Thromboembolic Drugs Flashcards

1
Q

Reason for selecting heparin (i.e. due to its inability to cross membrane barriers) as anticoagulant rather than warfarin)

A

Pregnancy

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2
Q

Doing this near eye, brain, or spinal cord is a contraindication for anticoagulants

A

Surgery

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3
Q

Can be used to measure anticoagulation for drugs such as rivaroxaban; not in notes but a version of this is not now also used to measure unfractionated heparin and low molecular weight heparin

A

Antixa

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4
Q

Recombinant human form purified from goat’s milk is available for those with deficiency, but it is expensive

A

Antithrombin

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5
Q

Substrate for plasmin

A

Fibrin

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6
Q

Vitamin K-dependent anti-clotting factor with shorter half-life than several other factors, its disappearance is reason warfarin administration can cause a pro-coagulant phase

A

Protein C

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7
Q

Indication for alteplase, especially when within 3-6 hours and option of percutaneous coronary intervention is unavailable

A

Acute myocardial infarction

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8
Q

Indication for rivaroxaban or dabigatran

A

Nonvalvular atrial fibrillation

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9
Q

Indication for GP IIb/IIIa inhibitor to limit/prevent ischemia

A

Acute coronary syndromes

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10
Q

Low-molecular weight heparins are now the drugs of first choice for the treatment and prevention of this

A

Deep venous thrombosis

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11
Q

Can be induced by unfractionated heparin and low-molecular weight heparin; fondaparinux will not induce but should not be used as a replacement anticoagulant as it can exacerbate the situation

A

Thrombocytopenia

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12
Q

Contraindication for alteplase and most serious concern with its use

A

Intracranial hemorrhage

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13
Q

If high risk for this causing acute coronary syndrome, a daily dose of aspirin may be indicated

A

Coronary heart disease

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14
Q

Leading to decreased levels of VKORC1 (Vitamin K epoxide reductase complex subunit 1) This is found in ~90% of asians and is why they are more sensitive to warfarin than blacks

A

Genetic variability

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15
Q

A treatment for bleeding (tranexamic acid is another), it prevents activation of plasminogen and directly inhibits plasmin

A

Amino caproicacid

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16
Q

Platelet derived ligand for autocrine/paracrine stimulation of aggregation via P2Y12 receptors

A

ADP

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17
Q

Among the best selling drugs in the world, it suppresses platelet aggregation by irreversibly blocking P2Y12 receptors

A

Clopidogrel

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18
Q

Indication for alteplase if acute and massive, otherwise focus on limiting likelihood of more with anticoaguluants

A

Pulmonary embolism

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19
Q

Release of this GPCR ligand from endothelial cells keeps platelets in an unactivated state

A

PGI2

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20
Q

Sequence of letters in a general drug name that suggests blockade of P2Y12 receptors

A

-GREL

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21
Q

Breaks down a blood clot when bound to it, when circulating it breaks down various clotting factors unless bound by alpha2-antiplasmin

A

Plasmin

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22
Q

Comparative color of arterial clots due to abundance of platelets of this side of circulation; reason platelet targeting drugs are chosen for problems there

A

White

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23
Q

Platelet receptors that allow the platelets to link together (aggregate), drugs that block these receptors block the final common pathway of platelet aggregation and are therefore the most effective antiplatelet drugs

A

GpIIb/IIIa

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24
Q

Dabigatran was found to be inferior to warfarin at inhibiting thromboembolism in these

