imbalance between the constriction and relaxation of a muscle so that parts of the muscle are always constricted
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acetylcholinesterase
enzyme that breaks acetylcholine in the synapse
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psuedocholinesterase
enzyme that breaks down any acetylcholine that makes it to the blood stream
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cholinergic receptors
receptors in the body that bind to acetylcholine
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muscarinic and nicotinic receptors
the 2 types of cholinergic receptors
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muscarinic receptors
a type of G coupled protein receptors that bind to acetylcholine and have a relatively slow reaction
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nicotinic receptors
a type of ligand gated ion channel receptors that bind to acetylcholine and have a relatively quick reaction
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muscarine
a poison found in mushrooms
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cardiovascular, respiratory, digestive, and reproductive systems
in which body systems are there muscarinic receptors
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presynaptic receptors
these muscarinic receptors are in charge of regulating acetylcholine release into the synapse
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Nicotinic 2/ N-N receptors
these nicotinic receptors are located in the ganglia where there is a connection between 2 nerves
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nicotinic 1/N-M receptors
these nicotinic receptors are located in the neuromuscular junction
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M1
this type of muscarinic receptor acts on the CNS and also stomach acid secretion
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M2
type of muscarinic receptor located in smooth muscle of the heart
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M3
type of muscarinic receptor located in the bladder, secretion glands, and smooth muscle
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sputum
acetylcholine and the PSNS causes the release of this in the lungs. It is released during PSNS because the body is relaxed and requires less oxygen
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calcium
mineral that causes muscle constriction
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magnesium
mineral that causes muscle relaxtion
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effects of acetylcholine
bradycardia; secretion of saliva, digestive juices, sputum, tears, sweat; bronchoconstriction, bradypnea, increased activity of the digestive and urinary systems, muscle constriction, miosis, sleep and memory regulation
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reasons why acetylcholine can't be used as a drug
acetylcholine can't pass through membranes, it would activated many body systems when administered, an enzyme would break it up quickly before it could have an effect
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parasympathomimetics/cholinomimetics
name of cholinergic agonists
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act similiar to acetylcholine, block AChE from working
what roles can cholinergic agonists have
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carbachol
a cholinergic agonist with a positive charge so it isn't absorbed in the digestive system. It is a muscarinic and nicotinic agonist and undergoes very slow metabolism
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things carbachol can treat
closed angle glaucoma, it can lower intraocular pressure, an antidote to a AChE inhibitor overdose
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closed angle glaucoma
a bulge around the cornea that stops fluids from being drained from the eye. carbachol treats it by causing miosis leading the bulge to pop and drain
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methacholine
a muscarinic agonist that is a quaternary nitrogen (amine) so it isn't absorbed by the digestive system or passes the BBB. it causes bradycardia and lowers blood pressure
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asthma
methacholine is mainly used to diagnose ____
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methacholine challenge test
methacholine is given in a small dose to the patient if it causes a higher than normal level of bronchoconstriction this indicated that the patient has asthma or COPD
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in a COPD patient the patient's bronchi won't dilate when given bronchodilaters
how do you differentiate between a COPD and an asthmatic patient during a methacholine challenge test?
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Bethanechol
a muscarinic agonist that undergoes extremely slow metabolism and has a long lasting effect
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Urecholine
brand name of bethanechol
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PO
in what route is bethanechol administered
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uses of bethanechol
treatment of constipation and digestive muscle weakness, cancels the effect of atropine after a surgery
a muscarinic agonist that is a poison that comes from a mushroom. it is a quaternary nitrogen (amine) and in high doses can pass through the BBB
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signs of muscarine poisoning
headaches, nausea, constrictions of the larynx and then it will progress to: increased saliva secretion, tears, miosis, blurry vision, diarrhea, increased urine excretion, bronchoconstrictions, dyspnea
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8-9 hours
if muscarine poisoning isn't treated within ________ the patient will die
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atropine
antidote to muscarine poisoning
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pilocarpine
alkaloid, muscarinic antagonist, that works mainly on the secretion glands
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uses of pilocarpine
to treat dry mouth and glaucoma, to diagnose CF by using it to increase sweat and then measuring the salt levels in the sweat
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side effects of pilocarpine
signs of acetylcholine overdose, headaches if it passes through the BBB, fogginess
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nicotine
nicotinic agonist, tertiary amine, that causes constriction of the intestines, bladder, and bronchioles
alertness, pleasure, hyperventilation, shaking, seizures, coma, death
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AChE blockers
this group of drugs connects to the serine of acetylcholinesterase so that acetylcholine can't, therefore blocking the enzyme from working
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effect of AChE blockers on skeletal muscle
small dose: increase strength of constriction medium dose: fibrillations, fasciculations large dose: the muscle will be stuck in a state of depolarization
a reversible anti AChE. It is a quaternary amine so it doesnt pierce the BBB or get absorbed in the digestive system. it blocks AChE and affects the neuromuscular junction
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prostigmine
brand name of neostigmine
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PO or IV
routes of administration for neostigmine
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uses of neostigmine
treatment of myasthenia gravis and an antidote of for tubocurarine
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myasthenia gravis
an autoimmune disease that destroys nicotinic receptors of skeletal muscle causing muscle weakness and fatigue
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tubocurarine
a nicotinic inhibitor that is used to paralyze muscles before surgery
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physostigmine
reversible anti AChE, tertiary amine, that is absorbed by the BBB and activates movement of the bladder and digestive system
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eserine
brand name of physostigmine
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uses of physostigmine
antidote of atropine, treats closed angle glaucoma
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pyridostigmine
reversible anti AChE, that has a 3-6 hour active time making it a good treatment for chronic myasthenia gravis
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mestinon
brand name of pyridostigmine
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edrophonium
a reversible anti AChE with a 10-20 minute active time and effects similiar to neostigmine. It is used to diagnose myasthenia gravis
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Alzheimer's
an irreversible condition that slowly gets worse charachterized by: decline in memory, decreased ability to perform routine actions and to orient themselves, decreased language and communication skills, changes in behavior, poor judgement, decreased acetylcholine levels in the brain
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Tetrahydroaminoacridine
medication effective in the early stages of alzheimer's. It slows development of the disease by increasing acetylcholine levels in the brain. It is given 4 times/day
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side effects of THA
nausea and vomiting, diarrhea, anorexia, fogginess, liver damage
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tacrine and cognex
brand names of THA
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donepezil
specifically effects cholinergic receptors in the brain and it doesn't have many side effects. administered once a day
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aricept, memorit
brands names of donepezil
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side effects of donepezil
nausea, vomiting, and diarrhea
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rivastigmine
blocks both acetylcholinesterase and pseudocholinesterase. Has similar effects as donepezil but with more side effects. taken twice a day
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sticker or pill
routes of administration of rivastigmine
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exelon
brand name of rivastigmine
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galantamine
AChE blocker that also activates pre and post-synaptic nicotinic receptors. administered once a day
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side effects of galantamine
nausea, vomiting, and sleep disturbances
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reminyl
brand name of galanatamine
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irreversible AChE blockers
organophosphates that connect covalently to the serine of AChE, this is irreversible and renders the enzyme inactive
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echothiophate
a hydrophilic irreversible AChE blocker. It has a much faster effect than reversible blockers
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drops or eye injection
route of administration of echothiophate
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organophosphates
lipophilic materials that can pierce body systems through the skin, respiratory, and digestive systems. examples include pesticides and nerve agents (gasses)