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BRS Pharm > Hypertension Pharmacology > Flashcards

Hypertension Pharmacology Flashcards

1
Q

What are the drugs for hypertension?

A

Angiotensin converting enzyme inhibitors

calcium channel blockers

thiazide or thiazide-like diuretics

angiotensin receptor blockers

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2
Q

Give examples of ACE inhibitors. (3)

A

suffix= pril

Ramipril
Lisinopril
Perindopril

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3
Q

Give examples of calcium channel blockers.

A

suffix= ipine

Amlodipine
Felodipine

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4
Q

Give examples of thiazide or thiazide-like diuretics.

A

suffix= ide

Bendro-flumethiazide (thiazide)

Indapamide (thiazide-like)

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5
Q

Give examples of angiotensin receptor blockers.

A

suffix= artan

Losartan
Irbesartan
Candesartan

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6
Q

What is the drug target for ACE inhibitors.

A

Angiotensin converting enzyme

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7
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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8
Q

What are the main side effects of ACE inhibitors. (6)

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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9
Q

What are most ACE inhibitors (except lisinopril)?

A

pro-drugs

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

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10
Q

What must be constantly monitored after prescribing ACE inhibitors.

A

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

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11
Q

What is the drug target of calcium channel blockers?

A

L-type calcium channel

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12
Q

What is the primary 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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13
Q

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

A

Ankle oedema

Constipation

Palpitations

Flushing/Headaches

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14
Q

What does Dihydropyridine, a type calcium channel blockers, demonstrate?

A

a higher degree of vascular selectivity

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15
Q

What are the drug targets of thiazide or thiazide-like diuretics?

A

Sodium/chloride
cotransporter

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16
Q

What is the mechanism of action of thiazide or 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.

17
Q

What are side effects of thiazide/ thiazide-like diuretics? (6)

A

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

18
Q

Do the diuretics given for hypertension lose effect?

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)

19
Q

What is the drug target for angiotensin receptor blockers?

A

Angiotensin receptor

20
Q

What is the primary mechanism of action for 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 are 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)-

22
Q

whatare more effective, angiotensin receptor blockers or ACEi?

A

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

23
Q

What angiotensin receptor blockers are considered as pro-drugs?

A

Losartan and candesartan

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

24
Q

What score do you use to calculate a patients risk of having a heart attack or stroke?

A

Q-risk

25
Q

What are the therapeutic objectives?

A

Set reasonable blood pressure reduction goals. In this case reduce below 140/90mmHg

Reduce cardiovascular risk associated with increased morbidity and mortality (modifiable risk factors = obesity and smoking).

For Mrs Turner, she would not want any new medication to interfere with her ability to undergo knee surgery.

26
Q

What are the 2 most commonly prescribed calcium channel blockers?

A

amlodipine and felodipine

27
Q

What is the mechanism of action of calcium channel blockers and its effect?

A

MLCK=myosin light chain kinase
MLCK-p= myosin light chain kinase phosphorylated

28
Q

What is clearance?

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.

29
Q

What is elimination half-life?

A

it is the length of time required for the conc of a particular drug to decrease to half of its starting dose in the body

30
Q

What is the time to peak plasma plasma levels?

A

is it 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

31
Q
A
32
Q

What is the effect of ACE inhibtors?

A

angiotensin causes=> vasoconstriction, salt and water retention, aldosterone secretion
ao ACE inhibitor= less of these

33
Q

What is the diagram/ page showing?

A

ACE and aldosterone

34
Q

What is a pro drug and what is an active drug?

A

pro= inactive before metabolism

active= drug takes effect directly

35
Q

What is the effect of thiazide-like diuretics?

A
36
Q

What do diuretics need to travel through to reach DCT?

A

The diuretic (labelled OA) needs to move from;

  1. The blood
  2. Transported on basolateral side
  3. Transporter on apical side

Only then can it access the sodium chloride transporter on the apical side of distal tubule

37
Q

Why do thiazides increase potassium excretion?

A

because they inhibit sodium and chloride reabsorption in the distal nephron, which causes the kidneys to pump sodium and water into the urine

38
Q

Why do thiazides only work for 1-2 weeks?

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.

The continuing anti-hypertensive effect of thiazides is due to a further (less well understood) vaso-dilating action.

BRS Pharm (9 decks)

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