HY Pharm Flashcards

1
Q

unfractionated heparin

A

low bioavailability
poor GI absorb, need SQ or IV admin
half life: 1/2 hr

MOA: induces conformational change in ATIII, augments neutralization of thrombin, Xa, IXa, XIa

impairs platelet fxn

AE: bleeding, HIT, osteoporosis (long-term use), transaminitis

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2
Q

fondaparinux

A

pure Xa inhibitor, but mediates effect thru ATIII

no HIT risk

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3
Q

DTIs

A

lepirudin
argatroban
dabigatran

inactivate thrombin in an ATIII-independent fashion

no HIT risk

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4
Q

Rivaroxaban

A

direct Xa inhibitor

renal clearance

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5
Q

lepirudin

A

DTI

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6
Q

argatroban

A

DTI

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7
Q

dabigatran

A

DTI

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8
Q

clopidogrel

A

anti-platelet

irreversibly inhibits P2Y12 receptor of ADP

slow onset

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9
Q

prasurgel

A

rapid onset

anti-platelet

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10
Q

abciximab

A

GPIIB/IIIa antagonist

inhibits platelet aggregation via binding site of fibrinogen between platelets

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11
Q

Desmopressin acetate (DDAVP)

A

pro-coagulant

promotes release of stored vWf from vascular endothelium

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12
Q

aminocaproic acid

A

anti-fibrinolytic

inhibits fibrinogen

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13
Q

odansetron

A

5HT antagonist

anti-emetic

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14
Q

aprepitant

A

NK-1 antagonist

blocks substance P at NK1 receptor centrally and peripherally

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15
Q

prochlorperazine

A

DA antagonist

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16
Q

metoclopramide

A

DA antagonist

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17
Q

nitrogen mustards

A

cyclophosphamide
ifosfamide
chlorambucil
melphalan

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18
Q

chorambucil

A

nitrogen mustard

AML
NHL
CLL

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19
Q

melphalan

A

nitrogen mustard

multiple myeloma
primary myelofobrosis
AML

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20
Q

triazenes

A

dacarbazine

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21
Q

dacarbazine

A

triazene

ABDC (HL)

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22
Q

polyglutamination

A

step that allows methotrexate to stay in cell for longer time

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23
Q

hydroxyurea

A

anti-metabolite
inhibits ribonucleotide reductase

dec wbc and platelet count

use: leukostasis in acute leukemia

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24
Q

antimetabolites

A

5FU
methotrexate
hydroxyurea

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25
Q

pyrimidine analogs

A

cytarabine (Ara-C)

Gemcitabine

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26
Q

cytarabine

A

pyrimidine analog

undergoes conversion by deoxycitidine kinase

incorporate into DNA, competitively inhibits DNAP

crosses BBB, intrathecal admin
-ocular toxicity/cerebellar ataxia

non-cardiogenic pulmonary edema

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27
Q

Gemcitabine

A

pyrimidine analog

intracellular activation by deoxycitidine kinase

inhibits DNAP, ribonculeotide reductase

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28
Q

fludarabine

A

purine analog

interferes w/ DNA synthesis

use: CLL

AE: immune damage to rbc –> hemolytic anemia

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29
Q

anthracyclines

A

doxorubicin
daunorubicin

diffuse into cell passively, intercalate between base pairs –> damage, breakage

also Topo II inhibition which disables strand repair

also undergo electron reductions that turn agents into ROS –> damage too lipid membranes, intracellular macromolecules, DNA

also release Fe –> more intercalation of DNA

myelosuppression
alopecia
N/V
urine color changes
vesicants (tissue damage if leaks out)
cardiotoxicity (acute: EKG changes, chronic: dec LVEF func)
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30
Q

bleomycin

A

binds to DNA and oxygen

free radical form –> single /ds breaks

  • cell cycle specific at G2
    use: Hodgkins

AE: pulm fibrosis

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31
Q

plant alkaloids

A

vinca alkaloids
tacanes
camptothecins

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32
Q

vincristine

A

plant alkaloid, m-phase, disrupts MT formation

NHL/ALL

neuropathies (paresthesias, dec autonomic fxn, constipation)

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33
Q

vinblastin

A

plant alkaloid, m-phase, disrupts MT formation

use: Hodgkins

BM suppression (*neutropenia)

