Term
| How do sulfonylureas work? |
|
Definition
(only effective if pancreas secretes >30% of normal insulin)
1. Bind to receptor near K+ channel and close it
2. decreased K+ efflux
3. depolarization
4. Ca channels open (Ca influx)
5. insulin is secreted |
|
|
Term
| What are the AE of sulfonylureas? |
|
Definition
*hypoglycemia (especially w/elderly)
GI Sxs
muscle weakness
mental confusion |
|
|
Term
| What are the first generation sulfonylureas? |
|
Definition
tolbutamide (6-12hrs)
tolazamide (10-14hrs)
chlorpropamide (up to 60 hrs) |
|
|
Term
| What are the 2nd generation sulfonylureas and why are they better? |
|
Definition
glyburide
glipizide
glimepiride
(they are 100x more potent--but easier to induce hypoglycemia) |
|
|
Term
| How long do Glyburide, Glipizide, and Glimepiride last? |
|
Definition
|
|
Term
| How does repaglinide/nateglinide work? |
|
Definition
stimulates insulin secretion by closing K+ channels
lasts for 1-3 hrs
take only with a meal (decreases incidence of hypoglycemia) |
|
|
Term
| What is the MOA of Metformin? |
|
Definition
liver: decrease gluconeogensis, ^ gluc uptake
**no hypoglycemia |
|
|
Term
| What are the AEs of Metformin? |
|
Definition
alcoholic or impaired renal fxn: lactic acidosis
metallic taste
GI upset
anorexia |
|
|
Term
|
Definition
| delays absorption: inhibits alpha-glucosidase and thus hydrolysis of dietary disacch and complex carbs |
|
|
Term
| What are the adverse effects of acarbose? |
|
Definition
flatulence
cramps
diarrhea
may reduce absorption of iron |
|
|
Term
Rosiglitazone
Pioglitazone |
|
Definition
decrease insulin resistance: ^ transcription of insulin-responsive genes by binding PPARY-receptor
decrease gluconeogenesis and ^ gluc uptake |
|
|
Term
| What drugs are available in combination w/metformin? |
|
Definition
| glyburide, glipizide, rosiglitazone |
|
|
Term
| What are the adverse effects of rosiglitazone and pioglitazone? |
|
Definition
| weight gain, edema, risk of heart failure |
|
|
Term
|
Definition
potentiate insulin synthesis and release, decrease glucagon production
MOA: inhibit DPP4 (prevents metab of incretin hormones) |
|
|
Term
| What are the AEs of sitagliptan/saxagliptan? |
|
Definition
mild GI upset
hypoglycemia |
|
|
Term
| What drugs decrease insulin resistance? |
|
Definition
rosiglitazone
pioglitazone |
|
|
Term
| What drugs stimulate insulin secretion? |
|
Definition
| sulfonylureas, repaglinide, Sitagliptan/Saxagliptan? |
|
|
Term
| What drug delays glucose absorption? |
|
Definition
|
|
Term
| What drug has the greatest incidence of hypoglycemia? |
|
Definition
|
|
Term
| What drugs do you take with a meal? |
|
Definition
| repaglinide/nateglinide, acarbose |
|
|
Term
| What drug increases glucose uptake? |
|
Definition
|
|
Term
| What is the result of chronic administration of sulfonylureas? |
|
Definition
| decreased glucagon and potentiation of insulin effects |
|
|
Term
|
Definition
injectable, 2x/day (add on to other medications: metformin or sulfonylureas)
for type II
GLP1 receptor agonist: stimulates insulin when glucose is high
delays gastric emptying
blocks glucagon release
AE: nausea |
|
|
Term
|
Definition
injectable analog of amylin
reduces glucagon secretion and modulates post-prandial glucose
Type I: give w/insulin
Type II: give w/insulin, metformin, or sulfonylureas
AE: hypoglycemia & GI distress |
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