Home Drug Guide Rosiglitazone Maleate

Drug Guide

Generic Name

Rosiglitazone Maleate

Brand Names Avandia

Classification

Therapeutic: Antidiabetic agent

Pharmacological: Thiazolidinedione, PPARγ agonist

FDA Approved Indications

Type 2 diabetes mellitus, as an adjunct to diet and exercise to improve glycemic control

Mechanism of Action

Rosiglitazone activates peroxisome proliferator-activated receptor gamma (PPARγ), which increases insulin sensitivity in adipose tissue, skeletal muscle, and the liver, thereby improving blood glucose control.

Dosage and Administration

Adult: Typically 4 mg once daily, may be increased to a maximum of 8 mg/day based on response and tolerability.

Pediatric: Not approved for pediatric use.

Geriatric: Use with caution; start at lower end of dosing range due to increased sensitivity and comorbidities.

Renal Impairment: Adjust dosage based on renal function; monitor kidney function regularly.

Hepatic Impairment: Use caution; contraindicated in severe hepatic impairment.

Pharmacokinetics

Absorption: Rapidly absorbed, peak plasma levels within 1 hour.

Distribution: Widely distributed; extensive binding to plasma proteins.

Metabolism: Metabolized primarily by CYP2C8, with minor contributions from CYP3A4.

Excretion: Excreted mainly in urine (via metabolites) and feces.

Half Life: 3-4 hours for unchanged drug, but effects last longer due to receptor binding.

Contraindications

Heart failure (NYHA Class III or IV)

Precautions

History of bladder cancer, liver disease, edema, or active hepatic disease; monitor liver function tests regularly. Use with caution in patients at risk for heart failure.

Adverse Reactions - Common

Weight gain (Common)
Edema (Common)
Upper respiratory tract infections (Common)

Adverse Reactions - Serious

Heart failure exacerbation (Uncommon but serious)
Hepatotoxicity (Rare)
Bone fractures (particularly in women) (Uncommon)
Myocardial infarction (controversial but noted in some studies) (Uncertain, but warrants caution)

Drug-Drug Interactions

Insulin - risk of edema and heart failure; hypoglycemia risk with insulin or other antidiabetics.
Ketoconazole - inhibits metabolism, increasing rosiglitazone levels.

Drug-Food Interactions

None specifically noted.

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor blood glucose, HbA1c, liver function tests, and signs of heart failure. Regularly assess weight and edema.

Diagnoses:

Impaired skin integrity due to edema
Risk for hypoglycemia
Risk for heart failure

Implementation: Administer with or without food; educate patient on signs of edema, HF, and liver dysfunction.

Evaluation: Ensure blood glucose levels are within target range; monitor for adverse effects.

Patient/Family Teaching

Take medication exactly as prescribed.
Report signs of edema, weight gain, or shortness of breath.
Attend regular liver function testing.
Do not use alcohol excessively, as it may increase the risk of liver damage.

Special Considerations

Black Box Warnings:

Increased risk of myocardial infarction and heart failure. Use only if benefits outweigh risks.

Genetic Factors: N/A

Lab Test Interference: N/A

Overdose Management

Signs/Symptoms: Hypoglycemia, edema, signs of heart failure.

Treatment: Supportive care; no specific antidote. Discontinue medication, provide symptomatic treatment, and manage heart failure symptoms if present.

Storage and Handling

Storage: Store at controlled room temperature, 20°C to 25°C (68°F to 77°F).

Stability: Stable under recommended storage conditions.