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313 Pharmacology PSNS 5th Lecture S
313 Pharmacology PSNS 5th Lecture S
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 (causing marked activation of these nicotinic receptors and initiates 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 Regarding 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
At larger concentrations, nicotine induces tremor, emesis, and stimulation of the respiratory center. At still higher levels, nicotine causes convulsions, which may terminate in fatal coma
The lethal effects on the CNS, and the fact that nicotine is readily absorbed, form the basis for the use of nicotine as an insecticide Ganglion stimulants are not used clinically, but only as experimental tools. They cause complex peripheral responses associated with generalized stimulation of ALL autonomic ganglia (sympathetic & parasympathetic)
Nicotinic Antagonists,
Ganglionic Blockers
The primary receptors at ganglia are cholinergic receptors of the nicotinic (NN) type Nearly all effects are predictable from the knowledge that ganglionic blockers reduce transmission in all autonomic ganglia, both sympathetic and parasympathetic In some sites, sympathetic activation seems to predominate over parasympathetic, while in other sites, the opposite is true Ganglionic blockade thus "uncovers" the predominant system This class of drugs is now rarely used Example: trimetaphan
Sweat glands
Sympathetic cholinergic/Anhidrosis