Pharmacology of the blood and blood clot Flashcards
(142 cards)
what’s the mechanism of aspirin
irreversible inhibitor of cyclooxygenase enzyme → ⭣TXA2 → antithrombotic
- blocks production of TXA2 by acetylation of a serine residue
- permanent for the platelets life (7-10 days)
what’s the “proper name” of aspirin
acetylsalicylic acid
what’s the use of aspirin
cardiovascular or cerebrovascular disease, Kawasaki disease
- acute coronary syndrome, ischemic stroke
- other indications → relief of moderate pain, headaches, inflammatory diseases and fever (including rheumatic fever), pregnant women with preeclampsia (low doses in the 2nd trimester)
adverse effects of aspirin
bleeding, gastric ulcer disease (⭣PGs), tinnitus, kidney injury (chronic aspirin use), allergic reactions (or DRESS syndrome), aspirin exacerbated respiratory disease
effect of aspirin in the kidneys
- low doses → uric acid retention
- high doses → uric acid excretion
what’s Reye syndrome
hepatic encephalopathy in children with viral illness when given aspirin
what are the contraindications of aspirin
- syndrome of asthma, rhinitis and nasal polyps
- children or adolescents w/ viral infections → reye’s syndrome
- increased alcohol consumption increases risk of bleeding
- hemophilia, liver disease, vitamin k deficiency → they’re all bleeding disorders
what medications are P2Y12 (ADP) receptor antagonist
clopidogrel, prasugrel, ticagrelor, ticlopidine
what’s the MOA of clopidrogel
P2Y12 receptor antagonist → changes shape of platelets →⭣ IIb/IIIa → no aggregation
- irreversible action
- it’s a prodrug → needs metabolic activation in the liver
- oral administration
what’s the use of P2Y12 receptor antagonist (like clopidogrel, prasugrel, etc.)
MAIN USE: cardiovascular disease (PCI), alternative to aspirin
- PCI = percutaneous coronary intervention → angioplasty and stenting
- can be used as a dual antiplatelet therapy (DAPT) w/aspirin in:
—-ST-elevation myocardial infarction (STEMI)
—-unstable angina/NSTEMI with recurrent isquemia
—-usually recommended for 1year after MI → then aspirin alone
adverse effects of P2Y12 receptor antagonists
bleeding, allergic reactions, neutropenia (ticlopidine → this one is irreversible)
thrombotic thrombocytopenic purpura → deficiency of ADAMTS13 → ⭡vWF multimerization
what are contraindications for P2Y12 receptor antagonist
- CYP2C19 inhibition by PPIs → less effect of clopridrogel
- cimetidine, amiodarone, omeprazole, etc.
- CYP2C19 inducers and opiods
- more risk of bleeding with: anticoagulants, NSAIDs and antidepressants
- nor effective in individuals with genetic polymorphisms of CYP enzimes
what meds are glycoprotein IIb/IIIa inhibitors
abciximab, eptifibatide, tirofiban
what’s abciximab
fragment of monoclonal antibody (Fab region vs GPIIb/IIIaR)
which med is stronger abciximab or tirofiban
abciximab
additional uses of tirofiban
- additionally from PCI can be used for acute coronary syndrome
- less risk of bleeding
mechanisms of abciximab
- glycoprotein IIb/IIIa inhibitors → inhibit binding of fibrinogen → inhibition of platelet agregation and thrombus formation
are glycoprotein IIb/IIIa inhibitors given orally?
NO
given by IV → used in the hospital
use of abciximab
high risk cardiovascular disease planning for PCI (Percutaneous Coronary Intervention → angioplasty)
used in prevention of thrombotic complications in high-risk patients with unstable angina(NSTEMI) going for PCI
adverse effects of glycoprotein IIb/IIIa inhibitors
thrombocytopenia, bleeding
**contraindication = px w/ platelets <100,000/mm3
what does Heparin due
mechanism = potentiates antithrombin → ⭣Xa activity, ⭣IIa (thrombin) activity
is heparin fast?
yes, it gives immediate anticoagulation
what do you have to monitor when giving heparin
aPTT (looking at the intrinsic pathway)
what types of heparin are there
unfractionated heparin
low molecular weight heparin
synthetic heparin