Sulfonylureas & Meglitinides Flashcards
Sulfonylureas Primary MOA
- Stimulate insulin release from beta cells
- “insulin secretagogues”
- Wakes up pancreas to make more insulin, which bring down blood sugar
Sulfonylureas Site of Action
- PANCREAS, beta cells
2nd Gen Sulfonylureas
- Glyburide (DiaBeta®, Micronase®, Glynase Prestabs®)
- Glipizide (Glucotrol®, Glucotrol® XL)
- Glimepiride (Amaryl®)
Glyburide Dosing
- 1.25-20mg PO QD
- Do not use in CrCl <50 mL/min
Glipizide Dosing
- IR: 2.5-20mg PO once-twice daily
- XL: 5-10mg PO daily
Glimepiride Dosing
- 1-4mg PO daily
Sulfonylurea: Side effects
- Hypoglycemia (since sulfonylurea tell pancreas to make insulin, which lowers blood sugar)
- N/V
- Weight gain (due to lots of insulin; does not mean it cannot be used in overweight patient)
Sulfonylurea: Drug interactions
- Alcohol
- Displaced protein binding
- DECREASE renal excretion
Sulfonylurea: Contraindications
- Hypersensitivity
- DKA
- CrCl < 50 (glyburide only)
- Pregnancy-near term (glyburide/glipizide only)
- All are Category C
- T1DM
Sulfonylurea: Precaution
- Impaired renal function
- Impaired liver function
- Elderly
- Sulfonamide allergy
- Thyroid dz.
- Adrenal insufficiency
- Malnutrition
- G6PD deficiency
Sulfonylurea: Counseling points
- Take first thing in the morning
- With breakfast or first main meal of the day
- Glipizide IR: 30 minutes before breakfast
- If upset stomach: take with food
- Avoid alcohol
- ASK ABOUT hypoglycemia and weight gain
Sulfonylurea: Monitoring
- Hypoglycemia
- A1c
- Weight gain
- Sun sensitivity (counsel)
Time to full effect: 4-6 weeks
Meglitinides Primary MOA
- Stimulate insulin release from beta cells
- Insulin secretagogues, SHORT ACTING
- Similar to sulfonylureas
Meglitinides: Site of Action
- PANCREAS, beta cells
Meglitinides Drugs
- Repaglinide (Prandin)
- Nateglinide (Starlix)
- Meglitinides should be taken with every single meal if pt don’t eat, not a good choice of drug
Nateglinide (Starlix): Dosing
- 60-120mg PO before meals
Repaglinide (Prandin): Dosing
- A1C <8%: start 0.5mg PO before meals
- A1C ≥8%: start 1-2mg PO before meals
- MDD: 4mg/dose or 16mg/day
Meglitinides: Side effects
- Hypoglycemia
- GI disturbances
NATEGLINIDE: Drug interactions
- Mifepristone: Do not use within 14 days
- Pazopanib: Increased nataglinide levels
REPAGLINIDE: Drug interactions
- Mifepristone: Do not use within 14 days
- Gemfibrozil: Increased repaglinide levels
- NPH insulin: Increased risk of MI*****
Meglitinides: CI/precaution
Contraindications: Hypersensitivity, T1DM, DKA
Precautions: Severe renal disease, Impaired liver function, Use with insulin
Meglitinides: Counseling points
Administered before meals (AC)
- Repaglinide: 15-30 minutes prior
- Nateglinide: 1-30 minutes prior
- Skip a meal, skip the dose
- Avoid Alcohol
ASK ABOUT: hypoglycemia and weight gain
Meglitinides: Monitoring
- PPG
Time to peak effect 4-6 weeks
