Cytoxan: Advanced Alkylating Agent for Targeted Cancer Therapy
Cytoxan
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Synonyms | |||
Cytoxan (cyclophosphamide) is a potent alkylating chemotherapeutic agent belonging to the nitrogen mustard class, widely utilized in oncology and immunology for its cytotoxic and immunosuppressive properties. As a prodrug requiring hepatic activation, it offers a targeted mechanism of action that disrupts DNA replication and transcription in rapidly dividing cells. Its clinical versatility spans numerous malignancies, autoimmune conditions, and preparative regimens for hematopoietic stem cell transplantation, establishing it as a cornerstone in multimodal treatment protocols. This comprehensive profile details its pharmacological characteristics, therapeutic applications, and essential safety considerations for healthcare professionals.
Features
- Prodrug formulation requiring cytochrome P450-mediated activation to 4-hydroxycyclophosphamide
- Bifunctional alkylating activity causing DNA cross-links and strand breaks
- Broad spectrum of antineoplastic activity against hematologic and solid tumors
- Variable oral bioavailability (≥75%) with extensive tissue distribution
- Elimination primarily renal (5-25% unchanged) with plasma half-life of 3-12 hours
- Available as oral tablets (25mg, 50mg) and IV formulations (100mg, 200mg, 500mg, 1g, 2g vials)
Benefits
- Induces tumor cell apoptosis through irreversible DNA damage and inhibition of protein synthesis
- Demonstrates synergistic effects when combined with other chemotherapeutic agents
- Provides flexible administration routes (oral and intravenous) for tailored treatment regimens
- Enables dose escalation in transplant protocols due to predictable hematologic toxicity
- Shows efficacy in treatment-resistant malignancies through multi-mechanistic action
- Permits long-term management of autoimmune disorders through immunomodulatory effects
Common use
Cyclophosphamide is indicated for the treatment of various malignant conditions including Hodgkin lymphoma, non-Hodgkin lymphoma, multiple myeloma, leukemias, mycosis fungoides, neuroblastoma, retinoblastoma, breast cancer, and ovarian adenocarcinoma. It is also employed in severe autoimmune disorders such as granulomatosis with polyangiitis, microscopic polyangiitis, and severe rheumatoid arthritis unresponsive to conventional therapies. In transplant medicine, it serves as a conditioning agent prior to bone marrow transplantation. Off-label uses include treatment of nephrotic syndrome, systemic lupus erythematosus, and other immune-mediated conditions where conventional immunosuppressants have proven inadequate.
Dosage and direction
Oral Administration: Typically initiated at 1-5 mg/kg/day depending on indication and patient status. For autoimmune conditions, doses generally range from 1-2 mg/kg/day. Higher doses (2-5 mg/kg/day) are used for neoplastic diseases.
Intravenous Administration: Varies significantly by protocol:
- Single agent: 40-50 mg/kg in divided doses over 2-5 days
- Combination chemotherapy: 500-1500 mg/m²
- Transplant conditioning: 50-60 mg/kg/day for 2-4 days
Dosage must be adjusted based on hematologic parameters, renal function (CrCl <25 mL/min requires 75% dose reduction), hepatic impairment, and previous radiation or chemotherapy. Administration should be followed by adequate hydration (minimum 2L daily) to prevent hemorrhagic cystitis. Morning administration is preferred to allow for adequate fluid intake and urinary excretion during waking hours.
Precautions
Complete blood counts should be monitored weekly during treatment and for at least 3 weeks after discontinuation. Urinalysis should be performed regularly to detect hemorrhagic cystitis. Cardiac function monitoring is recommended in patients receiving high doses (>100 mg/kg) or with preexisting cardiac conditions. Pulmonary function tests should be considered in patients developing respiratory symptoms. Fertility preservation options should be discussed before initiation due to high risk of gonadal toxicity. Patients should be advised to use effective contraception during and for at least 12 months after treatment completion. Vaccination with live vaccines is contraindicated during treatment.
