Unit 3- Adrenergic Agonists Flashcards
Sympathomimetic
Mimic effects of catecholamines, dependent on similarity of structure to NE and EPI
Direct Acting Agonists
Endogenous catecholamines, adrenergic receptor agonists
Indirect Acting Antagonists
Trigger catecholamine release, reduce metabolism, or inhibit reuptake
Mixed Acting Antagonists
Directly activate adrenergic receptors while increasing NE release
Desensitization
Reduced response of receptors to an agonist after prolonged exposure, reducing physiological response
Causes of Desensitization
Sequestration of receptors, destruction or decreased synthesis of receptors, receptor being phosphorylated and unable to couple to G-protein
α1 Agonists
EPI, NE, phenylephrine
α2 Agonists
EPI, NE, medetomidine, xylazine
β1 Agonists
EPI, NE, isoproterenol, dobutamine
β2 Agonists
EPI, ractopamine, isoporterenol, terbutaline
Phenylephrine Selectivity
α1
Dexmedetomidine Selectivity
α2
Xylazine Selectivity
α2
NE Selectivity
α>β1
EPI Selectivity
All receptors equal
Dobutamine Selectivity
β1
Isoproterenol Selectivity
β
Albuterol Selectivity
β2
Terbutaline Selectivity
β2
Dopamine Selectivity
D>β
Fendolapam Selectivity
D1
α Receptor Affinity
EPI, NE, isoproterenol
β Receptor Affinity
Isoproterenol, EPI, NE
α1 Activity
Vascular contraction, pupil dilation, urethral contraction, splenic contraction
α2 Activity
Platelet aggregation, NT release inhibition, vascular contraction
β1 Activity
Increase rate and force of heart contraction, increase renin release
β2 Activity
Relax bronchioles, relax uterus, relax vessels, gluconeogenesis, increase insulins secretion
β3 Activity
Lipolysis
D1 Activity
Vascular diation
D2 Activity
Modulate autonomic NT release
α Agonist Selectivity
Phenylephrine, EPI, NE, isoproterenol
β1 Agonist Selectivity
Isoproterenol, EPI, NE
β2 Agonist Selectivity
Isoproterenol, EPI, NE
Terbutaline
β2 agonist used for small animal bronchodilation, little effect on cardiac β1 receptors and virtually no α
Albuterol
β2 agonist used in cats and horses for bronchodilation, aerosol improves hypoxemia in anesthetized horse
Clenbuterol
β2 agonist used in horse for bronchodilator and uterine relaxant, contraindicated in food producing animals
Isoflurane
Vasodilator, reduces peripheral resistance, preserves cardiac output at normal dose, decreases cardiac output by depressing contraction at high dose
Anesthetic Hypotension
Dopamine, ephedrine, and dobutamine
Dopamine
D1 agonist with dose dependent effects, promotes vasodilation, activates cardiac β1 receptors to increase HR and output, activates vascular α1 receptors to constrict
Ephedrine
α1 and β agonist that induces NE release with dose dependent effects, activates cardiac and vascular β receptors to increase MAP and cardiac index with more effect at higher doses
Dobutamine
α1 and β1 agonist increasing contractility over HR, treats low cardiac output
Epinephrine
Cardiac stimulant, vasoconstrictive, renal vasoconstrictor
Norepinephrine
Vasoconstrictor and renal vasoconstrictor used in hypotension
Phenylephrine
Selective α1 agonist inducing peripheral vasoconstriction and splenic constriction
Nephrosplenic Entrapment
Horse colon becomes trapped between spleen and body wall phenylephrine reduces spleen size and frees colon
Pupillary Dilation
Phenylephrine dilates the pupil and contracts conjunctival vessels
Horner’s Syndrome
Constriction of the pupil, drooping of the eyelid, sinking eye, and protrusion of 3rd eyelid in affected eye; treated with phenylephrine
Apraclonidine
α2 agonist decreasing intraocular pressure in human
Brimonidine
α2 agonist decreasing intraocular pressure in human
Urethral Sphincter Incontinence
Most common urinary incontinence in female small animal, treated with phenylpropanolamine α2 agonist
Ractopamine