Title 18. CHEMOTHERAPY OF CANCER (NEOPLASMS).pdf ✅

PHARMD GURU Page 3 6. Epipodophyllotoxins: Etoposide, teniposide 7. Camptothecins: Topotecan, irinotecan 8. Antibiotics: Actinomycin D, bleomycin, mitomycin C, doxorubicin, daunorubicin 9. Enzyme: L-Asparaginase 10. Miscellaneous agents: Hydroxyurea, imatinib 11. Hormones and antagonists: a) Oestrogens: Ethinyl estradiol, fosfestrol b) Selective oestrogen receptor modulators (SERMs): Tamoxifen c) Selective oestrogen receptor downregulators (SERDs): Fulvestrant d) Aromatase inhibitors: Anastrozole, letrozole e) Progestins: Hydroxyprogesterone caproate, medroxyprogesterone acetate f) Antiandrogen: Flutamide g) 5%-Reductase inhibitor: Finasteride h) GnRH analogues: Buserelin, goserelin, nafarelin i) Corticosteroids: Prednisolone and others (Natural products: Vincristine, vinblastine, paclitaxel (from plants), doxorubicin, daunorubicin, mitomycin, L-asparginase from micro-organisms) 1)ALKYLATING AGENTS: All alkylating agents have alkyl group(s) and are capable of introducing these groups into nucleophilic sites on DNA bases through the formation of covalent bonds. Alkylating agents are CCNS drugs. They also have radiomimetic effect. MECHANISM OF ACTION:
PHARMD GURU Page 4 (A) NITROGEN MUSTARDS: CYCLOPHOSPHAMIDE:  Cyclophosphamide is a prodrug and is activated in liver (Fig. 11.17). The final active metabolites derived from cyclophosphamide are phosphoramide mustard and acrolein. Phosphoramide mustard produces cytotoxic effect and acrolein is responsible for haemorrhagic cystitis.  Cyclophosphamide is administered orally or intravenously. The metabolites are excreted mainly in urine. ADVERSE EFFECTS: Cyclophosphamide can cause general toxicity. The specific toxicity of cyclophosphamide is severe haemorrhagic cystitis. It is associated with dysuria and haematuria due to irritation of bladder mucosa by acrolein. It is a dose-limiting toxicity and can be reduced by adequate hydration and coadministration of i.v.