Angina 2&3

Question 1

nitrates are prodrugs, what are prodrugs?

Answer 1

drugs that need to be activated once they have been administered, once they have converted, they are active need to convert nitrate to nitric oxide

Question 2

what are the 3 main treatments of stable coronary artery disease ( angina and INOC- variant/ microvascular)

Answer 2

nitrates and nitrites
B- adrenoreceptor antagonists
CALCIUM CHANNEL BLOCKERS

Question 3

how do nitrates and nitrites work?

Answer 3

vasorelaxation-systemic vasodilatation -therapeutic effect

Question 4

what is the mechanism of vasodilation in nitrates and nitrites?

Answer 4

• converted to NO (reduced)
• This would activate guanylate cyclase, which would convert GTP to cyclic GMP
• This would activate protein kinase G – cause blood vessels to relax.

Question 5

how do nitrates and nitrites produce their anti-anginal effect?

Answer 5

• peripheral venodilatation decrease in-preload - and MVO2

- peripheral arterial& arteriolardilatation - decrease in :afterload and VO2

Question 6

what are the 3 ways that nitrates and nitrites are used clinically?

Answer 6

1-relief of acute angina attacks –GTN, amyl
2-nitriteprophylaxis of chronic angina –GTN, ISDN, ISMN
3-choice & mode of therapy

Question 7

what are 4 side effects of nitrates and nitrites?

Answer 7

1 flushing & throbbing headaches
2 postural hypotension & syncope (low bp- take sitting down)
3 reflex tachycardia & myocardial contractility (inc MOD- not desirable)
4 tolerance
depletion of thiol (-SH) groups
physiological adaptation

Question 8

name 1 problems associated with nitrates

Answer 8

• must pass first pass metabolism

-

Question 9

how long is a nitrate free period?

Answer 9

8-10 hours

Question 10

what is the pharmacological action of b-adrenoceptor antagonists?

Answer 10

antagonise the effects of sympathetic nervous activation (i.e. noradrenaline & adrenaline) at β-adrenoceptors

Question 11

how many subtypes of beta-adrenoceptors are there?

Answer 11

3 but focus on 1 and 2
1-ARs –heart & kidney
2-ARs –heart, smooth muscle (e.g. vascular & bronchial)
3-ARs –adipocytes

Question 12

what are the two subclasses of b-Blockers?

Answer 12

1-‘non-selective’ –e.g. propranolol

2- B1-receptor selective (‘cardioselective’) –e.g. atenolol

Question 13

what happens when b2 adrenoceptors activate?

Answer 13

• When B2 activate in blood vessels- relax
• When in lungs – cause bronchioles to dilate
• When activated on heart reduce force of contraction

Question 14

how do b-b produce their anti-anginal effect?

Answer 14

haemodynamic effects dec myocardial O2demand
dec myocardial contractility
dec heart rate
dec system blood pressure

Question 15

what is the first line treatment for prophylaxis of chronic stable angina

Answer 15

beta-adrenoceptor antagonists

Question 16

what are the two classes of drugs used to treat chronic stable angina classified based on?

Answer 16

where they are eliminated:
1 eliminated via hepatic metabolism
2 eliminated unchanged via the kidney

Question 17

what are the features of drugs eliminated via hepatic metabolism?

Answer 17

more lipid soluble
almost completely absorbed from the gut
largely metabolised in the liver
very variable bioavailability
short plasma half-life

Question 18

what are the features of drugs eliminated via the kidney?

Answer 18

more water soluble
incompletely absorbed from the gut
largely eliminated unchanged
less variable bioavailability
longer plasma half-life

Question 19

what happens if you withdraw a Beta-blocker from treatment abruptly?

Answer 19

rebound phenomenon- increase force of contraction and MOD on heart- don’t stop taking unless doctor says so/ dose tapered down slowly- risk of angina agitation

Question 20

what are some adverse side effects of beta-blockers?

Answer 20

bronchoconstriction -exacerbation of asthma
peripheral vasoconstriction -cold extremities
myocardial depression -risk of heart failure
masking of signs of impending hypoglycaemiasexual dysfunction
poor patient compliance
CNS disturbances –nightmares, depression, confusion
inc LV size =inc myocardial O2consumption

Question 21

what is the pharmacological action of Calcium channel blockers?

Answer 21

inhibit entry of Ca into cells via voltage-gated calcium channels i.e. if heart(node cells) blocks entry of calcium cells it reduces force of contraction

Question 22

what are the vascular effects that CCB have?

Answer 22

block of Ca influx into arterioles -arteriolar dilatation

Question 23

what are the two mechanisms of anti-anginal effects of CCB?

Answer 23

Reduced myocardial O2 demand

Increased myocardial blood flow

Question 24

What is CCB a first line treatment for?

Answer 24

chronic stable angina

also for management of variant angina

Question 25

what does sublingual mean?

Answer 25

under tounge

Question 26

what does buccal mean?

Answer 26

between cheek and gum

Question 27

what are the 3 miscellaneous treatments of SCAD?

Answer 27

1-Potassium channel openers
2-Sinus node (Ifcurrent) inhibitors
3-Late Sodium Current Blockers

Question 28

what are the two revascularisation procedures?

Answer 28

Percutaneous Coronary intervention (PCI)-balloon

Coronary artery by-pass graft (CABG) -sew

Question 29

when do you consider a 3rd anti-anginal drug?

Answer 29

when 2 don’t satisify