14. CHOLINERGIC AGONISTS AND CHOLINESTERASE INHIBITORS CHOLINERGIC AGONISTS
" muscarinic receptor agonistsвЂќ cholinergic agonists will be drugs that act on acetylcholine receptors, hence causing excitation of the parasympathetic autonomic nervous system you will find 2 types of acetylcholine receptors 1) NICOTINIC RECEPTORS - are receptor-mediated ion channels - 3 types RECEPTOR TYPE MUSCLE TYPE GANGLION TYPE LOCATION -- neuromuscular verse - sympathetic autonomic ganglia - parasympathetic autonomic ganglia - CNS
agonists of nicotinic receptors happen to be discussed afterwards (" depolarizing neuromuscular blocking agentsвЂќ, see 16)
2) MUSCARINIC PAIN - will be g-protein coupled receptors -- 3 types RECEPTOR TYPE M1 SITE - CNS - exocrine glands (gastric. bronchial-, salivary-, lacrimal-, and sweat glands) - CNS - GI tract clean muscle -- atria of the heart - exocrine glands - GI tract easy muscle - 37 -
- genito-urinary tract easy muscle -- bronchial easy muscle -- smooth muscle mass of the eye - endothelium of blood vessels
8 types ORGAN CNS EFFECT - increased bone muscle anxiety - tremor - hypothermia - better cognition (improved learning) - decreased heart rate (" bradycardiaвЂќ) - reduced force of contraction -- decreased blood pressure (due to vasodilation) - myosis (due to shrinkage of the pupilary sphincter) - accomodation to near eyesight (due to contraction in the ciliary muscle) - reduced intraoccular pressure (due to opening in the schlemm canal) - GI tract draining (due to increased peristalsis) - urinary bladder emptying (due to contraction with the detrusor muscle) - bronchoconstriction (due to contraction of bronchial soft muscle) - increased gastric secretion -- increased bronchial secretion - increased salivation - elevated lacrimation - increased perspiration
BLOOD VESSELS EYE
GI TRACT GENITO-URINARY TRACT
3 types - 38 -
MEDICINE NAME ACETYLCHOLINE
DESCRIPTION General information - acetylcholine by itself - non-selective acetylcholine radio agonist (acts on equally nicotinic- and muscarinic receptors) - not really used clinically General details - selective muscarinic receptor agonist (acts only about muscarinic receptors) - picky to the eye and exocrine glands Specialized medical uses - treatment of glaucoma (by reduction of intraoccular pressure)
Basic information - same as pilocarpine (see above) - discovered naturally in toadstool - the instrumental agent of mushroom poisoning - not really used medically
there are 2 types of cholinesterase enzymes
ENZYME NAME PLASMACHOLINESTERASE
DESCRIPTION - " butyrylcholinesteraseвЂќ - located in the blood - responsible for the breakdown of acetylcholine in the blood stream - not discussed further in this article - positioned in the cholinergic synapses -- responsible for the breakdown of acetylcholine inside the cholinergic jonction
cholinesterase inhibitors (" anticholinesterases" ) prevent the destruction of acetylcholine by acetylcholinesterase at the nicotinic cholinergic crevices, thus prolonging it's impact
- 39 -
two types ORGAN PARASYMPATHETIC POSTGANGLIONIC SYNAPSES RESULT - increased parasympathetic effects (see above) - large doses can lead to decreased parasympathetic effects (due to depolarization block in autonomic ganglia caused by ongoing acetylcholine action) - elevated skeletal muscles tension -- large dosages may lead to paralysis (depolarization block)
2 classes 1) INVERTABLE - several types DRUG NAME NEOSTIGMINE DESCRIPTION Clinical uses - treatment of myasthenia gravis Specialized medical uses -- same as neostigmine (see above) General data - may possibly cross the blood-brain hurdle Clinical uses - remedying of glaucoma Unwanted side effects - coma and breathing failure (due to primary...
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