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PHARM 233 > Obesity > Flashcards

Obesity Flashcards

1
Q

Non-Pharmacological Treatments of Obesity

A

Exercise

Diet
- Calorie Restrictions
- Ketogenic Diet

Surgical/Medical Devices
- Gastric Bypass

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2
Q

NPY Neurons

A

Oxygenic

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3
Q

AgRP Neurons

A

Oxygenic

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4
Q

POMC Neurons

A

Anorexigenic

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5
Q

CART Neurons

A

Anorexigenic

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6
Q

Oxygenic

A
  • Promote Food Intake
  • Decrease Energy Expenditure
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7
Q

Anorexigenic

A
  • Inhibit Food Intake
  • Increase Energy Expenditure
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8
Q

POMC/CART
- Leptin

A

Leptin stimulates POMC/CART
- Increases Energy Expenditure
- Decreases Feeding

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9
Q

POMC/CART
- GLP-1

A

GLP-1 stimulates POMC/CART
- Increases Energy Expenditure
- Decreases Feeding

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10
Q

POMC/CART
- Insulin

A

Insulin stimulates POMC/CART
- Increases Energy Expenditure
- Decreases Feeding

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11
Q

POMC/CART
- 5-HT

A

5-HT stimulates POMC/CART
- Increases Energy Expenditure
- Decreases Feeding

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12
Q

POMC/CART
- Opioids

A

Opioids inhibits
POMC/CART
- Decreases Energy Expenditure
- Increases Feeding

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13
Q

POMC/CART
- NPY

A

NPY inhibits POMC/CART
- Decreases Energy Expenditure
- Increases Feeding

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14
Q

POMC/CART
- Orexin

A

Orexin inhibits
POMC/CART
- Decreases Energy Expenditure
- Increases Feeding

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15
Q

Leptin
- MOA

A

Adipokine
- Peptide Hormone from Adipose Tissue
- Doesn’t treat obesity, decreases appetite, only really works on people with Leptin deficiency

Acts on Leptin Receptors in the Hypothalamus
- Reduces AMPK Signals
–> Less Protein Kinase leading to suppression of appetite

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16
Q

AMPK Signaling

A

High AMPK Signals
- Happens when Low Energy/Hungry
- Increases Appetite

Low AMPK Signals
- Happens when High Energy/Well Fed
- Decrease Appetite

17
Q

Liraglutide
- MOA
- Adverse

A

GLP-1R Agonist
- GPCR (Gs)

Activates GLP-1R in the Hypothalamus
- Increases cAMP
–> Reduced appetite

Adverse:
- Increases Heart Rate
- Pancreatitis

18
Q

Liraglutide
- Dose

A

1.8 mg for Type 2 Diabetes
3.0 mg for Obesity

19
Q

Semaglutide
- MOA
- Adverse

A

Newer Treatment
GLP-1R Agonist
- GPCR (Gs)

Activates GLP-1R in the Hypothalamus
- Increases cAMP
–> Reduced appetite

Adverse:
- Increases Heart Rate
- Pancreatitis

20
Q

Semaglutide
- Dose

A

1.0 mg once weekly for type 2 diabetes
2.4 mg once weekly for obesity

21
Q

Liraglutide/Semaglutide
- Kinetic

A

Kinetic:
- Acylation prolongs half life, allows it to bind to albumin

22
Q

Orlistat
- MOA
- Adverse

A

LIpase Inhibitor
- Targets serine residues on active sites of gastric and pancreatic lipases
–> Reversibly inhibits enzymatic activity of lipases

Lipases can no longer break down fat meaning fat can not be absorbed
- Only therapy that functions peripherally and does not centrally act for diabetes

Adverse:
- Flatulence/Fecal Incontinence
- Intestinal Borborygmic
- Oily Spotting

23
Q

Orlistat
- Kinetic

A

Kinetic
- Primarily excreted in the feces (~97%) with minimal metabolism (~83% unchanged)
- Half-life of 1-2 hours

24
Q

Lorcaserin
- MOA
- Adverse

A

Selective 5-HT2C Receptor Agonist
- Increases POMC expression in Hypothalamus
–> Increases satiety (fullness)

Adverse:
Valvular Heart Disease

25
Q

Phentermine/Topiramate
- MOA
- Dose
- Adverse

A

Phentermine: Sympathomimetic Amine
- Amine Receptor Agonist

Topiramate: Anticonvulsant Agent
- Acts on Na+/Ca2+ –> Inhibits Carbonic Anhydrase

Dose:
3.75x / 23y

Adverse:
- Paresthesia (Tingling)
- Insomnia
- Heart Rate Elevation
–> Do not take with Monoamine Oxidase Inhibitors
- Teratogenic

Graduated downtitration over 3-5 days due to seizure risk with immediate withdrawal

26
Q

Topiramate

A

Topiramate: Anticonvulsant Agent
- Acts on Na+/Ca2+ –> Inhibits Carbonic Anhydrase

Monotherapy can decrease appetite in binge eating

Combination Therapy with Phentermine
- Reduces Body Weight

27
Q

Bupropion/Naltrexone
- MOA
- Dose
- Adverse

A

Bupropion: NA/DA Reuptake Inhibitor
- Treats depression
- Metabolite (Hydroxybupropion) can antagonize nicotinic acetylcholine receptors

Naltrexone: Competitive Opioid Receptor Antagonist
- Mu and K Opioid Receptor Antagonist

Together they modify the reward pathway to reduce appetite

Dose:
Week 1: 8 mg / 90 mg
Week 2: 16 mg / 180 mg
Week 3: 24 mg / 270 mg
Week 4: 32 mg / 360 mg

Adverse:
- Increased Heart Rate and Blood Pressure

28
Q

Tirzepatide

A

Unimolecular Co-Agonist
- GLP-1 Receptor Agonist
- GIP Receptor Agonist

Greater weight loss than just a mono GLP-1 agonist

29
Q

Retatrutide

A

Triple Agonist
- GLP-1 Receptor Agonist
- GIP Receptor Agonist
- Glucagon Receptor Agonist

Makes co-agonist better
Glucagon increases energy expenditure

30
Q

Picking a suitable drug for obesity

A

If 5% weight loss is not achieved in first 3-4 months change medications (Unless risk factors show improvement)

PHARM 233 (10 decks)

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