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Tianeptine and other stuff - ALL SHOULD READ

Posted by Michael Bell on September 13, 2004, at 18:30:44

In reply to Re: Social Anxiety help: generic tips » Jasmine, posted by Philidor on September 9, 2004, at 11:00:53

I've been on tianeptine for about a week now, along with extremely low doses of Klonopin (about .25 mg per day, since I'm trying to taper off) and occasional Picamilon.

I'll try to answer both btnd's and Franz's questions, but I have to give you some background and other information first.

First, let me start by saying that my primary problem is SP, and rather severe at that, or at least it was until I started Klonopin. I've never suffered from depression, except for what would probably be considered low-grade dysthimia or anhedonia. For the SP, over the course of about 5-6 years I've tried many, many drugs for the symptoms, including Nardil, Klonopin, Amisulpride, Adrafinil, Parnate, Prozac, Reboxetine, Picamilon, Moclobemide, Deprenyl, Adderall, Codeine (extended release), Percocet, Gotu Kola, SJW, and more that I can't think of off the top of my head.

I've been on a mission to stamp out SP in its entirety, and I've made great progress, so I'm hoping to pass on some tips to those still struggling with debilitating SP.

Now, I'm not a neuropsychologist and don't have a medical degree, but I've read just about every medline, medscape, NIMH, Psychiatry Times and other article on the internet and in the library dealing with Social Phobia and the involvement of the various neurotransmitters. Literally thousands of hours have gone into my research and comparing notes with others of various discussion boards.

To attack SP, we must first understand it. First, a little DISCLAIMER - I know everybody's experience is different, but it seems highly evident to me that for most people with SP, there are three major problems: PHYSICAL SYMPTOMS OF ANXIETY/FEAR, WARPED MENTAL PERCEPTION and REWARD DEFICIENCY.


***ELEMENTS OF SP***

PHYSICAL SYMPTOMS: If SP is truly your primary problem, the physical symptoms generally include include racing heartbeat, excessive sweating, blushing, excessive salivating, irritable bowels, essentially things that are associated with very high levels of anxiety

MENTAL PERCEPTION: This is the "psychological" aspect of SP, and the main issue is feelings that every little thing you do is social situations is being watched and judged. The important thing is that, even though people with SP KNOW that these feelings of anxiety and paranoia are completely illogical, no matter how many times we tell ourselves this the feelings always occur nonetheless.

REWARD DEFICIENCY: This is probably the hardest element of SP to stamp out. Basically, the issue is that social interaction (and related activities) don't activate the reward mechanisms in our brain like they do with "normal people", so that even if you get rid of the anxiety and fear (with Klonopin, for example), you still don't feel a DESIRE to socialize. This is why so many people with SP are desperately seeking a prosocial drug to add to their benzo or ssri, or whatever else it is they are taking.


*** THE NEUROTRANSMITTERS RESPONSIBLE***: (DISCLAIMER - Yes, I know that there are many different sub-receptor types and that you can't just draw overbroad conclusions about these complex systems, but I'm convinced certain general conclusions can be made, as discussed below) -

GABA - Again, like I've said before, I believe an inefficient GABA system to one of the most, if not THE most, important issue in the physical aspect of SP. The research has without a doubt proven that GABA is the primary brain hormone/transmitter responsible for anxiolytic and anti-fear mechanisms. If you want me to post sites that prove this, I'll be happy to do so.

SEROTONIN - I actually believe that with most people with SP, there is actually TOO MUCH serotonin transmission, or that the serotonin receptors are hypersensitive. Yes, serotonin is associated with wellbeing and social dominance, but too much is also associated in a plethora of studies with fear, harm avoidance and anxiety. I think that limiting the amount of serotonin being transmitted across the synapsis is actually beneficial for those with SP

DOPAMINE - As this is the primary transmitter associated with reward, euphoria and extroversion, there is an issue with dopamine as well. From everything I've read, my belief is that dopamine transmission in those with SP has little to do with dopamine levels, but rather poor and inconsistent TRANSMISSION of the transmitter. Moreover, I believe this poor transmission to be an INDIRECT result of problems with the other transmitters.

