Blood Flashcards
list three antiplatelet (ADP receptor) drugs
clopidogrel
ticagrelor
prasugrel
clopidogrel, ticagrelor and prasugrel belong to which drug class?
Antiplatelets (ADP-receptor agonists)
list three indicatiosn for prescription of antiplatelet drugs?
- treatment of ACS
- prevention of coronary artery stent occlusion
- long-term secondary prevention of thrombotic arterial events in pts w cardiovascular, cerebrovascular and peripheral arterial disease
antiplatelet drugs are commonly prescribed with which other drug?
aspirin
MOA of antiplatelets?
prevent platelet aggregation by binding to ADP receptors (P2Y12 subtype) on platelet surface.
The MOA of antiplatelets is synergistic/additive with that of aspirin?
synergistic: ADP binding process is independant of the COX pathway
what is the most common adverse effect of antiplatelets?
Bleeding
GI upset (common)
Thrombocytpenia (very rare)
list contraindications to prescribing antiplatelets
pts with active bleeding
elective surgeries (should be stopped 7 days prior)
renal and hepatic impairment should be used with caution
clopidogrel is a pro-drug which requires metabolism by which hepatic enzyme?
cytochrome P450 (CYP enzymes)
which class of drug may inhibit the efficacy of clopidogrel?
CYP inhibitors i.e. omeprazole, ciprofloxacin, erythromycin
are ticagrelor and prusagrel also pro-drugs?
prasugrel yes- less suceptible to interactions
ticagrelor no- but interacts with CYP inhibitors possibly inc risk of toxicity
available preparation of clopidogrel?
only oral preparaption
low doses of clopidogrel require how long to reach their full anitplatelet effect?
up to a week
if rapid effect required what loading dose of clopidogrel should be prescribed?
this is followed by what maintainence dose?
300mg orally for ACS
once only before commencing maintainence dose of 75mg orally daily
how should clopidogrel use be comunicated to the pt?
used to reduce risk of MI or strokes and ot prolong life
if treatment following stent insertion emphasise importance of continuing treatment and usually for 12 months
is clopidogrel a reversible drug?
NO it is irreversible- takes up to 7-10 days (lifetime of a platelet) for its antiplatelet effect to wear off
what kind of drug is aspirin?
antiplatelet
common indications for aspirin use?
- treatment of ACS and acute ischaemic stroke
- long-term secondary prevention of thrombotic aarterial events in pts with cardiovascular, cerebrovascular and peripheral arterial disease
what is the MOA of aspirin?
irreversibly inhibits cyclooxygenase (COX) reducing production of factor thromboxane
how long does the antiplatelet effect of aspirin last?
the lifetime of a platelet
(platelets do not have a nuclues to synthesis new COX)
what are the common adverse effects assoc with aspirin?
GI irritation
peptic ulceration, haemorrhage, bronchospasm (hypersensitivity)
*life threatening in overdose*
why can aspirin not be given to children under 16 years?
risk of Reyes syndrome
life threatening illness affecting liver and brain
who should not be prescribed aspirin?
those with aspirin hypersensitivity
third trimester of pregnancy (prosaglandin inhibition may lead to premature closure of ductus arteriousus)
those with peptic ulcers (prescibe gastroprotection)
gout- can trigger ana cute attack
what prepararions of aspirin are available?
oral and rectal
how should aspirin be prescribed for 1. ACS and 2. acute ischameic stroke?
- 300mg loading dose followed by 75mg daily
- 300mg daily for 2 weeks
(75mg daily for long-term prevention fo thrombosis)
why should aspirin be taken with or after food?
minimise gastric irritation
*those who are high risk for GI upset should be coprescribed gastric protection i.e. omeprazole 20mg daily
name the 4 most common direct oral anticoagulants or DOACs?
apixaban, dabigatran, edoxaban, rivaroxiban
list two common indications for DOACs
- venous thromboembolism (DVT and PE)
- AF (prevent stroke and sytemic embolism)
what is teh MOA of DOACs?
act on the final common pathway of coagulation cascade:
apixaban, endoxaban, rivaroxaban inhibit activated factor X (Xa)
dabigatran inhibits thrombin (inhibits conversion of fibrinogen to fibrin)
what are the common adverse effects of DOACs?
bleeding: greater GI bleed risk than warfarin but lower risk of major bleed or intracranial haemorrhage
others: anaemia, GI upset, dizzness, elevated liver enzymes
DOACs should be avoided in which groups of people?
active, clinically significant bleeding
those with risk factors for major bleeding i.e. peptic ulcers, cancer, recent surgery
hepatic/ renal disease- DOACs can be esxcreted using CYP enzymes