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7361 Hem/Onc Block 1 > Microtubule Agents, Cell Cycle Inhibitors > Flashcards

Microtubule Agents, Cell Cycle Inhibitors Flashcards

1
Q

Antimitotic anticancer agents disrupt which phase of the cell cycle?

A

M phase

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2
Q

Antimitotics (vinca alkaloids, taxanes, epothilones) exert their effects by disruption of __ dynamics

A

microtubule

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3
Q

What happens to tubules during cell division?

A

alternating periods of elongation and shortening

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4
Q

ixabepilone is what drug class?

A

epothilone

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5
Q

Which drug class INHIBITS the ASSEMBLY of microtubules?

A

vinca alkaloids

vincristine, vinblastine, vinorelbine

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6
Q

Which two drug classes PROMOTE microtubule assembly and INHIBIT disassembly?

A

taxanes
epothilone (ixabepilone)

stabilize microtubules

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7
Q

What mediates resistance to vinca alkaloids?

A

MDR1 and P-gp

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8
Q

Pts with what disorder should have dose reductions of vinca alkaloids?

A

hepatic dysfunction

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9
Q

Approximately half of US children with cancer who get chemotherapy will be given what drug?

A

vincristine

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10
Q

What is the most significant dose limiting toxicity of vincristine?

A

peripheral neuropathy

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11
Q

Where should vinca alkaloids NEVER be injected

A

CSF

Inadvertent injection of vinca alkaloids into the CSF causes a devastating and often fatal irreversible coma and seizures

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12
Q

What toxicity is associated with vinblastine?

A

myelosuppression (leukopenia)

usually reaches its maximum 7-10 days post dose with recovery ~ 7 days after maximum myelosuppression is reached

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13
Q

Does vinblastine have severe neurological side effects?

A

no

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14
Q

What toxicity is associated with vinorelbine?

A

granulocytopenia

neurotoxicity typically mild

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15
Q

Which drug class has a tricyclic core?

A

taxanes

fused to oxetane ring and a beta phenylisoserine ester

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16
Q

Which taxane is more lipophilic?

A

paclitaxel

17
Q

A hydroxyl group at what carbon enhances the solubility of docetaxel?

A

C10

18
Q

A modified side chain at what carbon of docetaxel and cabazitaxel causes enhanced cytotoxic potency?

A

C13

19
Q

How do taxanes interrupt cell division?

A

form large and dense aberrant structures

20
Q

Which drug class binds polymerized β-tubulin of microtubules promoting a stable conformation that promotes elongation and inhibits depolymerization?

A

taxanes

21
Q

Taxanes are substrates of what transporter?

A

P-gp

efflux via P-gp contributes to resistance

22
Q

What is the major metabolite of paclitaxel?

A

6 alpha hydroxypaclitaxel

23
Q

What CYP forms the major metabolite of paclitaxel?

A

2C8

24
Q

Which taxane is O-demethylated at C10 and C7 by CYP3A4/5?

A

cabazitaxel

forms three active metabolites including docetaxel

25
Q

Most taxane metabolites are excreted via what route?

A

biliary

26
Q

Which taxane has very limited water solubility?

A

paclitaxel

27
Q

Which taxane is administered in a vehicle of 50% ethanol and 50% polyethoxylated castor oil?

A

paclitaxel

causes hypersensitivity rxns

28
Q

What must pts on paclitaxel be premedicated with?

A

H1 antagonist
H2 antagonist
glucocorticoid

29
Q

A formulation of paclitaxel bound to ___ has better water solubility and does not require pretreatment.

A

albumin

30
Q

Caution should be used when co-administering paclitaxel with drugs that compete for what CYP?

A

2C

ex. ethinyl estradiol, diazepam

31
Q

Which has better solubility paclitaxel or docetaxel?

A

docetaxel

can be used with more tolerable vehicle (polysorbate 80)

32
Q

What is required for pretreatment with docetaxel?

A

glucocorticoid (dexamethasone)

required to prevent t progressive fluid retention

33
Q

What reduces P-gp affinity of cabazitaxel resulting in longer retention in tumor cells and improved BBB penetration?

A

methyl ethers

34
Q

Which taxane is formulated with polysorbate 80, but does NOT cause fluid retention?

A

cabazitaxel

35
Q

Which is less susceptible to P-gp mediated drug resistance, taxanes or epothilones?

A

epothilones (ixabepilone)

36
Q

What enhances the metabolic stability of ixabepilone relative to epothilone B?

A

lactam replacement

37
Q

Ixabepilone has very good water solubility.

a. true
b. false

A

b. false

like paclitaxel, ixabepilone has very limited water solubility

38
Q

What part of ixabepilone formulation causes hypersensitivity reactions?

A

50% polyethoxylated castor oil

7361 Hem/Onc Block 1 (9 decks)

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