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Pharmacology > Antihypertensives > Flashcards

Antihypertensives Flashcards

1
Q

What lifestyle advise to give patient with hypertension?

A

< weight

reduce salt

reduce alcohol

increase exercise

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2
Q

What is vascular endothelial cell dysfunction?

A

The endothelium regulates vascular smooth muscle tone through synthesis and release of relaxing factors such as nitric oxide and prostacyclin.

And vasoconstricting factors such as angiotensin II. Angiotensin II can cause vascular injury by activating growth factors that cause vascular plasia/ trophy/ fibrosis.

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3
Q

What’s the target BP for diabetics?

A

130/80 mmHg

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4
Q

What two factors (physiologically) is going in influence BP?

A

Cardiac output (volume)

PVR -peripheral vascular resistance

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5
Q

Vasoconstriction at three levels

A
  1. arteriolar smooth muscle contraction via Alpha 1 adrenoceptors of sympathetic nervous system.
  2. Blood-borne vasopressin and angiotensin II
  3. Locally; released adenosine, serotonin, endothelin, prostaglandins.
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6
Q

Short term control of BP via….

A

sympathetic n.s.

  • baroreceptor reflex.

Good for increases in activity and postural changes.

Adjusts CO and PVR

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7
Q

Long term control of BP….

A

Kidneys!

regulation of plasma volume

AND renin-angiotensin-aldosterone axis

(Usually water follows salt >> urine)

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8
Q

Interesting fact about managment of BP….

A

2/3 rds of patients with hypertension cannot control their blood pressure with one single type of drug.

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9
Q

What is the function of Renin?

A

Renin activates the renin-angiotensin system by cleaving angiotensinogen, produced by the liver, to yield angiotensin I,

which is further converted into angiotensin II by ACE, the angiotensin-converting enzyme primarily within the capillaries of the lungs. Angiotensin II then constricts blood vessels, increases the secretion of ADH and aldosterone, and stimulates the hypothalamus to activate the thirst reflex, each leading to an increase in blood pressure. Renin’s primary function is therefore to eventually cause an increase in blood pressure, leading to restoration of perfusion pressure in the kidneys.

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10
Q

How do centrally acting sympatholytic drugs work?

A

Reduce PVR. No effect on the HT.

reduce sympathetic outflow from the central vasomotor centre (medulla) to the circulation

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11
Q

What are atenolol and bisoprolol examples of?

A

B - blockers

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12
Q

What drug blocks both alpha and beta receptors?

A

Carvedilol

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13
Q

Name the renin inhibitor

A

Aliskiren

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14
Q

What drugs can’t be used during prenancy?

A

ACE Inhibitors

ARBs

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15
Q

What class do most CCBs belong to?

A

dihydropyridine

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16
Q

What drug can cause “first dose” syncope?

A

alpha1 blockers (especially in combo with a diuretic)

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17
Q

Why do thiazide diuretics cause hypokalaemia?

A

Because of Na+ / K + exchange in the collecting tubules.

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18
Q

How can you reduce the hypokalaemia effect of thiazides?

A

Combine with a Potassium Sparing diuretic - this isn’t done in practice.

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19
Q

What are the two drugs that are NOT members of the CCB dihydropyridine group?

A

Verapamil

Diltiazem

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20
Q

What group is amlodipine and what is it used for?

A

CCB (dihydropyridine class); reduce PVR by vasodilation, and thus are also indicated for angina.

(more non-dihydropyridine class cause also affect rate - for AF patients)

CCBs block the movement of calcium into heart and blood vessel muscle, thus decreasing the pumping strength of the heart and relaxes blood vessels.

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21
Q

Important adverse effects of B-blockers (3)

A
  • reduce exercise capacity (bradycardia)
  • contraindicated in asthma and COPD due to bronchospasm
  • impaired glycogenolysis
  • also causes cold extemities because of the contraction of smooth muscle in peripheral arteries.
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22
Q

Adverse effects of ACE inhibitors

A

fetal and neonatal injury/ death

dry cough

angioedema (due to >> bradykinin)

can cause hyperkalaemia

23
Q

What two groups are contraindicated in pregnancy?

A

ACE Inhibitors

ARBs

24
Q

Give two examples of ARBs

A

Losartan

Valsartan

25
Q

What has a recent study of losartan indicated? (and which group is this drug?)

A

ARBs

losartan produced a greater reduction of left ventricular hypertrophy, reduced risk of stroke, and new-onset diabetes.

26
Q

What is Spironolactone?

A

Potassium-sparing diuretics

Mineralocorticoid receptor antagonists = aldosterone receptor antagonists.

