Anticholinesterases Flashcards
AchE
Most active in hydrolyzing Ach to acetate nad choline
In CNS, ganglia, post ganglionic PS fibers and NMJ
Butyrylcholinesterase
In plasma, liver, insestines, and skin
Important for metabolism of some drugs
Point mutations increase procaine duration to days
Impact of AChE inhibitor depends on
Tone present at organ
Physostigmine
Uses for glaucoma and to increase tone in bladder and GI after surgery
High doses can cause paralysis, can be poison, or antidote in atropine posioning
Physostigmine distribution
COunteract restlessness, tremors, confusion, ataxia
Slurred speech or hallucinations from dextromethorphan abuse, dissociateive anesthesia (PCP, ketamine)
Neostigmine
Synthetic version of physostigmine but does NOT cross BBB
Antidote to tubocurarine poisoning
Improves smptoms of MG and xerostomia and induces tone in GI and bladder
Edrophonium
Diagnosis of MG
Echthiophate
Irreversible
Prolonged Tx of glaucoma
Parathion
Cross BBB and irreversible
Cousin malathion is used for head lice
Need O to S substitution to become active…more efficient in insects
IN presence of Stigmines, AChE is
Carbamoylated
In presence of organophosphates, AChE is
Phophorylated and “ages”
Can occur fast and antidote is pralidoxime
Nerve gas symptoms
Miosis, blurred vision, sweating, broncho…etc.
Antidote and prophylactics for organophosphates
Atropine, scopolamine, 2-PAM are antidotes
Pyridostigmine is prophylactic
Parathion solubility
Penetrates skin and mucous membranes
Access to CNS
Tertiary like physostigmine can cross BBB while quaternary cnanot
