Heme Onc Flashcards

1
Q

Heparin

A
  • Increases binding affinity of antithrombin for factor 2 (thrombin) and 10a
  • Causes impaired coagulation, followed with PTT
  • Has a short half life and rapid onset of action (IV only)
  • Used for quick antiocagulation, also used when warfarin is started to prevent skin necrosis
  • Does not cross the placenta and is safe to use in pregnancy
  • Overdose can predispose to bleeding and can be treated with protamine sulfate
  • LMWH has more effect on factor 10 and has a longer half life
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2
Q

HIT

A
  • IgG antibodies to hapten of heparin and platelet factor 4.
  • Causes destruction of platelets leading to thrombocytopenia and also causes thrombosis from platelet fragments in circulation.
  • Give direct thombin inhibitors otherwise (lepirudin, bilirudin)
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3
Q

Lepirudin

A
  • Leech protein analog that directly inhibits thormbin

- Used in pts that need anticoagulation that have HIT

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4
Q

Bilirudin

A
  • Leech protein analog that directly inhibits thormbin

- Used in pts that need anticoagulation that have HIT

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5
Q

Agatroban

A
  • Leech protein analog that directly inhibits thormbin

- Used in pts that need anticoagulation that have HIT

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6
Q

Warfarin

A
  • Inhibit vitamin K dependent gamm carboxylation of factors 2, 7, 9, 10, C, S in liver. Epoxide reductase
  • Most commonly used for anticoagulation with A fib or DVT prophylaxis
  • INR is how you follow it (PT)
  • Metabolized by P450 system. Inducers will decrease anti-coagulation effects
  • Can cross the placenta and cause teratogenicity including blindness and hydrocephalus
  • Causes warfarin induced skin necrosis (C has shorter half life. Always give heparin at first does)
  • Overdose treated with vitamin K. If acute need give FFP that contains clotting factors.
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7
Q

Ateleplase

A
  • Activates Plasminogen to Plasmin which cleaves Fibrin, FIbrinogen, and decreases platelet adherence
  • Used in ischemic stroke, PE, MI without Cath available
  • Contraindicated in any bleeding risk and patients with severe hypertension
  • Increase PT and PTT without effecting platelet count
  • Overdose treated with aminocaproic acid (anaolog of lysine that inhibits proteases that cleave at lysine sites)
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8
Q

Aspirin

A
  • Covalently acetylates Cox-I and Cox-2 (Suicide inhibition (penicilin also)) irreversible inihbition that requires platelets to be resynthesized to overcome effects (Weeks later)
  • Prevents production of TXA2 which prevents vasoconstriction and platelet aggregation
  • Prophylaxis in MI and other coagulation risks
  • S/E: Tinnitus, GI bleed (PG)
  • Intersitial nephritis with longterm use
  • Respiratory alkalosis (Depresses breathing center) followed by metabolic acidosis (Salicylic acid)
  • Reyes Syndrome with viral infection (flu/VZV) Cirrhosis and mental status changes.
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9
Q

Clopidrogel

A
  • Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
  • Used commonly post stent
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10
Q

Ticlopodine

A
  • Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
  • Used commonly post stent
  • MAY CAUSE NEUTROPENIA, only one of ADPR inhibitors to do this
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11
Q

Prasugrel

A
  • Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
  • Used commonly post stent
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12
Q

ticagrelor

A
  • Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
  • Used commonly post stent
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13
Q

Cilostazol

A
  • Inhibit PDE III leads to decreased cAMP and decreased platelet activation. Also causes vasodilation
  • Primarilly indicated in claudication, TIA, Angina
  • S/E: Hypotension, headache, nasuea
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14
Q

Dipridamole

A
  • Inhibit PDE III leads to decreased cAMP and decreased platelet activation. Also causes vasodilation
  • Primarilly indicated in claudication, TIA, Angina
  • S/E: Hypotension, headache, nasuea
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15
Q

Abciximab

A
  • Directly bind to Gp2b3a R and inhibit binding to fibrinogen an platelet aggregation
  • Used in angioplasty and acute coronary syndrome
  • Risk of thombocytopenia and bleeding
  • Fab PORTION OF MAb (only abciximab)
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16
Q

eptifibatide

A
  • Directly bind to Gp2b3a R and inhibit binding to fibrinogen an platelet aggregation
  • Used in angioplasty and acute coronary syndrome
  • Risk of thombocytopenia and bleeding
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17
Q

Tirofiban

A
  • Directly bind to Gp2b3a R and inhibit binding to fibrinogen an platelet aggregation
  • Used in angioplasty and acute coronary syndrome
  • Risk of thombocytopenia and bleeding
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18
Q

Rivaroxiban

A
  • Direct factor 10a inhibitor
  • Used prophylaxis in A Fib and other clotting disorders
  • Oral administration and no checking blood levels (INR)
  • Increase risk of bleeding with no reversal
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19
Q

