-
MTX: MOA
Folic acid analog inhibits dihydrofolate reductase, decreasing dTMP
-
MTX: how to rescue patient from myelosuppression
Leucovorin (folinic acid)
-
5-FU: MOA
- Pyrimidine analog covalently complexes folic acid
- Inhibits thymidylate synthase and decreases dTMP
-
5-FU: overdose rescue
thymidine
-
6-MP: MOA
- Purine analog decreases purine synthesis
- Activated by HGPRTase
-
6-thioguanine (6-TG): MOA
Purine analog like 6-MP but can be given with allopurinol
-
Cytarabine (ara-C): MOA
Pyrimidine antagonist inhibits DNA polymerase
-
Dactinomycin: MOA
Intercalates in DNA to inhibit DNA dependent RNA polymerase
-
Dactinomycin: use
Kids' tumors e.g. Ewing's, Wilms', Rhabdo
-
Doxorubicin (Adriamycin): MOA
- Generates free radicals
- Nocovalently intercalates in DNA and puts breaks in it
-
-
Bleomycin: MOA
- G2 phase induction of free radicals, causing DNA strand breaks
- Combines with Fe2+
-
Bleomycin: toxicity
- Pulmonary fibrosis
- sin changes
- Uniquely, causes little myelosuppression
-
Etoposide: MOA
- Inhibits DNA topoisomerase II-DNA complex
- Causes dsDNA breaks during replication
-
Cyclophosphamide and ifosfamide: MOA
Activated in P-450 system (liver) then covalently X-link DNA at guanine N-7
-
Cyclophosphamide and ifosfamide: toxicity
- Hemorrhagic cystitis, minimized with MESNA
- Neurotox with ifosfamide
-
Nitrosureas (-mustine and streptozocin): MOA
Require bioactivation, then alkylate DNA
-
Nitrosureas (-mustine): use
CNS tumors
-
Busulfan: MOA
Cross-links DNA
-
-
Busulfan: toxicity
- pulmonary fibrosis
- hyperpigmentation
-
Name the alkylating agents
- Cyclophosphamide
- -mustines (nitrosureas)
- streptozocin
- cisplatin
- busulfan
- dacarbazine/procarbazine
- mechlorethamine
-
Paclitaxel: MOA
Bind beta-tubulin subunit of microtubules to prevent their disassembly
-
Vincristine, vinblastine: MOA
Bind tubulin to prevent microtubule assembly
-
Vinblastine: toxicity
bone marrow suppression
-
Vincristine: toxicity
neurotoxicity, paralytic ileus
-
Cisplatin: toxicity
- Nephrotoxicity
- Ototoxicity
-
Hydroxyurea: MOA
- Urea analogue inhibits ribonucleotide reductase
- S phase specific
-
Name the selective estrogen receptor modulators
-
Which SERM increases the risk of endometrial carcinoma?
Tamoxifen
-
Trastuzumab (herceptin): MOA
- Monoclonal antibody against HER-2 (erb-B2)
- Encourages antibody-dependent cytotoxicity
-
Trastuzumab: toxicity
cardiotoxicity
-
Imatinib: MOA
Tyrosine kinase inhibitor for bcr-abl
|
|
