Cardiovascular Drugs - IO
Cardiovascular Drugs - IO
Cardiovascular Drugs - IO
Dr Ian Oberholzer
UNAM 2023
The Circulatory System
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Regulation of Blood pressure
BP = CO x TPR
BP – Blood Pressure
CO – Cardiac Output
PVR – Peripheral Vascular Resistance
CO = HR x SV
HR – Heart Rate
SV – Stroke Volume
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Hypertension
Hypertension is defined as an elevated blood pressure
(above 140/90 mmHg, normal reading being 120/80
mmHg)
TOTAL PERIPHERAL
CARDIAC OUTPUT
RESISTANCE
Actions of Angiotensin II
The most prominent actions are vasoconstriction and aldosterone
release
Vasoconstriction:
ANG II is a powerful vasoconstrictor of arterioles (less of veins).
It works by causing contraction of vascular smooth muscle by
binding directly to the vascular smooth muscle.
Indirect vasoconstriction is caused by stimulation of the sympathetic
nervous system
Release of Aldosterone:
ANG II acts on the adrenal cortex to promote synthesis and secretion
of aldosterone
Alteration of cardiac and vascular structure:
ANG II can cause hypertrophy and remodeling of the cardiac muscle
ANG II is thought to be responsible for increasing the thickness of
blood vessel walls
Actions of Aldosterone
• Type A, B, C, D, and E
Adverse effects
• Unique AADME
11 Pharmacokinetics
Angiotensin-Converting Enzyme Inhibitors
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pressure
Stroke Prevention in patients with hypertension and LV dysfunction
ARBs cont’d…
Adverse effects
Hyperkalemia
Fetal kidney injury
Angioedema
Contraindicated in patients with bilateral renal artery
stenosis
Pharmacokinetics
All ARBs are given orally
Excreted via the kidneys
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Direct Renin Inhibitor
Example: Aliskiren
MOA: Binds tightly to Renin and inhibits the cleavage
of Angiotensinogen to ANG I
Prevents ANG II and aldosterone production
Indications
Hypertension
Pharmacokinetics:
Orally bioavailability is low (2.5%)
Half life of 24 hours
Adverse Effects:
Generally well tolerated but at higher doses can cause
diarrhoea
16 Contraindicated in pregnancy
Aldosterone Antagonists
Example: Eplerenone and Spironolactone
MOA: Inhibits the actions of aldosterone (Eplerenone
is more selective to aldosterone receptors)
Excretion of sodium and water
Indications
Hypertension
Heart Failure
Pharmacokinetics:
Administered orally
Adverse Effects:
Gynecomastia
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END
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