Education Anti-cholinergics


Cholinergic agents are compounds which mimic the action of acetylcholine and/or butyrylcholine. In general, the word choline refers to the various quaternary ammonium salts containing the N,N,N-trimethylethanolammonium cation. Found in most animal tissues, choline is a primary component of the neurotransmitteracetylcholine and functions with inositol as a basic constituent of lecithin.  

The parasympathetic nervous system, which uses acetylcholine almost exclusively to send its messages, is said to be almost entirely cholinergic. Neuromuscular junctions, preganglionic neurons of the sympathetic nervous system, the basal forebrain, and brain stem complexes are also cholinergic. In addition, the receptor for the merocrine sweat glands are also cholinergic, since acetylcholine is released from postganglionic sympathetic neurons.

In neuroscience and related fields, the term cholinergic is used in these related contexts:

An anticholinergic agent is a substance that blocks the action of the neurotransmitter acetylcholine at synapses in the central and the peripheral nervous system.These agents inhibit parasympatheticnerve impulses by selectively blocking the binding of the neurotransmitter acetylcholine to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible for the involuntary movement of smooth muscles present in the gastrointestinal tracturinary tractlungs, and many other parts of the body. Anticholinergics are divided into three categories in accordance with their specific targets in the central and peripheral nervous system: antimuscarinic agents, ganglionic blockers, and neuromuscular blockers.

Anticholinergics are classified according to the receptors that are affected:

Examples of common anticholinergics:

Those that preferentially inhibit the reuptake of norepinephrine (by at least 10-fold over serotonin) include:

Whereas either fairly balanced reuptake inhibitors of serotonin and norepinephrine or unspecified inhibitors include:

And the following are TCAs that act via main mechanisms other than serotonin or norepinephrine reuptake inhibition:

Many of the agents proposed to remyelinate are anti-cholinergics.

ProfG has said he is not a fan of these.

Read this as homework for the weekend

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  • As a pwms I am confused as to the desired take away. For example should a pwMS and comorbid breathing conditions avoid or prefer inhaled anti cholinergic such as tiotropium?

  • Even the diphenhydramine (Benadryl) I get before every Ocrevus infusion is an anticholeneric. They’re gonna be hard to avoid.

  • So, time for me to stop taking promethazine on long hall flights. I’ll have to find something else to knock me out (5-10 bloody mary’s Should do the trick.

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