5.2 REVISED Important INFO from drug tables & Notes

Which are antiplatelet drugs?

1. Aspirin

2. Plavix (clopidogrel)

3. Effient (prasugrel)

4. Brilinta (ticagrelor)

5. Kengreal (cangrelor)

6. Integrilin (eptifibatde)

7. Aggrastat (tirofiban)

Which are the anticoagulant drugs?

1. Unfractionated heparin

2. Fragmin (dalteparin)

3. Lovenox (enoxaparin)

4. Arixtra (fondaparinux)

5. Argatroban

6. Angiomax (bivalirudin)

7. Coumadin (warfarin)

8. Eliquis (apixaban)

9. Pradaxa (dabigatran)

10. Savaysa (edoxaban)

11. Xarelto (rivaroxaban)

Which are the Fibrinolytic Drugs?

- Activase (alteplase)

- TNKase (tenecteplase)

Aspirin inhibits ____ to decrease production of thromboxane A₂.

COX-1

Aspirin is hydrolyzed to ____

salicylic acid

Aspirin's platelet inhibition lasts ____ to ____ days.

7; 10

Aspirin's inhibition of platelet function is ____.

irreversible

Aspirin does not require laboratory monitoring but should be monitored for signs of ____.

bleeding

Aspirin is indicated for the primary and secondary prevention of ____.

ACS

The most common adverse effect of aspirin is ____

GI bleeding.

_______ compete for the same spot as Aspirin and should be avoided post ACS

NSAIDs

If a patient NEEDS to take an NSAID take either with aspirin _______ prior to NSAID or take aspirin __________ after taking NSAID

- 60 minutes

- 8 hours

Clopidogrel prevents binding of ____ to the P2Y12 receptor.

ADP

Clopidogrel is a ____ that requires CYP activation.

prodrug

The primary CYP enzyme activating clopidogrel is ____.

CYP2C19

Clopidogrel requires a loading dose of ________ in the setting of ACS and maintenance dose of __________

300-600 mg PO

75 mg PO

Clopidogrel is used for ___________

ACS and secondary prevention of ACS.

Clopidogrel is preferred in patients allergic to ________.

aspirin

Prasugrel is a ____ that requires hepatic activation via CYP.

prodrug

Prasugrel is contraindicated in patients with a history of _________

stroke or TIA

Prasugrel's active metabolite is the same as clopidogrel but requires no ____ testing.

pharmacogenomic

Prasugrel in the setting of ACS requires a Loading dose of _________

60 mg PO

Prasugrel's maintenance dose depends on body weight and age

10 mg PO daily if body weight ≥ 60 kg and age < 75 years.

5 mg PO daily if body weight < 60 kg or age ≥ 75 years (use caution).

Ticagrelor is a ____ inhibitor of the P2Y12 receptor.

reversible

Ticagrelor and its metabolite are both ____.

active

Ticagrelor should be avoided with aspirin doses above ____

100 mg

Ticagrelor inhibits ____ reuptake into red blood cells.

adenosine

Ticagrelor can cause ____ as a side effect.

dyspnea

Ticagrelor can increase serum _____________

creatinine and uric acid levels.

Ticagrelor loading dose is ________, and maintenance dose is __________

180 mg PO daily

90 mg PO BID

Cangrelor is administered via the ____ route.

IV

Cangrelor platelet inhibition occurs ________.

only during the infusion

Cangrelor is indicated for _____________.

acute management of ACS

If a patient is on a P2Y12 inhibitor, and they are going to have a surgery, they should hod Ticagrelor for _______, Clopidogrel for ________, and Prasugrel for _______.

Tica: 5 days

Clopi: 7 days

Prasu: 9 days

Tirofiban and Eptifibatide prevent binding of fibrinogen to the _______

GPIIb/IIIa receptor

Eptifibatide is administered as ___________

an IV bolus followed by a continuous infusion

Eptifibatide requires dose reduction if CrCl is less than ____ mL/min.

50

Eptifibatide may cause ____ as an adverse effect.

thrombocytopenia

Tirofiban and Eptifibatide monitoring includes ___________.

aPTT, ACT, platelets, and SCr

Tirofiban is not a ____ (unlike eptifibatide).

peptide

Tirofiban requires dose reduction if CrCl is less than ____ mL/min.

60

Anti-Xa levels are only going to be required for special populations such as

1. Renal dysfunction

2. Pregnancy

3. Obesity

Which are the anticoagulants that require anti-Xa monitoring?

