-
Pilocarpine
- alkaloid --> directly acting
- cholinoceptor activating
- natural alkaloid
- well-absorbed
- uses limited --> opthalmic use
- muscarinic agonist*
-
Bethanechol
- not susceptible to cholinesterase nor nicotinic action.
- susceptible to muscarinic action.
-
Pralidoxime
- "2-PAM"
- can treat the phosphorylation of enzymes of the ireversible organophosphates (pesticides, nerve gas agents- sarin) by reactivating ACHe if not AGED.
- doesn't get into the brain.
- seems to "pick-off" the phosphorous group of ACHe & reactivates it.
- best to be given to "fresh" phosphorylated ACHe.
- seems to work pereferentially at the skeletal N receptor.
-
Carbachol
- not susceptible to cholinesterase.
- more susceptible to nicotinic action than muscarinic.
- ester--> directly acting.
- not susceptible to antagonism by atropine as other esters.
-
ACh
- agonist for both muscarinic & nicotinic cholinergic receptors.
- released from parasympathetic terminals wil activate M receptors.
- released from parasympathetic terminal can interact with presynaptic receptors on the terminals to reduce further transmitter release.
- -on parasympathetic terminals, decrease ACh
- -on sympathetic terminals, decrease E / NE
- ester --> directly acting
- susceptible to cholinesterase, muscarinic, and nicotinic action.
-
Echothiophate
- irreversible inhibitor of cholinesterase.
- used in treatment of glaucoma.
- organophosphorous compound.
- exception to OP's --> poorly absorbed.
- extremely potent choline derivative.
- long acting ( > 100 hours).
-
Endrophonium
- indirectly acting cholinergic agonist.
- short acting (5 minutes).
- reversible.
- quarternary ammonium alcohol (simple alcohol).
- cholinesterase inhibitor.
-
Physostigmine
- indirectly acting cholinergic agonist.
- intermediate acting (0.5-6 hrs).
- reversible cholinesterase inhibitor.
- enters the CNS b/c no (+) charge.
-
Neostigmine
- indirectly acting cholinergic agonist.
- intermediate acting (0.5- 6 hrs).
- reversible cholinesterase inhibitor.
- carbamic acid ester with tertiary or quartenary ammonium.
- mixed function.
- charged --> poorly absorbed.
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