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CMOD/PCM- Block 2 > Pharm: Anticancer Drugs 3 > Flashcards

Pharm: Anticancer Drugs 3 Flashcards

1
Q

List the two drug classes that act by blocking microtubule activity in the nucleus.

A

vinca alkaloids= vincristine & vinblastine

taxanes= docetaxel & paclitaxel

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2
Q

Vinca alkaloids block:

Cancers can overcome this MOA by:

A

tubulin polymerization

Overcome by mutation in the beta-tubulin structure, reducing drug affinity for target

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3
Q

What are universal resistance mechanisms to vinca alkaloids?

A

increased drug efflux (multi-drug resistance protein MRP or breast cancer resistance protein BCRP)

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4
Q

What phase of the cell cycle to vinca alkaloids halt the tumor cell in?

A

Metaphase> results in apoptosis

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5
Q

Describe the toxicities of the vinca alkaloids.

A

Leukopenia with vinblastine, NOT vincristine
Alopecia and local cellulitis if extravasated
neurotoxic symptoms, more so in vincristine
Extravasational necrosis
High-dose vincristine causes severe constipation

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6
Q

Although both vinca alkaloids and taxanes inhibit microtubule function, taxanes work differently than vincas. Explain how.

A

Taxanes inhibit disassembly of the microtubules, in contrast to vincas, which prevent assembly.

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7
Q

Describe the side effects of the taxanes.

A

Paclitaxel:
Bone marrow suppression
High incidence of peripheral neuropathy
Hypersensitivity infusion rxns

Docetaxel:
Peripheral neuropathy
More severe, but short-lived neutropenia

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8
Q

List the 3 classes of anticancer drugs most commonly associated with neurotoxicity.

A

Microtubule blockers: vinca alkaloids & taxanes

Alkylating agent: Cisplatin

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9
Q

Vinca alkaloids and taxane drugs will cause peripheral neuropathy because:

A

They inhibit microtubules that are necessary for transport of signaling molecules to terminal ends of an axon.

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10
Q

Whereas the vincas and taxanes affect the distal axons of the nerves, alkylating agents such as Cisplatin will produce their toxicity by:

A

accumulating in the ganglion cells where apoptosis ensues

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11
Q

Describe the character of the neuropathies caused by the vinca alkaloids, taxanes, and the alkylating agent Cisplatin.

A

Neuropathies seen as paresthesias in a stocking-glove distribution, areflexia, loss of proprioception, vibratory sensation, and loss of taste

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12
Q

___________ (drug) is associated, especially, with a “glove and stocking” neuropathy characterized by tingling that originates in the tips of the hands and soles of the feet, sharply stopping at the wrists and ankles.

A

Paclitaxel (a taxane)

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13
Q

This enzyme cuts both strands of the DNA helix in order to manage DNA tangles and supercoils. This is essential for strand separation and DNA replication.

A

Topoisomerase II

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14
Q

Are the drugs that inhibit the action of topoisomerase II cell cycle specific?

A

No

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15
Q

What is the class of drugs that blocks Topo II function?

A

Camptothecins

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16
Q

How can tumor cells overcome the action of the Camptothecins?

A

Efflux mechs, alter the drug target (topo II)

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17
Q

Name the two Camptothecin drugs.

A

Irinotecan & Topotecan

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18
Q

The camptothecins are specific for which phase of the cell cycle?

A

They are not cell cycle specific, remember?! They’re Topo II inhibitors!

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19
Q

Gilbert’s syndrome is associated with increased toxicity of which camptothecin drug?

A

irinotecan

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20
Q

The camptothecins are associated with what toxicities?

A

Topotecan:
myelosuppression, musositis & diarrhea, elevated hepatic enzymes

Irinotecan:
dose limiting diarrhea, myelosuppression, N/V, mucositis, alopecia, elevated hepatic enzymes

21
Q

Describe the MOA of etopside.

A

Topoisomerase II inhibitor

22
Q

Describe the side effects of etopside.

A

Typical of chemo drugs: alopecia, myelosuppression

23
Q

Describe the MOA of the Anthracycline class of anticancer drugs.

A

Intercalate with DNA, altering critical topography.
Free radical formation
Topo II stabilization, inhibiting DNA replication

24
Q

Describe how the increased glutathione peroxidase expression by cancers can cause resistance to anthracyclines.

