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PHARMACOLOGY phase 1b > Hypertension > Flashcards

Hypertension Flashcards

1
Q

What is the drug target for ACE Inhibitors?

A

Angiotensin converting enzyme

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2
Q

What is the mechanism of action for 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 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/Angioedema

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4
Q

Why are ACE inhibitors considered pro drugs (lisinopril) ?

A

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

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5
Q

What must be regularly monitored when prescribing ACE inhibitors?

A

eGFR and serum potassium must be regularly monitored when prescribing ACE inhibitors.

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6
Q

What are some examples of ACE inhibitors?

A

Ramipril
Lisinopril
Perindopril

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7
Q

What are some examples of calcium channel blockers?

A

Amlodipine
Felodipine

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8
Q

What are the side effects of CCB?

A

Ankle oedema
Constipation
Palpitations
Flushing/Headaches

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9
Q

What is the mechanism of action of CCBs?

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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10
Q

What is the drug target of CCBs?

A

L-type calcium channel

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11
Q

Which type of CCBs demonstrate a higher degree of vascular selectivity?

A

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

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12
Q

What is the mechanism of action of Thiazide?

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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13
Q

What is the site of action for Thiazide?

A

Sodium/chloride
co-transporter

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14
Q

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

A

Bendro-flumethiazide (thiazide)
Indapamide (thiazide-like)

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15
Q

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

A

Hypokalemia
Hyponatremia.
Metabolic alkalosis (increased hydrogen ion excretion)
Hypercalcemia.
Hyperglycemia (hyperpolarised pancreatic beta cells).
Hyperuricemia

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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 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)-

18
Q

What are some examples of angiotensin receptor blockers and which are pro drugs?

A

Losartan - pro drug
Irbesartan
Candesartan - pro drug

19
Q

What is the clearance of a drug?

A

Clearance is the measure of the ability of the body to eliminate a drug. Clearance by means of various organs of elimination is additive. Elimination of drug may occur as a result of processes that occur in the liver, kidney, and other organs.

20
Q

What is the elimination half life of a drug?

A

Elimination half-life is the length of time required for the concentration of a particular drug to decreasetohalf of itsstarting dose in the body.

21
Q

What is the time to peak plasma levels?

A

Time to peak concentration is the time required for a drug to reach peak concentration in plasma. The faster the absorption rate, the lower is the time to peak plasma concentration.

22
Q

Who are ARB’s for?

A

ARBs for patients of African or Caribbean descent

23
Q

Why are ACEi used ahead of ARB’s?

A

ACE inhibitors are typically used ahead of angiotensin 2 receptor blockers (partly due to cost/partly due to evidence that ACE Is are more effective).

24
Q

What are the effects of Thiazide-like diuretics?

A

Decrease blood volume
Decrease venous return
Decrease cardiac output

25
Q

how long do the diuretic effects?

A

The diuretic effect of thiazides only lasts for 1-2 weeks. - The kidney becomes tolerant to the diuretics because there is a rebound activation of the renin angiotensin system which counteracts the diuretic effect due to increasing sodium reabsorption.

PHARMACOLOGY phase 1b (8 decks)

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