Contraindications
Hypersensitivity to cyclophosphamide or any component of the formulation. Urinary outflow obstruction. Active urinary tract infection. Severely depressed bone marrow function (neutrophils <1500/mm³, platelets <50,000/mm³). Pregnancy and breastfeeding. Concurrent administration with live vaccines. Severe hepatic impairment (Child-Pugh Class C). Acute infections requiring active treatment.
Possible side effect
Hematologic: Myelosuppression (neutropenia typically nadir 7-14 days, recovery by day 21), thrombocytopenia, anemia, leukopenia Genitourinary: Hemorrhagic cystitis (5-40%), bladder fibrosis, renal tubular necrosis, hematuria Gastrointestinal: Nausea and vomiting (dose-related), mucositis, diarrhea, anorexia, hepatotoxicity Dermatologic: Alopecia (reversible upon discontinuation), skin pigmentation, nail changes Pulmonary: Interstitial pneumonitis, pulmonary fibrosis (especially with cumulative doses >100g) Cardiac: Cardiotoxicity with high doses (hemorrhagic myocarditis, pericarditis, heart failure) Reproductive: Amenorrhea, azoospermia, infertility (dose and age-dependent) Oncologic: Secondary malignancies (bladder cancer, myelodysplasia, acute leukemia) Other: Syndrome of inappropriate antidiuretic hormone, anaphylaxis, fatigue, fever
Drug interaction
Allopurinol: May enhance bone marrow suppression Cardiotoxic agents (anthracyclines): Increased risk of cardiac toxicity CYP2B6 inducers (rifampin, phenobarbital): May increase activation to toxic metabolites CYP2B6 inhibitors (fluoxetine, paroxetine): May decrease efficacy Succinylcholine: Prolonged apnea due to decreased pseudocholinesterase activity Live vaccines: Diminished immune response and increased vaccine-related complications Nephrotoxic agents (aminoglycosides, NSAIDs): Enhanced renal toxicity Radiation therapy: Enhanced toxicity to irradiated tissues
Missed dose
If a dose is missed, administer as soon as possible unless it is接近 the next scheduled dose. Do not double the dose to make up for a missed dose. For oral administration, if remembered within 12 hours of scheduled time, take immediately and resume regular schedule. If beyond 12 hours, skip the missed dose and resume normal schedule. Contact treating physician for specific guidance regarding IV administration schedules. Document all missed doses in medication administration record.
Overdose
Manifestations include severe bone marrow suppression, cardiotoxicity, hemorrhagic cystitis, and water intoxication. Management requires immediate discontinuation, supportive care including transfusion support, mesna administration for bladder protection, and aggressive hydration. Leukocyte growth factors may be administered for severe neutropenia. Hemodialysis may remove up to 30% of unmetabolized drug but is ineffective for active metabolites. Consultation with poison control center and hematology/oncology specialist is mandatory.
Storage
Store at controlled room temperature (20-25°C/68-77°F). Protect from light and moisture. Keep in original container with desiccant. Oral tablets should be kept in tightly closed containers. Reconstituted IV solution is stable for 24 hours at room temperature or 6 days refrigerated. Do not freeze. Keep out of reach of children and pets. Dispose of unused medication through approved pharmaceutical waste programs.
Disclaimer
This information is intended for healthcare professionals and should not replace clinical judgment. Dosage and administration must be determined by qualified physicians based on individual patient characteristics. Treatment protocols may vary based on institutional guidelines and evolving clinical evidence. Patients should be fully informed of benefits and risks before initiation. Regular monitoring and dose adjustments are essential for safe administration.
Reviews
“Cyclophosphamide remains a fundamental component of our lymphoma protocols, demonstrating consistent efficacy particularly in combination regimens. The predictable myelosuppression allows for appropriate supportive care planning.” - Hematologic Oncologist, Academic Medical Center
“In rheumatoid vasculitis cases refractory to conventional DMARDs, cyclophosphamide has proven invaluable. The oral administration option facilitates long-term management, though vigilant monitoring for bladder toxicity is mandatory.” - Rheumatologist, Tertiary Care Facility
“The dose-dependent toxicity profile requires careful patient selection and monitoring. While the risk of hemorrhagic cystitis has decreased with mesna prophylaxis, gonadal toxicity remains a significant concern for younger patients.” - Transplant Specialist