Cholinergic Agents Flashcards
parasympathetic direct agonist activates what
cholinoreceptors
parasympathetic indirect agonist stimulate the release of what
acetylcholine
parasympathetic indirect agonists inhibit what
acetylcholinesterase
Acetylcholine Biosynthesis & Neurotransmission
how is choline transported into the presynaptic nerve terminal?
by a sodium-dependent choline transporter (CHT)
Acetylcholine Biosynthesis & Neurotransmission
what transporter can be inhibited by hemicholinium
sodium-dependent choline transporter (CHT)
Acetylcholine Biosynthesis & Neurotransmission
what enzyme synthesizes choline and acetyl-coa into acetylcholine
choline acetyltransferase (ChAT)
cholinergic agonists are mostly (muscarinic/nicotinic)
muscarinic
what is special about quaternary amines
positive charge
State which receptor affects the following:
Bradycardia
M2, binds in the heart
State which receptor affects the following:
Nausea, cramps, vomiting, diarrhea
M3: bronchiolar smooth muscle
State which receptor affects the following:
visual disturbances
M1
T/F: Charged Muscarine has easy access into the BBB
F
what are the two main classes of direct acting cholinergic agonists
choline esters, alkaloids
what are the four direct acting choline esters
ACh, methacholine, carbachol, bethanechol
what are the two direct acting alkaloids
muscarine, pilocarpine
what are the 3 reversible indirect-acting cholinergic agonists
edrophonium, physostigmine, neostigmine
what is the irreversible indirect-acting cholinergic agonist
organophosphates
another name for direct acting cholinergic agonists
muscarine receptor agonists
another name for indirect-acting cholinergic agonists
AChE inhibitors
what is the effect of M2 activation on the heart
Decrease in heart rate, (bradycardia)
what is the effect of M3 activation on exocrine glands
increase in secretion
what is the effect of M3 activation on smooth muscles
increase in contraction
what is the effect of M3 on sphincters
relaxation
CNS effects are mainly mediated by which muscarinic receptor
M1
T/F Carbachol (a direct acting cholinoceptor agonist) is resistant AChE
True
other name for pilocarbine
isoptocarpine
pilocarbine is used for the treatment of what
glaucoma
T/F Pilocarbine cannot cross the BBB
F
what receptor does pilocarpine target and is it an agonist or antagonist
M3, agonist
what receptor does brimonidine target and is it an agonist or antagonist
alpha2, agonist
what receptor does timolol target and is it an agonist or antagonist
NE-beta, antagonist
what is classified as increased intraocular pressure
glaucoma
carbachol binds with which receptor(s)
muscarinic, nicotinic
pilocarpine binds with which receptor(s)
muscarinic
bethanechol binds with which receptor(s)
muscarinic
varenicline binds with which receptor(s)
nicotinic
which drug is used for the following clinical use: Intraocular use for miosis during surgery
acetylcholine
which drug is used for the following clinical use: intraocular use for miosis during surgery, glaucoma
carbachol
which drug is used for the following clinical use: glaucoma
pilocarpine
which drug is used for the following clinical use: urinary retention, post operative ileus
bethanechol
which drug is used for the following clinical use: smoking cessation
varenicline
which of the following drugs has cholinesterase sensitivity?
a. acetylcholine
b. carbachol
c. pilocarpine
d. bethanechol
e. varenicline
a. acetylcholine
M2 effect on cardiovascular
fall in blood pressure and heart rate
M3 effect on gastrointestinal
smooth muscle contraction/ sphincter relax
M3 effect on bladder
smooth muscle contraction/ sphincter relax
M3 effect on eye
miosis
M3 effect on sweating
increase
match the drug with the clinical use: open-angle glaucoma; dry mouth due to hypofunction of salivary glands e.g. Sjogren’s or cancer radiotherapy
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol
pilocarpine
match the drug with the clinical use: GI stimulation or treatment of urinary retention
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol
bethanechol
match the drug with the clinical use: provocative test for hyperactive airways
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol
methacholine
match the drug with the clinical use: ocular (surgery, glaucoma)
a. pilocarpine
b. bethanechol
c. methacholine
d. carbachol
carbachol
which cholinoreceptor is found at the skeletal muscle endplate
Nm
Which cholinoreceptor is found in autonomic ganglia
NN
which cholinoreceptor is found in the brain
NN
what does dibasic mean
2 nitrogens
effects of nicotine in low doses
stimulate reticular activating system (alerting) and dopamine release (addictive)
effects of nicotine in higher doses
CV effects (hypertension, tachycardia)
effects of nicotine in toxic doses
seizures, loss of receptor selectivity, neuromuscular blockade
what drug is often prescribed for intervention of nicotine dependence
Varenicline (chantix)
mechanism of chantix
an α4β2 neuronal nicotinic receptor partial agonist that binds in the central nervous system
what is the half life of varenicline (chantix) and how does it get excreted?
24 hours, urine
what are the adverse effects of varenicline (chantix)
nausea, headache, abnormal dreams, constipation, vomiting
what are the four forms of nicotine replacement therapy
Nicotrol inhaler, nicotrol nasal spray, nicorette gum, nicoderm transdermal patch
what disease states are a hypofunction of salivary glands
xerostomia and Sjogren’s syndrome
