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Vaso-active drugs
By
Dr. Ahmed Galal
PICU specialist
Definition of vasoactive drugs
These are drugs that has
effect on heart & circulatory
system
Adrenergic receptors
Β receptorsα receptors
β2β1α2α1
• Sm.ms.
Relaxation in
bronchioles,
blood vs., uterus
• Increase renin
• Gluconeogenesis
& glycolysis
• Heart: intropy,
chronotropy &
improve ejection
fraction
• Increase renin
• Inhibits insulin
release
• Stim. Glucagon
release
• Inhibit
noradrenaline
relase
• VC of bl.vs. of
skin, GIT, kidney,
brain
• Sm.ms.
Contraction of
uterus, ureter,
cilliary body
• Gluconeogenesis
& glycolysis
Classification of vasoactive drugs
Vasopressor Inotropic Vasodilator
Adrenaline
Noradrenaline
Phenyl epherine
Vasopressin
Ephidrine
Dopamine
Dobutamine
Amrinone
Milrinone
Adrenaline
Digoxin
Calcium
Na
Nitroperruside
Nitroglycerine
Hydralazine
Adrenaline
Mechanism of action:
It stimulates α1 & β1 & 2 adrenergic receptors
Vasoconstriction causing
hypertension
Inotropic & chronotropic
effect
Bronchodilatation
antishock
Action: Indications:
Shock (all types)
Heart failure
Asthma & croup
Anaphylaxis
Nasal obstruction & local
haemostasis
Adrenaline
Dosing
Shock (IV or IO): 0.05 – 1 mic/kg/min.
Anaphylaxis or asthma (IM or SC): 0.1 ml/kg of 1/1000 solution
Arrest (IV or IO): 0.1 ml/kg of 1/10,000 solution
Arrest (ET): 0.1 ml/kg of 1/1000 solution
Side effects
Tachycardia & tachy-arrythmia
Renal impairment & urine retention (in high doses)
Rebound bronchospasm
Skin necrosis
Mesenteric vaso-constiction & ischemia (in high doses)
RFVF
Nor-adrenaline
Mechanism of action:
It stimulates α1 & weaker on β1 adrenergic
receptors
Vasoconstriction causing
hypertension
Very weak Inotropic &
chronotropic effect
Action: Indications:
Shock (hypotensive&
vasoplegic)
Can be used in
hypotensive fallot
tetralogy patient
with cyanotic spell
Nor-adrenaline
Dosing
Shock (IV or IO): 0.05 – 2 mic/kg/min.
Side effects
Renal impairment even in low doses
Skin necrosis esp. if extravasated
Mesenteric vaso-constiction & ischemia (in high doses)
Tachycardia & tachy-arrythmia to a lesser extent
Dopamine
Mechanism of action:
It stimulates α1, α2, β1& to a lesser extent β2 adrenergic receptors
It also stimulates dopaminergic receptor (DA1 & DA2)
Low dose: ++ DA1 & DA2
Intermediate dose: ++ β
High dose: ++ α1
Action: Systematic action:
Low doses: for mesenteric
ischemia
Intermediate dose: cardiac &
septic shock
High doses: hypotensive
shock
Renal dose
become
obsolete
Dopamine
Dosing
Low dose: 2 – 5 mic/kg/min
Intermediate dose: 5 – 10 mic/kg/min
High dose:10 – 20 mic/kg/min
Side effects
Tachycardia & tachy-arrythmia
Skin necrosis if extravasated
Dobutamine
Mechanism of action:
It stimulates β1 & very mild β2& α1 adrenergic
receptors
Inotropic & chronotropic
effect
May cause mild
vasodilatation
Action: Indications:
Heart failure
Cold septic shock with
normal blood pressure
With noradrenaline to save
mesenteric vasculature
Improve the
diastolic
dysfunction
Dobutamine
Dosing
5 – 20 mic/kg/min may increase to 30 mic
Side effects
Tachycardia & tachy-arrythmia
Skin necrosis if extravasation
Milrinone
Mechanism of action:
It is phosphodiesterase inhibitor so, increase cAMP that
lead to increase Ca delivery to myocardium
Inotropic & chronotropic
effect
Vasodilatation (pulmonary
& systemic)
Action: Indications:
Cardiac failure
Pulmonary hypertension
Cold septic shock with
normal blood pressure
Improve the
diastolic
dysfunction&
Rt sided failure
Inhalation in
pulmonary
hypertension
Milrinone
Dosing
0.5 – 0.75mic/kg/min
Side effects
Hypotension
Tachycardia & tachy-arrythmia
Thrombocytopenia
Should be adjusted in renal imaprement
Vasopressine
Mechanism of action:
It stimulates VR1 causing increase cAMP that
