Antihypertensives

Question 1

Name 4 first line treatments for hypertension

Answer 1

1. ACE-Inhibitors, AT I Blockers
2. Beta blockers
3. Calcium channel blockers
4. Diuretics (Thiazides)

Question 2

Name 3 second line treatments for hypertension

Answer 2

1. Alpha blockers
2. Mineralocorticoid receptor antagonists
3. Hydralazine

Question 3

Name 2 ACE-I and give their suffix

Answer 3

Lisinopril, enalopril, captopril
Suffix is pril

Question 4

Give 2 MOA of ACE-I

Answer 4

Overall decrease in BP by:
1. Inhibiting conversion of Ang I to Ang II (causing decreased vasoconstriction and aldosterone)
2. Inhibiting breakdown of bradykinin (causing increase in NO and PG thus increasing vasodilation)

Question 5

Give 4 clinical uses of ACE-I

Answer 5

1. Hypertension
2. Cardiac failure
3. Renal insufficiency
4. Following myocardial infarction

Question 6

Give 5 ADRs of ACE-I

Answer 6

1. Severe hypotension
2. Hyperkalemia
3. Acute renal failure
4. Dry cough
5. Angioedema

Question 7

How does ACE-I cause dry cough?

Answer 7

Increased accumulation of bradykinin and PG which is postulated to increase sensitivity of bradykinin-dependent airway sensory nerve fibres

Question 8

How does ACE-I cause angioedema?

Answer 8

Increased PG and NO production causes inflammatory like responses like vasodilation, thus causing extravasation of plasma fluid into interstitial space

Question 9

ACE-I is contraindicated in

Answer 9

Pregnancy (due to increase risk of fatal renal failure)

Question 10

Name 2 AT1 blockers and give their suffix

Answer 10

1. Losartan, Valsartan, Candesartan, Irbesartan, Telmisartan
2. suffix is -sartan

Question 11

MOA of Angiotensin II Type 1 blockers

Answer 11

Directly binds to Ang II Type 1 receptors, which prevents the binding of Ang II, thus decreasing Ang II effects, eventually lowers BP (similar to ACE-Is)

Question 12

Which side effect of ACE-I is reduced with AT 1 blocker and why?

Answer 12

Reduced dry cough / productive cough.
AT 1 blocker does not interfere with breakdown of bradykinin

Question 13

Name 3 non-selective beta blockers

Answer 13

1. Propanolol
2. Pindolol
3. Carvedilol

Question 14

A non-selective beta blocker that can be used to treat both hypertension and heart failure

Answer 14

Carvedilol

Question 15

Name 3 cardioselective beta 1 blockers

Answer 15

1. Atenolol
2. Bisoprolol
3. Metoprolol XL / metoprolol succinate

Question 16

Name 2 cardioselective beta 1 blockers that can be used to treat both hypertension and heart failure

Answer 16

Bisoprolol and metoprolol XL

Question 17

Name a 3rd generation / mixed beta blocker

Answer 17

Nebivolol

Question 18

Give 2 MOA / features of nebivolol

Answer 18

1. Dose dependent selectivity: cardioselective at low doses, but non-selective at high doses
2. Vasodilation effect due to NO release

Question 19

Give 5 clinical uses of beta blockers

Answer 19

1. Hypertension
2. Cardiac failure
3. Arrythmias
4. Following myocardial infarction
5. Anxiety disorders

Question 20

Give 6 ADRs of beta blockers

Answer 20

1. Hypotension
2. Bradycardia
3. Bronchoconstriction especially in asthmatics
4. AV nodal block
5. Decreased exercise capacity
6. CNS Effects: vivid dreams, CNS depressant (beta-blocker blues)

Question 21

Name the 2 types of beta blocker blockades

Answer 21

1. beta 1 blockade
2. beta 2 blockade

Question 22

How does beta 1 blockade result in decreased cardiac contraction?

Answer 22

Inhibits activation of adenylyl cyclase, thus inhibiting cAMP production, causing inhibition of PKA, thus inhibiting CICR, decreasing formation of Ca-calmodulin complex, decrease activation of MLCK, inhibit actvation of myosin LC, thus decrease contraction

Question 23

How does beta 2 blockade cause bronchoconstriction / smooth muscle contraction

Answer 23

Inhibit cAMP production, thus inhibiting phosphorylation of MLCK, decrease bronchodilation, thus increase bronchoconstriction

Question 24

Which part of the nephron do thiazides work at?

Answer 24

Distal convoluted tubule

Question 25

MOA of thiazides

Answer 25

Inhibits Na+Cl- reabsorption by blocking the apical Na+ Cl- cotransporter of the DCT cells, leading to increased activity of the basolateral Na+ Ca2+ exchanger, thus enhancing calcium reabsorption

Question 26

Name 2 thiazides

Answer 26

1. Hydrochlorothiazide 2. Indapamide

Question 27

Name a class of drugs that interferes with thiazide action and explain why

Answer 27

NSAIDs Action of thiazides depend on renal PG synthesis. NSAIDs reduce PG synthesis, thus interfere with thiazide action

Question 28

Name 4 clinical uses for thiazides

Answer 28

1. Hypertension 2. Congestive heart failure 3. Nephrolithiasis due to idiopathic hypercalciuria 4. Nephrogenic diabetes insipidus

Question 29

Name 6 ADRs of thiazides

Answer 29

1. Hypokalemia metabolic alkalosis 2. Hyponatremia 3. Hyperglycemia 4. Hyperlipidemia 5. Hyperuricemia 6. Hypercalcemia

Question 30

Name 3 alpha-1 adrenergic antagonists and state their suffix

Answer 30

1. Prazosin 2. Alfuzosin 3. Terazosin Suffix: -zosin

Question 31

MOA of alpha 1 adrenergic antagonists

Answer 31

Antagonises / reduces alpha 1 mediated vasoconstriction effect, which keeps vessels dilated, thus increasing TPR which lowers BP

Question 32

Alpha-1 antagonists are safe to use in 2 kinds of patients

Answer 32

1. Renal impairment: No effect on renal blood flow and GFR 2. Pregnant patients: No known teratogenicity

Question 33

Name 3 common early ADRs of alpha-1 antagonists

Answer 33

1. Reflex tachycardia 2. Palpitations 3. Orthostatic hypotension

Question 34

Name 3 other ADRs of alpha-1 antagonists

Answer 34

1. Depression 2. Urinary frequency 3. Flushing