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53 Cards in this Set

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  • Back
The type of receptor at all preganglionic synapses
Nicotinic (Nn)
The transmitter for somatic motor systems
Nicotinic (Nm)
Postysynaptic and organ response receptors for parasympathetics
Muscarinic
Consists of 5 subunits 2alpha, beta, gamma and delta
motor system nicotinic
This antagonist can be used to distinguish M1 and M2 muscarinic receptors
pirenzepine
High affinity for pirenzepine
M1
Low affinity for pirenzepine
M2
Muscarinic found in vessels and postganlionic effector organs
M3
Muscarinic receptors found in the brain and sympathetic ganglion
M1
Muscarinic receptors found in the heart
M2
Muscarinic Agonists (4)
Methacholine
Carbachol
Bethanechol
Pilocarpine
Nicotinic Agonists (2)
Nicotine
Succinylcholine
Action of agonists at M2 and M3 recptors (6)
1. Stimulate glands
2. Stimulate smooth muscle contraction
3. Relax Sphincters
4. Vasodilation (if IV injected)
5. Cardiac slowing
6. Pupil constriction, accomodation
Used to demonstrate asthma
Methacholine
Used for miosis in opthalmic surgery
Carbechol
Minor uses for urinary retention or paralysis of GI tract
Bethanechol (little effect on CV system and nicotinic sites)
The actions of these drugs can exacerbate asthma, pepetic ulcer, coronary insufficiency and intestinal obstruction
Cholinergic agonists
The use of Pilocarpine
Used to treate open-angle glaucoma. Miosis and accomomodation spasm for upto 1 day
Muscarinic Antagonists (3)
Atropine
Scopolamine
Glycopyrrolate
cause:
excitation or respiration
restlessness
irritability
Atropine
causes:
drowsiness, sleep
hallucinations
delirium
Scopolamine
treatment of atropine poisoning
Physostigmine
(universal distribution, compared to neostigmine)
May cause sharp rise in intraocular pressure in those with narrow angle glaucoma
Atropine
Use of glycopyrolate
prevent excessive salivation caused by inhaled anesthetics
Used in cold preparation for symptomatic relief
Scopolamine
Used to treat overactive bladders
Tolerodine
Ipratropium Bromide
dilates bronchial airways and less drying than atropine.
Nictotine stimuates NMJ or ganglia better?
Ganglia are more sensitive to nicotine than NMJ
Cholinesterase Inhibitors (4)
Physostigmine
Neostigmine
Edrophonium
Pyridostigmine
Absorbed poorly from GI tract and do not penetrate CNS
Relatively selective for the NMJ
Edrophonium, neostigmine and pyridostigmiine
The more lipid soluble cholinesterases that are well absorbed with ubiquitous distribution
physostigmine and isoflurophate
actions of anti-AChE drugs
Miosis, spasm of accomodation
GI contraction
stimulation of skeletal muscle
stimulate glands, contraction, bradycardia and low C.O.
Because of their quaternary ammonium structure, they are poorly absorbed and large oral doses are necessary. Duration 4-6 hours
Anti-AChE drugs (except physostigmine)

Ipratroprium Bromide has quat ammonium
Isoflurophate
organophosphours anti-AChE that binds irreversibly to AChE
(clinically used drug similar to insecticides)
Use to treat intoxication with organophosphates
Pralidoxime (reverse the irreversible binding of isofluorate and regenerates AChE)
Pralodoxime used in the absence of DFP
Weak anti-AChE activity
Parlytic Illeus and Urinary Retention
neostigmine
Glaucoma
physostigmine
Myastenia Gravis
neostigmine, pyridostigmine
Termination of neuromuscular blocade
neostigmine or edrophonium
Atropine poisioning
physostigmine
Non Depolarizing muscle relaxers
Curare
Mivacurium
Rocuronium
Cisatracurium
Depolarizing muscle relaxers
Succinylocholine
Actions of Succinylcholine
depolarize muscle
no CNS effect
bradycardia and hypotension
Histamine release
Used to reverse neuromuscular blockaed by non-depolarizing antagonists
Neostigmine and edrophonium
Risk when using halogenated anestehtics and succinylcholine
malignant hyperthermia (treat with dantrolene)
Which sphincters are naturally contracted in man
Cardiac
Pyloric
Ileocecal
Which cholinergic agonist has action on both muscarinic and nicotinic receptors
Carbechol
Which cholinergic agonist is not antagonized by atropine
Carbechol (acts on N and M receptors)
What are the relative sensitivities to atropine
Salivary, respiratory, cardiac and ophthalmic are more sensitivie than GI and GU
Which effects of nicotine does tolerance develop in and which does it not
Tolerance to GI effects
no tolerance to cardiovascular effects
Tetracycline and Succinylcholine
Tetra's chelate calcium (need for exocytosis) and thus potentiate NMJ blockade
To prevent injury when performing ECT
Succinylcholine (depolarizing NMJ blocker)