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Posted by sukarno on November 10, 2010, at 7:30:21
In reply to Re: Stablon update » Conundrum, posted by sukarno on November 8, 2010, at 12:43:23
http://www.mdpi.com/1424-8247/3/10/3143/pdf
Pharmaceuticals 2010, 3, 3143-3166; doi:10.3390/ph3103143
pharmaceuticals
ISSN 1424-8247
www.mdpi.com/journal/pharmaceuticals
Review
Beneficial Effects of Tianeptine on Hippocampus-Dependent
Long-Term Memory and Stress-Induced Alterations of Brain
Structure and Function
Phillip R. Zoladz 1, Carmen Muñoz 2 and David M. Diamond 3,4,5,*
1 Department of Psychology & Sociology, Ohio Northern University, Ada, OH 43222 USA
2 Servier International, 35 rue de Verdun, 92284 Suresnes, France
3 Research & Development Service, James A. Haley VA Hospital, Tampa, FL 33612, USA
4 Department of Psychology, Cognitive and Neural Sciences Division, University of South Florida,
Tampa, FL 33612, USA
5 Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, FL
33612, USA
* Author to whom correspondence should be addressed; E-Mail: ddiamond@mail.usf.edu;
Tel.: 813-974-0480; Fax: 813-974-4617.
Received: 19 July 2010; in revised form: 26 August 2010 / Accepted: 31 August 2010 /
Published: 11 October 2010===
Excellent, comprehensive article about tianeptine.
I propose that tianeptine causes headaches in the beginning of treatment because it stimulates adenosine-1 receptors. This would cause vasodilation and is the reason behind the headache caused by acute caffeine withdrawal (caffeine is an adenosine receptor antagonist/blocker).
I feel more activating effects today although the antidepressant effect is slow in expressing itself. I seem to have lost my previous tolerance. It is almost like it is 2005 and I'm trying tianeptine all over again.
I've only been on it a few days, so I think in a few more days I will feel better.
I already sleep better (8 to 10 hours a day) and wake up feeling less dread and far less anxiety. I was surprised I could give up diazepam abruptly without any additional anxiety. I also cut back on my caffeine consumption by 50% so this could account for the stress relief too.
I can breathe a lot better (I'm asthmatic). Tianeptine piles serotonin onto platelets, the opposite action of SSRIs in this mode of action. For some reason this helps asthma because the severity of asthma attacks is correlated with higher levels of free plasma serotonin.
I do feel warm in the forehead and eyelids in the morning...almost like a low grade fever but this disappears within 30 minutes of taking a Stablon tablet. This also happened sporadically when I took Stablon regularly for 5 years. I think it might be that its short half-life results in it wearing off somewhat in the morning and then dopamine takes a nose dive. Low dopamine can raise body temperature and abruptly discontinuing dopamine boosting drugs can result rarely in neuroleptic malignant syndrome or fever.
It could also be because Stablon affects the hypothalamus which regulates body temperature. I feel cooler after taking a Stablon.
Paul
Posted by Conundrum on November 10, 2010, at 11:02:44
In reply to Tianeptine activates A1 adenosine receptors, posted by sukarno on November 10, 2010, at 7:30:21
I have to say I'm losing patience with the drug. The drugs I've responded to best in the past have had some mechanism of increasing norepinephrine, but this drug lowers it. I don't know if its the drug or what, but I feel like I just don't care about anything, not sure if thats more than usual for me.
> http://www.mdpi.com/1424-8247/3/10/3143/pdf
>
> Pharmaceuticals 2010, 3, 3143-3166; doi:10.3390/ph3103143
> pharmaceuticals
> ISSN 1424-8247
> www.mdpi.com/journal/pharmaceuticals
> Review
> Beneficial Effects of Tianeptine on Hippocampus-Dependent
> Long-Term Memory and Stress-Induced Alterations of Brain
> Structure and Function
> Phillip R. Zoladz 1, Carmen Muñoz 2 and David M. Diamond 3,4,5,*
> 1 Department of Psychology & Sociology, Ohio Northern University, Ada, OH 43222 USA
> 2 Servier International, 35 rue de Verdun, 92284 Suresnes, France
> 3 Research & Development Service, James A. Haley VA Hospital, Tampa, FL 33612, USA
> 4 Department of Psychology, Cognitive and Neural Sciences Division, University of South Florida,
> Tampa, FL 33612, USA
> 5 Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, FL
> 33612, USA
> * Author to whom correspondence should be addressed; E-Mail: ddiamond@mail.usf.edu;
> Tel.: 813-974-0480; Fax: 813-974-4617.
