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Lorcaserin, A Potential Anti-obesity Drug Essay Example

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Lorcaserin, A Potential Anti-obesity Drug

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Lorcaserin, A Potential Anti-obesity Drug. Activated, like in other anti-obesity drugs which were non selective 5HT receptor agonist.GCPR’s is a large family of protein receptors that bind with extracellular ligands and promote second messenger production which is POMC pro-opiomelanocortin, if 5HT2C is activated in CNS, and initiate intracellular events, which is the suppression of appetite.Lorcaserin (formerly APD356) has a two ringed structure with high and selective affinity for 5HT2C receptor. It has low molecular weight, nonpolymer structure that alters biotargets function. Chemically it is [1R]-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine.15 to 100 times more selective for 5HT2c then 5HT2a and 5HT2b.Lorcaserin undergoes rapid GIT absorption (almost 90%) and achieve maximum blood concentration in 0.

Maximum brain exposure in 1hr, elimination half life is from blood and brain is 4-6 hrs. Lorcaserin daily 10mg will achieve steady state of plasma concentration with in 4 days, with maximum blood concentration up to 30% higher then day 1. Maximum tolerance dose in a single oral dose was found to be 40 mg. half life is 10- 12 hrs. Mainly excreted in urine (92%), in the form of lorcaserin N-carbamoyl glucuronide. Volume of distribution is 252L in 92.5 kg subject. Hepatic disfunction increases the plasma T1/2 by 5-9 hrs. Lorcaserin is mild inhibitor of CYP2D6 so drug interaction with dextromethorphen and desipramine should be noted.Lorcaserin hydrochloride [(1R)-8-chloro-2, 3, 4, 5 tetrahydro-1-methyl-1H-3-benzazepine] is a substituted 3-benzazepine, structurally resembling serotonin synthesized from phenyl ethylamine precursor with chlorine at the 8th-position, yeilding higher selectivity for 5HT2C. Half life of metabolite is 41. Substitution of chlorine, bromine or trifluoromethyl at 8-position, or chlorine at 7-position will lead to better affinity for 5HT2C. Substitution of chlorine at 6 or 9 positions will lead to reduced affinity.Weight loss can cause improvement in the mental health of the obese person by improving attitude and mood thus increasing life’s quality; this is the aim of the use of lorcaserin. Obesity is the major risk factor for health, which mainly affects cardiovascular system, diabetes, stroke, dislipidemia, obstructive sleep apnea, musculoskeletal disorders and cancers. Weight loss improves metabolic, cardiac and vascular functions of the body for example reduction in 5%body weight reduces the risk of diabetes type 2. Blood pressure reduction can easily. Lorcaserin, A Potential Anti-obesity Drug.

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