Pharmacology of Hypertension Flashcards

Angiotensin converting enzyme (ACE) inhibitor Angiotensin receptor blockers Calcium channels blockers Thiazide / Thiazide-like diuretics

1
Q

What are angiotensin converting enzyme (ACE) inhibitors used for?

A
  • ACE inhibitors are used to treat hypertension, heart failure, and acute myocardial infarction
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2
Q

What is the primary drug target of angiotensin converting enzyme (ACE) inhibitors?

A
  • Angiotensin converting enzyme
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3
Q

What is the drug target type of angiotensin converting enzyme (ACE) inhibitors?

A
  • Enzyme antagonist
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4
Q

What is the location of action of angiotensin converting enzyme (ACE) inhibitors?

A
  • Endothelium (Lungs & Kidneys)
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5
Q

What is the mechanism of action of angiotensin converting enzyme (ACE) inhibitors?

A
  • Inhibit the angiotensin converting enzyme
  • Prevent conversion of angiotensin I to angiotensin II by ACE
  • Decrease sympathetic nervous stimulation
  • Decrease vasoconstriction
  • Decrease Blood Pressure
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6
Q

What are the main adverse effects of angiotensin converting enzyme (ACE) inhibitors (6)?

A
  • Cough
  • Hypotension
  • Hyperkalaemia
  • Foetal injury
  • Renal failure
  • Urticaria / Angioedema
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7
Q

Give 3 examples of angiotensin converting enzyme (ACE) inhibitors.

A
  • Ramipril
  • Lisinopril
  • Perindopril
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8
Q

What considerations should be taken when prescribing angiotensin converting enzyme (ACE) inhibitors?

A
  • Hepatic considerations:
    • Most ACE inhibitors (not lisinopril) are pro-drugs (they require hepatic activation to generate metabolites required for therapeutic effects)
  • Renal considerations:
    • eGFR and serum pottasium must be regularly monitored when prescribing ACE inhibitors
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9
Q

What are angiotensin receptor blockers used for?

A
  • Angiotensin receptor blockers are used to treat hypertension, delay progression of diabetic nephropathy, and treat congestive heart failure
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10
Q

What is the primary drug target of angiotensin receptor blockers?

A
  • Angiotensin receptor
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11
Q

What is the drug target type of angiotensin receptor blockers?

A
  • Receptor antagonists
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12
Q

What is the location of action of angiotensin receptor blockers?

A
  • Kidneys and Vasculature
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13
Q

What is the mechanisms of action of angiotensin receptor blockers?

A
  • Angiotensin receptor blockers act as non-competitive antagonists at AT1 receptor
  • Decrease sympathetic nervous stimulation
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14
Q

What are the main adverse side effects of angiotensin receptor blockers (4)?

A
  • Hypotension
  • Hyperkalaemia
  • Foetal injury
  • Renal failure
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15
Q

Give 3 example of angiotensin receptor blockers.

A
  • Losartan
  • Irbesartan
  • Candesartan
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16
Q

What considerations should be taken when prescribing angiotensin receptor blockers?

A
  • Hepatic considerations:
    • Losartan & Candesartan are pro-drugs (they require hepatic activation to generate the active metabolites required for therapeutic effects)
  • Other medication options:
    • Most trials indicate that angiotensin receptor blockers are not as effective anti-hypertensive agents as ACE inhibitors
17
Q

What are calcium channel blockers used for?

A
  • Calcium channel blockers are used to treat hypertension and angina
18
Q

What is the primary drug target of calcium channel blockers?

A
  • L-type calcium channel
19
Q

What is the drug target type of calcium channel blockers?

A
  • Ion channel antagonist
20
Q

What is the location of action of calcium channel blockers?

A
  • Heart and Blood vessels
21
Q

What is the mechanism of action of calcium channel blockers?

A
  • Block L-type calcium channel (predominantly on smooth muscular vescels)
  • Decrease in calcium influx
  • Inhibition of myosin light chain kinase & prevention of cross-bridge formation
  • Vasodilation
  • Decrease in blood pressure
22
Q

What are the main adverse effects of calcium channel blockers (4)?

A
  • Ankle oedema
  • Constipation
  • Palpitations
  • Flushing / Headaches
23
Q

Give 2 examples of calcium channel blockers.

A
  • Amlodipine
  • Felodipine
24
Q

What type of calcium channel blockers demonstrate a higher degree of vascular selectivity?

A
  • Dihydropyridine type calcium channel blockers
25
Q

What are thiazide / thiazide-like diuretics used for?

A
  • Thiazide / Thiazide-like diuretics are used to suppress lactation and to treat hypertension and edema
26
Q

What is the primary drug target of thiazide / thiazide-like diuretics?

A
  • Sodium / Chloride co-transporter
27
Q

What is the drug target type of thiazide / thiazide-like diuretics?

A
  • Transport protein antagonist
28
Q

What is the location of action of thiazide / thiazide-like diuretics?

A
  • Kidneys
29
Q

What is the mechanism of action of thiazide / thiazide-like diuretics?

A
  • They block the Na+/Cl- cotransporter in the early DCT
  • Na+/Cl- reabsorption is inhibited
  • Increased osmolarity of the tubular fluid
  • Decrease osmotic gradient for water reabsorption in the collecting duct
  • Decrease in volume of fluid in body
  • Decrease in bloop pressure
30
Q

Why is there an increase in calcium reabsorption with using thiazides?

A
  1. Calcium is reabsorbed across the lumen membrane down its concentration gradient that is generated by the activity of the sodium calcium exchanger
  2. Blocking the entry of sodium into the cell through the Na+/Ca2+ exchanger , whilst the Na+/K+still works means that the return of sodium into the cell via the Na+/Ca2+ ​ is increased
  3. This reduces sodium calcium concentration in the cell and therefore increases the potential for calcium to be removed from the tubular fluid
31
Q

What are the main adverse effects of thiazide / thiazide-like diuretics (6)?

A
  • Hypokalaemia
  • Hercalcaemia
  • Metabolic alkalosis (increased H+ excretion)
  • Hyponatraemia
  • Hyperuricemia
  • Hyperglycaemia (hyperpolarised pancreatic β-cells)
32
Q

Give 2 examples of thiazide / thiazide-like diuretics.

A
  • Bendroflumethiazide (thiazide diuretic)
  • Indapamide (thiazide-like diuretic)