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Therapeutics Exam 2 > Anticoagulation > Flashcards

Anticoagulation Flashcards

0
Q

Intrinsic Pathway

A

Damage to blood vessel
Negatively charged surface
Factor 12…11…9…10(with 7a)…2(thrombin)…1(fibrin)

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1
Q

Extrinsic pathway

A

Damage to tissue outside the vessel
Trauma
Tissue Factor
Factor VIIa…X (with IX)

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2
Q

Hypercoaguable states

A 
FVL
Prothrombin (20210A) gene mutation
Antithrombin, Protein C and S Deficiency
Antiphospholipid antibodies (lupus)
HYPERhomocysteinemia
IBD
Nephrotic Syndrome
Pregnancy
Malignancy
Drug Induced
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3
Q

Ideal anticoagulant

A 
Oral
Daily dose
Rapid onset/offset
Predictable PK/PD
Few food/drug interactions
Fixed doses
Wide therapeutic window
Easily reversed
No monitoring
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4
Q

List Factor Xa Inhibitors

A

Fondaparinux
Rivaroxaban
Apixaban

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5
Q

List Direct Thrombin Inhibitors

A

Argatroban
Bivalrudin (Angiomax™)
Dabigatran (Pradaxa™)

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6
Q

List LMWH’s

A

Enoxaparin (Lovenox™)

Dalteparin (Fragmin™)

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7
Q

Heparin routes of admin

A

Parenterally (IV and SQ) rapid acting anticoagulant

Not IM - why?

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8
Q

Heparin MOA

A

Potentiates the action of antithrombin III
…thereby inactivating thrombin
…as well as activated coagulation factors 9, 10, 6 and 7, and plasmin
…prevents conversion of fibrinogen to fibrin

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9
Q

Heparin Labeled Indications

A

Px/Tx of thromboembolic disorders

Anticoagulant for extracorporeal and dialysis procedures

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10
Q

Heparin Unlabeled Indications

A

STEMI/NSTEMI
USA
During PCI (stent)

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11
Q

Heparin ADE’s

A 
Bleeding
Bruising at admin sites
HIT
Osteoporosis
HYPERkalemia
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12
Q

Increases risk of bleeding with heparin

A 
Surgery
Hemostatic defects
Heavy alcohol consumption 
Renal failure
Peptic ulcers
Cancer
Uncontrolled HT
History of hemorrhagic stroke
Recent GI bleeding
Thrombocytopenia 
Sever liver disease
Retinopathy
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13
Q

HIT

A

50% decrease in platelet count from pretreatment
Occurs 5-10 days after initiation of heparin or
Earlier with previous exposure (last 3-4 mo)
Diagnosed by assay for antibodies

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14
Q

Osteoporosis and heparin

A

Full therapeutic doses for extended (>6mo) period

Due to reduction in bone mineral density

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15
Q

HYPERkalemia and heparin

A

Heparin suppresses aldosterone production

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16
Q

Protamine sulfate

A 
Heparin reversal
Occurs within 5mins after IV admin
1mg neutralizes 100 units of heparin
Slow IV infusion
Max dose 50mg
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17
Q

Heparin Monitoring

A

aPTT/PTT (activated partial thromboplastin time)
CBC
Platelets

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18
Q

aPTT/PTT ranges

A

Institution specific
Correlates with plasma heparin conc 0.3-0.7 unit/
ml anti-Xa assay
Target aPTT range is 1.5-2.5 x control

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19
Q

LMWH MOA

A

Inactivate Factor Xa
Higher ratio of anti factor Xa to anti factor IIa
(thrombin) activity
More predictable PK, anticoagulant response
LMWH does not bind to heparin binding proteins
Peak 3-5 hrs
Half-life enox 4.5-7hr, dalteparin 2-5hr
Renal elimination

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20
Q

LMWH Labeled Indications

A

DVT Px in…
Hip or Knee replacement, or Abdominal surgery
Risk of thrombus complications in acute illness
Tx DVT/PE
USA
NSTEMI/STEMI

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21
Q

LMWH Unlabeled Indications

A 
Bridge therapy
DVT Px following mod-risk surgery
Anticoagulant in extracorporeal circuit in dialysis
ANTICOAGULANT OF CHOICE IN PREGNANCY
Anticoagulant for PCI
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22
Q

LMWH BBW

A

Risk for epidural and spinal hematomas resulting in permanent paralysis. Placement or removal of spinal catheter delayed for at least 12 hr after admin of Px dose and consider 24 hr after therapeutic dose. Post-procedural dose should be given no sooner than 4 hr after spinal catheter removal.

