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M3 Pharm B3 > Anti-neoplastic Agents 2 - Antimetabolites > Flashcards

Anti-neoplastic Agents 2 - Antimetabolites Flashcards

1
Q

Antimetabolites: Purine Analog - 6-Mercaptopurine (6MP) MOA and Reduce dose when?

A

Activated by HGPRT to 6-thioinosinic monophosphate –> inhibition of purine nucleotide synthesis

Reduce dose if given with allopurinol

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2
Q

Antimetabolites: Purine Analog - 6-thioguanine (6TG) (1)

A

No dose modification with allopurinol

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3
Q

Antimetabolites: Pyrimidine Antagonists - 5-fluorouracil (5FU) (MOA (2)

A

5FU –> Fdump

Inhibits thymidylate synthase –> thymineless death

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4
Q

Antimetabolites: Pyrimidine Antagonists - 5-fluorouracil (5FU) Toxicities (4)

A
  1. Nausea
  2. Mucositis (esophageal ulcers)
  3. Diarrhea
  4. Hand and foot syndrome
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5
Q

Antimetabolites: Pyrimidine Antagonists - 5-fluorouracil (5FU) Capecitabine MOA

A

Convereted to fluorouracil in the tumor

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6
Q

Antimetabolites: Pyrimidine Antagonists - 5-fluorouracil (5FU) Cytarabine Dependent and Use

A

Highly schedule dependent (S phase)

Used in acute myelogenous leukemia

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7
Q

Antimetabolites: Folate Antagonist - Methotrexate (MTX) MOA (4)

A

Inhibits dihydrofolate reductase (DHFR)

Tetrahydrofolate not synthesized

Inhibits DNA, RNA, and protein synthesis

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8
Q

Antimetabolites: Folate Antagonist - Normal cells require folic acid, so what do we do?

A

Leucovorin rescue (folinic acid)

Antidote to methotrexate toxicity

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9
Q

Antimetabolites: Others - Hydroxyurea Use (2)

A

Used for CML

Used for Sickle Cell Anemia (low dose) –> increase fetal Hbf synthesis

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10
Q
  1. Antibiotics (Anthracyclines): Doxorubicin and Daunorubicin MOA (3)
A
  1. Inhibits topoisomerase II
  2. Binds to DNA through intercalation blockade of the synthesis of DNA and RNA, and DNA strand scission
  3. Generation of semiquinone free radicals
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11
Q
  1. Antibiotics (Anthracyclines): Doxorubicin and Daunorubicin Side Effects (3) and Antidote
A
  1. Cardiotoxicity (side effects)
  2. Acute: pericarditis, arrythmia, ECG changes
  3. Chronic: CHF

Antidote: Dexrazoxane (prevents CHF) - chelating agent

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12
Q
  1. Antibiotics (Anthracyclines): Radiation Recall Reaction - Bleomycin MOA
A

Causes DNA strand scission

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13
Q
  1. Antibiotics (Anthracyclines): Radiation Recall Reaction - Bleomycin Side effects (2)
A
  1. Pulmonary toxicity (pneumonitis with cough, dyspnea, rales, infiltrates)
  2. Skin (redness, hyperpigmentation, and skin tenderness)
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14
Q
  1. Mitotic Inhibitors: Vinca Alkaloids MOA (2)
A

Bind to tubulin: block microtubular polymerization

Cell division is arrested in meta phase

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15
Q
  1. Mitotic Inhibitors: Vinca Alkaloids - Vinblastine Side Effects (2)
A
  1. Bone marrow suppression

2. Alopecia (side effect)

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16
Q
  1. Mitotic Inhibitors: Vinca Alkaloids - Vincristine Side Effects (1)
A

Peripheral neuropathy

17
Q
  1. Mitotic Inhibitors: Vinca Alkaloids - Vinorelbine Side Effect (1)
A

Bone Marrow Suppression

18
Q
  1. Mitotic Inhibitors: Taxanes - Paclitaxel (Taxol) MOA
A

Enhancement of tubulin polymerization

19
Q
  1. Mitotic Inhibitors: Taxanes - Paclitaxel (Taxol) Rx of (3)
A
  1. Breast cancer
  2. Lung cancer
  3. Ovarian cancer
20
Q
  1. Mitotic Inhibitors: Taxanes - Docetaxel Rx of (1)
A

