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BMS3052 > 30. Anti-Obesity & T2 Diabetes Therapies > Flashcards

30. Anti-Obesity & T2 Diabetes Therapies Flashcards

1
Q

Define

Laproscopic sleeve gastrectomy (LSG)

A

a weight loss procedure where about 75% of the stomach is removed leaving a narrow gastric “tube” or “sleeve”

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2
Q

Define

Sulfonylureas

A

a group of medicines used to treat type 2 diabetes. They act by increasing insulin release from the beta cells in the pancreas.

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3
Q

Define

Orlistat

A

a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake

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4
Q

Define

Lorcaserin

A

a weight-loss drug developed by Arena Pharmaceuticals. It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the hypothalamus, which is known to control appetite

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5
Q

Define

Contrave

A

a combination (naltrexone/bupropion) medication for chronic weight management. It is for people with overweight and weight-related complications or obesity. It is meant to be used together with a lifestyle therapy regimen involving a reduced calorie diet and increased physical activity

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6
Q

Define

Laproscopic adjustable gastric band (LAGB)

A

a type of weight-loss surger where an inflatable silicone device placed around the top portion of the stomach to treat obesity, intended to decrease food consumption

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7
Q

Define

Incretin

A

a group of metabolic hormones that stimulate a decrease in blood glucose levels

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8
Q

Define

GLP-1 receptor agonists

A

a type of incretin-based medicine for type 2 diabetes. This type of medicine is based on the action of hormones called incretins, which help control how the pancreas works

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9
Q

Define

Bariatric surgery

A

surgery that affects your stomach and how you digest food. It’s designed to make your stomach much smaller, which causes you to feel full after eating only a small amount of food

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10
Q

Define

Metformin

A

marketed under the trade name Glucophage among others, is the first-line medication for the treatment of type 2 diabetes, particularly in people who are overweight. It is also used in the treatment of polycystic ovary syndrome. It is not associated with weight gain.

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11
Q

Definition

a weight loss procedure where about 75% of the stomach is removed leaving a narrow gastric “tube” or “sleeve”

A

Laproscopic sleeve gastrectomy (LSG)

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12
Q

Definition

a group of medicines used to treat type 2 diabetes. They act by increasing insulin release from the beta cells in the pancreas.

A

Sulfonylureas

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13
Q

Definition

a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake

A

Orlistat

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14
Q

Definition

a weight-loss drug developed by Arena Pharmaceuticals. It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the hypothalamus, which is known to control appetite

A

Lorcaserin

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15
Q

Definition

a combination (naltrexone/bupropion) medication for chronic weight management. It is for people with overweight and weight-related complications or obesity. It is meant to be used together with a lifestyle therapy regimen involving a reduced calorie diet and increased physical activity

A

Contrave

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16
Q

Definition

a type of weight-loss surger where an inflatable silicone device placed around the top portion of the stomach to treat obesity, intended to decrease food consumption

A

Laproscopic adjustable gastric band (LAGB)

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17
Q

Definition

a group of metabolic hormones that stimulate a decrease in blood glucose levels

A

Incretin

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18
Q

Definition

a type of incretin-based medicine for type 2 diabetes. This type of medicine is based on the action of hormones called incretins, which help control how the pancreas works

A

GLP-1 receptor agonists

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19
Q

Definition

surgery that affects your stomach and how you digest food. It’s designed to make your stomach much smaller, which causes you to feel full after eating only a small amount of food

A

Bariatric surgery

How well did you know this?
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20
Q

Definition

marketed under the trade name Glucophage among others, is the first-line medication for the treatment of type 2 diabetes, particularly in people who are overweight. It is also used in the treatment of polycystic ovary syndrome. It is not associated with weight gain.

A

Metformin

21
Q

What are the complications of diabetes?

A

Macrovascular disease (heart attack, stroke, angina etc)

Microvascular disease (diabetic retinopathy, end-stage renal disease, neuropathy etc.)

22
Q

What causes the complications seen in diabetes?

A

Increased glucose levels cause an increase in glycosylation

23
Q

What is the most common cause of blindness in industrialised countries?

A

Diabetic retinopathy

24
Q

What percentage of diabetics have neuropathy?

A

50%

25
Q

What is the first-line treatment for diabetes?

A

Changing lifestyle habits (diet and exercise)

26
Q

What therapies are used for diabetes?