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23
Q

LMWH Admin

A

SQ in abdomen or outer thigh

IV in STEMI/PCI for enoxaparin

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24
LMWH Dosing
Fixed or weight based every 12-24 hr according to product indication
25
LMWH Monitoring
Baseline CBC with platelet count and SrCr Advantage over UFH- Does NOT require routine coagulation testing Small effect on aPTT - NO need to monitor Only in acute dosing in pregnancy or extreme obesity (>190 kg) or wt <50 kg
26
LMWH ADE's
``` Major bleeding Easy bruising Osteoporosis HIT (less than UFH) If pt has HIT history, do NOT use LMWH ```
27
Reversal for UFH
``` Protamine sulfate Reversal occurs w/in 5mins after IV admin 1mg neutralizes 100 units of heparin Slow IV infusion Dose NOT to exceed 50mg ```
28
Anticoagulant DOC in pregnancy
LMWH
29
LMWH elimination
Renally
30
Fondaparinux MOA
Indirect factor Xa inhibitor through interaction with antithrombin
31
Fondaparinux admin
Admin SQ DAILY into fatty tissue of abdominal wall | Do NOT expel air bubble from syringe before injecting
32
Fondiparinux elimination
Unchanged in urine
33
Fondaparinux peak and half-life
Peak conc in 2 hrs Half life 17-24 hrs Anticoagulant effect lasts 2-4 days after DC in normal renal fx
34
Fondaparinux contraindications
CrCl <30ml/min | Use caution in CrCl 30-50
35
Fondaparinux Labeled Indications
DVT Px in... hip or knee replacement hip fractures abdominal surgery Tx of acute DVT/PE
36
Fondaparinux Unlabeled Indications
NSTEMI/STEMI USA DVT Px in pts with Hx of HIT Tx of acute thrombosis in pts with past Hx of HIT
37
Fondaparinux monitoring
Baseline CBC/SrCr (DC if CrCl <30) | NO routine coagulation monitoring
38
Fondaparinux ADE's
Bleeding major hemorrhage 1-3% <6 hr post-op increases bleeding to 5% Rare reports of HIT however, has been given to pts with current or Hx of HIT due to lack of an immune-mediated effect on plts
39
Examples of biologic anticoagulant
UFH | LMWH
40
Example of synthetic anticoagulant
Fondaparinux
41
Anticoagulant with 100% Bioavailability
Fondaparinux
42
Anticoagulant with only 30% Bioavailability
UFH
43
Anticoagulant with half life of 17 hrs
Fondaparinux
44
Anticoagulant with half life of 1.5 hrs
UFH
45
Anticoagulant with half life of 4 hrs
LMWH
46
Anticoagulant with renal excretion
LMWH | Fondaparinux
47
Anticoagulant without renal excretion
UFH
48
Anticoagulant with NO antidote
Fondaparinux
49
Anticoagulant with partial antidote
LMWH
50
Target for Fondaparinux
Xa
51
Target for UFH and LMWH
Xa and IIa
52
Pt with CrCl of 28 should be given anticoagulant of
Heparin because LMWH and Fondaparinux are eliminated renally
53
List two Oral Factor Xa inhibitors
Rivaroxaban (Xarelto) | Apixaban (Eliquis)
54
PC for rivaroxaban
15 and 20 mg MUST BE TAKEN WITH FOOD
55
What is the safest new anticoagulant in renal patients?
Apixaban
56
Rivaroxaban bioavailability
``` 10mg = 80-100% 15&20mg = ~66% MUST BE TAKEN WITH FOOD ```
57
Rivaroxaban half life
5-9 hrs | 11-13 hrs in elderly
58
Rivaroxaban elimination
Primarily urine via active tubular secretion/feces
59
Rivaroxaban substrates
CYP3A4/5 CYP2J2 PGP
60
Apixaban bioavailability
50% May be taken with or without food
61
Only anticoagulants indicated for stroke in nonvalvular afib
Rivaroxaban | Apixaban
62
Only anticoagulant indicated for secondary Px against DVT/PE
Rivaroxaban
63
Rivaroxaban labeled indications
DVT Px in hip/knee replacement Stroke prevention in nonvalvular afib Secondary Px against DVT/PE
64
Apixaban labeled indications
DVT Px in hip/knee replacement | Stroke prevention in nonvalvular afib
65
Apixaban substrates
CYP3A4/5 mainly
66
Apixaban elimination
Feces / 25% Renal | Safest new anticoagulant in renal pts
67
Apixaban half life
~12 hrs
68
Monitoring for Oral Factor Xa Inhibitors
Bleeding CBC with plts, SrCr, hepatic fx Monitoring of coagulation tests not required
69
Oral Xa Inhibitor Drug Interactions
``` Avoid with STRONG CYP3A4... inhibitors (clarithromycin, -azoles, -avirs, nefazodone) and inducers (rifampin, phenytoin, carbamazepine, St. John's wort) ```
70
Oral Factor Xa Inhibitor Reversal
No specific antidote Rivaroxaban NOT dialyzable Therapy for severe hemorrhage: PCC or APCC or Recombinant Factor VIIa
71
Dabigatran contraindications
Pts with mechanical heart valves
72
DTI that does not require adjustment in renal dysfunction
Argatroban
73
DTI that does not require adjustment in hepatic dysfunction
Bivalrudin
74
DTI metabolized by CYP3A4
Argatroban
75
Argatroban labeled indications
HIT-Monitor PTT | PCI-Monitor ACT
76
Argatroban unlabeled indications
Extracorporeal circuit patency of CRRT
77
Bivalrudin labeled indications
USA undergoing PTCA or PCI- monitor ACT
78
Bivalrudin unlabeled indications
HIT- monitor PTT | STEMI undergoing PCI- monitor ACT
79
DTI metabolized by blood proteases
Bivalrudin (B-Blood)
80
Oral DTI bioavailability
3-7% for dabigatran (Pradaxa)
81
Dabigatran metabolism
Metabolized to active form by plasma and hepatic esterases and hepatic glucuronidation
82
Dabigatran substrate
P-glycoproteins
83
Dabigatran elimination
Excreted in urine
84
Dabigatran half life
12-17 hrs Elderly 14-17 hrs Mild-Mod renal 15-18 hrs (GFR 30-89) Severe renal impairment 28 hrs (GFR <30)
85
Dabigatran labeled indications
DVT/PE Tx and Px | Stroke Px in nonvalvular afib
86
Dabigatran unlabeled indications
Postoperative thromboprophylaxis with total hip or knee replacement surgery

Therapeutics Exam 2 (15 decks)

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