Drug Guide
Sunitinib Malate
Classification
Therapeutic: Antineoplastic agent
Pharmacological: Tyrosine kinase inhibitor
FDA Approved Indications
- Renal cell carcinoma (advanced and metastatic)
- Gastrointestinal stromal tumor (GIST) refractory to imatinib or imatinib-intolerant
Mechanism of Action
Sunitinib inhibits multiple receptor tyrosine kinases, including VEGFR and PDGFR, leading to angiogenesis inhibition and tumor cell proliferation suppression.
Dosage and Administration
Adult: 50 mg once daily, 4 weeks on treatment followed by 2 weeks off (6-week cycle); dose adjustments may be necessary based on tolerance and side effects.
Pediatric: Not established for pediatric use.
Geriatric: Use with caution; no specific dose adjustments required but consider renal and hepatic function.
Renal Impairment: Adjust dose based on severity; severe impairment may require dose reduction.
Hepatic Impairment: Adjust dose in patients with hepatic dysfunction.
Pharmacokinetics
Absorption: Well absorbed orally, peak plasma concentration in 6-12 hours.
Distribution: High protein binding (~95%).
Metabolism: Metabolized by the liver, primarily via CYP3A4/5.
Excretion: Excreted mainly in feces; minor urinary excretion.
Half Life: Approx. 40-86 hours, allowing for once-daily dosing.
Contraindications
- Hypersensitivity to sunitinib or any component of the formulation.
Precautions
- Monitor for bleeding, hypertension, hypothyroidism, hepatic impairment, cardiotoxicity, and GI perforation or fistulae. Risks during pregnancy and lactation.
Adverse Reactions - Common
- Fatigue (Very common)
- Nausea (Very common)
- Diarrhea (Very common)
- Hand-foot syndrome (Common)
- Hypertension (Common)
Adverse Reactions - Serious
- Cardiotoxicity (heart failure, decreased ejection fraction) (Uncommon)
- Bleeding (hemorrhage) (Uncommon)
- Hepatotoxicity (Uncommon)
- GI perforation or fistulae (Rare)
- Severe bleeding or thrombosis (Rare)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin) may increase sunitinib levels.
- CYP3A4 inducers (e.g., rifampin) may decrease effectiveness.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood pressure, cardiac function, hepatic enzymes, and complete blood count.
Diagnoses:
- Risk for bleeding
- Impaired skin integrity due to hand-foot syndrome
- Risk for hypertension
Implementation: Administer with or without food; monitor for side effects and toxicities.
Evaluation: Assess for tumor response, tolerance to therapy, and adverse effects.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any signs of bleeding, severe fatigue, chest pain, or signs of infection.
- Avoid grapefruit and its juice, as it may increase drug levels.
Special Considerations
Black Box Warnings:
- Hepatotoxicity, hemorrhage, impairment of wound healing, cardiac failure.
Genetic Factors: None specified.
Lab Test Interference: May cause false-positive urine protein tests.
Overdose Management
Signs/Symptoms: Severe bleeding, hypotension, or adverse effects typical of toxicity.
Treatment: Supportive care; no specific antidote. Remove the drug and provide symptomatic treatment.
Storage and Handling
Storage: Store at room temperature, 20-25°C (68-77°F).
Stability: Stable when stored properly; check expiration date before use.