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Pharmacology II > Lecture 36: Anti-Neoplastic Agents > Flashcards

Lecture 36: Anti-Neoplastic Agents Flashcards

1
Q

What are proto-oncogenes

A

Activating mutations, promote cell growth in the absence of cell signals

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2
Q

What are tumor suppressor genes

A

Inactivating genes, overrride checkpoints that prevent growth or cause cell death

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3
Q

Fraction of dividing cells in a tumor ___as tumor size increases

A

Decrease

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4
Q

What are the 2 contributions of mutations to cancer

A
  1. Acting on cancer cells
  2. Acting on micro environment
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5
Q

What are some examples of mutations acting on cancer cells

A

Genome instability and mutation, resisting cell death, deregulating cellular energetic, sustained proliferative signaling, enabling replicative immortality

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6
Q

What are some contributions of mutations acting on the micro environment

A

Evading the growth suppressors, avoiding immune destruction, tumor promoting inflammation, inducing angiogenesis, activating invasion and metastasis

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7
Q

What are some advantages of chemotherapy

A
  1. Tx diffuse disease
  2. Tx areas of difficult anatomical locations
  3. Improved sx outcome
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8
Q

What are some disadvantages of chemotherapy

A
  1. Solid tumors >1mg of tissue resistant
  2. Selection for resistant cells
  3. Adverse effects
  4. Expensive
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9
Q

What is the CHOP protocol for lymphoma

A
  1. Cyclophophamide
  2. Hydroxydanorubicin (doxorubicin)
  3. Oncovin (vincristine)
  4. Prednisone
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10
Q

What is the PD of alkylating agents

A

Convent bonding/cross linking to DNA bases (prefer guanine base), resulting in deletion of modified guanine bases during DNA replication and induce cell apoptosis

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11
Q

What stages of cell cycle to alkylating agents act on

A

All stages

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12
Q

Platinum alkylating agents are strongly absorbed by __, __ and __

A

Liver, bone, GI tissues

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13
Q

Which alkylating agents crosses BBB

A

Procarbazine and active metabolites of limestone

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14
Q

What alkylating agents are prodrugs

A

Dacarbazine, iomustine, cyclophosphamide

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15
Q

What alkylating agent is good for patients with liver issues and why

A

Melphalan because metabolized in plasma by hydrolysis

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16
Q

How are alkylating agents eliminated

A

Renal

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17
Q

What are the adverse effects of alkylating agents

A
  1. Vesication
  2. Dose-limiting toxicity
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18
Q

What is vesication

A

Severe tissue damage resulting from drug getting out of circulation

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19
Q

Which are at higher risk of vesication: pro-drugs or active dugs

A

Active drugs

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20
Q

What is dose limiting toxicity

A

Most severe toxic effect of the drug that does not lead to acute dead

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21
Q

Why is dose limiting toxicity the dosing goal for anti-neoplastic drugs

A

Kills the most cancer cells and reduces risk of developing resistant cancer cells

