Adrenergic agonists and antagonists Flashcards
CNS Dopamine receptors and effects
D1, D2, D3, D4, D5
Essential NT in many neural circuits
Renal afferent BV Dopamine receptor and effect
D1
Dilation - increase flow to kidney
Nerve ending Dopamine receptor and effect
D2
Modulate NT release
Good treatment during shock
Dopamine
B1 receptor and heart effect
Stimulation of HR and force
Muscarinic receptor and heart effect
Decrease HR
A1 receptor and vessels
Vasoconstriction
B2 receptor and vessels
Vasodilation
Baroreceptor reflexes
Indirect effect on heart
Increase BP -> increase baroreceptor firing -> increase parasympathetics, decrease sympathetics
Norepinephrin
A1, A2, B1, B3 agonist
Low B2 effect -> high peripheral resistance, reflex HR decrease
Use during anesthesia and shock -> maintain stable BP
Epinephrin
A1, A2, B1, B2, B3 agonist
Good B2 agonist -> skeletal and mesentary dilation BUT some A1 constriction
Not as useful for maintaining BP artificially
Isoproterenol
B1, B2, B3 agonist
Big B2 agonist -> drop in BP and reflex increase in HR
CV clinical uses of epinephrin
During CPR for asystole
Hemodynamic support after CABG surgery
Anaphylaxis
Local or topical hemostatic
CV clinical uses of norepinephrin
Pressor agent of choice for septic shock and may be more appropriate than dopamine as first-line treatment for other types of shock as well, especially cardiogenic shock
NE can be used as a pressor agent to support blood pressure in surgery and ICU
NE decreases renal blood flow
Phenylephrine (Neosynephrine) actions
Vasoconstriction
Increase peripheral resistance and increase BP
Increased blood pressure causes reflex bradycardia - blocked by atropine
Phenylephrine (Neosynephrine) clinical use
IV vasopressor agent:
Maintain BP in hypotensive states - spinal anesthesia
Paroxysmal atrial tachycardia - induces baroreceptor reflex slowing of rate
Over-the-counter nasal decongestant
Dopamine receptor affinity
D1 > B1 > A1
Higher doses increase CO but also cause vasoconstriction
Dopamine effect on BV
Vasodilates renal, coronary, & mesenteric vascular beds
Dopamine effect on Heart
Mild increase in rate and force
B1 agonist and increase NE
High dose dopamine effect on BV
Vasoconstriction and increased BP
Bad for shock
Clinical uses of dopamine
Shock, cardiogenic shock, unstable CHF
Increases cardiac output and enhances perfusion of kidney
**Must monitor BP carefully
Sometimes used in manage acute crisis in chronic CHF
Dobutamine
B1 selective agonist
Positive inotropic and some increase HR
CO increases
Little vascular effect
Dobutamine clinical uses
Cardiogenic shock, MI, CHF
Adverse effects of dobutamine
May increase size of infarct
Potential arrhythmias
Increases work and O2 requirement
A1 selective receptor blocker
Treat essential HTN
Decrease PVR, venous return and preload
No effect on CO, HR or NE release
Decrease LDL and TG, and increase HDL
A1 selective receptor blocker adverse effects
Can cause marked postural hypotension and syncope, orthostatic hypotension, especially with initial doses
Usually given at bedtime to minimize hypotensive effects
Prazosin
A1 selective receptor blocker
VERY selective
Short half life
Terazosin
A1 selective receptor blocker
High bioavailability
Doxazosin
A1 selective receptor blocker
High bioavailability
1st generation B blockers
Both B1 and B2 blocker *Propranolol (prototype) Nadolol Timolol Pindolol - partial agonist Carteolol - partial agonist Sotalol - ISA
2nd generation B blockers
Cardioselective *Atenolol *Metoprolol Bisoprolol *Esmolol - very short acting, use during surgery Acebutolol - partial agonist, ISA
Alpha and beta blockers (3rd generation)
Labetolol
Carvedilol