vasoactive Trigger of release action of of vasoactive inhibitor drugs

Amines

angiotensin II Renin release stimulate AGll ● potent pressor beta-blockers.

release: ● stimulates autonomic ganglia. ● block renin
● Decreased stretch ● increases the release of secretion
(hypotension) catecholamine aliskiren
● Decreased distal delivery of ● direct inotropic action on the heart. ● Renin
sodium ● aldosterone biosynthesis. inhibitors
● SNS stimulates renin ● Stimulates drinking. captopril
release ● Increases the secretion of ● ACE inhibitor
vasopressin. losartan
● renal vasoconstriction. ● AT-1 receptor
● Increases sodium reabsorption. antagonists
● Inhibits the secretion of renin.
● development of cardiovascular
hypertrophy.

Aldosterone ● Decrease BP ● Acts on late distal tubule and spironolactone

collecting duct.
● Causes salt and water retention.
● Increases K+ and H+ excretion

Bradykinin ● Plasma kininases ● vasodilatation

● rapid and very brief decrease in
blood pressure.when given IV
● natriuresis
○ inhibiting sodium
reabsorption

ADH ● rising plasma tonicity increase water reabsorption. Conivaptan

● falling blood pressure. ● long term treat (hyponatremia)
vasoconstrictor ● V1a and V2
● Vasoconstriction antagonist
Tolvaptan
treat (hyponatremia)
● V2 antagonists
vasoactive Trigger of release action of of vasoactive inhibitor drugs
Amines

ANP ● atrial stretch. ● Increases sodium excretion and

● sympathetic stimulation,
● endothelins and
vasopressin.
urine flow
● increase in glomerular filtration
rate.
● decrease in proximal tubular
sodium reabsorption.

● Inhibits the release of renin,

aldosterone and vasopressin
● increase sodium and water
excretion.
● vasodilation
● decreases arterial blood pressure.

Endothelins ● vasoconstriction in vascular beds Bosentan

● exert direct positive inotropic and ● ETA-ETB
chronotropic actions. receptor
● potent coronary vasoconstrictors. antagonist
● Decrease GFR and sodium and ● pulmonary
water excretion. arterial
● ETA receptors:vasoconstriction hypertension.
● ETB receptors: PGI2 and nitric Ambrisentan
oxide. ● ETA
antagonist.
 Positive inotropic agents

Drug Action Effect Used Adverse effect

Digoxin inhibit the cardiac increase Force of Heart failure. ▪Narrow margin of safety.
Na+/K+ pump cardiac contraction. Atrial flutter ▪Altered color perception
Atrial fibrillation. ▪Nausea, vomiting and
Increase [Na+]i increase Stroke Paroxysmal atrial abdominal pain.
concentration volume atrioventricular nodal ▪Arrhythmias (most
tachycardia. frequent and most
Increase [Ca++]i . Increase Cardiac serious).
output. ▪Headache, fatigue, and
sleeplessness
Increase vagal activity ▪Gynecomastia

Reduce conduction
through AV Toxicity
▪Hypokalemia.
▪Hypercalcemia.
▪Hypomagnesmia.
▪Renal failure.

Dopamine Activation of Beta 1 increase contractility Severe Heart failure

force

Dobutamine selective β-1 agonist increase cardiac short-term treatment increased blood
contractility of congestive heart pressure and
Increase cardiac failure. heart rate, ventricular
output. ectopic activity.

Milrinone Inhibits increase cAMP acute heart failure

phosphodiesterase increase cardiac Used for an
enzyme contractility and exacerbation of chronic
vasodilatation. heart failure.
Increases cardiac
output and reduce
peripheral
vascular resistance.
 Diuretics
Thiazide furosemide Potassium sparing diuretics

Site Distal convoluted tubule Thick ascending limb Late distal tubule and collecting duct

Action Inhibition of Na\Cl channel Block Na/K/Cl spironolactone

Reduce reabsorption of Na ● Direct antagonism of
mineralocorticoid receptors
amiloride
● Inhibition of Na+ influx through
ion channels in the luminal
membrane (

Side effect Metabolic alkalosis. Metabolic alkalosis hyperkalemia

Hypokalemia. Hypokalemia.
Hyponatremia. Hypomagnesemia.
Hyperglycemia. Ototoxicity.
Hyperuricemia. Hyperuricemia.
Hyperlipidemia Allergic reactions.

● Reduce salt and water retention

● reduce ventricular preload.
● reduction in venous pressure
○ Reduction of edema
○ Reduction of cardiac size
type Drug effect

Vasodilators Hydralazine Afterload reduction

Vasodilators Nitrates mainly Preload reduction

ACEI Enalapril Reduce salt and water retention by

Lisinopril reducing aldosterone secretion
● reduce preload.
Reduce peripheral resistance
● reduce afterload.

Reduce sympathetic activity.

Reduce long-term remodeling

Beta-adrenoceptors blockers Carvedilol (non selective) reduce Heart rate.

Metoprolol reduce Renin angiotensin system.
Bisoprolol (beta 1 selective reduce Atrial and ventricular
arrhythmias
Anti-ischemic effects.
Reduce remodeling.

Angiotensin receptor Valsartan and sacubitril inhibiting neprilysin

neprilysin inhibitor ● degradation of NPs and other
peptides slowed.
High circulating (ANP) and BNP
● enhancing diuresis, natriuresis
and anti-remodelling.
ANP and BNP inhibit renin and
aldosterone secretion.
Selective AT1-receptor blockade reduce:
● vasoconstriction,
● sodium and water retention
● myocardial hypertrophy.

cardiac pacemaker inhibitor Ivabradine Slow HR