Pharm

Alkylating Agent

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Alkylating Agent

  • Mechanism
  1. Exert cytotoxic effects via transfer of alkyl group
    1. DNA alkylation (key to cellular lethality)
    2. Chemically react with many cellular constituents
  2. DNA cross linking is a primary role of agents
  3. Replicating cells are most susceptible to agents
  4. Alkylating Agents are not cell cycle specific
  • Types
  1. Bis (chloroethyl) amines
    1. Cyclophosphamide
    2. Mechlorethamine
    3. Chlorambucil
    4. Melphalan
  2. Nitrosoureas
    1. Carmustine (BCNU)
    2. Lomustine (CCNU)
    3. Semustine (Methyl-CCNU)
  3. Aziridines
    1. Thiotepa
    2. Triethylenemelamine
  4. Alkylsulfonates
    1. Busulfan
  5. Other drugs causing alkylation
    1. Procarbazine
    2. Dacarbazine
    3. Hexamethylmelamine
    4. Cisplatin