Antihypertensives

Question 1

What are the therapeutics effects of ACE inhibitors?

Answer 1

Vasodilations, increase in Na and water secretion

Question 2

What are the indications of ACE inhibitors?

Answer 2

Hypertension, heart failure, preserve renal function in diabetes

Question 3

What are some clinical considerations of ACE inhibitors?

Answer 3

Low renin in African patients reduces effect
Not in bilateral renal artery stenosis
Avoid in pregnancy

Question 4

List side effects of ACE inhibitors

Answer 4

Cough - reduced bradykinin breakdown
Hypotension, hyperkalaemia
Tachycardia, palpitations, anginal pain
Renal impairment
Head ache, nausea, angio-oedema, tase disturbace, vomiting, abdominal pain

Question 5

What are the therapeutics effects of AT1R antagonists?

Answer 5

Inhibit angiotensin-induced vasoconstriction and aldosterone release
Increase Na, water excretion

Question 6

What are the indications of AT1R antagonists?

Answer 6

Hypertension, heart failure, diabetic nephropathy, intolerance to ACE inhibitors

Question 7

List side effects of AT1R antagonists.

Answer 7

As ACE inhibitors

Question 8

What are some clinical considerations for AT1R antagonists?

Answer 8

Avoid in pregnancy and renal artery stenosis.

Question 9

What is the mechanism of action of Ca2+ channel blockers?

Answer 9

Block L-type (voltage-gated) Ca2+ channels, reducing Ca2+ entry into vascular and cardiac cells.

Question 10

What are the clinical effects of Ca2+ channel blockers?

Answer 10

Vasodilation, reduced cardiac contractility and atrio-ventricular conduction.

Question 11

Which group of Ca2+ channel blockers has predominantly vascular effects?

Answer 11

Dihydropyridines, e.g. nifedepine, amlodipine

Question 12

Which group of Ca2+ channel blockers has predominantly cardiac effects?

Answer 12

Non-dihydropyridines, e.g. verapamil, diltiazem

Question 13

What are the contraindications of Ca2+ channel blockers?

Answer 13

Hypertension, angina, tachydysrhythmia

Question 14

What are the side effects of Ca2+ channel blockers?

Answer 14

Orthostatic hypertension
Reduced myocardial workload, bradycrdia, dysrhythmia
Oedema, headache, syncope, nausea, face and neck flushing, diarrhoea

Question 15

What are the most commonly used diuretics in hypertension?

Answer 15

Thiazides

Question 16

What are the short term and long term effects of diuretics?

Answer 16

Short term: decrease blood volume, reducing CO

Long term: Normalise CO and decrease TPR

Question 17

What is the site of action of thiazides?

Answer 17

Na+/Cl- transporter in distal tubule.

Question 18

What is the site of action of loop diuretics?

Answer 18

Na+/2Cl- transporter in the loop of Henle

Question 19

What are the side effects of diuretics?

Answer 19

Hypokalaemia, hyperuricaemia, glucose intolerance, hypercholesteraemia, rash

Question 20

What are the side effects more common to loop diuretics?

Answer 20

Hypovolaemia, hearing impairment

Increased Mg2+, Ca2+ excretion

Question 21

What are the side effects of thiazides?

Answer 21

Dehydration, electrolyte imbalance, hypotension, dizziness

Pruritus, anorexia, urinary frequency, erectile dysfunction, reduce oedema.

Question 22

What is the first line pharmacological treatment for hypertension?

Answer 22

ACE inhibitors or AT1R or Ca2+ channel blocker or low-dose thiazide diuretic for > 65yo

Question 23

What is the second line treatment for hypertension?

Answer 23

ACE inhibitor (or AT1R) + Ca2+ channel blocker or
ACE inhibitor (or AT1R) + low-dose thiazide diuretic

Question 24

What is the third line treatment for hypertension?

Answer 24

ACE inhibitor (or AT1R) + Ca2+ channel blocker + low-dose thiazide diuretic

Question 25

What are the actions of beta-blockers in hypertension?

Answer 25

Decrease SNS in heart - reduce CO, HR and TPR Inhibit renin release, decreasing angiotensin II Reduces SNS outflow from CNS if lipid-soluble

Question 26

What are the indications for beta-blockers?

Answer 26

Angina, post-myocardial infarct, dysrhythmia, clinically stable heart failure

Question 27

What are the side effects of beta-blockers?

Answer 27

Reduced HR, force of contraction, cardiac disturbances Bronchoconstriction Hypotension, reduced blood glucose Increased peristalsis, flatulance Lassitude, nightmares, depressed mood, loss of libido.

Question 28

List SNS inhibitors that can be used in hypertension.

Answer 28

Beta-blockers CNS-acting: alpha2 receptor agonists, methyldopa (false transmitter with no post-ganglionic effect, alpha2 agonist) Alpha1 antagonists

Question 29

Give example of CNS-acting alpha2 receptor agonists.

Answer 29

Clonidine, methyldopa

Question 30

What is the mechanism of action of methyldopa (alpha-methyl NA)?

Answer 30

Alpha-2 receptor agonist in CNS, methylates NA at presynaptic terminals.

Question 31

What are the side effects of methyldopa?

Answer 31

Sedation, depression, fatigue, rebound hypertension on withdrawal.

Question 32

What are the indications for methyldopa?

Answer 32

Pregnancy

Question 33

What are the indications for clonidine?

Answer 33

Emergency hypertension, menopausal flushing

Question 34

What are the side effects of alpha1 receptor antagonists?

Answer 34

First dose syncope, postural hypotension, reflex tachycardia (less with selective), urinary urgency

Question 35

What are the indications of alpha1 receptor antagonists ?

Answer 35

Co-treatment in hypertension and benign prostatic hyperplasia (BPH)

Question 36

List "other" vasodilators used in hypertension.

Answer 36

``` Hydralazine (arteriolar) Cromokalim, minoxidil (arteriolar) - increase K+ channel permeability and hyperpolarisation Sodium nitroprusside (arterial and venous) - donates NO ```

Question 37

What are the indications for "other" vasodilators, e.g. hydralazine, cromokalim, minoxidil, sodium nitroprusside?

Answer 37

I.V. for emergency hypertension, resistant hypertension as adjuncts