Drug Guide
Temsirolimus
Classification
Therapeutic: Antineoplastic Agent
Pharmacological: mTOR Inhibitor
FDA Approved Indications
- Treatment of advanced renal cell carcinoma (RCC)
Mechanism of Action
Temsirolimus inhibits the mammalian target of rapamycin (mTOR) pathway, which is involved in cell growth, proliferation, and angiogenesis, thereby inhibiting tumor cell growth and angiogenesis.
Dosage and Administration
Adult: 25 mg IV weekly over 30–60 minutes
Pediatric: Not approved for pediatric use
Geriatric: No specific dosage adjustments recommended based on age alone, but consider renal and hepatic function
Renal Impairment: Use with caution; no specific dose adjustment, monitor renal function
Hepatic Impairment: Use with caution; reduce dose in severe hepatic impairment; no specific dose adjustment for mild to moderate impairment
Pharmacokinetics
Absorption: Administered intravenously, bypassing absorption issues
Distribution: Extensively bound to plasma proteins
Metabolism: Metabolized primarily via CYP3A4/5 enzymes
Excretion: Excreted mainly in feces, minimal urinary excretion
Half Life: Approximately 14–18 hours
Contraindications
- Known hypersensitivity to temsirolimus or its components
Precautions
- Use in patients with pre-existing lymphopenia, active infection, bleeding disorders, hepatic impairment, or renal impairment; monitor blood counts and hepatic function regularly
Adverse Reactions - Common
- Mucositis/stomatitis (Common)
- Fatigue (Common)
- Nausea and vomiting (Common)
- Hyperglycemia (Common)
- Hyperlipidemia (Common)
- Thrombocytopenia (Common)
Adverse Reactions - Serious
- Interstitial lung disease/pneumonitis (Serious but rare)
- Severe infection (Rare)
- Anaphylaxis (Rare)
- Hepatotoxicity (Rare)
Drug-Drug Interactions
- CYP3A4 inducers (e.g., rifampin), CYP3A4 inhibitors (e.g., ketoconazole)
Drug-Food Interactions
- Grapefruit and grapefruit juice (may inhibit CYP3A4)
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor blood counts, liver and renal function, lipid profile, signs of infection, and pulmonary symptoms before and during therapy
Diagnoses:
- Risk for infection
- Impaired skin integrity
- Risk for bleeding
Implementation: Administer IV as scheduled, monitor for adverse effects, educate patient on signs of toxicity and infection, manage mucositis with appropriate care
Evaluation: Assess response to therapy through imaging, monitor lab values and side effects, ensure patient adheres to scheduled assessments
Patient/Family Teaching
- Report signs of infection, bleeding, or lung problems promptly
- Maintain good skin and oral hygiene
- Follow dietary and activity recommendations
- Understand the importance of regular lab monitoring
Special Considerations
Black Box Warnings:
- Risk of infection and pulmonary toxicity (pneumonitis/Interstitial lung disease)
Genetic Factors: No specific genetic testing recommended, but pharmacogenomic data may influence metabolism
Lab Test Interference: May cause elevated lipid levels, hyperglycemia, and abnormal liver function tests
Overdose Management
Signs/Symptoms: Severe mucositis, infection, pulmonary symptoms, thrombocytopenia
Treatment: Supportive care, monitor vital signs and labs, consider hospitalization for severe reactions, no specific antidote
Storage and Handling
Storage: Store at room temperature (20°C to 25°C), protected from light
Stability: Stable for the duration of the labeled expiration date when stored properly