Heme Drugs Flashcards
Heparin
- immediate effect
- use: coronary syndrome, PE, MI, DVT, ok for pregnancy
- binds endothelial surface and accelerates antithrombin IIIa to inhibit 2a,9a,10a,11a,12a
- increases PTT
- short 1/2 life
- injection only
- adverse: HIT, osteoporosis, hyperkalemia
Enoxaprin (LMWH)
- more bioavailability, longer 1/2 life, easier dosing
- less risk than heparin
- inhibits 10a more than 2a
Warfarin
- slow onset, limited by 1/2 life
- acts on liver, oral, must monitor pt
- ok for chronic use, NOT ok for pregnancy
- impairs post translational mods of Factors 2,7,9,10
- reverse: use Vitamin K1 , 4 factor prothrombin complex concentrates
Aspirin
- blocks cyclooxygenase, lowers TXA2 levels, inhibits platelet aggregation
- use: early MI, ischemic stroke
- adverse: bleeding, GI upset
Abciximab
- use: unstable angina, percutaneous coronary intervention
- blocks fibrinogen receptor (GP 2b,3a) on activated platelets, blocks aggregation
- IV use, rapid acting
- adverse: bleeding, thrombocytopenia
Clopidigrel, ticagrelor, prasugrel
- ADP(P2Y12) receptor antagonists
- use: acute coronary syndrome, coronary stenting, decrease stroke risk
- prevents expression of GP 2b,3a on platelet surface
- oral use, often use with aspirin
- adverse: bleeding, thrombocytopenia
Dipyrimidamole, Cilostazol
- PDE inhibitors
- use: intermittent claudication, coronary vasodilation, TIA, stroke prevention
- increases cAMP, prevents aggregation, vasodilation
- adverse: bleeding, nausea, headache, hypotension, abdominal pain
Bivalirudin, argatroban, dabigatran
- thrombin inhibitors
- directly inhibit free and clotted thrombin, competitively bind active site
- use:venous thrombosis, prevent stroke in a fib, use in HIT
- dabigatran is only oral
- adverse: bleeding, use of P-GP inhibitors at same time can increase levels of bivalirudin and argatroban
Idarucizumab
- monoclonal antibody
- reversal of dabigatran anticoagulant effects
Rivaroxiban, apixaban
- 10a inhibitors
- directly inhibit factor 10a by binding it
- oral
- use: prophylaxis for DVT, PE, stroke with a fib
- adverse: bleeding, use of p-GP drugs could increase levels
- Rivaroxiban absorption is mediated by p-GP transporter
Fondaparinux
- 10a inhibitor
- inactivated 10a indirectly by accelerating ATIII, no action on 2a
- injection
- no issues with HIT, no PF4 antibody is formed
- long 1/2 life
- adverse: bleeding
Alteplase (tPA), reteplase (rTPA), tenecteplase (TNK-tPA)
- fibrinolytics, plasminogen activators
- early MI, ischemic stroke, direct thrombolysis of severe PE
- directly or indirectly aid the conversion of plasminogen to plasmin which then cleaves thrombin and fibrin clots
- no effect on platelet count
- adverse: bleeding, can reverse with antifibrinolytics, platelet transfusion, FFP, PCC
Tranexamic acid, Aminocaproic acid
- antifibrinolytic
- reversible blockade of lysine binding sites on plasminogen molecules to inhibit fibrin formation
- use: reduce perioperative bleeding, prevent blood loss from trauma, postpartum hemorrhage, prophylaxis for hemophilia, heavy periods
- adverse: bradyarrhythmia, hypotension, seizures
Cytarabine and anthracycline
-induction: 7 days + 3 days
-extremely toxic therapy
-consolidation: high dose cytarabine, given 3-4 times after remission
toxicities: Anthracycline=cardiac failure
Cytarabine=cerebellar toxicity
Imatinib, Dasatinib, Nilotinib
-tyrosine kinase inhibitors target BCR-ABL1 protein and block activity
-toxicities:
Imatinib- fluid retention, muscle pain/cramps, GI disturbance
Dasatinib- 20-25% pleural effusions, rare pulmonary arterial hypertension
Nilotinib- vascular events, peripheral arterial occlusive disease, CAD, hyperglycemia, hypercholesterolemia
