Pharm. I Final Notes - Receptor Nicotonic Muscarinic Alpha...

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Receptor Location Response Cholinergic Autonomic Receptors Nicotonic Autonimic Ganglia To postganglionic neurons Muscarinic all parasympathetic effect cells (organs) smooth muscle: contraction Cardiac muscle: decrease HR Exocrine glands: increases secretion Sweat glands: increases secretion Adrenergic Autonomic Receptors Alpha 1 vascular smooth muscle Intestine smooth muscle Iris radial muscle Urinary sphincter Contaction Relaxation contraction (mydriasis) contraction Alpha 2 CNS inhibitory synapses decreases sympathetic discharge from presynaptic neuron Adrenergic Autonomic Receptors Beta 1 cardiac muscle kidney increases heart rate Increase rennin secretion Beta 2 Lung smooth muscle Arterioles GI smooth muscle Uterus Relaxation Vasodilation Decrease motility relaxation 1
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Autonomic Pharmacology Drug Mechanism of Action PK Clinical Uses ADRs Acetylcholin e endogenous agonist for muscarinic & nicotinic receptors. primary neurotransmitter responsible for neurotransmission at: 1) all autonomic ganglia (sympathetic & parasympathetic)(nicotinic), 2) all post-ganglionic parasympathetic neurons (e.g. vagal innervation of the heart) (muscarinic), 3) post-ganglionic motor neurons (which innervate skeletal muscle) (nicotinic), 4) sympathetic postganglionic neurons that innervate sweat glands (muscarinic), 5) preganglionic sympathetic nerves that innervate the adrenal medulla (nicotinic), resulting in the release of epinephrine and norepinephrine into the systemic circulation. Muscarinic receptors mediate their responses by G-proteins. Nicotinic receptors mediate their responses by opening a cationic ion channel that is an intrinsic component of the nicotinic-receptor-channel complex. inactivate d by AchE via hydrolysis to acetic acid and choline. miosis ( of iris size) Norepinephri ne (catecholami ne, sympathomi metic) peripheral vasoconstrictor (by stimulating alpha-1 and alpha-2 adrenergic receptors) and as an inotropic stimulator of the heart (by stimulating beta-1 adrenergic receptors). Norepinephrine is an endogenous catecholamine synthesized in the adrenal medulla that is the biochemical precursor of epinephrine. Norepinephrine is the transmitter of most sympathetic postganglionic fibers of the CNS. Axns terminate d by neuronal uptake. Diffusion and degradati on by extracellul ar COMT BP control by being a potent vasocontrictor and cardiac stimulant. Adjunt Tx for cardiac arrest and profound hypotension Ischemic injury Used with caution in pts on monoamine oxidase inhibitors (MAOIs) or antidepressants prolonge d HTN Epinephrine Stimulates alpha 1 & 2 and beta 1, 2 on B1 inc. HR and Tachycardia, HA, 2
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(catecholami ne, sympathomi metic) sympathetic effector cells. ventricular contract. Rise diastolic P due to
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Pharm. I Final Notes - Receptor Nicotonic Muscarinic Alpha...

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