When are oral hypoglycemics used?
-Control glucose in type 2
What are sulfonylureas MOA?
- Act at pancreas to release insulin
- Decreases insulin resistance
What are the failure rates of sulfonylureas?
- 20% primary
- 10-15% secondary
When should sulfonylureas be avoided?
-With a patient with a sulfa allergy
What are the pharmocokinetics of sulfonylureas?
- Metabolized by liver
- Excreted by kidneys
- Active and inactive metabolites
Sulfonylureas most severe side effect? and what drugs have the greatest risk?
- Hypoglycemia
- One’s w/ longest half life (glyburide and chlorproamide)
can Sulfonylureas cross the placenta?
yes
besides hypoglycemia, What are the other Sulfonylureas side effects?
- Increase CV mortality by inhibiting ischemic preconditioning and less effect on lipids
- GI disturbances (N/V, abnormal LFT’s, cholestasis)
Sulfonylureas should be avoided in patients with liver disease except for what drug?
acetohexamide
Tolbutamide (orinase) tidbits. {1st gen}
- Shortest acting and least potent
- Fewest side effects (less potent metabolites)
Acetohexamide tidbits {1st gen}
- hypoglycemic action from its metabolite
- Uricosuric
Chlorpropamide (diabinese) tidbits {1st gen}
- Longest acting
- Prolonged w/ impaired kidneys
- Disulfiram reactions
- Hyponatremia
Glyburide {2nd gen} tidbits
- Single daily dose for 24 hour effects
- Increase sensitivity to insulin
- Decrease hepatic glucose production
Glipizide {2nd gen} tidbits
- Stimulates insulin secretion for 12 hrs
- increase peripheral glucose uptake
- Suppress hepatic glucose output
- no metabolite
Glimepiride {2nd gen} tidbits
- Stimulate insulin secretion
- decrease hepatic glucose production
Name the 2 meglitinides.
- Repaglinide
- Nateglinide
What do meglitinides do?
-Increase insulin secretion from islet cells
When should meglitinides be administered? and when should they not be administered?
- 15-30 mins before meals
- While fasting
how do meglitinides compare to sulfonylureas?
-Faster onset, shorter duraton
When are meglitinides active?
-When in presence of glucose
How do Alpha-Glucosidase Inhibitors work?
- Decrease carbohydrate digestion
- slows absorption of glucose from GI tract
When are Alpha-Glucosidase Inhibitors useful as monotherapy?
-when postprandial hyperglycemia is problem
Name 2 Alpha-Glucosidase Inhibitors.
- Acarbose
- Miglitol
What are the benefits of Biguanides?
- Inhibit glucose production by liver
- Positive effect on lipids
- Mild weight loss
- Low risk of hypoglycemia
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