> Received: 19 July 2010; in revised form: 26 August 2010 / Accepted: 31 August 2010 /
> Published: 11 October 2010
>
> ===
>
> Excellent, comprehensive article about tianeptine.
>
> I propose that tianeptine causes headaches in the beginning of treatment because it stimulates adenosine-1 receptors. This would cause vasodilation and is the reason behind the headache caused by acute caffeine withdrawal (caffeine is an adenosine receptor antagonist/blocker).
>
> I feel more activating effects today although the antidepressant effect is slow in expressing itself. I seem to have lost my previous tolerance. It is almost like it is 2005 and I'm trying tianeptine all over again.
>
> I've only been on it a few days, so I think in a few more days I will feel better.
>
> I already sleep better (8 to 10 hours a day) and wake up feeling less dread and far less anxiety. I was surprised I could give up diazepam abruptly without any additional anxiety. I also cut back on my caffeine consumption by 50% so this could account for the stress relief too.
>
> I can breathe a lot better (I'm asthmatic). Tianeptine piles serotonin onto platelets, the opposite action of SSRIs in this mode of action. For some reason this helps asthma because the severity of asthma attacks is correlated with higher levels of free plasma serotonin.
>
> I do feel warm in the forehead and eyelids in the morning...almost like a low grade fever but this disappears within 30 minutes of taking a Stablon tablet. This also happened sporadically when I took Stablon regularly for 5 years. I think it might be that its short half-life results in it wearing off somewhat in the morning and then dopamine takes a nose dive. Low dopamine can raise body temperature and abruptly discontinuing dopamine boosting drugs can result rarely in neuroleptic malignant syndrome or fever.
>
> It could also be because Stablon affects the hypothalamus which regulates body temperature. I feel cooler after taking a Stablon.
>
> Paul
>
Posted by sukarno on November 10, 2010, at 11:46:44
In reply to Re: Tianeptine activates A1 adenosine receptors » sukarno, posted by Conundrum on November 10, 2010, at 11:02:44
I hope you'll give it another week or two. I'm feeling adrenaline (although that might not be it..could be dopamine) surging through my body all the time now (activating) as it did after a few days on it. The first few days were more anxiolytic and caused drowsiness, but then it made me feel wired along with an anorectic effect/less appetite. Headaches became more common and sometimes my hands felt like they were trembling slightly. The antidepressant effect took hold after several days of feeling wired/jittery.
Someone on pbabble said it felt a bit like ephedrine.. somewhat anorectic. I thought I also read about some who said it seemed to have a synergistic effect with caffeine.
Everyone is different though. Maybe you can increase the dosage to 4 tablets a day to see if you can bring on the activating effects.
I did notice some apathy - or better described as "comfort even in the face of adversity" - with long term use. The manufacturer claims it is good for adjustment disorders.
I felt a lot less culture shock while on Stablon, but when I quit, all the anxiety and depression came back.
I hope someday we can have a "cure" for severe depression, but perhaps I am being far too optimistic.
Every antidepressant I've tried has pooped out except for nortriptyline, but I was only on it for six months, so I don't know if it would have pooped out if I had continued it for years.
Take care and keep us updated. Perhaps you could take two in the morning to see if it jump-starts your day. ;-)
Paul
Posted by Conundrum on November 10, 2010, at 15:05:44
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by sukarno on November 10, 2010, at 11:46:44
hmm i'd be skeptical if its adrenaline, although anything is possible. From what I have read though, tianeptine decreases cortisol and stress hormones. Maybe 2 in the morning would be better. I found the tiredness isn't as bad as last week but I can't say I notice feeling any more joy doing things or improvements in motivation.
Posted by g_g_g_unit on November 11, 2010, at 4:04:37
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by sukarno on November 10, 2010, at 11:46:44
> I hope you'll give it another week or two. I'm feeling adrenaline (although that might not be it..could be dopamine) surging through my body all the time now (activating) as it did after a few days on it. The first few days were more anxiolytic and caused drowsiness, but then it made me feel wired along with an anorectic effect/less appetite. Headaches became more common and sometimes my hands felt like they were trembling slightly. The antidepressant effect took hold after several days of feeling wired/jittery.
