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59-291 Section 2, Lecture 4 Adrenergic Receptor Agonists -termed sympathomimetic 3 Groups:

59-291 Section 2, Lecture 4 Adrenergic Receptor Agonists -termed sympathomimetic 3 Groups: Direct-acting Indirect-acting mixed-acting Direct-acting Subdivided into: -catecholamines -non catecholamines. Catecholamines Naturally occuring- NE, E, dopamine

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59-291 Section 2, Lecture 4 Adrenergic Receptor Agonists -termed sympathomimetic 3 Groups:

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  1. 59-291 Section 2, Lecture 4 • Adrenergic Receptor Agonists • -termed sympathomimetic • 3 Groups: • Direct-acting • Indirect-acting • mixed-acting • Direct-acting • Subdivided into: • -catecholamines • -non catecholamines

  2. Catecholamines Naturally occuring- NE, E, dopamine Synthetic- isoproterenol and dobutamine These are rapidly inactivated by 2 enzymes found in the gut and liver and in many other tissues: monoamine oxidase (MAO) and catechol-o-methyltransferase (COMT); low oral bioavailabilities and short t ½ therefore must be administered parenterally.

  3. Mechanisms and Effects Catecholamines differ wrt affinities and specificities for the receptors Draw relative response vs log [Catecholamine] plots for the agonists in the box.

  4. Sys, Dias., MeanArt. P

  5. Adverse effects: -excessive vasoconstriction leading to ischemia -reduces blood flow to vital organs such as kidneys; cause excessive cardiac stimulation leading to myocardial ischemia ar arrythmias --adrenergic agonists: hyperglycemia undesirable in diabetics Indirect-Acting Amphetamine- induces the release of NE Cocaine-prevents reuptake of NE

  6. Mixed-Acting: the name says it all! activate both α and  receptors Ephedrine and Pseudoephedrine vasoconstriction via 1 receptors; useful as nasal decongestants; via  bronchodilate Adverse effects: tachycardia, hypertension, urinary retention

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