Hypertension drugs Flashcards
What is desired blood pressure in adults?
120/80 mmHg “desired”
Define stages of hypertension
1: 140/90 mmHg to 159/99 mmHg
2: 160/100 mmHg to 180/120 mmHg
3: higher than 180/120 mmHg
Where is ACE found?
luminal surface of capillary endothelial cells, predominantly in the lungs
What are the steps of angiotensinogen?
angiotensinogen from liver, renin from kidney converts it to angiotensin I. ACE from lungs converts that to angiotensin II,
what are the actions of angiotensin II?
acts at AT1, vasoconstriction
stimulation of aldosterone which acts at distal renal tubule
cardiac and vascular muscle cell growth
vasopressin (ADH) release from posterior pituitary
How is angiotensin II created?
converted from. the angiotensin I via ACE or chymases
How do ACEi cause hypotension and dry cough
potentiates bradykinin
- vasodilatation via NOS/NO
What are the ACEi names?
lisinopril, ramipril
What is the mechanism of action for ACEi?
inhibiting circulating and tissue ACE •
A reduction in Angiotensin-II activity,
vasodilation (↓ peripheral resistance: ↓ afterload)
reduction in aldosterone release (↑ Na + H2O excretion)
reduced vasopressin (ADH) release (↑ H2O excretion)
reduced cell growth and proliferation
ACEi
Hypotension, Dry cough (10-15% - bradykinin association)
hyperkalaemia (lower aldosterone - ↑[K+])
cause or worsen renal failure
angioedema
X ACEi
Renal artery stenosis, AKD,, (CKD - caution),
idiopathic angioedema
pregnancy
^ACEi
↑K+ drugs,
NSAIDs,
other antihypertensive agents
ARB names
candesartan, losartan
ARB mechanism
AT 1 and AT2 receptors antagonist, no effect on bradykinin
ARB
Hypotension!
hyperkalaemia (low aldosterone ↑K+)
cause or worsen renal failure
X ARB
Renal artery stenosis, AKD,, (CKD
pregnancy
^ARB
↑K+ drugs,
NSAIDs
What do CCB do?
target calcium initiated smooth muscle contraction, primary choice for low renin patients
What are the 2 groups of CCB
dihydropyridines
- non-dihyropyridin
What are dihydropyridines?
amlodipine (long half life) nifedipine nimodipine (selective for cerebral vasculature)
dihydropyridine
Ankle swelling, flushing, headaches (vasodilation)
Palpitations
mechanism for dihydropyridine
little chronotropic or inotropic effects
cerebral vs peripheral selectivity
x dihydropyridine
Unstable angina, severe aortic stenosis
^ dihydropyridine
amlodipine + simvastatin (increased effect of statin)
non-dihydropyridine examples
phenylalkylamines =verapamil and benzothiazapines=diltiazem
phenylalkylamines mechanism
depresses SA node and slows AV conduction, prolongs the action potential
Class IV anti-arrhythmic agent
Less peripheral vasodilatation,
negative chronotropic and inotropic effects
Phenylalkylamines
Constipation,
bradycardia (i .v. ), heart block and cardiac failure
X Phenylalkylamines
Poor LV function (caution), AV nodal conduction delay
^ Phenylalkylamines
β-blockers,
other antihypertensive and antiarrhythmic agents
thiazide examples
bendroflumethiazide
indapamide
thiazide mechanism
• Inhibit N+/Cl- co-transporter in distal convoluted tubule
↓Na+ and H2O reabsorption
thiazide
Hypokalaemia, hyponatraemia, hyperuricemia (gout), arrhythmia ↑glucose (especially with beta-blockers) small ↑cholesterol and triglycerid
X thiazide
Hypokalaemia, hyponatraemia, gout
^ thiazide
NSAIDs, ↓K+ drugs such as loop diuretics
aldosterone antagonist example
spironolactone
mechanism of spironolactone
K sparing, mineralcorticoid aldosterone antagonist
spironolactone
Hyperkalaemia, gynaecomastia (moobs)
Xspironolactone
Hyperkalaemia, Addison’s
^spironolactone
↑K+ drugs (monitoring), pregnancy
β-adrenoceptor blockers examples
labetalol
bisoprolol
metoprolol
β-adrenoceptor blockers mechanism
Decrease sympathetic tone
reducing myocardial contraction
bisoprolol resulting in reduced cardiac output
↓ renin secretion β1
β-adrenoceptor blockers
Bronchospasm, heart block, Raynaud’s (cold hands), lethargy, impotence
Mask tachycardia – sign of insulin induced hypoglycaemia
X β-adrenoceptor blockers
Asthma, (COPD), haemodynamic instability, hepatic failure
^β-adrenoceptor blockers
non-dihydropyridine CCBs - verapamil and diltiazem – asystole!
α-adrenoceptor blockers examples
doxazosin,
tamulosin(renal, BPH)
α-adrenoceptor blockers mechanism
Selective antagonism of α-1 adrenoceptors •
Reduce peripheral vascular resistance •
Urinary tract including bladder neck and prostate – benign prostatic hyperplasia (tamsulosin), Relatively safe in renal disease
α-adrenoceptor blockers
Postural hypotension
dizziness, syncope, headache and fatigue
Xα-adrenoceptor blockers
postural hypotension
^ α-adrenoceptor blockers
dihydropyridine CCB - ↑oedema
What is MAP?
DBP+(SBP-DBP)/3)
loop diuretics example
bumetanide
furosemide
loop diuretics mechanism
• Inhibit N+/K+/2Cl- co-transporter in ascending limb of LoH,
↓ N+ K+ 2Cl- into epithelium H2O follows by osmosis
Direct dilation of capacitance veins – reduces preload
For :pulmonary oedema, fluid overload in HF, adjunct in nephrotic syndrome
loop diuretics
Dehydration, hypotension!
Hypokalaemia, hyponatraemia, hyperuricemia (gout) with chronic treatment, arrhythmia, tinnitus ↑cholesterol and triglyceride
X loop diuretic
Hypokalaemia, hyponatraemia, gout, hepatic encephalopathy
^ loop diuretic
aminoglycosides, digoxin, lithium
K sparing diuretic example
amiloride
K sparing diuretic mechanism
Block ENaC
↓Na+ reabsorption in DCT and reduce K+ excretion, adjunct to loop or thiazide like in HF to limit ↓K+
K sparing diuretic
Hyperkalaemia, potential arrhythmia
X K sparing diuretic
Addison’s, potassium supplement
^ K sparing diuretic
K+ sparing drugs, ACEi, ARBs