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Antiobesity Drugs PowerPoint Presentation

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Description : Drugs used for obesity with their MOA, side effects and clinical uses

Tags : obesity,anti obesity,antiobesity,body fat,fat,overweight

Published on : May 22, 2022 | Views : 2213 | Downloads : 18

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Slide 1-

ANTI OBESITY DRUGS
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OBESITY Defined as an excess of body fat. Marker for body fat content Body Mass Index. BMI= Weight (in kg) Height (in m2)
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BODY MASS INDEX According to National Institute of Health:
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EPIDEMIOLOGY Obesity “Killer lifestyle disease” According to WHO, In 2016 1.9 billion people were overweight worldwide Of these 650million adults were obese Overall 13% of world’s adult population (11% of men and 15% of women) were obese in 2016
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According to the 2016 WHO statistics 20.8% of the population is overweight and 4.8% is obese
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OBESITY Obesity results expenditure. from greater energy intake than energy 9.3 Cal 1gm fat
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OBESITY Infancy; childhood hyperplastic obesity adipocytes number of Adults Hypertrophic obesity size of adipocytes Extremely obese size and number of adipocytes contains double amount of lipids as a lean person
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Hyperplastic Hypertrophic
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WHAT CAUSES OBESITY????
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OBESITY AND GENETICS 20-25% How genes contribute to obesity??? One/ more abnormality of pathway regulating feeding center Abnormality of energy expenditure and fat storage
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PATHOPHYSIOLOGY
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Neural centers regulating appetite, feeding behavior and energy status: Hypothalamus; the amygdala; nucleus tractus solitarius (NTS). Lateral nuclei hypothalamus feeding center Ventromedial nuclei satiety center
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COMPLICATIONS OF OBESITY
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TREATMENT OF OBESITY
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GOAL: To improve obesity-related comorbid conditions and to reduce the risk of developing future comorbidities. Treatment approaches- Lifestyle modification (meal plan, physical activity and behavioral interventions). Pharmacotherapy. Surgery.
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BMI ≥ 30 kg/m². OR BMI ≥ 27 kg/m²- For patients who have concomitant obesity-related diseases and for whom dietary and physical activity therapy has not been successful. Drug therapy is adjunctive to lifestyle intervention. Indication for Pharmacotherapy
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ANTIOBESITY DRUGS
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Orlistat- pancreatic lipase inhibitor Sibutramine- serotonin-norepinephrine reuptake inhibitor Rimonobant- cannabinoid type-1 receptor antagonist
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Newer drugs approved by FDA Lorcaserin- June 2012 Phentermine & Topiramate ER- July 2012 Naltrexone & Bupropion- Sept 2014 Liraglutide- Dec 2014
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ORLISTAT Reversible inhibitor of lipase- inhibits absorption of dietary fats Empirical formula- C29H53NO5 Molecular weight- 495.7 FDA approved- April 1999
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ORLISTAT- MECHANISM OF ACTION Exerts therapeutic activity- lumen of stomach and small intestine Inactivated enzyme inhibits hydrolysis of dietary fat (TG) to absorbable free fatty acids and monoglycerides. Undigested TG unabsorbed caloric deficit positive effect on weight control. Therapeutic dose- 120 mg TID- fat absorption inhibited by 30%
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Adverse Effects Fatty/oily stool Flatus with discharge Fecal incontinence Increased defecation Abdominal cramps
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SIBUTRAMINE Serotonin-norepinephrine reuptake inhibitor Empiric formula- C17H29Cl2NO Molecular weight- 334.33 FDA approved- November 1997
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SIBUTRAMINE- MOA Inhibits reuptake of serotonin; norepinephrine at hypothalamic sites Increases levels of these substances- enhances satiety Reduction in waist circumference Decrease in plasma TG and VLDL Increase in HDL Dose- 5-15 mg/day
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Adverse Effects Dry mouth Constipation Insomnia Increased BP; Heart rate
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RIMONABANT Cannabinoid type-1 receptor antagonist Developed for smoking cessation; facilitate weight loss Initially used in pts with BMI> 30kg/m2 Frequent adverse effects most notably severe depression risk of suicide this drug is no longer used clinically
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LORCASERIN Serotonin 2C receptor agonist Selectively activates serotonin 2C receptors promotes satiety in brain Indicated as an adjunct to low calorie diet and increased physical activity BMI> 27 kg/m2 associated with weight-related comorbid condition or BMI >30kg/m2
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LORCASERIN Dose- 10 mg twice daily Adverse Effects- Headache, dizziness, fatigue Nausea, dry mouth Constipation Backache Cough Hypoglycemia
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QSYMIA Combination of Phentermine & Topiramate ER. Phentermine mediates release of catecholamine's in hypothalamus reduced appetite; decreased food consumption Topiramate precise mechanism unknown Dose- start 3.75mg/23mg daily for 14 days; increase to 7.5mg/46mg once daily. After 12 weeks, <3% weight loss discontinue
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Adverse Effects Paresthesia Dizziness Insomnia Constipation Dry mouth
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CONTRAVE Naltrexone & Bupropion Schedule for treatment: Week 1 1 tab- morning Week 2 1 tab- morning & evening Week 3 2 tab- morning; 1 tab- evening Week 4 2 tab- morning & evening After 12 weeks, <5% weight loss discontinue
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CONTRAVE- MOA Effect on 2 separate areas of brain Hypothalamus Mesolimbic dopamine circuit Exact neurochemical effects not known
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Adverse Effects Nausea, vomiting Headache, dizziness, insomnia Dry mouth Constipation Has potential to cause suicidal thoughts & behaviors.
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LIRAGLUTIDE Glucagon like peptide 1 receptor agonist. A physiological regulator of appetite; calorie intake GLP-1 receptor- present in several areas of brain regulating appetite. Dose- 3mg subcutaneously
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Hypoglycemia Nausea, vomiting Constipation Dyspepsia Fatigue, Dizziness Pain abdomen Adverse Effects
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AGENTS WITHDRAWN IN THE LAST DECADE Sibutramine (2010) – ↑ Cardiovascular risks. Rimonabant (2008) - Serious psychiatric side effects.
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BARIATRIC SURGERY Most effective long-term treatment for obesity Several approaches used- performed laproscopically Goal- disrupting release of ghrelin and other peptides enhancing satiety
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Complications: Post-operative respiratory problems, wound infection Staple leaks, stomal stenosis, Marginal ulcers and venous thrombosis
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THANK YOU