Pharm Flashcards

1
Q

Ondansetron (zofran)

A

Anti-emetic - acute

MOA: bind serotonin receptors in GI tract

Tox: Headache, hiccups, QT long, constipation

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2
Q

Aprepitant (Emend)

A

Anti-emetic - delayed

MOA: NK1 receptor antagonist (central and peripheral action)

Tox: drug interaction, hiccups, fatigue

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3
Q

Prochlorperazine (compazine)

A

Anti-emetic - delayed

MOA: bind dopamine D1/D2 receptors in chemoreceptor trigger zone

Tox: extrapyramidal side effects, sedation

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4
Q

Dexamethasone (Decadron)

A

corticosteroid used for anti-emetic properties

MOA: unknown

Tox: glucose intolerance, insomnia, agitation

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5
Q

Lorazepam (Ativan)

A

benzo used for anit-emetic properties

MOA: limbic, thalamic and hypothalamic areas via GABA

Tox: sedation, retrograde amnesia

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6
Q

Metoclorpramide (Reglan)

A

Anti-emetic

MOA: bind dopamine D1/D2 receptors in chemoreceptor trigger zone

Tox: extrapyramidal side effects, sedation

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7
Q

Epoetin alfa

A

short acting RBC growth factor
- must have adequate iron stores

Tox: hypertension, rash, arthralgias

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8
Q

Darbepoetin

A

long acting RBC growth factor

- must have adequate iron stores

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9
Q

Filgrastim

A

G-CSF - myeloid growth factor for neutropenia

Tox: fever (cytokines), bone pain (marrow elements), increase in uric acid, LDH, alk phos, rash

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10
Q

Pegfilgrastim

A

G-CSF - myeloid growth factor for neutropenia

  • also has PEG to double weight (decreases clearance)

Tox: fever (cytokines), bone pain (marrow elements), increase in uric acid, LDH, alk phos, rash

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11
Q

Alkylating agents toxicity

A
  • Bone marrow suppression
  • nausea, vomiting diarrhea, anorexia
  • sterility
  • amenorrhea
  • 2nd malignancy
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12
Q

MOA of platinum compounds

A

binds to DNA, RNA and produces covalent crosslinks

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13
Q

resistance mechanisms

A
  • increase glutathione-S-transferase
  • augmented DNA repair
  • altered cellular transport
  • altered DNA repair mechanism
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14
Q

Cisplatin

A

Platinum alkylating agent

  • highly emetogenic (use zofran and dexamethasone)
  • nephrotoxic
  • neurotoxic
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15
Q

Cisplatin nephrotoxicity

A

inactivation of renal brush border (rf = high plasma levels, kidney damage, hypoalbumin, female, other drugs)

  • acute - decrease electrolyte, increase BUN
  • chronic - reduced GFR, normal creatinine
  • anemia

Prevention - hydration, hypertonic saline, mannitol (osmotic diuretic), infusions

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16
Q

cisplatin neurotoxicity

A
  • axonal degeneration
  • peripheral neuropathy (stocking glove, cumulative doses)
  • auditory impairment
  • visual disturbances
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17
Q

oxaliplatin

A

Platinum alkylating agent

  • sensory neuropathy in cold
  • infusion reaction
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18
Q

carboplatin

A

Platinum alkylating agent

  • hypersensitivity
  • nausea vomiting
  • neurotoxicity
  • taxane?
  • no nephrotoxicity
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19
Q

cyclophosphamide

A

Nitrogen mustard alkylator

MOA: binds to nucleophiles, DNA crosslinking, inactivation of template

Extra: removed by dialysis, is a prodrug activiated in lived

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20
Q

cyclophosphamide toxicity

A
  • N/V
  • myelosuppressive
  • cardionecrosis
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21
Q

ifosfamide

A

nitrogen mustard alkylator

  • requires hepatic P450 for activation
  • produces acrolein
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22
Q

