Coagulation Disorder Drugs Flashcards
ASPIRIN
irreversible COX inhibitor (acetylation); reduces TxA2
preferentially targets platelets: endothelial cells can produce new prostacyclin; platelet has no nucleus to produce more TXA2
AE: GI, allergy (bronchospasm)
Use: secondary prevention of CV events
overdose: hepatic and renal toxicity
ibuprofen
COX inhibitor
CLOPIDOGREL
oral: prodrug
irreversible ADP receptor (P2Y12) inhibitor
poor 2C19 metabolizers have reduced response
use: post-MI, stroke, PAD (peripheral artery disease), PCI (percutaneous coronary intervention)
*ischemic heart disease
TICLOPIDINE
oral: metabolite more potent
irreversible ADP receptor (P2Y12) inhibitor
BB: agranulocytosis, neutropenia, thrombocytopenia, TTP, anemia
use: secondline due to AE
prasugrel
oral: prodrug
irreversible ADP receptor (P2Y12) inhibitor
use: acute MI, arterial thromboembolism, prophylaxis, PCI, unstable angina
dipyridamole
Oral/IV
phosphodiesterase (PDE) inhibitors
1. prostacyclin released-> increase adenylate cyclase-> cAMP increases: AA acid not released: decrease TXA2
2. adenosine accumulates (vasodilation)
3. decreases cAMP breakdown
use: prophylaxis of thrombosis for prosthetic heart valve (with warfarin)
CI: hypotension, asthma
hepatic glucoronidation; fecal elimination
ABCIXIMAB
IV
non-competitive, irreversible GPIIb/IIIa inhibitor
persists for 2 weeks after stopping administration
AE: bleeding, thrombocytopenia, anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty
EFTIFIBATIDE
IV
reversible GPIIb/IIIa inhibitor
only persists 4 hrs
AE: bleeding, thrombocytopenia (less), anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty
tirofiban
IV
reversible GPIIb/IIIa inhibitor
only persists 4 hrs
AE: bleeding, thrombocytopenia, anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty
vorapaxar
PAR-1 inhibitor: blocks thrombin induced platelet aggregation
slower onset than for GPIIb/IIIa inhibitors
T1/2: 8 days
persists: 4 weeks
CYP3A4 metabolism
AE: bleeding
HEPARIN
IV/SC: rapid onset ONLY for inpatient use indirect thrombin inhibitor: accelerates AT3 binding coagulation factors (2, 10) monitor: aPTT (want 1.5-2.5x normal) SE: bleeding, antigenic (from animals and easy to get) anaphylaxis, thrombocytopenia acts in blood, rapid onset, use is acute need to monitor short T1/2 80 u/kg bolus followed by 18 u/kg/hr
PROTAMINE SULFATE
IV
heparin antidote (v. basic): binds up heparin
incompletely neutralizes LMWH; does not reverse fondaparinux
SE: allergy to fish/DMT2: protamine rxn, too much is anticoagulative
DABIGATRAN
oral
direct thrombin inhibitor
Tx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)
bivalirudin
IV
direct thrombin inhibitor
Tx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)
lepirudin
IV
direct thrombin inhibitorTx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)