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Cancer Chemotherapy Flashcards

15.21 (73 cards)

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1
Q

Cisplatin; Carboplatin - Tx

A

Chemo for advanced metastatic bladder cancer (use MVAC)

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2
Q

Cisplatin; Carboplatin - MOA

A

Displacement of Cl by water activates –> crosslinks DNA by binding guanines to prevent replication; drug-DNA complex attracts HMG-1 (high mobility group-1) repair proteins which become irreversibly bound –> prevents effective repair and leads to apoptosis

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3
Q

Does activation occur more slowly in cisplatin or carboplatin?

A

Carboplatin

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4
Q

Cisplatin; Carboplatin - MOR (2)

A

1) . Increased nucleotide excision repair protein;

2) . loss of function of mismatch repair (HMG-1)

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5
Q

Cisplatin; Carboplatin - Tox and how to minimize them (4)

A
  1. Nephrotoxicity (minimized w/ hydration/saline diuresis)
  2. Ototoxicity
  3. Marked nausea/vomiting (given w/ anti-emetic)
  4. Myelosuppression (Carboplatin only)
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6
Q

What is MVAC combo?

A

Methotrexate, vinblastine, doxorubicin, cisplatin

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7
Q

Which is generally less toxic: carboplatin or cisplatin?

A

Carboplatin

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8
Q

Which is used for pts w/renal dysfunction: carboplatin or cisplatin? (+1 more drug)

A

Carboplatin in combo w/paclitaxel

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9
Q

What is used w/cisplatin to minimize renal damage?

A

Hydration/saline diuresis

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10
Q

Doxorubicin; Mitoxantrone - Tx

A

Chemotherapy - Hormone Refractory/metastatic prostate cancer

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11
Q

Doxorubicin; Mitoxantrone - MOA

A

Intercalates DNA

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12
Q

Mitoxantrone - Class; used w/

A

Doxorubicin analog (sometimes used w/prednisone)

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13
Q

Doxorubicin; Mitoxantrone - SE (3)

A

Myelosuppression, cardiac toxicity, mucositis

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14
Q

Doxorubicin; Mitoxantrone - C/I

A

Cardiac disease

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15
Q

Which has less cardiotoxicity: doxorubicin or mitoxantrone?

A

Mitoxantrone

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16
Q

Paclitaxel; Docetaxel - Tx; used w/

A

Chemotherapy - Hormone refractory prostate cancer; docetaxel used in combo w/estramustine

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17
Q

Paclitaxel; Docetaxel - MOA

A

Antagonizes/blocks microtubule spindle disassembly by inhibiting mitosis by binding to beta-tubulin

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18
Q

Paclitaxel; Docetaxel - MOR (2)

A
  1. Multidrug resistance pumps

2. Beta-tubulin mutations

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19
Q

Paclitaxel; Docetaxel - Tox (3)

A

(1) Neutropenia, (2) peripheral neuropathy, (3) hypersensitivity (can use w/ dexamethasone)

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20
Q

Flutamide, Bicalutamide, Nilutamide - Tx

A

Chemotherapy; hormonal tx of prostate cancer

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21
Q

Flutamide, Bicalutamide, Nilutamide - Class

A

Nonsteroidal Androgen Receptor Antagonists

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22
Q

Flutamide, Bicalutamide, Nilutamide - MOA

A

Inhibit ligand binding of receptor and translocation of the androgen receptor-ligand complex to the nucleus

***Rarely used alone; used in combo w/ GnRH agonist during first few weeks of treatment to prevent excess androgen production

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23
Q

Flutamide, Bicalutamide, Nilutamide - SE (2)

A
  1. Gynecomastia

2. Mild hepatic toxicity

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24
Q

Which is more potent of the nonsteroidal androgen receptor antagonists?

A

Bicalutamide/Nilutamide –> orally active, more potent w/ fewer side effects compared to Flutamide

