Cancer Pharmacology Flashcards

1
Q

Methotrexate is a ___ analog

A

Folic Acid

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2
Q

MOA of Methotrexate

A

Inhibits dihydrofolate reductase

Blocks conversion of folic acid to tetrahydrofolic acid

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3
Q

When treating with methotrexate, there with be decreased synthesis of ____ (4x)

A

1) Denovo synthesis of Thymidylate
2) Purine nucleotides
3) Serine
4) Methotrexate

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4
Q

What is the rescue drug that is used with methotrexate

A

Leucovorin (Folinic Acid)

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5
Q

Leucovorin bypasses the ___ and is converted to ___

A

1) Dihydrofolate reductase

2) N5N10 Methylene FH4

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6
Q

With Leucovorin administration with Methotrexate, there will be less severe ____ and ____ toxicity

A

1) Gastrointestinal

2) Bone Marrow

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7
Q

Adverse Effects of Leucovorin

A

Mucositis: Mucosal Ulceration and Myelosuppression

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8
Q

Pt comes in with a glioblastoma. What is the MOA of the agent that you would use to treat this CNS tumor?
What is the name of the agent?

A

1) Forms covalent linkages with DNA via intra- and inter strand crosslinking
2) Carmustine

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9
Q

How does DNA crosslinking prevent replication in cancer?

A

1) Prevents unwinding DNA for mRNA production or DNA replication

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10
Q

List the microtubule drugs

A

1) Vinca Alkaloids

2) Taxanes

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11
Q

Examples of Vinca Alkaloids - microtubule drug

A

1) Vinblastine

2) Vincristine

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12
Q

Examples of Taxanes - Microtubule drugs

A

Paclitaxel

Docetaxel

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13
Q

MOA of Vinca Alkaloids

A

Microtubule Destabilization: Binds B-tubulin and inhibits microtubule assembly

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14
Q

MOA of Taxanes

A

B-tubulin and promote microtubule formation and stabilization

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15
Q

Adverse Effects of Vinca Alkaloids

A

1) Hair loss and local Cellulitis

2) Numbness and Tingling of extremities and loss of deep tendon reflexes –> Motor weakness

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16
Q

Adverse Effects of Taxanes

A

1) Peripheral Sensory Neuropathy (Paclitaxel)
2) Fluid retention
3) Neutropenia (Docetaxel)

17
Q

Vinca Alkaloids and Taxanes both halt cell in ___

A

M phase

18
Q

Use ___ for treatment of non-small cell lung cancer with high levels of cell surface P-glycoprotein

A

Cabazitaxol

19
Q

___ expression often confers resistance to natural product chemotherapies

A

P-glycoprotein

20
Q

Treat CLL with ___

A

Antracyclins (Doxorubicin)

21
Q

MOA of Doxorubicin (4x)

A

1) Topoisomerase II Inhibitor *******
2) Intercalates DNA and Blocks synthesis of DNA and RNA and blocks DNA strand scission
3) Generates semiquiones and Oxygen free radicals
4) Binds to cellular membrane to alter fluidity and ion transport

22
Q

Acute effects of Doxorubicin (5x)

A

1) Nausea
2) Red Urine
3) Alopecia
4) Myelosuppression
5) Stomatitis

23
Q

Bleomycin v. Doxorubicin Toxicity

A

1) Doxorubicin - Cardiac Toxicity

2) Bleomycin - Pulmonary Toxicity: Pneumonitis w/ cough, SOB, dry crackles, infiltrates on CXR

24
Q

A pt with constipation due to colon cancer can be treated with Ziv-aflibercept and Bevacizumab. What are the MOAs of both?

A

1) Growth Factor Inhibitor - prevents the ligand from interacting with the target
- Ziv-Aflibercepet binds VEGFA1, VEGFB1, and PIGF (Placental Growth factor)
- Bevacizumab binds ALL forms of VEGFA

25
Q

Imatinab treats ___

A

CML

26
Q

MOA of Imatinab (2x)

A
  • ***1) Prevents phosphorylation of kinase substrate by ATP

2) Inhibits PDGFR, Stem cell factor, and cKit (GI stromal Tumors)

27
Q

Adverse side effects of Imatinab

A

1) Fluid Retention of Ankle
2) Periorbital Edema
3) Diarrhea
4) Myalgias

28
Q

6-mercaptopurine is a ___ analog

A

purine

29
Q

6-MP is metabolized via ___ via the 1st pass metabolism

A

Xanthine Oxidase

30
Q

Allopurinol is often given with 6-MP in order to reduce the effects of hyperuricemia due to tumor lysis. If this occurs what must you do?

A

Reduce the dosage of Allopurinol (by 50-75%)

31
Q

List the drugs that are sus. to P-glycoprotein Resistance (5x)

A

1) Anthracyclines: Doxorubicin and Daunorubicin
2) Vinca Alkaloids: Vinblastine and Vincristine
3) Epipodophyllotoxins (Etoposide)
4) Taxanes: (Paclitaxel)
5) Dactinomycin - Antitumor Antibiotic

32
Q

MOA of Anthracyclines

A

Inhibits Topoisomerase II

33
Q

MOA of Vinca Alkaloids

A

antimitotic

34
Q

MOA of Epipodophyllotoxins

A

Inhibits Topoisomerase II via DNA strand breakage

35
Q

What is the DNA strand breakage induced by in Epipodophyllotoxins

A

Ternary Complex of Drug , DNa, and Enzyme

36
Q

List the Epipodophyllotoxins

A

1) Etoposide

2) Teniposide

37
Q

Dactinomycin MOA

A

1) binds dsDNA and intercalates between adj. guanine -cytosine base pairs

38
Q

Dactinomycin will prevent ___ polymerase from transcribing RNA

A

DNA-dependent RNA polymerase