Oral Hypoglycemics Flashcards
Which class of oral hypoglycemic medications has the highest risk of hypoglycemia?
Sulfonylureas
Esp if used with insulin
MOA of sulfonylureas?
Act at pancreatice beta cells to stimulate release of insulin
What are examples of sulfonylureas?
- Glyburide ( Diabeta, Micronase)
- Glipizide (Glucotrol)
- Glimepiride (Amaryl).
1st Generation:
- Tolbutamide (Orinase)
- Acetehexamide
- Chlorpropamide (Diabinese)
Sulfonylureas should be avoided in patients with what allergy?
Sulfa drugs
Where are sulfonylureas metabolized?
Liver and excreted by kidneys
Which patients are at an even higher risk of hypoglycemia with sulfonylureas?
Patients with renal failure
Do sulfonylureas cross the placenta?
May cross and may cause fetal hypoglycemia
What is duration of action of sulfonylureas?
Up to seven days and patients may require prolonged infusions of glucose-containing solutions
Side effects of sulfonylureas?
- (most common) Hypoglycemia
- Weight gain
- GI disturbances (PONV can be common)
What are contraindications/precautions with sulfonylureas?
- Sulfa drug allergy
- Patients with hypoglycemia unawareness
- Poor renal function
- Liver disease (except acetohexamide)
T/F: Sulfonylureas have metabolites that can be of concern with renal patients; however, Glipizide is safe ?
True; Glipizide is safe down to CrCl of 10 and has NO active metabolite
Which class of hypoglycemic drugs can cause severe GI upset and is intolerable for many patients?
Alpha-Glucosidase inhibitors
What are examples of Alpha Glucosidase Inhibitors?
- acarbose (Precose)
- miglitol (Glyset)
MOA of Alpha-Glucosidase Inhibitors?
Decrease intestinal hydrolysis of complex carbs
Which patients should Alpha-glucosidase inhibitors be avoided in?
IBS and bowel obstructions
T/F: Meglitinides have mostly replaced sulfonylureas as hypoglycemic agents?
False; Meglitinides have mostly been replaced by sulfonylureas
MOA of Meglitinides?
Increase insulin secretion from islet cells like sulfonylureas
What are examples of Meglitinides?
- repaglinide (Prandin)
- nateglinide (Starlix)
Why is there a reduced risk of prolonged hypoglycemic episodes with meglitinides ?
**Only active in the presence of glucose**
If they are NPO or not eating a lot, should be withheld until back to regular food intake
Meglitinides versus sulfonylureas, how does onset/duration compare?
Meglitinides have faster onset (1hr) and shorter duration of action (4hrs)
Administer 15-30 minutes a.c. and NEVER while fasting
What are adverse effects of Meglitinides?
- Hypoglycemia (less than sulfonylureas)
- Weight gain
- URI
What is the most widely prescribed oral hypoglycemic?
Metformin (Glucophage)
What drug class does metformin belong to?
Biguanides
MOA of Metformin?
- Dec hepatic glucose production
- Dec glucose absorption from intestine
- Increase insulin sensitivity
In what ways do gut microbiota change with metformin?
- Reduced bacteroides fragilis (this organism has high rates linked to obesity, glucose intolerance, reduced insulin sensitivity)
- Increase glycoursodeoxylcholic acid (GUDCA)
- Inhibit signaling of intestinal farnesoid X receptor (FXR)