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cyclophosphamide (Rx)Brand and Other Names:Cytoxan

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

powder for injection

  • 500mg
  • 1g
  • 2g

tablet

  • 25mg
  • 50mg
more...

Malignant Diseases

IV (intermittent therapy): 40-50 mg/kg (400-1800 mg/m²) divided over 2-5 days; may be repeated at intervals of 2-4 weeks  

IV (continuous daily therapy): 60-120 mg/m²/day (1-2.5 mg/kg/day)

PO (intermittent therapy): 400-1000 mg/m² divided over 4-5 days

PO (continuous daily therapy): 50-100 mg/m²/day or 1-5 mg/kg/day 

Nephrotic Syndrome

2-3 mg/kg/day for up to 12 weeks when corticosteroids unsuccessful 

Non-Hodgkin Lymphoma

600-1500 mg/m² IV with other antineoplastics (part of CHOP regimen); dose intensification possible 

Breast Cancer

600 mg/m² IV with other antineoplastics; dose intensification possible 

Juvenile Idiopathic Arthritis/Vasculitis (Off-label)

10 mg/kg IV every 2 weeks 

Lupus Nephritis (Off-Label)

Induction therapy for lupus nephritis (American College of Rheumatology Guidelines 2012)

Low-dose: 500 mg IV every 2 weeks for 6 doses plus corticosteroids, then maintenance with mycophenolate mofetil or azathioprine

High-dose: 500-1000 mg/m² IV monthly for 6 doses plus corticosteroids

Systemic Sclerosis (Orphan)

Prevention of graft-versus-host disease after allogeneic hematopoietic stem cell transplant

Orphan designation sponsor

  • Accentia Biopharmaceuticals, 324 South Hyde Avenue, Suite 350, Tampa, FL 33606

Dosing Modifications

Hepatic impariment: Give 75% of normal dose if transaminase levels are >3 times upper limit of normal or bilirubin is 3.1-5 mg/dL

Renal impairment: CrCl <10 mL/min, give 75% of normal dose; CrCl >10 mL/min, give full dose 

Dosage Forms & Strengths

powder for injection

  • 500mg
  • 1g
  • 2g

tablet

  • 25mg
  • 50mg
more...

Malignant Diseases

IV (intermittent therapy): 40-50 mg/kg (400-1800 mg/m²) divided over 2-5 days; may be repeated at intervals of 2-4 weeks  

IV (continuous daily therapy): 60-120 mg/m²/day (1-2.5 mg/kg/day)

PO (intermittent therapy): 400-1000 mg/m² divided over 4-5 days

PO (continuous daily therapy): 50-100 mg/m²/day  

Juvenile Idiopathic Arthritis/Vasculitis

10 mg/kg IV every 2 weeks 

Nephrotic Syndrome

2-3 mg/kg/day for up to 12 weeks when corticosteroids unsuccessful 

Systemic Lupus Erythematosus

500-750 mg/m² IV monthly; not to exceed 1 g/m² 

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Interactions

Interaction Checker

cyclophosphamide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
             activity indicator 

            >10%

            Alopecia (40-60%)

            Nausea and vomiting

            GI toxicity

            Leukopenia

            Amenorrhea

            Sterility

            1-10%

            Facial flushing

            Headache

            Rash

            Syndrome of inappropriate antidiuretic hormone secretion (SIADH)

            Nasal congestion

            Frequency Not Defined

            Cardiomyopathy, CHF (high dose)

            Stevens-Johnson syndrome

            Toxic epidermal necrolysis (rare)

            Hemorrhagic cystitis

            Azoospermia

            Oligozoospermia

            Interstitial pneumonia

            Infectious disease

            Secondary malignancies: Urinary bladder, myeloproliferative, lymphoproliferative

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            Warnings

            Contraindications

            Severe myelosuppression

            Hypersensitivity

            Cautions

            Use with caution in patients with hepatic or renal impairment, leukopenia, thrombocytopenia, recent radiation therapy or chemotherapy

            Pelvic irradiation potentiates hemorrhagic cystitis

            Potential for radiation recall when used in conjunction with radiation therapy

            Risk of potentially fatal and irreversible interstitial pulmonary fibrosis if given over prolonged periods

            May cause infertility in male patients who received high doses as children

            Monitor for secondary malignancies

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            Pregnancy & Lactation

            Pregnancy category: D

            Lactation: Drug excreted in breast milk; do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Metabolites interfere with malignant cell growth by cross-linking tumor cell DNA; drug does not have specificity for any phase of the cell cycle; also has potent immunosuppressive activity

            Absorption

            Bioavailability: 75%

            Onset: 2-3 hr

            Peak plasma time: Cyclophosphamide, 1 hr; metabolites, 2-3 hr

            Distribution

            Protein bound: Cyclophosphamide, low; metabolites, >60%

            Vd: 0.48-0.71 L/kg

            Metabolism

            Metabolized by liver

            Metabolites: 4-hydroperoxycyclophosphamide, 4-aldophosphamide

            Elimination

            Half-life: 3-12 hr

            Excretion: Urine

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            Administration

            Give dose early in day

            Patients should drink plenty of fluids with PO doses

            Patients should empty bladder frequently to prevent hemorrhagic cystitis

            Sometimes, mesna is used concomitantly as prophylaxis against hemorrhagic cystitis

            Monitor blood counts during therapy (WBC count may decrease to 2000-3000/μL without serious risk of infection)

            May be administered IM, intraperitoneally, intrapleurally, by IV piggy-back, or by continuous IV infusion    

            IV Incompatibilities

            Y-site: Amphotericin B cholesteryl sulfate

            IV Compatibilities

            Additive: Cisplatin/etoposide, fluorouracil, hydroxyzine, methotrexate, methotrexate/fluorouracil, mitoxantrone, ondansetron

            Syringe: Bleomycin, cisplatin, doxapram, doxorubicin, droperidol, furosemide, heparin, leucovorin, methotrexate, metoclopramide, mitomycin, vinblastine, vincristine

            Y-site (partial list): Allopurinol, amifostine, bleomycin, most cephalosporins, cisplatin, diphenhydramine, doxorubicin, doxorubicin liposomal, filgrastim, fluorouracil, furosemide, gemcitabine, linezolid, lorazepam, mitomycin, morphine, paclitaxel, prochlorperazine, propofol, sodium bicarbonate, trimethoprim/sulfamethoxazole, vancomycin, vinblastine, vincristine

            IV Preparation

            Maximum concentration of cyclophosphamide is limited to 20 mg/mL because of solubility

            IV push: Reconstitute with NS (do not use SWI, because it is hypotonic)

            Infusion: Reconstitute with SWI to concentration of 20 mg/mL

            May dilute further with D5W, NS, lactated Ringer solution, or other compatible fluids

            IV Administration

            Infusions may be administered over 1-2 hours

            Doses >500 mg up to ~1 g may be administered over 20-30 minutes

            To minimize bladder toxicity, increase normal fluid intake during and for 1-2 days after cyclophosphamide therapy; most adult patients will require fluid intake of at least 2 L/day; high-dose regimens should be accompanied by vigorous hydration with or without mesna therapy

            Storage

            Store intact vials at room temperature

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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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