OPIOIDS - also heavily involved in the reward pathway (especially mu-opioids), there is definitetly an issue with opioid efficiency in the brain of those with SP. This connection will be discussed below when I talk about the most effective meds for SP and WHY those drugs are so effective.

And this brings us to:
***CHOLECYTOSKININ (CCK)***: The more I read about CCK and CCK receptors in the brain, the more I believe this largely ignored peptide to be the missing link that ties all the elements of physical anxiety, learned fear and reward deficiency together. It is the most abundant peptide in the brain, and has been proven numerous times to have the following effects.
- CCK is directly linked with fear conditioning
- CCK agonists consistently elicit panic attacks in anxious and normal persons
- CCK is essentially the anti-opioid, meaning it's effects are to neutralize opioids in the brain and body
- CCK antagonists are extremely anxiolytic and neutralize the effects of anxiety-provoking substances
- CCK levels skyrocket after people and animals experience social defeat
- CCK has a modulatory effect on dopamine and is very important in the reward cascade

***THE MOST EFFECTIVE DRUGS***: From talking to several psychologist, doing countless research, visiting numerous discussion boards and from person experience, it is evident that the most effective drugs for SP are the following (in no particular order): KLONOPIN, NARDIL, ALCOHOL and GHB (Xyrem).

KLONOPIN - Great for the phyical symptom element SP. Part of the benzo family, it locks on to receptors to greatly increase the efficiency and transmission of the GABA system. Should be the first line of defense for anxiety problems (as opposed to SSRIs, which I do NOT think are nearly as effective or get to the root problem). For doctors who SPECIALIZE in anxiety problems, it is the first line of defense. However, prolonged use often causes or exacerbates feelings of dysthimia or anhedonia

NARDIL: The so-called golden standard for SP, it is an anxiolytic agent and anti-depressive all wrapped into one. It is an MAOI that increases the levels of dopamine, serotonin, norepinephrine, and GABA. It is the action on GABA tansanimase that makes this drug so much more effective for SP than other MAOIs that don't effect GABA. It is also great for staving off dysthimia since it is an AD, but is not necessarily pro-social

ALCOHOL - Acute alcohol intake increases GABA transmission and stimulates dopamine release, probably through activation of the mu-opioid receptors. In my experience, it is one of the most prosocial substances out there, but the effects are very short-lived.

GHB - probably the pinnacle of anti-SP substances, it latches onto GHB receptors, stimulates the release of GABA, stimulates the mu-opioid receptors, increases serotonin turnover and initially blocks then releases dopamine.

***POLYPHARMACY***

The common thread between all the above substances (except Klonopin) is that they effect many transmitter systems, but primarily the GABA, mu-opioid and dopamine systems. And therein lies the trick. To really kick SP in the nuts, I think there nees to a combo of meds that do the following: increase GABA, increase OPIOID (or alternatively decrease CCK-B receptor activation), increase DOPAMINE transmission, and DECREASE SEROTOTIN overproduction.

Following that line of thinking, the most effective and side-effect free combo of meds I've ever tried (never tried GHB) is:
1) small dose KLONOPIN
+
2) 2 pills of TIANEPTINE 3x/day
+
3) occasional ADDERALL supplementation

The Klonopin potentiates GABA, the TIANEPTINE is a Serotonin reptake ***enhancer***(meaning it decreases serotonin transmission) and the ADDERALL stimulates the release of dopamine.


This combo is damn good for SP. However, in the quest to always improve, I plain in the near future to try small doses of buprenorphine and/or a CCK antagonist to see just how on point my theories really are.

I hope I haven't bored you to death. Again, I'm not a doctor, I'm just an avid researcher obsessed with nipping this thing in the bud.

Hope this helps anyone who needs it. Thanx.


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Psycho-Babble Medication | Framed

poster:Michael Bell thread:386382
URL: http://www.dr-bob.org/babble/20040909/msgs/390429.html