Dabigatran

Question 1

What is another name for dabigatran

Answer 1

Pradaxa

Question 2

how is dabigatran administered

Answer 2

orally, dose twice @ 110mg per day

Question 3

What is the mechanism of action for dabigatran

Answer 3

its a direct thrombin inhibitor

Question 4

How is dabigatran able to produce a predictable therapeutic effect

Answer 4

it does not bind to plasma proteins

Question 5

Explain the route of dabigatran in the body

Answer 5

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

Question 6

In what ways is dabigatran better than warfarin

Answer 6

it can decrease systemic embolism and stroke better

Question 7

Where is dabigatran mostly excreted

Answer 7

88% through renal clearance

Question 8

What patients is dabigatran a good preventive medicine for

Answer 8

patients with nonvalvular atrial fibrillation

Question 9

What are some other benefits of dabigatran

Answer 9

lower bleeding
decreases stroke incidence
lowers death rates

Question 10

Compared to warfarin what are some bad side effects

Answer 10

more indigestion known as dyspepsia

Question 11

How is diabigatran monitored

Answer 11

it really doesn’t need to be because it has more predictable anticoagulation response

Question 12

What is P glycoprotein

Answer 12

multidrug resistance protein- part of ABC transport family; re-transports the drug across cellular membrane

Question 13

What are some inhibitors of P-glycoprotein; how should you dose warfarin with these

Answer 13

ketoconazole
verapamil
amiodarone
quinidine
clarithromycin 

just keep warfarin at same dose

Question 14

In what cases is dabigatran contraindicated

Answer 14

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

Question 15

What is considered moderate renal impairment and what dose of dabigatran should be given

Answer 15

moderate is CrCl from 30-50 mL/min; and reduce the dose

Question 16

Compare the cost of warfarin to dabigatran

Answer 16

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

Question 17

Compared to warfarin what are five benefits of dabigatran and one down side

Answer 17

less bleeding 
less monitoring 
less toxic- wider therapeutic index 
less dietary restrictions 
less drug interactions 

BUT its still not as effective as warfarin

Question 18

What are the side effects of dabigatran

Answer 18

dyspepsia-indigestion
gastrointestinal bleeding
MI

Question 19

What are the disadvantages of dabigatran

Answer 19

1. twice daily dosing-nonadherence
2. still some bleeding for patients at risk
3. no antidote for it- nothing to stop activity
4. if a person has renal and hepatic impairment it will be a problem with it leaving body, esp renal