Rosiglitazone
Indications
Rosiglitazone is used for:
Type 2 Diabetes Mellitus
Adult Dose
Type 2 Diabetes Mellitus
Initial 4 mg PO qDay or divided q12hr
If inadequate response afer 8-12 weeks, may increase dose to 8 mg PO qDay or divided q12hr
Active liver disease (ALT >2.5 x ULN): Do not inititate rosiglitazone
Child Dose
Renal Dose
Renal impairment: No dosage adjustments required
Administration
Contra Indications
Hypersensitivity to rosiglitazone
Diabetic ketoacidosis
Heart failure NYHA class III-IV
Active liver disease: do not start rosiglitazone if ALT >2.5 x ULN
Precautions
Fluid retention, which may exacerbate or lead to heart failure, may occur; combination use with insulin and use in congestive heart failure NYHA Class I and II may increase risk of other cardiovascular effects
If ALT >3 x ULN stop treatment; if 1.5-3 x normal, retest qWeek until normal or 3 x normal and need to discontinue
Not for use in diabetes mellitus type 1; mechanism requires presence of endogenous insulin; use with insulin may increase risk of heart failure; not recommended
Thiazolidinediones, which are peroxisome proliferator-activated receptor (PPAR) gamma agonists, can cause dose-related fluid retention, particularly when used in combination with insulin; dose-related edema and weight gain may occur
When used in combination with other hypoglycemic agents, a dose reduction of concomitant agent may be necessary to reduce risk of hypoglycemia
Associated with rare cases of new onset or worsening of macular edema
May result in ovulation in some premenopausal anovulatory women; ensure adequate contraception
Increased risk of fractures of upper arm, hand, or foot in female patients
Dose-related decreases in hemoglobin and hemocrit reported
Monitor: ALT at start of treatment, qMonth for 12 months then q3Months thereafter
Lactation: Unsafe
Pregnancy-Lactation
Interactions
Adverse Effects
Side effects of Rosiglitazone :
>10%
Increased LDL-cholesterol,Increased HDL-cholesterol,Increased total cholesterol
1-10%
Edema,Hypertension,Heart failure/congestive heart failure,Myocardial ischemia,Diarrhea,Upper respiratory tract infection
Frequency Not Defined
Accidental injury
Anemia
Back pain
Fatigue
Headache
Hypoglycemia
Myalgia
Sinusitis
Weight gain
Mechanism of Action
Lowers glucose by improving target cell response to insulin without increasing pancreatic cell secretion; activates nuclear peroxisome proliferator-activated receptor gamma, which influences the production of gene products involved in glucose and lipid metabolism