Unit 5-Diabetes Flashcards
Metformin
Drug class
Biguanide
Metformin
Mechanism
Activates AMP-kinase and inhibits mitochondrial isoform of glycerophosphate dehydrogenase => decreases hepatic glucose production
Metformin
Uses
First-line therapy in diabetes due to no weight gain or hypoglycemia, reduction in cardiovascular events and mortality
Metformin
Side effects
Lactic acidosis (rare)
GI (diarrhea, abdominal discomfort, N & V), B12 deficiency
Contraindicated in renal impairment; low cost
Glipizide
Drug class
Sulfonylurea
Glipizide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glipizide
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Generally well-tolerated; low cost
Glyburide
Drug class
Sulfonylurea
Glyburide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glyburide
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Long-acting (in general, avoid)
Glimepiride
Drug class
Sulfonylurea
Glimepiride
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Glimepiride
Side effects
Weight gain; hypoglycemia
May blunt myocardial ischemic preconditioning
Generally well-tolerated; low cost
Repaglinide
Drug class
Meglitinide
Repaglinide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Repaglinide
Uses
Short-acting; dose with meals
Generic repaglinide available
Repaglinide
Side effects
Weight gain; hypoglycemia (less than sulfonylureas)
Nateglinide
Drug class
Meglitinide
Nateglinide
Mechanism
Closure of ATP-sensitive K+ channels on β-cell plasma membrane –> stimulation of insulin release
Nateglinide
Uses
Short-acting; dose with meals
Nateglinide
Side effects
Weight gain; hypoglycemia (less than sulfonylureas)
Pioglitazone
Drug class
Thiazolidinedione
Pioglitazone
Mechanism
Binds PPAR-γ, a nuclear transcription factor; increases peripheral insulin sensitivity
Pioglitazone
Uses
No hypoglycemia; increases HDL cholesterol, decreases triglycerides
Pioglitazone
Side effects
Weight gain; edema; heart failure; bone fractures; macular edema
Increased risk of bladder cancer; possible reduction in myocardial infarctions
Generic available
Rosiglitazone
Drug class
Thiazolidinedione
Rosiglitazone
Mechanism
Binds PPAR-γ, a nuclear transcription factor; increases peripheral insulin sensitivity
Rosigitazone
Uses
No hypoglycemia
Rosiglitazone
Side effects
Weight gain; edema; heart failure; bone fractures; possible increase in cardiovascular events
Increased LDL cholesterol
Expensive; contraindicated in heart disease
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Drug class
GLP-1 receptor agonist
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Mechanism
Activates GLP-1 receptor in β-cells in the pancreas and brain; increases insulin secretion and decreases glucagon secretion in a glucose-dependent fashion; slows gastric emptying, increases satiety; can cause weight loss
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Uses
SubQ injection only (exenatide twice daily, extended release once weekly,liraglutide once daily, others once weekly
Exenatide (Byetta, extended release Bydureon); Liraglutide (Victoza); Albiglutide (Tanzeum); Dulaglutide (Trulicity)
Side effects
GI (nausea, vomiting, diarrhea); acute panceatitis
Hypoglycemia (less than sulfonylureas; caution with renal insufficiency; C cell hyperplasia/medullary thyroid tumors in rodents
expensive
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Drug class
DPP-4 inhibitor
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Mechanism
Inhibition of GLP-1 metabolism; increases insulin and decreases glucagon secretion
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Uses
No hypoglycemia, weight neutral
Sitagliptin (Januvia); Alogliptin (Nesina); Saxagliptin (Onglyza); Linagliptin (Tradjenta)
Side effects
Well tolerated; rarely urticaria/angioedema & pancreatitis; arthralgias
Expensive
Canagliflozin (Invokana); Dapaglifloxin (Farxiga); Empaglifloxin (Jardiance)
Drug class
SGLT2 inhibitor