+Cancer Pharmacology Shan Nanji

+Cancer Rx: Anti-Metabolites

nMethotrexate Inhibits __________________ n Used also for Molar Pregnancies and Rheumatoid Arthritis

n Rescue __________________ n replenishes Folate in the form of Folinic Acid,

which is recognized by the body but NOT by cancer

nara-C/Cytarabine (Pyrimidine Anolog) n Inhibition of DNA polymerase

nara-A

Shan Nanji - NanjiMD@gmail.com

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+Cancer Rx: Anti-Metabolites n6-Mercaptopurine 6-mercap-TOE-purine

n (Purine [thio] analog)

n Decreases de novo purine synthesis n Activated by HGPRTase, promotes

______________

n6-Thioguanine n Same as 6-MP n can be given with allopurinol

n5-Flourouracil 5-FU n Inhibits __________________ n Rx: Colon Cancer Shan Nanji - NanjiMD@gmail.com

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+Cancer Rx: Antitumor Antibiotics

nAdriamycin ATRIA-mycin MOA: n Free Radical Formation n Breaks in DNA

n Can cause __________________

n Rescue __________________

Shan Nanji - NanjiMD@gmail.com

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+Cancer Rx: Antitumor Antibiotics

nBleomycin MOA: nCause Free Radical Formation

nDNA breaks n S/E:

n __________________

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+Cancer Rx: Alkylating Agents nCisplatin cis-PLATIN n MOA: n DNA Cross-Linking

n Can cause __________________ and __________________

nRescue __________________

nCyclophosphomide n Pro-drug: require activation by the liver n Covalently X-Link DNA at Guanine N-7 n Can Cause __________________

n Rescue __________________ Shan Nanji - NanjiMD@gmail.com

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+ Cancer Rx: Alkylating Agents nBusulfan

MOA: nAlkylates DNA

nS/E: n __________________

nHydroxyurea hydRoxyuRea n Inhibits __________________ n can raise HbF in Sickle Cell

nMelphalan n Rx: Multiple Myeloma

Shan Nanji - NanjiMD@gmail.com

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+ Cancer Rx: Alkylating Agents

nNitrosureas MOA: nRequire Bioactivation

n S/E:

n __________________

nChlorambucil MC Alkylating agent

Shan Nanji - NanjiMD@gmail.com

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+Cancer Rx: Microtubule Inhibitors

nVinblastine n Blocks polymerization therefore mitotic spindle cant form

n S/E: n Blasts Bone Marrow -> Bone Marrow Suppression

nVincristine Blocks polymerization so mitotic spindle cant form n S/E: n Neurotoxicity (Areflexia, Peripheral Neuritis) n Paralytic Ileus

nPaclitaxel __________________polymerized microtubules in M-phase so that mitotic spindle __________________ (anaphase can not occur)

Shan Nanji - NanjiMD@gmail.com

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+Cancer Rx: SERMS

nTamoxifen/Raloxifene MOA: n Receptor __________________ in Breast

n Receptor __________________ in Bone n S/E: n Tamoxifen n Increase Risk __________________ n Hot Flashes

n Raloxifene n RELAXifeneNo Increased Risk!

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