A
  • Lifestyle (diet & exercise)
  • Metformin (e.g. Glucophage, Glumetza)
  • Sulfonyureas (e.g. Diabeta, Glucotrol)
  • GLP-1 receptor agonists (e.g. Exenedin/ Liraglutide)
  • DPP-4 inhibitors (e.g. Januvia, Onglyza)
  • Thiazolidinediones (TZDs; e.g. Avandia, Actos)
  • SGLT2 inhibitors new (e.g. Ivokana, Farxiga)
  • Insulin
  • Bariatric surgery
27
Q

What is the first-line pharamcological treatment for diabetes?

A

Metformin

28
Q

How does Metformin treat diabetes?

A

Prevents the progression of impaired glucose tolerance to T2DM by mimicing insulin

Increases levels of AMPK which allows GLUT4 translocation

29
Q

How does Metformin act to improve glucose metabolism in the liver and skeletal muscle?

A
30
Q

Why are Sulfonylureas no longer the first-line treatment for diabetes?

A

Complications include:

  • May induce hypoglycemia as a result of excess insulin production and release (high dose, fasting).
  • Weight gain.
  • Can’t be used in pregnancy (may cause birth defects).
  • Can’t be used in renal / liver failure due to high risks of hypoglcemia.
31
Q

Why are Sulfonylureas not effective in T1D?

A

It acts to increase levels of insulin but insulin cannot be produced in T1D

32
Q

What is the mechanism of sulfonylurea action?

A

Sulfonylureas block ATP-sensitive potassium channels causes K+ to acculmulate in the cell.

This causes cell depolarisation through calcium influx

Increased calcium levels cause insulin to be released from pancreatic beta cells

33
Q

Where was GLP-1 receptor agonists originally found?

A

Saliva of the Gila monster

34
Q

What are GLP-1 receptor agonists?

A

Incretin mimetics

The cause an increase in the amount of insulin released from the beta cells, even before glucose is is elevated

Works within 10 minutes of administration

35
Q

What does the GLP-1 receptor do?

A

Inhibits food intake via GLP1-R

GLP-1 act directly at POMC neurons

Indirectly inhibits NPY/AGRP neurons via GABA

36
Q

What are the new generation drug development strategies for diabetes?

A

Monotherapies

Combination Therapy

Personalised Medicine

Targeted Therapy

37
Q

Which type of new gen drug does not act in the brain?

A

Orlistat (lipase inhibitor)

38
Q

Where do the new generation drugs (Orlistat, Contrave, Liraglutide, Lorcaserin and Qsymia) act to treat diabetes?

A
  • Lipase inhibitor
    • Orlistat
  • Predominant action via the melanocortin pathway
    • Contrave
    • Liraglutide
    • Lorcaserin
  • Wise-spectrum pharmacology acts at the brain
    • Qsymia
39
Q

What is the mode of action of Orlistat and what are the side-effects?

A

Inhibits lipase molecules preventing the breakdown and absorption of fats

Side effects include include cramping, gas, diarrhea, anal leakage and oily underwear stains

40
Q

What is Lorcaserin and how does it treat diabetes?

A

Lorcaserin is a monotherapy that acts as a serotonin agonist selectively activates POMC neurons by targeting the 5-HT 2CR receptor specificlly

41
Q

What two drugs does contrave include?

A

Bupropion

Naltrexone

42
Q

How do the two contrave drugs (Naltrexone and Bupropion) cause synergistic effects?

A

Bupropion stimulates POMC neurons to release α-MSH

Naltrexone prevents the β-endorphin mediated POMC autoregulation

43
Q

How are POMC cells autoregulated?

A

POMC cells produce both α-MSH and β-endorphins. The endorphins act on self receptors to repress activity

44
Q

What is the only effect mechanims of long-term weight loss?

A

Bariatric surgery

45
Q

Why is a Roux-en-Y gastric bypass (RYGB) rarely used in Australia?

A

High rates of malnutrition

46
Q

At what point does the gastric band improve insulin sensitivity?

A

Following the weight loss caused by the surgery

47
Q

What effects does the gastric sleeve have on ghrelin and gut peptides?

A

↓ ghrelin

↑ GLP-1

48
Q

At what points does the gastric sleeve have an effect on insulin sensitivity?

A

Immediately irrespective of weight loss

Rapid nutrient passage into the small intesitine causes increased post-prandial insulin secretion cause glucose uptake

49
Q

List the bariatric surgeries in order of decreasing effectiveness

A
  1. RYGB
  2. Sleeve (LSG)
  3. Band (LAGB)

BMS3052 (26 decks)

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