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Endocrine Block 3 > Obesity drugs > Flashcards

Obesity drugs Flashcards

1
Q

What is the mechanism of action of orlistat?

A

Orlistat alters fat digestion by inhibiting pancreatic lipases, fat is incompletely hydrolyzed and fecal fat excretion is increased

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2
Q

What are the indications for Orlistat?

A
  • Weight loss and maintenance of weight loss in patients with a BMI>30 or BMI >27 + weight related comorbidities
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3
Q

What side effects are associated with Orlistat?

A

GI- borborygmi, flatus (some discharge), cramps, fecal incontinence, oily spotting
- Malabsorption of fat soluble vitamins A, D, E and K
(should supplement these vitamins)
- Oxalate induced kidney injury
- Fat binds to calcium and more free oxalate is delivered to the colon
- Intestinal oxalate absorption and urinary excretion are increased

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4
Q

What are some of the other benefits of Orlistat?

A
  • Modest weight loss (9-10 kg vs. 3 kg in placebo
  • Improves total cholesterol, hypertension, hyperglycemia, hyperlipidemia
  • Less conversion from glucose intolerance to diabetes
  • Better results when added to behavioral change
  • Covered by medicaid
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5
Q

How long does Orlistat work?

A

Weight loss maintained up to 36 months

- After which weight comes back

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6
Q

What is the mechanism of action of lorcaserin?

A
  • Serotonin (5-HT) decreases food intake in humans
  • Selective 5-HT2C receptor agonist
  • 5-HT2C receptor activation of proopiomelanocortin (POMC) neurons => alpha -MSH activation of melanocortin-4 receptor
  • Increases satiety
  • Nonselective agonist also cause weight loss but are associated with cardiac valvular disease (fenfluramine/dexfenfluramine)
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7
Q

What is the indication for lorcaserin?

A
  • Weight loss and maintenance of weight loss in patients with a BMI>30 or BMI >27 + weight related comorbidities
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8
Q

What are the benefits of lorcaserin?

A
  • Mean difference in weight loss between lorcaserin and placebo is 3-4 kg (5.8 kg lorcaserin vs 2.2 kg placebo)
  • Decreases heart rate and BP
  • Decreases in HgA1c and fasting blood sugar
  • However, it is often NOT covered by insurance and is very expensive
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9
Q

What side effects are associated with lorcaserin?

A
  • Upper respiratory infections, headache, dizziness, nasopharyngitis, and nausea
    • most side effects improve with use
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10
Q

What is the mechanism of action of combination phentermine/topiramate (Qsymia)?

A
  • Phentermine
    • Sympathomimetic amine with pharmacologic activity similar to amphetamine
    • Weight management is likely mediated by release of norepinephrine in the hypothalamus, resulting in reduced appetite and decreased food consumption.
  • Topiramate
    • Fructose monosaccharide derivative with sulfamate functionality.
    • The effect on chronic weight management is not known.
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11
Q

What is the most effective medical therapy for weight loss?

A

Phentermine/topiramate combination therapy => 12 weeks (due to tolerance)

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12
Q

What are the major side effects of phentermine/topiramate?

A
  • Paresthesias, Dry mouth, Constipation, Dysgeusia, Insomnia
  • Pregnancy category X, Topiramate-teratogenic-oral cleft defects
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13
Q

What is the mechanism of Naltrexone-Bupropion combination therapy (Contrave) ?

A

Bupropion

  • Dopamine/noradrenaline reuptake inhibitor
    • Stimulates POMC neurons in the arcuate nucleus which release a-MSH and b-endorphin.
    • A-MSH acts on MC4 receptors and decrease appetite and increase energy expenditure

Naltrexone

  • Opioid receptor antagonist.
    • B-endorphin is an auto antagonist of POMC pathway and causes increase in food intake in rodents.
    • Blocking the opioid receptor decreases the effect of endogenous b-endorphin

*makes food less rewarding

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14
Q

What is the indication for naltrexone-bupropion?

A

Indication: weight loss and maintenance of weight loss in patients with a BMI>30 or BMI >27 + weight related comorbidities

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15
Q

What are the major side effects of naltrexone-bupropion?

