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Re:Neuroleptics brain specific antihistaminergic?

Posted by undopaminergic on February 6, 2023, at 12:58:00

In reply to Re:Neuroleptics brain specific antihistaminergic?, posted by SLS on February 6, 2023, at 8:03:02

> Hi.
> In re: The Blood-Brain Barrier and anticholinergic drugs.
> Anticholinergic drugs enter the brain at different rates.
> Trospium (Sanctura) is an anticholinergic (muscarinic) drug used to treat overactive bladder, a peripheral function. However, it seems to be blocked from entering the brain almost entirely by the BBB. It can't even be detected in the cerebrospinal fluid (CSF). Trospium effectively treats a broad array of maladies like overactive bladder. It accomplishes this by reducing the tone of the muscles involved. Anticholinergics work by blocking the (muscranic) acetylcholine receptors that normally innervate muscles to contract. These are peripheral effects. However, when an anticholinergic drug makes its way into the brain / CNS, central side-effects can occur:
> 1. Short-term: Produces impairments in cognition and memory, confusion, impaired concentration, restlessness, agitation, and delirium.
> 2. Long-term: Increases risk for developing irreversible dementia.
> Hopefully, the risk of contracting dementia when using trospium long-term will be much lower than for other anticholinergic drugs.
> - Scott

For local (such as nasal mucosa) treatment ipratropium and tiotropium are other antimuscarinics that don't cross the blood-brain-barrier. I'm using the former to reduce night-time salivation.





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