1. thrombocytopenia (HIT) 2. osteoporosis

Heme/oncology drugs Flashcards by Hoi Wan

mech: heparin

cofactor for antithrombin activation

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PT or PTT elevated with heparin?

Only PTT

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heparin side effects

thrombocytopenia (HIT)

2. osteoporosis

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benefit of low molecular weight heparins?

act more on factor Xa, better bioavailability and a longer half life
–no lab monitoring needed

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pathophys: hepariin induced thrombocytopenia

development of IgG antibodies against heparin bound to platelet factor 4

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Lepirudin, bivalirudin: derived from?

derivative of hirudin, from leeches

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mech: lepirudin, bivalirudin?

inhibit thrombin

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when would you use lepirudin/bivalirudin?

If a pt cannot use heparin because of HIT

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warfarin metabolized by

cytochrome P450

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warfarin affects PT or PTT?

PT. affects extrinsic pathway.

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clinical use of warfarin

chronic anticoagulation after STEMI, DVT, prevention of stroke in Afib

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warfarin contraindicated in

pregnancy. Unlike heparin, which does NOT cross the placenta

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Tox: warfarin

skin/tissue necrosis
drug/drug interactions
-teratogenic

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which inhibits coagulation in vitro, heparin or warfarin?

heparin

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alteplace, reteplace, tenecteplase

tPA, rPA, TNK-tPA

thrombolytics

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tPA mechanism

aids conversion of plasminogen to plasmin, which cleaves thrombin and fibrin

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tPA: PT or PTT change?

Increases both

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reversal of tPA overdose with

aminocaproic acid

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tPA contraindicated in

active bleed
history of intracranial bleed
bleeding diathesis
severe hypertension

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aspirin effect on PT or PTT

none

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aspirin decreases plasma levels of

TXA2 and prostaglandins

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tox: ticlopidine

neutropenia

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clopidogrel
ticlopidine
prasugrel
ticagrelor

ADP receptor inhibitors

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ADP receptor inhibitor: usage

acute coronary syndrome
coronary stenting
decreased incidence of thrombotic stroke

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cilostazol mechanism

phosphodiesterase III inhibitor. Increases cAMP in platelets, inhibiting aggregation --also a vasodilator

indications: cilostazol

intermittent claudication, prevention of stroke | angina prophylaxis

dipyridamole class

phosphodiesterase II inhibitor like cilostazol.

tox: cilostazol

nausea, headache, facial flushing, hypotension

eptifibatide

GpIIb/IIIa inhibitor

tirofiban

GpIIb/IIIa inhibitor

toxicity of GpIIb/IIIa inhibitors

bleeding, thrombocytopenia

which cancer drugs work on the M phase

vinca alkaloids | taxols

which cancer drugs work on the G2 phase

bleomycin and etoposide

which cancer drugs work on the S phase

etoposide and antimetabolites

Methotrexate: mechanism

decreases dTMP | decreases dNA

methomtrexate for which cancers?

leukemia lymphoma choriocarcinoma sarcoma

methotrexate use: nonneoplastic

abortion ectopic pregnancy RA psoriasis

tox: methotrexate

myelosuppression macrovesicular fatty change in liver mucositosis teratogen

tx of methotrexate myelosuppression

folinic acid | leucovorin

5-FU: indication

colon cancer | basal cell carcinoma, topical

tox: FU

myelosuppression. | photosensitivity

tx for FU myelosuppression?

thymidine. Note: leucovorin does NOT help! Because even if sufficient amount of N5, N10 THF, the enzyme thymidylate synthase doesn't work

mechanism: cytarabine

inhibition of DNA polymerase. A pyrimidine analog

Use: cytarabine

leukemia and lymphoma

tox: cytarabine

leukopenia thrombocytopenia megaloblastic anemia

azathioprine, 6mercaptopurine, and 6thioguanine mech

purine analog decrease purine synthesis

activation of azathioprine/6MP requires

HGPRT

tox of azathioprine

bone marrow, GI, liver

what drug should you NOT give with azathioprine and 6MP?

allopurinol. Because it's metabolized by xanthine oxidase!

mechanism: dactinomycin

intercalates DNA

tox: dactinomycin

myelosuppression

clinical use of dactinomycin

wilms' tumor ewing's sarcoma rhabdomyosarcoma CHILDHOOD tumors

doxo/daunorubicin mechanism

generates free radicals | --INTERCALATES into DNA, causing breaks

Clinical use of doxorubicin

solid tumors, leukemias, lymphomas

toxicity of doxo/dauno

dilated cardiomyopathy myelosuppression alopecia

prevention of doxo/dauno cardiotoxicity

dexrazoxane

Bleomycin mechanism

free radicals | -breaks DNA

use: bleomycin

testicular cancer | hodgkins

toxicity of bleomycin

pulmonary fibrosis | skin changes

which cancer agents are alkylating

cyclophosphamide, ifosfamide busulfan nitrosoureas

cyclophosphamide, ifosfamide mech

covalently X links DNA at guanine N7

cyclophosphamide requires activation by

liver

Side effects of cyclophosphamide

myelosuppression | hemorrhagic cystitis

how to prevent cyclophosphamide hemorrhagic cystitis

mesna, binds toxic metabolite

use: cyclophosphamide

solid tumors, brain cancers | leuk, lymph

carmustine, lomustine, semustine, stretpzocin

nitrosureas

carmustine and friends mechanism

bioactivation then crosses blood brain barrier

use: nitrosureas (carmustine)

brain tumors like GBM

tox of nitrosureas

CNS dizziness and ataxia

busulfan mechanism

alkylates DNA

use: busulfan

CML | --also bone marrow ablation

tox: busulfan

pulmonary fibrosis | hyperpigmentation

Mech: vincrinstine, vinblastine

Bind tubulin and block microtubule polymerization

vincristine tox

neurotox (areflexia, peripheral neuritis, ileus)

vinblastine tox

bone marrow suppression

paclitaxel mechanism

stabilizes polymerized microtubules in M phase. mitotic spindles can't break down-->no anaphase

indications of paclitaxel

ovarian/breast

tox of paclitaxel

myelosuppression | hypersensitivity

cisplatin/carboplatin tox

nephrotoxicity and acoustic nerve damage

prevent cisplastin nephrotoxicity with

amifostine, a free radical scavenger and chloride diuresis

indications of cisplatin

testicular, bladder, ovary, lung cancer

etoposide, teniposide mechanism:

inhibit topoisomerase II=DNA degradation

tox of etoposide

myelosuppression GI alopecia

hydroxyurea affects which phase of cell cycle

S phase | --inhibits ribonucleotide reductase

prednisone cancer use?

CLL | non-hodgkins. triggers apoptosis

tamoxifen/raloxifene mechanism

blocks estrogen binding to receptor

SERM indication

breast cancer and osteoporosis

tamoxifen tox

increased endometrial cancer and hot flashes. partial endometrial agonist

raloxifen tox

NO increase in endometrial carcinoma. complete antagonist

trastuzumab mechanism

antibody against HER2, a tyrosine kinase

trastuzumab tox

cardiotoxicity

imatinib toxicity

fluid retention

rituximab indications

NHL, rheumatoid arthritis

vemurafenib mechanism

inhibits B-Raf kinase with V600E mutation

use: vemurafenib

metastatic melanoma

bevacizumab use:

Solid tumors

mechanism bevacizumab

monoclonal antibody against VEGF

Heme/oncology drugs Flashcards

(97 cards)