14)Describe the mechanisms by which adrenergic agonists and muscarinicantagonists both produce mydriasis.
Adrenergic agonists stimulate the alpha-adrenergic receptors (α
), which normally occurs due to norepinephrine released fromthe postganglionic fibers to the dilator pupillae muscle, resulting in mydriasis.Muscarinic antagonists prevent parasympathetic stimulation of the constrictor papillaemuscle by acetylcholine causing it to relax, which results in mydriasis.
15)Describe what is meant by denervation supersensitivity.
When the nervous supplyof a muscle or gland is interrupted, the effector organ slowly becomes increasinglysensitive to the neurotransmitter of which it is deprived. This occurs because of upregulation of receptors after one to two weeks.
16)List the common side effects seen with the use of cholinergic antagonists.
Muscarinic receptor antagonists
: dry mouth, constipation, decreased sweating,mydriasis (dilation of pupil), urinary retention (especially in elderly males with benign prostatic hypertrophy), tachycardia, decreased lacrimation, precipitation of glaucoma,and decreased respiratory secretions (increased susceptibility to respiratory infections.
Nicotinic receptor antagonists
(sympathetic and parasympathetic ganglionic blockers):constellation of severe side effects – constipation (blocking enteric ganglia), atony of the bladder, cycloplegia, decreased sweating, postural hypotension, and tachycardia(SA node dominated by parasympathetics).
17)Contrast the therapeutic advantage of pilocarpine to acetylcholine.
exhibits primarily muscarinic receptor agonist actions and it is notdegraded by cholinesterases thus it has a 2-3 hour duration. It can be given orally.
however, is a non-selective agonist of both muscarinic and nicotinicreceptors and its duration is very brief because it is rapidly hydrolyzed by plasmacholinesterases. It cannot be given orally.
18)Describe the differences between a direct and indirect acting cholinergic drug.
agonists bind to the cholinergic receptor and mimic the effects of thenatural receptor ligand acetylcholine.
agonists inhibit the destruction of acetylcholine by acetylcholinesterase,thereby increasing the synaptic concentration of acetylcholine which then acts on thecholinergic receptor.
19)Identify the major advantage for using quaternary cholinesterase inhibitors.
Quaternary cholinesterase inhibitors, neostigmine and edrophonium, do notsignificantly cross the blood-brain barrier, and therefore, they are useful for treating peripheral disorders like intestinal and bladder atony and for the management of myasthenia gravis.
20)Describe the drug of choice for reactivating cholinesterase shortly afterorganophosphate poisoning.
The treatment of choice for severe intoxication withcentrally acting cholinesterase inhibitors is atropine, given in large doses to combat thecentral manifestations (confusion, ataxia, convulsions, coma, and respiratory paralysis)and the peripheral signs (bronchial secretions, hypotension, and involuntary twitchingleading to paralysis) resulting from overstimulation of muscarinic receptors.
isa muscarinic receptor antagonist, a tertiary amine capable of penetrating into the CNSand blocking all subtypes of muscarinic receptors.
21)Describe the major symptoms of a cholinergic crisis.
The common signs of “cholinergic crisis” are salivation, lacrimation, urination, defecation, emesis (“SLUDE”syndrome).
22)Describe the therapeutic uses of muscarinic agonists.