Radiance Research AcademyInternational Journal of Current Research and Review2231-21960975-5241EnglishN2022December31Pharmaceutical SciencesRevisiting the Most Successful United States Food and Drug Administration-approved Anti-obesity Drug Sibutramine sulfate: A Comprehensive Pharmacotherapeutic Review English0109Yadav LEnglish Sahu SEnglish Agrawal BEnglish Meshram REnglishYadav L, Post Graduate Student, Department of Pharmaceutical Chemistry, School of Pharmacy, Chouksey College of Engineering, NH-49, Masturi - Jairamnagar Road, Lalkhadan, Bilaspur 495004, Chhattisgarh, Indiahttps://doi.org/10.31782/IJMPS.2022.121201Introduction: Serotonin (5-HT) and noradrenaline (NA) reuptake inhibitor sibutramine work together. Sibutramine primarily affects food intake and energy expenditure by way of its two pharmacologically active metabolites, primary and secondary amines, which cause significant weight loss. In addition to stimulating thermogenesis and enhancing the physiological process of satiety, it can also increase the efferent sympathetic activity to brown fat that is thermochemically active. Aim: Revisiting the Most Successful United States Food and Drug Administration-approved Anti-obesity Drug Sibutramine sulfate. Methodology: For a duration of 10 years, literature is covered. Results: Clinical studies using sibutramine show a dose-related decrease in body weight, with weight loss up to 11% below the baseline that can last up to 18 months with ongoing therapy. Patients assigned to the sibutramine medication continued to lose weight throughout a 1-year period, reaching 15% below baseline, while the patients receiving the placebo treatment had some weight increase when weight loss is induced with a very low-calorie diet (VLCDL). By lowering the biochemical risk factors for obesity, such as plasma triglycerides, total cholesterol, low-density lipoprotein (LDL) cholesterol, glucose, and insulin, and raising HDL cholesterol, sibutramine enhances metabolic fitness. Conclusion: Sibutramine has been shown to be a beneficial treatment for obese people with moderately high blood pressure, and it has even been shown to reduce blood pressure on average as a result of weight reduction. The potential for misuse that is associated with amphetamine is not present with sibutramine, and in investigations evaluating abuse potential, it is identical to placebo. EnglishAnti-obesity drugs, Metabolic fitness, Obesity, Obesity-related disorders, Sibutramine, Pharmacotherapeuticshttp://ijcrr.com/abstract.php?article_id=217http://ijcrr.com/article_html.php?did=2171. World Health Organization. Obesity: Preventing and Managing the Global Epidemic. World Health Organization: Geneva, 1998. 2. Pi-Sunyer FX. Medical hazards of obesity. Ann Int Med 1993; 119: 655–660. 3. Wickelgren I. Obesity: how big a problem? Science 1998; 280: 1364–1357. 4. Williamson DF, Pamuk E, Thun M, Flanders D, Byers T, Heath C. Prospective study of intentional weight loss and mortality in never-smoking US white women aged 40–64 years. Am J Epid 1995; 141: 1128–1141. 5. Hill JO, Peters JC. Environmental contributions to the obesity epidemic. Science 1998; 280: 1371–1374. 6. Woods SC, Seeley RJ, Porte Jr D, Schwartz MW. Signals that regulate food intake and energy homeostasis. Science 1008; 280: 1378–1383. 7. Blackburn L, Miller D, Chan S. Pharmaceutical treatment of obesity. Nurs Clin North Am 1997; 32: 831–848. 8. Heal D, Aspley S, Prow MR, Jackson HC, Martin K, Cheetham SC. Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from D-Amphetamine D-Fenfluramine Int J Obesity 1998; 22 (1): S18–S28. 9. Cheetham SC, Viggers JA, Slater NA, Heal DJ, Buckett WR. [3H]Paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: effect of administration of various antidepressant treatments. Neuropharmacol 1993; 32: 737–743. 10. Cheetham SC, Viggers JA, Butler SA, Prow MR, Heal DJ. [3H]Nisoxetine – a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect od DSP-4 lesioning and antidepressant treatments. Neuropharmacol 1996; 35: 63–70. 11. Heal DJ, Cheetam SC, Prow MR, Martin KF, Buckett WR. A comparison of the effects on central 5-HT function of sibutramine hydrochloride and other weight-modifying agents. Br J Pharmacol 1998; 125: 301–308. 12. Heal DJ, Frankland AT, Gosden J, Hutchins LJ, Prow MR, Luscombe GP, Buckett WR. A comparison of the effects of sibutramine hydrochloride, bupropion and methamphetamine on dopaminergic function: evidence that dopamine is not a pharmacological target for sibutramine. Psychopharmacol 1992; 107: 303–309. 13. Carruba MO, Picotti GB, Zambotti F, Mantegazza P. Effects of mazindol, fenfluramine and chlorimipramine on the 5-hydroxytryptamine uptake and storage mechanism in rat brain: similarities and differences. Naunyn Schmiedeberg’s Arch Pharmacol 1977; 300: 227–232. 14. Carruba MO, Picotti GB, Zambotti F, Mantegazza P. Mazindol and amphetamine as inhibitors of the uptake and releasers of [3H] dopamine by rat striatal synaptosomes. Naunyn Schmiedeberg’s Arch Pharmacol 1977; 298: 1–5. 15. Stock MJ. Sibutramine: a review of the pharmacology of a novel anti-obesity agent Int J Obesity 1997; 21 (1): S25–S29. 16. Buckett WR, Thomas PC, Luscombe GP. The pharmacology of sibutramine hydrochloride (BTS 54 524), a new antidepressant which induces rapid noradrenergic down–regulation. Prog Neuropsychopharmacol Biol Psych 1988; 12: 575–584. 17. Gundlah C, Martin KF, Heal DJ, Auerbach SB. In vivo criteria to differentiate monoamine reuptake inhibitors from releasing agents: sibutramine is a reuptake inhibitor. J Pharmacol Exp Ther 1997; 283: 581–591. 18. Fantino M. Decrease of food intake and weight loss induced by sibutramine in the rat. Obesity Res 1995; 3 (4): 1995. 19. Stricker-Krongrad A, Burlet C, Souquet AM, Courcier A. Sibutramine effects on feeding behaviour: a dose-dependence and microstructural analysis Obesity Res 1995; 3 (4): 631S. 20. Stricker-Krongrad A, Souquet AM, Burlet C. Effects of sibutramine on feeding behaviour in obese and lean Zucker rats. Int J Obesity 1995; 19 (2): P399. 21. Stricker-Krongrad A, Souquet AM, Burlet C. Effects of sibutramine on feeding behaviour in dietary-induced obesity: a role of dietary components Int J Obesity 1995; 19 (2): P398. 22. Rolls BJ, Shide DJ, Thorwart ML, Ulbrecht JS. Sibutramine reduces food intake in non-dieting women with obesity. Obesity Res 1998; 6: 1–11. 23. Halford JCG, Wanninayake SC, Blundell JE. Behavioral satiety sequence (BSS) for the diagnosis of drug action on food intake. Pharmacol Biochem Behav 1998; 61: 159–168. 24. Jackson HC, Bearham MC, Hutchins LJ, Mazurkiewicz SE, Needham AM, Heal D. Investigation of the mechanisms underlying the hypophagic effects of the 5-HT and noradrenaline reuptake inhibitor, sibutramine, in th