Heparin - mech - clin use, follow what lab? - tox - reversal effects w/? - big SE = ?

cofactor for act'n of ATIII -> decr'd thrombin and FXa, short t 1/2 - immediate anticoag, can use during preg bc doesn't X placenta; follow PTT - bl'ing, HIT, osteoporosis, drug interactions - protamine sulfate (+ molec binds - hep) - HIT = IgG Abs to hep:PF4 (on plts) -> thrombosis and thrombocytopenia

Warfarin (Coumadin) - mech - metab'd by - clin use, follow what lab? - tox - reverse effects w/?

interferes w/ gamma-carboxyl of VitK-dep CFs (2, 7, 9, 10, PrC/S), long t 1/2 - P450 - chronic anticoag, not used in preg women bc can X placenta follow PT - bl'ing, teratogenic, skin/tissue necrosis (bc prC/S decr before others -> thrombosis), drug interactions - VitK, for rapid effect give FFP

Heparin vs. Warfarin: - size - route of administration - onset of action - duration of action - inhib's coag in vitro

- lg anionic acidic polymer vs. sm lipid-soluble molec - IV/SC vs. PO - rapid (s) vs. slow (need CFs to end t 1/2) - acute (hrs) vs. chronic (d's) - yes vs. no

Thrombolytics = - MoA - how do labs change? - clin use - tox - C/I'd in? - trt tox w/?

"-plase" Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA) - convert plasminogen to plasmin - incr'd PT/PTT, no plt ct change - early MI, early stroke, severe PE - bl'ing - active bl'ing, hx of head bl, recent surgery, severe HTN - aminocaproic acid (inhib's fibrinolysis)

ASA - mech - how do labs change? - clin use - tox - don't use in kids w/ viral infec, why? - overdose causes?

irreversibly inhib's plt COX-1/2 by covalent acetylation (lasts until new plts are made) - no change in PT/PTT, incr'd BT, decr'd TXA2 and PGEs - antipyretic, analgesic, anti-inflamm, anti-plt aggregation - gastric ulcers, tinnitus (CNVIII), chronic use can cause ARF, interstitial nephritis and upper GI bl'ing - risk of Reye's synd - resp alk and metab acidosis

ADP R inhib's = - mech - clin use - tox

Clopidogrel, ticlopidine, prasugrel, ticagrelor - block ADP Rs -> inhib plt aggregation bc no GpIIb/IIIa R available for fibrinogen to bind - ACS, coronary stenting, to decr chance of thrombotic stroke - neutropenia (ticlopidine)

PDE III inhib's = - mech - clin use - tox

cilostazol, dipyridamole - incr cAMP in plts -> inhib aggregation; vasodilators too - intermittent caudication, coronary vasodil, prevent stroke/TIA (w/ ASA), angina prophylaxis - N, HA, facial flushing, hypotension, ab pain

GP IIb/IIIa inhib's = - mech - made from - clin use - tox

Abciximab, eptifibatide, tirofiban - bind GP IIb/IIIa inhib on act'd plts, prevents aggregation - mAB Fab fragments - ACS, PCT coronary angioplasty - bl'ing, thrombocytopenia

Heme/Onc Flashcards by Hannah Shull

Heparin

mech
clin use, follow what lab?
tox
reversal effects w/?
big SE = ?

cofactor for act’n of ATIII -> decr’d thrombin and FXa, short t 1/2

immediate anticoag, can use during preg bc doesn’t X placenta; follow PTT
bl’ing, HIT, osteoporosis, drug interactions
protamine sulfate (+ molec binds - hep)
HIT = IgG Abs to hep:PF4 (on plts) -> thrombosis and thrombocytopenia

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Lepirudin, bialirudin =

- used when?

direct thrombin inhib’s, deriv’s of hirudin

- alt to heparin for anticoag w/ HIT pt’s

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Warfarin (Coumadin)

mech
metab’d by
clin use, follow what lab?
tox
reverse effects w/?

interferes w/ gamma-carboxyl of VitK-dep CFs (2, 7, 9, 10, PrC/S), long t 1/2

P450
chronic anticoag, not used in preg women bc can X placenta follow PT
bl’ing, teratogenic, skin/tissue necrosis (bc prC/S decr before others -> thrombosis), drug interactions
VitK, for rapid effect give FFP

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Heparin vs. Warfarin:

size
route of administration
onset of action
duration of action
inhib’s coag in vitro

lg anionic acidic polymer vs. sm lipid-soluble molec
IV/SC vs. PO
rapid (s) vs. slow (need CFs to end t 1/2)
acute (hrs) vs. chronic (d’s)
yes vs. no

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Thrombolytics =

MoA
how do labs change?
clin use
tox
C/I’d in?
trt tox w/?

