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76 Cards in this Set

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Antiplatelet agents?
Thienopyridine Agents
Glycoprotein IIb/IIIa Inhbitors
Aspirin MoA?
Irreversible inhibition of platelet cyclooxygenase-1 -> Blocking of the formation of TxA2 from arachidonic acid -> decreased platelet aggregation
Astra is a Cock Blocker, Forming from Archaic Autistic Texans
Lifespan of platelets?
7 days
PKs of Aspirin
Rapid absorption in stomach and upper intestine; platelet inhibition after 1 hr of ingestion which takes effect for lifespan of platelet
Main thienopyridine?
Theo Clops along with the Dog
Clopidogrel MoA?
irreversible inhibition of ADP pathway receptor antagonist to inhibit platelet aggregation
Chloe Angrily Decides Peter Must Be Stopped
Clopidogrel has no sig effect on the synthesis of what two products?
TxA2 & prostacyclin
Texas Protons
Dipyridamole MoA?
Vasodilatior that inhibits platelet function by inhibiting adenosine uptake and cGMP phosphodiesterase activity which is reversible
The Pyramids Were Slow TO Build for Queen Esther
Dipyridamole bioavail: low or high?
Dipyridamole clinical use:
Used with aspirin to prevent cerebrovascular ischemia (Aggrenox)

Ltd to no effect mono
AEs of dipyridamole?
Headache and bleeding not a/w dypyridamole alone
Primary Glycoprotein IIb/IIIa inhibitor?
I Glide My Finger over the Axim
Abciximab (Glycoprotein IIb/IIIa inhibitor) MoA?
inhibits formation of platelet thrombi by inhibiting activated receptors from binding with fibrinogen and forming bridges between activated platelets
Andy Stops Bitches from Getting over Fiborous Bridges
AEs of Abciximab (Glycoprotein IIb/IIIa inhibitors)?
thrombocytopenia (low platelet count)


hypersensity rxn with 2nd dose
Abciximab is what kind of molecule?
Antibody which destroys platelets via antibody action
Anticoag agts?
Unfractioned heparin
Low molecular weight heparin
Direct thrombin inhibitors
suffix for all LMWHs?
-parin or -parinux
Coag cascade purpose?
formation of clots to stop bleeding
Unfractioned Heparin MoA?
Binds to antithrombin III (ATIII) -> enhanced activity

ATIII binds to factors
What clotting factors does ATIII bind to and inhibit?
IIa (PT), IXa, Xa, XIa, & XIIa
Which pathway does ATIII inhibit?
What does UH not affect?
formed thrombi which were present prior to UH therapy which are cleared by physiologic thrombolytic mechanisms and it has no fibrinolytic activity
Ursula Fibs and Lies
What kind of mix is UH and what is the compound?
It's heterogenous mix of complex mucopolysaccharides
Ursula is snotty
What portion of heparin molecules are pharmacologically active?
Approx 1/3rd
What does UH bind together, what is the complex called, and what happens after they bind?
It binds ATIII with clotting enzyme; forms a ternary complex formation; it then dissociates and starts again
What is the change UH induces in the ternary complex called?
Conformational change
What are direct thrombin inhibitors not?
clot busters
What are the 2 routes for UH?
SQ or IV
Half-life of UH?
1-2 hrs in healthy adults
Metabolism of UH?
hepatic heparinases (still slightly renal)
What happens to UH 1/2 life in renally impaired pts?
It's slightly prolonged; not diazyble
How is UH given?
First bolus, then maintainence dosing
What is UH dosage based on?
What is monitored after UH admin?
activated partial thromboplastin time (aPTT)
What is aPTT sensitive to?
Inhibitory effects of heparin on thrombin, factor Xa & XIa
What do you maintain aPTT after bolus?
1.5x-2.5x reference
AEs of UH?
Bleeding (increases w/ dose and duration)

