Pharm Sci Anti-coag Flashcards

0
Q

Charge of UFH

A

Negatively

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1
Q

UFH

A

From pig, glycosaminoglycan consisting of sulfated repeating disaccharide units

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2
Q

MW of UFH

A

12,000 to 15,000

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3
Q

What are the natural anticoagulants?

A

Protein C and S

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4
Q

MOA of UFH

A

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

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5
Q

MOA of LMWH

A

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

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6
Q

MOA of Fondaparinux

A

No tail so only inactivates Factor Xa

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7
Q

Common denominator of UFH, LMWH, and Fonda?

A

All bind anti thrombin

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8
Q

ADR of UFH

A

High risk of bleeding, hypersensitivity, HIT

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

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9
Q

ADR of LMWH

A

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

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10
Q

ADR of Fondaparinux

A

Bleeding

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11
Q

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

A

By binding through Anti-thrombin

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12
Q

LMWH inactivate what better then what?

A

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

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13
Q

Type 1 HIT

A

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

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14
Q

HIT treatment

A

D/c all heparin therapy

Use: refiudam, argatroban, orgaran

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15
Q

Type 2 HIT

A

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

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16
Q

Rivaroxaban

A

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

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17
Q

Half life and peak effect time for rivaroxaban?

A

Half life 7-11 hrs

Peak effect 2-4 hrs

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18
Q

Precautions for rivaroxaban

A

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

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19
Q

Apixaban

A

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

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20
Q

Caution with Apixaban

A

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

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21
Q

Edoxaban

A

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

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22
Q

Dabigatran

A

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

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23
Q

Peak effect and half life of dabigatran

A

Peak 1-3 hrs

T half 9-15 hrs

24
Q

Caution with dabigatran

A
Increased risk hematomas 
Rebound thromboembolic events 
Anti platelets and NSAIDs increase risk bleeding 
Go intolerance dyspepsia 
No antidote 
Expensive
25
Q

What can help with the side effect of dyspepsia for dabigatran

A

Food, h2 blocker, ppi

26
Q

Aspirin

A

Cox inhib

27
Q
Ticlodipine 
Clopidegrel
Prasugrel
Oangrelor
Ticagrelor
A

P2y12 antag

28
Q

SCH530348

A

Thrombin inhib

Competitive inhib of par1

29
Q

Abciximab
Eptifbatide
Tirofiban

A

GP11b/111a antag

Prevents fibrin binding

30
Q

MOA aspirin

A

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

31
Q

Peak effect of aspirin

A

1-3 hrs

32
Q

How long is life of platelet?

A

5-7 days

33
Q

Max effective doses of aspirin?

A

75-325 mg/day

34
Q

Dose of aspirin at 325 mg/day indicates what?

A

Resistance

35
Q

Acetaminophen

A

No anti platelet and no interference with aspirin

36
Q

Ibuprofen

A

Competitive inhib to cox
No anti platelet activity
Interferes with aspirin

37
Q

Give aspirin how long before ibuprofen?

A

2 hrs

38
Q

Give ibuprofen first, how long can give aspirin after?

A

8 hrs

39
Q

ADR aspirin

A
Bleeding 
Dyspepsia 
Erosive gastritis 
Peptic ulcers 
Hypersensitivity
40
Q

Interactions with aspirin

A

Other NSAIDs

41
Q

P2y12 antagonists

A

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

42
Q

Ticlodipine

A
N/v/d 
Rash 
Prodrug 
Cyp2c19 inhibitor and metabolized by it 
Po bid 
Max inhibition 8-11 days
43
Q

Clopidogrel

A

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

44
Q

Prasugrel

A

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

45
Q

Black box warning for Ticlodipine

A

Neutropenia
Thrombotic thrombocytopenia purpura
Aplastic anemia

46
Q

Differences btwn clopidogrel and prasugrel

A

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

47
Q

Ticagrelor

A
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
48
Q

Dipyridamole

A

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

49
Q

Dipyridamole plus aspirin

A
Weak anti platelet 
Po bid 
Half life 10 h 
Elimin as glucuronide in bile 
ADR- vasodilation and hypotension (gets better with use)
50
Q

Cilostazole

A
Po bid 
Reversible pde3 inhib 
Targets platelets and vsm 
Blocks adenosine 
Half life 10 h 
3a4 metabolism 
Elimin in urine
51
Q

ADR of cilostazole

A

Ventricular arrhythmias
Ha
Hypotension

52
Q

G2b/3a receptor antag blocks what

A

Fibrinogen binding platelets

53
Q

Which G2b/3a antagonists are irreversible?

A

Abicimab

54
Q

Which G2b/3abare reversible?

A

Eprifibatide

Tirofiban

55
Q

ADR of G2b/3a antag

A

Bleeding

Thrombocytopenia

56
Q

Which G2b/3a antag are renally cleared

A

Epitifbatide

Tirofiban

57
Q

Thrombaxane inhib can also inhibit what?

A

Txa2 syn

58
Q

Par 1 inhibitors block?

A

Block thrombin mediated platelet activation