Coagulation drugs Flashcards
1
Q
Unfractionated heparin: routes of administration?
A
Mainly IV, also subQ.
2
Q
Unfractionated heparin: MoA?
A
Complexes w/AT III and mainly inhibits factors Xa and IIa. (also XIa, XIIa).
Increases AT-III’s binding affinity by 1000x.
3
Q
Unfractionated heparin: indications?
A
Surgical anticoagulation
4
Q
Unfractionated heparin: adverse effects?
A
Bleeding, HIT, osteoporosis, alopecia
5
Q
How is unfractionated heparin monitored?
A
Monitored by APTT (2-2.5x baseline therapeutic)
6
Q
LMW heparins: routes of administration?
A
SubQ
7
Q
LMW heparins: MoA?
A
Complexes w/AT and mainly inhibits factors Xa and IIa.
8
Q
LMW heparins: indications?
A
Prophylaxis and tx of DVT and ACS. (Alt. tx for HIT)
9
Q
LMW heparins: adverse effects?
A
Bleeding
10
Q
How is LMW heparin monitored?
A
Monitored by anti-Xa.
11
Q
Fondaparinux (pentasaccharide): route of administration?
A
SubQ
12
Q
Fondaparinux (pentasaccharide): MoA?
What class of drugs does it fall under?
A
Complexes w/AT to inhibit factor Xa (not IIa)
“Heparin anticoagulants”
13
Q
Indications for fondaparinux?
A
Mgmt of DVT
14
Q
Toxic/adverse effects of Fondaparinux?
A
Bleeding
15
Q
Argatroban: route of administration?
A
IV
16
Q
Argatroban: MoA?
What drug category does it fall under?
A
Direct IIa inhibitor
“Heparin anticoagulants”
17
Q
Argatroban: indications?
A
Anticoagulant mgmt of HIT pts
18
Q
Argatroban: adverse effects?
A
Bleeding
19
Q
*Besides argatroban, name 2 other drugs with the same MoA, indications, and toxic effects?
A
Bivalrudin & hirudin
(“Heparin anticoagulants.”
MoA: direct IIa inhibitor.
Indications: mgmt of HIT pts.
Adverse effects: bleeding)
20
Q
Argatroban, bivalrudin, and hirudin are all direct IIa inhibitors. How are each of them excreted?
Is there T1/2 longer or shorter?
A
- Argatroban: Liver
- Bivalrudin: Renal
- Hirudin: Renal
All short T1/2
21
Q
How is antithrombin concentrate administered?
A
IV
22
Q
Antithrombin concentrate: MoA?
A
Direct IIa inhibitor
23
Q
Antithrombin concentrate: indications?
A
DIC, sepsis, thrombophilia, hypercoagulable state
24
Q
Antithrombin concentrate: toxicity?
A
None!
25
What is protamine sulfate? What is it used for?
* Heparin antagonist
* Reverses the effects of heparin
26
Protamine sulfate: adverse effects/toxicity?
Bradycardia, hypotension
27
One USP unit of heparin is neutralized by ___ ug of protamine sulfate.
10
28
Try to name all all 8 types of "heparin anticoagulants," including the inhibitor.
1. Unfactionated heparin
2. LMW heparin (branded + generic)
3. Fondaparinux (pentasaccharide)
4. Argatroban
5. Bivalirudin
6. Hirudin
7. Antithrombin concentrate
8. Protamine sulfate
29
What is the brand name of warfarin?
How is it administered?
Coumadin
PO ("oral anticoagulant")
30
Warfarin: MoA?
Competitive antagonist of vitamin K. Suppresses the synthesis of functional forms of factors II, VII, IX and X by blocking enzyme **epoxide reductase** in liver
31
Warfarin: indications?
Prolonged tx of a-fib and DVT
32
\*Warfarin: toxic/adverse effects?
Bleeding, _coumadin induced necrosis_. Has interaction with several medications which can either potentiate the effects or inhibit the effects. *Crosses placental barrier* causing birth defects.
33
How are warfarin levels monitored?
Monitored via PT/INR.
34
How is vitamin K administered?
PO
| ("oral anticoagulants")
35
Vitamin K: MoA?
*Cofactor* in the synthesis of functional forms of factors II, VII, IX and X.
36
Vitamin K: indications?
* Hypoprothrombinemia
* Intestinal disorders
* Gastrectomy
* Reverses the effects of warfarin
37
Vitamin K: adverse effects?
Hemolysis
38
How is vitamin K monitored?
Trick: monitoring not required
39
\*Name the 3 *oral* anti-Xa anticoagulant drugs.
* Rivaroxaban
* Apixaban
* Edoxaban
(EAR)
40
Edoxaban, apixaban, rivaroxaban (ear): MoA?
Route of administration?
Xa inhibitor
PO
41
Edoxaban, apixaban, rivaroxaban (ear): indications?
