Pharm Sci Anti-coag

Question 0

Charge of UFH

Answer 0

Negatively

Question 1

UFH

Answer 1

From pig, glycosaminoglycan consisting of sulfated repeating disaccharide units

Question 2

MW of UFH

Answer 2

12,000 to 15,000

Question 3

What are the natural anticoagulants?

Answer 3

Protein C and S

Question 4

MOA of UFH

Answer 4

Binds anti-thrombin, undergoes a conformational change, it increases the infinity for thrombin, the complex which increases thrombin inhibition- means that it increases the inhibitory activity of anti thrombin

Also binds and I activates factor Xa- no tail involved

Question 5

MOA of LMWH

Answer 5

Pentasaccharide structure binds anti thrombin; has shorter tail so mainly inactivates factor Xa

Question 6

MOA of Fondaparinux

Answer 6

No tail so only inactivates Factor Xa

Question 7

Common denominator of UFH, LMWH, and Fonda?

Answer 7

All bind anti thrombin

Question 8

ADR of UFH

Answer 8

High risk of bleeding, hypersensitivity, HIT

Long term use: osteoporosis, fractures, decreased effectiveness of clotting

Question 9

ADR of LMWH

Answer 9

Bleeding, hematoma, lower risk of HIT than UFH avoid if have history of HIT

Question 10

ADR of Fondaparinux

Answer 10

Bleeding

Question 11

How are anti-coagulant effects mediated for UFH, LMWH, and Fondaparinux?

Answer 11

By binding through Anti-thrombin

Question 12

LMWH inactivate what better then what?

Answer 12

Inactivate factor 10a better than thrombin b/c of shorter tail

Question 13

Type 1 HIT

Answer 13

Presents 2 days after heparinuse, platelet count normalizes after continuous heparin use, no immune disorder

Question 14

HIT treatment

Answer 14

D/c all heparin therapy

Use: refiudam, argatroban, orgaran

Question 15

Type 2 HIT

Answer 15

Immune mediated disorder that occurs that occurs 4 to ten days after heparin exposure, life and limb threatening thrombotic complications, norm platelets decrease by fifty percent, skin lesions at injection site, marked by VTE

Question 16

Rivaroxaban

Answer 16

Direct factor Xa inhibitor
Po daily with largest meal of day no monitoring
Hepatic and renal elimination
Cyp3a4 metabolism to inactive metabolites
Pgp substrate

Question 17

Half life and peak effect time for rivaroxaban?

Answer 17

Half life 7-11 hrs

Peak effect 2-4 hrs

Question 18

Precautions for rivaroxaban

Answer 18

Risk of hematomas
Caution with renal or hepatic impairment
Anti platelets or NSAIDS increase bleeding
Rebound thromboembolic events
No antidote
Expensive

Question 19

Apixaban

Answer 19

Direct factor Xa selective, po bid, no monitoring, hepatic and renal elimination, cyp3a4 metabolism to inactive metabolites, pgp substrate
Expensive,

Question 20

Caution with Apixaban

Answer 20

Caution with Renal or hepatic impairment
Anti platelets and NSAIDs increase bleeding
Rebound thromboembolic events
No antidote
Expensive

Question 21

Edoxaban

Answer 21

Not yet approved
Direct Xa inhibitor
Oral
3a4 and pgp substrate renal component

Question 22

Dabigatran

Answer 22

Direct thrombin inhibitor
Doesn’t require anti thrombin to function
Selective
Inhibits both circulating and clot bound thrombin
Oral bid, no monitoring
Ester prodrug requiring ester hydrolysis for activation
80 percent elimin in urine
Undergoes glucuronidation

Question 23

Peak effect and half life of dabigatran

Answer 23

Peak 1-3 hrs

T half 9-15 hrs

Question 24

Caution with dabigatran

Answer 24

``` Increased risk hematomas Rebound thromboembolic events Anti platelets and NSAIDs increase risk bleeding Go intolerance dyspepsia No antidote Expensive ```

Question 25

What can help with the side effect of dyspepsia for dabigatran

Answer 25

Food, h2 blocker, ppi

Question 26

Aspirin

Answer 26

Cox inhib

Question 27

