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Parenteral Anticoagulation Drugs
Pharmacotherapy Fall 2013 Exam 3
59
Pharmacology
Professional
12/01/2013

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Term
unfractionated Heparin
Definition
glycosaminoglycan found in the secretory granules of mast cells; enhances activity of antithrombin
Term
no intrinsic activity
Definition
unfractionated heparin
Term
Unfract heparin absorption
Definition
variable; SC 30-75% dose dependent
Term
unfract heparin distribution
Definition
0.07L/Kg
Term
metabolism of unfract heparin
Definition
hepatic and reticulo-endothelial
Term
elimination of unfract heparin
Definition
half-life 30-90 minutes, saturable enzymatic cleavage, renally excreted
Term
unfract heparin administration
Definition
intermittent IV, IV infusion, Deep SC injection
Term
unfract heparin monitoring
Definition
aPTT target range reflecting institutions reagents; NOT required for prophylactic dosing!
Term
unfract heparin adverse efeects
Definition
hemorrhage, osteoporosis, hyperkalemia (especially in renal failure), hypersensitivity reactions, thrombocytopenia
Term
management of bleeding due to heparin
Definition
discontinue, protamine 1% solution as a dose of 1 mg per 100 U of heparin
Term
protamine
Definition
neutralizes heparin by forming an inactive complex with heparin
Term
max single dose of protamine
Definition
50 mg in 10 minutes but may be repeated; infuse SLOWLY over 3-5 minutes
Term
suspected HIT treatment
Definition
discontinue all sources of Heparin, initiate alternative agents (argatroban, bivalrudin, lepirudin), VKA or other anticoagulant therapy will be necessary upon platelet recovery
Term
direct thrombin inhibitors
Definition
prevent an interaction between thrombin and substrates, does not require antithrombin as a cofactor; able to inactivate both free thrombin and thrombin bound to fibrin
Term
doesnot interact with plasma proteins or platelet factors; structurally unrelated to heparins
Definition
direct thrombin inhibitors
Term
argatroban
Definition
small synthetic molecule, binds only to active catalytic site of thrombin, ability to inhibit clot-bound thrombin
Term
elimination of argatroban
Definition
hydrocylated and aromatization in liver to inactivate metabolites
Term
half-life of argatroban
Definition
39-51 minutes, longer with hepatic insufficiency
Term
monitor argatroban
Definition
LFT's, hypotention, aPTT and ACT tests
Term
argatroban indications
Definition
first line for IV infusions in HIT patients, acute MI and fibrinolytics, percutaneous coronary intervention
Term
argatroban when starting oral anticoagulation
Definition
significantly influences INR
Term
when switching argatroban to oral anticoag; initiate warfarin therapy
Definition
using expected daily dose of warfarin while maintaining infusion of argaroban; do NOT use loading dose of warf
Term
measure INR daily when switching argatroban to oral VKA
Definition
INR/= 4.0, stop argatroban and repeat INR q4-6h...if INR is therapeutic continue VKA monotherapy, resume argatroban if not therapeutic
Term
formation of antibodies
Definition
lepirudin and maybe bivalrudin
Term
lepirudin elimination
Definition
renal
Term
bivalrudin elimination
Definition
proteolysis and renal
Term
half life lepirudin
Definition
1.7 hours
Term
half-life bivalrudin
Definition
36 minutes
Term
desirudin (Iprivask)
Definition
does not have indication in HIT treatment; only for DVT prophylaxis in pts undergoing surgery for hip replacement
Term
LMWH pharmacokinetics
Definition
more predictable response compared to UFH due to reduced binding to proteins and cells
Term
LMWH absorption
Definition
90-100% subcutaneous; peak effect 3-5 hours
Term
LMWH elimination
Definition
primarily renal; clearance independent of dose
Term
LMWH administration
Definition
SQ (abd area, upper outer part of thigh while patient is supine), IV
Term
LMWH monitoring
Definition
anti-Xa monitoring (4 hours after injection) especially in renal impairment, weight <50kg, morbidly obese, required prolonged therapy (ie. preggers), and high risk of bleeding or thrombotic recurrence (ie. cancer pts)
Term
LMWH dosing interval
Definition
every 12-24 hours depending on indication and product
Term
dose adjustments for LMWH
Definition
monitoring and adjustment for renal impairment
Term
plasma half-life LMWH
Definition
119-234 minutes (2-4 hours)
Term
adverse effects of LMWH
Definition
NO reversal agent, bleeding (major bleed, hemorrhage, hematoma), thrombocytopenia, injection site rxns (bruising, hemorrhage, skin necrosis)
Term
fondaparinux (Arixtra)
Definition
synthetic active pentasaccharide binds specifically but reversibly to ATIII and selectively inactivates Xa
Term
no significant impact on thrombin, platelets or aPTT
Definition
fondaparinux
Term
adverse effects of fondaparinux
Definition
bleeding (weight-related), HIT--very rare
Term
weight-related contraindication of fondaparinux
Definition
<50 kg for VTE prophylaxis, high risk for bleed
Term
fondaparinux absorption
Definition
100% SQ bioavailability
Term
fondaparinux distribution
Definition
does not bind RBC or other plasma proteins including albumin, glycoproteins, platelets or PF-4
Term
peak plasma concentration fondaparinux
Definition
achieved after 2 hours after single dose, 3 hours with repeated doses
Term
elimination of fondaparinux
Definition
unchanged in urine; contraindicated in patients with severe renal dysfunction CrCl < 30
Term
half-life fondaparinux
Definition
15-18 hours
Term
glycoprotein IIb and IIIa inhibitors
Definition
surface receptor inhibitor for von willebrand factor and fibrinogen, preventing the anchorage of platelets to surfaces and to each other
Term
final pathway of platelet aggregation
Definition
glycoprotein IIb and IIIa inhibitors
Term
abciximab (Reopro)
Definition
chimeric monoclonal antibody (Fab), irreversibly binds to GPIIb and IIIa receptor
Term
used in combo with ASA, clopidogel and UFH/LMWH
Definition
abciximab (Reopro)
Term
positive impact of Reopro
Definition
reduction of restenosis, recurrent MI and death, reduces ischemic events associated with high risk PTCA, and preventing restenosis in PCI patients
Term
Eptifibatide (Integrillin)
Definition
cyclic peptide inhibitor of fibrinogen binding sites of GPIIb/IIIa
Term
use of eptifibatide
Definition
high risk NSTEMI patients as medical management without planned revascularization, NSTEMI with planned PCI, adjunctive for pts with recurrent ischemia despite use of ASA, clopidogrel and an anticoag
Term
tirofiban (aggrastat)
Definition
tyrosine derivative (non-peptide) inhibitor of GPIIb/IIIa
Term
indication of aggrastat
Definition
inferior to abciximab for use in PCI, failure to prove non-inferiority; main place in therapy NSTEMI and UA in hih risk patients or with those with recurrent symptoms
Term
advantage of aggrastat over peptide-based GP inhibitors
Definition
rapid onset f action and little/no immunogenicity
Term
risk of therombocytopenia
Definition
tirofiban and eptifibatide lower than abciximab
Term
renal adjusting in renal insufficiency for GPIIb/IIIa
Definition
eptifibatide and tirofiban
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