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Vasoactive drugs
- 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
- 22. Thank you