acrolein

A

metabolite of cyclophosphamide and ifosfamide

urotoxic

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23
Q

ifosfamide toxicity

A

neurotoxicity
hemorrhagic cystitis
neutropenia
nephrotoxicity - ATN

treated with methylene blue

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24
Q

mensa

A

binds acrolein in the bladder, requires multiple doses

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25
Q

prednisone

A

glucocorticoid

  • immunsuppressive effects
  • lympholytic
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26
Q

flutamide

A

anti androgen receptor

Tox: hot flashes, gynecomastia and breast tenderness

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27
Q

bicalutamide

A

anti androgen receptor

Tox: hot flashes, gynecomastia and breast tenderness

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28
Q

tamoxifen

A

anti estrogen binder, cell cycle specific

stimulates TGF-beta which inhibits TGF alpha and IGF-1 leading to decreased proliferation

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29
Q

raloxifene

A

anti estrogen binder, cell cycle specific

stimulates TGF-beta which inhibits TGF alpha and IGF-1 leading to decreased proliferation

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30
Q

letrozole

A

aromatase inhibitor - blocks conversion of androgen to estrogen, no effects of
cotricosteroid

Tox: arthralgias, ms pain, hot flashes, LFT

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31
Q

anastrozole

A

aromatase inhibitor - blocks conversion of androgen to estrogen, no effects of corticosteriod

Tox: astheia, hot flashes, peripheral edema, arthralgias

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32
Q

exemestane

A

aromatase inhibitor - blocks conversion of androgen to estrogen, no effects of corticosteriod

Tox: hot flashes, fatigue, headache

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33
Q

leuprolide

A

LH-RH agonist - suppression of gonadotropin, results in LH/FSH decrease

Usually has short term disease flare due to short term surge

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34
Q

goserelin

A

LH-RH agonist - suppression of gonadotropin, results in LH/FSH decrease

Usually has short term disease flare due to short term surge

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35
Q

methotrexate

A

binds reversibly to DHF reductase, S phase specific - leads to no purine synthesis

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36
Q

methotrexate pharmokinetics

A
  • binds to albumin = drug interactions
  • can accumulate in effusions
  • high doses can cross to CNS
37
Q

most important type of methotrexate metabolism

A

polyglutamation by enzyme FPGS

38
Q

leucovorin

A

stable form of reduced folate, used for rescue of healthy cells

timing is very important should be continued until MTX is less than .05uM

39
Q

methotrexate toxicity

A
  • renal toxicity (need to hydrate/alkalyze urine)
  • GI toxicity
  • effusions

Rare

  • hepatotoxicity
  • derm
  • myelosuppression
  • others
40
Q

methotrexate drug interactions

A
  • albumin binding
  • nephrotoxic drugs
    • can be helped with L-asparaginase
41
Q

cytarabine

A

Chain elongation terminator

only available as an infusion, can cross BBB, can distribute into tears

42
Q

cytarabine toxicity

A

normal

  • myelosuppression
  • flu like
  • mucositis
  • hand and foot

high

  • cerebellar tox
  • ocular tox - tearing
  • pulmonary edema
43
Q

5-Fluorouracil

A

false pyrimidine that inhibits formation of thymidine, effects augmented by leucovorin

44
Q

5-Fluorouracil pharmacokinetis

A

metabolized by DPD (many polymorphisms)

can be used in pts with hepatics and renal dysfunction

45
Q

5-Fluorouracil toxicity

A
  • myelosuppresion
  • mucositis/diarrhea
  • hand/foot
  • neurotox
  • chest pain, EKG
  • photosensitivity
46
Q

gemcitabine

A

similar to cytarabine, can incorporate in RNA, metabolized by cytidine deaminase (in urine)

47
Q

gemcitabine tox

A
  • myelosuppression
  • flu
  • flushing/headache
48
Q

gemcitabine interactions

A

radiosensitizer, enhances cytotoxicity of cisplatin

49
Q

anthracyclines MOA

A

passive diffusion, nucleated cells, intercalate DNA, Topo 2 inhibitor, form reactive compounds, oxygen radicals, uses iron 3+, important in cardiotox

