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Flashcards in Hema/Onco Deck (42)
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1

Heparin
MOA

Antithrombin activator.
Dec. thrombin, Dec. FXa.
Short half life.

2

Heparin
Clinical use

Immediate anticoagulation (PE, ACS, MI, DVT).
Can be used in pregnancy.
Monitor w/ PTT.

3

Heparin
[Toxicity, antidote]

Bleeding, thromboctyopenia
Osteoporosis
Drug-drug interactions
Antidote: Protamine sulfate

4

Heparin-induced Thrombocytopenia

Develop IgG-Abs against heparin-bound platelet factor 4 (PF4).
Complex activates platelets -- thrombosis, thrombocytopenia.

5

Warfarin
MOA

Blocks epoxide reductase -- prevents gamma-carboxylation of vit k-dependent clotting factors.
(Effects extrinsic pathway)

6

Warfarin
Clinical use

Chronic anticoagulation -- venous thromboemobolism prophylaxis, prevent stroke in A-fib.
Not for pregnancy.
Follow w/ PT/INR.

7

Warfarin
Toxicity

Bleeding, teratogenic, skin/tissue necrosis.
Early transient hypercoagulability -- proteins C and S have short half-lives.

8

Heparin Bridging

Heparin used when starting warfarin.
Heparin allows anticoagulation when in initial, transient hypercoagulable state caused by warfarin.
Reduces risk of venous thromboembolism and skin/tissue necrosis.

9

Thrombolytics
Drug names

Alteplase (tPA)
Reteplase (rPA)
Streptokinase
Tenecteplase (TNK-tPA)

10

Thrombolytics
MOA

Convert Plasminogen --> Plasmin.
Plasmin cleaves thrombin --> fibrin clots.
Inc. PT/PTT

11

Thrombolytics
Clinical use

Early MI
Early ischemic stroke
Severe PE

12

Thrombolytics
[Toxicity, CI, antidote]

Bleeding.
CI in pts. w/ active bleeding, hx of intracranial bleed, recent surgery, bleeding diatheses, severe HTN.
Antidote: aminocaproic acid (fibrinolysis inhibitor).

13

ADP receptor inhibitors
Drug names

Clopidogrel
Prasugrel
Ticagrelor (reversible)
Ticlodipine

14

ADP receptor inhibitors
MOA

Irreversibly blocks ADP receptors -- Prevents GpIIb/IIIa expression on platelet surface -- inhibits platelet aggregation

15

ADP receptor inhibitors
Clinical use

Acute coronary syndrome.
Dec. incidence/recurrence of thrombotic stroke.

16

Factor Xa inhibitors (Apixaban, Rivaroxaban)
[MOA, clinical use]

Bind and directly inhibit FXa.
For DVT, PE (rivaroxaban).
Stroke prophylaxis in pts w/ AFib.

17

Aspirin
[MOA, Labs, clinical use, Toxicity]

>Irreversibly inhibits COX-1 and COX-2.
>Inc. BT, dec. TXA2, dec. PGs.
>No effect on PT, PTT.
>Antipyretic, analgesic, anti-inflammatory, Antiplatelet.
>Toxicity: ARF, gastric ulcer, tinnitus; Reye syndrome in kids w/ viral infection.

18

Gp IIb/IIIa inhibitors (Abciximab, Eptifibatide, Tirofiban)
[MOA, clinical use]

>Binds receptor for Gp IIb/IIIa on activated platelets -- prevents aggregation.
>For unstable angina, PTCA (percutaneous transluminal coronary angioplasty).

19

Azathioprine, 6-MP, 6-TG
[MOA, clinical use, toxicity]

>Purine analogs; dec. de novo purine synthesis.
>Activated by HGPRT.
>Prevent organ rejection, RA, IBD, SLE.
>Tox: myelosuppression; Azathioprine and 6-MP metabolized by xanthine oxidase -- toxicity w/ Allopurinol or febuxostat.

20

Cladribine (2-CDA)
[MOA, clinical use, toxicity]

>Purine analog; inhibits DNAp; DNA strand breaks.
>For Hairy cell leukemia.
>Tox: nephrotoxicity, neurotoxicity, myelosuppression.

21

Cytarabine (arabinofuranosyl cytidine)
[MOA, clinical use, toxicity]

Pyrimidine analog -- inhibits DNAp.
For AML, lymphomas.
Tox: pancytopenia

22

5-FU
[MOA, clinical use, toxicity]

>Active metabolite is 5F-dUMP, w/c complexes w/ Folic acid -- inhibits Thymidylate synthase -- dec. dTMP -- dec. DNA synthesis.
>For colon cancer, pancreatic cancer, basal cell CA.
>Tox: not reversible w/ Leucovorin (folinic acid, vs. Methotrexate)

23

Methotrexate
[MOA, clinical use, toxicity]

>Folic acid analog; competitively inhibits dihydrofolate reductase -- dec. dTMP -- dec. DNA synthesis.
>For cancers, ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis.
>Tox: hepatotoxic, pulmo fibrosis; reversible w/ Leucovorin (vs. 5-FU)

24

Bleomycin
[MOA, clinical use, toxicity]

>Induces free radical formation -- breaks in DNA strands.
>For testicular cancer, Hodgkin Lymphoma.
>Tox: pulmo fibrosis, skin hyperpigmentation

25

Dactinomycin
[MOA, clinical use]

>Intercalates in DNA --> causes breaks in DNA.
>For Wilms tumor, Ewing sarcoma, rhabdomyosarcoma.
>Used for kids tumors.

26

Doxorubicin, Daunorubicin
[MOA, clinical use, toxicity]

>Generates free radicals.
>Intercalates in DNA --> causes breaks in DNA --> dec. replication.
>For solid tumors, leukemias, lymphomas.
>Tox: cardiotoxicity (prevent w/ Dexrazoxane, an iron chelator), myelosuppression, alopecia.

27

Busulfan
[MOA, clinical use, toxicity]

Crosslinks DNA
For CML
Tox: severe myelosuppression (almost all cases)

28

Cyclophosphamide, Ifosfamide
[MOA, clinical use, toxicity]

>Crosslink DNA at guanine N7. Needs bioactivation by liver.
>For solid tumors, leukemia, lymphoma.
>Tox: hemorrhagic cystitis -- partially prevented w/ mesna, w/c binds to toxic metabs.

29

Nitrosureas (Carmustine, Lomustine, Semustine, Streptozocin)
[MOA, clinical use, toxicity]

>Needs bioactivation. Cross BBB into CNS, where it crosslinks DNA.
>For brain tumors (glioblastoma multiforme)
Tox: CNS toxicity

30

Paclitaxel (other taxols)
[MOA, clinical use, toxicity]

>Hyperstabilizes polymerized microtubules in M phase so mitotic spindle can't break down (prevents anaphase).
>For ovarian and breast CA.
>Tox: alopecia