Heme/Onc Flashcards

1
Q

Heparin

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

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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2
Q

Lepirudin, bialirudin =

- used when?

A

direct thrombin inhib’s, deriv’s of hirudin

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

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3
Q

Warfarin (Coumadin)

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

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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4
Q

Heparin vs. Warfarin:

  • size
  • route of administration
  • onset of action
  • duration of action
  • inhib’s coag in vitro
A
  • 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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5
Q

Thrombolytics =

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

“-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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6
Q

Aminocaproid acid =

A

inhib’s fibrinolysis; use for tPA tox

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7
Q

Protamine sulfate =

A

trt heparin overdose

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8
Q

ASA

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

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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9
Q

ADP R inhib’s =

  • mech
  • clin use
  • tox
A

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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10
Q

Clopidogrel =

A

ADP R inhib

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11
Q

Ticlopidine =

A

ADP R inhib

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12
Q

Prasugrel =

A

ADP R inhib

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13
Q

Ticagrelor =

A

ADP R inhib

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14
Q

PDE III inhib’s =

  • mech
  • clin use
  • tox
A

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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15
Q

Cilostazole =

A

PDE III inhib

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16
Q

Dipyridamole =

A

PDE III inhib

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17
Q

GP IIb/IIIa inhib’s =

  • mech
  • made from
  • clin use
  • tox
A

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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18
Q

Abciximab =

A

GP IIb/IIIa inhib

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19
Q

Eptifibatide =

A

GP IIb/IIIa inhib

20
Q

Tirofiban =

A

GP IIb/IIIa inhib

21
Q

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

  • Antimetabolites
  • Bleomycin
  • Etoposide
  • Vinca alkaloids and taxols
A
  • S (DNA syn)
  • G2 (syn of mitosis things)
  • S and G2
  • M (mitosis)
22
Q

MTX =

  • mech
  • clin use
  • tox
  • reverse effects w/
A

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)
23
Q

5-FU =

  • mech
  • clin use
  • tox
  • reverse overdose w/
A

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
24
Q

Cytarabine (arabinofuranosyl cytidine) =

- mech, clin use, tox

A

antimetab, works at S phase

  • pyrimidine analog, inhib’s DNAP
  • leuk’s, lymph’s
  • leukopenia, thrombocytopenia, megaloblastic anemia
25
Q

Azathioprine, 6-MP, 6-TG =

  • mech, clin use, tox
  • act’d by?
A

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
26
Q

Dactinomycin (actinomycin D) =

- mech, clin use, tox

A

antitumor abx

  • intercalates in DNA
  • Wilms’ tumor, Ewing sarcoma, rhabdomyosarcoma (childhood tumors bc kids “act” out)
  • myelosupp’n
27
Q

Doxorubicin (Adriamycin), daunorubicin =

  • mech, clin use, tox
  • prevent tox w/?
A

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
28
Q

Bleomycin =

- mech, clin use, tox

A

antitumor abx

  • induces FRs which brk DNA strands
  • testicular ca, HL
  • pulm fibrosis, skin changes, minimal myelosupp’n
29
Q

Cyclophosphamide, ifosfamide =

  • mech, clin use, tox
  • prevent SE w/?
A

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
30
Q

Nitrosoureas =

  • end in? + ?
  • mech, clin use, tox
A

alkylating agents

  • “mustine” (carmustine, lomustine, semustine) + streptozocin
  • need bioact’n, X BBB to CNS
  • brain tumors (glioblastoma multiforme)
  • CNS tox (dizzy, ataxia)
31
Q

Busulfan =

- mech, clin use, tox

A

alkylating agent

  • alkylates DNA
  • CML, to ablate pt’s BM before trplt
  • pulm fibrosis, hyperpigmentation
32
Q

Vincristine, vinblastine =

- mech, clin use, tox

A

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)
33
Q

Paclitaxel, other taxols =

- mech, clin use, tox

A

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
34
Q

Cisplatin, carboplatin

  • mech, clin use, tox
  • prevent tox w/?
A

X-link DNA

  • testic, bladder, ov and lung ca’s
  • nephrotox and acoustic n. damage
  • no nephrotox w/ amifostine (FR scavenger) and Cl diuresis
35
Q

Etoposide, teniposide

- mech, clin use, tox

A

inhib topoII -> incr’d DNA degradation in S and G2 phases

  • solid tumors, leuks/lymphs
  • myelosupp’n, GI irritation, alopecia
36
Q

Hydroxyurea

- mech, clin use, tox

A

inhib’s ribont reductase -> decr’d DNA syn (S phase sp)

  • melanoma, CML, SCA (incr HbF)
  • BM supp’n, GI upset
37
Q

Prednisone, prednisolone

- mech, clin use, tox

A

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
38
Q

Tamoxifen, raloxifene

- mech, clin use, tox

A

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
39
Q

Trastuzumab (Herceptin)

- mech, clin use, tox

A

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

  • HER-2(+) br ca
  • cardiotox
40
Q

Imatinib (Gleevec)

- mech, clin use, tox

A

phil chr bcr-abl TK inhib

  • CML, GI stromal tumors
  • fluid retention
41
Q

Rituximab

- mech, clin use, tox

A

mAb to CD20 (B cell neoplasms)

  • NHL, RA (w/ MTX)
  • none
42
Q

Vemurafenib

- mech, clin use, tox

A

sm molec inhib of forms of B-raf kinase w/ V600E mutation

  • metastatic melanoma
  • none
43
Q

Bevacizumab

- mech, clin use, tox

A

mAb to VEGF, inhib’s angiogenesis

  • solid tumors
  • none
44
Q

Enoxaparin =

- benefits of using it?

A

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

45
Q

Dalteparin =

- benefits of using it?

A

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