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
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)
3
Q
Lepirudin
A
- Leech protein analog that directly inhibits thormbin
- Used in pts that need anticoagulation that have HIT
4
Q
Bilirudin
A
- Leech protein analog that directly inhibits thormbin
- Used in pts that need anticoagulation that have HIT
5
Q
Agatroban
A
- Leech protein analog that directly inhibits thormbin
- Used in pts that need anticoagulation that have HIT
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.
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)
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.
9
Q
Clopidrogel
A
- Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
- Used commonly post stent
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
11
Q
Prasugrel
A
- Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
- Used commonly post stent
12
Q
ticagrelor
A
- Direct inhibitor of ADP receptor that prevents the expression of Gp2b3a on plateltes and prevents coagulation
- Used commonly post stent
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
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
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)
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
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
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
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
D-Actinomycin
- Intercalates with DNA
- Works in all phases of cell cylce
- Myelosupression
26
Doxorubacin
- 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
Dexrazoxane
-Given with doxorubicin to reduce risk of DCM
28
Bleomycin
- Causes free radical damage to DNA and DNA breaks.
- Used in G2 phase
- Toxicity: Pulmonary fibrosis, skin changes. Minimal myelosupression
29
Cyclophosphamide/ifosphamide
- 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
Mesna
-Thiol containing molecule that complexes with acroelin of cyclophophamide to impede hemorrhagic cystitis
31
Carmustine, lomustine, semustine
- 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
streptozocin
- 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
Busulfan
- 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
Vincristine
- Binds to tubulin and inhibits polymerization of MT
- Active during M phase
- Cristing causes peripheral neuropathy and paralytic ileus
35
Vinblastine
- Binds to tubulin and inhibits polymerization of MT
- Active during M phase
- Blastine causes myelosupression
36
Paclitaxel
- Binds Tubulin in polymerized state and prevents depolymerization and MT dynamics
- Active during M phase
- Toxicity: Myelosupression and may cause female infertility
37
Cisplatin
- Cross Links DNA
| - Toxicity: Nephrotoxicity (prevent with amiphostine) and Acoustic nerve toxicity
38
Amiphostine
-Scavenges free radicals and reduces nephrotoxicity caused by cisplatin
39
Etoposide
- Antibiotic that interferes with DNA topoisomerase 2 leading to DNA degredation
- Active during G2 and S phase
40
Hydroxyurea
- Inhibits ribonucleotide reductase
- Only functions in S phase
- Used in sickle cell to increase HbF production
41
Prednisone
- Induces apoptosis
| - Associated with cataracts, osteoporosis, psychosis and other symptoms
42
Tamoxifen, Reloxifen
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
Trastuzumab
Monoclonal antibody to Her2-Neu TK
- Used in Her2 positive breast cancers
- Toxicity: Cardiotoxicity
44
Imatinib
- Binds BCR-ABL in CML. TKI
| - Tox: Fluid retention
45
Rituximab
- CD20 Ab
| - Reduces B cells. NHL and RA
46
Vemurafenib
- Inhibitor of Braf kinase at V600E mutation
| - Used in melanoma
47
Bevacizumab
-Anti VEGF inhibits angiogenesis