Hmm, I have that feeling of adrenaline coursing through my body (kinda like hypervigilance), and was hoping Stablon might *treat* - rather than induce - it.
Does the activating effect go away?
Posted by sukarno on November 11, 2010, at 11:42:05
In reply to Re: Tianeptine activates A1 adenosine receptors » sukarno, posted by g_g_g_unit on November 11, 2010, at 4:04:37
The last two times I restarted Stablon after a drug holiday I noticed that there were adrenaline-like stimulatory effects in the beginning, but that wore off within two weeks. Maybe it's dopamine because it is supposed to decrease the secretion of stress hormones.
In the long-term I felt relaxed and much less depressed. I wouldn't say it made me more motivated with extended use. Motivation, for me, seems to be a temporary effect that lasts maybe a week.
It's hard to say for sure though too because I'm also on a moderate to high dose of alprazolam. Benzodiazepines can definitely reduce ambition/motivation and induce apathy.
Posted by sigismund on November 11, 2010, at 19:53:13
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by Conundrum on November 10, 2010, at 15:05:44
It's a bit hard to say.
It certainly made me dreamy and calm, and it made me feel wired on other occasions.
Over time the wiredness got worse so I stopped.
But from the first dose I knew it suited me.
I got that thick head thing to begin with too.
Posted by g_g_g_unit on November 12, 2010, at 0:03:14
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by sigismund on November 11, 2010, at 19:53:13
It made me feel nice and euphoric in the morning, but now I just feel like killing my parents.
Posted by sigismund on November 12, 2010, at 0:49:45
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by g_g_g_unit on November 12, 2010, at 0:03:14
>but now I just feel like killing my parents.
Like it's worn off? :)
Posted by sukarno on November 12, 2010, at 7:51:05
In reply to Re: Tianeptine activates A1 adenosine receptors » g_g_g_unit, posted by sigismund on November 12, 2010, at 0:49:45
I quit using caffeine yesterday and was surprised not to have any withdrawal symptoms. Maybe the stimulating effects of tianeptine are suppressing them or maybe it is the action at the adenosine receptor. I can't use my lightbox today because I think I'd feel overstimulated or swing into mild hypomania.
I slept a lot again and had intense dreams just like the last time I was on tianeptine. I had a dream there was a riot and I had nowhere to go. Some guy got burned alive by a petrol bomb / molotov cocktail. It's crap like that that is very disturbing and makes me reconsider Stablon, but I put up with it in the past for 5 years. I guess it's better than being depressed.
I did wake up almost in tears (because the dream shook me up so much, as it was so real).
I do feel an antidepressant effect beginning now. I just feel more in control.. more confident. My self-esteem is up. This is about day 7 or 8, so if the antidepressant effect kicks in completely it should happen in a few days.
I'm only on 1/2 tablet 4x/day due to expense. When I get more money I'll try to increase it later on to the recommended dose of 1 tablet 3x/day.
Posted by g_g_g_unit on November 12, 2010, at 7:55:04
In reply to Re: Tianeptine activates A1 adenosine receptors » g_g_g_unit, posted by sigismund on November 12, 2010, at 0:49:45
> >but now I just feel like killing my parents.
>
> Like it's worn off? :)I donno, I heard it can accentuate the negative?
They're also being jerks, so maybe I shouldn't blame Servier.
Posted by Conundrum on November 12, 2010, at 9:23:00
In reply to Re: Tianeptine activates A1 adenosine receptors » sigismund, posted by g_g_g_unit on November 12, 2010, at 7:55:04
wow are we all taking the same drug? the best it made me feel was like numb like novacaine and the worst groggy.
hypomania, irritibility? this must be a normal person's response to the increase in DA.
> > >but now I just feel like killing my parents.
> >
> > Like it's worn off? :)
>
> I donno, I heard it can accentuate the negative?
>
> They're also being jerks, so maybe I shouldn't blame Servier.
Posted by sigismund on November 12, 2010, at 13:04:32
In reply to Re: Tianeptine activates A1 adenosine receptors » sigismund, posted by g_g_g_unit on November 12, 2010, at 7:55:04
> heard it can accentuate the negative?
It used to hype me up a bit. Later I came to feel this effect as anxiety. Benzos would cover it. But it became intense enough.
