Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
90 Cards in this Set
- Front
- Back
anticoagulation drugs
|
indirect thrombin inhibitors, direct thrombin inhibitors, vit K antagonist, factor Xa inhibitor
|
|
Indirect thrombin inhibitor
|
heparin, fondaparinux
|
|
direct thrombin inhibitors
|
hirudin, bivalirudin, lepirudin, argatroban, dabigatrom
|
|
vitamin K antagonist
|
warfarin
|
|
factor Xa inhibitor
|
rivaroxaban
|
|
Thrombolytic Drugs
|
streptokinase, anistreplase, urokinase, alteplase, reteplase, tenecteplase,
|
|
antplatelet agents
|
aspirin, clopidogrel, ticlopidine, abiciximab, eptifibatide, tirofiban
|
|
Drugs used to facilitate clotting
|
vitamin K, clotting factors, fibrinoltic inhibitors, serine protease inhibitors
|
|
clotting factors
|
7,8,9,10, FFP, cryoprecipates
|
|
fibrinolytic inhibitors
|
aminocaproic acid
|
|
serine protease inhibitors
|
aprotinin
|
|
component factor 1
|
fibrinogen
|
|
component factor 2
|
prothrombin
|
|
component factor 4
|
calcium
|
|
component factor 7
|
proconvertin
|
|
component factor 8
|
Antihemophilic factor (AHF)
|
|
component factor 9
|
Christmas factor
|
|
component factor 10
|
Stuart Prower factor
|
|
Disorders treated by anticoagulants
|
venous thrombosis, arterial thrombosis, embolism
|
|
endogenous anticoagulants
|
antithrombin, protein C and protein S
|
|
Antithrombin (AT or AT III)
|
a serine protease inhibitor, inactivates clotting factors 2,9,10
|
|
protein C
|
vitamin K dependent serine protease, activated by thrombin to APC, Degrades cofactor 5 and 8
|
|
protein C deficiency may display
|
increased thrombosis
|
|
Protein S
|
vitamin K dependent glycoprotein. Free form acts as a cofactor to Protein C
|
|
Indirect thrombin inhibitor
|
Heparin (UFH, LMWH) fondaparinux
|
|
indirect thrombin inhibitors activity is mediated through
|
their interaction with antithrombin (AT). Inactivate thrombin, 2,9, 10, 11, 12. Heparin increases lipoprotein lipase
|
|
Heparin (UHF)
|
a mixture of sulfated mucopolysaccharides, extracted from porcine gut or bovine lung
|
|
Clinical use of Heparin
|
use parenterally (IV,SC), do not use IM (risk of hematoma). Short half life, preferred for pregnant women
|
|
LMWH
|
enoxaparin dalteparin tinzaparin
|
|
clinical LMWH
|
inhibit Xa (less effect on thrombin), less frequent dosing and less side effects/tox, no routine monitoring of aPTT
|
|
monitoring heparin effect UFH level
|
close monitoring of the activated partial thromboplastin time (aPTT) or by protamine titration or anti Xa units
|
|
monitoring of heparin effect LMWH level
|
weight based dosing. aPTT measured only in obesity, pregnancy and renal insufficiency
|
|
Heparin toxicity
|
bleeding, HIT, allergy, hair loss/alopecia, osteoporosis/fracture (long term use)
|
|
Bleeding in Heparin
|
major adverse effect close monitoring needed, increase in elderly, female, and pt's with renal failure
|
|
HIT
|
heparin induced thrombocytopenia, an immunohematological disorder (hypercoagulation ) in pts treated with UFH for > than 7 days. Esp surgical pts. Venous thrombosis is the most common
|
|
if HIT noticed what should you do
|
discontinue use and use a direct thrombin inhibitor or fondaparinux
|
|
Cause of HIT
|
development of Abs against heparin/platelet factor 4 complex.
