Obesity treatments Flashcards

1
Q

how do most people maintain constant body fat and weight

A

homeostatic mechanisms that control energy balance

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2
Q

how does obesity happen if the body should have homeostatic mechanisms that control energy balance

A

disturbance in these mechanisms, genetic influence, food, activity, social and cultural things

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3
Q

what is the current view in obesity causes

A

susceptibility cause by genes, expression determined by environment

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4
Q

what are 2 things that can disturb homeostasis

A
  • types of food (mechanisms respond slower to fat than protein)
  • quantity of food (if previously obese, need less calories to maintain weight than if never been obese)
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5
Q

what are 4 therapeutic strategies for obesity

A
  • modulate fat metabolism/storage (diet exercise)
  • reduce food intake, amplify satiety signals/ block hunger signals
  • block nutrient absorption in intestine
  • increase thermogenesis (increase metabolism, dissipate food energy as heat)
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6
Q

what is sibutramine (generally what does it do to person)

A

a drug that regulates food intake, enhances satiety (appetite suppressant)

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7
Q

what is the mechanism of action of sibutramine

A

inhibits 5-HT, DA and NA uptake at hypothalamic sites that regulate food intake (ARC)

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8
Q

which drug is the SSRI anorexic

A

sibutramine

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9
Q

what are the beneficial effects of sibutramine

A

decrease food intake (ARC), weight loss (thermogenesis!), less plasma TGs, increased HDL

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10
Q

how does sibutramine cause weight loss (diff than decreased food intake)

A

higher energy expenditure through thermogenesis mediated by sympathetic nervous system)

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11
Q

why was sibutramine withdrawn from maker

A

increased BP and HR

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12
Q

what is a similar drug to sibutramine that also got withdrawn from the market

A

lorcaserin

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13
Q

what is the mechanism of action of lorcaserin and what does it cause

A

5-HT2C receptor agonist that suppresses appetite (weight loss too)

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14
Q

what are 2 main drugs that are used to increased thermogenesis

A

phentermine and topiramate

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15
Q

what is phentermine mechanism

A

sympathomimetic by preventing NA uptake, more NA in CNS to enhance satiety and more NA in periphery for thermogenesis

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16
Q

what are 3 side effects of phentermine and why

A

high BP and HR (sympathetic stimulation) and potential for addiction

17
Q

what is topiramte mechanism

A

GABA signalling enhancer, blocks neuronal Na+ channels, activates K+ channels

18
Q

what does topiramate do for obesity

A

it enhances satiety

19
Q

where are 5-HT2C neurons most found

A

in hypothalamic POMC producing neurons

20
Q

what does 5-HT2C activation cause

A

release of alpha-MSH which activates anorexogenic pathways

21
Q

what does alpha-MSH do

A

activates anorexogenic pathways

22
Q

why is lorcaserin slightly safer than some other drugs

A

low affinity for other 5-HT subtypes (like 2B) which have been associated with developing valvular heart diseases

23
Q

what is a main drug that is used to block nutrient absorption

A

orlistat

24
Q

what is the mechanism of orlistat

A

irreversible inhibitor of gastric and pancreatic lipases

25
Q

what are 5 main obesity drugs we gotta know

A

sibutramine, orlistat, topiramate, phentermine, lorcaserin

26
Q

so what does orlistat do to fat taken in diet

A

prevents breakdown of dietary fat, dose related decrease in fat absorption and increase in fat excretion

27
Q

what happens if you take orlistat with low fat/ calorie diet

A

modest weight reduction and lower LDL

28
Q

what is an advantage of orlistat

A

very little is absorbed (97% excreted in feces) so low risk of drug interactions

29
Q

what are 2 main side effects with orlistat

A
  • decreased absorption of fat soluble vitamins

- bad GI symptoms (gas, bloating, rumbles)

30
Q

why would some people argue that orlistat is just aversion therapy

A

because you are scared to eat oily foods or else you soil your pants

31
Q

what are 4 other approaches for drugs in obesity

A
  • leptin analogues
  • PYY analogues
  • AGRP antaognists
  • GLP-1 analogues
32
Q

what is the best obesity drug for limiting drug interactions

A

orlistat