Cyclophosphamide

Indications
 Oral
As part of the conditioning regimen in patients undergoing bone marrow transplantation
Adult: 60 mg/kg daily for 2 days.
Oral
Malignancies
Adult: Low-dose regimen: 2-6 mg/kg wkly in divided dose. May also be given as a single IV dose.
Intravenous
Malignancies
Adult: Moderate dose regimen: 10-15 mg/kg wkly; high dose regimen: 20-40 mg/kg every 10-20 days. Dosage may vary depending on the disease state, patient's condition, state of the bone marrow and whether it is used as a single agent or in combination regimens.
Contraindications
 Bladder haemorrhage. Patients with bone-marrow aplasia, acute infection, drug- or radiation-induced urothelial toxicity. Porphyria. Pregnancy and lactation.
Warnings / Precautions
 Blood disorders. Elderly or debilitated patients. Diabetic patients. Renal or hepatic impairment or who have gone adrenaloctomy. Previous treatment with x-ray or cytotoxic agents. Monitor haematological profile and presence of RBCs in urine regularly. Maintain adequate hydration and frequent micturition to reduce the risk of cystitis.
Adverse Reactions
 Congestive heart failure; leucopenia; poor wound healing; anorexia. Nausea, vomiting; alopoecia; oral mucosal ulceration; thrombocytopenia, anaemia; nonhaemorrhagic cystitis and/or fibrosis of the bladder; gonadal suppression, ovarian or skin and nail pigmentation, dermatitis, jaundice.
Potentially Fatal: Myelosuppression; haemorrhagic cystitis; interstitial pulmonary fibrosis; tachyarrhythmias and intractable heart failure (high doses). Increased risk of developing acute leukaemias.
Overdose Reactions
 Symptoms are mainly extensions of adverse reactions, especially severe leukopenia, thrombocytopenia and cardiotoxicity. Impairment of water excretion with hyponatremia, weight gain, and inappropriately concentrated urine has been reported. Treatment is supportive and there is no known specific antidote. Although cyclophosphamide theoretically is dialyzable, no studies have been done.
Drug Interactions
 Chronic high-dose administration of phenobarbital can increase the metabolism and leukopaenic activity of cyclophosphamide. Doxorubicin and daunorubicin increase risk of cardiotoxicity. Allopurinol may increase risk of bone marrow toxicity while chloramphenicol may increase the serum T1/2 of cyclophosphamide.
Potentially Fatal: Serious toxicity when combined with other myelotoxic drugs or radiotherapy.
See Below for More cyclophosphamide Drug Interactions
Mechanism of Actions
 Cyclophosphamide is a prodrug which is converted in the body to the active metabolites. It acts at any stage of the cell cycle but its main action is blockage at the G2 stage. It arrests cell division by alkylating the DNA in a dose-dependent manner. It also exerts immunosuppressive effects possibly due to a cytotoxic effect on lymphocytes.
Absorption: Well absorbed from the GI tract (oral).
Distribution: Widely distributed; crosses the blood-brain barrier and placenta; enters breast milk.
Metabolism: Hepatic; converted to 4-hydroxycyclophosphamide and aldophosphamide.
Excretion: Urine (as metabolites and unchanged drug).
Administration
 Should be taken on an empty stomach. (Preferably taken on an empty stomach, but may be taken w/ meals to minimise GI irritation. Ensure adequate fluid intake. Swallow whole.)
Storage Conditions
 Intravenous: Store below 25°C. Oral: Store below 25°C.
ATC Classification
 L01AA01 - cyclophosphamide ; Belongs to the class of alkylating agents, nitrogen mustard analogues. Used in the treatment of cancer.
Storage
 Intravenous: Store below 25°C. Oral: Store below 25°C.
Available As
  • Cyclophosphamide 100 mg
  • Cyclophosphamide 1000 mg
  • Cyclophosphamide 200 mg
  • Cyclophosphamide 50 mg
  • Cyclophosphamide 500 mg

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