Pharmacology of Hypertension Flashcards

1
Q

What are the 3 main examples of Angiotensin converting enzyme inhibitors?

A
  • Ramipril
  • Lisinopril
  • Perindopril
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2
Q

What is the primary mechanism of action of Angiotensin converting enzyme inhibitiors?

A
  • inhibits the angiotensin converting enzyme
  • prevents the conversion of angiotensin I to angiotensin II by ACE.
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3
Q

What is the main drug target of ACE inhibitors?

A

Angiotensin Converting Enzyme (ACE)

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4
Q

What are the main side effects of ACE inhibitors?

A
  • cough
  • hypotension
  • hyperkalaemia
  • foetal injury
  • renal failure (in those with renal artery stenosis)
  • urticaria
  • angioedema
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5
Q

What does pro-drug mean?

A

drugs that require hepatic activation to generate the active metabolites required for therapeutic effects.

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6
Q

Which ACE inhibitors are pro-drugs?

A

most ACE inhibitors except Lisinopril

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7
Q

What must be regularly monitored while taking ACE inhibitors?

A

eGFR and serum potassium

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8
Q

Which is more effective, angiotensin receptor blockers or ACE inhibitors as anti-hypertensive agents?

A

ACE inhibitors

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9
Q

What are some examples of calcium channel blockers?

A
  • Amlodipine
  • Felodipine
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10
Q

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

A
  • block L-type calcium channels (on vascular smooth muscle)
  • decreased calcium influx
  • prevents muscle contraction
  • results in vasodilation which leads to reduced peripheral resistance
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11
Q

What is the primary drug target of calcium channel blockers?

A

L-type calcium channel

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12
Q

What are the side effects of calcium channel blockers?

A
  • ankle oedema
  • constipation
  • palpitations
  • flushing
  • headaches
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13
Q

Which type of calcium channel blockers show higher vascular selectivity?

A

Dihydropyridine type calcium channel blockers

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14
Q

What are examples of Thiazide or Thiazide-like diuretics?

A

Thiazide:
Bendro-flumethiazide
Thiazide-like:
Indapamide

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15
Q

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

A
  • block the Na+/Cl- co-transporter in the early distal convoluted tubule
  • reduces Na+ and Cl- reabsorption
  • osmolarity of the tubular fluid increases, decreasing the osmotic gradient for water reabsorption in the collecting duct
  • less water reabsorption
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16
Q

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

A

Na+/Cl- co-transporter

17
Q

What are the side effects of Thiazide/Thiazide-like diuretics?

A
  • hypokalaemia
  • hyponatremia
  • metabolic alkalosis (increased H+ excretion)
  • hypercalcaemia
  • hyperglycemia (hyperpolarised pancreatic beta cells)
  • hyperuricemia
18
Q

How long do the effects of Thiazide and Thiazide-like duiretics last?

A
  • lose their diuretic effects in 1-2 weeks of treatment
  • continuing anti-hypertensive action appears to be due to vasodilating properties (more pronounced for Thiazide-like diuretics)
19
Q

What are some examples of Angiotensin receptor blockers?

A
  • Losartan
  • Irbesartan
  • Candesartan
20
Q

What is the mechanism of action of angiotensin receptor blockers?

A

Non-competitive antagonists at AT1 receptors (found on kidneys and vasculature)

21
Q

What is the drug target of angiotensin receptor blockers?

A

angiotensin (AT1) receptor

22
Q

What are the side effects of angiotensin receptor blockers?

A
  • hypotension
  • hyperkalaemia
  • foetal injury
  • renal failure (in those with renal artery stenosis)
23
Q

What is the Q-risk?

A

risk of a specific person having a stroke or a heart attack.

24
Q

When hypertensive, when should drug treatment start?

A

One of the following:
- target organ damage
- CVD (or a 10 year risk>10%)
- Renal disease
- Diabetes

25
Q

What is the impact of calcium channel blockers on the heart?

A
  • decreased muscular contraction
  • reduced cardiac contraction
  • reduced cardiac output
  • reduced blood pressure
26
Q

What is the impact of calcium channel blockers on blood vessels?

A
  • decreased muscular contraction
  • reduced vasoconstriction
  • reduced peripheral resistance
  • reduced blood pressure
27
Q

What is the definition of clearance?

A

measure of the ability of a body to eliminate a drug

28
Q

What is the definition of elimination half-life?

A

length of time required for the concentration of particular drug to decrease to half it’s starting dose in the body

29
Q

what does time to peak plasma levels mean?

A
  • time required for a drug to reach peak concentration in plasma
  • the faster the absorption rate, the less time needed to reach peak concentration.
30
Q

What is the difference between felodipine and amlodipine?

A

amlodipine has a longer half-life and a slow onset

31
Q

What are the main effects of ACE inhibitors?

A
  • vasoconstriction
  • salt and water retention
  • aldosterone secretion
32
Q

When are angiotensin receptor blockers prefered over ACE inhibitors?

A

in those of african or caribbean descent

33
Q

Why are ACE ihibtors contraindicated in patients with bilateral renal artery stenosis?

A
  • inhibits angiotensin II
  • helps maintain GFR when renal perfusion is low
  • can cause acute renal failure
34
Q

What are the main effects of Thiazide-like diuretics?

A
  • decrease blood volume
  • decrease venous return
  • decrease cardiac output
  • Na+ and H2O loss
35
Q

Why do the effects of Thiazide/Thiazide-like diuretics stop after 2 weeks?

A
  • kidney becomes tolerant to the diuretics
  • due to rebound activation of the renin-angiotensin system
  • counteracts the diuretic effect by increasing Na+ reabsorption.
36
Q

Why is it important that thiazide-like diuretics are excreted unchanged in the urine?

A

Needs to move from blood to basolateral side to apical side to access the Na+/Cl- co transporter