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FIU - Thrombolytic agents
Thrombolytic agents
30
Pharmacology
Professional
01/05/2012

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Term
Intrinsic coagulation pathway: initiated by? Slower or faster pathway? clotting factors involved? Test for the pathway? Drug that inhibits clotting?
Definition
Contact (endothelial damage/inside cut); slower/longer path; XII -> XI -> IX -> VIII -> X/II (common pathway); aPTT (activated partial thromboplastin time) test; heparin (fast acting)
Term
Extrinsic coagulation pathway: initiated by? Slower or faster pathway? clotting factors involved? Test for the pathway? Drug that inhibits clotting?
Definition
Trauma (outside the cut in plasma/vitamin K-liver dependent); faster/shorter path; tissue factor (III) -> VII -> X/II (common pathway); INR (International Normalized Ratio) test; warfarin (slow acting: preformed factors)
Term
warfarin mode of action; derivative of?
Definition
inhibits vitamin K epoxide reductase, which recycles oxidized vitamin K that has assisted carboxylation of pro-coagulation factors II, VII, IX and X AND anti-coagulation factors C and S; coumarin derivative
Term
warfarin sensitive factors?
Definition
pro-coagulation: II, VII, IX, X; anti-coagulation: Protein C and S
Term
warfarin mode of action, use, deliverery, test; pharmocogenomics?
Definition
inhibits production of clotting factors 2, 7, 9, 10 and anti-clotting proteins C and S; used for anti-coagulation (esp. extrinsic pathway); oral; INR (0.8 to 1.2 normal); VKORC1 (vitamin K epoxide reductase complex subunit 1 polymorphisms: African Americans more resistant/Asian Americans more sensitive (more bleeding), also different 2C9 phenotypes: fast (more clotting) and slow (more bleeding) metabolizers.
Term
Warfarin CPY450 metabolizer? inducers? inhibitors?
Definition
C29; inducers: Phenobarbitol, rifampin; inhibitor: amiodarone, fluoxetine, fluvastatin, zafirlukast
Term
Effects on warfarin of fibrates (why?), of high vitamin K foods, of antibiotics?
Definition
fibrates increase INR (higher INR = less clotting) because fibrates bind plasma proteins, freeing warfarin; foods decrease INR replacing unrecycled vitamin K; antibiotics increase INR, kills vitamin K producing bacteria, further decreasing available vitamin K.
Term
Warfarin antagonist (antidote)?
Definition
Vitamin K (delayed effect), FFP (fresh frozen plasma)
Term
Warfarin side effects? Why not aspirin for DVT?
Definition
necrosis from clots (if anti-clot proteins C & S are more sensitive to warfarin than clotting factors. Give heparin), osteoporosis, purple toe syndrome, FDA category X (not for use during pregnancy); aspirin inhibits platelet aggregation in arteries but veins are platelet poor.
Term
Heparain mode of action, use, delivery, test; found where endogenously? endogenous antagonist?
Definition
pentasacharide portion increases ATIII (antithrombin III) activation which inhibits factor X, 18 unit oligosacharide inhibits factor II (thrombin); used for anti-coagulation (esp intrinsic pathway); subcutaneous or IV; aPTT for high molecular weight version only;acid substance complexed with histamine in basophils; platelet factor IV (PF IV) - can't antagonize exogenous heparin
Term
Low molecular weight (LMW) heparin mode of action, test, advantages vs. high molecular weight (HMW) heparin? Disadvantages?
Definition
clean ATIII activators (factor X inhibitors); no aPTT (only can monitor factor X activity); adv: longer t1/2, more predictable response (factor X inhibition without factor II inhibition), outpatient; disadv: expensive, no reliable antagonist
Term
Heparain onset? with pregnancy? antagonist? side effects?
Definition
immediate onset (unlike warfarin); OK with pregnancy; protamine; Heparin-induced thrombocytopenia, osteoporosis (like warfarin)
Term
Protamine mode of action? side effect? use by itself?
