Anticoagulants

Question 1

Argatroban given

Answer 1

IV

Question 2

Dabigatran given

Answer 2

orally

Question 3

Argatroban and dabigatron active on

Free thrombin?
fibrin bound thrombin?
Both?

Answer 3

Both

Question 4

Used for treatment and prophylaxis of HIT

Monitor with PTT

Answer 4

Argatroban

Question 5

Prodrug converted by esterases to active glucuronides. Not a P450 substrate (so less drug-drug interactions). Substrate for p-glycoprotein transport (rifampin decreases its levels). Caution in renal problems

Answer 5

Dabigatran

Question 6

Inhibits phosphodiesterase increasing cAMP.

Always used in combo, no effect if given alone

Answer 6

Dipyridamole

Question 7

Warfarin usually given in combo with __________ for prosthetic heart valves

Answer 7

dipyridamole

Question 8

Clopidogrel, ticlopidine, and cangelor are

Answer 8

P2Y12 receptor inhibitors

Question 9

Block ADP binding at P2Y12 receptors

Answer 9

Ticlopidine and clopidogrel

Question 10

Prodrugs. Metabolites are __________ inhibitors of P2Y12 receptor

Answer 10

Ticlopidine and clopidogrel

Irreversible

Question 11

Reversible inhibitor of P2Y12 given IV

Answer 11

Cangrelor

Question 12

Preferred. Better safety profile and shorter duration of action

Answer 12

Clopidogrel

Question 13

Peak action takes 5 days. Residual action for 72 hrs after stopped.
New plts have to be made to regain normal plt fn, which normally takes 7-14 days

Answer 13

Ticlopidine

Question 14

Increased risk of TTP and agranulocytosis with

Answer 14

ticlopidine

Question 15

Abciximab and eptifibatide are

Answer 15

Glycoprotein 3A/2B inhibitors

Question 16

Abciximab and eptifibatide are __________ inhibitors of gp 2B/3A

Competitive, noncompetitive?
Irreversible, reversible?

Answer 16

Competitive

Reversible

Question 17

Abciximab and eptifibatide inhibit

Answer 17

platelet crosslinking via fibrinogen

Question 18

Do not use if major surgery or trauma in past 6 weeks, or concurrently with warfarin

Answer 18

glycoprotein 2B/3A inhibitors

Question 19

alpha2-antiplasm binds _________ plasmin to inactive it

Answer 19

circulating

Question 20

Circulating plasmin > alpha2-antiplasmin

Answer 20

Lytic state

Question 21

Derived from beta-hemolytic strep. Binds 1:1 with plasminogen. Causes conformational change exposing catalytic site for conversion of 2nd plasminogen > plasmin

Answer 21

Streptokinase

Question 22

Acts on fibrin bound and circulating plasminogen. May cause lytic state

Answer 22

streptokinase

Question 23

Do not use if surgery/trauma in past 10 days. Or have had intracranial trauma

Answer 23

Streptokinase

Question 24

Streptokinase complexed with human lys-plasminogen. Active site blocked by acyl group, which is removed by plasma enzymes

Answer 24

Anistreplase

Question 25

More specific binding to thrombin

Answer 25

anistreplase

Question 26

Tissue type plasminogen activator. More selective for fibrin bound plasminogen, so less of a lytic state

Answer 26

Alteplase (rt-PA)

Question 27

Genetic derivative of alteplase

Answer 27

Tenecteplase

Question 28

Has longer t1/2, greater fibrin specificity, and slower inactivation by PAI-1.

Answer 28

Tenecteplase

Question 29

Inhibits plasminogen activation.

Answer 29

Aminocaproic Acid

Question 30

Lysine analog. Competes for lys binding site on plasminogen and plasmin

Answer 30

Aminocaproic Acid

Question 31

Argatroban and Dabigatran are

Answer 31

Direct thrombin inhibitors