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CMOD Pharm > Topoisomerase and Spindle Inhibitors > Flashcards

Topoisomerase and Spindle Inhibitors Flashcards

1
Q

Drug classes for mitotic spindle inhibitors

A
  1. Vinca alkaloids

2. Taxanes

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2
Q

Drug classes for topoisomerase inhibitors

A
  1. Camptothecin analogs
  2. Podophyllotoxins
  3. Anthracyclins
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3
Q

Drugs in vinca alkaloid class

A
  1. Vincristine
  2. Vinblastine
    M phase arrest
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4
Q

Mechanism for vinca alkaloids

A

Bind to beta-tubulin to block alpha-beta polymerization of microtubules form the + end –> causes M phase arrest

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5
Q

Unique toxicities of vinca alkaloids

A
  1. Leukopenia with vinblastine

2. Significant neurotoxicity due to disrupted microtubule formation (worse with Vincristine)

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6
Q

Unique mechanism of resistance for vinca alkaloids

A

Mutation of beta-tubulin structure

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7
Q

Drugs in taxane class

A
  1. Paclitaxel
  2. Docataxel –> semi-synthetic, less hypersensitivity
    M phase specific
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8
Q

Mechanism for taxanes

A

Binds to microtubules (B-tubulin) and prevents disassembly –> disrupts mitotic spindle

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9
Q

Taxane IV infusion

A
  1. Paclitaxel –> cremaphor
  2. Docataxel –> Polysorbate 80
    Co-administer with antihistamines and steroids to prevent hypersensitivity
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10
Q

Unique toxicities of taxanes

A

Blood dyscriasis and peripheral neuropathy

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11
Q

Neurotoxicity or nerve axons and/or dorsal root ganglion of sensory nerves caused by?

A
  1. Vincas
  2. Taxanes
  3. Platinum drugs
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12
Q

Drugs in camptothecin analog class

A
  1. Topotecan

2. Irinotecan

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13
Q

Camptothecin analog mechanism

A

Stabilizes DNA topoisomerase I cleavable complex leading to single and double stranded DNA breaks

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14
Q

Unique toxicity of irinotecan

A

Metabolized by Phase II glucuronidation so some patients can receive toxic dose if they have mutations in UDP-glucuronosyltransferase 1A1 gene

dose limiting toxicity is diarrhea believe it or not

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15
Q

Drug in podophyllotoxin class

A

Etoposide (VP-16)

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16
Q

Mechanism of etoposide

A

Binds to the DNA-topoisomerase II complex and prevents religation of DNA –> strand breaks and apoptosis

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17
Q

Drugs in anthracyclines class

A
  1. Doxorubicin
  2. Daunorubicin
  3. Idarubicin
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18
Q

Mechanism of anthracyclines

A
  1. DNA intercalation
  2. Stabilize DNA-topoisomerase II complex
  3. Generate free radicals
19
Q

Unique toxicities of anthracyclines

A

Cardiotoxicity (primarily doxorubicin)
Acute: tachycardia, arrhythmia, hypotension
Chronic: CHF
Dilated, flabby heart

20
Q

Ways to reduce toxicity of anthracyclines

A
  1. Co-administer dexrazoxane to prevent free radical damage

2. Liposomal formulations of doxorubicin (less cardiotoxic)

21
Q

Do both Vinca Alkaloids cause leukopenia?

A

No, Vincristine does not

22
Q

How are Vinca Alkaloids excreted?

A

Hepatically

23
Q

What can occur with Vinca Alkaloids upon IV administration?

A

Extravasational Necrosis, local tissue necrosis if the drug escapes the vasculature into the surrounding tissues

24
Q

How must the Taxanes be administered?

A

IV infusion with cermaphor or polysorbate (both surfactants). Taxanes are very insoluble by themselves

25
Q

What physical exam findings would you look for if concerned about taxane peripheral neuropathy?

A

1) loss of deep tendon reflex (patellar)

2) inability to get up out of a chair without using arm muscles

26
Q

Are taxanes and vincas cell cycle specific?

A

Yes, both are only effective during mitosis

27
Q

Mechanism of bleomycin

A

Bleomycin-Fe complex oxidizes deoxyribose on nucleotides causing single and double strand breaks

28
Q

Unique toxicities of tretinoin

A

Dry skin, bone tenderness, hyperlipidemia, cheilitis (inflammation of lips)

29
Q

Mechanism of pegaspargase

A

Asparagine supply broken down so protein synthesis is halted

30
Q

Unique toxicities of pegaspargase

A

Necrotic pancreatitis (THIS), immune suppression, and poor regulation of blood sugar

31
Q

Lenalidomide mechanism

A
  1. Inhibits tumor cell proliferation
  2. Inhibits tumor cell adhesion
  3. Inhibits angiogenesis
  4. Enhances NK cell activity
32
Q

Unique toxicities of lenalidomide

A

Peripheral neuropathy, sedation, constipation, arterial/venous embolism

33
Q

Mechanism of tretinoin

A

High dose of tretinoin binds to PML-RAR cancer fusion protein and releases it from co-repressors allowing promyelocytes to mature and stop proliferating

34
Q

Unique toxicities of tretinoin

A

Dry skin, bone tenderness, hyperlipidemia, cheilitis

35
Q

Rules for combination therapies

A
  1. No two drugs act through same mechanism
  2. Drugs with overlapping toxicities are avoided
  3. Proven activity against the tumor type
36
Q

Dose limiting toxicity of Irinotecan

A

Diarrhea

37
Q

Cell Cycle specificity of Etoposide?

A

Late S/Early G2

38
Q

Indications for Doxorubicin

A

Solid tumors, especially breast

39
Q

Problem with administering liposomal Doxorubicin?

A

It causes Hand Foot Syndrome

40
Q

Unique mechanism of resistance to Doxorubicin?

A

Increased Glutathione Peroxidase expression

41
Q

Cell cycle specificity of Bleomycin?

A

Early G2

42
Q

Problem with administration of Pegaspargase?

A

Some people have hypersensitivity reactions to it, Aspargase generated from bacteria

43
Q

What is Chemo-Fog??

A

Impaired verbal/visual memory, attention deficits, concentration problems, issues with speech, multitasking, and organization post chemotherapy… Cytotoxic therapy releases lots of TNF-a which crosses the BBB and can permanently damage brain by production of reactive Nitrogen Species

44
Q

pharmacogenomic risk factor of toxicity w/ Irinotecan

A

Gilbert’s syndrome

CMOD Pharm (8 decks)

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