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10 Cards in this Set

  • Front
  • Back

Metformin

MOA: decreases hepatic glucose production (decreases gluconeogenesis), improves insulin sensitivity

FIRST LINE


Advantages: dec A1C by 1-2%, $4 generic, weight nutral, NO hypoglycemia, dec in micro- and macro vasc complications (UKPDS)


Disadvantages: GI intolerance, vit B12 deficiency, CI's (all of them incr risk of lactic acidosis) = SCr >/= 1.5 men, 1.4 women, hepatic dx, excessive EtOH intake, elderly (80+ yo), acute illness, major surgery, or severe infection, Hypoxic states (acute CHF, acute MI), dehydration, iodinated contrast media


Use based on eGFR: >60 = no renal C.I., 45-60 = monitor renal fxn Q3-6 mos, 30-45 = use lower dose & with caution (50% of max) and monitor Q3 mos. <30 = stop metformin


Dosing: 500-850 QD-BID with meals..increase by 500-850 mg Q1-2wks as tolerated. Target: 1000mg BID, Max: 2550mg QD (2000 max effective). XR improves tolerability

Sulfonylureas

MOA: increase insulin secretion


Advantages: dec A1C by 1-1.5%, $4 generic, well tolerated, dec microvasc outcomes (UKPDS)


Disadvantages: risk of hypoglycemia (elderly, debilitated, malnourished, renal/hepatic fxn; greater risk w/glyburide - BEERS), weight gain, low durability


Dose Response: the max effective dose is about half of the maximum approved dose


Initial Dose: start at low end and work up to prevent hypoglycemia


Rare Adverse Rxn: SIADH, disulfuram (1st gen), hepatotoxicity, hemolytic anemia

Glimepiride

Class: Sulfonylurea


Duration: 24 hours


Clearance: hepatic/renal


Active Metabolites: yes but with minimal activity


Initial Dose: 1-2 mg QD


Max/day: 8 mg (4 mg max effective)

Glipizide

Class: Sulfonylurea


Duration: 10-24 hours


Clearance: hepatic/renal


Active Metabolites: no


Initial Dose: 5 mg QD-BID


Max/day: 40 mg, 20 mg if XL (20 mg max effective, 10 mg if XL)

Glyburide

Class: Sulfonylurea


Duration: 12-24 hours


Clearance: Renal


Active Metabolites: no


Initial Dose: 2.5-5 mg QD-BID


Max/day: 20 mg (10 mg max effective)

Meglitinides

Drugs: Repaglinide, Nateglinide


MOA: Increase insulin secretion (bind to a different location on the sulfonylurea receptor)


Advantages: dec post-prandial glucose excursions, dosing flexibility, rapid onset (quick on/off, take at onset of meal)


Disadvantages: hypoglycemia, weight gain, frequent dosing, expensive, modest efficacy (dec A1C by 0.5-1%), CYP3A4 interactions (gemfibrozil, itraconazole

Repaglinide

Class: Meglitinide


Duration: <4 hours


Clearance: hepatic; 3A4


Active Metabolites: yes


Initial Dose: 0.5-1 mg TID


Max/day: 16 mg

Nateglinide

Class: Meglitinide


Duration: 0.5-2 hours


Clearance: hepatic; 2C9 (and inhibits 2C9), 3A4


Active Metabolites: yes


Initial Dose: 60 mg TID


Max/day: 360 mg

Thiazolidinedione

MOA: potent peroxisome proliferator - activated receptor (PPAR-gamma) agonist -> increases insulin sensitivity in the muscles and liver


Advantages: dec A1C by 0.5-1.4%, NO hypoglycemia, inc HDL, dec TG, ?dec CVD events (ProACTIVE)


Disadvantages: 8-12 week delay to onset of full effect, weight gain, edema/HF, ?inc bladder cancer (dose/duration effect), inc risk of fractures


CI's: HF (NYHA Class 3 or 4


Precautions: risk factors for HF, edema, additional risk factors for fracture (female, elderly), active liver dx (beneficial in fatty liver dx, avoid use if ALT > 2.5 x ULN), combo tx with sulfonylurea and/or insulin may exacerbate weight gain (consider tzd dose reduction if adding agents), prior hx of bladder cancer

Alpha-Glucosidase Inhibitors

Drugs: acarbose, miglitol


MOA: delays intestinal CHO digestion and absorption by competitively inhibiting enzymes in the small intestine


Advantages: NO hypoglycemia, reduces postprandial hyperglycemia, ?dec CVD events (STOPP-NIDDM)


Disadvantages: flatulence, diarrhea, bloating/gas (70%), abdominal pain, frequent dosing schedule, modest efficacy (dec A1C 0.5-0.9%)


start with low dose and build up


Dosing: