Does Sertraline block acetylcholine? (1+ effects)

In this article, we will answer the question, “Does Sertraline block acetylcholine?”. We will discuss the mechanism through which Sertraline inhibits acetylcholine, what research suggests and what other possible anticholinergic effects can occur while taking Sertraline.

Does Sertraline block acetylcholine?

Yes, Sertraline can block acetylcholine. Sertraline is an antidepressant that affects serotonin levels and is not an anticholinergic drug. However, Sertraline may inhibit acetylcholine to some extent and this inhibition depends on various factors.

Sertraline (also known as Zoloft), is an antidepressant drug belonging to the class of selective serotonin reuptake inhibitors (SSRIs). This medication is approved by the FDA to help in the management of various depressive illnesses like major depressive disorder (MDD), obsessive-compulsive disorder (OCD), premenstrual dysphoric disorder (PMDD) etc. (1).

Acetylcholine is a neurotransmitter required by the body for various processes. It is most commonly present in the neuromuscular junction and plays a role in the regulation of blood pressure, intestinal movements and cardiac rhythms (2).

The inhibition of acetylcholine can cause an array of side effects like dry mouth, constipation, blurred vision and even cognitive impairment. Sertraline may show anticholinergic activity and trigger these side effects.

However, Sertraline does not show anticholinergic activity in every individual taking the medication. The side effects caused by Sertraline may vary from person to person.

How does Sertraline block acetylcholine?

SSRIs like Sertraline are found to have a mild effect on the inhibition of nicotinic acetylcholine receptors. This inhibition can cause side effects like dry mouth, constipation, blurred vision etc.

Keep in mind that not all individuals experience this anticholinergic effect of Sertraline. The occurrence of side effects depends on various factors with individual variability being the most important one.

If you experience any of these side effects or any other symptoms that do not resolve on their own, make sure to contact your healthcare provider for proper guidance.

What does research suggest?

Research studies have shown the impact of Sertraline and other SSRIs in inhibiting the acetylcholine receptors.

A study assessing the antidepressant effects of SSRIs stated that this class of medications can also act on neurotransmitters other than serotonin. The SSRIs may act on the nicotinic acetylcholine receptors which also help in mood regulation (3).

Another study assessed the activity of SSRIs including Sertraline on the neurotransmitter acetylcholine. This study reported that Sertraline, Paroxetine, Nefazodone and Venlafaxine can inhibit the nicotinic acetylcholine receptors and could play a role in depressive illnesses (4).

One study examining the effects of SSRIs on neuronal nicotinic acetylcholine receptors also concluded that this class of medications can have an inhibitory effect on acetylcholine. Acetylcholine is needed for the regulation of mood and any related disorder (5).

What are the anticholinergic side effects caused by Sertraline?

Sertraline is not associated with severe anticholinergic side effects like other medications. Paroxetine, of the same class of drugs, shows more side effects as compared to Sertraline. However, some individuals taking Sertraline have reported the occurrence of the following anticholinergic side effects:

Dry mouth

Dry mouth is a common side effect that can occur if a medication has anticholinergic properties. Sertraline may also cause dry mouth in individuals taking the medication.

Constipation

Another frequently reported side effect of anticholinergic medication is the occurrence of constipation. This can occur as a side effect of the anticholinergic properties of Sertraline on the gastrointestinal tract of individuals taking this medication.

Keep in mind that Sertraline tends to cause different side effects in different individuals. Not all patients taking Sertraline will experience these or any other anticholinergic side effects. However, these effects should be considered while starting or stopping treatment with Sertraline.

What are the other side effects of Sertraline?

Sertraline may cause other side effects like:

Make sure to have open communication with your doctor about any side effects or unusual symptoms that you may experience while taking Sertraline.

What to do if Sertraline causes anticholinergic side effects?

If Sertraline blocks acetylcholine to such an extent that it causes anti-cholinergic side effects, you should monitor any symptoms that may present a problem.

The first thing that you should do on experiencing any such side effect is to contact your healthcare provider. Your doctor will assess your situation and figure out the underlying cause of your symptoms.

You should monitor and record all of your symptoms so that you can report them to your healthcare provider. Your doctor will assess your situation and recommend an appropriate plan of action.

Your healthcare provider may lower the dose of Sertraline to help manage the side effects or may change your medication altogether. Your doctor may prescribe you another medication that is better tolerated by your body.

Make sure to not stop this medication cold turkey. If you abruptly stop taking Sertraline, you may experience a withdrawal syndrome which may worsen your condition.

To the best of my knowledge and according to research, Sertraline does have a mild blocking effect on acetylcholine. It also does not cause severe anticholinergic side effects and is normally well-tolerated by individuals receiving therapy.

In my opinion, if Sertraline causes side effects that increase discomfort and do not subside, you should consult your healthcare provider for a detailed assessment of the situation and guidance on management strategies.

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References

1.-

The Food and Drug Administration (FDA). HIGHLIGHTS OF PRESCRIBING INFORMATION. ZOLOFT® (sertraline hydrochloride) tablets, for oral use. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019839s74s86s87_20990s35s44s45lbl.pdf 

2.-

Sam C, Bordoni B. Physiology, Acetylcholine. [Updated 2023 Apr 10]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-. Available from: https://ncbi.nlm.nih.gov/books/NBK557825/

3.-

Arias HR, Targowska-Duda KM, García-Colunga J, Ortells MO. Is the antidepressant activity of selective serotonin reuptake inhibitors mediated by nicotinic acetylcholine receptors?. Molecules. 2021 Apr 8;26(8):2149. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8068400/

4.-

Fryer JD, Lukas RJ. Antidepressants noncompetitively inhibit nicotinic acetylcholine receptor function. Journal of neurochemistry. 1999 Mar;72(3):1117-24. https://onlinelibrary.wiley.com/doi/abs/10.1046/j.1471-4159.1999.0721117.x

5.-

García-Colunga J, Targowska-Duda KM, Arias HR. Functional and structural interactions between selective serotonin reuptake inhibitors and nicotinic acetylcholine receptors. Neurotransmitter. 2016;3(1293):10-4800. https://www.semanticscholar.org/paper/Functional-and-structural-interactions-between-and-Garc%C3%ADa-Colunga-Targowska-Duda/26fd9b6ac58dd07503e1af8cb2950b602645a256?p2df

6.-

Muijsers RB, Plosker GL, Noble S. Spotlight on sertraline in the management of major depressive disorder in elderly patients. CNS drugs. 2002 Nov;16:789-94. https://pubmed.ncbi.nlm.nih.gov/12383038/

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