Definition
heparain antagonist (pro-coagulant); vasodilation and lowered blood pressure; by itself is an anti-coagulant
Term
Hirudin mode of action, use, origin?
Definition
direct thrombin (factor II) inhibitor that stops fibrin formation from fibrinogen; anti-coagulation; leech buccal glands
Term
-rudin mode of action, use, advantage over heparin, examples
Definition
direct thrombin inhibitors (IV delivery); anti-coagulation; no ATIII activator and so no HIT (heparin-induced thrombocytopenia: occurs when antibodies to PF4/heparin complex form, activating platelets and leading thrombosis and lowered platelet count)
Term
lepirudin, desirudinm, and bivalirudin mode of action, use
Definition
direct thrombin inhibitors, anti-coagulation with out HIT
Term
argatroban mode of action, use, advantage over other similar drugs?
Definition
direct thrombin inhibitor, anti-coagulation, reversible
Term
-gatran mode of action, use, examples
Definition
direct thrombin inhibitor (oral delivery); anti-coagulation; ximelagatran (off market) and dabigatran
Term
-xabans mode of action, use, examples?
Definition
direct factor X inhibitors (oral delivery); anti-coagulation; apixaban and rivaroxaban
Term
Activation of which platelet receptors promote platelet aggregation? All of these activated receptors activate what receptor?
Definition
Thrombin, 5-HT (serotonin), epinephrine, ADP, PAF (Platelet activating factor), TXA2 (thromboxane A2); activate IIb/IIIa receptors that bind fibrinogin (factor I), which other platelets bind to as well causing aggregation.
Term
Activation of which platelet receptors inhibit platelet aggregation? All of these activated receptors deactivate what receptor?
Definition
cAMP/cGMP, adenosine (opposite of ADP), PGI2 (prostacyclin, opposite of TXA2), NO/EDRF (endothelial-derived relaxing factor, two terms often used interchangeably); deactivate IIb/IIIa receptors
Term
Asprin mode of action (with regard to platelets), use, dosage?
Definition
irreversible COX I inhibitor (thru acetylation) that stops production of PG, PCyclin & TX from arachidonic acid; because platelets mostly produce TX from COX-1 (which increases platelet aggregation), inhibition = anti-coagulation; works in LOW doses more selectively on platelet COX-1 than endothelial COX-1;
Term
thienopyridine mode of action, use
Definition
P2Y12/ADP receptor blocker; decreases platelet aggregation
Term
ticlopidine mode of action, use, indication?
Definition
P2Y12/ADP receptor blocker; decreases platelet aggregation; use when ASA is contra-indicated
Term
Clopidogrel, mode of action, use, indication, brand name, similar drug?
Definition
prodrug P2Y12/ADP receptor blocker (only 15% become active metabolites, rest degraded by esterases); decreases platelet aggregation; use when ASA is contra-indicated; Plavix; prasugrel
Term
Dipyridamole mode of action, use?
Definition
Platelet PDE-Inhibitor that stops adenosine reuptake, increasing adenosine; decreases platelet aggregation...There are also direct IIb/IIIa receptor inhibitors
Term
Anti-coagulants that can be used after thrombus is formed? coadminster with?
Definition
plasminogen activators (which break down fibrin/factor I); co-administer with a platelet aggregation inhibitor (because fibrin metabolites activate thrombin/factor II)
Term
streptokinase mode of action, use, advantage, disadvantage
Definition
plasminogen activator (also degrades factors V and VII (extrinsic path); thrombus breakdown; adv: cheap; disadv: binds with complexed and uncomplexed, plasma fibrin
Term
alteplase mode of action, use, advantage, disadvantage
Definition
plasminogen activator; thromus breakdown; adv: activates only plasminogen bound to fibrin (clot specificity) so fewer side effects; disadv: expensive
Term
Aminocaproic acid
Definition
antidote for overdose of a plasminogen activator
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