Acetylcholinesterase is the primary target of these drugs, but (blank) is also inhibited.
butyrylcholinesterase
Acetylcholinesterase is an extremely active enzyme. In the initial catalytic step, acetylcholine binds to the enzyme's active site and is hydrolyzed, yielding free (blank) enzyme.
choline and the acetylated
In the second step, the (blank) bond is split, with the addition of (blank)(hydration). The entire process occurs in approximately
covalent acetyl-enzyme,water , 150 microseconds.
increase the concentration of endogenous acetylcholine at cholinoceptors by inhibiting acetylcholinesterase.
All the cholinesterase inhibitors
The organophosphate inhibitors are sometimes referred to as
"irreversible" cholinesterase inhibitors
_____ are considered "reversible" inhibitors because of the marked differences in duration of action.
Edrophonium and carbamates
Edrophonium
Uses
Myasthenia gravis, ileus, arrhythmias
Myasthenia gravis, ileus
Neostigmine
Myasthenia gravis
Pyridostigmine
For anticholinergic poisoning
Physostigmine
Glaucoma
Echothiophate
5–15 minutes
Approximate Duration of Action
Edrophonium
0.5–4 hours
Neostigmine
4–6 hours
Pyridostigmine
0.5–2 hours
Physostigmine
100 hours
Echothiophate
is an autoimmune neuromuscular disease characterized by weakness and fatigue of the skeletal muscles of the face and extremities.
Myasthenia gravis
It affects people of both sexes and all ages.
Myasthenia Gravis
are affected twice more commonly than male patients.
Female patients
Myasthenia gravis usually strikes in women in their
third decade of life