VASOACTIVE DRUGS

   PRESENTED BY
MWADZIWANA LOUIS LAW
DEFINATIONS
• These are drugs that affect the vasomotor
  tone.
• They are subdivided into two vasoconstrictors
  and vasodilators
Vasodilators
• They are subdivided into arterial (eg
  hydralazine, nicardipine) or venous (eg
  nitroglycerine)
• Many of them are mixed arteriovenous
  vasodilators (eg nitropruside, α-adrenoceptor
  antagonists)
Mechanism of action of
              VASODILATORS
• Stimulation of peripheral β2 adrenoceptor (eg
  isoproterenol)
• Antagonism of α adrenoceptor (phentolamine)
• Inhibition of inward flow of calcium ions through calcium
  channels(nicardipine)
• Stimulation of dopaminergic receptors (fenoldopam)
• Nitric oxide induced formation of cyclic guanosine
  monophosphate inhibition of breakdown of cyclic AMP (
  milrinone)
• Angiotensin converting enzyme inhibition ( enalapril)
Mechanism of Action Of
            Vasoconstrictors
• Stimulation of peripheral α adrenoceptors (
  phenylephrine)
• Arginine vasopresin V1a receptors (
  vasopressin)
• Released when there is low blood volume
Direct Cardiac Effects
• Many vasoactive drugs directly affect cardiac
  performance because they act on receptors, ion
  channels, or enzymes that are located in the
  vascular system and the heart.
• Vasoactive drugs can be a pure vasoconstrictor
  (phenylephrine),
• a combined vasoconstrictor and positive inotrope
  (norepinephrine),
• A pure vasodilator ( isoproterenol)
• A combined vasodilator and negative inotrope
Dopamine
• Precursor of norepinephrine
• In high dosage
• In the periphery, dopamine stimulates prejunctional
  dopaminergic DA2 receptors, which results in the
  inhibition of norepinephrine release, facilitating
  vasodilation
• At low doses, dopamine stimulates the dopaminergic
  receptors in the arteries located in the kidneys,
  abdomen, heart, and brain.
• The vasodilation of renal and mesenteric arteries
  causes an increase in urine output and a decreased
  preload.
Mixed inotropic vasodilator Drugs
             (Inodilators)
• Milrinone and enoximone are
  phosphodiesterase inhibitors
• They inhibit the breakdown of cAMP in cardiac
  and peripheral vascular smooth muscle
  resulting in increased cardiac contractility and
  arterial and venous vasodilation.
Milrinone
•   PDE inhibitor
•   Positive inotropic effect
•   No effects on the heart rate
•   Systemic vascular resistance decrease
Nitroglycerin
• Dilate the venous system, reducing pressure
  needed to circulate the blood around.
Dobutamine
• Increase contractility and heart rate via β1
  receptors
• Increase vasodilation resulting in decrease
  afterload/SVR
• Increase in blood pressure
Norepinephrine
• Vasoconstrictor via α adrenergic receptors
• Severe hypertension
• Increase in blood pressure
Phenylephrine
• Powerful vasoconstrictor
• Increase in blood pressure
Epinephrine
• Vasoconstrictor via α adrenergic receptors
• Increased heart rate and contractility via β1
  receptors
• Increased vasodilation via β2 receptors

Vasoactive drugs

  • 1.
    VASOACTIVE DRUGS PRESENTED BY MWADZIWANA LOUIS LAW
  • 2.
    DEFINATIONS • These aredrugs that affect the vasomotor tone. • They are subdivided into two vasoconstrictors and vasodilators
  • 3.
    Vasodilators • They aresubdivided into arterial (eg hydralazine, nicardipine) or venous (eg nitroglycerine) • Many of them are mixed arteriovenous vasodilators (eg nitropruside, α-adrenoceptor antagonists)
  • 4.
    Mechanism of actionof VASODILATORS • Stimulation of peripheral β2 adrenoceptor (eg isoproterenol) • Antagonism of α adrenoceptor (phentolamine) • Inhibition of inward flow of calcium ions through calcium channels(nicardipine) • Stimulation of dopaminergic receptors (fenoldopam) • Nitric oxide induced formation of cyclic guanosine monophosphate inhibition of breakdown of cyclic AMP ( milrinone) • Angiotensin converting enzyme inhibition ( enalapril)
  • 5.
    Mechanism of ActionOf Vasoconstrictors • Stimulation of peripheral α adrenoceptors ( phenylephrine) • Arginine vasopresin V1a receptors ( vasopressin) • Released when there is low blood volume
  • 6.
    Direct Cardiac Effects •Many vasoactive drugs directly affect cardiac performance because they act on receptors, ion channels, or enzymes that are located in the vascular system and the heart. • Vasoactive drugs can be a pure vasoconstrictor (phenylephrine), • a combined vasoconstrictor and positive inotrope (norepinephrine), • A pure vasodilator ( isoproterenol) • A combined vasodilator and negative inotrope
  • 7.
    Dopamine • Precursor ofnorepinephrine • In high dosage • In the periphery, dopamine stimulates prejunctional dopaminergic DA2 receptors, which results in the inhibition of norepinephrine release, facilitating vasodilation • At low doses, dopamine stimulates the dopaminergic receptors in the arteries located in the kidneys, abdomen, heart, and brain. • The vasodilation of renal and mesenteric arteries causes an increase in urine output and a decreased preload.
  • 8.
    Mixed inotropic vasodilatorDrugs (Inodilators) • Milrinone and enoximone are phosphodiesterase inhibitors • They inhibit the breakdown of cAMP in cardiac and peripheral vascular smooth muscle resulting in increased cardiac contractility and arterial and venous vasodilation.
  • 9.
    Milrinone • PDE inhibitor • Positive inotropic effect • No effects on the heart rate • Systemic vascular resistance decrease
  • 10.
    Nitroglycerin • Dilate thevenous system, reducing pressure needed to circulate the blood around.
  • 11.
    Dobutamine • Increase contractilityand heart rate via β1 receptors • Increase vasodilation resulting in decrease afterload/SVR • Increase in blood pressure
  • 12.
    Norepinephrine • Vasoconstrictor viaα adrenergic receptors • Severe hypertension • Increase in blood pressure
  • 13.
  • 14.
    Epinephrine • Vasoconstrictor viaα adrenergic receptors • Increased heart rate and contractility via β1 receptors • Increased vasodilation via β2 receptors