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19
Antihypertensives II
61
Pharmacology
Undergraduate 1
12/18/2016

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Cards

Term
What do diuretics do?
Definition
decrease sodium ion reabsorption
increase urine volume
Term
Is endothelium-1 a vasoconstrictor?
Definition
yes
Term
What effects does captopril have?
Definition
ACE inhibitor
Term
What effects does spironolactone have?
Definition
antagonist at the aldosterone receptor
increases synthesis of sodium channels which boosts reabsorption of sodium
Term
What effects does amlodipine have?
Definition
blacks voltage gated calcium channels
Term
What effects does b blockers have have?
Definition
blocks vasodilation effects
Term
What is produced by the action of COX enzymes?
Definition
prostacyclin
Term
What is textbook physiological blood pressure?
Definition
S=120, D=80
“120/80”
Term
What is white coat hypertension?
Definition
increased blood pressure due to blood pressure recording
therefore several readings are taken, sometimes outside of clinic
Term
What is ambulatory blood pressure monitoring?
Definition
device worn during waking hours
BP measured every 30 min
Term
What is home blood pressure monitoring?
Definition
2 readings 1 min apart
morning and evening for 7 days
Term
Describe stage 1 hypertension
Definition
S=140-159 or D=90-99

>140/90
Term
Describe stage 2 hypertension
Definition
S=160-179 or D=100-109

> 160/100
Term
Describe stage 3 hypertension
Definition
S=180-219 or D=110-119

> 180/110
Term
What is the action taken in stage 1
Definition
Confirm over 1-2 weeks then treat.
Term
What is the action taken in stage 2
Definition
Confirm over 3-12 weeks then treat. If patient has complications e.g. diabetes then treat earlier.
Term
What is the action taken in stage 3
Definition
Confirm over 12 weeks and treat if there are complications. Life-style change, if there are no complications.
Only treat if hypertension persists.
Got to allow for complications...
Term
When is severe hypertension and what actions are taken
Definition
>220/120 or accelerated/malignant.

Immediate treatment required.
Term
What is the target?
Definition
Target = S<140, D<90 (lower if there is established underlying disease).
Term
How is treatment initiated in stage 1 hypertension?
Definition
1. assess for any end organ damage
2. age
Term
How is end organ damage assessed?
Definition
heart - hypertrophy (ECG)
kidney - renal function limited (urine/blood test)
eye - papilloedema, retinal haemorrhage
Term
What happens if you have stage 1 and >20% CV risk?
Definition
you will be treated
Term
If a patient has no end-organ damage and is 40-80 years of age, what happens?
Definition
lifestyle advice:
- Stop smoking.
- Lose weight.
- Reduce alcohol consumption.
- Reduce dietary salt.
- Reduce total and saturated fat intake.
- Increase fruit and vegetable intake.
- Increase exercise.
Term
If a patient has no end-organ damage and is below 40 years of age, what happens?
Definition
check for secondary cause, if there is one, treat it. If there isn't, follow lifestyle advice.
Term
How is treatment initiated in stage 2 hypertension?
Definition
> 160/100 confirmed home readings
treat hypertension
Term
How is treatment initiated in stage 3 hypertension?
Definition
> 180/110
1. immediately start antihypertensive drug treatment, without waiting for ABPM or HBPM
2. immediately refer person to specialist care the same day if they show signs of papilloedema and/or retinal haemorrhage (accelerated hypertension)
Term
38 year old male
152/90mmHg
overweight
drinks 30 units a week
Definition
arrange for home measurement of BP
if there is > 135/85 check for end organ damage and secondary causes
if none , suggest lifestyle changes
Term
Give an example and identifier of diuretics
Definition
bendroflumethiazide
'thiazide'
Term
Give an example of aldosterone antagonist
Definition
spironolactone
Term
Give an example and identifier of ACE inhibitor
Definition
captopril
'pril'
Term
Give an example and identifier of AT1 blocker
Definition
candesartan
'sartan'
Term
Give an example and identifier of ca channel blocker
Definition
amlodipine
'dipine'
Term
Give an example of k channel blocker
Definition
minoxidil
Term
Give an example and identifier of alphal blocker
Definition
doxazosin
'zosin'
Term
Give an example and identifier of beta blocker
Definition
propranolol
'lol'
Term
Give an example of a nitrate
Definition
sodium nitroprusside
Term
What does systemic hypertension treatment depend on?
Definition
age and ethnic background
Term
How are young caucasians treated?
Definition
ACE inhibitor or AT1 anatgonist
(perhaps beta-blocker if other not tolerated)
Term
How are Afro-Caribbeans and >55 years olds treated?
Definition
Thiazide or Ca2+-receptor antagonist.
Term
Discuss Combination Therapy and Progressive Therapy
Definition
Even for ‘standard hypertension’, a single antihypertensive drug is often not sufficient. When this is the case, combination therapy is used. For example:
ACE inhibitor or AT1 antagonist with thiazide or Ca2+-channel antagonist.

