Vidaza, Onureg, Astamin
Generic Name
azacitidine
Manufacturer
Bristol Myers Squibb (original), various generics
Country
USA (original approval)
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Description
Overview of the medicine
Azacitidine is a pyrimidine nucleoside analog of cytidine. It is a hypomethylating agent used to treat myelodysplastic syndromes (MDS) and certain types of acute myeloid leukemia (AML). It works by inhibiting DNA methyltransferases, leading to hypomethylation of DNA and subsequent cell differentiation and apoptosis.
Uses & Indications
Dosage
Adults
Injectable: 75 mg/m² subcutaneously or intravenously daily for 7 days, repeated every 28 days for a minimum of 4 cycles. Oral (Onureg): 300 mg once daily for 14 days of a 28-day cycle, continued as long as clinical benefit is observed.
Elderly
No specific dose adjustments needed based on age alone, but monitor closely for adverse reactions.
Renal_impairment
Initial dose of 75 mg/m² is recommended; reduce dose or extend treatment interval if unexplained reductions in serum bicarbonate or renal impairment occur.
How to Take
For injection, reconstitute with sterile water for injection and administer subcutaneously or intravenously. For oral tablets, take whole with or without food, around the same time each day. Do not crush or chew tablets.
Mechanism of Action
Azacitidine is incorporated into DNA and RNA. In DNA, it covalently binds to and inhibits DNA methyltransferases (DNMTs), leading to hypomethylation of newly synthesized DNA. This hypomethylation can restore normal function to genes that are critical for cell differentiation and proliferation, which are often silenced in cancer cells. In RNA, it is thought to interfere with RNA synthesis.
Pharmacokinetics
Onset
Therapeutic effects are typically observed after multiple treatment cycles (usually 4-6 cycles).
Excretion
Primarily renal excretion (approximately 85% of the dose within 24 hours, mainly as metabolites). Minimal fecal excretion.
Half life
Approximately 1 to 4 hours (parenteral), ~30 minutes (oral).
Absorption
Subcutaneous (SC): Rapidly absorbed, peak plasma concentration reached in 0.5-1 hour. Oral: Bioavailability is low and variable, about 11%.
Metabolism
Primarily metabolized by hydrolysis (non-enzymatic and via cytidine deaminase) in the liver.
Side Effects
Contraindications
- Hypersensitivity to azacitidine or mannitol.
- Severe hepatic impairment (for oral formulation).
- Breastfeeding mothers.
Drug Interactions
Live vaccines
Avoid use with live or live-attenuated vaccines due to immunosuppression.
Cytotoxic agents
Potential for increased myelosuppression when given concurrently with other myelosuppressive chemotherapeutic agents.
Storage
Unopened vials of powder for injection should be stored refrigerated (2°C to 8°C or 36°F to 46°F). Oral tablets should be stored at room temperature (20°C to 25°C or 68°F to 77°F). Protect from light.
Overdose
Symptoms of overdose are primarily myelosuppression, including thrombocytopenia, leukopenia, and anemia. Gastrointestinal toxicity (nausea, vomiting, diarrhea) may also occur. Management is supportive care, including blood product transfusions and antimicrobials as needed.
Pregnancy & Lactation
Pregnancy Category D. Azacitidine can cause fetal harm when administered to a pregnant woman. Women of childbearing potential should use effective contraception. It is not known whether azacitidine is excreted in human milk, but due to potential for serious adverse reactions in breastfed infants, breastfeeding is contraindicated.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 2-3 years for unopened vials/blister packs when stored as recommended. Reconstituted solution shelf life is much shorter (e.g., 8 hours at room temperature, 22 hours refrigerated).
Availability
Hospitals and specialized pharmacies
Approval Status
FDA approved
Patent Status
Patent expired, generics available
Clinical Trials
Azacitidine continues to be investigated in various clinical trials for its use in other hematologic malignancies, combination therapies, and different dosing regimens to improve efficacy and reduce toxicity.
Lab Monitoring
- Complete blood counts (CBC) with differential before each cycle and as needed to monitor for myelosuppression.
- Liver function tests (LFTs) before each cycle.
- Renal function tests (RFTs) before each cycle.
- Serum electrolytes periodically.
Doctor Notes
- Careful monitoring of CBC, LFTs, and RFTs is crucial throughout treatment.
- Be aware of potential for severe myelosuppression and manage with dose adjustments or supportive care.
- Educate patients on signs of infection and bleeding and emphasize prompt reporting.
- Consider antiemetic prophylaxis for injectable azacitidine.
Patient Guidelines
- Report any signs of infection (fever, chills) or bleeding/bruising immediately.
- Maintain adequate hydration during treatment.
- Use antiemetics as prescribed to manage nausea and vomiting.
- Avoid contact with people who are sick or have infections.
- Follow all instructions regarding dose and administration precisely.
Missed Dose Advice
If a dose is missed, contact your doctor immediately. Do not take a double dose to make up for a missed dose. Follow your doctor's instructions.
Driving Precautions
Azacitidine may cause fatigue, dizziness, or weakness. Patients should be cautious when driving or operating machinery until they know how the drug affects them.
Lifestyle Advice
- Practice good hand hygiene and avoid crowded places to reduce infection risk.
- Discuss fertility preservation options before starting treatment.
- Avoid consuming raw or undercooked foods to minimize foodborne illness risk.
- Report any unusual bleeding or bruising.
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