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Muscarinic/Cholinomimetics
Pharmacology
34
Medical
Professional
09/05/2011

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Cards

Term
what recpetors do Ach act on?
Definition
muscarinic and nicotinic receptors
Term
M1,3,5
Definition
Gq-PLC-IP3-DAG
Term
M2,4
Definition
Gi pathway
M2-K+ channels
Term
What are the two types of nicotinic receptors
Definition
ganglia
skeletal muscle end plates
Term
what are the two types of cholinergics?
Definition
direct acting
Indirect (Ach esterase)
don't confuse w/anti-cholinergics!!!
Term
M1 receptors are located where?
Definition
Nerves (Gq)
Term
M2 receptors are located where?
Definition
Heart, nerves, smooth muscle (Gi)
Term
M3 receptors are located where?
Definition
Glands, smooth muscle, endothelium
Term
M4 and 5 receptors are located where?
Definition
CNS
Term
Muscarinic receptor effect on blood vessels
Definition
M3 receptor
NO production in endothelium
decrease resistance and BP
Tachycardia (baroflex)
Term
Muscarinic receptor effect on Heart
Definition
M2
decreases Ca; activates K+ channels
symp nerve endings- inhibit NE
Para nerve endings- inhibit Ach
Term
Muscarinic receptor effect on bronchial smooth muscle
Definition
M3
direct contraction (constriction)
Term
Muscarinic receptor effect on on Bronchial glands
Definition
M3 increased secretion
Term
Muscarinic receptor effect on urinary bladder
Definition
M3
Contraction of detrusor muscle
relaxation of sphincter muscle
Term
Muscarinic receptor effect on GI tract
Definition
M1 receptor- myenteric plexus
M3/M2 secretions muscles
Term
Muscarinic receptor effect on exocrine glands
Definition
M3- incr secretions
Term
Muscarinic receptor effect on the eye
Definition
M3/M2 miosis and accomodation for near vision
lowers intraocular pressure
Term
Muscarinic receptor effect on CNS
Definition
M1- epileptogenesis
M2/4- anagesia
M3-food intake (hypothalamus)
M5- reward circuitry
Term
What are the two groups of direct acting cholinomimetics
Definition
Choline esters and alkaloids
Term
What are the 3 choline esters?
Definition
methacholine, carbachol, bethanechol
Term
PCKN of choline esters
Definition
less susceptible to degradation than Ach
more selective in organ effects
quaternary amine, hydrophillic
poor PO
Term
What are the two natural alkaloids
Definition
Muscarine -quat. less absorbed
Pilocarpine- tert. well absorbed
CAN cross BBB
Term
Methacholine use
Definition
inhalation spray in bronchial provocation test
Term
Carbachol actions
Definition
eye drop
greater nicotinic actions than Ach
Greater GI, Bladder, Eye
Less effective: CV
resist to AchE
Term
Carbachol use
Definition
Wide angle glaucoma
constricts eyes during surgery
Term
Carbachol side effects
Definition
pupillary constriction
cyclospasm
conjunctival hyperemia
Term
Bethanechol PCKN
Definition
musc similar to carbachol
M2/3 receptors
NO nicotinic activity
Term
Bethanechol uses
Definition
resist. to AchE
Urinary retention
Post-op abdominal distention
Term
Bethanechol side effects
Definition
Flushing
epigastric distress, abd cramps
Term
Bethanechol contraindications
Definition
Peptic ulcer
asthma
CV insufficiency
Term
Bethanechol drug interactions
Definition
quinidine and procainamide antagonizes
reserpine- profound hyperthermia
Term
Muscarine
Definition
alkaloid responsible for mushroom poisoning (atropine treats it)
Term
Pilocarpine
Definition
eye drop
M3 activity
reduce open angle glaucoma or closed
Term
Pilocarpine side effects
Definition
ciliary spasm
reduced visual acuity
conjunctival vascular congestion
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