Anticoagulants & Thrombolytics Flashcards by Sarah Gillen

purified Fab fragments of monoclonal antibody that prevent GP IIb/IIIa receptors from binding to fibrinogen

abciximab

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indication for GP IIb/IIIa inhibitor to limit/prevent ischemia (3 words)

acute coronary syndromes

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indication for alteplase, especially when within 3-6 hrs and option of percutaneous coronary intervention is unavailable (3 words)

acute myocardial infarction

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platelet derived ligand for autocrine/paracrine stimulation of P2Y12 receptors

ADP

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glycoprotein produced via recombinant DNA technology that is identical in aa sequence to human tissue plasminogen activator

alteplase

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a treatment for bleeding, it prevents activation of plasminogen and directly inhibits plasmin (2 words)

aminocaproic acid

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no reliable way to monitor the degree of this for either dabigatran or rivaroxaban

anticoagulation

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

antithrombin

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contraindication for alteplase (2 words)

aortic dissection

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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 a short half-life and multiple sites of nonspecific binding, some of which can hasten its clearance

aPTT

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hirudin analog administered IV for the prophylaxis and treatment of thrombosis in patients with or at great risk for developing heparin-induced thrombocytopenia

argatroban

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irreversibly blocks the synthesis of thromboxane A2 by platelets, one of the agents that promotes the activation and aggregation of platelets; taking this at low-doses for cardiovascular prophylaxis is now (as of March 2019) no longer recommended for anyone without clinical signs of heart disease or stroke

aspirin

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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 intravenously and much more expensive than heparin

bivalirudin

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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

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obvious and effective treatment for bleeding (2 words)

blood replacement

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type 3 phosphodiesterase inhibitor used to suppress platelet aggregation, indicated for intermittent claudication

cilostazol

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

clopidogrel

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depending on risk for this, a daily dose of aspirin may be indicated (3 words)

coronary heart disease

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blocking stenosis here is an indication for clopidogrel (2 words)

coronary stents

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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

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needed by clopidogrel for activation and inhibited by proton pump inhibitors; reason Prilosec media mention Plavix and vice versa

CYP2C19

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orally active and reversible direct inhibitor of thrombin

dabigatran

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low-molecular weight heparins are now the dugs of first choice for the treatment and prevention of this (3 words)

deep venous thrombosis

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dabigatran is unstable and must be stored in this type of bottle, also avoiding excess heat or cold

desiccator

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a vasopressin V2 analog that can be useful for treating VWD and hemophilia, it promotes release of vWF and factor VII

desmopressin

abbr. for condition treated with heparin

DIC

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

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 (2 words)

drug interactions

example of a low-molecular weight heparin made by depolymerizing heparin; with its shorter chain length, its binding to antithrombin inhibits factor Xa but is generally unable to form the ternary complex with thrombin needed for its inhibition

enoxaparin

small peptide inhibitor of GP IIb/IIIa receptor approved for use during acute coronary syndromes and percutaneous coronary intervention

eptifibatide

substrate for plasmin

fibrin

bridging molecule between activated gp IIb/IIIa receptors on platelets

fibrinogen

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

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

GPIIb/IIIa

sequence of letters in a generic drug name that suggests blockade of P2Y12 receptors

grel

the use of heparin increases the risk for one of these forming and damaging the brain or spinal cord

hematoma

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

when severe and uncontrolled, a relative contraindication for alteplase

hypertension

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

not required for dabigatran or rivaroxaban (2 words)

INR monitoring

contraindication for alteplase and most serious concern with its use (2 words)

intracranial hemorrhage

contraindication for alteplase unless has occurred within past 3 hrs, when it is an indication (2 words)

ischemic stroke

duration of clopidogrel and aspirin effects on platelets

lifetime

dabigatran was found to be inferior to warfarin at inhibiting thromboembolism in these (3 words)

mechanical heart valves

warfarin has the potential to cause this in skin, occurs when rapid fall in protein C leads to a hypercoagulable state

necrosis

indication for rivaroxaban or dabigatran (3 words)

nonvalvular atrial fibrillation

seeing this sequence of letters in a generic drug name suggests product is some sort of heparin analog

parin

procedure (abbr.) that is indication for a GP IIb/IIIa inhibitor, which is used to prevent rapid re-occlusion

