Chlorambucil alkylating agent

Chlorambucil -alkylating agent (cell cycle-independent) -bone marrow suppression -nausea and vomiting -CNS stimulation (uncommon)... 

Fig. 3.11 Alkylating polyamide binding site model and structures of polyamide-alkylator conjugates. The dotted triangle represents the alkylating agent. All other symbols are defined in Fig. 3.4. The CBI and chlorambucil alkylator domains are boxed...

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

Campath was given accelerated approval on the basis of response rate. The pivotal trial was a study in 93 pahents who had been previously treated with an alkylating agent and whose disease had progressed on treatment with fludarabine. The FDA requested a follow-up sfudy for full approval of Campafh by randomizing patients between Campath and chlorambucil (Leukeran) as front-line therapy This trial is ongoing. Thus, Campath has had a convenhonal development approach. 

Alkylating agents Chlorambucil Murine thymoma, Murine lymphoma. Melanoma... 

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. 

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). 

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. 

CHLORAMBUCIL H2 RECEPTOR BLOCKERS -CIMETIDINE t adverse effects of alkylating agent, e.g. myelosuppression Additive toxicity Monitor more closely monitor FBC regularly... 

Alkylating agents interfere with DNA replication and transcription, resulting in depression of T- and/or B-cell populations. The most commonly used alkylating agents in uveitis management include cyclophosphamide (Cytoxan ) and chlorambucil (Leukeran ). 

Alkylating agents. Busulfan is a radio-mimetic cytotoxic agent that is effective in PRV, reducing vascular events and delaying myelofibrosis. Its mutagenic potential should restrict its use to older patients. Chlorambucil and combination chemotherapy should be avoided because of excessive leukaemogenic risk. 

Some alkylating agents cyclophosphamide and chlorambucil (see Table 30.2)... 

Nitrogen mustard and related alkylating agents, such as cyclophosphamide, chlorambucil, triethylmelamine, and thiophosphoramide, prolong the action of suxamethonium (282,283). Plasma cholinesterase activity is reduced, possibly by alkylation of the enzyme. It has been suggested that azathioprine may potentiate suxamethonium by inhibition of phosphodiesterase activity (SEDA-4, 87) (284). 

Chlorambucil is an alkylating agent that retards or stops growth of cancer cells. It is used to treat chronic lymphocytic leukemia, malignant lymphomas such as lymphosarcoma, giant follicular lymphoma, ovarian cancer, and Hodgkin s disease. 

Chlorambucil is a cytotoxic agent. As a bifunctional alkylating agent, it causes breaks in DNA thus interfering with DNA replication and transcription. 

Alkylating agents and related compounds act by forming covalent bonds with DNA. thus impeding DNA replication. They can be divided into five subgroups (i) nitrogen mustards (e.g. chlorambucil, cyclophosphamide, melphalan and mustine (ii) platinum drugs (coordination complexes of platinum) (e.g. cisplatin and carboplatin) ... 

---