Pharm1E1 Cholinergic Agonists Flashcards
muscarinic receptors
only in CNS?
inhibitory?
stimulatory?
M4, M5
M2, M4 (M2 decreases effects on heart)
M1, M3, M5
M1 and M3 receptors are coupled to stimulatory ? proteins
- leads to an increase in ? and ?
- leads to an increase in intracellular ?
Gq/11 G-proteins
IP3, DAG
Ca2+
M2 receptors are coupled to inhibitory ? proteins
- inhibits production of ?
- leads to ? through the opening of K channels
Gi/G0
cAMP
hyperpolarization
nicotinic receptors are ?, ? channels
muscarinic is 7 transmembrane G
pentameric, ion
both Nn and Nm mediate fast ? ? potentials resulting in the activation of the post synaptic cell
excitatory, postsynaptic
direct effects of muscarinic agonists on the CV system can be altered through ?
EX: IV infusion of a low dose of Ach will cause a drop in blood pressure that is detected by ?, resulting in an ?
-a larger dose of Ach will ? due to a slowed firing rate w/in the ? and a decreased conduction velocity of the ?
reflex arcs
baroreceptors, increase in SNS stimulation on the heart- increase HR- reflex tachycardia
result in bradycardia, SA node, AV node
muscarinic agonists on the ? terminals decrease the release of ? or ?
presynaptic nerve
Ach, NE
Nm receptors responds to both ? and ?
nicotine, acetylcholine
continued exposure to a nonhydrolyzable agonist like ? will lead to ? and eventually a ?
nicotine, depolarization blockade, flaccid paralysis
hyperthyroidism, asthma, CAD (hypotension), acid peptic disorders (increased gastric secretion), obstructive urinary retention
contraindications of choline esters
acetylcholine
bethanechol
carbechol
methacholine
choline esters
only high IV doses for short term effects
reduce postop IOP
last about 20 min
used in sweat spot test for diabetics
acetylCHOLine
longer lasting than Ach, more resistant to AchE
used to Dx bronchial airway hypersensitivity via bronchoconstriction
methaCHOLine (provoCHOLine)
is mostly NICOTINIC (other esters are M3)
increase in skeletal muscle activation
limit to opthalmic applications
IF YOU GIVE ATROPINE- it will block ? and you will see all of the effects of ?
carbaCHOL
muscarinic receptors
nicotine (it can only bind here)
promotes urination, NONobstructive urinary retention
only choline ester given SYSTEMICALLY
bethaneCHOL (URecholine)
CAN cross BBB
some are highly soluble and readily absorbed i.e. ?
some are quarternary amines and less readily absorbed i.e.?
cholinomimetic alkaloids
nicotine
muscarine
muscarINE
pilocarpINE
nicotINE
vareniclINE
alkaloids