Pmcol 344 Midterm 2 Exam Questions With
Correct Answers
Mechlorethamine - answer✔Nitrogen mustard alkylating agent: S-phase specific, bind
covalently to DNA, mutagenic (given in single high dose)
-Hodgkin's lymphoma
-Dose-limiting: myelosuppression
Chlorambucil - answer✔Nitrogen mustard alkylating agent: S-phase specific, bind covalently
to DNA, mutagenic (given in single high dose)
-Chronic lymphocytic leukemia
-Dose-limiting: myelosuppression
Malphalan - answer✔Nitrogen mustard alkylating agent: S-phase specific, bind covalently to
DNA, mutagenic (given in single high dose)
-Multiple myeloma (in combination with prednisone)
-Dose-limiting: myelosuppression
Cyclophosphamide (CPX) - answer✔Nitrogen mustard alkylating agent: S-phase specific, bind
covalently to DNA, mutagenic (given in single high dose)
-Dose-limiting: myelosuppression, hemorrhagic cystitis
-Activated by hepatic cytochrome oxidase, then non-enzymatic conversion to acrolein and
phosphoramide mustard (active)
-Given with Mesna
Acrolein - answer✔Side product of activation of CPX and ifosfamide
Potent lung irritant, also hemorrhagic cystitis and hematuria
-Giving Mesna with ifosfamide/CPX treatment forms adduct with acrolein to detoxify it, allows
higher doses of drug
Mesna - answer✔Forms adduct with acrolein to detoxify it, allows higher doses of drug
Ifosfamide - answer✔Nitrogen mustard alkylating agent: S-phase specific, bind covalently to
DNA, mutagenic (given in single high dose)
-Dose-limiting: myelosuppression, hemorrhagic cystitis
-Lymphoid and myeloid malignancies
-Always given with Mesna
Carmustine (BCNU) - answer✔Nitrosourea alkylating agent: requires activation in the liver to
active intermediate
-Lipid soluble: can get into cell through diffusion and act without the cell being active, also can
cross BBB so useful in brain tumours
-Myelosuppression, leukemogenic (causes leukemia), hepatotoxicity
Bifunctional agent
Lomustine (CCNU) - answer✔Nitrosourea alkylating agent: requires activation in the liver to
active intermediate
-Lipid soluble: can get into cell through diffusion and act without the cell being active, also can
cross BBB so useful in brain tumours
-Myelosuppression, leukemogenic (causes leukemia), hepatotoxicity
Monofunctional agent, only one reactive side chain
Busulfan - answer✔Alkyl sulphonate, alkylating agent.
Bifunctional, creates G-G and A-G intrastrand crosslinks
-Depression of blood cells, used in bone marrow transplant regimes to wipe everything out (in
chronic myelogenous leukemia)
Temozolomide - answer✔Triazine alkylating agent, prodrug of dacarbazine
Interact with guanine N7 or O6
Used for glioblastomas and melanomas
Dacarbazine - answer✔Triazine alkylating agent
Interact with guanine N7 or O6
Used for glioblastomas and melanomas
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