1 Anti-hypertensive Flashcards

1
Q

What are the mechanisms involved in controlling BP?

IMPT!

A

Short term -> Sympathetic Activity (on heart and smooth muscles)

Long term -> RAAS

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2
Q

Name 4 classes of anti-hypertensives

A

ACE-I , AT1 blockers
Beta blockers
Calcium channel blockers
Diuretics

ACE-I: angiotensin-converting enzyme inhibitors
AT1 blockers: angiotensin II receptor type 1 antagonist

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3
Q

Why do we not prescribe both ACE-I & Angiotensin II receptor type 1 antagonists together?

A
  • Efficacy is not additive (reach saturated stage of block Angiotensin pathway)
  • May lead to additive adverse effects e.g. worsen renal function or hyperkalemia more

both work on the same pathway /:

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4
Q

Name 3 ACE-I

A

Lisinopril, Captopril, Enalapril

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5
Q

MoA of ACE-I

vvv IMPT!

A
  1. inhibits ACE enzyme
    decreases Angiotensin II formation
    - decreases vasoconstriction → decreases peripheral vascular resistance
    +
    - decreases aldosterone secretion → decrease salt + fluid retention
    Hence decreased BP
  2. blocks inactivation of bradykinin (additional effect)
    → increases NO and prostaglandin production
    → increases vasodilation
    Hence also decreased BP

see diagram on pg 13

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6
Q

Name 4 clinical uses for ACE-I

A
  1. Hypertension
  2. Cardiac failure (reduce preload and afterload)
  3. following MI
  4. Renal insufficiency

Renal insufficiency is poor function of the kidneys that may be due to a reduction in blood-flow to the kidneys caused by renal artery disease.

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7
Q

Name 4 adverse effects of ACE-I.
What is ACE-I contraindicated in?

A
  1. severe hypotension
  2. acute renal failure (due to decrease in aldosterone secretion)
  3. hyperkalemia (due to decrease in aldosterone secretion)
  4. angioedema & dry cough (bradykinin & substance P)

contraindication: pregnancy (damage renal function of fetus)

recall aldosterone reabsorb Na+ and water, excretes K+

recall ACE-I decrease Angiontensin II -> decrease aldosterone
recall ACE-I blocks inactivation of bradykinin -> a lot of bradykinin

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8
Q

Name 5 angiotensin II receptor type 1 receptor antagonists

A

Losartan
Valsartan
Candesartan
Irbesartan
Telmisartan

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9
Q

MoA of (Angiotensin II receptor type 1) AT1 blockers

A

binds to AT1 receptor and blocks action of Angiotensin II (vasoconstriction, ADH secretion, stimulates thirst, aldosterone production)
→ decrease BP

AT1 receptor receives signal from Angiotensin II but this drug cut queue and block Angiotensin II
Competitive inhibitor

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10
Q

Name 1 adverse effect of (Angiotensin II receptor type 1) AT1 blockers.
What is AT1 blockers contraindicated in?

A
  • Less / no dry cough (as compared to ACE-I)
  • Same contraindication: pregnancy
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11
Q

Name 3 (β1, β2) non-selective beta blockers

A
  1. Propanolol
  2. Pindolol
  3. Carvedilol

blocks β1 and β2 equally well

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12
Q

Name 3 cardioselective β1 blockers

A
  1. Atenolol
  2. Bisoprolol
  3. Metoprolol

higher affinity for β1 doesn’t mean doesn’t block β2 at all

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13
Q

Name a mixed (3rd generation) beta blocker

A

Nebivolol

  • β1 selective in low dose / fast metabolizers (majority of population)
  • Non-selective in high dose/ slow metabolizers
  • also has vasodilatory effects through ↑ NO release
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14
Q

MoA of beta blockers in cardiac myocytes

A

block β1
→ reduce cAMP
→ reduce PK A
→ reduce activation of Ca2+ channel
→ less Ca2+ get into cytosol
→ less Ca2+ release from sarcoplasmic reticulum
→ less activation of actin-myosin complex
→ reduce contractility of cardiac muscles

see diagram on pg 18

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15
Q

Which beta blockers are also approved to treat heart failure?

lower BP + treat heart failure wow

A
  • Carvedilol
  • Bisoprolol
  • Metoprolol
  • Nebivolol
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16
Q

Name 5 clinical uses for beta blockers

A

1. Hypertension
2. Cardiac failure

3. Following MI
4. Arrhythmia
5. Anxiety disorders (not first line)

17
Q

Name 6 adverse effects of beta blockers
What is beta blockers contraindicated in?

Contraindication - MUST KNOW!

A
  1. Hypotension
  2. Bradycardia (blocks β1-AR of heart → ↓ contractility and HR)
  3. AV nodal block - useful for tachycardia
  4. Reduced exercise capacity (↓ contractility → ↓CO)
  5. Bronchoconstriction - asthma
  6. CNS: Vivid dreams, clinical depression (“beta-blocker blues”)

Contraindications: diabetic patients (because it will mask the symptoms of hypoglycemia) - MUST KNOW!

no feedback to tell if hypoglycaemia because heart cannot beat fast (blocked by β blocker)
patient may fall into hypoglycaemic coma

18
Q

Diuretics

specifically Thiazides

note that Thiazides (Indapamide) was tested in CA2 MEQ

A