CVS Flashcards
Captopril
ACE inhibitor inhibits Ang I conversion to Ang II vasoconstriction no reflex sympathetic stimulation splits off a dipeptidyl segment from - ACE, bradykinnin, substance P, stem cell regulator peptide feedback increase in renin Ang I is diverted to Ang 1-7 ADR: hypotension, hyperkalameia, cough, rahses, angioedema, dysgeuisia, airway obstruction, foetopathy, granulocytopenia and proteinuria, ac. renal failure (in pt with bilateral renal artery stenosis)
kinnins
acute vasopressor
cough
angioedema
stem cell regulator peptide
cardioprotective
greater fall in BP by captopril
when Na has been depleted
CHF
renovascular, accelerated and malignant hypertension
Captopril pk
70% oral food reduce absorption excretion in urine half life- 2 hour action - 12 hours
food reduce absorption of all ace inhibtors except
enaliprilat, trandolapril (only delayed)
enalapril
desterified into enaliprilat, injectable more potent slow onset longer duration
lisinopril
lysine deravative of enalprilat oral slow absorption, incomplete duration longer decrease in vr, and co
perindopril
long acting slow onset 20% perindoprilat extensive metabolism
fosinopril
phosphinate
glucuronide conjugated
liver, urine - elimination
First dose hypotension
fosinopril
Ramipril
extensive tissue distribution- bound drug
8-18 hours- t half life
quinapril
prodrug carboxyl - quinaprilat
bound to tissue
elimination urine, bile
biphasic half life
quinapril - 2- 24 hours
trandolapril - 10-24 hrs
trandolapril
carboxyl prodrug
40-60%
eliminated urine, faeces