If this is inadequate,

Thiazide and Ca2+-channel antagonist.

Then may add,

α(1)-blocker, spironolactone, another diuretic or a β-blocker.
Additional pharmacological options for very severe hypertension include diazoxide, hydralazine, sodium nitroprusside and/or minoxidil.
Term
Why is combination therapy used?
Definition
Combination therapy is used because one drug may have its effects more or less balanced by the baroreceptor reflex, which would detect the vasodilatory effects of the drugs used, and act to reverse the drop in MAP thus exacerbating the hypertension.
Term
Describe the acute treatment for very severe hypertension
Definition
1. minoxidil, diazoxide (K channel openers)
2. hydrazine (K channel opener, inhibits SR Ca release and NO production)
3. sodium nitroprusside (NO donor)

used with e.g. beta-blocker to inhibitor reflex tachycardia
Term
Does hypertension arise in pregnancy?
Definition
either pre-existing or occurs in 3rd trimester (pre-eclampsia)
Term
Define pre-eclampsia
Definition
a medical condition characterised by high blood pressure and high urine protein content in pregnant women. Pre-eclampsia leads to eclampsia: the life-threatening occurrence of seizures during pregnancy
Term
What is prescribed for pre-existing hypertension (pre-eclampsia)?
Definition
methyldopa
acts as an alpha-2 agonist in medulla to reduce sympathetic outflow
Term
What would be used in hypertensive crisis in pregnancy?
Definition
• Labetolol or hydralazine is used in hypertensive crises.
Term
What other drugs are used in pregnancy hypertension?
Definition
β-blockers are used in third trimester.
Nifedipine: a dihydropyridine Ca2+-channel blocker that primarily blocks L-type Ca2+-channels.
Term
How is pulmonary hypertension identified?
Definition
Difficult to measure pulmonary pressure – only severe cases identified – but regurgitation from right ventricle to right atrium is an indicator.
Term
What is a common feature of pulmonary hypertension? therefore, how is it treated?
Definition
pulmonary emboli
anticoagulants
Term
What is pulmonary hypertension usually due to?
Definition
an underlying disease which must be addressed by therapy
Term
Which drugs are used to treat pulmonary hypertension?
Definition
sildenafil
bosentan
epeprostenol
iloprost
Term
Describe sudenfil
Definition
sildenafil - 'fil'
phospodiesterase 5 inhibor (PDE5 inhibitor)
PDE5 breaks down cGMP to GMP

given orally
Term
Describe bosentan
Definition
non-selective endothelium 1 receptor antagonist 'entan'
blocks ETA and ETB receptors

because of the potent vasoconstrictive effects of ET1, receptor blockade promotes vasodilation

given orally
Term
Describe epoprostenol
Definition
prostacyclin
causes vasodilation through increased cAMP production
inhibits platelet aggregation
provides symptomatic relief and increases exercise tolerance
not orally bioavailable
Term
How is epoprostenol given
Definition
i.v. long term via central venous catheter
inhalation (to limit systemic hypotension)
Term
Describe iloprost
Definition
synthetic prostacyclin anologue
given by inhalation
Term
Adverse effects of captopril
Definition
renal impairement
dry cough
Term
Adverse effects of minoxidil
Definition
hypertrichosis
Term
Adverse effects of propranolol
Definition
fatigue
Term
Which drugs cannot be used in pregnant women?
Definition
captopril, candesartan and bosentan
Term
Which drugs cannot be used in breastfeeding women?
Definition
candesartan and bosentan
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