Rosiglitazone Maleate

(roe-sih-GLIH-tah-sone MAL-ee-ate)

  Action:
Increases insulin sensitivity.

  Indications:
Improves glycemic control of type 2 diabetes mellitus as monotherapy as an adjunct to diet and exercise; in combination with metformin when diet, exercise, and either agent alone does not result in adequate glycemic control in patients with type 2 diabetes mellitus.

  Contraindications:
Standard considerations.

  Route/Dosage:

Monotherapy:

Adults:
PO Initiate therapy at 4 mg daily, administered as a single dose or 2 divided doses. For patients not responding adequately, the dose may be increased to 8 mg daily after 8 to 12 wk of therapy.

Combination therapy

Metformin:

Adults:
PO In combination with metformin, initiate therapy with 4 mg of rosiglitazone as a single dose or 2 divided doses.

Sulfonylureas:

Adults:
PO In combination with sulfonylureas, the recommended dose of rosiglitazone is 4 mg as a single dose or 2 divided doses. If patient reports hypoglycemia, decrease the sulfonylurea dose.

  Interactions:
None well documented.

  Lab Test Interferences:
None well documented.

  Adverse Reactions:

CNS:

Headache; fatigue.

EENT:

Sinusitis.

GI:

Diarrhea.

HEMA:

Anemia; decreased hematocrit; decreased hemoglobin.

META:

Decreased free fatty acids; hyperglycemia; hypoglycemia; increased total cholesterol, LDL, and HDL.

RESP:

Upper respiratory tract infection.

OTHER:

Back pain; edema.

  Precautions:

Pregnancy: Category C.

Lactation: Undetermined.

Children: Safety and efficacy not established.

Edema: Use with caution.

Hepatic function impairment: Use with caution.

Ovulation: May result in resumption of ovulation in premenopausal, anovulatory women with insulin resistance.

  Administration/Storage:

• Store at room temperature in a tight, light-resistant container.
• Administer with or without food.
• Do not administer to patients with clinical evidence of active liver disease or elevated liver enzymes (ALT > 2.5 × upper limit of normal) at the initiation of therapy.
• Administer with caution to patients with CHF as rosiglitazone has been associated with fluid volume expansion and preload-induced cardiac hypertrophy.
• Do not administer to nursing mothers.
• Do not administer to pregnant women. Most experts recommend that insulin be used during pregnancy to maintain as close to normal as possible.

  Assessment/Interventions:

• Assess for signs and symptoms of adverse reactions.
• Obtain a complete history of prescription and nonprescription drugs and any history of hypersensitivities.
• Monitor liver enzymes prior to initiation of treatment and periodically thereafter as another agent in the thiazolidinedione class has been associated with idiosyncratic hepatic toxicity and rare cases of liver failure, liver transplants, and death.

  Patient/Family Education:

• Instruct patient to take the medication as prescribed.
• Instruct patient that management of type 2 diabetes includes diet control, caloric restriction, and weight loss because these factors help improve insulin sensitivity and are effective functions of other metabolic processes. In addition, these nonpharmacologic interventions aid in the effectiveness of pharmacologic therapy.
• Emphasize the importance of adhering to dietary instruction and maintaining a normal blood glucose level.
• Emphasize the importance of regular daily blood glucose monitoring and periodic glycosylated hemoglobin (HbA1c) tests.
• Inform patient that blood will be drawn to check liver function prior to the start of therapy and about every 2 mo for the first 12 mo, and periodically thereafter.
• Warn patient to report any nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, or any sign of liver impairment immediately to health care provider.
• Caution women that rosiglitazone can cause resumption of ovulation in premenopausal, anovulatory women with insulin resistance. Address adequate contraceptive measures for these women.
• Caution women to inform their primary caregivers if they are or plan to become pregnant.
• Warn nursing mothers that a decision to discontinue the drug or nursing should be made in collaboration with their primary health care providers.

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