- Which are approved for prophylaxis and tx of DVT?
- Which are approved for tx of ACS?
Stroke prevention in patients with a-fib.
**R** & **A** also approved for prophylaxis and treatment of DVT.
**R** approved for ACS.
42
Edoxaban, apixaban, rivaroxaban (ear): toxic effects?
Bleeding; liver toxicity
43
How are Edoxaban, apixaban, rivaroxaban (ear) monitored?
Monitoring not required
44
What are the names of the 2 *oral* anticoagulants that inhibit thrombin?
* Oral antithrombin
* Dabigatran
45
What is the MoA of both oral antithrombin and dabigatran?
Routes of administration?
Inhibits IIa
PO
46
What are the indications for oral antithrombin and dabigatran?
Stroke prevention for pts w/a-fib
47
Oral antithrombin and dabigatran: toxic effects?
Bleeding; liver toxicity
48
What organ clears oral antithrombin and dabigatran?
The kidney (could be problems for pts w/renal failure. Also, don't confuse it since it can also cause liver toxicity)
49
How are oral antithrombin and dabigatran monitored?
Trick: they do not need monitoring
50
Try to name the 7 oral anticoagulants discussed in class.
1. Warfarin
2. Vitamin K
3. Edoxaban
4. Apixaban
5. Rivaroxaban
6. Oral antithrombin
7. Dabigatran
51
1. Name 3 cyclooxigenase inhibitors that affect platelets.
1. Which affect which COX enzymes?
2. How are they administered?
1. ASA, NSAIDs, celecoxib
1. ASA/NSAIDs: inhibit COX-1 and 2. Celecoxib only inhibits COX-2
2. PO
52
How does a platelet aggregation assay work?
1. Prepare platelet-rich plasma
2. Activate platelets (ADP, TRAP, epi, 5-HT, collagen, ristocetin, AA)
3. Measure light transmittence
53
Genearlly, why might one prefer an anti-platelet drug to an oral anticoagulants or heparin?
Anti-platelet drugs are effective in the _arterial circulation_, where anticoagulants such as heparin and oral anticoagulants have relatively little effect.
54
What condition is ASA resistance a/w?
May be a cause of *recurrent ischemic vascular events* in patients taking aspirin.
55
Dual anti-platelet therapies usually combine ___________ with another anti-platelet drug such as ADP receptor inhibitors, gp IIb/IIIa inhibitors, or phosphodiesterase inhibitors.
Aspirin
(can do double or triple inhibitor therapy)
56
Name some drugs that can interact w/anti-platelet drugs.
1. Thrombolytic agents (urokinase, streptokinase and tPA)
2. Heparin/LMW Heparin/oral anticoagulants
3. Warfarin and other oral anticoagulant drugs
4. Antithrombin agents (hirudin, bivalirudin and argatroban)
57
The cyclooxygenase pw produces \_\_\_\_\_\_\_\_\_\_\_\_\_\_, while the lipooxygenase pw produces \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_.
Prostaglandins
Leukotrienes
58
Prostacyclin (PGI2) causes vaso-\_\_\_\_\_\_\_\_\_\_ and __________ platelet aggregation, while TXA2 causes vaso-\_\_\_\_\_\_\_\_\_\_ and __________ platelet aggregation.
* PGI2
* Vasodilation
* Inhibits
* TXA2
* Vasoconstriction
* Promotes
59
ASA: indications?
ACS, CVA, aterial thrombosis (long-term vascular events)
60
NSAIDs (propionic acid derivatives): indications?
Pain, inflammation, pyrexia (fever)
61
Celecoxib: indications?
RA, OA
62
Aspirin: adverse effects?
Bleeding, gastric irritation
63
NSAIDs/celecoxib: which has more adverse effects?
NSAIDs (bleeding)
64
\*Name the 5 ADP-receptor inhibitor anti-platelet drugs.
Clopido**grel**, prasu**grel**, tica**grel**or, ticlodipine, can**grel**or
65
How are clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor adminsitered?
What is their MoA?
PO
ADP-receptor inhibitors (anti-platelet)
66
Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor: indications?
ACS, CVA, in stent thrombosis (long-term vascular events)
67
What are the adverse effects of the ADP-receptor inhibitors?
Which of them has 1 additional side effect and what is it?
Bleeding
Clopidogrel also causes _TTP_
(Clopidogrel, prasugrel, ticagrelor, ticlodipine, cangrelor)
68
What is the name of the receptor on platelets that bind ADP?
P2Y12 receptor
69
If aspirin is intollerable, what would be a good class of drugs to consider giving?
Anti-platelet drugs
70
What drug class is recommended as duel-antiplatelet therapy w/ASA in conditions including STEMI, stent placement, and cerebrovascular dz?
Anti-platelet drugs
| ("grel"s)
71
Name the 2 drugs that are phosphodiesterase inhibitors?