A

produces increased ability for the cell to “soak up” free radical generated by the drug treatment.

25
Q

List the 3 anthracycline drugs.

A

Daunorubicin, Doxorubicin, Idarubicin

26
Q

Describe the side effects of the anthracycline class of drugs.

A

Myelosuppression, alopecia, GI disturbances
Acute: tachycardia, arrhythmias, hypotension, reduced ejection fraction (tachycardia), troponin-T release
Chronic: CHF- 50% mortality
Cardiotoxicity= most distinctive ADE

27
Q

How can you protect normal tissue from the ADEs of anthracyclines?

A

dexrazoxane, iron chelating agent (inhibits Fe free radical generation), may protect against cardiotoxicity
Liposomal Dox preps less cardiotoxic

28
Q

Describe the MOA of Bleomycin

A

Causes single & double strand DNA breaks

29
Q

Describe a mechanism of drug resistance tumor cells express towards bleomycin.

A

Increased capacity for inactivation, degradation by specific hydrolase

30
Q

Describe the side effects of treatment with bleomycin.

A

pulmonary dysfunction (dose limiting)
Hypersensitivity rxns
alopecia, blisters, keratosis
(skin/lung tox. may be related to low levels of hydrolysis)

31
Q

How does asparaginase (Pegaspargase) work as an anticancer drug?

A

degrades asparagine, thus ‘starving’ protein synthesis of this essential component.

32
Q

What are the significant toxicities of pegaspargase?

A

pancreatitis, immune system suppression and problems in regulating blood sugar levels.

33
Q

Describe the indications and specific actions of Lenalidomide.

A

Indications: myeloma and myelodyspastic syndrome
Uses: Inhibits tumor cell proliferation, inhibits tumor cell adhesion to stroma, inhibits angiogenesis, enhances NK cell activity

34
Q

Describe the side effects of lenalidomide.

A

blood dyscrasias, peripheral sensory neuropathy, sedation, constipation, venous and atrial embolism

35
Q

Describe the MOA of the retinoid class of anticancer drugs.

A

Overcome the block (by transcriptional co-repressors) in myeloid differentiation that contributes to acute promyelocytic leukemia (APML). Retinoic acid binds transcriptional co-activators resulting in proper gene expression and granulocytic differentiation.

36
Q

As a reminder:

Allopurinol and rasburicase are given as adjuvants to mitigate the effects of:

A

Tumor lysis syndrome

- reduce uric acid level; renal protective

37
Q

As a reminder:

Mesna is given as an adjuvant to mitigate the negative effects of:

A

Cyclophosphamide, ifosfamide

- protect against acrolein product

38
Q

As a reminder:

Amifostine is given as an adjuvant with:

A

Cisplatin

- cytoprotection

39
Q

As a reminder:

Leucovorin is given as an adjuvant with:

A

MTX- metabolic rescue

5-FU- enhanced action

40
Q

As a reminder:

Allopurinol is given as an adjuvant with:

A

6-MP (mercaptopurine)

- CAUTION: increases toxicity!

41
Q

As a reminder:

Dexroxazone is given as an adjuvant with:

A

Anthracyclines

- Fe chelator; reduces cardiotoxicity

42
Q

Neurotoxicity is especially associated with which anticancer drug?

A

Vincristine

43
Q

Leukopenia and lesser peripheral neurotoxicity are associated with which vinca alkaloid?

A

Vinblastine

44
Q

GI toxicity, avoidance of Gilbert syndrome, and AchE inhibition are associated with which camptothecin?

A

irinotecan

45
Q

Peripheral neuropathy is especially associated with which taxane?

A

Paclitaxel

46
Q

Edema-fluid retention and peripheral neuropathy are associated ADEs with which taxane?

A

Docataxel

47
Q

Cardiotoxicity is especially associated with which class of anticancer drugs?

A

Anthracyclines

48
Q

Pulmonary fibrosis is especially associated with which anticancer drug?

A

Bleomycin

49
Q

Pancreatitis is especially associated with which anticancer drug?

A

Asparaginase (Pegaspargase)

CMOD/PCM- Block 2 (41 decks)

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