Hypertension Core Drugs Flashcards

1
Q

What are examples of angiotensin converting enzyme inhibitors?

A
  1. Ramipril
  2. Lisinopril
  3. Perindopril
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2
Q

What is the primary mechanism of action of ACE inhibitors?

A
-Inhibit the angiotensin converting 
enzyme
-Prevent the conversion of 
angiotensin I to angiotensin II 
by ACE
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3
Q

What is the drug target of ACE inhibitors?

A

Angiotensin converting enzyme

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4
Q

What are the main side effects of ACE inhibitors?

A
  1. Cough
  2. Hypotension
  3. Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)
  4. Foetal Injury (AVOID IN PREGNANT WOMEN)
  5. Renal failure (in patients with renal artery stenosis)-
  6. Urticaria/Angioedema
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5
Q

What type of drug are most ACE inhibitors?

A
  • Most ACE inhibitors (not lisinopril) are pro-drugs
  • require hepatic activation to generate the active metabolites required for therapeutic effects
  • Losartan and candesartan are pro-drugs. They require hepatic activation to generate the active metabolites required for therapeutic effects
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6
Q

Are ACE or angiotensin receptor inhibitors more effective?

A

Most trials indicate that angiotensin receptor blockers are not as effective anti-hypertensive agents as ACE inhibitors

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7
Q

What needs to be monitored when you take ACE inhibitors?

A

eGFR and serum potassium

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8
Q

How commonly prescribed are these drugs in 2020 in West London area?

A
  1. Angiotensin receptor blocker:
    - losartan: 13th
    - irbesartan: 57th
    - candesartan: 80th
  2. Calcium Channel Blockers:
    - amlodipine: 2nd
    - felodipine: 98th
  3. Thiazide/thiazide-like diuretics:
    - bendro-flumethiazide: 38th
    - indapamide: 46th
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9
Q

What are examples of calcium channel blockers?

A
  • Amlodipine

- Felodipine

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10
Q

What is the primary mechanism of action for calcium channel blockers?

A
  1. Block L-type calcium channels – predominantly on vascular smooth muscle. 2. results in a decrease in calcium influx, with downstream inhibition of myosin light chain kinase and prevention of cross-bridge formation
  2. resultant vasodilation reduces peripheral resistance
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11
Q

What is the drug target for calcium channel blockers?

A

L-type calcium channel

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12
Q

What are the side effects of calcium channel blockers?

A
  1. Ankle oedema
  2. Constipation
  3. Palpitations
  4. Flushing/Headaches
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13
Q

What type of calcium channel blocker has a higher degree of vascular selectivity?

A

Dihydropyridine type calcium channel blockers demonstrate a higher degree of vascular selectivity

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14
Q

What are examples of thiazide or thiazide -like diuretics?

A
  • Bendro-flumethiazide (thiazide)

- Indapamide (thiazide-like)

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15
Q

What is the primary mechanism of action of thiazide or thiazide like diuretics?

A
  1. They block the Na+, Cl- co-transporter in the early DCT
  2. . Therefore Na+ and Cl- reabsorption is inhibited
  3. As a result the osmolarity of the tubular fluid increases, decreasing the osmotic gradient for water reabsorption in the collecting duct
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16
Q

What is the drug target for thiazide or thiazide like diuretics?

A

Sodium/chloride

cotransporter

17
Q

What are the main side effects of thiazide or thiazide like diuretics?

A
  1. Hypokalemia
  2. Hyponatremia.
  3. Metabolic alkalosis (increased hydrogen ion excretion)
  4. Hypercalcemia.
  5. Hyperglycemia (hyperpolarised pancreatic beta cells).
  6. Hyperuricemia.
18
Q

In how long do thiazide and thiazide like diuretics lose their diuretic effects? Why do they still have an anti-hypertensive action?

A
  • within 1-2 weeks of treatment
  • continuing anti-hypertensive action appears to be due to vasodilating properties (these are more pronounced for the thiazide-like diuretics)
19
Q

What are examples of angiotensin receptor blockers?

A
  • Losartan
  • Irbesartan
  • Candesartan
20
Q

What is the primary mechanism of action of angiotensin receptor blockers?

A

These agents act as insurmountable (i.e. non-competitive) antagonists at AT1 receptor (found on kidneys and on the vasculature)

21
Q

What is the drug target of angiotensin receptor blockers?

A

Angiotensin receptor

22
Q

What is the main side effect of angiotensin receptor blockers?

A
  1. Hypotension
  2. Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)
  3. Foetal Injury (AVOID IN PREGNANT WOMEN)
  4. Renal failure (in patients with renal artery stenosis)