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63 Cards in this Set

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What is methotrexate?
S-phase specific antimetabolite
What is mechanism of methotrexate?
Inhibits dihydrofolate reductase, causing decreased dTMP and therefore decreased DNA adn protein synthesis.
What can methotrexate be used for?
RA
Psoriasis
Leukemias
Lymphomas
Abortion
What is the toxicity of methotrexate?
myelosuppression, stomatitis, mucositis, renal dysfunction.

**Myelosuppression is reversible with leucovorin (folinic acid) rescue. Can cause MACROVESICULAR FATTY CHANGE IN THE LIVER!!
What is 5-fluorouracil?
S-phase specific metabolite.

Inhibits thymidylate synthase, causing decrease in dTMP. And decreasing DNA synthesis.
What is 5-FU used for?
Mainly for GI malignancies: colon cancer, gastric, rectal. It has synergism with MTX
What is the toxicity of 5-FU?
Myelosuppression; NOT reversible with leucovorin
What is mechanism of 5-FU?
Inhiits thymidylate synthase, so cant produce dTMP!

dUMP ------------> dTMP
How is methotrexate synergistic with 5 FU?
MTX inhibits dihydrofolate reductase, which is needed to make THF and then CH2-THF, and this CH2-THF is required to convert dUMP to dTMP.

So what is required to make dTMP?
1) CH-THF (from dihydrofolate reductase)
2) Thymidylate synthase.
What is 6-mercaptopurine (6-MP)?
Agent metabolized into false purine analogs (hence the name)!

Blocks de novo purine synthesis.

***MUST BE ACTIVATED BY HGPRTase!!!
What is the toxicity of 6-MP?
Neutropneia!! Mercaptopurine CAPTUres neutrophils.
How is 6-MP metabolized?
By Xanthine oxidase, so if you have allopurinol drug, it will increase the concentration of 6-MP and increase toxicity!


S phase specific metabolite.
What is cytarabine (ara-C)
Used for AML

Blcoks DNA polymerase!!

Leukopenia, thrombocytopenia, megaloblastic anemia
What is mechanism of cyclophosphamide?
Alkylating Agent: covalent x-links DNA at guanine N-7!!

Doesnt differentiate between resting and cycling cells.
What is one requirement for cyclophosphamide to work?
Needs bioactivation by the liver! (cytochrome P450).
What is cyclophosphamide used for?
Immunosuppression, breast, ovary carcinomas.
What are side effects of cyclophosphamide?
Hemorrhagic cystitis (can be prevented by mensa): antidote that helps excrete the toxic metabolit.
What are nitrosureas used for?
1) Alkylate DNA. Require liver
2) CROSS BBB --> CNS
3) used for brain tumors.

PUlmonary fibrosis if chronic use.
What is cisplatin, carboplatin mechanism of action?
Act like alkylating agents: forms cross links in DNA
What is cisplatin/carboplatin used for?
Testicular, bladder, ovary, and lung carcinomas.
What is toxicity of cisplatin?
Nephrotoxicity (Cant PISS)
Acoustic nerve damage (MISS what people say).

Neuropathy
What is busulfan mechanism of action?
Alkylates DNA
What are some side effects of busulfan?
Pulmoanry fibrosis, hyperpigmentation!

Used in CML!
What is the mechanism of action of doxorubicin (adriamycin)?
Generate free radicals and noncovalently intercalates in DNA.

**Part of ABVD combo for Hodgkins and myeloma
What is side effects of doxorubicin and daunorubucin?
cardiotoxicity: delayed cardiomyopathy!

Used as the ABVD combination regimen for Hodgkins, myeloma, sarcoma, and solid tumors.
What is the ABVD regimen?
Adriamycin (doxorubucin)
Bleomycin
Vinblastine
Dacarbarzine.
What is mechanism of action of dACTinomycin?
Intercalates in DNA

ACTinomycin is used for childhood tumors (children ACT out)!!

1) Wilms Tumor
2) Ewings Sarcoma
3) Rhabdo
What is mechanism of bleomycin?
Free radical formation causing breaks in DNA strand. Works in G2 mainly!!

Forms a ferrous iron oxygen drug complex.
What is the side effect of bleomycin?
Pulmonary fibrosis, skin changes
What is action of mitomycin C?
Cross-links DNA

Used for bladder cancer
What are side effects of mitomycin C?
Interstitial pneumonitis, nephrotoxicty.
What is leukovorin rescue?
Treatment with methotrexate includes adding leucovorin (folinic acid)

Its a reduced form of folate not requiring Dihydrofolate reductase (which is blocked by methotrexate).

