Autonomic Pharmacology 3 Flashcards
What are the 2 classifications for cholinergic agonists?
muscarinic and nicotinic
Name 4 choline esters.
acetylcholine
carbachol
bethanechol
methacholine
Are choline esters poorly or well absorbed from the GI tract?
poorly absorbed
Classify ACh, carbachol, and bethanecol as:
-nicotinic
-muscarinic
-nicotinic and muscarinic
-neither nicotinic nor muscarinic
ACh and carbachol = nicotinic and muscarinic
bethanecol = muscarinic
Which 2 choline esters are not hydrolized by acetylcholinesterase?
carbachol and bethanecol
Which drug (choline ester) is used as a challenge to test for asthma?
methacholine
TRUE or FALSE: muscarinic agonists are both parasympathomimetic and sypathomimetic.
FALSE –> muscarinic agonists are parasympathomimetic
Name 3 muscarinic agonists.
muscarine, oxotremorine, pilocarpine
How do muscarinic agonists affect heart rate?
decreases heart rate
How do muscarinic agonists affect blood vessel dilation/constriction? Explain the process.
muscarinic agonist binds to M3 on the blood vessel ENDOTHELIUM –> nitrogen monoxide (NO) is released from the endothelium –> NO stimulates guanylyl cyclase and production of cyclic GMP –> vascular smooth muscle relaxes –> blood vessel DILATES
How do mAChR agonists affect the bronchiole smooth muscle?
mAChR agonists contract the bronchiole smooth muscle
TRUE or FALSE: increased secretion at the mAChR can relieve asthma.
FALSE –> increased secretion at mAChR EXACERBATES asthma b/c it causes CONTRACTION of bronchiole smooth muscle (restrict airway)
mAChR agonists ____________ secretion of saliva and stomach acid. mAChR agonists also ___________ motility and peristalsis.
Fill in the blanks with either ‘increase’ or ‘decrease’.
mAChR agonists INCREASE both secretion of saliva and stomach acid, and motility and peristalsis
Do mAChR agonists in the bladder promote or inhibit micturition/voiding/urination?
mAChR agonists PROMOTE micturition
What is the major nicotinic agonist?
Nicotine
What are some of the main CNS effects of nicotinic agonists? What do high doses cause? What do the highest doses cause?
- mild STIMULATION
- high dose causes EMESIS
- highest dose causes COMA
TRUE or FALSE: Muscarine can be used as an insecticide.
FALSE –> NICOTINE and MALATHION act as insecticides
Which branch(es) of the ANS does nAChR stimulate? What branch(es) of the ANS does mAChR stimulate?
nAChR - both sympathetic and parasympathetic
mAChR - parasympathetic only
Are nicotine’s cardiovascular effects sympathetic or parasympathetic? Give some examples of the effects.
sympathetic; e.g. hypertension, cardiac stimulation
Are nicotine’s effects on the GI tract sympathetic or parasympathetic? Give some examples of the effects.
parasympathetic; increased secretion and motility
What are the skeletal muscle effects of nAChR?
a) depolarization/excitation
b) hyperpolarization/inhibition
a) depolarization/excitation
What is the function and mechanism of an anticholinesterase?
function: stimulate both nAChR and mAChR
mechanism: prevent hydrolysis of ACh
Do anticholinesterases directly stimulate their receptors? Why or why not?
- NO –> anticholinesterase INDIRECTLY stimulates nAChR and mAChR
- indirect stimulation b/c anticholinesterase acts by preventing hydrolysis of ACh
Which 2 anticholinesterases have reversible action and can be used therapeutically? Describe their structures.
EDROPHONIUM - simple alcohol
NEOSTIGMINE - carbamic ester of alcohols with quaternary/tertiary ammonium group
Which anticholinesterase can be used as an insecticide? Describe its structure.
MALATHION - organophosphate
Which anticholinesterase acts as nerve gas? Describe its structure?
SOMAN - organophosphate
Which 4 locations of the body are anticholinesterases best absorbed?
skin, gut, lung, conjuctiva (eye)
What are the effects of anticholinesterases on the eyes?
miosis, myopia, decreased IOP (intra-ocular pressure)
What are the effects of anticholinesterases on respiration?
bronchiole constriction, increased secretion
What is the effect of anticholinesterases on the gut?
increased motility