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25
Cyproterone - Class
Steroidal androgen receptor antagonist
26
Cyproterone - Tx
Chemo - prostate cancer
27
Cyproterone - MOA
Steroidal androgen receptor antagonist/partial agonist
28
Cyproterone - Used w/
Rarely used alone Used in combo w/ GnRH agonist (Leuprolide, Goserelin) during first few weeks of treatment to prevent excess androgen production
29
Leuprolide, Goserelin - Tx
Chemo- prostate cancer
30
Leuprolide, Goserelin - Class and MOA
GnRH agonist --> 1st 2-4 wks causes agonism at receptor to exacerbate symptoms via promotion of testosterone production=> eventually downregulate GnRH receptors to decrease LH production and thus androgen production => pharmacological castration ; Altered amino acid sequence-> less degradation and greater affinity for GnRH receptor compared to GnRH
31
Leuprolide, Goserelin - SE (5)
Headache, lightheadedness, nausea, injection site reactions; hypogonadism (pharmacological castration)
32
Degarelix - Tx
Hormonal tx of prostate cancer
33
Degarelix - Class/MOA
GnRH antagonist
34
Advantage of Degarelix
Avoids flare phenomenon of GnRH agonists and is not associated w/systemic allergic rxns
35
Abiraterone - Class
Irreversible inhibitor of 17-hydroxylase and C-17,20-lyase CYP17 activity that blocks testosterone biosynthesis (so inhibitor of steroidogenesis)
36
Abiraterone used w/
Glucocorticoid prednisone b/c abiraterone increases ACTH levels, resulting in mineralocorticoid excess
37
Which has greater potency: abiraterone or ketoconazole?
Abiraterone
38
Abiraterone - Tx
Castration-resistant prostate cancer (as secondary hormone therapy)
39
Finasteride - Tx
Hormonal tx- benign prostatic hypertrophy (BPH) (**as used for male pattern baldness**)
40
Finasteride - MOA
Inhibits 5a-reductase-> prevents conversion of testosterone to dihydrotestosterone
41
Finasteride - SE (2)
Impotence, gynecomastia
42
Ketoconazole - Tx
Chemo- prostate cancer (2nd hormone therapy to reduce adrenal androgen synthesis in castration-resistant prostate cancer)
43
Ketoconazole - MOA
Decreases CYP17 (17-hydroxylase) production and inhibits sex steroid synthesis (by both testicular and adrenal steroidogenesis)
44
Ketoconazole - SE
Diarrhea and hepatic enzyme elevations
45
Thiotepa - Tx
Chemo- bladder cancer
46
Thiotepa - MOA
Intravesicular agent; Activated by CytP450 to an alkylator --> crosslinks DNA;
47
Thiotepa - SE
Mild myelosuppression due to some systemic absorption
48
Mitomycin - Tx
Chemo- bladder cancer
49
Mitomycin - MOA
Intravesicular agent Dual alkylator-> crosslinks DNA @ G and A=> prevents DNA synthesis and repair attempts lead to strand breaks *Requires activation for alkylation*
50
Mitomycin - MOR (2)
Decreased activation, efflux pump
51
Mitomycin - SE (2)
Myelosuppression, nephrotoxicity
52
Bacillus Calmette-Guerin - Tx
Chemo- bladder cancer
53
Bacillus Calmette-Guerin - MOA
Intravesicular agent (given intravesicularly) Live, attenuated Mycobacterium bovis --> induces granulomatous rxn in bladder wall
54
Bacillus Calmette-Guerin - SE (6)
Hypersensitivity, shock, chills, fever, malaise, immune complex disease
55
Interleukin-2 (IL-2) - Tx
Chemo - renal cell carcinoma and melanoma; used in cancers that are refractory to conventional treatment
56
Interleukin-2 (IL-2) - MOA
Stimulate proliferation and activation of lymphokine-activated killer (LAK) cells
57
Interleukin-2 (IL-2) - SE (12)
Hypotension, arrhythmia, peripheral edema, azotemia, increased liver enzymes, anemia, thrombocytopenia, nausea, vomiting, diarrhea, confusion, fever
58
Sunitinib, Sorafenib - Tx
Renal cell carcinoma
59
Sunitinib - MOA
Inhibitor of receptor tyrosine kinases (VEGF-R2, PDGF-R, others) to reduce proliferation and angiogenesis
60
Sorafenib - MOA
Oral inhibitor of VEGF-R1,2,3 tyrosine kinases within tumor cells to reduce proliferation and angiogenesis
61
Sunitinib, Sorafenib - SE (6)
bleeding, HTN, proteinuria, thromboemboli, intestinal perforation, myelosuppression
62
Bevacizumab (Avastatin) - Tx
Renal cell carcinoma
63
Bevacizumab (Avastatin) - MOA
Humanized monoclonal Ab against VEGF --> inhibits interaction with VEGF receptors (VEGF-Trap) => inhibits angiogenesis in tumors
64
Bevacizumab (Avastatin) - SE/Toxicity (7)
Severe HTN, proteinuria, CHF, hemorrhage, stroke, MI, gastric perforation
65
Pazopanib - Tx
Renal cell carcinoma
66
Pazopanib - MOA
Inhibits the tyrosine kinase activity of VEGFR-2; inhibitor of angiogenesis
67
Which 3 drugs inhibit tyrosine kinase activity of VEGFR-2?
Pazopanib, sorafenib and sunitinib
68
Temsirolimus (metabolized to sirolimus), Everolimus (Rapamycin) - MOA
Normally: mTOR forms the mTORC1 complex with a member of the FK506-binding protein family, FKBP12. Among other actions, mTORC1 phosphorylates S6 kinase and also relieves the inhibitory effect of 4EBP on initiation factor elf-4E, thereby promoting protein synthesis and metabolism. MOA: The antitumor actions of the Rapamycins result from their binding to FKBP12 and inhibition of mTORC1.
69
Temsirolimus (metabolized to sirolimus), Everolimus (Rapamycin) - Effects
Sirolimus, temsirolimus (metabolized to sirolimus) or everolimus (Rapamycins) have immunosuppressive effects, inhibit cell-cycle progression and angiogenesis, and promote apoptosis.
70
Temsirolimus (metabolized to sirolimus), Everolimus (Rapamycin) - Class/Tx
mTOR Inhibitors: Rapamycin Analogs | Post-transplant immunosuppression; renal cancer (including intermediate, advanced, and poor prognosis)
71
mTOR stands for?
Mammalian target of rapamycin, or mTOR, an effector PI3 kinase signaling
72
What is rapamycin?
Sirolimus; a fungal fermentation product that inhibits the proper functioning of a serine/threonine protein kinase in mammalian cells
73
Temsirolimus (metabolized to sirolimus), Everolimus (Rapamycin) - SE (8)
Mild maculopapular rash, mucositis, anemia, and fatigue, leukopenia or thrombocytopenia (reversed w/discontinuation of drug), hyperglycemia, and hypertriglyceridemia

Renal Pharmacology (17 decks)

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