|
|
when is HIT suspicious
|
decreased platelet count, new thrombus, thrombocytopenia
|
|
reversal of heparin action
|
discontinue the drug and use an antagonist (protamine sulfate)
|
|
Heparin is contraindicated in
|
active bleeding, intracranial hemorrhage, advanced liver/kidney disease, severe hypertension, infective endocarditis, active tuberculosis…. Gi ulcer, hemophilia, purpura, threatened abortion, visceral carcinoma
|
|
Heparin is avoided in
|
post surgery of brain, spinal cord, eyes, pts undergoing LP, pregnant unless clearly indicated
|
|
Fondaparinux
|
long half life (sub Cu) effective in the prevention/treatment of venous thromboembolism, alternative anticoagulant in pts with HIT
|
|
direct thrombin inhibitors
|
hirudin, bivalirudin, lepirudin, argatroban, dabigatran
|
|
special about hirudin and bivalrudin
|
bivalent DTI's which also bind to the substrate recognition
|
|
how do direct thrombin inhibitors work
|
binding directly to the active site of thrombin
|
|
Hirudin
|
isolated from leech saliva, bivalent irreversible thrombin inhibitor
|
|
Lepirudin
|
a recombinant form of hirudin. Used in pts with HIT. Caution in pts with renal insufficiency
|
|
Bivalirudin
|
bivalent reversible thrombin inhibitor also inhibits platelet activation. IV, rapid on off action short half life
|
|
argatroban
|
used in pts with thrombosis and HIT. IV, short half life. Monitor aPTT, liver clearance (caution in liver disease). Increased international normalized ratios (INRs)
|
|
attributes of an ideal anticoagulant
|
oral, rapid onset, wide therapeutic range, predictable therapeutic effect, no food or drug-drug interactions
|
|
oral anticoagulants currently
|
Dabigatran, warfarin, rivaroxaban
|
|
dabigatran
|
oral prodrug, fast onset of action, assess renal function prior to prescription. Contraindicated in renal failure. No antidote. Reports of fatal bleeding
|
|
warfarin
|
vitamin K epoxide reductase. Blocks the gamma carboxylation of the glutamate residue in prothrombin 7, 9, 10 protein Cand S (8-12 hr delay in action)
|
|
warfarin special
|
racemix misture, potency S>>R, long half life, slow onset and slow offset
|
|
warfarin contraindications and adverse rxn
|
cross the placenta, hemorrhage in the fetus, serious birth defect( affect other fetal proteins in the bones and blood). Adverse reaction skin necrosis aka WISN, decrease protein C activity
|
|
warfarin clinical
|
oral, std dose 5-10 mg, adjustment of the prothrombin time (PT). Extrinsic pathway 1 week. PT should be increased. Therapeutic range is define by INR. Recommended INR for prophylaxis and treatment of thrombotic disease is 2-3
|
|
Reversal of warfarin action
|
stop the drug, admin vit K1, fresh frozen plasma, prothrombin cplx, rFIIa
|
|
factor Xa inhibitor
|
rivaroxaban
|
|
special for rivaroxaban
|
oral, fast onsel, liver metabolism (cyp3a4), no monitoring. Drug interaction with p450 inducers inhibitors
|
|
rivaroxaban antidote
|
factor Xa
|
|
Thrombolytic Drugs
|
streptoinase, anistreplase, urokinase, tPA, alteplase, reteplase, tenecteplase
|
|
streptokinase
|
bacterial protein, binds to activate plasminogen. Potential allergic rxn (no repeat use)
|
|
anistreplase
|
complex of human plasminogen and streptokinase
|
|
urokinase
|
human enzyme directly converts plasminogen to active plasmin
|
|
alteplase and reteplase
|
recombinant tissue plasminogen activators (tPA's, preferentially activate the fibrin bound plasminogen
|
|
tenecteplase
|
mutant tPA, longer half life
|
|
clinical uses of thrombolytic drugs
|
IV for pulmonary embolism, DVT and ascending thrombophlebitis. Management of acute MI
|
|
Recombinant t PA's are also used in
|
acute ischemic stroke
|
|
antiplatelet drugs
|
ADP receptor antagonists, thromboxane inhibitor, IIIa/Iib receptor antagonist
|
|
thromboxane inhibitor
|
aspirin
|
|
aspirin
|
irreversibly inhibits the synthesis of thromboxane A2, promary prophylaxis of MI 325 mg/d
|
|
antiplatelet drugs Adp receptor antagonists
|
clopidogrel and ticlopidine
|
|
MOA of antiplatelet drugs
|
inhibit the ADP receptor P2y12 on platelet, prevent thrombosis.
|
|
clopidogrel special
|
prodrug
|
|
adv rxn ticlopidine
|
GI tox, hemorrhage, TTP, neutropenia
|
|
clopidogrel adv rxn
|
less adverse effects, avoid concomitant use with PPI's ie omeprazole due to redued antiplatelet activity
|
|
antiplatelet drugs 3a/2b receptor antagonists
|
abciximab, eptifibatide, tirofiban
|
|
abciximab
|
chimeric mab against 2b/3a receptor, blocks activation of the Iib/3a receptor and vibronectin receptor
|
|
eptifibatide
|
analog of the delta chain of fibrinogen, blocks the binding of fibrinogen to the 2b/3a receptor
|
|
tirofiban
|
smaller molecule similar to eptifibatide
|
|
Factor 11 deficiency
|
hemophilia C, 2nd most common bleeding disorder among women
|
|
factor 7 deficiency
|
serum prothrombin converse accelerator. Diagnosed in newborns (bleeding into the brain as a result of traumatic delivery)
|
|
Agents used to facilitate clotting
|
vitamin k, antiplasmin drugs, clotting factors
|
|
vitamin K
|
fat soluble, found in leafy green veggies and synthesized by bacteria. Used to treat excessive warfarin or vitamin K deficiency
|
|
What is given to all newborns
|
Vitamin K1
|
|
fibrinolytic inhibitors
|
aminocaproic acid, aprotinin
|
|
aminocaproic acid
|
synthetic inhibitor of fibrinolysis. Competitivly inhibits plasminogen activation
|
|
administration of aminocaproic acid
|
loading dose when IV (>30 min to avoid hypertension)
|
|
adverse effects of aminocaproic acid
|
intravascular thrombosis, hypotension
|
|
aprotinin
|
serine protease inhibitor, inhibits figrinolysis by free plasmin, reduces bleeding from surgery.
|