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34
Q

vinorelbine

A

plant alkaloid, m-phase, disrupts MT formation

use: NSCLC, breast

BM suppression

35
Q

taxanes

A

paclitaxel
docetaxel

enhance MT polymerization

use: breast/lung/ovarian

myelosuppresion - neutropenia
thrombocytopenia
hand-foot syndrome

36
Q

camptothecins

A

irinotecan

inhibit topo I (can’t relax/nick ssRNA to replicate DNA, transcribe RNA etc)

AE: diarrhea! (atropine for acute, loperamide for delayed)

37
Q

dexamethasone

A

glucocorticoids

cytotoxic action, immunosuppressive effects by reducing activity and number of lymphocytic cells

AE: glucose intolerance, insomnia, agitation, jitteriness, appetite stimulation, weight gain, fluid retention

38
Q

prednisone

A

glucocorticoid

39
Q

danazol

A

androgen

suppresses pituitary output of FSH and LH

use: BM failure and myelodysplasia

AE: edema/flushing/HTN/hirsuitism/voice changes/inc in leukocytes/erythrocytes/platelers

40
Q

flutamide

A

anti-androgen

binds androgen receptor and inhibits uptake binding in nucleus

use: prostate cancer

AE: hot flashes, dec libido, gynecomastia, transient LFT abnormalities

41
Q

bicalutamide

A

anti-androgen

binds androgen receptor and inhibits uptake binding in nucleus

use: prostate cancer

AE: hot flashes, dec libido, gynecomastia, transient LFT abnormalities

42
Q

tamoxifen

A

anti-estrogen

competes w/ estrogen for binding to estrogen receptor

cell cycle specific –> blocks in mid-G1

also stimulate TGF-beta which then inhibits TGF-alpha and IGF-1 –> dec proliferation of cell

AE: menopausal, fluid retention, tumor flare, DVT, PE, endometrial hypERplasia

43
Q

raloxifine

A

anti-estrogen

competes w/ estrogen for binding to estrogen receptor

cell cycle specific –> blocks in mid-G1

also stimulate TGF-beta which then inhibits TGF-alpha and IGF-1 –> dec proliferation of cell

AE: menopausal, fluid retention, tumor flare, DVT, PE, endometrial hypERplasia

44
Q

anastrozole

A

aromatase inhibitor, blocks conversion of androgens to estrogens (via inhib P450)

use: post-menopausal women w/ breast cancer

AE: hot flashes, tumor flare, peripheral edema, asthenia

45
Q

letrozole

A

selective, reversible aromatase inhibitor

use: post-menopausal women w/ breast cancer

AE: arthralgia, musculoskeletal pain, hot flashes, LFT elevations

46
Q

exemestane

A

IRreversible aromatase inhibitor

use: post-menopausal women w/ breast cancer

AE: hot flashes, fatigue, HA

47
Q

leuprolide

A

LH-RH agonist

inhibit gonadotropin via neg feedback inhib of pituitary, ultimately –> dec prod of endogenous testosterone/estrogen

use: PRE-menopausal women w/ breast cancer, testicular cancer

AE: tumor flare (initial LH/FSH release)
peripheral edema
asthenia
hot flashes
gynecomastia
alterations in serum lipids
bone loss w/ long-term use
48
Q

goserelin

A

LH-RH agonist

use: breast/prostate

49
Q

trastuzumab

A

anti-HER2

breast cancer

AE:
infusion rxn
generalized pain/asthenia/HA
myelosuppression 
cardiotox (unique to this MoAb)
50
Q

bevacizumab

A

anti-VEGF

colorectal/lung/breast/renal cell/brain

AE:
BLACK BOX--> impaired wound healing, GI perforation, hemorrhage
HTN
thrombotic events
bleeding episodes
51
Q

rituximab

A

anti-CD20

NHL

AE: 
immunosuppressive
infusion rxn
tumor lysis
(hyperkalemia, hyperphosphatemia, hypOcalcemia, inc in uric acid)
skin rxn
52
Q

