Oral Anti-Hyperglycaemic Agents

Question 1

Alpha-glucosidase inhibitors ex. Acarbose:

• Site of Action
• MOA
• Side effects

Answer 1

Acarbose:
Site of action: gut/intestines
MOA: delays glucose/carbohydrate absorption, competitive inhibitor of intestinal brush border alpha-glucosidases
Side effects: Flatulence, diarrhea bloating
Contraindications: GI disease ex. Crohn’s

Question 2

Biguanide ex. Metformin:

• Site(s) of action
• MOA
• Side effects
• Contraindications

Answer 2

Metformin:
Sites of action: adipose tissue, muscle, liver
MOA: decrease hepatic glucose output, improves insulin resistance, cellular mechanisms unclear
Side effects: GI (anorexia, diarrhea), rarely lactic acidosis
Contraindications: Kidney disease, Liver disease, CHF

Question 3

Thiazolidinediones (TZDs) ex. Rosigitazone, Pioglitazone:

• Site(s) of action
• MOA
• Side effects
• Contraindications

Answer 3

Rosigitazone:
Sites of action: adipose, muscle, liver
MOA: PRARy agonist
Side effects: FLUID RETENTION, EDEMA, CHF, WEIGHT GAIN, fracture risk, bladder cancer, MI; no longer used due to side effects
Contraindications: CHF (NYHA III, IV), heart disease, kidney disease

Question 4

Insulin Secretagogues ex. Glyburide (Sulphonylureas) and Repaglinide (Meglitinides)

• Sites of action
• MOA
• Side effects
• Contraindications

Answer 4

Sulphonylureas (long acting) and Meglitinides (short acting):
Site of action: pancreas
MOA: insulin secretion and replacement
Side effects: RISK OF HYPOGLYCEMIA
Contraindications: Kidney disease, liver disease

Question 5

Incretins ex. Eventide

• Sites of action
• MOA
• Side effects
• Contraindications

Answer 5

Incretins
Site of action: pancreas
MOA: GLP1 agonist and DPP-IV inhibitors
Side effects: ACUTE PANCREATITIS, nausea, vomiting
Contraindications: Kidney disease, pancreatitis