anti-coagulant/anti-platelet_PHARM Flashcards
Anti-coagulant drugs
- heparins
- heparin
- LMWH - warfarin
- DOACs
- Direct thrombin inhibitors (dabigatran)
- Direct Xa inhibitors (endoxaban, rivaroxaban, apixaban)
Platelet activation
- Thrombin (IIa)
- Collagen
- PAF
- TXA2
- ADP
Anti-platelet drugs
- COX inhibitors
- ASA - P2Y12 Receptor Inhibitor
- Clopidogrel
- Prasugrel
- ticagrelor
- ticlopidine - GPIIb/IIIa inhibitor
- ABCIXIMAB
Heparin
MOA
- Bind to anti-thrombin
- increases anti-thrombin affinity for Xa and IIa
- also binds and inhibits intrinsic coagulation factors (XII, XI, IX, X, II)
Heparin
Route, 1/2 life
Route: IV
1/2 life: 60-90minutes
D/C 4hours before surgery
Heparin
Reversal agent
1mg protamine sulfate : 100U heparin
binds heparin-anti-thrombin complex; stronger inhibition IIa
Heparin
Dosage and theraputic monitoring
aPTT
60-80 seconds
Therapeutic monitoring
- aPTT
- Platelet count
AE Heparin
HIT
- heparin induced thrombocytopenia
- drop platelets > 50%
- 2-3 weeks therapy
- D/C heparin
SE Heparin
GI bleeding
hematomas, hemorrhages
melena stools
haematuria
HIT
Heparin
Contraindications
Hemorrhages, bleeding
HIT
anti-coagulation, anti-platelet therapy
brain, spinal, eye surgery
Heparin
Special populations
reduce dosage in old people, osteoporosis
safe in pregnancy, doesn’t cross placenta
Anti-coagulants for HIT
Fondaparinux*
DOAC (Argatroban, dabigatran)
danaparoid*
*safe in pregnancy
LMWH
MOA
bind anti-thrombin
increase affinity for Xa > IIa
List of LMWH
enoxaparin
dalteparin
fondaparinux (irreversible, no antidote)
LMWH
reversal agent/antidote
protamine sulfate
1mg per 100U
only works on enoxaparin and dalteparin (IIa)
LMWH
Dose, half life
dosage
- weight based
half life
- up to 6 hours
D/C
- 24 hours before procedure
LMWH
monitoring
No monitoring needed
Lower risk of HIT
Can look at aPTT
LMWH
SE and AE
higher risk of bleeding than heparin
decrease dosage in liver, kidney disease, old age, low body weight
Contraindications
anti-platelets, anti-coagulation, bleeding disorders/conditions
Warfarin
MOA
inhibits VKORC1
inhibits activation Vitamin K and formation Vitamin K dependent coagulation factors (VII, IX, X, II)
Warfarin
route, dose
PO
dosing based on INR (2-3 seconds)
Warfarin
Therapeutic monitoring
INR (daily, 2-3x per week, weekly, monthly)
Warfarin
Education
Soft tooth brush
medic alert bracelet
electric razor
stop 5 days before surgery
Warfarin antidote
vitamin K (phytonadione)
fresh frozen plasma
warfarin
Contraindications
pregnancy , breast feeding
hemorrhage
antiplatelets, anticoagulants, thrombocytopena
spine, brain, eye surgery
vitamin K deficiency
alcoholism
warfarin
Foods/ drugs decrease effect
Foods
- canola oil, soyabean, mayonase, leafy green
drugs
- oral contraceptives
- vitamin K
- AEDs
Warfarin
Drugs that increase bleeding
acetaminophen
anti-platelets
anti-coagulants
azoles
amiodarone
cimetidine
TMP-SMX
Direct thrombin inhibitors
Dabigatran
argatroban IV
Dabigatran
Route, Dose, monitoring
PO
same dosage
no monitoring
Antidote dabigatran
idaricuxumab
Dabigatran
MOA
binds II directly
- free
- clot
binds XIII directly
- prevents insoluble fibrin
SE
Dabigatran
GI upset, ulcers, bleeds
Rx. PPI
Drugs that increase
Dabigatran
P-glycoprotien (kidney) inhibitors
- verapamil
- amiodarone
- azoles
Contraindications
Dabigatran
- GI
- hemorrhages
- pregnancy
- liver disease
- kidney disease
Direct Xa inhibitors
apixaban
rivaroxaban
endoxaban
MOA
Rivaroxaban
binds Xa directly
antidote rivaroxaban
andexanet alphaanti
anti-platelet drugs
- aspirin
- COX inhibitor - P2Y12 inhibitors
- ticagrelor
- clopidogrel
Aspirin
MOA
< 325mg (anti-platelet function)
inhibition COX1
- inhibits vasoconstrictino
- inhibits platelet activation (inhibition AA to TXA2)
> 325mg
inhibition COX 2
- inhibits vasodilation (decrease GI and kidney blood flow, increase MI)
_ decrease mucous, bicarb, increase acid
- inhibits PGI2 formation (prevention vasodilation, platelet inhibition)
Aspirin SE
Reyes syndrome (brain swelling, fatty liver, organ failure) < 18 years
Salicylism (old age)
GI bleeding, hemorrhages (Silent)
Kidney damage
MI, stroke
Premature closure ductus arterosus and still birth
Health teaching aspirin
no paediatrics < 18 years
d/c old age
monitor tinnitus
smallest dose shortest time
no BP > 150mmHg
D/C last term
monitor melena stools
Clopidogrel, Ticagrelor
MOA
inhibitioin P2Y12 receptor
prevention platelet activation
Clopidogrel
SE
GI upset and bleeding
Rx. PPI
TTP
Thrombotic thrombocytopenia
monitor platelets
Ticagrelor
SE
Gout
TTP