with higher dosagesused to induce euphoria. Lorcaserin HCL does not increase suicidal thoughts or actions, and does not cause mood changes or trouble sleeping when used as recommended.

Prolactin levels may be increased in some patients taking lorcaserin HCL, althoughgalactorrhea and gynecomastia were not reported in a premarketing study of 6,888 patients. Hypoglycemia is more common in patients with type 2 diabetes mellitus. Lorcaserin HCL is a pregnancy category X drug because of the risk of fetal harm from weight loss and therisk of hypoglycemia.

COA

• Pi-Sunyer X, Shanahan W, Fain R, Ma T, Garvey WT. Impact of lorcaserin on glycemiccontrol in overweight and obese patients with type 2 diabetes: analysis of week 52 responders and nonresponders. Postgrad Med. 2016 Jul 18:1-7. [Epub ahead of print] PubMedPMID: 27389084.
• Farr OM, Upadhyay J, Gavrieli A, Camp M, Spyrou N, Kaye H, Mathew H, Vamvini M,Koniaris A, Kilim H, Srnka A, Migdal A, Mantzoros CS. Lorcaserin administration decreasesactivation of brain centers in response to food cues and these emotion- and salience-related changes correlate with weight loss effects: a four week long randomized, placebo-controlled, double-blinded clinical trial. Diabetes. 2016 Jul 6. pii: db160635. [Epub ahead ofprint] PubMed PMID: 27385157.
• Higgins GA, Silenieks LB, Altherr EB, MacMillan C, Fletcher PJ, Pratt WE. Lorcaserin and CP-809101 reduce motor impulsivity and reinstatement of food seeking behavior in male rats: Implications for understanding the anti-obesity property of 5-HT2C receptor agonists. Psychopharmacology (Berl). 2016 Jul;233(14):2841-56. doi: 10.1007/s00213-016-4329-3. Epub 2016 May 30. PubMed PMID: 27241709.
• Nguyen CT, Zhou S, Shanahan W, Fain R. Lorcaserin in Obese and Overweight PatientsTaking Prohibited Serotonergic Agents: A Retrospective Analysis. Clin Ther. 2016 Jun;38(6):1498-509. doi: 10.1016/j.clinthera.2016.04.004. Epub 2016 May 17. PubMed PMID: 27206567.