ROSIGLITAZONE MALEATE

ROSIGLITAZONE MALEATE
(ros-i-glit'a-zone)
Avandia
Classifications: hormone; antidiabetic; thiazolidinediones;
Therapeutic: antidiabetic

Pregnancy Category: C

Availability

2 mg, 4 mg, 8 mg tablets

Action

Antidiabetic agent that lowers blood sugar levels by improving target cell response to insulin in Type 2 diabetics. It reduces cellular insulin resistance and decreases hepatic glucose output (gluconeogenesis).

Therapeutic Effect

Reduces hyperglycemia and hyperlipidemia, thus improving hyperinsulinemia without stimulating pancreatic insulin secretion. Indicated by decreased HbA1C.

Uses

Adjunct to diet in the treatment of type 2 diabetes. May also be used in combination with metformin.

Contraindications

Hypersensitivity to rosiglitazone; cardiovascular disease, particularly hypertensive patients with New York Heart Association Class III and IV cardiac status (e.g., CHF); pregnancy (category C), lactation; active hepatic disease or ALT >2.5 times normal.

Cautious Use

As monotherapy in Type 1 diabetes mellitus or diabetic ketoacidosis; CHF or risk for CHF; hepatic impairment. Safety and efficacy in children <18 y are not established.

Route & Dosage

Type 2 Diabetes Mellitus
Adult: PO Start at 4 mg q.d. or 2 mg b.i.d., may increase after 12 wk (max: 8 mg/d in 1–2 divided doses)

Hepatic Impairment
Do not use if ALT >2.5 x ULN.

Administration

Oral
  • Do not initiate therapy if baseline serum ALT >2.5.
  • Store at 15°–30° C (59°–86° F) in tight, light-resistant container.

Adverse Effects (≥1%)

Body as a Whole: Edema, anemia, headache, back pain, fatigue. CV: edema, fluid retention, exacerbation of heart failure, increased risk of heart attack. GI: Diarrhea. Respiratory: Upper respiratory tract infection, sinusitis. Special Senses: Macular edema. Other: Hyperglycemia.

Interactions

Drug: Insulin may increase risk of heart failure or edema; enhance hypoglycemia with oral antidiabetic agents, ketoconazole, gemfibrozil may increase effect. Bosentan may reduce effect. Herbal: Garlic, ginseng, green tea may potentiate hypoglycemic effects.

Pharmacokinetics

Absorption: 99% from GI tract. Peak: 1 h, food delays time to peak by 1.75 h. Duration: >24 h. Distribution: >99% protein bound. Metabolism: In liver (CYP2C8) to inactive metabolites. Elimination: 64% urine, 23% feces. Half-Life: 3–4 h. Liver disease increases serum concentrations and increases half-life by 2 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S of hypoglycemia (possible when insulin/sulfonylureas are coadministered).
  • Monitor for S&S of CHF or exacerbation of symptoms with preexisting CHF.
  • Lab tests: Liver function and serum ALT at baseline, then q2mo for first year; then periodically (more often when elevated); periodic HbA1C, Hgb and Hct, and lipid profile.
  • Withhold drug and notify physician if ALT >3 times normal or patient jaundiced.
  • Monitor weight and notify physician of development of edema.

Patient & Family Education

  • Have blood tested for liver function every 2 mo for first year; then periodically.
  • Be aware that resumed ovulation is possible in nonovulating premenopausal women.
  • Use or add barrier contraceptive if using hormonal contraception.
  • Report immediately to physician: S&S of liver dysfunction such as 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.

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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