“-plase” Alteplase (tPA), reteplase (rPA), tenecteplase (TNK-tPA)

convert plasminogen to plasmin
incr’d PT/PTT, no plt ct change
early MI, early stroke, severe PE
bl’ing
active bl’ing, hx of head bl, recent surgery, severe HTN
aminocaproic acid (inhib’s fibrinolysis)

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Aminocaproid acid =

inhib’s fibrinolysis; use for tPA tox

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Protamine sulfate =

trt heparin overdose

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ASA

mech
how do labs change?
clin use
tox
don’t use in kids w/ viral infec, why?
overdose causes?

irreversibly inhib’s plt COX-1/2 by covalent acetylation (lasts until new plts are made)

no change in PT/PTT, incr’d BT, decr’d TXA2 and PGEs
antipyretic, analgesic, anti-inflamm, anti-plt aggregation
gastric ulcers, tinnitus (CNVIII), chronic use can cause ARF, interstitial nephritis and upper GI bl’ing
risk of Reye’s synd
resp alk and metab acidosis

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ADP R inhib’s =

mech
clin use
tox

Clopidogrel, ticlopidine, prasugrel, ticagrelor

block ADP Rs -> inhib plt aggregation bc no GpIIb/IIIa R available for fibrinogen to bind
ACS, coronary stenting, to decr chance of thrombotic stroke
neutropenia (ticlopidine)

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Clopidogrel =

ADP R inhib

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Ticlopidine =

ADP R inhib

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Prasugrel =

ADP R inhib

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Ticagrelor =

ADP R inhib

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PDE III inhib’s =

mech
clin use
tox

cilostazol, dipyridamole

incr cAMP in plts -> inhib aggregation; vasodilators too
intermittent caudication, coronary vasodil, prevent stroke/TIA (w/ ASA), angina prophylaxis
N, HA, facial flushing, hypotension, ab pain

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Cilostazole =

PDE III inhib

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Dipyridamole =

PDE III inhib

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GP IIb/IIIa inhib’s =

mech
made from
clin use
tox

Abciximab, eptifibatide, tirofiban

bind GP IIb/IIIa inhib on act’d plts, prevents aggregation
mAB Fab fragments
ACS, PCT coronary angioplasty
bl’ing, thrombocytopenia

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Abciximab =

GP IIb/IIIa inhib

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Eptifibatide =

GP IIb/IIIa inhib

Tirofiban =

GP IIb/IIIa inhib

What stage of cell cycle do these ca drugs work at?

Antimetabolites
Bleomycin
Etoposide
Vinca alkaloids and taxols

S (DNA syn)
G2 (syn of mitosis things)
S and G2
M (mitosis)

MTX =

mech
clin use
tox
reverse effects w/

antimetab, works at S phase

folic acid analog, inhib’s dihydrofolate reductase -> decr’d dTMP and decr’d DNA and pr syn
leuk’s, lymph’s, chorioca, sarcomas; abortion, ectopic preg, RA, psoriasis
myelosupp’n, macrovesic fatty change in liver, mucositis, teratogenic
leucovorin (folinic acid)

5-FU =

mech
clin use
tox
reverse overdose w/

antimetab, works at S phase

pyrimidine analog, act’d to 5F-dUMP, covalently complexes w/ folic acid -> inhib’s thymidylate synthase -> decr’d dTMP and decr’d DNA/pr syn
colon ca, BCC (topical)
myelosupp’n, photosensitivity
thymidine

Cytarabine (arabinofuranosyl cytidine) =

- mech, clin use, tox

antimetab, works at S phase

pyrimidine analog, inhib’s DNAP
leuk’s, lymph’s
leukopenia, thrombocytopenia, megaloblastic anemia

Azathioprine, 6-MP, 6-TG = - mech, clin use, tox - act'd by?

antimetab's, work at S phase - purine (thiol) analogs -> decr'd de novo purine syn - leuk's - BM, GI, liver; metab'd by xanthine oxidase so incr'd tox w/ allopurinol - by HGPRT

Dactinomycin (actinomycin D) = | - mech, clin use, tox

antitumor abx - intercalates in DNA - Wilms' tumor, Ewing sarcoma, rhabdomyosarcoma (childhood tumors bc kids "act" out) - myelosupp'n