``` Ticlodipine Clopidegrel Prasugrel Oangrelor Ticagrelor ```

Answer 27

P2y12 antag

Question 28

SCH530348

Answer 28

Thrombin inhib | Competitive inhib of par1

Question 29

Abciximab Eptifbatide Tirofiban

Answer 29

GP11b/111a antag | Prevents fibrin binding

Question 30

MOA aspirin

Answer 30

Nonselective cox inhib Irreversibly acetylates ser res near active site Blocks arachadonic acid, pg syn, txa2 form, and platelet activation

Question 31

Peak effect of aspirin

Answer 31

1-3 hrs

Question 32

How long is life of platelet?

Answer 32

5-7 days

Question 33

Max effective doses of aspirin?

Answer 33

75-325 mg/day

Question 34

Dose of aspirin at 325 mg/day indicates what?

Answer 34

Resistance

Question 35

Acetaminophen

Answer 35

No anti platelet and no interference with aspirin

Question 36

Ibuprofen

Answer 36

Competitive inhib to cox No anti platelet activity Interferes with aspirin

Question 37

Give aspirin how long before ibuprofen?

Answer 37

2 hrs

Question 38

Give ibuprofen first, how long can give aspirin after?

Answer 38

8 hrs

Question 39

ADR aspirin

Answer 39

``` Bleeding Dyspepsia Erosive gastritis Peptic ulcers Hypersensitivity ```

Question 40

Interactions with aspirin

Answer 40

Other NSAIDs

Question 41

P2y12 antagonists

Answer 41

Prevent ADP binding increasing camp and pka activity No platelet activation Block g2b/3a receptors

Question 42

Ticlodipine

Answer 42

``` N/v/d Rash Prodrug Cyp2c19 inhibitor and metabolized by it Po bid Max inhibition 8-11 days ```

Question 43

Clopidogrel

Answer 43

85% inactive via esterases 15% active via cyp2c19 metabolism Take ppi Genetic testing rec

Question 44

Prasugrel

Answer 44

Prodrug Cyp3a4 and 286 to active form Inactive in intestines by esterases

Question 45

Black box warning for Ticlodipine

Answer 45

Neutropenia Thrombotic thrombocytopenia purpura Aplastic anemia

Question 46

Differences btwn clopidogrel and prasugrel

Answer 46

Larger onset and max effect for clopidogrel Shorter half life for clopidogrel Clopidogrel altered by 2c19 Clopidogrel has black box warning for poor metabolizers

Question 47

Ticagrelor

Answer 47

``` Reversible inhib of p2y12 Adenosine analog blocks adp binding Po bid - increas bleeding and sob Onset 2 hrs Half life 9 h- biliary elimination 3a4 and pgp substrate Metabolite and parent active ```

Question 48

Dipyridamole

Answer 48

Inhibit pde3 which increases camp and decreases calcium Also can block reputakei of adenosine Blocks platelets

Question 49

Dipyridamole plus aspirin

Answer 49

``` Weak anti platelet Po bid Half life 10 h Elimin as glucuronide in bile ADR- vasodilation and hypotension (gets better with use) ```

Question 50

Cilostazole

Answer 50

``` Po bid Reversible pde3 inhib Targets platelets and vsm Blocks adenosine Half life 10 h 3a4 metabolism Elimin in urine ```

Question 51

ADR of cilostazole

Answer 51

Ventricular arrhythmias Ha Hypotension

Question 52

G2b/3a receptor antag blocks what

Answer 52

Fibrinogen binding platelets

Question 53

Which G2b/3a antagonists are irreversible?

Answer 53

Abicimab

Question 54

Which G2b/3abare reversible?

Answer 54

Eprifibatide | Tirofiban

Question 55

ADR of G2b/3a antag

Answer 55

Bleeding | Thrombocytopenia

Question 56

Which G2b/3a antag are renally cleared

Answer 56

Epitifbatide | Tirofiban

Question 57

Thrombaxane inhib can also inhibit what?

Answer 57

Txa2 syn

Question 58

Par 1 inhibitors block?

Answer 58

Block thrombin mediated platelet activation