ace ihibitors

Question 1

ace and diaretics used for?

Answer 1

hyperntesniom, LVH, diabetic neuropathy, heart failure, secondary prevention of MI and stroke

Question 2

angiotensin II?

Answer 2

increase aldosterone, sympathetic tone, Ca2+ in VSMC, thirst and ADH secretion

decrease baroreceptor reflex.

this all cuase BP to raise

Question 3

first aceI?

Answer 3

catpropril from venom of snake bothrops jararaca.

captopril was mae by QSAR and adding a thiol (-SH) group

Question 4

ace ihibit -

Answer 4

bioisosteric group variation ont he drug alters ACEi’s PKPD profile

ACEi work by accuying active site, normally taken by angiotensin I’s proline residue

in addition, the -COOH (or -SH) of the ace inhibitor blocks the catalytic potential of the Zn2+ ion in the ACE active site.

Question 5

esterified pro-drugs?

Answer 5

carboxylated acei (-COOH). they are more potent and tolerable than SH-.

ramipril is desterified by the gut and hepatic esteraes to its active metaolite ramiprilat.

Question 6

adr and contraindications of ACEi?

Answer 6

ADR

dry persitent cough, thought o be a result of ACEi blcking degredation of bradyknini in the bronchial mucosa (kininase II=ACE)

hypotension

facial angioedema (rare/chronic use)

hyperkalaemia

contraindications

pregnancy

renal artery stenosis where AII mediated pressure gradient is required to maintian GFR

Question 7

ace can be given with

Answer 7

calcium channel blockers and diuertic

Question 8

saralasin?

Answer 8

first ARB - could’t be given orally

Question 9

arb

Answer 9

bings to at1 leaving at2 open for AII. binding to AT2 in cerbral blood is cerebro protective and lowers incidence of CVA. At2 has oppsotive effdect sof AT1

Question 10

Arb adr and contra?

Answer 10

adr

hypotension

dry cough

angiodema

hyperkalaemia

contraindications

pregnancy

previous sensitivity to ACEi

renal artery stenosis where AII mediated pressue gradient is required to maintain GFR

Question 11

digoxin?

Answer 11

cardiac glycoside

comprised of an aglycone head wchich confers most of the bioactivity and a glycone tail whidch determines the oral bioavaiabilty

it inhibits the brainstem cardiac centre neurones.

increased parasympathetic vagal nerve stimultion ofthe AV node slows the rhythm

Question 12

digoxin adr and cons?

Answer 12

adr

nausea and vomiting

CNs distubrances, hallucinations

biogeminal cardiac arrythmias

hyperkalaemia

conta

renal impairment

AV heart block