PCI

because predictable for both fondaparinux and low-molecular weight heparins, these agents can be self-administered at home

pharmacokinetics

generic ending of name for drugs that function as tissue plasminogen activators

plase

when clot-bound, converted by alteplase to enzyme responsible for clot breakdown

plasminogen

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

plasmin

a P2Y12 inhibitor similar to clopidogrel and competing for market share

prasugrel

platelet Fc receptors bind an IgG bound to heparin and this in heparin-induced thrmobocytopenia, leads to platelet activation/thrombosis and platelet removal by splenic macrophages

platelet factor 4

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

pregnancy

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

protein C

antidote for "oops, too much heparin"

protamine

aspirin has this for ischemic strokes, transient ischemic attacks, stable and unstable angina and myocardial infarction among others (2 words)

proven efficacy

indication for alteplase if acute and massive (2 words)

pulmonary embolism

advantage of dabigatran and rivaroxaban in comparison to warfarin (2 words)

rapid onset

ticagrelor differs from clopidogrel by causing this type of P2Y12 receptor block

reversible

a direct inhibitor of activated factor X, it therefore rapidly inhibits the generation of thrombin from prothrombin

rivaroxaban

characteristic of both onset and offset of warfarin's anticoagulant effects

slow

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

surgery

potent activator of platelets; it exerts these effects by cleaving a peptide from protease activated receptors (PAR1, PAR4) on the platelet surface, thereby allowing the ligand tethered to the GPCR to activate the receptor

thrombin

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

thrombocytopenia

useful for diagnosing heparin-induced thrmbocytopenia, expect onset between days 5-14 after heparin exposure

timing

prevention of this and its potential adverse consequences is a common reason for taking warfarin (2 words)

venous thrombosis

required for synthesis of biologically active clotting factors II, VII, IX, X, protein C and protein S among others, and antidote for warfarin (2 words)

vitamin K

newly approved (5/2014) reversible (but long half-life) PAR1 antagonist indicated for reduction of thrombotic cardiovascular events in patients with history of myocardial infaction or with peripheral arterial disease; life-threatening/fatal bleeding is a side effect that will limit its use

vorapaxar

exerts its slow onset anticoagulation effects by blocking the conversion of vitamin K epoxide to its active reduced form; depletion of biologically active vitamin K results in an inability to post-translationally carboxylate specific glutamate residues and results in enzyme proteins with a non-functional active site

warfarin

type of bleeding seen primarily at platelet counts below 10,000/microL

spontaneous

comparative color of arterial clots

white

type of bleeding common with platelet defects (along with rapid/greater bleeding from cuts)

mucocutaneous

common with platelet defects, uncommon with clotting factor defects

petechiae

bleeds here (e.g., hematomas) are a common manifestation of clotting factor deficiencies

deep tissue

leading to decreased levels of VKORC1 (vitamin K epoxide reducatase complex subunit 1), this is found in ~90% of asians and is why they are more sensitive to warfarin than blacks (~14% incidence)

genetic variability

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 (10-20%) in caucasians, increasing warfarin potency 3-5X

CYP2C9

a challenge for both heparin and warfarin, reason that frequent coagulation tests are required

dosing

humanized antibody recently available to neutralize/serve as an antidote for dabigatran

idarucizumab

recently approved as a reversal agent for factor Xa inhibitors rivaroxaban and apixaban

andexanet alfa

second physiological activator of plasminogen activator to degrade clotting factors, acts in fluid phase/extravascular compartment; was withdrawn from market but now back for treatment of pulmonary embolism needing a clot buster

urokinase