cetuximab

A

anti-EGFR

colorectal/H,N/lung

AE:
infusion rxn
acneiform rash
asthenia
N/V
hepatotoxicity
53
Q

ecluzimab

A

anti-complement C5

54
Q

Imatinib

A

BCR-ABL inhibitor

CML

AE: edema, fluid retention
cytopenia
elevated LFTs
cardiotoxicity

55
Q

erlotinib

A

EGFR inhibitor

lung cancer

AE: acneiform rash
diarrhea
rash
ILD

56
Q

thalidomide

A

imid, inhibit fb gfac and inhibit VEGF

also immunomodulatory, inhibit TNF-alpha … etc

use: multiple myeloma

AE: 
TERATOGEN
neurotoxicity (axonal damage)
sedation
depression
hypOthyroidism
CV asymptomatic bradycardia
peripheral edema
thrombosis
57
Q

lenalidomide

A

imid, unkown mech (moreso immunomodulatory)

use: multiple myeloma

AE:
TERATOGEN
cytopenia
thrombotic events

58
Q

azacytidine

A

hypOmethylation agent (re-expression of epigenetically silenced genes)

use: MDS

AE: myelosuppression
N/V
diarrhea

59
Q

decitabine

A

hypOmethylation agent (re-expression of epigenetically silenced genes)

use: MDS

AE: myelosuppression
N/V
diarrhea

60
Q

bortezomib

A

proteasome inhibitor

acts like a spoon in the proteosome disposal, blocking access by ubiquitinated proteins –> accumulation of cell cycle speciqc proteins, ultimately preventing cell cycle progression and leading to apoptosis

(also lead to accumulation of IkB which then inactivates NFkB, preventing growth of myeloma cells and prompting apoptosis)

use: MM, NHL

AE: fatigue/malaise
myelosuppression
peripheral neuropathy

61
Q

Idarucizumab

A

DTI reversal agent

62
Q

Andexanet-alpha

A

direct factor Xa inhibitor reversal agent

63
Q

interferons

A

immunomodulatory agents that bind to specifc cell receptors –> enhanced activity of immune effector cells, etc

use: AIDS Kaposi sarcoma, chronic leukemias, renal cell cancers, and malignant melanoma

AE: flu-like syndrome, can be severe and dose-limiting, fatigue, anorexia, liver infammation, and autoimmune disorders

64
Q

interleukins

A

use: RCC, malignant melanoma

AE: 
CV effects
CNS
GI
Hematologic
renal 
pulm
65
Q

Romiplostim

A

Thrombopoietin mimetics

use: stimulating the production of platelets in patients with ITP, an AI disease where platelets and megakaryocytes are destroyed by auto-antibodies

66
Q

Eltrombopag

A

Thrombopoietin mimetics

use: stimulating the production of platelets in patients with ITP, an AI disease where platelets and megakaryocytes are destroyed by auto-antibodies

67
Q

Erythropoietin stimulating agents (ESAs)

A

epoetin alfa
darbepoetin alfa

indicated for pt receiving chemo

AE: hypertension, arthralgias, and rash

68
Q

epoetin alfa

A

Erythropoietin stimulating agent

69
Q

darbepoetin alfa

A

Erythropoietin stimulating agent

70
Q

granulocyte colony-stimulating factor (G-CSF)

A

filgrastim

pegfilgrastim

71
Q

filgrastim

A

granulocyte colony-stimulating factor (G-CSF)

72
Q

pegfilgrastim

A

granulocyte colony-stimulating factor (G-CSF)

73
Q

leucovorin effect on MTX

A

reversal

74
Q

leucovorin effect on 5FU

A

synergistic (enhances cytotoxic effects)

75
Q

mesna

A

neutralizes bladder-toxic metabolite prod by ifosfamide and cyclophisohamide

76
Q

dexrazoxane

A

protects against cardiotoxicity during arthacyclines

give w/I 30 min!!!!

77
Q

atropine

A

tx cholinergic acute diarrhea seen w/ irinotecan (camptothecin, topo I inhibitor)

78
Q

enoxaparin

A

LMWH

79
Q

dalteparin

A

LMWH

80
Q

protamine sulfate

A

reverses UFH, LMWH

81
Q

which heparin is not reversed by protamine sulfate?

A

Fondaparinux

82
Q

diphenhydramine

A

tx of

  • DA antagonist AE
  • Erlotinib AE (acneiform rash pruitus)
83
Q

Rasburicase

A

tx of tumor lysis syndrome

catalyzes the oxidation of uric acid to the more soluble allantoin

84
Q

allopurinol

A

tx of tumor lysis syndrome

prevents the accumulation of uric acid by blocking the metabolism of hypoxanthine and xanthine to uric acid