Anti-metabolites

अब Quizwiz के साथ अपने होमवर्क और परीक्षाओं को एस करें!

What cancer is pemetrexed used in?

Lung

What cancer is pralatrexate used in?

Lymphoma

T/F: 5-FU can incorporate into both DNA and RNA

True Blocks DNA and protein synthesis

What happens if a normal adult is deficient in folic acid?

Macrocytic anemia Peripheral neuropathy Depression

What are the folic acid analogs (antifolates)

Methotrexate Pemetrexed Pralatrexate (I take folic acid in the PPM)

Purines have ____ rings and pyrimidines have ____ rings

2, 1

How many enzymes alter capecitabine to make 5-FU

3

What are the pyrimidine analogs?

5-FU Capecitabine Cytarabine Gemcitabine

What 2 antimetabolites are available PO?

6-mercaptopurine Hydroxyurea

What are the purine analogs?

6-mercaptopurine Fludarabine Pentostatin Clofarabine Nelarabine

Clofarabine is used in _____ cancer

ALL

What cancers is 6-Mercaptopurine used in?

ALL

What cancer types is Methotrexate used for?

ALL Breast Lymphoma

Nelarabine is used in _____ and _____ cancers

ALL and lymphoma

What cancer types is cytarabine used in?

AML ALL (All my cytosines, all my cytosines *Beyonce voice*)

Fludarabine is used in _____ cancers

AML, CLL, lymphoma

Folic acid is a water-soluble ____ vitamin

B

What cancer types is gemcitabine used in?

Breast and lung

What cancer type is hydroxyurea used in?

CML (also melanoma, ovarian, head/neck)

What is folate's biological function as THF forms

Carry one-carbon groups for methylation reactions in amino acid and nucleotide synthesis

What cancer type is capecitabine used for?

Colorectal (Also breast and pancreatic)

What cancer types is 5-FU used in?

Colorectal Breast

Methotrexate-PGs inhibit what 2 enzymes?

DHFR Thymidylate synthase (More effective in some cancers, but also more toxic)

Which purine inhibitor is adenosine deaminase-resistant?

Fludarabine

Gemcitabine (dFdC)

GEMZAR

The primary effects of purine analogs are

Gradual myelosuppression GI (mucositis) Opportunistic infections Some hepatotoxicity

How do purine analogs work?

Inhibit de novo synthesis of purine nucleotides Inhibit RNA/DNA synthesis

How does pralatrexate work?

Inhibits DHFR Inhibits polyglutamylation by the enzyme folypolyglutamyl synthetase (further depletes dTMP)

How does methotrexate work?

Inhibits DHFR so there is NO THF, No dTMP

How does 5-FU work?

Inhibits thymidylate synthase (no dTMP made)

How does hydroxyurea work?

It inhibits ribonucleotide reductase so there is no biosynthesis of DNA because of lack of deoxynucleotides.

Name the drug that is a reduced folic acid (folinic acid)

Leucovorin

What can you give with 5-FU to enhance it?

Leucovorin (makes the 5-FU stay around longer)

What clinical toxicity can you see with hydroxyurea?

Myelosuppression GI Disturbances Alopecia

What are the primary toxic effects of pyrimidine analogs?

Myelosuppression GI issues (mucositis) Alopecia

Is 5-FU the active form?

No, it is a prodrug that is converted in the body to 5dUMP

What is capecitabine?

Prodrug of 5-FU (prodrug of a prodrug!) INCEPTION drug (dream within a dream)

All antimetabolites are ____ phase specific drugs

S

How does pemetrexed work?

Same as methotrexate-PGs...inhibits DHFR and thymidylate synthase

How does cytarabine work?

Think cytarabine-CYTOSINE competes with dCTP for DNA incorporation and blocks DNA synthesis

What is the other S phase specific inhibitor?

Topoisomerase inhibitors

T/F: Leucovorin is used in combo with other chemotherapy drugs to enhance effectiveness or chemoprotect

True

Is THF essential for DNA synthesis?

YES!

Can leucovorin be used as an antidote to effects of chemo?

Yes

What happens if you are pregnant and deficient in folic acid?

Your baby can have neural tube defects and other issues

Clinical toxicity of methotrexate is reduced by _____, a reduced folate coenzyme

folinic acid

The primary toxic effects of antifolates is on rapidly dividing cells of the bone marrow and GI epithelium. This causes

mucositis myelopsupression thrombocytopenia

Folic acid is the _____ form and folate is the ______ form which both coexist in water

protonated- acid deprotonated- ion

Structurally, folic acid contains a ______ ring, PABA, and glutamic acid groups

pteridine

antimetabolites inhibit DNA ________

synthesis (think S phase- synthesis)


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