synthetic analogs + incretin mimetics

Question 1

synthetic amylin analog: (drug name)

Answer 1

1. pramlintide (used for DM type 1 & 2)

Question 2

incretin mimetics: (GLP-1 agonists) (drug names)

Answer 2

SHORT-acting:

1. exenatide
2. lixisenatide

LONG-acting:

1. liraglutide
2. albiglutide
3. dulaglutide
4. exenatide-LAR

Question 3

pramlintide → mechanism of action:

Answer 3

1. delays gastric emptying
2. ↓ postprandial glucagon secretion → improves satiety
3. ↓ glucagon
4. ↓ gastric emptying
5. ↑ anorectic
6. ↑ energy expenditure
7. ↑ satiety
8. ↑ weight loss
9. ↓ glucose

Question 4

pramlintide → pharmacokinetics:

Answer 4

1. SC admin.

Question 5

GLP-1 agonists → pharmacokinetics:

Answer 5

1. SC admin.
2. exenatide → 2x/day
3. lixisenatide → 1x/day

Question 6

pramlintide → indications:

Answer 6

1. used as adjunct to mealtime insulin in DM1 & 2
2. injected SC → immediately prior to meals
3. when initiated, mealtime dose of insulin should be ↓50% → avoid severe hypoglycemia

Question 7

pramlintide → indications:

Answer 7

1. used as adjunct to mealtime insulin in DM1 & 2
2. injected SC → immediately prior to meals
3. when initiated, mealtime dose of insulin should be ↓50% → avoid severe hypoglycemia

Question 8

GLP-1 agonists → indication:

Answer 8

in DM2 → reduced incretin effect

incretin is resp. for 60-70% of postprandial insulin secretion

Question 9

pramlintide → CONTRAindications:

Answer 9

1. diabetic gastroparesis
2. cresol hypersensitivity
3. hypoglycemic unawareness

Question 10

GLP-1 agonists → CONTRAindication:

Answer 10

exenatide → avoid in renal impairment

Question 11

pramlintide → side effects:

Answer 11

1. nausea
2. vomiting
3. anorexia
4. abdominal pain
5. fatigue
6. dizziness
7. headache
8. hypoglycemia → in combination with insulin

Question 12

GLP-1 agonists → side effects:

Answer 12

1. nausea
2. vomiting
3. diarrhea
4. constipation
5. heart rate acceleration → tachycardia
6. pancreatitis

Question 13

mechanism of action → SHORT-acting GLP-1 agonists:

Answer 13

1. inhibit gastric motility → reducing transpyloric flow
2. delayed intestinal glucose absorption
3. reduction in postprandial insulin secretion
4. appetite suppression & nausea
5. direct effects on CNS & glucagon secretion

Question 14

mechanism of action → LONG-acting GLP-1 agonists:

Answer 14

1. act directly on the pancreas → stimulate insulin secretion
2. suppress glucagon secretion via paracrine release of somatostatin
3. through actions on the CNS → reduced appetite & might induce nausea