Antiplatelet, Anticoagulant, Thrombolytic Flashcards
ASA is reversible/irreversible platelet inhibitors?
irreversible
Drugs that are P2Y12 receptor inhibitor
Clopidogrel, Prasugrel, Ticagrelol, Ticlopidine
P2Y12 receptor inhibitor which shows irreversible platelet inhibition
Clopidogrel, Prasugrel
Direct acting Reversible platelet inhibitor
Ticagrelor
If patient is allergic to Ibuprofen, can a low dose ASA is used?
ASA is not used if patient allergic to any of NSAIDs
RIng present in Ticagrelor
Cyclopentyl-triazolo-pyrimidines
RIng present in Prasugrel & Clopidogrel
Thienopyridine ring system
ASA shows antiplatelet effect for
7 to 10 days.
Drug having CYP2C19 drug interactions.
Clopidogrel (Prodrug activated by CYP2C19). Clopidogrel is a prodrug that requires conversion to thiol metabolite and this thiol group binds with ADP receptor. INtermediate formed is 2-oxo-clopidogrel. Proton pump inhibitor are inhibitors of CYP2C19 and produce Drug interaction. Less interaction with pantoprazole
Is prasugrel a prodrug?
Yes. Activated by hydrolysis in intestine. and metabolized by 3A4 & 2B6
Why Ticlopidine Not used ?
serious agranulocytosis and neutropenia side effects.
MOA of Clopidogrel, prasugrel, ticagrelor and ticlopidine?
1) blocks ADP induced platelet aggregation.
2) Interact with glycoprotein IIb/IIIa (a fibrinogen receptor) resulting in an inhibition of the fibrinogen to form aggregated plug
The minimum dose required ASA to produce antiplatelet effect ?
60 to 80 mg
Strength of schedule II aspirin
80 mg (chewable) behind the counter
Which is Not prodrug? Ticagrelor Ticlopidine Prasugrel Clopidogrel
Ticagrelor
Antiplatelet effect of Ticagrelol last for ?
2 to 8 hours
the drug of choice in patient usually cannot tolerate ASA or in patient with allergic to ASA.
ADP inhibitor
Ticlopidine
hemorrhagic complications(Agranulocytosis,thrombocytopenia ,neutropenia ), Rash and diarrhea CBC 2 wk for 1st 3 months
antiplatelet agents used in stroke prophylaxis in cerebrovascular ischemia or aft er prosthetic valve replacement
Dipyridamole and cilostazol
antiplatelet agents used for intermittent claudication.
cilostazol
Contraindication of P2Y12 receptor inh.
hematopoietic disorders
Hemorrhagic diathesis/intracranial bleeding
severe liver dysfunction.
Storage conditions of P2Y12 receptor inh.
Store at room temperature. Dispense in light-resistant containers. Blister packs should not be exposed to light.
Does clopidogrel require renal dose adjustment?
Clopidogrel hepatic elimination, renal dose adjustment is not necessary.
Mechanism of action of abciximab, eptifibatide , and tirofiban
parenteral agents that reduce the interaction of platelets via the GPIIb/IIIa receptors to fibrinogen.
monoclonal antibody directed against GPIIb/IIIa
Abciximab is the Fab fragment of a monoclonal antibody directed against GPIIb/IIIa
Structure AND action of eptifibatide?
cyclized heptapeptide with high affi nity for the fi brinogen receptor
Agents used after a myocardial infarction or during angioplasty and stent placement
Glycoprotein IIb/IIIa inhibitors
How are Thienopyridine used?
are used to decrease clot formation aft er
angioplasty and stenting procedures and are oft en combined with aspirin or GPIIb/IIIa inhibitors.
Aspirin is used for the
prophylaxis of myocardial
infarctions and, in conjunction with other agents, it decreases thrombosis aft er coronary stenting
abciximab can causes hypotension, nausea, vomiting, and atrial fi brillation.
