Usmle Step 1 High Yield Systems Heme/onc Pharmacology 2013

Front 1

Heparin MOA

Back 1

Cofactor for the activation of antithrombin
DEC thrombin
DEC factor Xa

(short half life)

Front 2

Heparin clinical use

Back 2

IMMEDIATE anticoag for PE, acute coronary syndrome, MI, DVT

Used during pregnancy (does NOT cross placenta)

Follow PTT

Front 3

Heparin TOX

Back 3

Bleeding
Thrombocytopenia (HIT)
Osteoporosis
DDI

HIT: IgG ab against Heparin-PF4 complex.
Ab-Heparin-PF4 complex activates platelets-->thrombosis and thrombocytopenia

PROTAMINE SULFATE

Front 4

LMWH (Enoxaparin, Dalteparin)

Back 4

Act more on factor Xa
Better bioavaliability
2-4x longer half life
No monitoring necessary
NOT easily reversible

Front 5

Lepirudin, Bivalirudin MOA

Back 5

Derivatives of hirudin (anticoag used by leeches; inhibits thrombin)

Alternatives for HIT patients

Front 6

Warfarin MOA

Back 6

Interferes with normal syn and gamma-carboxylation of vit-k dep clotting factors (2, 7, 9, 10, C, S)

Metabolized by P450

Monitor PT

Front 7

Warfarin clinical use

Back 7

Chronic anticoag

NOT used in pregnant women (cross placenta)

Need overlapping coverage initially

Front 8

Warfarin TOX

Back 8

Bleeding
Teratogenic
Skin/tissue necrosis
DDI

REVERSAL: Vitamin K
Rapid reversal of severe OD: Fresh frozen plasma

Front 9

Thrombolytics

Back 9

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

Front 10

Thrombolytics (-plase) MOA

Back 10

Aid conversion of plasminogen to plasmin

PLasmin cleaves thrombin and fibrin cloths

INC PT and PTT
NO change in platelet count

Front 11

Thrombolytics Clinical use

Back 11

Early MI (<3hrs), severe PE

Front 12

Thrombolytics TOX

Back 12

CONTRA in active bleeding, recent srugery, hemophilia

TX: Aminocaproic acid (inhibitor of fibrinolysis)

Front 13

Aspirin MOA

Back 13

IRREVERSIBLY inhibits COX by covalent acetylation

INC BT
DEC TXA2 and PG
NO effect on PT or PTT

Front 14

Aspirin clinical use

Back 14

Antipyretic, analgesic, anti-inflamm, anti-platelet

Front 15

Aspirin TOX

Back 15

Gastric ulceration
Tinnitus
Acute renal failure (chronic use)
Reye's syndrome (hepatoencephalopathy) in children with viral infection (unless Kawasaki)

OD= Respiratory alkalosis and metabolic acidosis

Front 16

ADP receptor inhibitors

Back 16

Clopidogrel, Ticlodipine, Prasugrel, Ticagrelor

Front 17

ADP receptor inhibitors MOA

Back 17

Inhibit platelet aggregation by IRREVERSIBLY blocking ADP receptor (prevents conformational change and GIIb/IIIa transition to membrane surface)

Front 18

ADP receptor inhibitor clinical use

Back 18

Acute coronary syndrome
Coronary stenting
DEC incidence/recurrece of thrombotic stroke

Front 19

ADP receptor inhibitor TOX

Back 19

Neutorpenia (Ticlodipine)

Front 20

Cilostazol, Dipyridamole MOA

Back 20

Phosphodiesterase III inhibitor
INC cAMP in platelets= inhibiting platelet aggregation

Vasodilators

Front 21

Cilostazol, Dipyridamole clinical use

Back 21

Intermittent claudication
coronary vasodilation
Prevent stroke or TIAs
Angina prophylaxis

Front 22

Cilostazol, Dipyrdamole TOX

Back 22

N, headache, facial flushing, HYPO tension, abdominal pain

Front 23

GPIIb/IIIa inhibitors

Back 23

Abciximab, Eptifibatide, Tirofiban

Front 24

GpIIb/IIIa inhibitors MOA

Back 24

Bind to IIb/IIIa receptor on activated platelet preventing aggregation

Abciximab made from monoclonal ab Fab fragments

Front 25

GpIIb/IIIa inhibitors clinical use

Back 25

Acute coronoary syndrome
Percutaneous transluminal coronary angioplasty

Front 26

GpIIb/IIIa inhibitors TOX

Back 26

bleeding
thrombocytopenia

Front 27

Methotrexate (MTX)

