Brands, Medical Use, Clinical Data
Drug Category
- Antineoplastic Agents
- Antirheumatic Agents
- Immunosuppressive Agents
Dosage Forms
- Oral tablets
- Oral liquid
- Parenteral solution
Brands / Synonyms
ASTA; Asta B 518; Clafen; Claphene; CP; CPA; CTX; CY; Cyclophosphamid; Cyclophosphamide; Cyclophosphamide Monohydrate; Cyclophosphamide Sterile; Cyclophosphamidum; Cyclophosphan; Cyclophosphane; Cyclophosphoramide; Cyclostin; Cyklofosfamid; Cytophosphan; Cytoxan; Cytoxan Lyoph; Endoxan; Endoxan R; Endoxan-Asta; Endoxana; Endoxanal; Endoxane; Enduxan; Genoxal; Hexadrin; Lyophilized Cytoxan; Mitoxan; Neosar; Procytox; Rcra Waste Number U058; Semdoxan; Sendoxan; Senduxan; Zyklophosphamid
Indications
For management of malignant lymphomas, multiple myeloma,leukemias, mycosis fungoides (advanced disease), neuroblastoma (disseminated disease), adenocarcinoma of the ovary, retinoblastoma and carcinoma of the breast
Pharmacology
Cyclophosphamide is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.
Mechanism of Action
Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.
Absorption
90-100%
Toxicity
infection, myelosuppression, and cardiac toxicity
Biotrnasformation / Drug Metabolism
hepatic
Contraindications
Continued use of cyclophosphamide is contraindicated in patients with severely depressed bone marrow function. Cyclophosphamide is contraindicated in patients who have demonstrated a previous hypersensitivity to it.
Drug Interactions
The rate of metabolism and the leukopenic activity of cyclophosphamide reportedly are increased by chronic
administration of high doses of phenobarbital.
The physician should be alert for possible combined drug actions, desirable or undesirable, involving
cyclophosphamide even though cyclophosphamide has been used successfully concurrently with other drugs, including
other cytotoxic drugs.
Cyclophosphamide treatment, which causes a marked and persistent inhibition of cholinesterase activity,
potentiates the effect of succinylcholine chloride.
If a patient has been treated with cyclophosphamide within 10 days of general anesthesia, the anesthesiologist
should be alerted.
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