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What is the mechanism of action for cyclophosphamide?
MECHANISM OF ACTION: Cyclophosphamide is an alkylating agent of the nitrogen mustard type. 2 An activated form of cyclophosphamide, phosphoramide mustard, alkylates, or binds, to DNA. Its cytotoxic effect is mainly due to cross-linking of strands of DNA and RNA, and to inhibition of protein synthesis.
What is cyclophosphamide pharmacokinetics?
It remains one of the most useful anticancer agents, and is also widely used for its immunosuppressive properties. Cyclophosphamide is inactive until it undergoes hepatic transformation to form 4-hydroxycyclophosphamide, which then breaks down to form the ultimate alkylating agent, phosphoramide mustard.
What is the target of cyclophosphamide?
5.14. Cyclophosphamide is converted to active metabolites in the liver, one of the major active metabolites being 4-hydroxycyclophosphamide, and targets rapidly proliferating malignant cells.
What is the route of administration of cyclophosphamide?
It is usually given through a vein by injection or infusion (intravenous, IV) or by mouth in tablet form, depending upon diagnosis. Cyclophosphamide is also approved to be given by a shot into a muscle (IM), into the abdominal lining (intraperitoneal, IP), or into the lining of the lung (intrapleural).
How does cyclophosphamide work on a cellular level?
The ability of cyclophosphamide to kill cancer cells depends on its ability to halt cell division. Usually, the drug works by damaging the RNA or DNA that tells the cell how to copy itself in division. If the cells are unable to divide, they die.
Does cyclophosphamide cross the blood brain barrier?
In contrast, cyclophosphamide (CYC), an alkylating agent, penetrates the blood—brain barrier and CNS parenchyma well.
What drugs interact with cyclophosphamide?
Some products that may interact with this drug include: allopurinol, chloramphenicol, chloroquine, digoxin, phenobarbital, phenothiazines, primidone, St John’s wort, turmeric (curcumin), voclosporin.
Why is cyclophosphamide a prodrug?
Cyclophosphamide is actually a prodrug, converted in the liver by mixed–function oxidase enzymes to the active metabolites 4-hydroxy–cyclophosphamide and phosphoramide mustard. The result is the binding of these agents to and the cross–linking of DNA, thus inhibiting cell proliferation and function.
Why mesna is used with cyclophosphamide?
Mesna, sold under the brand name Mesnex among others, is a medication used in those taking cyclophosphamide or ifosfamide to decrease the risk of bleeding from the bladder.
How is cyclophosphamide metabolized in the body?
London: The Chemical Society, 1975., p. 473 Cyclophosphamide is well absorbed orally, and peak plasma levels appear about one hour after oral use. It is also administered intravenously. This drug is metabolized in the liver to the cytotoxic metabolite, 4-hydroxycyclophosphamide, which is in equilibrium with the acyclic tautomer, aldophosphamide.
What is the effect of cyclophosphamide on DNA?
The previous IARC Monograph (IARC, 1987b) states that cyclophosphamide was found to bind to kidney, liver and lung DNA in mice. It also induced dominant lethality, chromosomal aberrations, micronuclei, sister chromatid exchange, mutations, and DNA damage in rodents in vivo.
How is cyclophosphamide used to treat lymphoma?
Cyclophosphamide can be used to cause immunologically mediated regression of the immunogenic, cyclophosphamide-resistant L5178Y lymphoma in syngeneic and semisyngeneic mice (B6D2F1 (C57BL/6 x DBA/2) females).
How do you make cyclophosphamide?
Cyclophosphamide can be prepared by treating N,N-bis (B-chloroethyl)-phosphamide dichloride with propanolamine in the presence of trimethylamine and dioxane. IARC. Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans.