CHOLINERGICS

ACh M1, M2, M3 MOA -All choline esters/natural alkaloids activate M1, M2, M3 receptors -postsynaptic receptors alter function of effector organ -presynaptic receptors inhibit release of neurotransmitter MOA

USE

Diarrhea Urination Miosis Bronchicon Bradycardia Excitation o Lacrimation Salivation

Carbachol * insensitive to Ach Esterase

USE
Open Angle Glaucoma o Causes contraction of ciliary muscle resulting in outflow through trabecular meshwork Stimulates both N & M receptors

Diarrhea Urination Miosis Bronchicon Bradycardia Excitation o Lacrimation Salivation

Bethanechol * insensitive to Ach E * No Nicotinic effect Pilocarpine -tertiary amine form from plant genus Pilocarpus Muscarine -quaternary ammonium compound from mushrooms Inocybe and Clitocybe Edrophonium

M1, M2, M3

MOA

USE
Bowel & Bladder Constipation Urinary Retention (post-op/postpartum) Xerostomia Post-op nonobstructive ileus Neurogenic Bladder

Diarrhea Urination Miosis Bronchicon Bradycardia Excitation o Lacrimation Salivation

M1, M2, M3

MOA

USE
Open Angle Glaucoma o Causes contraction of ciliary muscle resulting in outflow through the trabecular meshwork Xerostomia due to Siorgen Syn. or radiation

Diarrhea Urination Miosis Bronchicon Bradycardia Excitation o Lacrimation Salivation

M1, M2, M3

MOA

USE **Poisoning from mushroom is called mycetism

Indirect Cholinergic Agonist Reversible Cholinesterase Inhibitor

MOA -reversibly binds to the active site of enzyme so preventing Ach abscess

USE
Diagnosis of Myasthenia Gravis Differentiate between MG & Cholinergic Crisis o MG Improvement of symptoms

Excessive D

CC symptoms get worse

Physostigmine -carbamate

Indirect Cholinergic Agonist Reversible Cholinesterase Inhibitor Indirect Cholinergic Agonist Reversible Cholinesterase Inhibitor Indirect Cholinergic Agonist Reversible Cholinesterase Inhibitor Indirect Cholinergic Agonist Irreversible Cholinesterase Inhibitor

MOA -undergo two-step hydrolysis similar to Ach, but is more resistant to hydrolysis MOA -undergo two-step hydrolysis similar to Ach, but is more resistant to hydrolysis * can also directly activate nicotinic receptors at neuromus. junction MOA -selective inhibitor of Ach E in the BRAIN

USE
Glaucoma Bowel & Bladder Atonia Overdose of
o o

Convulsion Muscle Par Excessive D

Atropine Phenothiazide Neuroleptics TCAs

Neostigmine -carbamate

USE
Reversible Cholinesterase Inhibitor Myasthenia Gravis treatment Paralytic Ileus Antidote for Polarizing NMJ blockade (tubocurarine)

Excessive D

Donezepil

USE
Treatment of ALZHEIMERS by slowing the deterioration of cognitive function

Parathion
(organophosphate)

MOA -binds to the esteratic site; phosphorylated enzyme is extremely stable Aging loss of alkyl group strengthens complex MOA - Spontaneous hydrolytic regeneration of phosphorylated Ach E -Oximes have high affinity for Phosphorus atom and can rapidly regenerate the enzyme IF it did not AGE

USE
Insecticide

Diarrhea Urination Miosis Bronchicon Bradycardia Excitation o Lacrimation Salivation

Pralidoxime

Ach E reactivator

USE
AChEsterase Reactivator in Organophosphate poisoning

-Muscu he