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22
Q

What is an adverse effect of lomustine

A

Cumulative myelosuppression

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23
Q

What is an adverse effect of cyclophosphamide

A

Necrotizing hemorrhagic cystitis

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24
Q

What alkylating agent causes lethal pulmonary edema in cats

A

Cisplatin

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25
What is an adverse effect of carboplatin
Leukopenia
26
What is resistance mechanism against cyclophosphamide
Aldehyde dehydrogenase inactivates drug
27
What are some resistance mechanisms common to all alkylating drugs
1. Increased expression of DNA repair enzymes 2. Increasing expression of P-gp
28
Melphalan is taken up by the __transport system and therefore reducing expression of enzymes in that transport drug can cause resistance
Leucine
29
Mechlorethamine is taken up by __transport system and therefore reducing expression of enzymes that transport drug can cause resistance
Chlorine
30
What are anthracyclines- doxorubicin, mitoxantrone, and dactinomycin used to tx
Canine lymphoma
31
What is PD for doxorubicin
Combines with iron and catalyzes generation of oxygen radicals causing DNA damage leading to apoptosis, lipid perioxidation of cell membrane
32
Doxorubicin and mitoxantrone inhibit __ and therefore block __ and reduce ___
Topoisomerase II, DNA replication, RNA/protein synthesis
33
Dactinomycin inhibits ___
DNA dependent RNA synthesis
34
Where does doxorubicin, mitoxantrone and dactinomycin act in cell cycle
All phases
35
Anthracyclines- doxorubicin, mitoxantrone, and dactinomycin are excluded from CNS by __ and therefore problem in ___
P-gp, collies
36
How are anthracyclines metabolized
Hepatic
37
How is doxorubicin eliminated
40-50% in feces, 10% in urine
38
How is mitoxantrone eliminated
100% drug eliminated unchanged in urine
39
How is dactinomycin eliminated
Unchanged in urine and feces
40
What are some early adverse effectives of doxorubicin
Nausea, vomiting, anaphylaxis, ventricular arrhythmia
41
What are some intermediate adverse effects of doxorubicin
Alopecia, thrombocytopenia, neutropenia, vesication
42
What drug can be used to mitigate vesication caused by doxorubicin
Dexrazoxane
43
What are some chronic adverse effects in dogs associated with doxorubicin and how does it happen
DCM- oxygen radicals damage cardiomyoctes in SR
44
What type of dogs are more susceptible to DCM from doxorubicin
ABCB1-/- (collies)
45
What are some chronic adverse effects in cats with doxorubicin and how does it happen
Chronic renal failure - oxygen radicals damage podocytes of renal glomeruli
46
What are some adverse effects of dactinomycin
Myelosuppression, diarrhea, ulcerative stomatitis, urate sone formation in dogs with SLC2A9 mutation (Dalmatians), vesicant
47
What are some mechanisms of resistance to anthracyclines
1. Increased P-gp expression 2. Increased glutathione- reduces free radical production
48
What is the PD for nucleotide analogs- cytarabine, gemcitabine
Incorporated into growing DNA strand during S phase, DNA polymerase can;t read modified sugars, resulting in death of daughter cells
49
You can only give gemcitabine ___only
IV
50
How is cytarabine and gemcitabine metabolize
Converted to Ara-U in liver and kidneys by cytosine deaminase
51
What are some adverse effects of cytarabine and gemcitabine
Myelosuppression- leukopenia most common, anemia, thrombocytopenia
52
How does resistance develop to cytarabine and gemcitabine occur
1. Increased P-gp 2. Increased expression of cytosine deaminase
53
What is rabacfosadine labeled for
Canine lymphoma
54
What is the PD for rabacfosadine
Guanine analog incorporated into DNA chain of replicating cells, does not have ribose base that DNA polymerase recognizes and terminates DNA replication in S phase
55
What are some adverse effects of rabacfosadine
Pulmonary fibrosis, tachypnea, cumulative dermatology, bone marrow suppression, GI effects, lethargy, tachycardia
56
What are some CI of rabacfosadine
1. Existing pulmonary fibrosis 2. Chronic pulmonary disease 3. West Highland White Terriers
57
What is the PD for vincristine, vinblastine, paclitaxel
Act to stabilize microtubules, prevent proper breakdown of mitotic spindle during cytokinesis and induce apoptosis during M phase of cell cycle
58
Vincristine and paclitaxel sites of action differ, theses drugs act __
Synergistically
59
Vincristine, vinblastine and paclitaxel are excluded from CNS via __, therefore problem in ___
P-gp, collies
60
Which one has more CNS toxicity: vincristine or vinblastine
Vincristine
61
How is vincristine, vinblastine and paclitaxel metabolized
Hepatic
62
How is vincristine, vinblastine, and paclitaxel eliminated
GI, biphasic, slow elimination
63
What is an adverse effect of vincristine
Neurotoxicity- interaction with axonal microtubules
64
What is an adverse effect of paclitaxel
Histamine release
65
Which is more myelosuppressive: vinblastine or vincristine
Vinblastine
66
What is C-kit
Receptor tyrosine kinase that drives leukopoesis, induces cell cycle activation, protein synthesis
67
C-kit has greatest proliferative effects on __cells and therefore is a proto-oncogene in __
Mast cells, canine mast cell tumors
68
What is Toceranib indicated for
Mast cell tumors
69
What is the PD for toceranib
Competitive antagonist of ATP binding to the kinase domain of C-kit at G1 phase of cell cycle
70
What are some adverse effects of toceranib
GI, bone marrow suppression (anemia, neutropenia), changes in coat color, thromboembolic dz and inappropriate bleeding
71
What is L-asparginase used to tx
Lymphoma
72
What is the PD of L-asparaginase
Blocks conversion of aspartame to asparagine in G1 phase of cell cycle
73
You cant give L-asparaginase __because it can cause fatal anaphylaxis
IV
74
How is L-asparagine metabolized and eliminated
Hydrolyzed to amino acids and used for new protein synthesis
75
What are some adverse effects of L-as-arginine
Pruritus, urticaria, dyspnea, hypotension, vomiting, diarrhea, hepatoxicity, defective coagulation production, hyperglycemia
76
How does prednisone work
Induces apoptosis of most immune cell linages
77
What is the DOC for TCC
Piroxicam
78
What is the PD for piroxicam
Nonspecific cyclooxygenase inhibitor, induces tumor cell apoptosis by reducing angiogenesis
79
What are some adverse effects of piroxicam
GI ulcerative and renal papillary necrosis

Pharmacology II (36 decks)

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