What does inhibiting phosphodiesterase do?
Dipyridamole and cilostazole
They are anti-platelet drugs
72
Dipyridamole and cilostazole: MoA?
Phosphodiesterase inhibitors (^cAMP)
73
Dipyridamole and cilostazole: routes of administration?
PO
74
Dipyridamole: indications?
Cilostazol: indications?
* Dipyridamole: Arterial thrombosis, CVA
* Cilostazol: \*Intermittent claudication
(both phosphodiesterase inhibitors)
75
Dipyridamole: toxicity?
Cilostazol: toxicity?
* Dipyridamole: Bleeding
* Cilostazol: Hypotension (due to vasodilation)
76
Name 2 leukotriene receptor inhibitor drugs.
What overall class of drugs do these belong in?
Monteleukast and zafirleukast
Anti-platelet drugs
77
Monteleukast and zafirleukast: MoA?
Leukotriene receptor inhibitor (anti-platelet)
78
Monteleukast and zafirleukast: route of administration?
PO
79
Indications:
* Monteleukast
* Zafirleukast
* Monteleukast: Allergies (allergic rxns)
* Zafirleukast: Asthma
80
Adverse effects:
* Monteleukast
* Zafirleukast
* Monteleukast: Hypotension; behavioral changes
* Zafirleukast: Hypotension
81
Name 3 GP IIb/IIIa inhibitors.
"II/III TEA"
Abciximab, eptifibatide, tirofiban
82
Abciximab, eptifibatide, tirofiban: MoA?
What class of drugs do they belong in?
Inhibit gp IIb/IIIa receptor on platelets
Antiplatelet
83
\*Abciximab, eptifibatide, tirofiban: indications?
ACS/PCI (percutaneous coronary intervention)
84
Abciximab, eptifibatide, tirofiban: toxicity?
Bleeding
85
What is the MoA of iloprost? (not on chart)
Thromboxane receptor antagonist
86
What is the active anti-platelet agent of fish oil?
Omega-3 fatty acids
87
What is the MoA of omega-3 fatty acids (in fish oil)?
Indications?
* Membrane effects; TXA3 (?)
* Prevention of heart dz (?)
88
\*What is the route of administration for the gp IIb/IIIa inhibitors?
IV (pretty sure all others we looked at were PO)
89
What class of drug is zileuton?
What's its MoA?
Antiplatelet
Lipooxygenase inhibitor
90
Zileuton: indications?
Asthma
91
Zileuton: toxicity?
Hypotension
92
Name 4 thrombolytic agents.
Name 3 anti-thrombolytic agents.
Streptokinase, urokinase, tPA, ancrod
Epsilon amino caproic acid, aprotinin, tranexamic acid
93
What type of drug is streptokinase?
How is it adminsitered?
Thrombolytic
IV
94
What type of drug is urokinase?
How is it adminsitered?
Thrombolytic
IV
95
What type of drug is tissue plasminogen activator (tPA)?
How is it adminsitered?
Thrombolytic
IV
96
What type of drug is ancrod?
How is it adminsitered?
Fibrinolytic
IV
97
What are the indications for streptokinase and urokinase?
Thrombolysis: CVA, MI, PE
98
What is the MoA for the thrombolytic agents urokinase, streptokinase, ancrod, and tPA?
Fibrinolysis (convert plasminogen to plasmin)
99
What are the indications for tPA?
Thrombolysis: CVA, MI
100
What are the indications for ancrod?
Under what conditions would it be used?
CVA
\*Used when pts allergic to heparin
101
Where does ancrod come from?
Snake venom
102
What are the adverse effects of all thrombolytic agents?
Which have additional adverse effects?
Bleeding, as well as re-occlusion and CVA
Steptokinase: mild allergic rxns
Ancrod: allergic rxns
103
What are 3 drugs/drug classes that thrombolytics interact w/?
Antiplatelet drugs, dextrans, heparin
104
\*What are the absolute contraindications of thrombolytics? (4)
* Head trauma
* Recent intracranial surgery
* Severe HTN
* Cerebral hemorrhage (white on CT)
105
What type of drug is epsilon amino caproic acid, EACA (MoA)?
Anti-thrombolytic (blocks plasminogen to plasmin)
106
What type of drug is aprotinin? (MoA?)
Anti-fibrinolytic (inhibits kallikrein to decrease factor XII)
107
What type of drug is tranexamic acid? (MoA?)
Anti-fibrinolytic: blocks plasminogen to plasmin
108
What are the indications for EACA, aprotinin, and tranexamic acid?
Reversal of bleeding
109
What toxic effects are a/w epsilon amino caproic acid?
Hypotension
110
What toxic effects are a/w aprotinin?
Graft thrombosis
111
What toxic effects are a/w tranexamic acid?
Retinopathy
112