Advanced breast cancer

21
Q
  1. Mitotic Inhibitors: Taxanes - Paclitazel and Docetaxel are metabolized by?
A

Cytochrome P450

22
Q
  1. Miscellaneous: Topoisomerase Inhibitors - 2 types and use
A
  1. Etopside and Teniposide: lung cancer

2. Irinotecan and Topotecan: colorectal cancer

23
Q
  1. Miscellaneous: Enzymes - L-Asparaginase MOA
A

Catalyses hydrolysis L-asparagine to aspartic acid (tumor cells require L-asparagine for growth)

24
Q
  1. Miscellaneous: - L-Asparaginase Side Effects (1)
A

Pancreatitis

25
Q
  1. Miscellaneous: Tyrosine Kinase Inhibitors - Imatinib (GLEEVEC) MOA (2) and Use (1)
A

Inhibitor of tyrosine kinase domain bcr-able oncoprotein

Prevents the phosphorylation of kinase substrate by ATP

First line therapy in chronic phase of CML and blast crisis

26
Q
  1. Miscellaneous: Tyrosine Kinase Inhibitors - Vemurafenib (2)
A
  1. B-raf enzyme inhibitor

2. Used in melanoma patients whose cancer has a V600E BRAF mutation

27
Q
  1. Miscellaneous: Growth Factor Receptor Inhibitors - Gefitinib (IRESSA) and Erlotinib (TARCEVA) MOA
A

Inhibitor of the tyrosine kinase domain assoicated with the EGFR (epidermal growth factor receptor)

Used in non-small cell lung cancer

28
Q
  1. Miscellaneous: Growth Factor Receptor Inhibitors - Cetuximab (ERBITUX)
A

EGFR inhibitor used in metastatic colorectal cancer

29
Q
  1. Miscellaneous: Growth Factor Receptor Inhibitors - Rituximab (RITUXAN) Target and Use (2)
A

Attacks CD20

Used in B cell lymphoma

30
Q
  1. Miscellaneous: Growth Factor Receptor Inhibitors - Trastuzamab (HERCEPTIN) Target and Use
A

HER2/Neu (ErbB-2)

Used in breast cancer

31
Q
  1. Miscellaneous: Growth Factor Receptor Inhibitors - Lapatinib (TYKERB) Chemo protocols
A

Hodgkin’s Disease: ABVD region

Adriamycin (doxorubicin)
Bleomycin
Vinblastine
Dacarbazine

32
Q

Resistance to Chemotherapy: Formation of cancer drug inactivating enzymes

A

6-mercaptopurine and 5-FU

33
Q

Resistance to Chemotherapy: Decrease of binding affinity and drug sensitivty (4)

A
  1. Etoposide
  2. Methotrexate
  3. Vincristine
  4. Vinblastine
34
Q

Resistance to Chemotherapy: Decrease drug accumulation or permeability (3)

A
  1. Methotrexate
  2. Dactinomycin
  3. Cyclophosphamide
35
Q

Resistance to Chemotherapy: Chemical Reactions Inactivating Chemotherapy (3)

A
  1. Cyclophosphamide
  2. Bleomycin
  3. Cisplatin
36
Q

Resistance to Chemotherapy: Increased nucleic acid repair mechanism (2)

A
  1. Cisplatin

2. Cyclophosphamide

37
Q

Resistance to Chemotherapy: Reduced activation of pro-drgs 2)

A
  1. 6-mercaptopurine

2. 5 FU

38
Q

Resistance to Chemotherapy: Multdrug resistances MOA (2)

A
  1. Increased expression of MDR1 gene for P-glycoprotein

2. Overexpression of the multidrug resistance protein 1 (MRP1_ t

M3 Pharm B3 (10 decks)

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