Cool thing about leukovorin --> picked up by regular cells more so than cancer cells!!
What is mechanism of etoposide (VP-16)?
G2 phase specific!!

Inhibits topoisomerase II, which increases DNA degradation
What stage does bleomycin work on?
G2
What stage does etoposide work on?
Maily on G2 to inhibit topo II

But then indirectly on S inhibiting DNA synthesis.

Tangles the cells DNA and it cant divide.
What is most common glucocorticoid used in cancer chemotherapy?
Prednisone. Thought to trigger apoptosis?
What is toxicity of prednisone?
Cushing-like symptoms; immunosuppression,
CATARACTS
OSTEOPOROSIS
HTN
Acne
What is action of tamoxifen?
It antagonizes estrogen receptors in the breast, but actually stimulates estrogen receptors of the uterus.
What is side effect of tamoxifen?
Can cause endometrial carcinoma via partial agonist effects.

Actually induces a low estrogen state, so causes hot flashes, nausea, vomiting.
What is tamoxifen used for?
Breast Cancer

Osteoporosis.
What is action of raloxifene?
Acts as an antagonist in BOTH breast and endometrial tissue! So mainly used for osteoporosis and breast cancer.
What is mechanism of trastuzumab (herceptin)?
Monoclonal antibody against HER-2 receptor. (This is a type of erb-B2 gene overamplification).

Helps kill cancers that overexpress HER-2, possibly through antibody-dependent cytotoxicity.
What is HER-2?
Epidermal growth factor receptor: expressed in cells of breast, endometrium, ovary, and lung.
What is side effect of trastuzumab?
Herceptin

Cardiotoxicity.
What is imantinib?
Gleevec

Monoclonal antibody against philadelphia chromosome bcr-abl tyrosine kinase!!

TYROSINE KINASE.

Used in CML.
What is the toxicity of imatinib?
Gleevec

Fluid retention.
What is vincristine, vinblastine mechanism of action?
M-phase specific alkaloids!!

Bind to tubulin and block polymerization of microtubules, so cant form mitotic spindle.
What is side effect of vincristine?
1) M phase specific
2) Inhibits polymerization of microtubules

Neurotoxicity (areflexia, peripheral neuritis).
what is side effect of vinblastine?
Blasts Bone marrow!!
What is paclitaxel and other taxol mechanism of action?
1) M-phase specific
2) Bind to tubulin and hyperstabilize polymered microbutules!!

Note: you can polymerize, but then stabilized so you cant break down mitotic spindle --> PREVENTS ANAPHASE FROM OCCURRING!!
What is action of flutamide?
1) Anti-androgen
2) Used for prostate cancer
3) Inhibits androgen uptake and binding in target tissue
What is side effect of flutamide?
Impotence, hot flashes, gynecomastia.
What is anastrazole, letrozole mechanism of action?
Aromatase inhibotrs, decreasing conversion of androgens to estrogen.

Side effects: hot flashes, edema
What is action of leuprolide/goserelin?
GnRH receptor agonists, which suppresses production of LH and FSH, ultimiately suppressing ovaries and testes.

Used for prostate CA/endometriosis.
What is mechanism of rituximab?
Monoclonal antibody directed against CD20 surface antigen expressed on B-lymphocytes.

ADCC death.
What is mechanism of azothioprine?
It gets converted to 6-MP which is a purine metabolite inhibiting purine synthesis.

Inhibits synthesis of DNA and ultimately proteins.
What is side effect of azothioprine?
Bone marrow depression

Used for non-selective immunosuppression for organ transplant.
What is mechanism fo action of mycophenolate?
inhibits inosine monophosphate dehydrogenase. This blcoks formation of GMP. Inhibits purines.

Also used for immunosuppression!
What is mechanism of action of cyclosporine?
inhibits gene transcription of several factors produced by activated T cells including IL-2.
What is side effect of cyclosporine?
nephrotoxicity.
What is mechanism of action of tacrolimus (FK 506)?
Diffuses into T cells where it binds to FK binding protein causing inhibition of cytokine synthesis.

10-100x more potent that cyclosporine.
What is murumonab (OKT-3) MOA?
OKT-3 is a monoclonal Ab directed against the CD3 molecule of human T cells!!

Used ina cute rejection of renal, cardiac, or hepatic allografts.
When is muromonab contrindicated?
In patients with history of seizure, heart failure, or pregnancy.