Sulfonylureas, Metformin, Glucagon Flashcards
Sulfonylureas MOA (4)
- Enhancement of insulin secretion
- Bind to sulfonylurea receptor (SUR) on pancreatic B cells
- Closes ATP-dependent K channels, influx of Ca
- Suppresses hepatic glucose production
Sulfonylureas Generation 1 (4)
- Acetohexamide
- Chlorpropamide
- Tolazamide
- Tolbutamide
Sulfonylureas Generation 2 (3)
- Glimepiride
- Glipizide
- Glyburide
Sulfonylureas PK/PD (3)
1, Metabolized by the liver
- 2nd generation more ‘potent’ than 1st generation sulfonylureas
- All sulfonylureas equally effective at equipotent doses
Sulfonylureas ADE (5)
- Hypoglycemia
- Hyponatremia
- Weight gain
- Rashes
- Abdominal discomfort
Sulfonylureas Interactions w/ Medications
- Displacement from protein binding sites (3)
- Alters hepatic metabolism (3)
- Alters renal excretion (1)
- Warfarin, salicylates, sulfonamides
- MAOIs, rifampin, cimetidine
- Allopurinol
Sulfonylureas Pearls (5)
- HbA1c reduction of 1.5-2%
- FPG reduction of 60-70 mg/dL
- Generally dosed once daily
- Adverse events increased when taken on empty stomach or if meals are skipped
- Take ~30 minutes prior to meals
Metformin (Glucophage) MOA (3)
- Increases insulin sensitivity
- Decreases hepatic glucose production
- Decreases intestinal glucose absorption
Metformin (Glucophage) ADE (4)
- Abdominal discomfort (N/V/D especially with IR)
- Metallic taste disturbances
- Lactic acidosis (rare but serious complication)
- Decreased B12
Metformin (Glucophage) Contradindications (2)
- Renal impairment
2. Radiographic contrast – Hold day of procedure, Restart 2-3 days after procedure
Metformin (Glucophage) Pearls (6)
- HbA1c reduction of 1.5-2%
- FPG reduction of 60-80 mg/dL
- Decreases plasma triglycerides and LDL-C by 8-15%
- Increases HDL by 2%
- Modest reduction in weight
- Only oral agent approved for pediatric use
Managing Hypoglycemia (2)
- 15 grams CHO
2. Glucagon
Glucagon (GlucoGen) MOA
Stimulates adenylate cyclase increasing cAMP and gluconeogenesis
Glucagon (GlucoGen) PK
Onset within 5-10 min
Glucagon (GlucoGen)
ADE (2)
- Hypotension
2. N/V
Glucagon (GlucoGen) Admin (3)
IV, IM, SC
Glucagon (GlucoGen) Place in Therapy
Acute hypoglycemia episodes
Medications increases glucose effects (7)
- Diuretics – increases
- Glucocorticoids – increases
- Nicotinic Acid – increases
- Oral contraceptives – increases
- Phenytoin – increases
- B-Blockers – increases
- Clozapine – increases
Medications decreasing glucose effects (4)
- Ace I – decreases
- Alcohol – decreases
- Pentamide – decreases
- Salicylates – decreases