PHARM_GICANCER Flashcards

1
Q

what are the 2 anticancer drugs used to treat carcinoid tumors?

A

IFN-alpha

octreotide

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2
Q

what are the 2 anticancer agents used to treat GIST tumors?

A

imatinib

sunitinib

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3
Q

all pts with gastric cancer should be tested for what mutation?

A

HER-2 for trastuzumab

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4
Q

how does octreotide work in the treatment of GI carcinoid tumors?

A

acts at somatostatin receptors to inhibit the secretion of serotonin & other GI-pancreatic peptides, which results in increased intestinal absorption of water & electrolytes, decreased gastric acid secretions, and increased intestinal transit time

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5
Q

which class of drugs used to treat carcinoid tumors inhibits disease progression and provides symptom relief in 75% of pts?

A

TNF-alpha inhibitors (may be have greater antitumor activity than somatostatin analogs)

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6
Q

why don’t conventional cytotoxic chemotherapeutic agents work in GIST tumors?

A

due to P-gp overexpression

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7
Q

which drug is used as 1st line treatment of unresectable metastatic or recurrent GIST?

A

imatinib

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8
Q

what is the main mutation in GIST tumors?

A

KIT-mutant

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9
Q

how is sunitinib used to treat GIST tumors?

A

given to pts with unresectable dz who progress on higher dose imatinib

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10
Q

80% of liver cancer worldwide are associated with what 2 kinds of infections?

A

HBV & HCV

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11
Q

explain how TACE is used in liver cancer

A

Trans-catheter arterial chemoembolization

  • doxorubicin is injected while hepatic arterial branch feeding tumor is occluded with an emboli agent
  • selective catheterization spares normal tissue & minimizes dispersion of drug away from tumor site
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12
Q

Bevacizumab MOA

A

inhibits binding of VEGF to its receptor, resulting in inhibition of tumor vascularization

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13
Q

capecitabine MOA

A

oral pro-drug metabolized to 5-FU

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14
Q

cetuximab MOA

A

rh/mMAb-EGFR

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15
Q

Cisplatin MOA

A

forms DNA intrastrand crosslinks & adducts

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16
Q

Docetaxel MOA

A

microtubule stabilizer inhibiting depolymerization

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17
Q

erlotinib MOA

A

EGFR-TKI

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18
Q

Fluorouracil MOA

A

pyrimidine antimetabolite that inhibits thymidylate synthase & interferes w/ RNA synthesis & function. Also has some effects on DNA

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19
Q

Gemcitabine MOA

A

DNA polymerase inhibitor via incorporation of triphosphate form during DNA synthesis

20
Q

imatinib MOA

A

oral TKI as adjuvant treatment following complete resection of Kit (CD117) positive GIST

21
Q

IFN-alpha MOA

A

enzyme activation following cell surface receptor binding and tyrosine kinase activation

22
Q

Mitomycin MOA

A

mono or bifunctional alkylating agent

23
Q

octreotide MOA

A

somatostatin analog; reduces duodenal bicarbonate, amylase, reduces gastric acidity, inhibits gallbladder contractility & bile secretions, inhibits meal-induced increases in SMA & portal venous blood flow

24
Q

Sorafenib MOA

A

oral multi-kinase inhibitor targeting serine/threonine & receptor tyrosine kinases in both tumor & vasculature.

25
Q

Sunitinib MOA

A

inhibits >80 receptor tyrosine kinases including PDGFR, VEGFR, KIT, FLT3, CSR-1R, RET

26
Q

Trastuzumab MOA

A

HER-2/neu ab; HER2 is downregulated, cyclin-dependent kinase inhibitor p27 accumulates, & cell cycle arrest occurs. Also inhibits the constitutive HER2 cleavage/shedding mediated by metalloproteases, which may correlate with the clinical activity

27
Q

AEs of bevacizumab

A
Bleeding
GI perforation
wound dehiscence
HTN
hypersensitivity
28
Q

capecitabine AEs

A
Dihydropyrimidine DH deficiency (familial pyrimidinemia) prevents metabolic activation.
Contraindicated in renal dysfunction
Adverse CV events
Neurologic & hematologic toxicities
Interacts with coumarin
29
Q

AEs of cetuximab

A

cardiac arrest, respiratory arrest, and/or sudden death

  • infusion rxns
  • acneiform rash common (76-88%)
30
Q

Cisplatin AEs

A

dose limiting nephrotoxicity
bone marrow suppression
hearing impairment (ototoxicity)
Platinum hypersensitivity

31
Q

Docetaxel AEs

A

increased treatment realted mortality in NSCLC
Edema
Contraindicated in hepatic dz
neutropenia (dose-limiting tox.)

32
Q

what is the dose-limiting toxicity of docetaxel?

A

neutropenia

33
Q

AEs of erlotinib

A
GI toxicity (N/V, diarrhea)
prolonged bleeding
elevated LFTs
ocular toxicities
rarely ILD
34
Q

what are the AEs of fluorouracil?

A

Severe hematological tox. including BM suppression
dihydropyrimidine dehydrogenase deficiency (familial pyrimidinemia) lead to enhanced neurotoxicity; enzyme necessary for degrading fluorouracil to an inactive compound

35
Q

AEs of gemcitabine

A
BM suppression
infection
peripheral neuropathy
arthralgia
drowsiness
fatigue
N/V, diarrhea
anorexia common (resolves in 2-3 days)
36
Q

AEs of imatinib

A

GI toxicities common (N/V/C)
CHF
neurologic tox.
fluid retention & edema

37
Q

what are the AEs of IFN-alpha?

A

Neuropsychiatric events including aggression, depression and suicide
Flu-like symptoms: fatigue fever, alaise, myalgia, arthralgia, chills, headache, weight loss

38
Q

what are the AEs of irinotecan?

A
BM suppresssion
Diarrhea
asthenia
fever
pain
weight loss
39
Q

which drug may used in place of 5-FU to treat colorectal cancer?

A

capecitabine

40
Q

which 2 targeted agents appear to improve outcomes in colorectal cancer, except in pts with KRAS mutations?

A

bevacizumab

cetuximab

41
Q

what drug class is the 2nd line therapy for esophageal cancer?

A

taxanes

42
Q

what are the AEs of mitomycin?

A

BM suppression
Thrombocytopenia
leukopenia
Hemolytic-Uremic Syndrome

43
Q

what are the AEs of octreotide?

A

dose related diarrhea

44
Q

what do you have to monitor with octreotide therapy?

A

serum glucose; b/c it inhibits insulin & glucagon

45
Q

which TKI causes QT prolongation, thrombocytopenia and bleeding?

A

sunitinib

46
Q

what are the AEs of sunitinib?

A

thrombocytopenia & bleeding
QT prolongation
sometimes fatal GI complications including GI perfs have occured rarely in pts with intraabdominal malignancies

47
Q

what are the AEs of Trastuzumab?

A

LVEF dysfunction & cardiomyopathy
Severe infusion-related rxns including anaphylaxis, angioedema, & pulmonary toxicity; pulm. tox worse in pts w/ intrinsic lung dz (COPD, asthma, Respiratory insufficiency)