Pharm: Coagulation drugs part 2

What is the fibrinolytic agent? (aka tissue plasminogen activator/ tPA)

alteplase

What drug is not recommended in patients that are 75+ years old?

prasugrel

What drug’s therapeutic uses include:

acute coronary syndrome (patients wiht a hidtory of MI or unstalbe angina), coronary artery disease, minor ischemic stroke

ticagelor

What drug has a short t1/2 of 5 minutes so it must be given as a continuous IV dose

alteplase

What drug’s MOA:

catalyzes the formation of plasmin from plasminogen

• induces rapid dissolution of thrombi

• both protective and target thromboemboli are broken down which can cause generalized lysis → hemorrhage

alteplase

What drug do we use for an acute ichemic stroke to decrease neuronal death, Pulmonary embolism treatment, central venous catheter/dialysis catheter clearance?

alteplase

What is the major toxicity of alteplase?

hemorrhage or hemorrhagic stroke

What are 7 absolute contraindications of alteplase?

• prior intracranial hemorrhage

• known structural cerebral vascular lesion

• known malignant intracranial neoplasm

• ischemic stroke within 3 months

• suspected aortic dissection

• active bleeding or bleeding diathesis (not including menses)

• significant close-head trauma or facial trauma within 3 months

What are 7 relative contraindications of alteplase?

• uncontrolled HTN

• traumatic or prolonged CPR or major surgery wihtin 3 weeks

• recent (2-4 weeks) internal bleeding

• noncompressible vascular punctures

• pregnancy

• active peptic ulcer

• current use of warfarin and INR > 1.7

What drug’s MOA:

inhibits TXA2 synthesis → reduced platelet aggregation and vasoconstriction

aspirin

explain the effects and dose of aspirin

the effects last the life of the platelet (7-10 days) so repeated low doses will produce a cumulative effect on platelet function

What drug’s therapeutic uses include:

cardiovascular protection to reduce the risk of thrombotic events (prevention), as well as secondary prevention to reduce risk of a subsequent CV disease

aspirin

Explain aspirin and pregnancy

low doses of aspirin for certain medical conditions have not been shown to cuase fetal harm

What are 4 cautions for taking low dose aspirin?

• upper GI bleeds

• surgery (avoid use 1-2 weeks prior)

• hypersensitivty

• Reye’s syndrome

What is Reye’s syndrome associated with?

this is why we do not give children with a fever aspirin (viral illness + aspirin = Reye’s syndrome)

What are the irreversible and reversible P2Y12 receptor inhibitors?

irreversible: clopidogrel

reversible: ticagrelor and cangrelor

What rdug is an oral prodrug with an onset of 2 days that is metabolized by CYP2C19 to an anctive thiol metabolite

clopidogrel

What drug is given as an IV bolus and then infusion, has a Tmax of 2 minutes and you see a rapid return of platelet function after d/c

cangrelor

What drug is oral, has an onset of 2 hours, and is metabolized by CYP3A4 to active thiol metabolites

ticagrelor

what is therapeutically used in dual therapy with aspirin?

clopidogrel

What drug would be implicated and have decreased metabolism to its active form is a patient was a CYP2C19 poor metabolizer?

clopidogrel

What drug’s AE include thrombocytopenic purpura, brdyarrythmia, and dyspnea

ticagrelor

What is the GpIIb/IIIa receptor antagonist?

eptifibatide

What drugs MOA is:

blocks platelet aggregation → reversibly blocks fibrinogen binding and bridging of platelets → prevents platelet aggregation

eptifibatide (by blocking GpIIb/IIIa)

What reversal agent MOA:

highly cationic protein combines with acidic UHF (unfractionated heparin) and LMWH (low molecular weigh heparin) forming a stable complex that is excreted

protamine

What reversal agent MOA:

outcompetes warfarin at VKORC1

vitamin K

What reversal agent MOA:

increased the levels of vitamin K dependent coagulation factors II, VII, IX, X plus protein S and C

reversal agent for: urgent reversal of VKAs and DOACs

prothrombin complex concentrate

What reversal agent MOA:

specifically binds dabigatran and its active acyglucuronide metabolites

reversal agent for: oral direct thrombin inhibitor

idarucizumab