Classifications: thiazolidinedione; antidiabetic;
Therapeutic: antidiabetic

Prototype: Rosiglitazone maleate
Pregnancy Category: C


15 mg, 30 mg, 45 mg tablets


Results in insulin sensitivity by affecting insulin receptors. Decreases hepatic glucose output and increases insulin-dependent muscle glucose uptake in skeletal muscle and adipose tissue. Improves glycemic control in noninsulin-dependent diabetic (type 2) patients by enhancing insulin sensitivity of cells without stimulating pancreatic insulin secretion.

Therapeutic Effect

Improves glycemic control as indicated by improved blood glucose levels and decreased HbA1C to 6.5 or lower.


Adjunct to diet in the treatment of type 2 diabetes mellitus.


Hypersensitivity to pioglitazone, troglitazone, rosiglitazone, englitazone; type 1 diabetes, or treatment of DKA; active liver disease or ALT levels >2.5 times normal limit; jaundice; pregnancy (category C), lactation.

Cautious Use

Liver dysfunction; cardiovascular disease [New York Heart Association (NYHA)] Class III and Class IV (e.g., CHF); hypertension, edema; renal impairment; older adults. Safety and efficacy in children <18 y are not established.

Route & Dosage

Type 2 Diabetes Mellitus
Adult: PO 15–30 mg once daily (max: 45 mg q.d.)


  • Give without regard to food.
  • Do not initiate therapy if baseline serum ALT >2.5 times normal.
  • Store at 15°–30° C (59°–86° F) in tightly closed container; protect from humidity and moisture.

Adverse Effects (≥1%)

Body as a Whole: Headache, myalgia, edema. CV: Edema, fluid retention, exacerbation of heart failure. GI: Tooth disorder. Respiratory: Upper respiratory tract infection, sinusitis, pharyngitis. Metabolic: Hypoglycemia, mild anemia.


Drug: Pioglitazone may decrease serum levels of oral contraceptives; ketoconazole, gemfibrozil may increase serum levels of pioglitazone. Herbal: Garlic, ginseng may potentiate hypoglycemic effects.


Absorption: Rapidly absorbed. Peak: 2 h; steady state concentrations within 7 d. Duration: 24 h. Distribution: >99% protein bound. Metabolism: In liver to active metabolites. Elimination: Primarily in bile and feces. Half-Life: 16–24 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S hypoglycemia (possible when insulin/sulfonylureas are coadministered).
  • Monitor closely for S&S of CHF or exacerbation of symptoms with preexisting CHF.
  • Lab tests: Baseline serum ALT, then q2mo for first year, then periodically (more often if elevated); periodic HbA1C, Hgb and Hct, and lipid profile.
  • Discontinue drug if ALT >3 x ULN or patient has jaundice.
  • Monitor weight and notify physician of development of edema.

Patient & Family Education

  • Be aware that resumed ovulation is possible in nonovulating premenopausal women.
  • Use or add barrier contraceptive if using hormonal contraception.
  • Report immediately to physician: Unexplained anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine; or S&S of fluid retention such as weight gain, edema, or activity intolerance.
  • Combination therapy: May need adjustment of other antidiabetic drugs to avoid hypoglycemia.
  • Learn of and adhere strictly to guideliness for liver function tests. Be sure to have blood tests for liver function every 2 mo for first year; then periodically.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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