1. Unfractionated Heparin

2. Low Molecular Weight Heparins

3. Fondaparinux

4. Direct Oral Anticoagulants (DOACs)

Unfractionated heparin binds antithrombin III to inactivate ____

thrombin and Factor Xa.

Heparin absorption is ____ when given IV, and ____ when given SC

complete; unpredictable

Heparin is cleared by the _________, and is a saturable process. After is saturated is cleared by __________

reticuloendothelial system; renal system

Enoxaparin binds antithrombin III to inactivate ____.

Factor Xa

Low Molecular weigh heparins include:

1. Enoxaparin (Levonox)

2. Dalteparin (Fragmin)

Dalteparin binds antithrombin III to inactivate ______.

Factor Xa

Dalteparin is indicated for management of ACS and ____.

ACS and VTE

Arixtra (fondaparinux) binds ATIII and inhibits ____.

Factor Xa

Fondaparinux is contraindicated in patients with a CrCl< _________

30 ml/min

Fondaparinux should not be used as __________

monotherapy

Fondaparinux is less likely to cause ____ than heparin.

HIT

Fondaparinux is indicated for ________.

ACS and VTE

Fondaparinux is the most specific for inhibition of ____.

Factor Xa

Argatroban binds to _______ to inactivate it.

free and clot-bound thrombin

Argatroban is administered by the ____ route.

IV

Argatroban is excreted primarily via the ____ system, therefore needs dose adjustment in patients with ____________

biliary; hepatic impairment

Bivalirudin and Argatroban require monitoring of ________.

aPTT and activated clotting time

Which is the drug of choice when a patient develops HIT?

Argatroban

Bivalirudin (Angiomax) binds to ______ to inactivate it.

free and clot-bound thrombin

Bivalirudin is administered via the ____ route.

IV

Bivalirudin dose must be reduced in patients with ___________

renal impairment

Bivalirudin is indicated for _______.

ACS and HIT

Bivalirudin is used in patients with ______

high-bleeding risk

Warfarin inhibits synthesis of vitamin K-dependent clotting factors _____, and proteins ______.

- factors II, VII, IX, and X (2, 7, 9, 10)

- proteins C and S

Warfarin inhibits the enzyme ____.

VKORC1

Warfarin is absorbed ____ with complete bioavailability.

orally

Warfarin metabolism occurs via hepatic ____.

CYP2C9

Warfarin half-life ranges from ____ to ____ hours.

20; 60

Warfarin monitoring is performed using the ____.

INR

Warfarin is indicated for prevention and treatment of ____ and ____.

VTE; AF

The ___-isomer of warfarin is more than the ___-isomer.

S>R

Dabigatran inhibits free and clot-bound thrombin ____________

directly

Dabigatran is a ____ hydrolyzed to its active form.

prodrug

Dabigatran requires dose adjustment in __________

renal impairment

Dabigatran requires monitoring of ____.

SCr

Dabigatran is a substrate for ____.

P-glycoprotein

Dabigatran is indicated for prevention and treatment of ____ and ____.

VTE; AF

________ selectively inhibits free and clot-bound factor Xa, while _____and ____ selectively inhibit only FREE Factor Xa

- Apixaban (eliquis)

- Edoxaban (Savaysa)

- Rivaroxaban (Xarelto)

Apixaban is metabolized primarily by hepatic ____.

CYP3A4

Apixaban, edoxaban, and rivaroxaban monitoring require monitoring of ____.

SCr

Apixaban and Edoxaban are more commonly used for

AFib

Edoxaban shouldn't be used if CrCl ________

>95 ml/min

In patients with very efficient kidneys (high CrCl), edoxaban can be ____.

ineffective

Rivaroxaban bioavailability increases when ____.

taken with food (except for 10 mg dose)

Rivaroxaban is dosed once daily except when treating, where it is dosed ____ for the first 3 weeks.

acute DVT ; BID

Fibrinolytic drugs are used only for ____

ST-segment elevated MI (STEMI)

Fibrinolytic drugs are also used in management of ____, and all available drugs are ______

pulmonary embolism; IV

_________ is used for both STEMI & PE, while ____ is used only in STEMI

Alteplase (activase)

Tenecteplase (TNKase)

Fibrinolytics should not be used in ____.

NSTEMI

Alteplase & Tenecteplase convert plasminogen to ____ to lyse fibrin.

plasmin

Alteplase is given as a bolus dose followed by an ____.

infusion

Alteplase & Tenecteplase require monitoring of __________

aPTT and thrombin time

Tenecteplase is not indicated for treatment of ____.

PE