Cytoxan (Cyclophosphamide)
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Cytoxan (Cyclophosphamide) is an alkylating agent used in the treatment of various cancers and autoimmune conditions. It works by cross-linking DNA strands, thereby inhibiting cell replication and promoting cell death in rapidly dividing cancer cells. Cytoxan is used for breast cancer, leukemia, lymphoma, multiple myeloma, nephrotic syndrome, and lupus. It can be administered orally or via IV, with dosage based on body surface area and treatment indication.

Cyclophosphamide

Other Popular and Common Names
Generic Cytoxan

Endoxan

Cycloblastin

Procytox

Cytophosphane

Cyclophosphamide is a nitrogen mustard alkylating agent. After hepatic activation to its active metabolites (phosphoramide mustard and acrolein), it binds to DNA through alkylation. This leads to the formation of cross-links between DNA strands, ultimately causing cell cycle arrest and apoptosis, particularly in rapidly proliferating cells such as cancer or immune cells.

Breast cancer

Ovarian cancer

Non-Hodgkin’s lymphoma

Hodgkin’s lymphoma

Chronic lymphocytic leukemia (CLL)

Multiple myeloma

Neuroblastoma

Retinoblastoma

Non-Oncologic Uses (Immunosuppressive):
Systemic lupus erythematosus (SLE)

Severe rheumatoid arthritis

Nephrotic syndrome (especially in children)

ANCA-associated vasculitis (e.g., granulomatosis with polyangiitis)

Scleroderma (diffuse cutaneous systemic sclerosis)

Cancer Therapy (IV or Oral):
Initial dose: 40–50 mg/kg over 2–5 days or 3–5 mg/kg/day

Maintenance: Based on treatment cycles, blood counts, and tolerability

Immunosuppression (Lupus, Vasculitis):
IV pulse therapy: 500–1000 mg/m² monthly

Oral daily dose: 1–3 mg/kg/day (titrated carefully)

Calculated by body surface area (BSA) or weight

Requires close renal, hepatic, and hematologic monitoring

Administration Notes:

Ensure adequate hydration to prevent hemorrhagic cystitis

Administer mesna (a uroprotectant) when appropriate

IV form must be prepared under sterile chemotherapy handling protocols

Drug Class: Alkylating Agent (Cytotoxic/Antineoplastic)

Legal Classification: Schedule H (Rx Only)

Monitoring Required: CBC, renal and liver function, urinalysis (hematuria), fertility preservation

Pregnancy Category: D (Positive evidence of fetal risk)

Teratogenic: Avoid use in pregnancy unless absolutely necessary

Fertility Effects: May cause ovarian failure or azoospermia—consider sperm or egg banking

Bladder Toxicity: Risk of hemorrhagic cystitis due to acrolein

Immunosuppression: Increases infection risk—monitor closely

Secondary Malignancy Risk: Long-term use may increase risk of bladder cancer, leukemia

Nausea, vomiting

Hair loss (alopecia)

Anorexia

Diarrhea

Mouth ulcers (mucositis)

Fatigue

Low blood counts (anemia, neutropenia, thrombocytopenia)

Hemorrhagic cystitis

Bone marrow suppression

Pulmonary fibrosis

Cardiotoxicity (especially with high-dose therapy)

Infertility (temporary or permanent)

Secondary cancers (bladder, leukemia)

Hemorrhagic Cystitis: Always ensure hydration; consider mesna with high-dose IV regimens

Infection Risk: Avoid live vaccines; consider antimicrobial prophylaxis

Hepatic/Renal Impairment: Dose reduction may be required

Fertility: Pre-treatment counseling strongly recommended

Long-Term Risk: Monitor for signs of bladder cancer, bone marrow suppression

Drug/Class Interaction Clinical Guidance
Allopurinol Enhanced bone marrow toxicity Monitor CBC closely
Live vaccines Reduced vaccine efficacy, infection risk Avoid during and after therapy
Doxorubicin Increased cardiotoxicity Monitor cardiac function
Phenobarbital/phenytoin May alter cyclophosphamide metabolism Monitor efficacy and toxicity
Immunosuppressants (e.g., azathioprine) Additive bone marrow suppression Adjust doses, monitor CBC

Breast Cancer Adjuvant Therapy: Cyclophosphamide is part of CMF and AC chemotherapy regimens proven to improve survival
Reference: Early Breast Cancer Trialists’ Collaborative Group (EBCTCG), Lancet, 2012

Lupus Nephritis: IV cyclophosphamide pulse therapy improved renal outcomes in severe SLE
Reference: NIH Lupus Nephritis Trial (Austin et al., NEJM, 1986)

Wegener’s Granulomatosis (ANCA Vasculitis): Cyclophosphamide with steroids induces remission
Reference: Fauci et al., Ann Intern Med. 1991

FAQs – Cytoxan (Cyclophosphamide)
Q1. What is Cytoxan used for?
A: Cytoxan is used to treat cancers like lymphoma, leukemia, breast cancer, and autoimmune conditions like lupus, nephrotic syndrome, and vasculitis.

Q2. Is Cytoxan a chemotherapy drug?
A: Yes, Cytoxan is an alkylating chemotherapeutic agent that kills rapidly dividing cells.

Q3. Can Cytoxan cause infertility?
A: Yes, especially with long-term or high-dose use. It can affect sperm or egg production.

Q4. How is Cytoxan administered?
A: It is available in both oral tablet and intravenous injection forms. The route depends on the condition and treatment plan.

Q5. How can bladder toxicity be prevented during treatment?
A: Adequate hydration and use of mesna help reduce the risk of hemorrhagic cystitis caused by Cytoxan.

Q6. Does Cytoxan suppress the immune system?
A: Yes, it can suppress white blood cells, increasing susceptibility to infections.

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