Antidiabetic Drugs

Question 1

Insulin Secretagogue Mechanism of Action

Answer 1

Block K secretion in beta cells, increasing intracellular Ca, leading to release of insulin

Question 2

Sulfonylurea Agents

Insulin Secretagogues

Answer 2

Lower fasting blood glucose levels by triggering the release of insulin from beta cells. Include glipizide (Glucotrol) and glimepiride (Amaryl)

Question 3

glipizide (Glucotrol)

Answer 3

[Sulfonylurea Agent]
5-10 mg q12h 30 min ac
Increases insulin secretion in T2 DM
High risk for hypoglycemia c impaired kidney function
Common SE: hypoglycemia, c/d/n/f, h/a, dizziness, asthenia, tremor
Serious SE: severe hypoglycemia, hemolytic anemia, Stevens-Johnson syndrome

Question 4

glimepiride (Amaryl)

Answer 4

[Sulfonylurea Agent]
1-2 mg daily (first meal) then 1-4 mg daily max 8 mg
Increases insulin secretion in T2 DM
Often combined with metformin or insulin for T2 DM
Common SE: hypoglycemia, nausea, dizziness, h/a
Serious SE: cutaneous hypersensitivity, Stevens-Johnson syndrome

Question 5

Meglitinide Analogs

Insulin Secretagogues

Answer 5

Actions and side effects similar to sulfonylureas. Trigger release of insulin from beta cells. May cause hypoglycemia. Include repaglinide (Prandin) and nateglinide (Starnix). Lower A1c by average of 1.5 points

Question 6

repaglinide (Prandin)

Answer 6

[Meglitinide Analog]
0.5-4 mg PO daily (1-30 min ac)
Rapid acting, short duration
Treats fasting and pc hyperglycemia
Omit when skipping meal
Common SE: hypoglycemia, diarrhea, arthralgia, h/a, sinusitis, upper resp. infection
Serious SE: angina, cardiac dysrhythmia, MI, myocardial ischemia

Question 7

nateglinide (Starlix)

Answer 7

[Meglitinide Analog]
60-120 mg PO TID 1-30 min ac
Rapid acting, short duration
Treats fasting and pc hyperglycemia
Omit when skipping meal
Common SE: hypoglycemia, upper resp. infection

Question 8

Insulin Sensitizers

Answer 8

Include [biguanides] and [thiazolidinediones]
Decrease liver glucose production and improve insulin receptor sensitivity.
[Biguanides] have low cost/few side effects. Should not be given to anyone with kidney disease/increased creatinine levels and witheld 48 before and after using contrast material and anesthesia. Lowers A1c by average of 1.5 points
[Thiazlidinediones] also improve insulin action in muscle, fat, and liver tissue; reduce blood lipid levels, increase adipose tissue/fluid retention. Lowers A1c by average of 0.5-1.4 points. May take 8-12 weeks for full therapeutic response.

Question 9

metformin (Glucophage)

Answer 9

[Insulin Sensitizer] (biguanide)
850 mg PO BID (morning/evening meal)
Reduces hepatic glucose production, increases insulin receptor sensitivity
Risk for lactic acidosis c renal/hepatic impairment, acute CHF, sepsis, dehydration, etoh intake
Common SE: cobalamin deficiency, d/f/n/v/i, malabsorption syndrome
Serious SE: (BLACK BOX lactic acidosis)

Question 10

rosiglitazone (Avandia)

Answer 10

[Insulin Sensitizer] (thiazolidinedione)
4 mg PO daily AM or 2 mg PO BID without regard to food
Improves tissue sensitivity to insulin in T2 DM
Need for liver function tests; report unexplained n/v, abd pain, fatigue, anorexia, dark urine. Monitor weight, edema
Common SE: edema, weight gain
Serious SE: angina, (BLACK BOX CHF), MI, myocardial ischemia, cholestatic hepatitis, hepatotoxicity, cerebrovascular accident, diabetic macular edema, pleural effusion, pneumonia, pulmonary edema

Question 11

pioglitazone (Actos)

Answer 11

[Insulin Sensitizer] (thiazolidinedione)
15 or 30 mg PO daily without regard to food
Improves tissue sensitivity to insulin in T2 DM
Need for liver function tests; report unexplained n/v, abd pain, fatigue, anorexia, dark urine. Monitor weight, edema
Common SE: edema, weight gain, anemia, bone fracture, myalgia, pharyngitis, sinusitis, upper resp. infection
Serious SE: (BLACK BOX CHF), liver failure (ALT/SGPT level raised), diabetic macular edema, malignant tumor of urinary bladder, pneumonia