A
  • Nausea 30% => main reason for stopping treatment
  • Headache, constipation, dizziness, vomiting and dry mouth
  • Transient increase BP 1.5 mmHg followed by decrease 1 mmHg
  • Cautious of suicidal ideation in young adults (18-24 yrs.)
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16
Q

What are the contraindications for naltrexone-bupropion?

A
  • Contraindicated in uncontrolled hypertension, seizures, eating disorders, chronic opioid use, MAOI’s
17
Q

What is the mechanism of action of liraglutide?

A

Long-acting GLP-1 analog; subcutaneous injection

  • Slows gastric emptying
  • Increases insulin release
  • Decreases hepatic glucagon production
18
Q

What is the indication for liraglutide?

A

Indication: weight loss and maintenance of weight loss in patients with a BMI>30 or BMI >27 + weight related comorbidities

19
Q

What are the benefits of liraglutide?

A
  • 4.8-7.2 kg (2.8 kg more than placebo)
  • Sustained mean weight loss 7.6 kg at 2 yrs.
  • Decreases blood pressure
  • Improves blood sugar control
20
Q

What are the major side effects associated with liraglutide?

A

Nausea 37-47%
Vomiting 12-14%
Pancreatitis
* avoid in patients with thyroid tumors

21
Q

What is the most common type of bariatric surgery?

A

Roux-en-Y Gastric Bypass- 80%

- Malabsorptive procedure

22
Q

What is the result/benefit of bariatric surgery?

A

5% of US population meets criteria for bariatric surgery, 1/3 of patients undergoing surgery have a BMI>50 => after surgery BMI>35
- Significant resolution or improvement of type 2 diabetes mellitus, hypertension, dyslipidemia and sleep apnea seen.

23
Q

What are the types of bariatric surgery?

A

1) Restrictive procedures
- Vertical banded gastroplasty
- Laparoscopic adjustable gastric banding)
2) Malabsorptive procedures
- Biliopancreatic diversion with duodenal switch
- Roux-en-Y gastric bypass

24
Q

Describe the mechanism of a restrictive procedure.

A

A small pouch restricts the volume of food intake, causing early satiety while allowing the normal absorption of fat, protein, and carbohydrates.

25
Q

Describe the mechanism of a malabsorptive procedure.

A

Through surgical alteration of the intestinal tract, food bypasses the portions of the small intestine where normal digestion and absorption occur.

26
Q

What is the most effective treatment for obesity?

A

Bariatric surgery

- significant weight loss maintained for 15 years

27
Q

What are the FDA requirements for anti-obesity drugs?

A
  • Decrease weight ≥ 5% in 12 months.
    OR 35% of participants must lose > 5% (if double the placebo and has achieved statistical significance).
  • Evidence needed for improvements in comorbidities e.g. lipids, glycaemia, blood pressure etc.
  • Weight loss should be predominantly from fat
  • Large focus is on potential for abuse, psychiatric side effects, drug withdrawal issues, fetal development and cardiovascular safety.
28
Q

Which gene codes for leptin?

A

The OB gene was one of the first of many genes found linked to obesity
- It codes for leptin which is expressed in adipose.

29
Q

What is leptin and what is its role in obesity?

A
  • Leptin is a hormone which can decrease appetite and stimulate metabolism.
  • Paradoxically many obese patients have high levels of leptin
30
Q

Where do long and short term signals for satiety come from?

A

Long term => leptin and adiponectin (adipose tissue)

Short term => PP, insulin, and amylin (pancreas); Ghrelin (GI tract)

31
Q

What are the criteria for anti-obesity medication usage?

A 
- BMI ≥ 30 kg/m2 
OR
- BMI ≥ 27 kg/m2 and at least 1 concomitant obesity-related risk factor or disease:
    - Type 2 diabetes
    - Heart disease
   - Atherosclerosis
   - Sleep apnea
   - Excessive waist circumference
   - Dyslipidemia
32
Q

Anti-obesity pharmacotherapy must be combined with what other therapy?

A

Anti-obesity pharmacotherapy must be combined with a weight management program => reduced calorie diet and increased physical activity

33
Q

What is considered an “excellent” response to anti-obesity pharmacotherapy?

A

An excellent response is 10-15% total body weight lost over 12 months

Endocrine Block 3 (5 decks)

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