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Tropisetron-Anyone know about this drug or tried it?

Navid

Senior Member
Messages
564
A 5-HT3 receptor antagonist is primarily used to reduce nausea or vomiting during chemotherapy but the drug is finding immune, neurotoxic, pain, skin and other applications.



Tropisetron started as an anti-nausea but is finding many other applications

Pain - Tropisetron reduces receptor activity associated with serotonin’s ability to enhance pain, fear and anxiety. 5-HT3 receptor antagonists both block serotonin’s pain facilitating properties andincrease GABA availability.

Tropisetron Might Work in Fibromyalgia and/or Chronic Fatigue Syndrome Because

of its neuroprotective, immune modulating and its ability to reduce pain and sensory gating issues and enhance cognition.

Tropisetron helped to normalize cardiac autonomic nervous system functioning and reduced ‘pain perception’ in a 2007 study. Forty-five percent of patients in a large 2004 trial reported having ‘good’ to ‘very good’ results in a large 2004 retrospective fibromyalgia study. Fifty percent of FM patients in a small trial reported Tropisetron had a good or very good influence on their pain with serum substance P levels dropping in the responders. Reduced activation of brain regions associated with pain production occurred in another small Tropisetron study. Forty percent of participants reported a greater than 35% reduction of pain in a large 2001 Tropisetron fibromyalgia trial. The number of tender points and sleep and dizziness were also significantly improved.
 

valentinelynx

Senior Member
Messages
1,310
Location
Tucson
Interesting. It seems that there's been a fair bit of research on the use of 5HT3 receptor antagonists for neuropathic pain. Not just tropisetron, but others, such as ondensetron (Zofran). Tropisetron is not available in the U.S. I think it's strange that, despite my training (anesthesiology and board-certified in pain) and my illness, that I've never before heard of this research! As far a fibromyalgia goes, it looks like the research with tropisetron stopped after the early 2000's?

Has anyone had experience with using any of the 5 HT3 antagonists for pain?
 

Navid

Senior Member
Messages
564
Is compazine similar to this class of drugs. It was one of the very few drugs I can tolerate.

The others are klonopin, dampens excitotoxicity; and narcotics help with pain, but I am able to tolerate with no side effects. Of course these last 2 drugs are very dangerous and easy to build a tolerance to, also difficult to stop taking after being on for many years.

Wish I had a deep knowledge of pharmaceuticals and which would be helpful in dealing with the myriad of symptoms in this disease....and also tolerable to my over stimulated system.

Thanks, Lisa
 

valentinelynx

Senior Member
Messages
1,310
Location
Tucson
Is compazine similar to this class of drugs. It was one of the very few drugs I can tolerate.

The others are klonopin, dampens excitotoxicity; and narcotics help with pain, but I am able to tolerate with no side effects. Of course these last 2 drugs are very dangerous and easy to build a tolerance to, also difficult to stop taking after being on for many years.

Wish I had a deep knowledge of pharmaceuticals and which would be helpful in dealing with the myriad of symptoms in this disease....and also tolerable to my over stimulated system.

Thanks, Lisa

Compazine is an anti-psychotic, also used for nausea. It is of a class called phenothiazines, and acts a multitude of receptors, including dopamine (source of anti-psychotic effects), antihistamine, and anticholinergic, all of which are involved in nausea. To my knowledge, it does not act on the 5 HT-3 or any of the other serotonin receptor.

Klonopin (clonazepam) is, of course, a benzodiazepine, used primarily for anxiety (prevention of!) and sometimes for muscle relaxation and neuropathic pain. Benzos have been used for nausea treatment and prevention (usually in the context of chemotherapy), but the mechanism of this action is unclear. They act on the GABA receptors, which are generally inhibitory in the nervous system, meaning they calm things down... Again, benzos don't act at serotonin receptors.

Opioids ("narcotic" is a legal/forensic term used to refer to illegal drugs, but often misused in the medical field to refer to opiates or opioids) are used mainly for pain. They act on opioid receptors.

Note: while some people (those with addictive tendencies) will abuse benzodiazepines and opioids, this does not mean they are dangerous for patients who do not have a genetic tendency to addiction, if you use the medication appropriately. Yes, tolerance does develop, but is not, in itself, harmful. And, yes, if you wish to stop taking these medications after taking them for an extended period of time, particularly if you have developed tolerance, you will need to taper off gradually to avoid withdrawal symptoms. Opioid withdrawal is uncomfortable, but not life-threatening, but benzodiazepine withdrawal can cause seizures and therefore, can be quite dangerous and should be avoided by careful tapering.
 

Navid

Senior Member
Messages
564
Wow Valentinelynx thank you so much for all the incredibly useful info.

Do you have an idea as to why I would be able to tolerate the above mentioned meds. Is it because they are calming down the nervous system or are they processed differently by the body.

Warmly, Lisa
 

Navid

Senior Member
Messages
564
P.S. Perhaps because they don't interact with serotonin receptors. I do have big problems with any drugs that hit those receptors....anti-depressants are terrible for me.