HY Pharm Flashcards
unfractionated heparin
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
fondaparinux
pure Xa inhibitor, but mediates effect thru ATIII
no HIT risk
DTIs
lepirudin
argatroban
dabigatran
inactivate thrombin in an ATIII-independent fashion
no HIT risk
Rivaroxaban
direct Xa inhibitor
renal clearance
lepirudin
DTI
argatroban
DTI
dabigatran
DTI
clopidogrel
anti-platelet
irreversibly inhibits P2Y12 receptor of ADP
slow onset
prasurgel
rapid onset
anti-platelet
abciximab
GPIIB/IIIa antagonist
inhibits platelet aggregation via binding site of fibrinogen between platelets
Desmopressin acetate (DDAVP)
pro-coagulant
promotes release of stored vWf from vascular endothelium
aminocaproic acid
anti-fibrinolytic
inhibits fibrinogen
odansetron
5HT antagonist
anti-emetic
aprepitant
NK-1 antagonist
blocks substance P at NK1 receptor centrally and peripherally
prochlorperazine
DA antagonist
metoclopramide
DA antagonist
nitrogen mustards
cyclophosphamide
ifosfamide
chlorambucil
melphalan
chorambucil
nitrogen mustard
AML
NHL
CLL
melphalan
nitrogen mustard
multiple myeloma
primary myelofobrosis
AML
triazenes
dacarbazine
dacarbazine
triazene
ABDC (HL)
polyglutamination
step that allows methotrexate to stay in cell for longer time
hydroxyurea
anti-metabolite
inhibits ribonucleotide reductase
dec wbc and platelet count
use: leukostasis in acute leukemia
antimetabolites
5FU
methotrexate
hydroxyurea
pyrimidine analogs
cytarabine (Ara-C)
Gemcitabine
cytarabine
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
Gemcitabine
pyrimidine analog
intracellular activation by deoxycitidine kinase
inhibits DNAP, ribonculeotide reductase
fludarabine
purine analog
interferes w/ DNA synthesis
use: CLL
AE: immune damage to rbc –> hemolytic anemia
anthracyclines
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)
bleomycin
binds to DNA and oxygen
free radical form –> single /ds breaks
- cell cycle specific at G2
use: Hodgkins
AE: pulm fibrosis
plant alkaloids
vinca alkaloids
tacanes
camptothecins
vincristine
plant alkaloid, m-phase, disrupts MT formation
NHL/ALL
neuropathies (paresthesias, dec autonomic fxn, constipation)
vinblastin
plant alkaloid, m-phase, disrupts MT formation
use: Hodgkins
BM suppression (*neutropenia)
vinorelbine
plant alkaloid, m-phase, disrupts MT formation
use: NSCLC, breast
BM suppression
taxanes
paclitaxel
docetaxel
enhance MT polymerization
use: breast/lung/ovarian
myelosuppresion - neutropenia
thrombocytopenia
hand-foot syndrome
camptothecins
irinotecan
inhibit topo I (can’t relax/nick ssRNA to replicate DNA, transcribe RNA etc)
AE: diarrhea! (atropine for acute, loperamide for delayed)
dexamethasone
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
prednisone
glucocorticoid
danazol
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
flutamide
anti-androgen
binds androgen receptor and inhibits uptake binding in nucleus
use: prostate cancer
AE: hot flashes, dec libido, gynecomastia, transient LFT abnormalities
bicalutamide
anti-androgen
binds androgen receptor and inhibits uptake binding in nucleus
use: prostate cancer
AE: hot flashes, dec libido, gynecomastia, transient LFT abnormalities
tamoxifen
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
raloxifine
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
anastrozole
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
letrozole
selective, reversible aromatase inhibitor
use: post-menopausal women w/ breast cancer
AE: arthralgia, musculoskeletal pain, hot flashes, LFT elevations
exemestane
IRreversible aromatase inhibitor
use: post-menopausal women w/ breast cancer
AE: hot flashes, fatigue, HA
leuprolide
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
goserelin
LH-RH agonist
use: breast/prostate
trastuzumab
anti-HER2
breast cancer
AE: infusion rxn generalized pain/asthenia/HA myelosuppression cardiotox (unique to this MoAb)
bevacizumab
anti-VEGF
colorectal/lung/breast/renal cell/brain
AE: BLACK BOX--> impaired wound healing, GI perforation, hemorrhage HTN thrombotic events bleeding episodes
rituximab
anti-CD20
NHL
AE: immunosuppressive infusion rxn tumor lysis (hyperkalemia, hyperphosphatemia, hypOcalcemia, inc in uric acid) skin rxn
cetuximab
anti-EGFR
colorectal/H,N/lung
AE: infusion rxn acneiform rash asthenia N/V hepatotoxicity
ecluzimab
anti-complement C5
Imatinib
BCR-ABL inhibitor
CML
AE: edema, fluid retention
cytopenia
elevated LFTs
cardiotoxicity
erlotinib
EGFR inhibitor
lung cancer
AE: acneiform rash
diarrhea
rash
ILD
thalidomide
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
lenalidomide
imid, unkown mech (moreso immunomodulatory)
use: multiple myeloma
AE:
TERATOGEN
cytopenia
thrombotic events
azacytidine
hypOmethylation agent (re-expression of epigenetically silenced genes)
use: MDS
AE: myelosuppression
N/V
diarrhea
decitabine
hypOmethylation agent (re-expression of epigenetically silenced genes)
use: MDS
AE: myelosuppression
N/V
diarrhea
bortezomib
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
Idarucizumab
DTI reversal agent
Andexanet-alpha
direct factor Xa inhibitor reversal agent
interferons
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
interleukins
use: RCC, malignant melanoma
AE: CV effects CNS GI Hematologic renal pulm
Romiplostim
Thrombopoietin mimetics
use: stimulating the production of platelets in patients with ITP, an AI disease where platelets and megakaryocytes are destroyed by auto-antibodies
Eltrombopag
Thrombopoietin mimetics
use: stimulating the production of platelets in patients with ITP, an AI disease where platelets and megakaryocytes are destroyed by auto-antibodies
Erythropoietin stimulating agents (ESAs)
epoetin alfa
darbepoetin alfa
indicated for pt receiving chemo
AE: hypertension, arthralgias, and rash
epoetin alfa
Erythropoietin stimulating agent
darbepoetin alfa
Erythropoietin stimulating agent
granulocyte colony-stimulating factor (G-CSF)
filgrastim
pegfilgrastim
filgrastim
granulocyte colony-stimulating factor (G-CSF)
pegfilgrastim
granulocyte colony-stimulating factor (G-CSF)
leucovorin effect on MTX
reversal
leucovorin effect on 5FU
synergistic (enhances cytotoxic effects)
mesna
neutralizes bladder-toxic metabolite prod by ifosfamide and cyclophisohamide
dexrazoxane
protects against cardiotoxicity during arthacyclines
give w/I 30 min!!!!
atropine
tx cholinergic acute diarrhea seen w/ irinotecan (camptothecin, topo I inhibitor)
enoxaparin
LMWH
dalteparin
LMWH
protamine sulfate
reverses UFH, LMWH
which heparin is not reversed by protamine sulfate?
Fondaparinux
diphenhydramine
tx of
- DA antagonist AE
- Erlotinib AE (acneiform rash pruitus)
Rasburicase
tx of tumor lysis syndrome
catalyzes the oxidation of uric acid to the more soluble allantoin
allopurinol
tx of tumor lysis syndrome
prevents the accumulation of uric acid by blocking the metabolism of hypoxanthine and xanthine to uric acid
