Solutions
Thiazolidinedione (TZD) Antihyperglycemic medication class
Mechanism: enhances insulin sensitivity in peripheral tissues and liver
Takes 6-12 weeks to achieve full glycemic affect
*Pioglitazone (Actos)*
Monotherapy or combination therapy (with an SU or metformin): 15-30 mg once daily (max
45mg/day)
*Rosiglitazone (Avandia)*
Monotherapy: Initial: 4 mg daily as a single daily dose or in divided doses BID. If response is
inadequate after 8-12 weeks can increase to 8 mg daily or divided BID
Combination therapy:
With metformin: dosing as above for monotherapy
With a sulfonylurea: dose should NOT exceed 4 mg daily when using in combination with a
sulfonylurea. Reduce dose of sulfonylurea if hypoglycemia occurs
NOTE:
,Negligible hypoglycemia when monotherapy
+Weight gain
Edema and CHF
*Do NOT use in patients with CHF or LV dysfunction*
Fracture risk
Bladder cancer risk (pioglitazone)
MI risk? (rosiglitazone)
Metformin Antihyperglycemic
Mechanism: enhances insulin sensitivity in peripheral tissue and liver
*Metformin (Glucophage)*
Allow 1-2 weeks between dose titrations: Generally, clinically significant responses are not seen
at doses <1500 mg daily; however, a lower recommended starting dose and gradual increased
dosage is recommended to minimize gastrointestinal symptoms
*Immediate release tablet*: 500mg po BID or 850mg po od, titrate in increments of 500 mg
weekly or 850 mg every other week
If a dose >2000 mg daily is required, it may be better tolerated in 3 divided doses. Maximum
recommended dose: 2550 mg daily
,*Extended release tablet* (If glycemic control is not achieved at maximum dose, may divide
dose and administer twice daily):
Fortamet®: Initial: 500-1000 mg od; dosage may be increased by 500 mg weekly; maximum
dose: 2500 mg once daily
Glucophage® XR: Initial: 500 mg od; dosage may be increased by 500 mg weekly; maximum
dose: 2000 mg once daily
NOTE:
Negligible hypoglycemia risk as monotherapy
Improved cardiovascular outcomes in overweight pts
Weight neutral and promotes less weight gain when combined with other antihyperglycemic
agents including insulin
CI if CrCl/eGFR <30ml/min or hepatic failure
GI side effects
DPP-4 Inhibitors Antihyperglycemic medication class
Mechanism: Amplifies incretin pathway activation by inhibiting GLP-1 and GIP breakdown
*Sitagliptin (Januvia)*
, 100mg po daily
CrCl 30-50: 50mg od
CrCl <30: 25mg od
*Saxagliptin (Onglyza)*
2.5-5mg po daily
CrCl <50: 2.5mg od
*Linagliptin (Trajenta)*
5mg po daily
No dose adjustment for renal failure
For all of the DPP-4 inhibitors, in combination with insulin or SU may require reduced dose of
insulin or SU
NOTE:
Weight neutral
Improved postprandial control
Negligible hypoglycemia
Rare cases pancreatitis