MOA/clinical use/TOX

Back 27

Folic acid analog that inhibits DHFR

Cancer, abortion, ectopic pregnancy, RA, psoriasis

TOX:
Myelosupression (reversible w/ LECUVORIN--Folinic acid)
Macrovesicular fatty change in liver
Mucositis
TERATOGENIC

Front 28

5-FU

MOA/Clinical use/TOX

Back 28

Pyrimidine analog covalently complexes folic acid

Complex inhibits THYMIDYLATE SYNTHASE

Use: colon cancer, BCC

Tox: Myelosuppression (Leucovorin)

OD rescue: Thymidine

Photosensitivity

Front 29

Cytarabine

MOA/Clinical use/TOX

Back 29

Pyrimidine analog-->inhibitor of DNA polymerase

Use: Leukemias, Lymphomas

TOX: Leukopenia, Thrombocytopenia, MEGALOBLASTIC anemia

Front 30

Azothioprine, 6-MP

Back 30

Purine (thiol) analogs

DEC de novo purine synthesis

Activated by HGPRT

Use: Leukemias

TOX: metabolized by XANTHINE OXIDASE; thus INC tox with allopurinol

Front 31

Actinomycin D

Back 31

Intercalates in DNA

Use: Wilm's tumor, Ewin's sarcoma, rhabdomyosarcoma

Front 32

Doxorubicin

Back 32

Generate free radicals that create breaks in DNA (DEC replication)

Use: tumors, leukemias, lymphomas

TOX: Dilated Cardiomyopathy

Front 33

Bleomycin

Back 33

Induces free radical formation--> breaks in DNA

USE: testicular cancer
Hodgkin's lymphoma

TOX: Pulmonary fibrosis, skin changes

Front 34

Cyclophosphamide

Back 34

Covalently X-link (interstrand) DNA at guanine N-7 (requires liver bioactivation)

USE: tumors, leuk, lymph, brain cancers)

TOX: hemorrhagic cystitis (partially prevented with MESNA- binds toxic metabolite)

Front 35

Nitrosureas (carmustine, lomustine, semustine, streptozocin)

Back 35

Require bioactivation. Cross BBB-->CNS

Use: Brain tumors (including glioblastoma multiforme)

TOX: CNS

Front 36

Busulfan

Back 36

MOA: alkylates DNA

Use: CML (ablate patients bone marrow before transplantation)

TOX: Pulmonary fibrosis, hyperpigmentation

Front 37

Vincristine, Vinblastine

Back 37

Bind to tubulin in M phase and block polymerization of microtubules so that mitotic spindle cannot form

TOX: Neuro, Bone marrow

Front 38

Paclitaxel, other taxols

Back 38

Hyperstablize polymerized microtubules in M phase so that mitotic spindle cannot break down

Use: ovarian and breast carcinomas

TOX: Myelosuppression, hypersensitivity

Front 39

Cisplatin, carbolplatin

Back 39

Cross-link DNA

Use: Testicular, bladder, ovary and lung carcinomas

TOX: Nephro, acoustic nerve damage (amifostine)

Front 40

Etoposide, teniposide

Back 40

Inhibit topoisomerase II--> INC DNA degradation

TOX: Myelosuppresion, GI irritation, alopecia

Front 41

Hyroxyurea

Back 41

Inhibits ribonucleotide reductase--> DEC DNA synthesis (S-phase specific)

USE: Melanoma, CML, Sickle cell disease (INC HbF)

TOX: bone marrow suppression, GI upset

Front 42

Predinose, Prednisolone

Back 42

Trigger apoptosis (may work on nondividing cells)

Use: CLL, non-hodgkin's lymphomas, immunosuppression

TOX: Cushing's like

Front 43

Tamoxifen, raloxifene

Back 43

SERMS- receptor antag in breast and agonist in bone

Use: Breast cancer, prevent osteoporosis

TOX: Tamoxifen- partial agonist in endometrium=INC risk of endometrial cancer

Front 44

Herceptin

Back 44

Monoclonal ab against Her-2, a tyrosine kinase
Kill breast cancer cells that overexpress HER-2 (ab-dep cytotox)

TOX: cardiotox

Front 45

Imantinib (Gleevac)

Back 45

Philadelphia chromosome bcr-abl tyrosine kinase inhibitor

Use: CML, GI stroma tumors

TOX: fluid retention

Front 46

Rituximab

Back 46

Monoclonal ab against CD20: B cell lymphomas

Use: Non-hodgkin's lymphoma, RA

Front 47

Vemurafenib

Back 47

small molecule inhibitor of forms of the B-raf kinase with V600E mutation

Use: metastatic melanoma

Front 48

Bevacizumab

Back 48

Monoclonal ab against VEGF. Inhibits angiogenesis

Use: Solid tumors