372 Section 9/ ChemotherapyALKYLATING AGENTSThe alkylating agents can transfer an alkyl
radical to a suitable receptor site. Alkylation
of DNA within the nucleus represent the
major interactions which will lead to cell
death. These agents react chemically with
sulfhydryl, carboxyl, amino and phosphate
groups of other cellular nucleophiles in the
cells which make them unavailable for the
normal metabolic reactions. Alkylating
agents react with nucleic acid and inhibit
DNA synthesis and also interfere with cell
replication. Alkylating agents has got cytotoxic
action and damage the nuclei of growing and
multiplying cells. They have got
immunosuppressant action also and suppress
antibody production. They also have
radiomimetic (like ionizing radiation) actions.
CYCLOPHOSPHAMIDE
It is an alkylating agent given orally or
by intravenous route. It exerts its action
by alkylation of DNA....Contd.
IV. Vinca alkaloids
Vincristine (Oncovin; BIOCRISTINE) 1.5 mg/m^2 BSA IV weekly
Vinblastine (CYTOBLASTIN) 0.1-0.15 mg/kg IV weekly (total 3 doses)
Vinorelbine (VINELBINE) 30 mg/m^2 BSA IV weekly
V. Taxanes
Paclitaxel (MITOTAX) 175 mg/m^2 BSA IV infusion repeated every 3 weeks
Docetaxel (DOXOTEL)
VI. Topoisomerase-I inhibitors
Irinotecan (IRINOTECAN) 125 mg/m^2 BSA weekly IV
Topotecan (TOPOTEL) 1.5 mg/m^2 BSA IV infusion for five consecutive days
VII.Hormone & hormone antagonists
Fosfestrol (Stilboestrol) 40-80 mg IM every 2-4 weeks
Ethinyl estradiol (LYNORAL) 1-3 mg daily
Tamoxifen (ONCOTAM) 10-20 mg BD
VIII.Radioactive isotopes
Radioactive iodine (^131 I) 3-6 mci oral/IV
Radioactive phosphorus (^32 P) 2.5-5.0 mci IV
Radioactive gold (^198 AU) 35-150 mci IP
IX. Miscellaneous agents
Hydroxyurea (CYTODROX) 20-30 mg/kg daily or 80 mg/kg every 3rd day
Procarbazine 100-300 mg/day
L-Asparaginase (LEUNASE) 50-200 KU/kg daily IV infusion for 2-4 weeks
Cisplatin 50-100 mg/m^2 BSA single IV dose every 3-4 wks
Interferon alfa (ALFERON) 3-36 million IU daily SC/IM (depending upon the
X. Immunosuppressants type of cancer)
Azathioprine
Cyclosporine- BSA = Body surface area