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pharm exam 2 > Topic 13 Bloooood > Flashcards

Topic 13 Bloooood Flashcards

1
Q

Anticoagulants indirect thrombin inhibitors

A

Warfarin (Coumadin)
Unfractionated heparin Low-molecular-weight heparin -Lovenox
Fondaparinux-Arixtra

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2
Q

Warfarin

A

Coumadin

Anticoagulants indirect thrombin inhibitors

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3
Q

Coumadin

A

Warfarin

Anticoagulants indirect thrombin inhibitors

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4
Q

Unfractionated Low-molecular-weight heparin

A

Lovenox

Anticoagulants indirect thrombin inhibitors

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5
Q

Fondaparinux

A

Arixtra

Anticoagulants indirect thrombin inhibitors

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6
Q

Lovenox

A

Unfrac Low MW Heparin

Anticoagulants indirect thrombin inhibitors

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7
Q

Arixtra

A

Fondaparinux

Anticoagulants indirect thrombin inhibitors

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8
Q

Anticoagulant: Direct Thrombin Inhibitor

A

Lepirudin (Refludon)
Argatroban
Bivalirudin (Angiomax)

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9
Q

Lepirudin

A

Refludon

Anticoagulant: Direct Thrombin Inhibitor

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10
Q

Argatroban

A

Anticoagulant: Direct Thrombin Inhibitor

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11
Q

Bivalirudin

A

Angiomax

Anticoagulant: Direct Thrombin Inhibitor

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12
Q

Refludon

A

Lepirudin

Anticoagulant: Direct Thrombin Inhibitor

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13
Q

Angiomax

A

Bivalirudin

Anticoagulant: Direct Thrombin Inhibitor

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14
Q

How do Anticoagulants work?

A

inhibit one or more steps in the clotting cascade that lead to fibrin formation…
*They do NOT dissolve clots

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15
Q

Heparin chemistry

A

It is a mix of straight-chain polymers consisting of extremely anionic repeating dissacharide units.

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16
Q

Heparin pH?

A

most acidic molecules in a critter’s body because so many carboxyl and sulfate groups are attached

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17
Q

Heparin lives where?

A

“lives” in mast cells and basophils (which are essentially circulating mast cells.)

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18
Q

Unfractionated Heparin size?

A

5000-30,000 Daltons

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19
Q

One (1) Unit of Heparin?

A

~0.002 mg of heparin/unit

“The quantity of heparin required to keep 1 milliliter of cat’s (sheep) blood fluid for 24 hours at 0°C”

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20
Q

Porcine intestinal- derived heparin may be better in preventing what complications ?

A

HIT

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21
Q

Heparin administration

A

ALWAYS Parentally

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22
Q

Fractionated LMW Heparin size

A

5,500 daltons

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23
Q

Heparin + AT-III > _____ more active anticoagulant activity than AT-III by itself

A

1000X

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24
Q

Heparin and LMWH:

Intravenous half life

A

Heparin: 2 hrs
LMWH: 4hrs

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25
Q

Heparin and LMWH:

Anticoagulant response

A

Heparin: Variable
LMWH: predicable

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26
Q

Heparin and LMWH:

Bioavailibility

A

Heparin: 20%
LMWH: 90%

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27
Q

Heparin and LMWH:

Major adverse effect

A

Heparin: Frequent Bleeding
LMWH: Less Frequent bleeding

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28
Q

Heparin and LMWH:

Setting for therapy

A

Heparin: Hospital
LMWH: Hospital and outpatient

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29
Q

Heparin Time to effect:
–Intravenous:
–Subcutaneous:

A

(IV): a few minutes

(SQ): 1-2 hours

30
Q

Heparin is cleared by what?

A

cleared by binding to macrophages and being depolymerized and desulfonated in the liver…and the metabolites are excreted in the urine

31
Q

Unfractionated heparin’s half-life?

A

~1-2 hours

32
Q

*Fractionated (LMWH) half-life

A

3-7 hours

33
Q

heparin’s half-life is prolonged by what dysfunctions?

A

either renal &/or liver dysfunction

34
Q

Heparins process is saturable (implied) - what does this mean?

A

Lower doses of heparin are cleared at a faster rate than higher higher doses

35
Q

Heparin is a metabolic process? how do we know this?

A

heparin clearance is (naturally) slower at lower temps and accelerated at higher temps

36
Q

Heparin side effects

A

excessive bleeding

HIT

37
Q

Fondaparinux

A

sunthetic LMWH (pentasaccharide)

38
Q

Fondaparinux t1/2

A

~20 hours and eliminated unchanged in the urine

39
Q

Major advantage of Fondaparinux?

