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53 Cards in this Set
- Front
- Back
The type of receptor at all preganglionic synapses
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Nicotinic (Nn)
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The transmitter for somatic motor systems
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Nicotinic (Nm)
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Postysynaptic and organ response receptors for parasympathetics
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Muscarinic
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Consists of 5 subunits 2alpha, beta, gamma and delta
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motor system nicotinic
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This antagonist can be used to distinguish M1 and M2 muscarinic receptors
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pirenzepine
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High affinity for pirenzepine
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M1
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Low affinity for pirenzepine
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M2
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Muscarinic found in vessels and postganlionic effector organs
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M3
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Muscarinic receptors found in the brain and sympathetic ganglion
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M1
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Muscarinic receptors found in the heart
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M2
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Muscarinic Agonists (4)
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Methacholine
Carbachol Bethanechol Pilocarpine |
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Nicotinic Agonists (2)
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Nicotine
Succinylcholine |
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Action of agonists at M2 and M3 recptors (6)
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1. Stimulate glands
2. Stimulate smooth muscle contraction 3. Relax Sphincters 4. Vasodilation (if IV injected) 5. Cardiac slowing 6. Pupil constriction, accomodation |
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Used to demonstrate asthma
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Methacholine
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Used for miosis in opthalmic surgery
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Carbechol
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Minor uses for urinary retention or paralysis of GI tract
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Bethanechol (little effect on CV system and nicotinic sites)
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The actions of these drugs can exacerbate asthma, pepetic ulcer, coronary insufficiency and intestinal obstruction
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Cholinergic agonists
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The use of Pilocarpine
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Used to treate open-angle glaucoma. Miosis and accomomodation spasm for upto 1 day
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Muscarinic Antagonists (3)
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Atropine
Scopolamine Glycopyrrolate |
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cause:
excitation or respiration restlessness irritability |
Atropine
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causes:
drowsiness, sleep hallucinations delirium |
Scopolamine
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treatment of atropine poisoning
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Physostigmine
(universal distribution, compared to neostigmine) |
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May cause sharp rise in intraocular pressure in those with narrow angle glaucoma
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Atropine
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Use of glycopyrolate
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prevent excessive salivation caused by inhaled anesthetics
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Used in cold preparation for symptomatic relief
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Scopolamine
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Used to treat overactive bladders
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Tolerodine
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Ipratropium Bromide
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dilates bronchial airways and less drying than atropine.
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Nictotine stimuates NMJ or ganglia better?
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Ganglia are more sensitive to nicotine than NMJ
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Cholinesterase Inhibitors (4)
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Physostigmine
Neostigmine Edrophonium Pyridostigmine |
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Absorbed poorly from GI tract and do not penetrate CNS
Relatively selective for the NMJ |
Edrophonium, neostigmine and pyridostigmiine
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The more lipid soluble cholinesterases that are well absorbed with ubiquitous distribution
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physostigmine and isoflurophate
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actions of anti-AChE drugs
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Miosis, spasm of accomodation
GI contraction stimulation of skeletal muscle stimulate glands, contraction, bradycardia and low C.O. |
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Because of their quaternary ammonium structure, they are poorly absorbed and large oral doses are necessary. Duration 4-6 hours
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Anti-AChE drugs (except physostigmine)
Ipratroprium Bromide has quat ammonium |
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Isoflurophate
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organophosphours anti-AChE that binds irreversibly to AChE
(clinically used drug similar to insecticides) |
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Use to treat intoxication with organophosphates
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Pralidoxime (reverse the irreversible binding of isofluorate and regenerates AChE)
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Pralodoxime used in the absence of DFP
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Weak anti-AChE activity
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Parlytic Illeus and Urinary Retention
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neostigmine
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Glaucoma
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physostigmine
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Myastenia Gravis
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neostigmine, pyridostigmine
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Termination of neuromuscular blocade
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neostigmine or edrophonium
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Atropine poisioning
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physostigmine
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Non Depolarizing muscle relaxers
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Curare
Mivacurium Rocuronium Cisatracurium |
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Depolarizing muscle relaxers
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Succinylocholine
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Actions of Succinylcholine
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depolarize muscle
no CNS effect bradycardia and hypotension Histamine release |
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Used to reverse neuromuscular blockaed by non-depolarizing antagonists
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Neostigmine and edrophonium
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Risk when using halogenated anestehtics and succinylcholine
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malignant hyperthermia (treat with dantrolene)
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Which sphincters are naturally contracted in man
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Cardiac
Pyloric Ileocecal |
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Which cholinergic agonist has action on both muscarinic and nicotinic receptors
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Carbechol
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Which cholinergic agonist is not antagonized by atropine
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Carbechol (acts on N and M receptors)
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What are the relative sensitivities to atropine
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Salivary, respiratory, cardiac and ophthalmic are more sensitivie than GI and GU
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Which effects of nicotine does tolerance develop in and which does it not
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Tolerance to GI effects
no tolerance to cardiovascular effects |
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Tetracycline and Succinylcholine
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Tetra's chelate calcium (need for exocytosis) and thus potentiate NMJ blockade
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To prevent injury when performing ECT
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Succinylcholine (depolarizing NMJ blocker)
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