Low platelet count
Cx of UH?
How does Low Molecular Weight Heparin (LMWH) differ from UH?
It's homogenous, has superior PK profile, doesn't need lab monitoring, and has decreased anti IIa activity relative to anti-Xa activity (more selective for Xa)
What is the mean mol weight of LMWH?
4000-5000 daltons
How does the ATIII binding action differ in UH versus LMWH?
LMWH ATIII binds much less to thrombin relative to factor Xa
Why are LMWH agts not interchangable?
Due to different PK and different ratios of Anti-Xa:IIa action.
What is the preferred LMWH agt? what is its Anti-Xa:IIa activity?
enoxaparin; 3.8:1
General PKs of LMWH?
SQ admin almost 100 percent bioavail

Peak effects occur 3-5 hours after admin

Renal dose adjustment required
AEs of LMWH?
Low platelet count

Injection site rxn(thrombocytophlebitis)
What reverses heparin action?
How does Protamine reverse heparin action?
Forms a stable, inactive complex by ionically binding w/ heparin
What 2 factors are involved in the efficacy of protamine reversal of heparin?
Dosage (should be 1 mg protamine:~100 units of heparin)

Less effective with LMWH
PKs of protamine?
Onset within 5 minutes; duration is 2 hours
AEs of protamine?

Heparin rebound (antithrombin activity of heparin returns even with effective dose)
Direct thrombin inhibitor agts and MoA?
Lepirudin, bivalirudin, & agratroban; block either the active site or both active site and exocite I
How do DTIs bind to thrombin?
inhibit free and clot-bound thrombin w/o requiring endogenous cofactors
Half life of DTIs?
25-60 mins (short)
-rudins PKs?
majority excreted renally
-rudins dosage considerations?
insufficient renal function
Agratroban PKs and doseage considerations?
Hepat metab; hepatic insuffiency
Unique AE of lepirudin?
antibody formation
Drawback of DTIs?
no reversal agt
Warfarin MoA?
inhibits vitamin K dependent clotting factor synthesis
What are the vitamin K dependent clotting factors and regulatory proteins?
Factors II, VII, IX, & X

protein C & S
What doesn't warfarin do?
dissolve the current clot
Which pathways does warfarin operate on?
Extrinsic (factors VII& X) and common (prothrombin (II))
Warfarin PKs?
100 % absorption

Hepatic metabolism through 3A4 & 2C9

Long 1/2 life
99 % protein binding
Warfarin monitoring?
Internation Normalized Ratio (INR) which is pts PTT over normal PTT raised to the power of the ISI value (1-1.4)
When initiating warfarin, what should it over lap with and for how long?
It should overlap w/ heparin for about 4 days until INR is therapeutic for 2 days
Warfarin dosing?
Highly individualized (PKs [particularly 2C9 & 3A4 inx] and PDs)
What population should never be given warfarin and why?
Pregnant women. It's preg cat X.
D-D interactions of warfarin that decrease coag?
Additive anticoag effect w/ APAP

EtOH acute ingestion -> increased INR -> inhibition (increased bleed)

Antimicrobials (fluoroquinolones) -> greater anticoag
D-D interactions of warfarin that increase coag?
EtOH chronic ingestion -> increased INR -> induction (decreased bleed)

Carbamazapine is 3A4 inducer -> need much higher warfarin
Pharmacodynamic interactions with warfarin?
anti-thyriod meds -> reduced thryoid function -> reduced warfarin effect
Reversal of warfarin is through what?
Vitamin K
MoA of Vit K reversal of warfarin?
factor II, VII, IX, & X dependent upon Vitamin K
Vitamin K route?
All 4.
Best routes of Vitamin K?
PO (absorbed in duodenum)
SQ (readily absorbed)
IV (fastest onset)
Vitamin K onset of action?
PO: 6-12 h
Parenteral: 1-2 h
Vitamin K AE?
Hypersensitivity w/ IV & IM route (rash, sometimes lethal), especially if admin is rapid