Drug Guide
Azacitidine
Classification
Therapeutic: Antineoplastic agent
Pharmacological: DNA methyltransferase inhibitor
FDA Approved Indications
- Myelodysplastic syndromes (MDS)
- Acute myeloid leukemia (AML) in certain settings
Mechanism of Action
Azacitidine incorporates into DNA and RNA, leading to hypomethylation of DNA and restoration of normal gene function, which inhibits abnormal cell growth.
Dosage and Administration
Adult: For MDS: 75 mg/m² subcutaneously or intravenously once daily for 7 days every 28 days. For AML: dosage varies based on patient status and specific protocols.
Pediatric: Not typically used in pediatric populations; consult specialized protocols.
Geriatric: Use with caution; adjust based on renal and hepatic function.
Renal Impairment: Adjust dosage based on severity; monitor renal function.
Hepatic Impairment: Use with caution; no specific dose adjustment established.
Pharmacokinetics
Absorption: Moderately absorbed after subcutaneous or IV administration.
Distribution: Widely distributed; crosses cell membranes via passive diffusion.
Metabolism: Metabolized primarily in the liver via cytidine deaminase.
Excretion: Excreted mainly in urine.
Half Life: Approximately 4-10 hours.
Contraindications
- Hypersensitivity to azacitidine or any component of the formulation.
Precautions
- Myelosuppression observation required.
- Monitoring liver and kidney function.
- Use with caution in pregnant or breastfeeding women.
Adverse Reactions - Common
- Nausea (Common)
- Vomiting (Common)
- Fatigue (Common)
- Thrombocytopenia (Common)
- Neutropenia (Common)
Adverse Reactions - Serious
- Severe myelosuppression (Serious)
- Infection (Serious)
- Bleeding complications (Serious)
- Gastrointestinal toxicity (Serious)
Drug-Drug Interactions
- Myelosuppressive agents (increased risk of myelosuppression)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor complete blood counts, renal and hepatic function.
Diagnoses:
- Risk for infection
- Risk of bleeding
- Impaired tissue perfusion
Implementation: Administer as prescribed, monitor for adverse effects, educate patient about signs of infection and bleeding.
Evaluation: Assess blood counts regularly, evaluate for side effects, monitor response to therapy.
Patient/Family Teaching
- Report signs of infection (fever, chills).
- Avoid invasive procedures without medical advice.
- Use effective contraception during treatment and for some time after.
- Follow scheduling and laboratory monitoring strictly.
- Report any unusual bleeding, bruising, or symptoms of anemia.
Special Considerations
Black Box Warnings:
- Myelosuppression, including neutropenia, thrombocytopenia, and anemia, which can be severe and lead to death.
Genetic Factors: No specific genetic screening required, but response may vary based on disease genetics.
Lab Test Interference: May cause false elevation of serum bilirubin levels.
Overdose Management
Signs/Symptoms: Severe myelosuppression, bleeding, infections.
Treatment: Supportive care, including blood product support and antibiotics; no specific antidote.
Storage and Handling
Storage: Store in a refrigerator at 2°C to 8°C (36°F to 46°F). Protect from light.
Stability: Stable for up to 24 hours at room temperature once reconstituted; reconstituted solution stable for up to 8 hours.