Cyclophosphamide alkylating agent

CHOP Cyclophosphamide Alkylating agent Prodrug CYP 3A4/5, 2D6 Hemorrhagic cystitis... 

Cyclophosphamide Alkylating agent—attacks guanine N7—dysfunctional DNA Non-Hodgkin s, ovarian, breast CA, neuroblastoma BMS, mucositis, hemorrhagic cystitis (mesna, traps acrolein and is protective), hepatotoxicity (high dose)... 

Crisantaspase - chemotherapy of cancers Cyclophosphamide - alkylating agent, cancer chemotherapy Cytarabine - chemotherapy of leukaemia Dactinomycin - chemotherapy of cancers Dantrolene - skeletal muscle relaxant spasticity Desflurane - general anaesthetic... 

Cyclophosphamide Alkylating agent cancer Decreased T cells, B cells, and... 

Chemotherapeutic agents are grouped by cytotoxic mechanism. The alkylating agents, such as cyclophosphamide [50-18-0] and melphalan [148-82-3] interfere with normal cellular activity by alkylation deoxyribonucleic acid (DNA). Antimetabohtes, interfering with complex metaboHc pathways in the cell, include methotrexate [59-05-2] 5-fluorouracil [51-21-8] and cytosine arabinoside hydrochloride [69-74-9]. Antibiotics such as bleomycin [11056-06-7] and doxombicin [23214-92-8] h.a.ve been used, as have the plant alkaloids vincristine [57-22-7] and vinblastine [865-21-4]. 

Alkylating Agents. Figure 2 Biotransformation of cyclophosphamide - formation of inactive ( ) and toxic ( metabolites. 

Alkylating agents Cyclophosphamide Myelosuppression, hemorrhagic cystitis Alopecia, stomatitis, amenorrhea, aspermia, secondary leukemias... 

Risk factors for the development of AML include exposure to environmental toxins, Hispanic ethnicity, and genetics.6 Of greater concern is the increased prevalence of AML as a secondary malignancy, resulting from chemotherapy and radiation treatment for other cancers. Alkylating agents, such as ifosfamide and cyclophosphamide, and topoisomerase inhibitors, such as etoposide, are linked to an increased risk of myelodysplastic syndrome (MDS) and AML.8... 

Initial therapy frequently consists of an alkylating agent in conjunction with corticosteroids these regimens can be found in the CLL (chlorambucil, cyclophosphamide) and multiple... 

The answer is a. (Hardman, p 1302.) Cyclophosphamide, an alkylating agent, reacts with purine and pyrimidine bases of DNA to form bridges and dimers. These products interfere with DNA replication. 5-FU, methotrexate, and 6-thioguanine are anti metabolites, and the steroid prednisone has some tumor-suppressive effects. 

Alkylating agents Nitrogen mustards (cyclophosphamide) Busulphan Platinum coordination complexes (cisplatin) Nitrosoureas Crosshnks DNA strands... 

Cyclophosphamide is an antineoplastic agent that causes DNA cross-linking and abnormal base-pairing through a mechanism called alkylation, hence the name alkylating agent. Cyclophosphamide may also be used in resistant rheumatoid arthritis. 

Alkyl halides, alkyl sulfonates and other alkylating agents have also been subject to scmtiny in spheres other than pharmaceuticals, such as in environmental analysis. Various approaches have included two-step SPE, derivatisation with trifluoroacetic anhydride followed by GC/MS (for cyclophosphamide and its analogues in sewage water) SPE on surface water to isolate the antineoplastic agents carmustine, chlorambucil, cyclophosphamide and melphalan for LC-UV and LC-fluorescence measurements and derivatisation of alkyl halides and epoxides with 4-nitrothiophenol followed by HPLC-UV detection (claimed to be better than NBP derivatisation). A patent exists for a field test kit for mustard gases in military use based on NBP derivatisation. 

Alkylating agents are compounds capable of reacting covalently with DNA bases. If a compound of this type contains two reactive groups, intramolecular or intermolecular crosslinking of the DNA double helix and bending of the double strand occurs. Examples of this type shown here are cyclophosphamide and the inorganic complex cisplatin. Anthracyclines such as doxorubicin (adriamy-cin) insert themselves non-covalently between the bases and thus lead to local alterations in the DNA structure (see p. 254 B). 

Despite the fact that alkylating agents exhibit a common mechanism of action, their clinical use varies depending on differences in pharmacokinetics, metabolism, hpid solubility, ability to penetrate membranes, and toxicity. They can be classified as nitrogen-containing mustard derivatives (mechorethamine, chlorambucil, melfalan, cyclophosphamide, ifos-famide), derivatives of ethylenimine (thiotepa), nitrosoureas (carmustine, lomustine, strep-tozocin), alkylsulfonates (busulfan), and derivatives of platinum (cwplatin, carboplatin). 

Besides being used as an alkylating agent in cancer chemotherapy, cyclophosphamide is a unique drug when used as an immunosuppressant. First, it is the most powerful of all such drugs. Second, it kills proliferating cells, and evidently alkylates a certain region of... 

The alkylating agents can be considered to be cell-cycle independent drugs. They are used for the management of leukemias, lymphomas, multiple myeloma and some carcinoma s and soft tissue tumors, generally as components of drug combination regimens. Cyclophosphamide is also used for its marked immunosuppressant properties. 

The ability of certain anticancer agents to suppress both humoral and cellular immunity has been exploited in the field of organ transplantation and in diseases thought to be caused by an abnormal or heightened immune response. In particular, the alkylating agents cyclophosphamide and chlorambucil have been used in this context, as have several of the antimetabolites, including methotrexate, mercaptopurine, azathioprine. 

Cyclophosphamide (Cytoxan) is the most versatile and useful of the nitrogen mustards. Preclinical testing showed it to have a favorable therapeutic index and to possess the broadest spectrum of antitumor activity of all alkylating agents. As with the other nitrogen mustards, cyclophosphamide administration results in the formation of cross-links within DNA due to a reaction of the two chloroethyl moieties of cyclophosphamide with adjacent nucleotide bases. Cyclophosphamide must be activated metabofically by microsomal enzymes of the cytochrome P450 system before ionization of the chloride atoms and formation of the cyclic ethylenimmonium ion can occur. The metabolites phosphoramide mustard and acrolein are thought to be the ultimate active cytotoxic moiety derived from cyclophosphamide. 

Alkylating agents Cyclophosphamide (CYCLOXAN) 2-3 mg/kg/day oral 10-15 mg/kg IV every 7-10 days... 

Cyclophosphamide is the most commonly used alkylating agents, and is also used as an... 

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