rosiglitazone maleate

rosiglitazone maleate Warning - High-alert drug!

Avandia

Pharmacologic class: Thiazolidinedione

Therapeutic class: Hypoglycemic

Pregnancy risk category C

FDA Boxed Warning

• Drug may cause or exacerbate heart failure in some patients. After initiating therapy or increasing dosage, observe patient carefully for heart failure signs and symptoms. If these occur, manage condition per current standards of care and consider withdrawing drug or lowering dosage.
• Drug isn't recommended in patients with symptomatic heart failure and is contraindicated in those with established New York Heart Association Class III or IV heart failure.

Action

Inhibits alpha-glucosidases, enzymes that convert oligosaccharides and disaccharides to glucose. This inhibition lowers blood glucose level, especially in postprandial hyperglycemia.

Availability

Tablets: 2 mg, 8 mg

⊘Indications and dosages

➣ Adjunct to diet and exercise in type 2 (non-insulin-dependent) diabetes mellitus (used alone); given with metformin, insulin, or a sulfonylurea when combination of diet, exercise, and monotherapy with another hypoglycemic drug don't achieve glycemic control

Adults: 4 mg P.O. once daily or 2 mg b.i.d. After 12 weeks, may increase to 8 mg daily or 4 mg b.i.d. if needed.

Off-label uses

• Polycystic ovary syndrome

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• diabetic ketoacidosis, type 1 (insulin-dependent) diabetes mellitus (use not recommended)
• edema, heart failure, jaundice, hypertension, hepatic impairment
• NYHA Class III or IV cardiac status
• pregnant patients
• breastfeeding patients (use not recommended)
• children (safety and efficacy not established).

Administration

• Give with or without food.
• Be aware that drug is active only in presence of endogenous insulin and thus is ineffective in diabetic ketoacidosis or type 1 diabetes mellitus.

Route	Onset	Peak	Duration
P.O.	Unknown	Unknown	12-24 hr

Adverse reactions

CNS: fatigue, headache

EENT: sinusitis

GI: diarrhea

Hematologic: anemia

Metabolic: hyperglycemia, hypoglycemia

Musculoskeletal: back pain

Respiratory: upper respiratory infection

Other: edema, injury, weight gain

Interactions

Drug-diagnostic tests. Free fatty acids, high-density lipoproteins, low-density lipoproteins, total cholesterol: increased levels

Hematocrit, hemoglobin: decreased levels

Drug-herbs. Aloe, bitter melon, chromium, coenzyme Q10, fenugreek, glucomannan, gymnema sylvestre, psyllium, St. John's wort: additive hypoglycemic effects

Glucosamine: poor glycemic control

Patient monitoring

• Monitor CBC, lipid panel, blood glucose, and glycosylated hemoglobin levels.
• Monitor patient's weight. Assess for fluid retention, which may lead to heart failure.
• Closely monitor liver function tests; drug may cause hepatotoxicity.

Patient teaching

• Tell patient he may take with or without food.
• Advise patient to monitor blood glucose level regularly and report significant changes.
☞ Inform patient that drug may increase fluid retention, causing or exacerbating heart failure. Encourage him to weigh himself regularly and report sudden weight gain, swelling, or shortness of breath.
• Tell patient he'll undergo regular blood testing during therapy.
• Caution female patient not to breastfeed during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the tests and herbs mentioned above.