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BRS Phase 1b > Pharmacology of Hypertension > Flashcards

Pharmacology of Hypertension Flashcards

1
Q

What are some examples of Angiotensin converting enzyme inhiitors?

A

Ramipril

Lisinopril

Perindopril



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2
Q

What is the 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 are the main side effects of ACE inhibitors?

A

Cough
Hypotension
Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)
Foetal Injury (AVOID IN PREGNANT WOMEN)
Renal failure (in patients with renal artery stenosis)-
Urticaria/Angioedem

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4
Q

What do most ACE inhibitors require to reap therapeutic effects?

A

Most ACE inhibitors (not lisinopril) are pro-drugs. They require hepatic activation to generate the active metabolites required for therapeutic effects.

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5
Q

What must be regulated when prescribing ACE inhibitors?

A

eGFR and serum potassium

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6
Q

What are some examples of Calcium channel blockers?

A

Amlodipine

Felodipine



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7
Q

What is the mechanism of action of calcium channel blockers?

A

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

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8
Q

What is the primary target for Calcium channel blockers?

A

L-type calcium channels

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9
Q

What are the main side effects of Calcium channel blockers?

A

Ankle oedema

Constipation

Palpitations

Flushing/Headaches



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10
Q

Which type of calcium channel blockers demonstrate greater vascular selectivity?

A

Dihydropyridine type calcium channel blockers

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11
Q

What are some examples of thiazide/thiazide-like diuretics?

A

They block the Na+, Cl- co-transporter in the early DCT.

Therefore, Na+ and Cl- reabsorption is inhibited.

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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12
Q

What is the primary target for thiazide/thiazide-like diuretics?

A

Sodium/chloride co-transporter



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13
Q

What are the main side effects of thiazide/thiazide-like diuretics?

A

Hypokalemia

Hyponatremia.

Metabolic alkalosis (increased hydrogen ion excretion)

Hypercalcemia.

Hyperglycemia (hyperpolarised pancreatic beta cells).

Hyperuricemia

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14
Q

What happens after 1-2 weeks of treatment with thiazide/thiazide-like diuretics?

A

Thiazide and thiazide-like diuretics both lose their diuretic effects 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)

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15
Q

What are some examples of Angiotensin receptor blockers?

A

Losartan

Irbesartan

Candesartan



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16
Q

What is the 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)

17
Q

What are the major side effects of Angiotensin receptor blockers?

A

Hypotension



Hyperkalaemia (care with K+ supplements or K+-sparing diuretics)



Foetal Injury (AVOID IN PREGNANT WOMEN)



Renal failure (in patients with renal artery stenosis)-

NOT AS EFFECTIVE AS OTHER HYPERTENSIVES.

18
Q

What do Losartan & Candesartan require to reap the desired therapeutic effects?

A

Losartan and candesartan are pro-drugs. They require hepatic activation to generate the active metabolites required for therapeutic effects.



19
Q

What can Felodipine result in ?

A

dose-dependent decrease in systolic+diastolic blood pressure. reflex tachycardia

20
Q

How does Amlodipoine mitigate the reflex tachycardia seen in many patients?

A

Slow onset

longer half life

21
Q

What is used prior to Angiotensin 2 blockers?

A

ACE inhibitors, partially due to cost/ACE is more effective

22
Q

What is the effect of thiazide like diuretics?

A

Decrease blood volume
Decrease venous return
Decrease cardiac output

23
Q

How can thiazide diuretic access the NaCl transporter on the apical side of the distal tubule?

A

diuretic needs to travel from the blood to the basolateral side to the transporter on the apical side

24
Q

How long does the diuretic effect of thiazides last?

A

1-2 weeks
kidney becomes tolerant, rebound activation of the renin angiotensin system which counteracts the diuretic effect due to Na reabsorption

25
Q

What causes the continued anti-hypertensive effect of thiazides?

A

less well understood vasodilating action

BRS Phase 1b (80 decks)

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