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Pharmacology > Antimetabolites > Flashcards

Antimetabolites Flashcards

1
Q

General

A

Cell Cycle Specific: S-Phase

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2
Q

Methotrexate (MTX) Mechanism

A

Folic Acid Analog

Inhibit DHFR: block Formation of FH4

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3
Q

MTX Use

A

Filtered/secreted by kidneys

acute lymphoblastic lymphoma

breast and choriocarcinoma

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4
Q

MTX Toxicity

A

Myelosuppression: add Leucovorin

high dose: nephrotoxicity: hydrate with bicarb to alkalinize urine/excretion

hepatotoxicity

mucositis

Teratogenic

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5
Q

Pyrimidine Analog Drugs

A

5-Flurouracil

Cytarabine

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6
Q

5-FU mechanism

A

prodrug

5-FUMP blocks RNA synthesis
Fdump blocks DNA synthesis

complex with FH4 cofactors and TS to block de novo thymidine synthesis

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7
Q

5-FU use

A

Leucovorin Potentiates 5-FU

Colorectal Cancer
Pancreatic Cancer
Actinic Keratosis
BCC

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8
Q

5-FU Side Effects

A

BM Depression
Oral and GI Mucositis
Plantar Erythrodysethetia: hand and foot

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9
Q

Cytarabine Mechanism

A

requires phosphorylation by Nucleoside kinase

AraCTri-Phosphate: inhibits DNA Pol

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10
Q

Cytarabine Use

A

Leukemia: AML and lymphomas

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11
Q

Cytarabine Side Effects

A

Myelosuppression with megaloblastic anemia

pancytopenia

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12
Q

Purine Analog Drugs

A

Azathiprine
6-MP
Cladribine
Pentostatin
Hydroxyurea

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13
Q

Azathioprine Mechanism

A

inhibit de novo purine synthesis

activated by HGPRT

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14
Q

Azathioprine use

A

acute lymphocytic leukemia

myelogenous leukemia

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15
Q

Azathioprine Side Effects

A

Myelosuppression
Hyperuricemia
Hepatotoxicity: high or chronic dose

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16
Q

6-MP mechanism

A

inhibit de novo purine synthesis

activated by HGPRT

17
Q

6-MP Use

A

acute lymphocytic leukemia

myelogenous leukemia

18
Q

6-MP side effects

A

Myelosuppression
Hyperuricemia
Hepatotoxicity: high or chronic dose

19
Q

Cladribine Mechanism

A

Prodrug

Inhibit both DNA POL-a and POL-b to interfere with DNA synthesis/repairCla

20
Q

Cladribine Use

A

Hairy Cell Leukemia

21
Q

Cladribine Side Effects

A

Myelosuppression
Nephrotoxic
Neurotoxicity

22
Q

Pentostatin Mechanism

A

Inhibit both DNA POL-a and POL-b to interfere with DNA synthesis/repair

23
Q

Pentostatin Use

A

Hairy Cell Leukemia

24
Q

Pentostatin Side Effects

A

Myelosuppression
Nephrotoxic
Neurotoxicity

25
Q

Hydroxyurea Mechanism

A

Block Ribonucleotide Reductase to decrease DNA Synthesis

26
Q

Hydroxyurea Use

A

Chronic Myelogenous Leukemia (CML)

27
Q

Hydroxyurea side effects

A

Severe Myelosuppression
Megaloblastic anemia

Pharmacology (18 decks)

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