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2nd U1 Pharm > Antimetabolites > Flashcards

Antimetabolites Flashcards

1
Q

What are antimetabolies an structural analog of and when do they act upon the cell?

A

Structural analogs of folic acid or of the purine/pyramidine bases found in DNA–act in S-phase

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2
Q

Name the two folate analog antimetabolites…

A

Methotrexate

Pemetrexed

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3
Q

Which folate analog antimetabolite inhibits dihydrofolate reductase–which is needed to convert folate to THF-needed for thymidine and purine synthesis?

A

Methotrexate

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4
Q

What enzyme is inhibited by methotrexate?

A

Dihydrofolate reductase

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5
Q

What does methotrexate ultimately inhibit the synthesis of?

A

Thymidine and purine

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6
Q

Which folate analog is used in the treatment of Childhood ALL and choriocarcinoma?

A

Methotrexate

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7
Q

Methotrexate is used in combination therapies for which cancers?

A 
Burkitt's Lymphoma
Carcinomas of:
-Breast
-ovary
-head and neck
-Bladder
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8
Q

Why does methotrexate have to be administered intrathecally for meningeal leukemia and meningeal metastases of tumors?

A

Unable to cross the BBB

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9
Q

What cancer can Methotrexate treat if given in high doses?

A

Osteosarcoma

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10
Q

What substance is formed to inhibit the THF-dependent enzymes when using the folate analog, pemetrexed?

A

Polyglutamate

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11
Q

Which folate analog forms polyglutamate and what is caused by this formation?

A

Pemetrexed–inhbits the THF dependent enzymes

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12
Q

Pemetrexed is used for the treatment of….

A

Colon cancer
Mesothelioma
Non-small cell lung cancer
pancreatic cancer

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13
Q

Name the side effects that can be seen with methotrexate?

A 
Renal toxicity
hepatotoxicity
reproductive
myelosuppression
GI toxicity
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14
Q

What can be used to prevent the toxic effects of methotrexate?

A

Leucovorin–taken up much easier by healthy cells compared to tumor cells

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15
Q

Name the 3 pyramidine analog antimetataboties…

A

5-Fluorouracil
Cytarabine
Gemcitabine

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16
Q

Cytarabine is in what drug class?

A

pyrimidine analog

17
Q

5-Fluorouracil is in what drug class?

A

pyrimidine analog

18
Q

Gemcitabine is in what drug class?

A

pyrimidine analog

19
Q

What are the two active metabolites of 5-Fluorouracil used to interrupt DNA synthesis and RNA function, respectfully?

A

DNA synthesis– FdUMP

RNA function– FdUTP

20
Q

What is the mechanism for action of 5-Fluorouracil?

A

Creates active metabolites that interrupt DNA synthesis and RNA function

21
Q

Cytarabine is a pyrimidine analog that terminates DNA synthesis, how is this done?

A

Converted by deoxycutidine kinase to Ara-CTP which terminates DNA synthesis

22
Q

What is the mechanism of action for Gemcitabine? what does it inhibit?

A

Converted to active metabolites which inhibit ribonucleotide reductase–incorpotates into DNA and terminates synthesis

23
Q

5-Fluorouracil is used in combination therapy for what type of cancers?

A 
Breast
Colorectal
Gastric
Head and neck
Cervical
Pancreatic
Basal cell carcinoma
24
Q

What pyrimidine analog is considered the most effective treatment for AML?

A

Cytarabine

25
Q

What pyrimidine analog is used for the treatment of AML, ALL and blast phase of CML?

A

Cytarabine

26
Q

Gemcitabine is used for the treatment of…

A 
Pancreatic cancer
non-small cell lung cancer
ovarian 
bladder
esophageal
head and neck cancers
27
Q

Hand-foot syndrome and cardiac toxicity are side effects seen with the use of which pyrimidine analog?

A

5-Fluorouracil

28
Q

What are other symptoms of 5-Fluorouracil?

A 
Anorexia
Nausea
Mucosal ulcerations
stomatitis
diarrhea
thrombocytopenia
anemia
29
Q

What drug can be given to potentiate the effects caused by the use of 5-Fluoruacil?

A

Leucovorin

30
Q

What are some side effects of Cytarabine, a pyrimidine analog?

A

Severe myelosuppression–leucopenia, thrombocytopenia, anemia
GI tract toxicity–ulceration, stomatitis, diarrhea

31
Q

What are the side effects of Gemcitabine, a pyrimidine analog?

A

Myelosuppression– leucopenia, thrombocytopenia, anemia

Flu-like symptoms

32
Q

Which pyrimidine is more effective against solid tumors when compared to Cytarabine, also a pyrimidine analog?

A

Gemcitabine

33
Q

What is the one purine analog antimetabolite?

A

6-Mercaptopurine

34
Q

What metabolizes 6-Meracaptopurine to cause it to be in its active form and what is its active form?

A

Hypoxanthine-guanine phosphoribosyl transferase (HGPRT)

Active form—TIMP (6-thioinosinic acid)

35
Q

6-meracaptopurine is converted to TIMP, its active form, by HGPRT. What are the two mechanisms of action of TIMP?

A

1) inhibits first step of de novo purine base synthesis and the formation of AMP and xanthinylic acid from inosinic acid–reduces purine levels
2) converted to thio-guanine ribonucleotides–inhibits DNA and RNA synthesis

36
Q

What is the primary use of 6-Mercaptopurine?

A

Maintain remission in acute ALL

37
Q

What are the side effects of 6-Mercaptopurine?

A

hepatotoxicity in prolonged use

Bone marrow suppression

38
Q

What drug interaction is seen with the use of 6-Mercaptopurine, why?

A

Allopurinol–inhibits xanthine oxidase

2nd U1 Pharm (11 decks)

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