Anti-cancer Drugs Flashcards

1
Q

How does methotrexate work

A

it’s an antimetabolite - inhibits dihydrofolate reductase, which inhibits the conversion of dUMP to dTMP, which decreases DNA and decreases protein synthesis

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2
Q

What are the 3 uses for methotrexate

A
  1. Solid cancer: leukemia, lymphoma, sarcomas, choriocarcinoma 2. Abortion, ectopic pregnancy 3. Immunosuppression: rheumatoid arthritis, psoriasis
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3
Q

Methotrexate toxicity

A

myleosuppresion that is reversible with folinic acid “rescue” (Leucovorin) and fibrotic lung

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4
Q

Mechanism of 5 flourouracil

A

a pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid - this inhibits thymidylate synthase, which decreases dTMP, which decreases DNA and protein synthesis

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5
Q

5FU has synergy with

A

Methotrexate

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6
Q

How is 5FU myelosuppression different from MTX

A

Myelosuppression is not reversible with leucocorin in 5-FU, but is with MTX. neeed thymidine rescue with 5-FU

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7
Q

What is the mechanism of 6-Mercaptopurine (6-MP)

A

A purine analogue (just like allopurinol) that decrease de novo synthesis. Activated by HGPRTase.

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8
Q

What is the toxicity of 6-MP increased with

A

It’s metabolized by xanthine oxidase, so toxicity increases with allopurinol

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9
Q

What is 6-Thioguanate (6-TG)

A

The same as 6-MP except it can be given with allopurinol

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10
Q

Cytarabine

A

A pyrimidine analog - inhibition of DNA polymerase

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11
Q

All anti metabolites work in

A

S phase

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12
Q

Dactinomyocin

A

Intercalates DNA

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13
Q

Dactinomyocin is used for

A

Children’s tumors: wilm’s tumor, ewing’ sarcoma, rhabdomyosarcoma

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14
Q

How does doxorubicin work

A

It generates free radicals by noncovalently (dactinomyocin covalently) intercalating DNA, causing breaks in DNA, which decreases replication

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15
Q

Doxorubicin toxicity and Rx for that

A

cardiotoxicity - because the heart lack superoxide dismutase, causing cardiomyopapthy; Dexrazoxane is used to prevent it

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16
Q

Bleomycin MOA

A

Induces free radical formation, which causes breaks in DNA strands

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17
Q

Eradicated Ball Cancer

A

Etoposide, Bleomycin, Cisplatin

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18
Q

Bleomycin toxicity

A

Pulmonary fibrosis

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19
Q

Etoposide (VP16) MOA

A

Inhibits topoisomerase 2, causing increased DNA degradataion - forms a complex between topoisomerase and 2 and DNA

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20
Q

Which antibiotics work like etoposide

A

Flouroquinolones

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21
Q

Etoposide is used for

A

Small cell carcinoma of the lung and prostate, testicular cancer

22
Q

This drug alkylates DNA and causes pulmonary fiborsis

A

Busulfan

23
Q

This drug fragments DNA and causes pulmonary fibrosis

A

Bleomycin

24
Q

This drug blocks purine synthesis, and is metabolized by xanthine oxidase

A

6-mercaptopurine: antimetabolite

25
Q

This drug cross links DNA and is neprho and oto toxic

A

Cisplatin, carboplatin, oxaliplatin

26
Q

Nitrogen mustard that alkylates DNA (electrophile that binds DNA)

A

Cyclophosphamide (DMARD)

27
Q

Folic acid analog that inhibits dihydrofolate reductase

A

Methotrexate

28
Q

Prevent tubulin dissasembly

A

Paclitaxel and other taxols P

29
Q

Pyrimidine analog that is bio-activated to 5F-dUMP, which covalently complexes folic acid. This complex inhibits thymidylate synthase, which decreases dTMP and decreases DNA and protein synthesis

A

5-FU

30
Q

Intercalates DNA, produces free oxygen radicals, and cardiotoxic

A

Doxorubicin

31
Q

DNA alkylating agent used in brain cancer

A

Nitrosureas cross blood brain bar

32
Q

Prevents Tubulin assembly

A

Vincristine and vinblastine

33
Q

Inhibits thymidylate synthase - leading to decrease nucleotide synthesis

A

5-FU

34
Q

SERM - blocking estrogen binding receptors

A

Tamoxifen, raloxifene: antagonist in breat and agonist in bone. tamoxifen may increase the risk of endometrial carcinoma via partial agonist effects - raloxifen is an endometrial antagonists

35
Q

Mechanism similar to antiviral acyclovir and foscarnet

A

Cytarabine (pyrimidine analog = inhibition of DNA polymerase)

36
Q

Mechanisms similar to flouroquionlones

A

Etoposide

37
Q

mechanisms similar to trimethoprim

A

methotrexate (folic acid analog that inhibits dihydrofolate reductase = dec dTMP = dec DNA = dec. protein synthesis

38
Q

monoclonal antibody against HER2 (erb-2)

A

Trastuzumab

39
Q

Free radical induced DNA strand breakage

A

Bleomycin, Doxorubicin, Daunorubicin

40
Q

Inhibitor of PRPP synthetase

A

6-MP: purine thiol analog = dec de novo purine synthesis, activated by HGPRtase

41
Q

Reversible with Leucovorin

A

Methotrexate

42
Q

Treatment for choriocarcinoma

A

Methotrexate, vinblastine, vincristine

43
Q

Treatment for AML

A

Cytarabine

44
Q

Treatment to CLL

A

Busulfan, Imatinib

45
Q

Prevents breast cancer

A

tamoxifen and raloxifene

46
Q

Treatment for testicular cancer

A

“Eradicate Ball Cancer”

  1. Etoposide
  2. Bleomycin
  3. Cisplatin
47
Q

Applied topically for AKs and basal cell cancers

A

5-FU

48
Q

Treatment for childhood tumors (ewing sarcoma, wilms tumor, rhabdomyosarcoma)

A

Dactinomcyin

49
Q

Inhibits ribonucleotide reductase

A

Hydroxyurea: dec DNA synthesis ( s phase specific)

50
Q

Side effect of hemorrhagic cystitis

A

Acrolein produced by cyclophophamide

51
Q

Antibody against Philadelphia chromsome

A

Imatinib

52
Q

Side Effects of prednisone

A

Immunosuppression - osteoporosis - acne - catarcts - cushingoid features - peptic ulcers - hypertension -hyperglycemia - insomnia - psychosis