Apcixiban

A
  • Direct factor 10a inhibitor
  • Used prophylaxis in A Fib and other clotting disorders
  • Oral administration and no checking blood levels (INR)
  • Increase risk of bleeding with no reversal
20
Q

Methotrexate

A
  • Inhibits DHFR leading to impaired TMP synthesis leading to reduced cellular division.
  • Functions in S phase
  • S/E: Myelosupression, treat with leucoverin (bypass DHFR)
21
Q

Leucoverin

A

Treats methotrexate induced myelosuprresion by providing folate that bypasses DHFR

22
Q

5-FU

A
  • Coverted to 5F-dUMP which Inhibits thymidylate synthesis and reduces TMP production resulting in decreased DNA snythesis
  • Used in S phase
  • Toxicity: Myelosupression, can’t treat with leucoverin but can be recovered by providing thymidine
23
Q

6-MP

A
  • Inhibits de novo Purine Synthesis leading to impaired DNA replication
  • Activated by HGPRT and metabolized by xanthine oxidase
  • Active during S phase
  • Metabolism will be impaired with use of allopurinol
24
Q

Cyterabine

A
  • Pyrimidine analog that inhibits DNA polymerase
  • Active in S phase
  • Toxicity: Megalolastic Anemia
25
Q

D-Actinomycin

A
  • Intercalates with DNA
  • Works in all phases of cell cylce
  • Myelosupression
26
Q

Doxorubacin

A
  • Intercalates with DNA, inhibits polymerase and causes free radical induced damage
  • Works in all stages of cell cycle
  • Toxicity: DCM Treatment with Dexrazoxane (Fe Chelator) will reduce risk of DCM
27
Q

Dexrazoxane

A

-Given with doxorubicin to reduce risk of DCM

28
Q

Bleomycin

A
  • Causes free radical damage to DNA and DNA breaks.
  • Used in G2 phase
  • Toxicity: Pulmonary fibrosis, skin changes. Minimal myelosupression
29
Q

Cyclophosphamide/ifosphamide

A
  • DNA Alkylating agent
  • Effective in all stages of cell cycle
  • Toxicity (acrolein) is hemorrhagic cystitis which can be treated with mesna
  • Also causes myleosupression
30
Q

Mesna

A

-Thiol containing molecule that complexes with acroelin of cyclophophamide to impede hemorrhagic cystitis

31
Q

Carmustine, lomustine, semustine

A
  • Alkylating agents that can cross the BBB and are effective in brain tumors
  • Effective in all stages of cell cycle
  • CNS toxicity: ataxia and dizziness
32
Q

streptozocin

A
  • Alkylating agents that can cross the BBB and are effective in brain tumors
  • Effective in all stages of cell cycle
  • CNS toxicity: ataxia and dizziness
33
Q

Busulfan

A
  • Alkylating agent, most commonly used as BM ablating agent before BM transplant
  • Works in all stages of cell cycle
  • Toxicity: Pulmonary fibrosis and hyperpigmentation
34
Q

Vincristine

A
  • Binds to tubulin and inhibits polymerization of MT
  • Active during M phase
  • Cristing causes peripheral neuropathy and paralytic ileus
35
Q

Vinblastine

A
  • Binds to tubulin and inhibits polymerization of MT
  • Active during M phase
  • Blastine causes myelosupression
36
Q

Paclitaxel

A
  • Binds Tubulin in polymerized state and prevents depolymerization and MT dynamics
  • Active during M phase
  • Toxicity: Myelosupression and may cause female infertility
37
Q

Cisplatin

A
  • Cross Links DNA

- Toxicity: Nephrotoxicity (prevent with amiphostine) and Acoustic nerve toxicity

38
Q

Amiphostine

A

-Scavenges free radicals and reduces nephrotoxicity caused by cisplatin

39
Q

Etoposide

A
  • Antibiotic that interferes with DNA topoisomerase 2 leading to DNA degredation
  • Active during G2 and S phase
40
Q

Hydroxyurea

A
  • Inhibits ribonucleotide reductase
  • Only functions in S phase
  • Used in sickle cell to increase HbF production
41
Q

Prednisone

A
  • Induces apoptosis

- Associated with cataracts, osteoporosis, psychosis and other symptoms

42
Q

Tamoxifen, Reloxifen

A

SERM that is partial agonist. Used in breast cancer because acts as an antagonist there.

  • Also prevents osteoporosis
  • Temoxifen risk of endometrial cancer
  • Reloxifen no risk of endometrial cancer
43
Q

Trastuzumab

A

Monoclonal antibody to Her2-Neu TK

  • Used in Her2 positive breast cancers
  • Toxicity: Cardiotoxicity
44
Q

Imatinib

A
  • Binds BCR-ABL in CML. TKI

- Tox: Fluid retention

45
Q

Rituximab

A
  • CD20 Ab

- Reduces B cells. NHL and RA

46
Q

Vemurafenib

A
  • Inhibitor of Braf kinase at V600E mutation

- Used in melanoma

47
Q

Bevacizumab

A

-Anti VEGF inhibits angiogenesis