A

Mechanical heart valves

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25
Can be used to assess anticoagulation caused by dabigatran
Diluted thrombin time
26
Characteristic of both onset and offset of warfarin’s anticoagulant effects
Slow
27
Synthetic pentasaccharide, the minimum sequence needed to bind to antithrombin and inhibit factor Xa; sequence is too short to form the ternary complex with thrombin that is needed to inhibit thrombin activity
Fondaparinux
28
Needed by clopidogrel for activation and inhibited by proton pump inhibitors; reason Prilosec media mention Plavix and vice versa
CYP2C19
29
Enzyme thought to be responsible for synthesis of platelet inhibitor PGI2 by endothelial cells; its selective sparing by low doses of aspirin is thought to explain the cardiovascular benefits of aspirin and the adverse effects associated with withdrawn drug rofecoxib
COX2
30
Procedure (abbr.) that is indication for a GpIIb/IIIa inhibitor, which is used to prevent rapid re-occlusion
PCI
31
Required for synthesis of biologically active clotting factors II, VII, IX, X, protein C, and protein S among others, and antidote for warfarin
Vitamin K
32
When severe and uncontrolled, a relative contraindication for alteplase
Hypertension
33
Bleeds here (e.g. hematoms) are a common manifestation of clotting factor deficiencies
Deep tissue
34
Platelet Fc receptors bind an IgG bound to heparin and this in heparin-induced thrombocytopenia, leads to platelet activation/thrombosis and platelet removal by splenic macrophages
Platelet factor 4
35
Dabigatran is unstable and must be stored in this type of bottle (i.e. can’t use a pill-minder) while also avoiding excess heat or cold
Desiccator
36
Contraindication for alteplase unless has occured within past 3 hours, when it is an indication
Ischemic stroke
37
A challenge for both heparin and warfarin, reason that frequent coagulation tests are required
Dosing
38
Lower than 2 and the risk for thromboembolism increases in patients treated with warfarin while higher than 3 and risk of intracranial hemorrhage increases
INR
39
Abbr. for condition treated with heparin
DIC
40
A P2Y12 inhibitor similar to clopidogrel and competing for market share, more effective with fewer drug interactions but also causes more major bleeding
Prasugrel
41
A nonpeptide inhibitor of GPIIb/IIIa used for acute coronary syndromes, patent recently expired
Tirofiban
42
A mixture of long highly negatively charged polysaccharide chains isolated from bovine lung or porcine intestine, a pentasaccharide sequence randomly distributed along its length binds to antithrombin to facilitate its inhibition of factor Xa and thrombin
Heparin
43
Risk of this can be reduced during alteplase administration by minimizing physical manipulation of the patient, avoiding subQ and IM injections, and minimizing concurrent use of anticoagulants and antiplatelet drugs
Bleeding
44
Glycoprotein produced via recombinant DNA technonlogy that is identical in aa sequence to human tissue plasminogen activator (t-PA)
Alteplase
45
Color of blood clots on the venous side of the circulation, consequence of fibrin mesh that forms
Red
46
Obvious and effective treatment for bleeding
Blood replacement
47
Had been no reliable way to monitor the degree of this for either dabigatran or rivaroxaban
Anti-coagulation
48
Purified Fab fragments of monoclonal antibody that prevent GpIIb/IIIa receptors from binding to fibrinogen
Abciximab
49
Blocking stenosis here is an indication for clopidogrel
Coronary stents
50
Drug class not part of this lecture, but first-line therapy for decreasing cardiovascular disease risk via lowering of LDL-C
Statins
51
Contraindication for alteplase
Aortic dissection
52
PAR1 antagonist indicated for reduction of thrombotic cardiovascular events in patients with history of myocardial infarction or with peripheral arterial disease; life-threatening/fatal bleeding is a side effect that has limited its use
Vorapaxar
53
Because predictable for both fondaparinux and low-molecular weight heparins, these agents can be self-administered at home
Pharmacokinetics
54
A direct inhibitor of activated factor X, it therefore rapidly inhibits the generation of thrombin from prothrombin
Rivaroxaban
55
Small peptide inhibitor of GpIIb/IIIa receptor approved for use during acute coronary syndromes and percutaneous coronary intervention
Epitifibatide
56
Seeing this sequence of letters in a generic drug name suggests product is some sort of heparin analog
Parin
57
Laboratory test used to monitor the anticoagulant activity of heparin; ideally kept at 1.5-2 but can be a challenge since heparin has highly variable plasma levels due to a short half-life and multiple sites of nonspecific binding, some of which can hasten its clearance
APTT
58
Ticagrelor differs from clopidogrel by not being a prodrug and by causing this type of P2Y12 receptor block
Reversible
59
Warfarin has a multitude of these that can influence its activity and mandates regular testing and additional testing whenever changes are made to the daily treatment regimen
Drug interactions
60
Recently approved as a reversal agent for factor Xa inhibitors rivaroxaban and apixaban
Andexanetalfa
61
A “T” useful for diagnosing heparin-induced thrombocytopenia; expect onset between days 5-14, after starting heparin exposure, or <= 1 day if previous heparin exposure in last 30 days
Timing
62
Type of bleeding seen primarily at platelet counts below 10,000/microL
Spontaneous
63
Warfarin has the potential to cause this in skin, occurs when rapid fall in protein C leads to a hypercoagulable state
Necrosis
64
Common with platelet defects, uncommon with clotting factor defects
Petechiae
65
Hirudin analog administered IV for the prophylaxis and treatment of thrombosis in patients with or at great risk for developing heparin-induced thrombocytopenia; classic answer but DOACs may eventually displace
Argatroban
66
Second physiological activator of plasminogen activator degrade clotting factors, acts in fluid phase/extrasvascular compartment; was withdrawn from market but now back for treatment of pulmonary embolism needing a clot buster
Urokinase
67
Bridging molecule between activated GpIIb/IIIa receptors on platelets
Fibrinogen
68
Protease-activated receptor on platelet surface that is permanently activated by thrombin to promote platelet aggregation
PAR1
69
Metabolizes the more potent S-warfarin to 7-OH-warfarin; there are numerous polymorphisms in this gene and those decreasing its activity against warfarin are more common in caucasians, increasing warfarin potency 3-5x
CYP2C9
70
Advantage of dabigatran and rivaroxaban in comparison to warfarin
Rapid onset
71
Potent activator of platelets; it exerts these effects by cleaving a peptide from protease activated receptors (PAR1, PAR4) ont he platelet surface, thereby allowing the ligand tethered to the GPCR to activate the receptor
Thrombin
72
Generic ending of name for drugs that function as tissue plasminogen activators
Plase
73
Deficiencies of these tend to manifest as deep tissue bleeding forming large subcutaneous and soft tissue hematomas, hemarthroses, may be delayed/oozing after procedures
Clotting factors
74
Durationn of clopidogrel and aspirin effects on platelets
Lifetime
75
When clot-bound, converted by alteplase to enzyme responsible for clot breakdown
Plasminogen
76
The use of heparin increases the risk of one of these forming and damaging the brain or spinal cord
Hematoma
77
A vasopressin V2 analog that can be useful for treating VWD and hemophilia, it promotes release of vWF and factor VII
Desmopressin
78
A synthetic peptide similar to leech anticoagulant hirudin, it is a direct inhibitor of thrombin, but class as a whole has had limited use since must be administered IV and much more expensive than heparin
Bivalirudin
79
Aspirin has this for ischemic strokes, transient ischemic attaacks, stable and unstable angina and MI among others
Proven efficacy
80
Suppresses platelet aggregation via uncertain mechanism (PDE inhibitor), synergizes with aspirin and used in combination to prevent recurrent ischemic stroke in patients with TIA or past stroke
Dipyridamole