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Heme & Lymph > Pharm- Pyrimidine Antimetabolites > Flashcards

Pharm- Pyrimidine Antimetabolites Flashcards

1
Q

5-Fluorouracil Distinctions

A

Active metabolites: FdUMP inhibs thymidylate synthase (inhibs dTMP synthesis) FdUTP & FUTP damage DNA & RNA

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2
Q

Capecitabine Distinctions

A

Oral pro-drug of 5FU

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3
Q

Gemcitabine Distinctions

A

Kinases convert gemcitabine to nucleotide analogs -> inhibs DNA synthesis

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4
Q

Cytarabine (Ara C) Distinctions

A

Kinases convert Ara-C to AraCTP -> inhibits DNA synthesis

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5
Q

5-FU Therapeutic Uses

A

Solid tumors: colorectal & other GI; breast, ovarian carcinomas. Topical: Basal cell carcinoma

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6
Q

Capecitabine Therapeutic Uses

A

Colorectal cancer; metastatic breast cancer (resistant to paclitaxel/anthracycline)

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7
Q

Gemcitabine Therapeutic Uses

A

Pancreatic Cancer

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8
Q

Cytarabine (Ara C) Therapeutic Uses

A

AML (with 6-thioguanine, daunorubicin)

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9
Q

5-FU Dose-Limiting Toxicity

A

Severe GI intolerance, mucositis, myelosuppression

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10
Q

Capecitabine Dose-Limiting Toxicity

A

Similar to 5FU + hand-foot syndrome

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11
Q

Gemcitabine Dose-Limiting Toxicity

A

Myelosuppression- Neutropenia

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12
Q

Cytarabine (Ara C)

A

Severe myelosuppression- Granulocytopenia

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13
Q

5FU

A

FdUMP inhibits thymidylate synthase -> thymineless death

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14
Q

what is 5FU almost always given with?

A

Folinic acid

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15
Q

clearance of 5FU

A

metabolic inactivation of 5FU by the liver

  • DHFU is inactive metabolite
  • inactivated by DPD in liver
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16
Q

DPD deficiency/slow metabolizer

A

prolonged/greater systemic exposure

-Neurologic sx (very common), stomatitis, leukopenia, thrombocytopenia, hair loss, diarrhea, fever, cerebellar ataxia

17
Q

capecitabine activation

A

1) in the liver

2) in the tumor cells

18
Q

Ara-CTP inhibits?

A

DNA polymerase and terminates further DNA elongation

19
Q

resistance to Ara-C

A

excess CDA

-liver & spleen contain very high levels of cytidine deaminase (CDA) -> inactivates the drug

Heme & Lymph (8 decks)

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