Sulfonylureas & Meglitinides

Question 1

Sulfonylureas Primary MOA

Answer 1

• Stimulate insulin release from beta cells
• “insulin secretagogues”
• Wakes up pancreas to make more insulin, which bring down blood sugar

Question 2

Sulfonylureas Site of Action

Answer 2

• PANCREAS, beta cells

Question 3

2nd Gen Sulfonylureas

Answer 3

• Glyburide (DiaBeta®, Micronase®, Glynase Prestabs®)
• Glipizide (Glucotrol®, Glucotrol® XL)
• Glimepiride (Amaryl®)

Question 4

Glyburide Dosing

Answer 4

• 1.25-20mg PO QD

- Do not use in CrCl <50 mL/min

Question 5

Glipizide Dosing

Answer 5

• IR: 2.5-20mg PO once-twice daily

- XL: 5-10mg PO daily

Question 6

Glimepiride Dosing

Answer 6

• 1-4mg PO daily

Question 7

Sulfonylurea: Side effects

Answer 7

• 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)

Question 8

Sulfonylurea: Drug interactions

Answer 8

• Alcohol
• Displaced protein binding
• DECREASE renal excretion

Question 9

Sulfonylurea: Contraindications

Answer 9

• Hypersensitivity
• DKA
• CrCl < 50 (glyburide only)
• Pregnancy-near term (glyburide/glipizide only)
• All are Category C
• T1DM

Question 10

Sulfonylurea: Precaution

Answer 10

• Impaired renal function
• Impaired liver function
• Elderly
• Sulfonamide allergy
• Thyroid dz.
• Adrenal insufficiency
• Malnutrition
• G6PD deficiency

Question 11

Sulfonylurea: Counseling points

Answer 11

• 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

Question 12

Sulfonylurea: Monitoring

Answer 12

• Hypoglycemia
• A1c
• Weight gain
• Sun sensitivity (counsel)

Time to full effect: 4-6 weeks

Question 13

Meglitinides Primary MOA

Answer 13

• Stimulate insulin release from beta cells
• Insulin secretagogues, SHORT ACTING
• Similar to sulfonylureas

Question 14

Meglitinides: Site of Action

Answer 14

• PANCREAS, beta cells

Question 15

Meglitinides Drugs

Answer 15

• Repaglinide (Prandin)
• Nateglinide (Starlix)
• Meglitinides should be taken with every single meal if pt don’t eat, not a good choice of drug

Question 16

Nateglinide (Starlix): Dosing

Answer 16

• 60-120mg PO before meals

Question 17

Repaglinide (Prandin): Dosing

Answer 17

• A1C <8%: start 0.5mg PO before meals
• A1C ≥8%: start 1-2mg PO before meals
• MDD: 4mg/dose or 16mg/day

Question 18

Meglitinides: Side effects

Answer 18

• Hypoglycemia

- GI disturbances

Question 19

NATEGLINIDE: Drug interactions

Answer 19

• Mifepristone: Do not use within 14 days

- Pazopanib: Increased nataglinide levels

Question 20

REPAGLINIDE: Drug interactions

Answer 20

• Mifepristone: Do not use within 14 days
• Gemfibrozil: Increased repaglinide levels
• NPH insulin: Increased risk of MI*****

Question 21

Meglitinides: CI/precaution

Answer 21

Contraindications: Hypersensitivity, T1DM, DKA

Precautions: Severe renal disease, Impaired liver function, Use with insulin

Question 22

Meglitinides: Counseling points

Answer 22

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

Question 23

Meglitinides: Monitoring

Answer 23

• PPG

Time to peak effect 4-6 weeks