Chapter 4: Cholinergic Agonists Drug Actions Receptor Therapeutic Effects Pharmacokine tics Adverse Effects Others Acetylchol ine (Direct) -decreases heart rate and cardiac output -decrease in BP by activating M 3 receptors on SM of BV -Increases salivary secretion and stimulates intestinal secretions and motility -Bronchiolar secretions are enhanced -Stimulates ciliary muscles to contract for near vision and pupillary muscles to constrict, causing miosis - acts on both muscarini c and nicotinic receptors -no importance therapeutically -Ach (1 % sol n ) instilled into anterior chamber of eye to produce miosis during ophthalmic surgery -actions are rapidly inactivated by Ach- esterase -Quaternary ammonium compound -ATROPINE blocks M receptors and prevents Ach from producing vasodilatation Bethanecho l (Direct) -Acts on the smooth muscles of bladder and GIT -Increased intestinal motility and tone -Expulsion of urine by stimulating detrusor muscle -Lacks nicotinic action -Strong muscarini c activity -Used to stimulate atonic bladder (postpartum, postoperative, nonobstructive urinary retention) -Neurogenic atony -Megacolon -Duration of action of 1 hour -Sweating -Salivation -Flushing -Decreased BP -Nausea -Abdominal pain -Diarrhea -Bronchospasm -Inactivated through hydrolysis by esterases -Ester of carbamic acid Carbachol (Direct) -Ganglion-stimulating activity effects CVS and -Both muscarini -Rarely used therapeutically -Single administratio -Uses in the eye cause -Ester of carbamic acid Sweta Patel Page 1
Chapter 4: Cholinergic AgonistsDrug Actions Receptor
TherapeuticEfectsPharmacokineticsAdverseEfectsOthersAcetylcholine
(Direct)-decreases heart rate and cardiac output-decrease in BP by
activatingM3 receptors on SM of BV-ncreases salivary secretion and
sti!ulates intestinal secretions and !otility -Bronchiolar
secretions are enhanced -Sti!ulates ciliary !uscles tocontract for
near vision and pupillary !uscles to constrict" causing !iosis -
acts on both !uscarinic and nicotinic receptors-no i!portance
therapeutically-Ach #$ % soln& instilled into anterior cha!ber
of eye to produce !iosis during ophthal!ic surgery -actions are
rapidly inactivated by Ach-esterase -'uaternary a!!oniu!
co!pound-A()*P+, bloc-sM receptors and prevents Ach fro! producing
vasodilatation Bethanechol (Direct)-Acts on the s!ooth !uscles of
bladder and .( -ncreased intestinal !otility and tone-,/pulsion of
urine by sti!ulating detrusor !uscle -0ac-s nicotinic action-Strong
!uscarinic activity -1sed to sti!ulate atonic bladder #postpartu!"
postoperative" nonobstructive urinary retention&-+eurogenic
atony-Megacolon -2uration of action of $
hour-S3eating-Salivation-4lushing-2ecreased BP-+ausea-Abdo!inal
pain-2iarrhea-Bronchospas!-nactivated through hydrolysis by
esterases -,ster of carba!ic
acidar!achol(Direct)-.anglion-sti!ulating activity e5ects CVS and
.(6 7rst sti!ulates and then depresses these syste!s -+icotinic
action causes release of epinephrine fro! adrenal !edulla-Causes
!iosis and spas! of-Both !uscarinic and nicotinic activity-)arely
used therapeutically-1sed as a !iotic agentin the eye to treat
glauco!a -Single ad!inistration can last up to $hour-1ses in the
eye cause little or no side e5ects-,ster of carba!ic acid
-Biotransfor!ed by esterases at slo3 rate S3eta Patel Page $Chapter
4: Cholinergic Agonistsacco!!odation #ciliary !uscles are in
constant stateof contraction&Pilocarpine (Direct)-(opical
application to corneaproduces rapid!iosis and contraction of
ciliary !uscles-Sti!ulates secretions #saliva" s3eat"
tears&-Muscarinicactivity-S8ogren9s syndro!e #pilocarpine :
C,VM,0+,&"DO in e!ergency cases of narro3-angle and 3ide-angle
glauco!a -Actions last upto ; hours -C+S disturbances-Sti!ulates
profuse s3eating and salivation -(ertiary a!ine-Can be hydroly
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