Dabigatran Flashcards
What is another name for dabigatran
Pradaxa
how is dabigatran administered
orally, dose twice @ 110mg per day
What is the mechanism of action for dabigatran
its a direct thrombin inhibitor
How is dabigatran able to produce a predictable therapeutic effect
it does not bind to plasma proteins
Explain the route of dabigatran in the body
First dabigatra etexilate mesylate is given orally
Next, because it is an ester it is hydrolyzed to form dabigatran (the active moiety)
Third, it is metabolized into four different acyl glucuronides
Both the acyl glucuronides and the active drug have same pharmacological activity
Double prodrug
In what ways is dabigatran better than warfarin
it can decrease systemic embolism and stroke better
Where is dabigatran mostly excreted
88% through renal clearance
What patients is dabigatran a good preventive medicine for
patients with nonvalvular atrial fibrillation
What are some other benefits of dabigatran
lower bleeding
decreases stroke incidence
lowers death rates
Compared to warfarin what are some bad side effects
more indigestion known as dyspepsia
How is diabigatran monitored
it really doesn’t need to be because it has more predictable anticoagulation response
What is P glycoprotein
multidrug resistance protein- part of ABC transport family; re-transports the drug across cellular membrane
What are some inhibitors of P-glycoprotein; how should you dose warfarin with these
ketoconazole verapamil amiodarone quinidine clarithromycin
just keep warfarin at same dose
In what cases is dabigatran contraindicated
if you can remember what we talked about before dabigatran is removed mostly by the kidneys therefore if the person has renal impairment
which is CrCl< 30mL/min then don’t give it
What is considered moderate renal impairment and what dose of dabigatran should be given
moderate is CrCl from 30-50 mL/min; and reduce the dose
Compare the cost of warfarin to dabigatran
well warfarin is cheaper because its only $2.5/day but you have to add up INR monitoring cost which makes it more expensive than dabigatran $6.75/day
Compared to warfarin what are five benefits of dabigatran and one down side
less bleeding less monitoring less toxic- wider therapeutic index less dietary restrictions less drug interactions
BUT its still not as effective as warfarin
What are the side effects of dabigatran
dyspepsia-indigestion
gastrointestinal bleeding
MI
What are the disadvantages of dabigatran
- twice daily dosing-nonadherence
- still some bleeding for patients at risk
- no antidote for it- nothing to stop activity
- if a person has renal and hepatic impairment it will be a problem with it leaving body, esp renal