A

eliminated risk of HIT type II

40
Q

Warfin sponsored by?

A

Wisconsin Alumni Research Foundation

41
Q

Warfin works by inhibiting what?

A

Works by inhibiting Vitamin K

42
Q

Vitamin K aka

A

phytonadione/Mephyton

43
Q

Warfarin blocks an enzyme named what?

A

named Vitamin K epoxide reductase

44
Q

Vitamin K epoxide reductase is required to allow the liver to do what?

A

“recycle” spent (oxidized) Vitamin K so eventually stores of Vitamin K are simply depleted

45
Q

Giving Vitamin K readily reverses the effects of what?

A

warfarin

46
Q

Warfin requires vitamin K to produce factors: (4)

A

II: Prothrombin
VII: Proconvertin
IX: Plasma Thromboplastin Component
X: Stuart-Prower Factor

47
Q

Warfin Blocks the γ-carboxylation sites of what factors? (which are also anticoagulants via their ability to block factors Va and VIIIa)

A

factors II, VII, IX, & X as well as Proteins C and S

48
Q

Takes a while for Warfarin to exert its clinical effect, why? when is peak effect?

A

(8-24 hours) since those Vitamin K stores have to be depleted.
Peak effects occur~2-4 days (once those stores are completely empty

49
Q

Warfarin side effects?

A 
#1 bleeding
birth/fetal deformities/death
warfarin necrosis (bc involves CNS)
50
Q

Warfarin typical dose

A

Typical dose is 5-7mg/day with adjustments made after ∽ one week

51
Q

Warfarin typically monitored via what?

A

prothrombin time (PT)

52
Q

What is added to plasma to monitor Warfarin?

A 
Tissue Factor (Factor III)
Calcium (Factor IV)
53
Q

INR

A

= “International Normalized Ratio”

= Critter’s PT / Laboratory “normal” PT mean

54
Q

Hirudin

A

Irreversibly binds to and deactivates thrombin

55
Q

Lepirudin

A

Refludan

56
Q

Lepirudin (Refludan) - how does it work?

A

synthetic, purified form of hirudin
Bivalently and irreversibly binds to thrombin
One molecule of lepirudin binds one molecule of thrombin

57
Q

Lepirudin (Refludan) how does it work differently than Heparin?

A

not dependent on interactions with AT III for its function

58
Q

Lepirudin (Refludan) T1/2

A

~ 1 hour, but can increase to several days in renal insufficiency/failure patients

59
Q

Lepirudin (Refludan) - ~50% of patients who receive this courses of therapy develop what?

A

Very antigenic.

  • develop antibodies to the lepirudin-thrombin complex.
  • These antibodies prevent Lepirudin’s clearance by the kidneys and increases its anticoagulant effect &/or can cause an anaphylactic reaction.
60
Q

Lepirudin - reversal ?

A

Unlike heparin, NO REVERSAL AGENT EXISTS!

61
Q

Bivalirudin what?

A

(Angiomax)
completely synthetic yet chemically smaller “cousin” of hirudin
a bivalent direct thrombin inhibitor, operates independent of AT III, and is given parenterally

62
Q

Bivalirudin (Angiomax) can be removed by what?

A

hemoconcentrators

63
Q

Drug that is also commonly used for anticoagulation for patients with HIT

A

Bivalirudin (Angiomax)

64
Q

Bivalirudin (Angiomax)

A

Very commonly used during PTCAs to prevent platelet activation
also commonly used for anticoagulation for patients with HIT

65
Q

Argatroban

A

A parenterally-administered small molecule direct thrombin inhibitor.
Short half-life (~40-50 minutes).

66
Q

Argatroban monitored with what?

A

Monitored with aPTTs

67
Q

Argatroban eliminated how?

A

*Eliminated by hepatic clearance

68
Q

Argatroban or Bivalirudin (Angiomax) how do you choose which one to use?

A

whether the patient has intact renal or hepatic function and ease of monitoring the anticoagulation
Bivalirudin - ok with liver failure

69
Q

Apixiban (Eliquis) and Rivaroxaban (Xarelto)

A

–Both are oral anticoagulants that directly inhibit Factor Xa
Both are cleared renally and used for a-fib

70
Q

Apixiban

A

Eliquis

Both are oral anticoagulants that directly inhibit Factor Xa

71
Q

Rivaroxaban

A

Xarelto

Both are oral anticoagulants that directly inhibit Factor Xa

pharm exam 2 (9 decks)

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