Hypertension Pharmacology Flashcards by rachael a

What are the drugs for hypertension?

Angiotensin converting enzyme inhibitors

calcium channel blockers

thiazide or thiazide-like diuretics

angiotensin receptor blockers

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Give examples of ACE inhibitors. (3)

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Ramipril
Lisinopril
Perindopril

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Give examples of calcium channel blockers.

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Amlodipine
Felodipine

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Give examples of thiazide or thiazide-like diuretics.

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Bendro-flumethiazide (thiazide)

Indapamide (thiazide-like)

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Give examples of angiotensin receptor blockers.

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Losartan
Irbesartan
Candesartan

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What is the drug target for ACE inhibitors.

Angiotensin converting enzyme

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What is the primary mechanism of action of ACE inhibitors.

Inhibit the angiotensin converting enzyme.

Prevent the conversion of angiotensin I to angiotensin II
by ACE.

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

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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What are most ACE inhibitors (except lisinopril)?

pro-drugs

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

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What must be constantly monitored after prescribing ACE inhibitors.

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

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What is the drug target of calcium channel blockers?

L-type calcium channel

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

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

Ankle oedema

Constipation

Palpitations

Flushing/Headaches

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

a higher degree of vascular selectivity

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

Sodium/chloride
cotransporter

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

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.

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

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

Do the diuretics given for hypertension lose effect?

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)

What is the drug target for angiotensin receptor blockers?

Angiotensin receptor

What is the primary mechanism of action for angiotensin receptor blockers?

These agents act as insurmountable (i.e. non-competitive) antagonists at AT1 receptor (found on kidneys and on the vasculature)

What are side effects of angiotensin receptor blockers?

Hypotension

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

Foetal Injury (AVOID IN PREGNANT WOMEN)

Renal failure (in patients with renal artery stenosis)-

whatare more effective, angiotensin receptor blockers or ACEi?

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

What angiotensin receptor blockers are considered as pro-drugs?

Losartan and candesartan

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

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

Q-risk

What are the therapeutic objectives?

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.

What are the 2 most commonly prescribed calcium channel blockers?

amlodipine and felodipine

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

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

What is clearance?

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.

What is elimination half-life?

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

What is the time to peak plasma plasma levels?

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

What is the effect of ACE inhibtors?

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

What is the diagram/ page showing?

ACE and aldosterone

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

pro= inactive before metabolism active= drug takes effect directly

What is the effect of thiazide-like diuretics?

What do diuretics need to travel through to reach DCT?

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

Why do thiazides increase potassium excretion?

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

Why do thiazides only work for 1-2 weeks?

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.