A: 16-19 Flashcards
3 types of anti-PLT therapy
COX inhibitiors: Aspirin
Glycoprotein IIb/IIIa receptor inhibitor: Abciximab
ADP-R antagonists: Clopidogrel, Prasugrel, Ticagrelor
ADP זה כמו שהקלידו סתם במקלדת
כמו גרל
Clap your hand and pres on the tica
What is the result of blocking COX in PLT?
Decrease TXA2 –> Decrease stimulatory effect of PLT aggregation
Other name for Aspirin
Acetylsalicylic acid
Aspirin dosage amount: Anti-PLT vs. Anti-inflammatory
Anti-PLT(anti-thrombotic) requires lower dose than anti-inflammatory dose
Aspirin indications
Prevention and treatment of arterial thrombosis
Prevents MI, TIA, Ischemic stroke
Prophylaxis in arrhythmias
Aspirin side effects
GI toxicity
Nephrotoxicity Apirinnn=neprho
hypersensitivity rxn due to increased Leukotrienea
Hyperventilation metabolic acidosis A=A
Hyperthermia
Coma (overdose)
HSN
Tinnitus
Glycoprotein IIb/IIIa receptor inhibitor=
Abciximab
Abciximab
How to give and what is the molecule?
Parenteral
IgG Ab
Abciximab indications
Acute coronary syndrome (short period) - eg. unstable angina, MI
Used during PCI to prevent re-stenosis
Post angioplasty to prevent stenosis
Abciximab side effects
Bleeding
Thrombocytopenia with prolonged use
ADP-R antagonists
Clopidogrel
Prasugrel
Ticagrelor
Clopidogrel
Prasugrel
What are they as molecules?
Do they require activation?
Prodrugs
Activated by CYP450
Oral
What can block the activation of Clopidogrel, Prasugrel?
Omeprazole
Which ADP-R antagonists does not require activation?
Ticagrelor
יש לו שם קצת שונה אז בטח הוא תרופה חדשה
Clopidogrel
Prasugrel
Ticagrelor
Indications
- Acute coronary syndrome
- prevention of restenosis after PCI
- prevention and treatment of arterial thrombosis
Post angioplasty to prevent stenosis
Prophylaxis in arrhythmias
- from book table
Clopidogrel
Prasugrel
Ticagrelor
Side effects
- Bleeding
- GI disturbances
- Neutropenia (hematologic abnormality) - clopidogrel less hematotoxic!
-TTP: disseminated formation of small thrombi, PLT consumption and
thrombocytopenia (very rare, by toclopidine)
Heparin inactivates
- complexes with anti-thrombin-3
- irreversibly inactivates : Thrombin and factor Xa
VII
IX
XI
XII
Heparin drugs
Unfractionated Heparin
Low Molecular Weight Heparin: Dalteparin, enoxaparin)
Fondaparinux (fond of the parinux) - similar to LMWH
Dalte is like smaller than alpha
Unfractionated Heparin
What is it
How to give it
How to monitor?
Acidic polysaccharide polymer
IV, SC. ( we dont use I.M because can cause hematoma!)
aPTT : activated partial thromboplastin time
Low Molecular Weight Heparin
Name of the drug
Dalteparin
enoxaparin
Low Molecular Weight Heparin
How is it different than Unfractionated Heparin?
Selective for Xa
Higher bioavailability
Longer duration of action
Renal metabolism
- note: protamine sulfate reversal in only “partially effective “ with LMWH
Synthestic Heparin=
Fondaparinux
Fondaparinux target
More selective for Xa
Fondaparinux
How to give?
SC
Heparin indicactions
Acute and rapid anticoagulation
DIC
Which anticoagulation will we give during pregnancy?
LMWH
Heparin side effects
Bleeding (monitor with aPTT)
HIT “heparin induced thrombocytopenia”
Osteoporosis (chronic use)
heppaa
לחשוב על בהד 10 ועל הבחורה ששברה את הגב שזה מתקשר לאוסטאופורוסיס
Warfarin is a type of ______ anticoagulants
Coumarin
Warfarin MOA
Inhibit Vitamin K epoxidase reductase (VKOR)
Prevents post-trans. gamma carboxylation of factors II, VII, IX, X
Vit. K is important for which factors?
II VII IX X Protein C, S
Complete theraputic effect with Warfarin is achieved after
2-3 days
Warfarin drug info
Lipid soluble
Oral
Highly bound to plasma proteins (albumin; NSAID can displace it )
Warfarin metabolism
CYP450
CYP450 inducers
- reduce the anticoagulant, increase warfarin clearance
- barbiturates
- carbamazepine
- phenytoin
- rifampin,
Cytochrome P450 inhibitors (cg,
- amiodarone
-selective serotonin reuptake inhibitors,
- cimetidine
reduce warfarin’ s clearance and increase the anticoagulant