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Cancer Pharmacology: Drug Mechanisms & Side Effects

The document discusses several classes of drugs used to treat cancer, including anti-metabolites like methotrexate and 5-fluorouracil which inhibit DNA synthesis, antitumor antibiotics like doxorubicin and bleomycin which cause DNA breaks through free radical formation, alkylating agents like cisplatin and cyclophosphamide which cross-link DNA, and microtubule inhibitors like vinblastine and paclitaxel which prevent polymerization of microtubules and formation of the mitotic spindle. Side effects of the drugs are also mentioned.

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Wil Lester
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63 views10 pages

Cancer Pharmacology: Drug Mechanisms & Side Effects

The document discusses several classes of drugs used to treat cancer, including anti-metabolites like methotrexate and 5-fluorouracil which inhibit DNA synthesis, antitumor antibiotics like doxorubicin and bleomycin which cause DNA breaks through free radical formation, alkylating agents like cisplatin and cyclophosphamide which cross-link DNA, and microtubule inhibitors like vinblastine and paclitaxel which prevent polymerization of microtubules and formation of the mitotic spindle. Side effects of the drugs are also mentioned.

Uploaded by

Wil Lester
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd
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Cancer Pharmacology
Shan Nanji
+ 2

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


+ 3

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 __________________
Shan Nanji - NanjiMD@gmail.com
n Rx: Colon Cancer
+ 4

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


+ 5

Cancer Rx:
Antitumor Antibiotics
nBleomycin
MOA:
n Cause Free Radical Formation
n DNA breaks
n S/E:

n __________________

Shan Nanji - NanjiMD@gmail.com


+ 6

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

n Can cause __________________ and __________________

n Rescue __________________

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
+ 7

Cancer Rx:
Alkylating Agents
nBusulfan
MOA:
n Alkylates DNA

n S/E:
n __________________

nHydroxyurea hyd RoxyuRea


n Inhibits __________________
n can raise HbF in Sickle Cell

nMelphalan
n Rx: Multiple Myeloma

Shan Nanji - NanjiMD@gmail.com


+ 8

Cancer Rx:
Alkylating Agents
nNitrosureas
MOA:
n Require Bioactivation
n S/E:

n __________________

nChlorambucil MC Alkylating agent

Shan Nanji - NanjiMD@gmail.com


+ Cancer Rx: 9

Microtubule Inhibitors
n Vinblastine
n Blocks polymerization therefore mitotic spindle cant form
n S/E:
n Blasts Bone Marrow -> Bone Marrow Suppression

n Vincristine Blocks polymerization so mitotic spindle cant form


n S/E:
n Neurotoxicity (Areflexia, Peripheral Neuritis)
n Paralytic Ileus

n Paclitaxel __________________polymerized microtubules in M-


phase so that mitotic spindle __________________ (anaphase can not
occur)

Shan Nanji - NanjiMD@gmail.com


+ Cancer Rx: 10

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!

Shan Nanji - NanjiMD@gmail.com

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