lead to increasing Ca delivery to bl. Vs wall
Vasoconstriction causing
hypertension
Water retention causing
renal impairment
Decrease intestinal motility
& gut ischemia
Action: Indications:
Profound hypotension
DI
GI bleeding
ADH analogue
Vasopressine
Dosing
0.0005 – 0.01mic/kg/hr
Side effects
Anuria & renal failure
Severe mesenteric ischemia
Hyponatremia
Vasodilator drugs
Inhibits ACE so, decrease
angiotensin 2 (potent VC)
Captopril,
ramipril
ACE inhibitors
Competitive inhibition to angio 2
receptors
LosartanAngiotengen 2
receptor antagonist
Block Ca entrance to vascular wall
causing relaxation
Nifidipine,
amlodipine
Ca channel blockers
NO donor, increase cGMP causing
relaxation
Nitroglycerine,
nitroperusside
Nitrates
Comprtitive inhibition of α1
receptors
PhentolamineAdrenoreceptor
antagonists
Bind to dopaminergic receptorsFenoldapamDopaminergic
receptor agonists
Bind to PG receptor increasing
cGMP
alprostadilProstaglandin
Direct areriolar dilatationHydralazine
Nitroglycerine
Mechanism of action:
It is NO donor so, stimulation of cGMP causing
vascular wall relaxation
Vasodilator mainly veins
Decrease myocardial oxygen
demands (by improving
atrial filling pressure by
venodilatation)
Action: Indications:
Heart failure
Cold septic shock with
normal blood pressure
Hypertensive urgencies
Cautious use
in shock
Nitroglycerine
Dosing
0.5 – 5 mic/kg/min upto 20 mic/kg/min in
hypertensive emergencies
Side effects
Tachycardia, hypotension
Prespiration
Headache
Nitroperosside
Mechanism of action:
It is NO donor so, stimulation of cGMP causing
vascular wall relaxation
Vasodilator mainly arteriolar
Hypotension
Action: Indications:
Hypertensive urgencies
Nitroperosside
Dosing
0.5 – 1 mic/kg/min
Side effects
Tachycardia, hypotension
Headache
Thank you

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Vaso-active drugs overview

  • 1. Vaso-active drugs By Dr. Ahmed Galal PICU specialist
  • 2. Definition of vasoactive drugs These are drugs that has effect on heart & circulatory system
  • 3. Adrenergic receptors Β receptorsα receptors β2β1α2α1 • Sm.ms. Relaxation in bronchioles, blood vs., uterus • Increase renin • Gluconeogenesis & glycolysis • Heart: intropy, chronotropy & improve ejection fraction • Increase renin • Inhibits insulin release • Stim. Glucagon release • Inhibit noradrenaline relase • VC of bl.vs. of skin, GIT, kidney, brain • Sm.ms. Contraction of uterus, ureter, cilliary body • Gluconeogenesis & glycolysis
  • 4. Classification of vasoactive drugs Vasopressor Inotropic Vasodilator Adrenaline Noradrenaline Phenyl epherine Vasopressin Ephidrine Dopamine Dobutamine Amrinone Milrinone Adrenaline Digoxin Calcium Na Nitroperruside Nitroglycerine Hydralazine
  • 5. Adrenaline Mechanism of action: It stimulates α1 & β1 & 2 adrenergic receptors Vasoconstriction causing hypertension Inotropic & chronotropic effect Bronchodilatation antishock Action: Indications: Shock (all types) Heart failure Asthma & croup Anaphylaxis Nasal obstruction & local haemostasis
  • 6. Adrenaline Dosing Shock (IV or IO): 0.05 – 1 mic/kg/min. Anaphylaxis or asthma (IM or SC): 0.1 ml/kg of 1/1000 solution Arrest (IV or IO): 0.1 ml/kg of 1/10,000 solution Arrest (ET): 0.1 ml/kg of 1/1000 solution Side effects Tachycardia & tachy-arrythmia Renal impairment & urine retention (in high doses) Rebound bronchospasm Skin necrosis Mesenteric vaso-constiction & ischemia (in high doses) RFVF
  • 7. Nor-adrenaline Mechanism of action: It stimulates α1 & weaker on β1 adrenergic receptors Vasoconstriction causing hypertension Very weak Inotropic & chronotropic effect Action: Indications: Shock (hypotensive& vasoplegic) Can be used in hypotensive fallot tetralogy patient with cyanotic spell