50
Q

anthracyclines Tox

A
  • myelosuppression
  • alopecia
  • N/V
  • extravasation
  • *cardiotoxicity acute and chronic (EKG changes vs LVEF chagnes)
51
Q

dexrazoxane

A

chelating agent used to prevent cardiotoxicity in anthracycline use, EDTA analog, binds to iron

52
Q

doxorubicin

A

anthracyclines

53
Q

daunorubicin

A

anthracyclines

54
Q

liposomal anthracycline

A

made to reduce cardiotoxicity, slows release of the drug

55
Q

irinotecan

A

topo 1 inhibitor, given by IV

56
Q

irinotecan side effects

A

neutropenia, thrombocytopenia, eosinophilia

  • diarrhea (early cholinergic - late watery diarrhea)
  • N/V
  • rare pneumonitis
57
Q

irinotecan resistance

A

p-glycoprotein - reduced drug accumulation

  • altered intracellular drug distribution
  • variability in drug metabolism
  • differences in Topo 1 expression/mutation
58
Q

vinca alkaloids MOA

A

disturb microtuble formation, prevent formation of mitotic spindle

59
Q

vinca alkaloids tox

A

vincristine - neurotoxicity (peripheral neuropathy)

  • decrease autonomic
  • NOT bone marrow

vinblastine - myelosuppression

60
Q

vinblastine

A

vinca alkaloid - bone marrow problems

61
Q

vincristine

A

vinca alkaloid - neurotoxicity problems

vesicant

62
Q

vinorelbine

A

vinca alkaloid - same toxicity as other vinca alkaloid

63
Q

paclitaxel

A

M phase - enhances microtubule polymerization
- resistance in MDR, alterations in tubules

tox: myelosuppression, meuropathy, infusion reaction

64
Q

docetaxel

A

M phase - enhances microtubule polymerization
- resistance in MDR, alterations in tubules

tox: myelosuppression, meuropathy, infusion reaction

65
Q

rituximab

A

anti-CD20, used in non-hodgkin lymphoma and RA

66
Q

rituximab

A

immunosuppressive, infusion related, tumor lysis, HAMA/HACA

67
Q

cetuximab

A

binds to EGFR

tox: infusion related, rash, asthenia, N/V, hepato

68
Q

trastuzumab

A

anti HER2/neu monoclonal

Tox: infusion related, pain, myelosuppresion, cardiotox`

69
Q

bevacizumab

A

anti VEGF preventing angiogenesis

Tox: imparied wound healing, hemorrhage, hypertension, trombotic events, bleeding

70
Q

ecluzimab

A

anti-complement (C5) used to treat PNH

71
Q

imatinib

A

small molecule inhibitor of BRC-ABL tyrosine kinase

Tox: edema, cytopenias, LFT, cardiotoxicity

72
Q

erlotinib

A

EGFR inhibitor

73
Q

MOA of imids

A

antiangiogensis

  • basic fibroblast growth factor and VEGF
  • immunomodulatory
  • induces apoptosis
74
Q

drugs that cause delayed nausea and vomiting

A

Cyclophosphamide, cisplatinum, and doxorubicin

75
Q

unfractionated hepartin

A

requires AT-III, augments its, neutralizes thrombin, 10, 9 and 11a

76
Q

argatroban

A

direct thrombin inhibitors used in HIT

77
Q

enoxaparin

A

LMWH inhibits factor Xa more than 2 (thrombin) - leads to less bleeding

78
Q

dalteparin

A

LMWH

79
Q

Fondaparinux

A

synthetic low molecular weight heparin

80
Q

protamine

A

used to reverse heparin, cant be used with fondazparinux

81
Q

Idarucizamab

A

reversal agent of direct thrombin inhibitors

82
Q

Lepirudin

A

direct thrombin inhibitor, no AT3 necessary

83
Q

Dabigatran

A

direct thrombin inhibitor - no ATIII necessary

84
Q

Rivaroxaban

A

direct factor Xa inhibitor

85
Q

Clopidogrel

A

ADP receptor antagonist

86
Q

Prasugrel

A

ADP receptor antagonist

87
Q

abciximab

A

GPIIb/IIIa blockers – IV

88
Q

tetratogenic antithromin med

A

warfarin