Increases secretions from salivary, lacrimal & sweat glands.
PILOCARPINE
The drug is unaffected by acetylcholinesterase & works on muscarinic receptors
PILOCARPINE
is used to stimulate miosis & opening the trabecular meshwork around the canal of Schlemm to treat glaucoma.
PILOCARPINE
those that result from excessive generalized cholinergic stimulation
CARBACHOL
generalized cholinergic stimulation
METHACHOLINE
CNS disturbances such as hallucinations & convulsions along with generalized cholinergic stimulations
PILOCARPINE
HYDROLYSIS
is accomplished by the action of _____, which is present in high concentrations in cholinergic synapses.
acetylcholinesterase
The _____ cholinomimetics have their primary effect at the active site of this enzyme, although some also have direct actions at nicotinic receptors.
indirect-acting
There are three chemical groups of cholinesterase inhibitors:
simple alcohols
carbamic acid esters of alcohols
organic derivatives of phosphoric acid
bearing a quaternary ammonium group (Edrophonium)
simple alcohols
having quaternary or tertiary ammonium groups (carbamates, neostigmine)
carbamic acid esters of alcohols
(organophosphates, echothiophate).
organic derivatives of phosphoric acid
are synthetic quaternary ammonium agents used in medicine
Edrophonium, neostigmine, and pyridostigmine
is typical of a large group of carbamate insecticides designed for very high lipid solubility so that absorption into the insect and distribution to its central nervous system are very rapid
Carbaryl (carbarilcarbaril)
a naturally occurring carbamate, is a tertiary amine.
Physostigmine
is not an ester but binds to the active site of the enzyme
Edrophonium
is used as an insecticide
Carbaryl
Many of the_____ (echothiophate is an exception) are highly lipid-soluble liquids. EchothiophateEchothiophate, a thiochol ine derivative, is of clinical value because it retains the very long duration of action of other organophosphates but is more stable in aqueous solution.
organophosphates
is an extremely potent "nerve gas."
Sarin
are thiophosphate (sulfur-containing phosphate) prodrugs that are inactive as such; they are converted to the phosphate derivatives in animals and plants and are used as insecticides.
Parathion and malathion