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Pharmacology Exam 2 (Year 2 sem 2) > Chapter 38: Cancer Genome Synthesis > Flashcards

Chapter 38: Cancer Genome Synthesis Flashcards

1
Q

What drug treats skin cancer (topical) by inhibiting thymidylate synthase leading to a thymineless cell death, and interfering with protein synthesis by being incorporated into mRNA?

A

5-fluorouracil

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2
Q

What combo is 1st line for colorectal cancer?

A

“leuovorin”: 5-FU and folinic acid

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3
Q

What is the orally available prodrug of 5-fluorouracil that is used to treat metastatic colorectal cancer and 2nd line for breast cancer?

A

capecitabine (5-FU becomes “FUC”/fuck)

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4
Q

What drug is a folate analogue that inhibits thymidylate synthase by binding to the methylenetetrahydrofolate (cofactor) site of the enzyme, and is administered with folic acid and vitamin B12 to reduce GI toxicity?

A

pemetrexed

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5
Q

What drug is used to treat malignant pleural mesothelioma in combination with cisplatin?

A

pemetrexed

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6
Q

What drug inhibits IMPDH, treats ALL, but has increased toxicity/effectiveness with allopurinol?

A

6-mercaptopurine

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7
Q

Which prodrug of 6-MP inhibits IMPDH and is used for immunosuppression of autoimmune diseases?

A

azathioprine (6-MP becomes “MAP”)

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8
Q

What drug inhibits IMPDH and is a selective inhibitor of adenosine deaminase, used to treat hairy cell leukemia and T-cell lymphoma?

A

pentostatin

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9
Q

What drug is an inhibitor of ribonucleotide reductase (RNA –> DNA) by scavenging a tyrosyl radical at the active site of an enzyme?

A

hydroxyurea

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10
Q

What drug treats and treats polycythemia vera, fibrocytosis, and controls blood counts in AML, and causes secondary leukemia with long-term use?

A

hydroxyurea

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11
Q

What does the drug thioguanine inhibit and what is it used to treat?

A

DNA polymerase (as all purine and pyrimidine analogues do, this one being a guanine analog), and AML

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12
Q

What side effects should be looked out for with thioguanine?

A

myelosuppression, intestinal perforation, hepatotoxicity

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13
Q

What is the composition and mechanism of fludarabine phosphate?

A

purine (adenosine and guanine) analog, inhibits DNA polymerase AND ribonucleotide reductase

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14
Q

What is the composition and main side effect of cladribine?

A 
adenosine analogue (clADribine)
- febrile neutropenia
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15
Q

What treats hairy cell leukemia?

A

pentostatin, cladribine

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16
Q

What is the composition and main side effects of cytarabine?

A 
cytidine analogue (CYTarabine)
- neuropathy & nephrotoxicity
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17
Q

What is the composition and main side effect of azacytidine?

A 
cytidine analogue (azaCYTidine)
- renal failure
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18
Q

Main drug used to treat myelodysplastic syndrome?

A

azacytidine

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19
Q

What is the composition and main side effects of gemcitabine?

A 
cytidine analogue (gemCITabine)
-  febrile neutropenia, pulmonary toxicity, HUS, & hepatotoxicity
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20
Q

What are the main side effects of fludarabine phosphate?

A

aplasia of skin, autimmune hemolytic anemia, neurotoxicity

21
Q

What is the main treatment for pancreatic cancer?

A

gemcitabine

22
Q

What drug for autoimmune diseases crosslinks DNA via bis-alkylation?

A

cyclophosphamide

23
Q

There is a cancer drug that causes hemorrhagic cystitis, alopecia, GI disturbance, and amenorrhea. What metabolite of the drug does this and what should it be coadministered with to avoid the 1st symptom?

A

acrolein (metabolite of cyclophosphamide); administer with mesna

24
Q

What alkylating cross-linking nitrosurea also attaches a carbamoyl group to proteins, and is used for brain cancer?

A

carmustine

25
Q

What crosslinking alkylating agent treats prostate cancer, but should not be used with thromboembolic disorder?

