COMT Inhibitors

[PetersKeys]

Do you think COMT inhibitors like Entacapone and Tolcapone have any usage for future antidepressants since they are related to MAO inhibitors in their action?

 

[King Kong]

COMT inhibitors dosen't influence the level of serotonin, on the contrary of MAOI-A.
So i think they will be useless to treat depression
(Bad english, i know...)

 

[PetersKeys]

Dopamine > serotonin for treating depression. In my experience serotonin from SSRIs or MAOIs makes me feel even crappier. Only MDMA seems to do it right.

Seratonin seems more for anxiety and hyperactivity, while dopamine is more for drive and motivation.

COMT doesn't effect seratonin, but effects dopamine, epinephrine, and norephinephrine, which are also chemicals involved greatly in depression.

 

[permastoned]

has anyone tried this? A combo of entacapone and selegiline would go nicely..

 

[Smyth]

The two COMT inhibitors on wikipedia look ugly.

For such a critical enzyme in terminating catecholamine activity in the synapse, its at least somewhat surprsing more drugs targeting this enzyme have not yet been reported.

See for example the long list of drugs known to interact with the MAO enzymes.

 

[permastoned]

^ I think they are a fairly recent development.. or maybe they don't have great therapeutic potential due to the locations/frequency of the COMM enzymes.. (of which I am not aware)?

Same as Dopamine Beta-hydroxylase inhibitors I guess.

Ok, now I want to take a combination of Selegiline, entacapone, nepicastat and methylphenidate.

Woot.

 

[grue]

For whatever reasons, in practice these don't seem all that interesting as one might hope, but I agree that it's largely unexplored territory.

 

[permastoned]

^So you have tried some of them? I believe they would be far better in combination than alone. (The enzyme inhibitors, only the methylphenidate if your head's dopamine receptors are downregulated to the extent that dopaminergic activation in my brain is like throwing a feather at a dart board).

From CHRONIC FATIGUE SYNDROME ASSOCIATION OF LONG ISLAND

NEW DRUG BENEFITS CFIDS!

A newly approved drug for Parkinson's disease is a real help for PWCs, said
Dr. Jay A. Goldstein. If it continues to be as useful as the initial PWCs have
found it, it could very well join his first five or six drugs in his treatment
protocol.

The new class of drug, called catechol-O-methyltransferase inhibitors (COMP),
helps both cognition and energy. You will know after just one 100-mg pill if
this treatment is effective for you. Dr. Goldstein is now prescribing 100 mg
twice daily for those who find benefits from the medication.

Toleopone, with the common name of Tasmar got USA clearance just this past
May. In Europe, a similar drug is available called Comtess. It is not as powerful
as Tasmar, however. In the US, Comtess is called Comtan. Tasmar is a much
more potent inhibitor of COMT and penetrates better into the brain. There do not
seem to be any adverse side effects from this medication. The drug has been
written up favorably in the April 25th, 1998 edition of The Lancet (Vol. 351)
but of course, refers only to Parkinsonian patients. You may want to request
that your physician give you a prescription for just one pill to see if it benefits
your energy and cognition.

"Tasmar is more effective (immediately) when combined with a dopamine
agonist such as Requip (quinpirol) or a reversible inhibitor of monoamine
oxidose (RIMA) such as medlobemide, which due to the wisdom of the FDA, is
available in every industrialized country in the world but the USA! When it
works, it's quite energizing," said Dr. Goldstein.

Pharmacogenetic Clinical Trial of Nepicastat for Post Traumatic Stress Disorder (PTSD)
This study is currently recruiting participants.
Verified by Synosia Therapeutics, Inc., November 2008
First Received: March 18, 2008 Last Updated: November 3, 2008 History of Changes
Sponsors and Collaborators: Synosia Therapeutics, Inc.
Lori Davis, MD Tuscaloosa VA Medical Center
Mark Hamner, MD Ralph H. Johnson VA Medical Center
Information provided by: Synosia Therapeutics, Inc.
ClinicalTrials.gov Identifier: NCT00641511
Purpose

Assess the effect of nepicastat in the treatment of in Post Traumatic Stress Disorder (PTSD) in conflict or combat zone experienced veterans, in comparison to placebo.

Condition Intervention Phase
Post Traumatic Stress Disorder (PTSD)
Drug: SYN117 (nepicastat)
Drug: Placebo comparator
Phase II

Study Type: Interventional
Study Design: Treatment, Randomized, Double Blind (Subject, Caregiver, Investigator, Outcomes Assessor), Placebo Control, Parallel Assignment, Safety/Efficacy Study
Official Title: Pharmacogenetic Clinical Trial of Nepicastat for PTSD