Alkylating Agents Flashcards
Alkylating Agent mechanism
Cell Cycle Non-Specific (CCNS)
produce strong electrophile through carbonium or ethyleneimonium ion intermediates, which covalently bond via alkylation of nuc. moieties in DNA
Mechlorethamine class and mechanism
nitrogen mustard
alk. agent, spontaneous conversion to active metabolites in body fluids or enz. converted in liver
Mechlorethamine therapeutics
hodgkin’s disease, topically for cutaneous T cell lymphoma
Cyclophosphamide (Cytoxan) class and mechanism
nitrogen mustard
alk. agent, conversion by hepatic C-P450 to active phosphoramide mustard, relatively long half life
Cyclophosphamide (cytoxan) therapeutics
most widely used alk. agent, used singly or in combo for ALL, CLL, non-hodgkins lymphoma, breast, lung, and ovarian cancer
Cyclophosphamide side effects
hemorrhagic cystitis due to acrolein (toxic drug metabolite)- minimize with hydration and MESNA (nausea, vomiting)
Alkylating Agent Side Effects
bone marrow, mucosal toxicity, nausea and vomiting, toxic effects on repro systems, increase leukemia rate
Ifosfamide (Ifex) class and mechanism
nitrogen mustard
alk. agent, conversion by hepatic C-P450 to active phosphoramide mustard, relatively long half life
Ifosfamide (Ifex) therapeutics
sarcoma and testicular cancer
Ifosfamide (Ifex) side effects
hemorrhagic cystitis due to acrolein (toxic drug metabolite)- minimize with hydration and MESNA (nausea, vomiting)
Carmustine (Gliadel) class and mechanism
nitrosoureas
alkylating agent
Carmustine (gliadel) therapeutics
brain tumors (cross BBB)
Carmustine (gliadel) side effects
renal toxicity, pulmonary fibrosis (other- profound myelosuppression, nausea, vomiting)
Lomustine (Ceenu) class and mechanism
nitrosoureas
alkylating agent
Lomustine (Ceenu) therapeutiics
brain tumors (cross BBB)