  • 8. Nor-adrenaline Dosing Shock (IV or IO): 0.05 – 2 mic/kg/min. Side effects Renal impairment even in low doses Skin necrosis esp. if extravasated Mesenteric vaso-constiction & ischemia (in high doses) Tachycardia & tachy-arrythmia to a lesser extent
  • 9. Dopamine Mechanism of action: It stimulates α1, α2, β1& to a lesser extent β2 adrenergic receptors It also stimulates dopaminergic receptor (DA1 & DA2) Low dose: ++ DA1 & DA2 Intermediate dose: ++ β High dose: ++ α1 Action: Systematic action: Low doses: for mesenteric ischemia Intermediate dose: cardiac & septic shock High doses: hypotensive shock Renal dose become obsolete
  • 10. Dopamine Dosing Low dose: 2 – 5 mic/kg/min Intermediate dose: 5 – 10 mic/kg/min High dose:10 – 20 mic/kg/min Side effects Tachycardia & tachy-arrythmia Skin necrosis if extravasated
  • 11. Dobutamine Mechanism of action: It stimulates β1 & very mild β2& α1 adrenergic receptors Inotropic & chronotropic effect May cause mild vasodilatation Action: Indications: Heart failure Cold septic shock with normal blood pressure With noradrenaline to save mesenteric vasculature Improve the diastolic dysfunction
  • 12. Dobutamine Dosing 5 – 20 mic/kg/min may increase to 30 mic Side effects Tachycardia & tachy-arrythmia Skin necrosis if extravasation
  • 13. Milrinone Mechanism of action: It is phosphodiesterase inhibitor so, increase cAMP that lead to increase Ca delivery to myocardium Inotropic & chronotropic effect Vasodilatation (pulmonary & systemic) Action: Indications: Cardiac failure Pulmonary hypertension Cold septic shock with normal blood pressure Improve the diastolic dysfunction& Rt sided failure Inhalation in pulmonary hypertension
  • 14. Milrinone Dosing 0.5 – 0.75mic/kg/min Side effects Hypotension Tachycardia & tachy-arrythmia Thrombocytopenia Should be adjusted in renal imaprement
  • 15. Vasopressine Mechanism of action: It stimulates VR1 causing increase cAMP that lead to increasing Ca delivery to bl. Vs wall Vasoconstriction causing hypertension Water retention causing renal impairment Decrease intestinal motility & gut ischemia Action: Indications: Profound hypotension DI GI bleeding ADH analogue
  • 16. Vasopressine Dosing 0.0005 – 0.01mic/kg/hr Side effects Anuria & renal failure Severe mesenteric ischemia Hyponatremia
  • 17. Vasodilator drugs Inhibits ACE so, decrease angiotensin 2 (potent VC) Captopril, ramipril ACE inhibitors Competitive inhibition to angio 2 receptors LosartanAngiotengen 2 receptor antagonist Block Ca entrance to vascular wall causing relaxation Nifidipine, amlodipine Ca channel blockers NO donor, increase cGMP causing relaxation Nitroglycerine, nitroperusside Nitrates Comprtitive inhibition of α1 receptors PhentolamineAdrenoreceptor antagonists Bind to dopaminergic receptorsFenoldapamDopaminergic receptor agonists Bind to PG receptor increasing cGMP alprostadilProstaglandin Direct areriolar dilatationHydralazine
  • 18. Nitroglycerine Mechanism of action: It is NO donor so, stimulation of cGMP causing vascular wall relaxation Vasodilator mainly veins Decrease myocardial oxygen demands (by improving atrial filling pressure by venodilatation) Action: Indications: Heart failure Cold septic shock with normal blood pressure Hypertensive urgencies Cautious use in shock
  • 19. Nitroglycerine Dosing 0.5 – 5 mic/kg/min upto 20 mic/kg/min in hypertensive emergencies Side effects Tachycardia, hypotension Prespiration Headache
  • 20. Nitroperosside Mechanism of action: It is NO donor so, stimulation of cGMP causing vascular wall relaxation Vasodilator mainly arteriolar Hypotension Action: Indications: Hypertensive urgencies
  • 21. Nitroperosside Dosing 0.5 – 1 mic/kg/min Side effects Tachycardia, hypotension Headache