Term
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Definition
| bind to P2Y (12) ADP receptor on platelet surface, inhibiting platelet activation |
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Term
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Definition
| irriversible inhibits COX1 within platelet, blocking production of thromboxane A2 and platelet aggregation |
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Term
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Definition
| inhibit the enzyme VKOR; only affects synthesis of new factors |
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Term
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Definition
| reduces oxidized Vitamin K for reuse |
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Term
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Definition
| is coupled to carboxylation of inactive forms of factors VII, IX |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| following oral and rectal is nearly complete |
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Term
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Definition
| detectable in plasma within 1 hour, peak 2-8 hours, 98% protein bound |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| primarily hepatic, metabolites primarily excreted in urine |
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Term
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Definition
| decreased ability to metabolize S-warfarin (increasing risk of bleeding) |
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Term
| carried by 25% European Americans |
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Definition
| CYP2C9 variability (*2 and *3) |
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Term
| heterozygosity (*2 and *3 on CYP2C9) |
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Definition
| decrease dose requirement of 20-30% |
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Term
| homozygosity (*2 and *3 on CYP2C9) |
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Definition
| decrease dose requirement of 50-70% |
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Term
| "FAB 4" warfarin interactions |
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Definition
| fluconazole, amiodarone, bactrim, metronidazole |
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Term
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Definition
| warfarin causes discoloration on toes within 3-8 weeks, color fades with elevation of leg, thought to be due to cholesterol emboli |
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Term
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Definition
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Term
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Definition
| Oral Vitamin K preferred; FFP or prothrombin complex can be used |
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Term
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Definition
| faster but risk of anaphylaxis |
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Term
| direct thrombin inhibitors |
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Definition
| bind directly to and inhibit free and clot-bound thrombin (factor IIa), prevents conversion of fibrinogen to fibrin, and inhibits thrombin mediated platelet activation |
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Term
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Definition
| oral direct thrombin inhibitor, first FDA approved oral DTI for thromboprophylaxis and non-valvular AFib |
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Term
| dabigatran bioavailability |
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Definition
| poor (3-7%), food slows absorption but does not affect bioavail |
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Term
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Definition
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Term
| peak plasma concentration of dabigatran achieved |
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Definition
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Term
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Definition
| 50-70L and is 35% protein bound |
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Term
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Definition
| prodrug that is rapidly converted to active form by serine esterase |
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Term
| interactions with P-glycoprotein subrates |
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Definition
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Term
|
Definition
| 12-17 hours, excreted primarily unchanged in the urine |
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Term
| dose adjustments for dabigatran |
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Definition
| CrCl 30 (150 mg BID), CrCl 15-30 (75 mg BID), CrCl of 30-50 with use of dronedarone or systemic ketoconazole (75 mg BID) |
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Term
| converting warfarin to dabigatran |
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Definition
| discontinue warf and start when INR is <2 |
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Term
|
Definition
| provides qalitative estimate of antocoagulant effect |
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Term
| monitoring for dabigatran |
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Definition
| monitor renal function and S/Sx of bleeding |
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Term
| adverse affects of dabigatran |
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Definition
| bleeding, dyspepsia reported in pre-marketing studies |
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Term
|
Definition
| discontinue drug, supportive care (blood products), 60% removed by dialysis |
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Term
|
Definition
| directly inhibits Xa preventing the conversion of II to IIa |
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Term
| factor X activated by intrinsic and extrinsic pathways |
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Definition
| activating factor Xa which converts II to IIa and promotes the clotting cascade |
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Term
| bioavalability of rivaroxiban |
|
Definition
| 66-100%, dose dependent decreases with larger doses, food increases availability of 20 mg doses |
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Term
|
Definition
| 50L, 92-95% protein bound to albumin |
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Term
| metabolism of rivaroxaban |
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Definition
| primarily hepatic via CYP3A4/5 and 2J2, also a p-glycoprotein substrate, inactive metabolites excreted in urine |
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Term
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Definition
| VTE prophylaxis (post-op), VTE treatment and secondary prophylaxis, non-valvular AFib |
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Term
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Definition
| renal function, S/Sx of bleeding, may increase INR but is not definitive test |
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Term
|
Definition
| abrupt discontinuation may increase risk of thrombolic events, risk of spinal/ epidural hematoma in PTs receiving neuraxial anesthesia or spinal puncture |
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Term
| rivaroxaban and hepatic impairment |
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Definition
| child-pugh class B and C associated with increased risk of coagulopathy |
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Term
|
Definition
| strong CYP3A4 and P glycoprotein inducers should be avoided |
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Term
|
Definition
| no specific or reliable reversal agent; discontinue drug, supportive care, activated charcoal may be used and Prothrombin Complex Concentrates may be an option |
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Term
| bioavailability of apixaban ADME |
|
Definition
| 50%, food slows absorption, but no affect on Cmax or AUC |
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Term
|
Definition
| 21-61L with 87% protein binding and also P-glycoprotein binding |
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Term
|
Definition
| primarily hepatic via CYP3A4, excretion primarily fecal with 7-12 hour half-life |
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Term
| apixaban dose adjustment to 2.5 mg PO BID |
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Definition
| with concomitant use of strong CYP3A4 and P-glycoprotein substrates, age >80 yr, weight < 60kg and SCr >1.5 |
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Term
|
Definition
|
|
Term
|
Definition
| abrupt discontinuation increases risk of thrombotic events |
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Term
|
Definition
|
|
Term
|
Definition
| 50L, 92-95% protein bound to albumin |
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|
Term
| metabolism of rivaroxaban |
|
Definition
| primarily hepatic via CYP3A4/5 and 2J2, also a p-glycoprotein substrate, inactive metabolites excreted in urine |
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Term
|
Definition
| VTE prophylaxis (post-op), VTE treatment and secondary prophylaxis, non-valvular AFib |
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|
Term
|
Definition
| renal function, S/Sx of bleeding, may increase INR but is not definitive test |
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Term
|
Definition
| abrupt discontinuation may increase risk of thrombolic events, risk of spinal/ epidural hematoma in PTs receiving neuraxial anesthesia or spinal puncture |
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Term
| rivaroxaban and hepatic impairment |
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Definition
| child-pugh class B and C associated with increased risk of coagulopathy |
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Term
|
Definition
| strong CYP3A4 and P glycoprotein inducers should be avoided |
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|
Term
|
Definition
| no specific or reliable reversal agent; discontinue drug, supportive care, activated charcoal may be used and Prothrombin Complex Concentrates may be an option |
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Term
| bioavailability of apixaban ADME |
|
Definition
| 50%, food slows absorption, but no affect on Cmax or AUC |
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Term
|
Definition
| 21-61L with 87% protein binding and also P-glycoprotein binding |
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Term
|
Definition
| primarily hepatic via CYP3A4, excretion primarily fecal with 7-12 hour half-life |
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|
Term
| apixaban dose adjustment to 2.5 mg PO BID |
|
Definition
| with concomitant use of strong CYP3A4 and P-glycoprotein substrates, age >80 yr, weight < 60kg and SCr >1.5 |
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Term
|
Definition
|
|
Term
|
Definition
| abrupt discontinuation increases risk of thrombotic events |
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Term
|
Definition
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