Drug treatment of hypertension Flashcards

(47 cards)

1
Q

What is advised before taking antihypertensive drugs

A

oModify diet
oIncrease exercise
oReduce alcohol consumption
oReduce coffee and other caffeine-rich products
oReduce sodium (salt) intake
oStop smoking

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2
Q

What controls BP

A

-nerves (ANS/baroreceptors)
-RAAS

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3
Q

How is angiotensin released

A

Renin is released from the kidneys
Renin (enzyme) converts angiotensinogen to angiotensin I (inactive)
Angiotensin converting enzyme (ACE) converts angiotensin I to angiotensin II

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4
Q

What regulates renin release

A

Beta adrenergic receptor agonists
Renal sympathetic nerve activity
Prostaglandin I2

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5
Q

Where does angiotensin II act

A

AT1 receptors
(increases BP)

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6
Q

What is the action of angiotensin II

A
  1. Vasoconstriction ↑total
    peripheral resistance
  2. Stimulates release of
    aldosterone (from adrenal gland) - salt retention
    which ↑blood volume
  3. Stimulates thirst and release of ADH which ↑blood volume, cardiac output and MAP
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7
Q

What is the action of ACE

A

on extracellular surface of endothelial cells
AT1 receptors on SMC
Gq - IP3 - Ca2+ release - contraction

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8
Q

What is the first ACEi

A

captopril

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9
Q

What is the effect of higher renin levels in patients

A

more angiotensin produced
greater effect of ACEi

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10
Q

Examples of ACEi

A

Ramipril
Lisinopril

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11
Q

Uses of ACEi

A

Hypertension
Heart failure
After MI

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12
Q

Adverse effects of ACEi

A

Cough
Hypotension
Reversible renal impairment
Hyperkalaemia

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13
Q

Elimination of ACEi

A

Mainly renal excretion

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14
Q

Examples of angiotensin receptor blockers (ARBs)

A

losartan
candesartan
irbesartan

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15
Q

Uses of ARBs

A

Hypertension
Heart failure

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16
Q

Adverse effects of ARBs

A

Hypotension
Reversible renal impairment
Hyperkalaemia

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17
Q

Elimination of ARBs

A

Mainly hepatic metabolism

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18
Q

Why is coughing an adverse effect of ACEi

A

ACE breaks down bradykinin
inhibiting ACE increases bradykinin levels
Bradykinin acts on itch channels causing coughs

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19
Q

Why do ACEi and ARBs cause hyperkalemia (high potassium)

A

Angiotensin II releases aldosterone
Aldosterone increases sodium reabsorption
from urine to blood and subsequent potassium loss into urine
Reduced angiotensin II = reduce aldosterone

20
Q

2 types of L-type calcium channel blockers

A

Cardiac selective - arrythmias
verapamil/diltiazem
vascular selective (SMC)
amlodipine/nifedipine

21
Q

Mechansim of vascular selective calcium channel blockers

A

In vascular smooth muscle,
influx of calcium through
calcium channels in the
cell membrane leads to
contraction and thus
vasoconstriction.
Vasodilation
 ↓ arterial resistance
 ↓ blood pressure
 ↓ cardiac afterload

22
Q

Adverse effects of vascular selective calcium channel blockers

A
  • Headache
  • Flushing
  • Dizziness
  • Peripheral oedema
  • ↑ gastro-oesophageal reflux
23
Q

What is the functional unit of the kidney

24
Q

Renal system

A

Blood is filtered at the glomerulus and fluid (filtrate)
containing small molecules moves into the Bowman’s
capsule.
* The filtrate proceeds through the tubule where
absorption and secretion occur. Many small molecules
and ions are returned to the blood. Some molecules
are secreted from the blood to urine (e.g. uric acid).
* The reabsorption of water from urine to blood is
regulated by hormones.
* The collecting duct collects the urine from many
nephrons.

25
Why do loop and thiazide diuretics increase urine output
Inhibit ion transporters ↓ sodium reabsorption in nephron which leads to greater urine volume.
26
How do diuretics treat hypertension
unclear Initial decrease in BP due to ↓ blood volume, cardiac output & peripheral resistance -RAAS system activated
27
Examples of loop diuretics
Furosemide/frusemide
28
Action of loop diuretics
Inhibit Na+/K+/2Cl- transporter in ascending loop of Henle * Increase Na+ in urine * Increased volume of urine * Very powerful “torrential”
29
Examples of thiazide diuretics
indapamide, bendroflumethiazide
30
Action of thiazide diuretics
* Bind to Cl- site of the Na+/Cl- transporter in the distal tubule Prevent Na+ movement into cell Increase sodium in urine Increased volume of urine. * Less powerful than loop diuretics
31
Adverse effects of loop diuretics
↑ loss of H+ = metabolic alkalosis ↑ loss of K + Use with K+ -sparing diuretics ↑ loss of Ca + ↑ loss of Mg + ↓ loss of uric acid = gout
32
Adverse effects of thiazide diuretics
↑ loss of H+ = metabolic alkalosis ↑ loss of K + Use with K+ -sparing diuretics ↑ loss of Mg + ↓ loss of uric acid = gout erectile dysfunction
33
Types of potassium sparing diuretics
* Epithelial sodium channel blockers e.g. amiloride, triamterene * Mineralocorticoid antagonists (a.k.a. aldosterone antagonists ) e.g. spironolactone, eplerenone
34
Mechanism of potassium sparing diuretics
High Na+ arriving at collecting tubule enters cell via epithelial sodium channel (ENaC). K+ moves out through leak channel * Amiloride blocks ENaC * Spironolactone reduces expression of ENaC and Na + /K+ ATPase.
35
Spironolactone adverse effects
-Hyperkalemia -GI upset -Gynecomastia, menstrual disorders, testicular atrophy (via action on progesterone/androgen receptors outside kidney)
36
Amiloride adverse effects
-Hyperkalemia -GI upset
37
Action of beta blockers on hypertension
e.g. propranolol block action of NA B1 - reduces contractility/HR (heart)/inhibits renin release (kidney) a1/b2 - blood vessels a1 stimulation = vasoconstriction B2 stimulation = vasodilation
38
Bisoprolol
B1 selective beta blocker
39
pindolol/celiprolol
partial agonists at B2 adrenoceptors in skeletal muscle
40
carvedilol/labetalol
B adrenoceptor& vasodilator a1 antagonist
41
Beta blocker adverse effects
B1 - cardiac depression/bradycardia B2 - Cold hands and feet/Bronchoconstriction/impaired glycogenolysis/gluconeogenesis Propranolol still prescribed for peripheral symptoms of anxiety – performers and exams.
42
Examples of a1 antagonists
doxazosin prazosin
43
Mechanism of a1 antagonists
Block effects of NA/adrenaline causing vasodilation -decreased peripheral resistance/BP Blocks: activation of Gq, Activation of PLC (phospholipase C) ↑IP3 ↑Ca2+ contraction
44
What does blockage of a2 adrenergic receptors cause
reflex tachycardia
45
Uses of a1 antagonists
* hypertension (occassionally) * congestive heart failure * benign prostatic hyperplasia (common use)
46
adverse effects of a1 antagonists
first dose - postural hypotension (fainting) and syncope limit initial dose/monitor BP both standing and recumbent BP
47
What drug is taken by over 55s/Black African/Caribbeans
CCB