Flashcards in Pharm1E1 Cholinergic Agonists Deck (44):
only in CNS?
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 ?
M2 receptors are coupled to inhibitory ? proteins
-inhibits production of ?
-leads to ? through the opening of K channels
nicotinic receptors are ?, ? channels
(muscarinic is 7 transmembrane G)
both Nn and Nm mediate fast ? ? potentials resulting in the activation of the post synaptic cell
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 ?
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 ?
Nm receptors responds to both ? and ?
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
only high IV doses for short term effects
reduce postop IOP
last about 20 min
used in sweat spot test for diabetics
longer lasting than Ach, more resistant to AchE
used to Dx bronchial airway hypersensitivity via bronchoconstriction
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 ?
nicotine (it can only bind here)
promotes urination, NONobstructive urinary retention
only choline ester given SYSTEMICALLY
CAN cross BBB
some are highly soluble and readily absorbed i.e. ?
some are quarternary amines and less readily absorbed i.e.?
no clinical uses
psychodelic effect- amanita muscaria (mushroom)
initial, acute treatment of open angle GLC
sjogren's syndrome- xerostomia
reverses mydratic actions
dont use in IOP that are >45 because it can close the angle further!
increase HR, secretions of NE&Epi
increase tone and motility of GI
(both PNS and SNS b/c it's nicotinic)
clinically used as a smoking cessation agent
partial agonist at neuronal nicotinic receptors
neuropsychiatric changes i.e. agitation, depressed mood, suicidal thoughts
vasodilation from release of nitric oxide
endothelium not intact
quarternary alcohols and carbamates are ?
organophosphates are ?
-last ? due to the ? bonding
-if given early enough- ? (cholinesterase regenerator) can treat patients suffering from organophosphate poisoning
hundreds of hours, covalent
moderate doses of cholinesterase inhibitors (indirect) will reduce HR/CO and increase ?, BUT large/toxic doses will result in marked bradycardia, reduced CO and ?
indirect acting reversible cholinesterase inhibitors
Dx of myasthenia gravis- increase in muscle strength is positive
assesses the long term anticholinesterase therapy used in MG (pryidoSTIGmine)
*decrease in muscle strength would indicate that they have been exposed to an anticholinesterase insecticide; driven from stimulation to depolarizing inhibition
antidote for anti-muscarinic toxicity
miosis, accomodation, decrease in IOP
nonobstructive paralytic ileus, postop atony of bladder
post-op bladder retention
REVERSES anaesthesia by reversing NM blockade
MG gravis FIRST LINE Tx
NM blockade reversal
**prophylactic Tx of NERVE GAS
Alzheimers disease Tx- 3
derived from daffodils
PD w/ dementia
used for MG
rarely used due to liver toxicity
malathion & parathion
nerve agents (gases)
irreversible cholinesterase inhibitors- mostly pesticides
low lipid solubility
used in GLC
opthal drops for GLC
organophosphate poisoning can be treated with ? (nucleophile) via regenerating the enzyme if given before ? occurs
rapidly metabolized by birds and mammals to non-toxic metabolites but not insects or fish
NOT rapidly detoxified in vertebrate; more dangerous and not available