Anticholinesterases Flashcards
What is cholinesterase?
enzyme that hydrolyse ACh to acetyl and choline
Name the 2 types of cholinesterases?
acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE)
Anticholinesterase is directly acting cholinergic drug. T/F
F. Indirectly acting
Examples of reversible anticholinesterase
Edrophonium , Pyridostigmine, Physostigmine
What is the drug name for irreversible anticholinesterase?
Ecothiopate
Why neostigmine cannot cross BBB?
Has quaternary ammonium group; lipid insoluble
Why physostigmine can cross BBB?
Has carbamate group but no quaternary ammonium group; lipid soluble thus can cross BBB
Why pyridostigmine is quite similar to neostigmine?
The chemical structure is similar except the quaternary amm group is incorporated into phenol ring
What drug is used to diagnose myasthenia gravis?
Edrophonium
What drug is used to reverse competitive neuromuscular block?
Neostigmine (IV)
What drug is used to manage myasthenia gravis?
Neostigmine and pyridostigmine (oral)
What happen if cholinergic receptors are overstimulated?
DUMBBELLS
Diarrhea, urination, miosis, bradycardia, bronchorrhea, emesis, lacrimation, salivation/sweating
What drug is used to treat paralytic ileus and atony of bladder?
Neostigmine
Why ecothiopate is used to treat glaucoma?
Stimulate muscarinic receptor and constrict the sphinter pupillae and ciliary muscle = miosis
What is the muscarinic side effects of anticholinesterase?
SLUDGE
Salivation, lacrimation, diaphoresis, GI upset, emesis