Exam IV - Diabetes Flashcards
Insulin
Indications
Hyperglycemia
Insulin
Mechanism
Rapid: ↑ Gluc transport Intermediate: Activates glycolytic enzymes, glycogen synthase; Blocks posphorylase & gluconeogenesis Delayed: Gene transcription; cell growth
Insulin
ADME
- Injected SQ, IV or IM in emergency 2. Ultra short acting: Lispro, Aspart, Glulisine 3. Rapid acting: standard, purified 4. Intermediate acting: Novolin-N, Humulin-N 5. Long Acting: Detemir, Glargine *use short acting at meals & longer for cont. effect
Insulin
Advantages
- Therapy is individualized: multidose regimens, repeated monitoring 2. Now other admin forms: pen, nasal spray
Insulin
Adverse
- “Dawn effect” - overnight dosing is important 2. Hypoglycemia (
Insulin
Contraindications
Pregnancy category B
Metformin (Biguanide)
Indications
Insulin sensitizer: blocks glucose release from liver
First line for DMII
Metformin
Mechanism
Activates AMPK in liver: ↑FA oxidation, ↑gluc uptake, ↓lipogenesis, ↓gluconeogenesis
Metformin
ADME
T½ 1.5-3H Non-protein binding Not metabolized Kidney excreted used in combo w/ PO antidiabetics: metformin+saxagliptin
Metformin
Advantages
- Doesn’t induce hypoglycemia 2. No weight gain 3. Inhibits microvascular complications
Metformin
Adverse
GI: N,V&D - dose dependent, transient, metallic taste
Metformin
Contraindications
- Pregnancy Category B 2. Renal & Hepatic Dz
- EtOH: lactic acidosis
Glipizide (Sulfonylurea)
Indications
Classic secretagogue: promotes pancreatic insulin secretion
Glipizide
Mechanism
- Binds & blocks ATP sensetive K+ channel β-cell → depolarization → Ca2+ influx
- Requires functional β-cells
- No effect on insulin resistance / sensitvity
Glipizide
ADME
Protein bound liver metab renal excretion
Glipizide
Advantages
↓ A1C by 1-2% 2nd generation: fewer adverse effects
Glipizide
Adverse
- Hypoglycemia 2. Weight gain
Glipizide
Contraindications
- Pregnancy Category C 2. Hepatic & renal Dz 3. Caution in elderly pts
Glipizide
Drug-Drug
- ↑ hypoglycemia: NSAIDS, MAOIs, sulfonamides, chloramphenicol, H2 antihistamines, EtOH 2. ↓hypoglycemia: β-blockers; thiazides, estrogens, rifampin