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Heme and Lymph > Chemo lecture 1 > Flashcards

Chemo lecture 1 Flashcards

1
Q

what are the PYRIMIDINE anti-metabolite drugs that inhibit DNA synthesis?

A
  • 5 Fluorouracil
  • Capecitabine
  • Cytarabine (Ara-C)
  • Gemcitabine
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2
Q

Given AFTER the tumor is removed by surgery?

A

Adjuvant chemo

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3
Q

What is the goal of adjuvant chemo

A

prevent cancer reoccurance

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4
Q

Given PRIOR to surgery to remove tumor

A

Neoadjuvant chemo

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5
Q

What is the goal of Neoadjuvant chemo

A

shrink the tumor so that the surgery is less extensive

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6
Q

Given specifically to address symptom management without expecting to significantly reduce the cancer

A

Palliative therapy

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7
Q

What is the active metabolite of 5-FU that inhibits thymidylate synthase and therefore inhibits dTMP synthesis?

A

FdUMP

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8
Q

What is the active metabolite of 5-FU that damages DNA?

A

FdUTP

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9
Q

What is the active metabolite of 5-FU that damages RNA?

A

FUTP

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10
Q

what is the ORAL pro drug of 5FU

A

Capecitabine

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11
Q

What drug gets converted by kinases to nucleotide analogs and inhibits DNA synthesis

A

Gemcitabine

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12
Q

What drug gets converted by kinases to AraCTP and inhibits DNA synthesis

A

Cytarabine (Ara C)

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13
Q

What cancers do you used 5FU for?

What is the topical use

A

Solid tumors: colorectal and other GI
Breast, ovarian carcinomas

-topical for Basal cell carcinoma

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14
Q

what cancers do you use Capecitabine for?

A
  • Colorectal

- metastatic breast cancer that is resistant to paclitaxel and anthracycline)

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15
Q

cancer for Gemcitabine

A

pancreatic

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16
Q

cancer for Cytarabine (Ara C) and what do you use this with

A
  • Acute myelogenous leukemia

- used with 6-thioguanine and daunorubicin

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17
Q

Dose limiting toxicity of 5FU

A
  • Severe GI intolerance
  • Mucositis
  • Myelosuppression
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18
Q

Dose limiting toxicity of Capecitabine?

A

similar to 5FU plus hand-foot syndrome

19
Q

Dose limiting toxicity of Gemcitabine

A

myelosuppression - neutropenia

20
Q

Dose limiting toxicity of Cytarabine (Ara C)

A

Severe myelosuppression - granulocytopenia

21
Q

Clinical use of 5FU

A

treat advanced colorectal cancer and adjuvant therapy of early stage colon cancer
-also other solid tumors (esophageal, gastric, pancreatic, colorectal, anal, and hepatocellular)

22
Q

What is 5-FU usually used in combo with

A

folate antagonists and other chemo drugs, radiation, and surgery

23
Q

5FU is an analog of what

A

uracil and thymidine (pyrimidines)

24
Q

Tumor cells activate 5FU through what enzymes

A

Thymidine phosphorylase –>5FUdR and then

Thymidine Kinase –> 5FdUMP

25
Q

What does the 5FU metabolite FdUMP do?

A
  • inhibits thymidylate synthase
  • Depletes dTMP (and dTTP downstream)
  • Distorts dNTP pools
  • CAUSES THYMINELESS DEATH
26
Q

Pyrimidine antimetabolite drugs target what phase of the cell cycle

A

S phase

27
Q

Co treatment of 5FU with what 2 things can increase the anticancer activity?

A

Leucovorin and methotrexate

28
Q

explain the selective toxicity of 5FU in tumors

A

thymidine and uracil phosphorylase activity in tumor tissue is greater than in normal tissue

29
Q

what is the most common mechanism of resistance to 5FU

A

alterations in thymidylate synthase

-tumors with higher levels of thymidylate synthase are relatively more resistant to 5FU

30
Q

what enzyme in the liver metabolizes 5FU?

What does it turn into?

A

dihydropyrimidine dehydrogenase

-DHFU

31
Q

What allelic variation can slow 5FU clearance and aggrevate its systemic toxicity

A

DPYD gene . . .DPD deficiency

-hereditary thymine-uraciluria or familial pyrimidinemia

32
Q

what are the symptoms of DPD deficiency

A

none . . to seizures

-also 5FU toxicity

33
Q

What are the symptoms of the 5FU toxicity from those with DPD deficiency

A
  • cerebellar ataxia

- neurologic symptoms

34
Q

what is on Capecitabine that makes it orally bioavailable

A

carbamate appendage

35
Q

what are the 2 enzymes in order that activate capecitabine in the LIVER to produce 5’-DFUR

A
  • Carboxyesterase 1A1 and 2

- Cytidine deaminase

36
Q

what enzyme in TUMORS convert 5’-DFUR to 5FU?

A

thymidine phosphorylase

37
Q

Clinical uses for Capecitabine

A
  • advanced metastatic colon cancer

- advanced breast cancer . .slows progression

38
Q

Ara-C and Gemcitabine are chemical analogs of what

A

Cytidine

39
Q

how do Ara-C and Gemcitabine enter tumors cells?

A

hENT1: equilibrative nucleoside transporter 1

40
Q

what are the 3 enzymes that turn Ara-C and Gemcitabine into triphosphates theat then inhibit DNA polymerase?

A
  • Deoxycytidine kinase
  • deoxycytidylate kinase
  • nucleoside diphosphate kinase
41
Q

mechanism of resistance to Ara-C

A

inactivation by pyrimidine nucleotidase and cytidine deaminase in tumor cells

42
Q

what organs have very high levels of cytidine deaminase and are a biochemical sanctuary for leukemic cells because they inactivate Ara-C to Ara-U

A

Spleen and Liver

43
Q

Differences b/t Ara-C and Gemcitabine

A
  • Gem-diphosphate inhibits ribonucleotide reductase and depletes cellular dNTPs
  • Ara-C is for acute myelogenous leukemia while Gem iss for pancreatic and non-small cell lung cancer
  • Gem causes Drug induced fever and flu like syndrome

Heme and Lymph (27 decks)

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