A

estramustine

26
Q

What crosslinking alkylating agent is good for hypoxic tumors (i.e. at the center of a solid tumor, usually gastric or pancreatic)?

A

mitomycin

27
Q

What crosslinking alkylating agent is used for bladder cancer but should not be used with hepatic/renal/bone marrow dysfunction (because powerful!)?

A

thiotepa

28
Q

What crosslinking alkylating agents are used for Hodgkin’s disease?

A

dacarbazine, procarbazine

29
Q

What crosslinking alkylating agent is used for glioblastoma multiforme with radiation, and is a derivative of dacarbazine?

A

temozolomide

30
Q

What crosslinking alkylating agent treats ovarian cancer but shouldn’t be used with neurologic toxicity?

A

altretamine

31
Q

What crosslinking alkylating agent treats germ cell testicular cancer and is coadministered with mesna to avoid hemorrhagic cystitis?

A

ifosfamide

32
Q

What in the body can deactivate crosslinking alkylating agents, leading to resistance?

A

glutathione

33
Q

What crosslinks GUANINE bases that treats genitourinary cancers? What can it be coadministered with to limit its side effect of nephrotoxicity?

A

cisplatin, carboplatin.

- amifostine (for cisplatin’s nephrotoxicity)

34
Q

What crosslinks GUANINE bases that treats colorectal cancers, and cold temperatures exacerbate neurotoxicity?

A

oxaliplatin

35
Q

What binds oxygen and chelates iron, and leads to DNA strand breaks through oxidative intermediates? (it treats testicular cancer)

A

bleomycin

36
Q

Name 4 bleomycin side effects

A

pulm fibrosis(irreversible, dose limiting), MI, stroke, Raynaud’s disease

37
Q

Endings of topoisomerase inhibitors

A

“-tecan, -bicin, -side, -crine”

38
Q

What drugs inhibit topoisomerase I, leading to DNA strand breakage in the S phase? They have a side effect of life-threatening diarrhea and should NOT be used with Gilbert’s syndrome

A

CAMPTOTHECINS: irinothecan, topothecan (“there CAN only be 1 = topo I”)

39
Q

What ARITHROCYCLINES inhibit topoisomerase II, leading to DNA strand breakage in the G2 phase? They cause heart failure and are excreted in bile.

A

doxorubicin, daunorubicin, epirubicin

40
Q

What EPIPODOPHYLLOTOXINS + one other drug inhibit topoisomerase II, leading to DNA strand breakage in the G2 and S phase? They cause heart problems

A

EPIPODOPHYLLOTOXINS: etoposide, teniposide
other: amsacrine

41
Q

What topoisomerase inhibitor is used for breast cancer?

A

epirubicin

42
Q

What drugs inhibit microtubule polymerization by being toxic to M phase cells, and bind at (+) ends where there is overlap with GTP binding protein

A

“vinka alkaloids”: vinblastine, vincristine, erbulin

43
Q

What drug is best for METASTATIC testicular cancer, but causes extensive bone marrow suppression?

A

vinblastine (BLASTS all those metastases)

44
Q

What drug is best for pediatric leukemias, but causes peripheral neuropathy and myelosuppression?

A

vincristine (kids love CHRIStmas, branches of christmas tree like your limbs = periph neurpathy?)

45
Q

What drug is best for METASTATIC breast cancer, but causes alopecia, myelosuppression, and peripheral neuropathy?

A

erbulin (BU-BEAUtiful = breasts)

46
Q

What drugs inhibit microtubule depolymerization by arresting cells in mitosis, leading to apoptosis?

A

“taxanes”: paclitaxel(binds to INSIDE of MTs), abraxane, docetaxel
(TAXING to keep something polymerized)

47
Q

What drug treats solid tumors of ovarian cancer and should be taken with H1 antagonist & dexamethasone to help with hypersensitivity?

A

paclitaxel

48
Q

What cancer drug can lead to fluid retention syndrome leading to severe edema, and can be relieved by glucocorticoids?

A

docetaxel

Pharmacology Exam 2 (Year 2 sem 2) (7 decks)

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