Tirofiban + Heparin = thrombocytopenia
glycoprotein IIb/IIIa also known as
integrin alpha, beta receptors
Antiplatelet Indicated for unstable angina
Eptifibatide and tirofiban
Antiplatelet Indicated during and after coronary artery procedures to prevent platelet aggregation.
Eptifibatide and tirofiban
Antiplatelet Indicated for NSTEMI
Eptifibatide and tirofiban
MOA of dipyridamol
TXA2 Inhibitor
mechanism of action of Acetyl Salicylic Acid (ASA) that results in greater effect as an antiplatelet drug is
Irreversible acetylation of cyclooxygenase
ASA 80-162 mg daily indication
stable & unstable angina, NSTEMI, STEMI
ASA 160 mg daily x 35d indication
Prophylaxis of VTE after total hip replacement
ASA dose for Primary coronary events prevention, Secondary prevention of ischemic stroke
80-325 mg daily po
DOC for patient allergic to Ibuprofen/ aspirin
CLopidogrel
Patient with Acute Coronary Syndrome (ACS) had STENT placed.How long is the combination of ASA and Clopidogrel used
1 year
Fibrinolytic/Thrombolytic
Plasmin degrades the fibrin mesh. Plasmin need to be activated form plasminogen and this is done by tissue plasminogen activator.
Streptokinase obtained from
Derived from beta-hemolytic streptococci cultures.
Both streptokinase and urokinase lack this specificity and act on free plasminogen inducing generalized thrombolytic state
Tissue Plasminogen Activators (tPAs) have low affinity for free plasminogen but a very high affinity for plasminogen bound to fibrin in a thrombus.
WHich thrombolytic have greater specificity to older clots than newer clots
Alteplase
Contraindiaction of thrombolytic
acute stroke >3 hours of stroke myocardial infarction >6 hours. Recent head trauma/cranial tumor Previous hemorrhagic stroke Active internal bleeding Major surgery within 2 wks Active peptic ulcer, diabetic, blood pressure, pregnancy
Don’t give second streptokinase within 6 months of the first treatment
Can produce allergic reactions (urticaria). Give antihistamine before starting the treatment. Because allergic reactions are more common with streptokinase urokinase.
Bronchospasm
Urokinase obtained from
A two-chain serine protease obtained form human kidney cell culture.
prodrug of streptokinase
Anistreplase
Thrombolytic Not used for MI and Stroke
Streptokinase
Thrombolytic having most Fibrin specificity
Tenecteplase
fi rst orally active direct
thrombin inhibitor and is used to prevent stroke in patients with atrial fi brillation.
Dabigatran
Drugs indicated for recurrent stroke prevention
ACE Inhibitors
Warfarin
Rivaroxaban ( direct factor Xa inhibitor)
DAbigatran ( Direct factor IIa inhibitor)
Entacapone
Patients may be at increased risk for cardiovascular events such as myocardial
infarction, stroke, and cardiovascular death
Which group blocks the catalytic site in Anistreplase?
anisoyl group
Recombinant DNA-derived plasminogen activators (t-PA) with 527 and 355 amino acids.
Alteplase, reteplase, and Tenecteplase
Structure of heparin responsible for heparin induced thrombocytopenia
long chain penta saccharides. Heparin penta saccharides are natural products
WHat are Fractionated heparin
Dalteparin sodium (Fragmin) Enoxaparin sodium (Lovenox) Nadroparin calcium (Fraxiparine) Tinzaparin sodium (innohep)
MOA of Fractionated heparin or LMWH?
Selective to factor Xa and IIa
Name factor II, X,
Thrombin (factor II
Factor X Stuart Prower Factor
Which type of heparin have a more predictable pharmacokinetic profile with longer half-life?
LMWHs ( ….parins_)
Heparins, both LMWH and uFH are
mucopolysaachrides
Drug that is a synthetic pentasaccharide
Fondaparinaux