thromboembolic drugs. Flashcards
TPA drugs
Alteplase
reteplase
tenecteplase
Plase suffix
Tissue plasminogen activators
Urokinase
a urokinase type plasminogen activator that is a fibrinolytic drug
Steptokinase
a Fibrinolytic thrombolytic drug that is from streptokinase preparations.
LMW heparin
has to be given subcutaneously
indirect inhibitor
binds to antithrombin III and inactivated Factor X
partially inactivates thrombin because it doesn’t bind it.
HMW heparin
binds to antithrombin III as well as factor X and Thrombin.
Indirect inhibitor of clot formation
also called unfractionated heparin.
Can cause HIT (heparin induced thrombocytopenia)
fondaparinux
A indirect inhibitor that is smaller than LMW heparin
Binds only to Antithrombin III and will inactivate factor X
rarely induces HIT
Not reversed by protamine sulfate
Used in DVT and PE
also used in conjunction with Warfarin.
a synthetic pentasaccharide
How to monitor heparins
aPTT -> monitors intrinsic and common pathway
HIT
Heparin induced thrombocytopenia
causes by immunogenicity of the complex of heparin with the platelet factor 4 (PF4)
leads to a hyper coagulable state
often have venous and arterial thrombosis
treat by giving a direct thrombolitic inhibitor
how to reverse heparin
protamine sulfate
Heparin sodium
HMW heparin
Enocaparin
LMW heparin
Tinzaparin
LMW heparin
Dalteparin
LMW heparin
Direct thrombin inhibitors (parenteral)
Lepirudin
Bivalirudin
Argatorban
Lepirudin
A direct thrombin inhibitor that is given parenterally
will cause irreversible inhibition of thrombin
repeated use can cause a anaphylactic reaction.
Bivalirudin
a direct thrombin inhibitor that is given parenterally
Reversibally inhibits thrombin
also causes platelet aggregation
Agatroban
A direct thrombin inhibitor that is given parenterally
Short acting drug
A small molecular weight inhibitor
Use of DTI
(direct thrombolytic inhibitor)
used in HIT and coronary angioplasty
Warfarin
oral anticoagulant
Inhibits vitamin K epoxide reductase which presents Vit. K’s reduction. This prevents the carboxylation of the decarboxyled-prothrombin into prothrombin by inhibiting GGCX enzyme that needs reduced Vit. K.
also effect factors X, IX, VII, II
difficult to dose
we use INR to measure effectiveness. we want level of 2-3. (normal .9-1.3) (.5 = high change of thrombosis) (4.0-5 = high change of bleeding)
S isomer more potent that R isomer
metabolized by liver
99% bound to albumin
used in thromboembolism prevention, A. fib, and prosthetic heart valves
important to know that warren is teratogenic
Rivaroxaban
a NOAC factor Xa inhibitor given at fixed doses orally and doesn't need monitoring Rapid onset (unlike warfarin) No antidote
monitored by Anti-Xa (common pathway)
Apixaban
a NOAC factor Xa inhibitor given at fixed doses orally and doesn't need monitoring Rapid onset (unlike warfarin) No antidote
monitored by Anti-Xa (common pathway)
Enoxaban
a NOAC factor Xa inhibitor given at fixed doses orally and doesn't need monitoring Rapid onset (unlike warfarin) No antidote
monitored by Anti-Xa (common pathway)
Dabigatran
NOAC direct thrombin inhibitor
used to reduce risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and DVT.
Antidote = idarucizumab
monitored by diluted thrombin time (TT) (common pathway)
Idarucizumab
A NOAC Direct thrombin inhibitor antidote for dabigatran
aspirin
inhibits COX and causes decrease TxA2 which leads to uncreased coagulability.
protamine sulfate
reverses HMW heparin and LMW heparin
Vitamin K treatment
Reverses the effects of Warfarin
clopidogrel
ADP receptor blocker
Inhibits AC by alpha I -> leads to increased production of cAMP
metabolized by CYP 2C19 -> not functional in 50% of chinese, 34% african, 25% caucasians and 19% mexicans.
used in Prevention of thrombosis in patients with ACS and recent AMI, stroke and peripheral arterial disease
Prasugrel
ADP receptor blocker
Inhibits AC by alpha I -> leads to increased production of cAMP
metabolized by CYP 2C19 -> not functional in 50% of chinese, 34% african, 25% caucasians and 19% mexicans.
used in Prevention of thrombosis in patients with ACS and recent AMI, stroke and peripheral arterial disease
Ticlopidine
ADP receptor blocker
Inhibits AC by alpha I -> leads to increased production of cAMP
metabolized by CYP 2C19 -> not functional in 50% of chinese, 34% african, 25% caucasians and 19% mexicans.
used in Thrombosis prevention in stroke patients
Ticagrelor
ADP receptor blocker
Inhibits AC by alpha I -> leads to increased production of cAMP
metabolized by CYP 2C19 -> not functional in 50% of chinese, 34% african, 25% caucasians and 19% mexicans.
used in Prevention of thrombosis in patients with ACS and recent AMI, stroke and peripheral arterial disease
Abciximab
Platelet glycoprotein receptor antagonist
used as a anti-platelet drug
prevents the binding of a ligand which causes the formation of platelets
used in unstable angina and other acute coronary syndromes
Given IV because of short half life.
can cause hypotension, myalgia, and thrombocytopenia
Eptifibatide
Platelet glycoprotein receptor antagonist
used as a anti-platelet drug
prevents the binding of a ligand which causes the formation of platelets
used in unstable angina and other acute coronary syndromes
Given IV because of short half life.
can cause hypotension, myalgia
tirofiban
Platelet glycoprotein receptor antagonist
used as a anti-platelet drug
prevents the binding of a ligand which causes the formation of platelets
used in unstable angina and other acute coronary syndromes
Given IV because of short half life.
can cause hypotension, myalgia, and thrombocytopenia
