Fitz- Antimitotics and Antineoplastics Flashcards

1
Q

Compare the mechanism of action among anti-mitotic drugs:
Vinca alkaloids
Taxanes
Epilone

A

Vinca alkaloids: Prevent extension of spindles

Taxanes: Enhance assembly

Epilone: Enhance spindle assembly

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2
Q

What is the primary advantage of ixabepilone w/ respect to development of resistance?

A

It is NOT limited by MDR (p-glycoprotein)

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3
Q

What are the mechanisms of resistance for VA and taxanes?

A

VA- decrease accumulation by increasing p glycoprotein, change tubulin so the drug doesn’t bind

Taxanes-p glycoprotein

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4
Q

What toxicities are associated w/ VA?

A

Neuotoxicity
cytotoxic- BMS, N/V
Vesicant

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5
Q

vinCristine is related to ______toxicity, so it’s more likely to be ___________.

A

Cns toicity (more lipid soluble–> fatal intrathecally)

neuotoxic

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6
Q

vinBlastine is realted to __________, so it’s more like to cause

A

cytotoxic sxs: BMS and N and V

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7
Q

When treating with vincristine, what does a loss of reflexes show? What does parasthesis show?

A

Loss of reflexes occurs in 100% of pts ands is a sign that you have titrated the drug correctly.

Parasthesis (pins and needles) is a severe side effect and suggests that you should decrease the dose.

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8
Q

What toxicities are associated w/ taxanes?

A

Drug interactions
Hypersensitivity
hypotension and arrythmias

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9
Q

What are the main differences in the use of glucocorticoids for cancer chemotherapy vs. immunosuppression?

A

Immunosuppression: glucocorticoids are given at a continuous low dose (targets specific antigens and synchronized cell division)

Cancer chemotherapy: glucocorticoids are given at a HIGH dose, pulse (allows normal cells to recover) (cell division is unstimulated and random)

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10
Q

What cytokines have been approved for use in cancer treatment?

A

IL-2
INF alpha
TNF alpha

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11
Q

How do the MOAs differ for the three cytokines?

A

IL-2-Induce and expand T cell
INF alpha- decrease FGF and decrease cell division
TNF alpha- causes fibroblast proliferation, increases IL-6 and 8 to activate B and T cells

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12
Q

Which cytokine has a t 1/2 of 13 mins and can cause fatal hypotension and a coma?

A

IL-2

It must be given continously or in multiple daily doses

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13
Q

Which cytokine causes BMS and depression?

A

IFN alpha

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14
Q

Which cytokine has a short half life and causes flu-like sxs?

A

TNF alpha

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15
Q

What monoclonal ab targets anti-CD 20 B cells?

A

Rituximab

NHL

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16
Q

What monoclonal ab targets anti-CD 53 B cells?

A

ALEM

CLL

17
Q

What monoclonal ab targets IL-2 and diptheria toxin?

A

Denileukin diffitux

18
Q

What are the common side effects of monoclonal antibodies?

A

Hypersensitivity rxns

Infections

19
Q

What monoclonal antibodies cause heart or lung toxicity?

A

Alem

Rituximab

20
Q

What monoclonal antibodies cause tumor lysis syndrome?

A

Alem

Rituximab

21
Q

What are the vinca alkaloids?

A

vincristine
vinblastine
vinorelbine

22
Q

What are taxanes?

A

cabazitaxel
cocetaxel
paclitaxel

23
Q

What is ixabepilone?

A

An epilone

24
Q

What type of drug resistance is commonly seen with vinca alkaloids?

A

Increased expression of p glycoprotein

25
Q

Why is ixabepilone often approved for use in breast cancer pts who have failed anthracycline antibioitc and taxane treatments?

A

Because it DOES NOT produce MDR

26
Q

This drug when used for cancer chemo therapy is given in higher doses w/ a “pulse” regimen.

A

Glucocorticoids

Dexamethasone and prednisone

27
Q

What immunosuppressive antibioitcs are used to prevent rejection following bone marrow transplants?

A

cyclosporin

tacrolimus

28
Q

What immunosuppressive antibiotics are used as angiogenesis inhibitors?

A

Everolimus

Temsirolimus

29
Q

Immunosuppressive antibiotics play a role in what two pathways?

A
  1. NFAT mediated regulation of IL synthesis

2. mTOR regulation of cell growth and angiogenesis

30
Q

What are the common characteristics shared by cytokines used for cancer chemotherapy?

A

Short half lives

NOT cytotoxic by themselves–> recruit immune cells to do the actual killing

31
Q

How are monoclonal antibodies used as drugs and what do they target?

A

They can selectively recruit the immune system to destroy cancer cells (specifically ones w/ molecular targets that distinguish cancer cells from normal cells)

They target CDs and surface proteins.

32
Q

What is the common dose limiting complication of many antineoplastic drugs?

A

BMS

33
Q

To combat BMS colony stimulating factors have been developed. What do they do?

A

Erythropoietin- RBC
FIlgrastim- neutrophils
Sagramostim- gm-csf–> granulocytes, eosinophils, basophils, monocytes
IL-11 and THrobopoietin–> platelets

34
Q

What protein function inhibitors target a unique aspect of a specific cancer type?

A

L asparaginase

Imatinib

35
Q

What protein function inhibitors target less specific cancer types and exploit the overexpression of a particular protein?

A

Erlotinib

Gefitinib

36
Q

What drugs target rapidly dividing cells and/or angiogenesis?

A

Bortezomib
ovrniostat
sorafenib
sunitinib

37
Q

What drugs can induce tumor cell differentiation and lead to apoptosis?

A

Tretinoin

rexinoids like bexarotene