Doxorubicin (Adriamycin), daunorubicin = - mech, clin use, tox - prevent tox w/?

antitumor abx - makes FRs; intercalates in DNA, brks DNA and decr's its rep'n - solid tumors, leuk/lymph's - cardiotox (dilated cardio.), myelosupp'n, alopecia, toxic to tissues following extravasation - Dexrazoxane (Fe chelating agent), prevents cardiotox

Bleomycin = | - mech, clin use, tox

antitumor abx - induces FRs which brk DNA strands - testicular ca, HL - pulm fibrosis, skin changes, minimal myelosupp'n

Cyclophosphamide, ifosfamide = - mech, clin use, tox - prevent SE w/?

alkylating agents - covalently X-link DNA at G N-7, req bioact'n in liver - solid tumors, leuk/lymph's, some brain ca's - myelosupp'n, hemorrhagic cystitis - mesna = thiol gp of it binds toxic metab to partially prevent hemorrhagic cystitis

Nitrosoureas = - end in? + ? - mech, clin use, tox

alkylating agents - "mustine" (carmustine, lomustine, semustine) + streptozocin - need bioact'n, X BBB to CNS - brain tumors (glioblastoma multiforme) - CNS tox (dizzy, ataxia)

Busulfan = | - mech, clin use, tox

alkylating agent - alkylates DNA - CML, to ablate pt's BM before trplt - pulm fibrosis, hyperpigmentation

Vincristine, vinblastine = | - mech, clin use, tox

microtubule inhib's - alkaloids that bind tubulin in M and S phase to block polymerization of microtubules so no mitotic spindle (microtubules are the vines of your cells) - solid tumors, leuk's/lymph's - Vincristine has neurotox and paralytic ileus; VinBLASTine BLASTs BM (supp'n)

Paclitaxel, other taxols = | - mech, clin use, tox

microtubule inhib's - hyperstabilize polymerized microtubules in M phase so mitotic spindle can't brk dwn (can't enter anaphase) (It's taxing to stay polymerized) - ov/br ca's - myelosupp'n and hypersensitivity

Cisplatin, carboplatin - mech, clin use, tox - prevent tox w/?

X-link DNA - testic, bladder, ov and lung ca's - nephrotox and acoustic n. damage - no nephrotox w/ amifostine (FR scavenger) and Cl diuresis

Etoposide, teniposide | - mech, clin use, tox

inhib topoII -> incr'd DNA degradation in S and G2 phases - solid tumors, leuks/lymphs - myelosupp'n, GI irritation, alopecia

Hydroxyurea | - mech, clin use, tox

inhib's ribont reductase -> decr'd DNA syn (S phase sp) - melanoma, CML, SCA (incr HbF) - BM supp'n, GI upset

Prednisone, prednisolone | - mech, clin use, tox

may trigger apoptosis, may work on nondividing cells - ca chemotx; CLL, NHL, immunosupp't for autoimm dz's - Cushing-like sx, immunosupp'n, cataracts, acne, osteoporosis, hyperGlc/HTN, peptic ulcers, psychosis

Tamoxifen, raloxifene | - mech, clin use, tox

SERMs; R antag's in br and agonists in bone - br ca trtmt/prevention; prevent osteoporosis (Estrogen agonist at bone) - Tamoxifen is partial agonist in endometrium -> risk of endometrial ca, hot flashes; Raloxifene is endomet antag so no incr'd ca risk

Trastuzumab (Herceptin) | - mech, clin use, tox

mAb to HER-2 (c-erbB2), a TK; kills br ca cells that overexp HER-2 thr ADCC - HER-2(+) br ca - cardiotox

Imatinib (Gleevec) | - mech, clin use, tox

phil chr bcr-abl TK inhib - CML, GI stromal tumors - fluid retention

Rituximab | - mech, clin use, tox

mAb to CD20 (B cell neoplasms) - NHL, RA (w/ MTX) - none

Vemurafenib | - mech, clin use, tox

sm molec inhib of forms of B-raf kinase w/ V600E mutation - metastatic melanoma - none

Bevacizumab | - mech, clin use, tox

mAb to VEGF, inhib's angiogenesis - solid tumors - none

Enoxaparin = | - benefits of using it?

LMWH - acts more on F Xa than plts, better bioav and 2-4x longer t1/2, can be given SC w/o lab monitoring, not easily reversible

Dalteparin = | - benefits of using it?

LMWH - acts more on F Xa than plts, better bioav and 2-4x longer t1/2, can be given SC w/o lab monitoring, not easily reversible