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31 Cards in this Set

  • Front
  • Back
ACh synthesis
- ChAT is the enzyme and its superfast
- get actyl from mito and choline from HAChTS (transport system)
ACh release
- AP -> Na entry -> depol,
- opens voltage-dependent Ca channels -> fusion of vesicles w/ PM and release
ACh metaboism
- AChE at pre and post synaptic elements
- BtCHE - plasma cholinestrase (nonspecific)
Muscarinic receptors
- on all autonomic effector cells, certain autonomic ganglion cells, and in CNS
- slow relative to nicotinic
- on Cholinergic pre elements for feedback
- G-protein-linked and
Nicotinic recetpors
- ones of autonomic ganglion distinct from ones at NMJ
- ligand-gated ion channels - binding of ACh -> rapid net influx of Na+ and Ca2+ into the cell -> depol
M1, M3, and M5
stimulate PIP2
M2, M4
inhibit cAMP
for skeletal muscle
parasympathomimetic drugs
act as direct agonists at cholinergic receptors
- direct parasympathomimetic
- B-methyl sub makes it a muscarinic agonist
- longer duration than Ach b/c is hydrolysis at 1/3 the rate as ACh
- used to test for bronchial hyperactivity and asthmaha
- SE after s.c. injection are hypotension, NandV, asthma attacks, heart block, SLUDS
- direct parasympathomimetic
- a carbamate sub that protects is, so long duration
- not selective
- gets muscarinic of ciliary to cause miosis and open canals
- so topically for glaucoma
- direct parasympathomimetic
- like methacholine and carbachol w/ a 13-methyl sub and a carbamate sub
- long (2-3 hour) duration
- selective for muscarinic
– orally or s.c., it exerts only mild CV - gets mainly the GI and bladder
– used to increase tone and contractions of pts intestine and bladder
- direct parasympathomimetic
- plant alkaloid
- selective for muscarinic
- not a choline ester, sp ChEs dont work
- 2-3 hour duration
- topically like carbachol for glaucoma
- systematically, you get usual side effects
will block or reverse the adverse effects of parasympathomimetics
- Reversible ChE Inhibitor
- short duration
– used as MG diagnostic test as IV will reverse muscle weakness
- Reversible ChE Inhibitor
- quaternary amine
– wont cross BBB, so good for peripheral disorders
– stimulates GI contractions and secretions, contractions of bladder, and improves neurotransmission at somatic nerves and SkM
– used for intestinal and bladder atony and for MG
- pyridostigmine and ambenonium replacing b/c they last longer
- Reversible ChE Inhibitor
- tertiary amine from plant
- can penetrate into CNS
- topically for glaucoma
Reversible cholinesterase inhibitors
- carbamyl esters that hydrolyze the ester linkage
– E site more resistant than A site, which slows the hydrolysis of Ach
– the free site can regenerate so its reversible
Irreversible cholinesterase inhibitors
- aka organophosphate ChEs
- inhibit AChE and plasma ChE
- when it interacts, its hydrolzed, but the Pd E site is not
- the free active site regenerates slowly or not at all
- recovery depends on the synthesis of new enzyme
- irreversalbe ChE inhibitor
– topically for glaucoma
- long duration, should
- overuse can lead to SLUD
- use to treat an overdose of irreversible ChE inhibitors
- if used prior to aging (alkyl group more tightly bound to E site), frees enzyme to an active unit
- most striking effect occurs at the NMJ
- does not penetrate BBB
methacholine trade name
carbachol trade name
(Carbastat; Isopto Carbachol)
bethanechol trade name
(Urecholine; Duvoid)
pilocarpine trade name
(Pilocar; Isopto Carpine)
edrophonium trade name
(Enlon; Reversol; Tensilon)
neostigmine trade name
physostigmine trade name
(Antilirium; Isopto Eserine; Synapton)
DFP trade name
pralidoxime trade name