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Sympathomimetics

Sympathomimetics. Naturally occurring catecholaminesSynthetic catecholamines Synthetic non-catecholamines (Direct and Indirect). Pharmacological effects. 1. Vasoconstriction (renal circulation, and cutaneous)2. Vasodilatation (skeletal muscle)3. Bronchodilation4. Cardiac stimulation

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Sympathomimetics

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    1. Sympathomimetics

    2. Sympathomimetics Naturally occurring catecholamines Synthetic catecholamines Synthetic non-catecholamines (Direct and Indirect)

    3. Pharmacological effects 1. Vasoconstriction (renal circulation, and cutaneous) 2. Vasodilatation (skeletal muscle) 3. Bronchodilation 4. Cardiac stimulation (increase heart rate) 5. Myocardial Contractility (increases irritability) 6. Hepatic glycogenolysis 7. Liberation of free fatty acids 8. CNS stimulation 9. Modulation of Insulin, renin and pituitary hormone

    4. Structure Activity Derived from beta-phenylethylamine. A hydroxyl group on positions three and four on the benzene ring. (these are catechols).

    5. Structure Activity Receptors: Need the hydroxyl group on the 3,4 position to maintain maximal alpha and beta stimulation.

    6. Structure Activity CNS stimulation occurs when the drugs lack substitutes on the benzene ring Substitutes on ring decrease lipid solubility, decreasing passage through the blood brain barrier

    7. Clinical uses 1. Most often used as positive inotropes 2. Vasopressors 3. Treatment of brochospasm (including allergic rxn) 4. Prolong duration of action of local anesthetics

    8. Metabolism Catecholamines: All catecholamines are inactivated by MAO (monoamine oxidase): They contain 3,4 dihydroxy benzene structure.

    9. Metabolism COMT (catechol-o-methyltransferease) methylates hydroxyl group

    10. Structure Activity Principle mechanism Uptake into the postganglionic sympathetic nerve endings.

    11. Non-Catecholamines Not effected by COMT (lack hydroxyl group) Relies on MAO

    12. NATURALLY OCCURRING CATECHOLAMINES Epinephrine Norepinephrine Dopamine

    13. SYNTHETIC CATECHOLAMINES Isuprel Dobutamine

    14. SYNTHETIC NON-CATECHOLAMINES Indirect Acting 1. Ephedrine 2. Mephentermine (Wyamine) 3. Metaraminol (Aramine) Direct Acting: 1. Phenylephrine (Neosynephrine) 2. Methoxamine (Vasoxyl)

    15. Selective Beta 2 Agonist 1. Metaproterenal (Alupent) 2. Albuterol (Proventil) 3. Terbutaline (Brethine) 4. Ritordine 5. Theophyilline

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