27
Q

What antihypertensive can you use in pregnancy?

(which group?)

A

Methyldopa

Centrally acting sympatholytic drug

28
Q

what are the changeable hypertension risk factors?

A

overweight

>> salt

alcohol

lack of physical exercise

smoking

stress

29
Q

Unchangeable risk factors with hypertension

A

aging

race

family history

gender

gestational hypertension

30
Q

First steps in antihypertensive treatment, what are they?

A

Aged under 55 years old - A for ACE inhibitor

Aged over 55 years, or African or Caribbean descent - C for Calcium-channel blocker

31
Q

Second stage in antihypertensive therapy is….

A

A + C

ACE inhibitor

and

Calcium Channel Blocker

32
Q

Third stage in antihypertensive therapy is…

A

A + C + D

Ace inhibitor

plus

Calcium channel blocker

plus

thiazide-like diuretic

33
Q

What is spironolactone an example of and when is it used?

A

Potassium-sparing diuretic

Best combined with other drugs when hypertension is not being controlled with other mixed. combinations.

34
Q

How do ACE inhibitors work?

A

Prevent the body from creating angiotensin II,
inhibiting angiotensin-converting enzyme.

This relaxes blood
vesselsand

helps to reduce the amount of water re-absorbed
by the kidneys thereby reducing BP (by reducing alderosterone secretion)

35
Q

ARBs are generally well tolerated, but what is a problem associated with them?

A

hyperkalemia

36
Q

What drug group can cause hypokalemia?

A

thiazides

(resulting in cardiac arrhymias and muscle weakness)

NB> thiazides are usually used in combination with other drugs.

37
Q

What antihypertensive drug (group) would be better suited for AF patients?

A

CCBs because studies show they provide better rate control and arrhymia-related symptom relief than beta blockers in patients with permanent AF.

38
Q

Which part of the nephron do thiazides work?

Also, give an example of a thiazide.

A

….. inhibiting sodium reabsorption at the beginning of the distal convoluted tubule

Bendroflumethiazide

(avoid alcohol if possible)

39
Q

What’s the duration of action of most ACE inhibitors?

A

24 hours

40
Q

What stimulates renin production?

A
  • A reduction in BP at the afferent renal arteriole
  • Direct sympathetic nervous system activation of B1 -adrenoceptors on juxtaglomerular cells.
  • + one other
41
Q

If antiotensinogen II is activated, what happens?

A

> PVR ( due to > contraction of vascular smooth muscle)

aldosterone secretion from the adrenal cortex.

> rebsorption of N2+ from proximal tubule.

> norepinephrine release from sympathetic nerves

IMP. ACE also inactivates bradykinin (endogenous vasodilator peptide)

42
Q

Main physiological action of ACE inhibitors?

A

REDUCE vascular resistance.

43
Q

ACE inhibitors can cause fetal and neonatal injury and death, dry cough (> bradykinin), and remember that…

A

ACE inhibitors can cause renal failure in patients with bilateral renal artery stenosis.

(these patients depend on angiotensin II to maintain renal blood flow and filtration)

44
Q

Common side effects of ACE inhibitors

A

dry cough

angioedema

45
Q

ACE inhibitors typically only reduce BP by approx 10mmHg. Therefore….

A

combine with other drugs for synergic effect (diuretics, CCBs)

46
Q

What group of drugs can impede ACE inhibitors?

A

NSAIDs

47
Q

Why are ACE inhibitors used for diabetes with no hypertension?

A

renoprotective effect with patients with early signs of renal impairment (e.g. albuminuria and >> serum creatinine levels)

48
Q

Which group of antihypertensives is associated with ankle oedema?

A

CCBs

(caused by >> capillary pressure causing leakage of fluids into surrounding tissues)

.. need to check this

49
Q

What is the danger of nitrates with angina treatment?

A

They preferentially relax venous smooth muscle, reducing cardiac preload. Thus could cause hypotension (reflex tachycardia can be invoked if << BP).

NB. Tolerance can occur if patches are not removed for at least 10 hours per day.

50
Q

What are the common side effects of nitrates (affect preload)

A

headache

hypotension

dizziness

reflex tachycardia

51
Q

Why do you often combine a B-Blocker with nitrates?

A

To prevent reflex tachycardia that would increase myocardial demand.

52
Q

Calcium ion channels are found on cardiac muscle tissue and what else?

A

smooth muscle (i.e. arteries, arterioles)

53
Q

What are the common side effects of CCBs?

A

Fatigue, headache, dizziness, flushing, peripheral odema.

(vasodilation/ hypotension)

54
Q
A

Pharmacology (13 decks)

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