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PHC 532- Exam 4 > Warfarin PK/PD > Flashcards

Warfarin PK/PD Flashcards

1
Q

Maintenance dose of warfarin

A

1.5-12 mg/day

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2
Q

Bioavailability of warfarin

A

> 90%

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3
Q

Tmax of warfarin

A

1-2 hours

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4
Q

Vd of warfarin

A

0.08-0.12 L/kg

aka SMALL Vd

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5
Q

Protein binding of warfarin

A

> 99%

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6
Q

Plasma concentration of warfarin

A

1.5-8 mmol/L

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7
Q

Which enantiomer has a longer half-life?

A

R-warfarin

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8
Q

Which enantiomer has a lower CL?

A

R-warfarin

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9
Q

Active form of warfarin

A

S-warfarin

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10
Q

Target-mediated drug disposition definition

A

Binding to the target influences the PK and disposition of the drug

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11
Q

PK characteristics of TMDD (6 things)

A 
Nonlinear Vd and CL
Steep distributive phase for low doses
Long terminal elimination
Dose proportional on MD
Time lag to Css with low dose IV infusion
Low doses=longer to get to Css
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12
Q

Warfarin is ? dependent.

A

CONCENTRATION

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13
Q

Is there saturable tissue binding with warfarin?

A

Yes

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14
Q

Is warfarin a low or high extraction drug

A

Low

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15
Q

S-warfarin is metabolized by what CYP enzyme?

A

2C9

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16
Q

R-warfarin is metabolized by what enzymes

A

1A1, 1A2, 2C19, 3A4, catechol-O-methyltransferase, ketoreductase

17
Q

Warfarin MoA

A

Inhibits the cyclic interconversion of vitamin K

18
Q

Warfarin’s indirect PD response

A

The peak response is delayed in relation to the concentration

19
Q

Clinical considerations of warfarin: Age

A

Increased age, decreased CL

20
Q

Clinical considerations of warfarin: genetic polymorphisms

A

CYP2C9 and VKORC1

21
Q

Clinical considerations of warfarin: body weight

A

Obese patients have decreased initial response

22
Q

Other clinical considerations of warfarin

A

Sex, DDIs, disease considerations, adherence, dietary intake of Vitamin K

23
Q

INR value for monitoring

A

2-3

24
Q

Pharmacogenetic testing for warfarin

A

Has either no or marginal usefulness in warfarin dosing

25
Q

Bayesian adaptive control of individual dosage regimens: components

A
  1. Population PK or PK/PD model
  2. Feedback measurements of drug concentrations and/or effects
  3. Patient characteristics for model covariate relationships
26
Q

MoA of Eliquis, Xarelto, edoxaban

A

Inhibit factor Xa

27
Q

MoA of dabigatran

A

Inhibits Factor IIa

PHC 532- Exam 4 (5 decks)

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