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Sertraline & melatonin = bad (?)

Reminisant B

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Joined
Nov 3, 2005
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401
Can anyone help enlight how this would be possible?

Just saw the article, seems a fair few people will be on sertraline whilst also supplementing with melatonin.

Can't understand the mechanism though.

Toxic optic neuropathy after concomitant use of melatonin, zoloft, and a high-protein diet.Lehman NL, Johnson LN.
Neuro-ophthalmology Unit, Mason Eye Institute, University of Missouri-Columbia, USA.

Melatonin is a neuromodulating hormone found in the pineal gland and retina. It is involved in light-dark circadian rhythms and mediates retinal processes in a manner antagonistic to that of dopamine. Zoloft (sertraline) is an antidepressant drug that blocks the reuptake of serotonin at the neural synapse. Serotonin is the natural precursor of melatonin. A 42-year-old woman sought treatment for visual acuity loss, dyschromatopsia, and altered light adaptation. Neuro-ophthalmologic examination was otherwise normal except for evolving bilateral cecocentral scotomas. She had taken Zoloft for 4 years and began a high-protein diet with melatonin supplementation 2 weeks before onset of visual symptoms. Visual acuity and color vision improved within 2 months after melatonin and the high-protein diet were discontinued. Combined use of melatonin, Zoloft, and a high-protein diet may have resulted in melatonin/dopamine imbalance in the retina, manifesting as a toxic optic neuropathy. Physicians and patients should be alerted to this potential drug interaction.

PMID: 10608673 [PubMed - indexed for MEDLINE]
 
melatonin is usually neuroprotective, no...

as what appears to maybe be n=1 this may just be some fluke occurrence


this is basically i guess just an alert to be wary of such a potential but as yet it is not hard science proving such
 
Well, it could just be toxicity from too much melatonin. In as much as I know, melatonin is a so so antioxidant (which could be where the so called neuroprotectant idea comes from), with about 10% of the power of vitamin C. However, at high doses needed to get this effect, it downregulates the melatonin receptors, which could cause problems with sleep and diurnal rhythms.

Most supplements come in 1-10 gram doses. for maximal effeciency you should take about .3g. I have a paper documenting that .3g is the optimal dose as it provides the highest amount of effects, even over long periods of time, and wihtout daytime groggyness. That is because .3g raises one's melatonin levels to the levels one usually sees at night, (~100-150pg/mL), therefore not causing any damage. However, most companies don't make this dose as anything under 1g is patented, so they have to pay the guy who owns that patent if they want to make that dose. However, everything over 1 gram isn't, so that is why super mega doses appear, even though they are terrible for long term use. Sometimes I hate commerce--putting money over human wellbeing.

Furthermore, high amounts of dopamine cause high amounts of norepineprine. Increasing norephenephrine causes increased melatonin production due to the fact that it causes more pineal seritonin to be released from their vescles and can act with the enzymes n-acetyl-transsferase and 5-hydroxyindole-o-methyltransferase. However, those two enzymes are regulated by the SCN in the brain, which is regulated by melatonin. So basically what I was getting at was that higher levels of norepinephrine could possibly be increasing her endogenous melatonin, however that could be counteracted by inhibition due to endogenous melatonin, so who knows. With so much melatonin, those receptors might get downregulated. If she was supplementing with melatonin she was probably getting too much anyway.

Melatonin was originally discovered for it's ability to blanche frogs. It basically makes all pigments stick together. Therefore, the high levels could have caused this sort of effect in her eyes, causing some sort of accumulation of the pigment molecules. I speculate that the cones in our eyes are somewhat related to pigment molecules as they probably have a pigment that react at a certain wavelength of light. By this theory, having an over abundance of melatonin could cause ocular disturbances especially in colors.

However, I don't know if this is right. I am just theorizing based on what I know. So don't take this as truth and cite it. I could be wrong. (especially the last part about eye pigments... as I don't know if that has ever been shown to be the case...)

Sorry if this seems a bit choppy and lopsided and written all corkscrewy. I am very sleep deprived. I really should try to take a nap, but I can't sleep whenever I try to lay down for a short nap, and I don't have time to take a sleeping aid and go to sleep as I have class soon. Maybe in a few days I will have time to rest.
 
well I assume above you meant to write mg (milligrams)

it does not note what amount she was taken

oral bioavailability may vary and may have been affteced and be an issue as normally it is low

again n=1 says very little
 
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