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Muscarinic agonists
Drug Structure Receptor specificity Musc Acetylcholine Carbachol Methacholine Bethanechol Muscarine Pilocarpine Oxotremorine +++ ++ +++ +++ +++ ++ ++ Nic +++ +++ + +++ ++ None None None Bladder* and Gl hypotonia None Glaucoma None Hydrolysis by AChE Clinical uses
Nicotinic Agonists
Nicotine is the most commonly encountered nicotinic agonist. It is a tertiary amine found in the leaves of the tobacco plant. It is sufficiently lipid-soluble to be absorbed across the skin. It is responsible for the addicting properties of tobacco. Nicotine has a greater affinity for neuronal than for skeletal muscle nicotinic receptors Nicotine's actions are complex. At low dosages it stimulates ganglionic nicotinic receptors (cause marked activation of these nicotinic receptors and initiate action potentials in postganglionic neurons) thus enhancing both sympathetic and parasympathetic neurotransmission
The initial response therefore often resembles simultaneous discharge of both the parasympathetic and the sympathetic nervous systems. In the case of the cardiovascular system, the effects of nicotine are chiefly sympathomimetic on blood vessels, and parasympathomimetic on the heart In the GI and urinary tracts, the effects are largely parasympathomimetic
As nicotine dosages increase, there is stimulation of nicotinic receptors in many other sites At high dosages, nicotine possesses some antagonist effect at nicotinic receptors
Prolonged exposure results in depolarizing blockade of the ganglia