Anti cancer Drugs 3 Flashcards

1
Q

Fulvestrant is an SERD (selective estrogen receptor downregulators). What is its mechanism

A

Binds to ER and inhibits its dimeriztain and increases its degradation

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2
Q

The only source of estrogen in post menopausal women is from the ocversoin of _________ to _______ by _________

A

Androstenedione; estrone; aromatase

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3
Q

Aromatase inhibitors are the used for ________

A

Adjuvant therapy for post menopausal women with hormone receptor positive breast cancer

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4
Q

Nonsteroidal aromatose inhibitors

A

Anastrozole and letrozole Reversible competitive inhibitor of aromatase

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5
Q

Steroidal aromatase inhibitors

A

Exemestane Irreversible inhibitor of aromatase

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6
Q

Examples of GnRH agonists and what do they do?

A

goserelin and leuprolide They cause an initial surge in LH and FSH followed by an inhibition of gonadotropin release

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7
Q

To prevent the intital increase of testosterone when administering GnRH agonsts, give _______

A

Flutamide

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8
Q

Mechanism of flutamide

A

It is a non steroidal anitandrogen that is a competitive antagonist at the androgen receptor

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9
Q

Mechanism of imatinib

A

Inhibitor fo tyrosine kinase of Bcr-Abl

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10
Q

Mechanism of Trastuzumab

A

Monoclonal antibody against ErB2

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11
Q

Mechanism of asparaginase

A

It hydrolyzes serum asparagine and thus depriving the tumor cells of the asparagine that is necessary for protein synthesis (Neoplastic tissues require exogenous source of asparagine)

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12
Q

Adverse effects of asparaginase

A

HS, ↓ in clotting factors (but paradoxically have more thrombotic events), liver abnormalities, pancreatitis (asparaginase can activate enzymes while they are in the pancreas), and seizures and coma due to ammonia toxicity

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13
Q

Hydroxyurea inhibits ______ causing …

A

Ribonucleotide reductase; depletion of deoxynucleoside triphasophate pools and thus arresting DNA synthesis /

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14
Q

Hydroxyurea kills cells in the ____ phase

A

S

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15
Q

Interferon α is used to treat:

A
  • hairy cell leukemia - CML - malignant melanoma - kaposi sarcoma
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16
Q

Mechanism of interferon α

A
  • increase the expression of HLA molecules on tumor cells so they can be destroyed - activates NK cells to destroy tumor cells
17
Q

Mechanism of vinca alkaloids

A

Binds to β tubulin and hinhits it’s ability polymerize to microtubules and cells arrest in metaphase and die by apoptosis

18
Q

Adverse effects of vincristine

A

Peripheral neuropathy with MILD bone marrow depression

19
Q

Adverse effects of vinblastine

A

Myelosuppresion is the dose limiting diverse effects and other adverse effects include alopecia and peripheral neuropathy

20
Q

What is the difference in adverse effects between vincristine and vinblastine?

A

Vincristine has mild bone marrow suppression while that is the dose limiting adverse effect for vinblastine Vincristine has much worse peripheral neuropathy

21
Q

Mechanism of taxaxes (paclitaxel and docetaxel)

A

Bind to β tubules but they allow for the polymerization of microtubules but PREVENTS DEPOLYMERIZATION

22
Q

What is the difference between the mechanism of vinca alkaloids and taxanes?

A

Vinca alkaloids do not allow for the polymerization of the microtubules while taxanes do but with taxanes no depolymerization

23
Q

Adverse effects of paclitaxel

A

HS, myelosuppresoin, peripheral neuropathy and alopecia

24
Q

Adverse effects of docetaxel

A

Peripheral neuropathy is not as bad as in paclitaxel

25
Q

_________ is required to prevent fluid retention when taking docetaxel

A

Dexamethasone

26
Q

__________ is dose limiting in docetaxel

A

Myelosuppresion

27
Q

Etoposide inhibits _____________ and blocks the cell at _______

A

Topoisomerase II (breaks DNA on BOTH strands) S-G2 phase

28
Q

Campothecins inhibits _____________

A

Topoisomerase I

29
Q

Prednisone is used for ___________ and what is its mechanism

A

Acute leukemia and malignant lymphomas Prednisone is a glucocorticoid and they are lymphocytic and suppress mitosis in lymphocytes

30
Q

Selective estrogen receptor modulators act as agonists on _______ and as antagonists on ________

A

Bone, endometrium; breast

31
Q

Tamoxifen is an _________ on breast cancer and is used for ____________ breast cancer

A

Antagonist; receptor positive

32
Q

Raloxifene is a SERM that acts as an ___________ on the bone to inhibit ________

A

Agonist; resorption

33
Q

_________ is a SERM that does not have risk for endometrial cancer when using it

A

Raloxifene

34
Q

What are some uses for raloxifene?

A

Prevention of post menopausal osteoporosis and prophylaxis of breast cancer in high risk post menopausal women