Lec 10: Antiobesity Drugs Flashcards
(31 cards)
What condition (disease) is improved after weight loss (in women)
PCOS
What hormones are released from adipocytes
Leptin (paired with insulin) Adiponectin - affect insulin sensitivity PAI-1 (haemostasis - form ลิ่มเลือด) Angiotensinogen Pro inflammatory cytokins
What does Beta-3 adrenergic receptor increase?
Lipolysis
Why was Canabinoid-1 receptor antagonist drug, Rimonabant, withdrawn?
Because inhibiting cannabinoid receptors to lose weight also inhibits happiness therefore can cause depression and suicide
1st step of obesity management?
Exercise and dietary control
When is pharmacotherapy applied immediately in obesity patients?
When the patient has a BMI =/> 30 or 27 with obesity related diseases
Bariatric surgery is applied immediately only when patient …..
Has a BMI =/> 40 or 35 with obesity related comorbidities
Mech of action of antiobesity drugs
Reduce energy intake
Alter metabolism
Increase energy expenditure
What are anorexic agents
Appetite suppressants
Appetite suppressants
Phentermine, diethylpropion
Fenfluramine, dexfenfluramine
Sibutramine
All กระตุ้น catecholamine receptors
Thermogenic drugs
Adrenergic drugs
Beta-3 agonists
Thyroxine
Sibutramine
Thermogenesis in BAT
Beta3 receptors activated by cold stress —> cAMP increases and increases PKA —> PGC 1 increases and increase transcription of UCP1 gene —> burn fat for heat synthesis
Orlistat
Orlestra (fat substitute for cooking)
Drugs that decreases absorption of fat
Orlistat
Pancreatic lipase inhibitor
SE: fecal incontinence, fatty stool
Cetilistat
New drug same as orlistat
Anorectic drugs that increases 5-HT functions
Fenfluramine **
Dexfenfluramine, fluoxetine
Sibutramine*
Agents increase catecholamine activities
Phentermine**
Phenylpropanolamine, mazindol, diethylproprion
Bulk preparation
Methylcellulose, sterculia
Expands in stomach to make you full faster, but also makes you hungry faster
E.g. เม็ดแมงลัก
Fen-phen
Fenfluramine (5-HT) and phentermine (catecholamine) —> appetite suppressant
AE: CARDIAC VALVULAR DISEASE & pulmonary hypertension —> withdrawn
Sibutramine (meridia)
SNRI - serotonin norepinephrine reuptake inhibitor
Increases 5HT and NE —> increases satiety, dec hunger
NE stimulate thermogenesis (beta3 stim.)
Treat BMI 30 or 27 with comorbidities
Absolute contraindication in SIBUTRAMINE
MAOI users (antidepressant) —> too much serotonin
Caution: SSRI users
Locaserin
Selective serotonin receptor agonist
Topiramate, zonisamide
Antiseizure agents
Leptin analogues, transporter, receptor promotors
Antiobesity drugs