Posted by Conundrum on November 12, 2010, at 13:07:17
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by sukarno on November 10, 2010, at 11:46:44
> Everyone is different though. Maybe you can increase the dosage to 4 tablets a day to see if you can bring on the activating effects.Hmm, I did some fuzzy math when buying the stuff, I only have about a week left and I can only enough for 3 a day that week. So if I don't notice anything soon that will be the end of the tianeptine experiment.
Posted by sigismund on November 12, 2010, at 13:10:14
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by Conundrum on November 12, 2010, at 9:23:00
>hypomania, irritibility? this must be a normal person's response to the increase in DA.
Maybe. I'd find myself day dreaming about sex a lot, so I expect that was.
What's the numbness? Like the anhedonia?
The worst groggy? You take mirtazepine, right? That made me so hung over I only took it twice.
Posted by g_g_g_unit on November 12, 2010, at 17:52:10
In reply to Re: Tianeptine activates A1 adenosine receptors, posted by Conundrum on November 12, 2010, at 9:23:00
> wow are we all taking the same drug? the best it >made me feel was like numb like novacaine and the >worst groggy.
Hmm, I get the grogginess, and also feel a little more flat/apathetic (well, after 2 days use anyway), which is a good thing for me.
Posted by sukarno on November 13, 2010, at 15:23:23
In reply to Re: Tianeptine activates A1 adenosine receptors » Conundrum, posted by g_g_g_unit on November 12, 2010, at 17:52:10
Although all prescription drugs in Indonesia require a prescription, many pharmacies sell non-scheduled (non-controlled) drugs without asking for a prescription. They aren't over-the-counter, but you have to ask for it and they just give it to you.
That's the way it is with antibiotics (unfortunately), antidepressants, tramadol, NSAIDs and Stablon, etc.
The problem is the pharmacist said that he's getting more reports of abuse regarding Stablon and they might start asking for prescriptions soon. Then he asked if I had a prescription but I said I've been a regular customer having bought Stablon in the past. Then he said "ahh, okay.".
However, he was a jerk about the Xanax and said it was too high of a dose despite the prescription originating from an expensive private hospital and psychiatrist to boot. When I mentioned that I have panic disorder he then backed down and agreed that the dosage I'm on would be acceptable. I suppose there are a lot of people on Xanax who don't have panic disorder. I suppose the dosage must be a lot less for average states of anxiety.
I hope Stablon doesn't become controlled! I don't think it will be harder to get, but it will mean more hassle such as having to see one (or more) doctors to get enough. Doctors here are ignorant about Stablon dosages. They think you must adhere to the generic Servier statement of "1 tablet three times a day from the start!". If you take 4 a day they say, "That is excessive!".
As far as I know, all antidepressants have large variations in dosage and Stablon in particular has a huge therapeutic range. Perhaps they don't have much knowledge and think that because Stablon is a "tricyclic" that it must somehow be cardiotoxic (it isn't). However, even the classic TCAs have a wide range of doses.
I hope Stablon doesn't follow the path of amineptine (Survector) and become controlled and then finally banned or pulled off the market. :-(
Indonesia is one of most liberal countries with regards to prescription drugs so if it became controlled here, just imagine what the other countries are thinking. I know it is controlled in Singapore and in one middle eastern country. In Russia it is under lock and key in many pharmacies.
Posted by g_g_g_unit on November 13, 2010, at 23:49:15
In reply to tianeptine might become scheduled/controlled, posted by sukarno on November 13, 2010, at 15:23:23
Hmm, it's making me feel worse at the moment - really lethargic and depressed. I just spend the morning/afternoon lying around the house, too tired and apathetic to do anything.
Posted by Conundrum on November 14, 2010, at 8:42:49
In reply to Re: tianeptine, posted by g_g_g_unit on November 13, 2010, at 23:49:15
> Hmm, it's making me feel worse at the moment - really lethargic and depressed. I just spend the morning/afternoon lying around the house, too tired and apathetic to do anything.
Thats what the first we was like for me. It got better thought, and I returned to my baseline depression.
I have about 4 days left of pills. Hopefully it kicks in or I"m done with it.
Posted by g_g_g_unit on November 14, 2010, at 21:49:20
In reply to Re: tianeptine » g_g_g_unit, posted by Conundrum on November 14, 2010, at 8:42:49
>
> Thats what the first we was like for me. It got better thought, and I returned to my baseline depression.
>
> I have about 4 days left of pills. Hopefully it kicks in or I"m done with it.Did it also make you more anxious at first? I'm getting this horrible adrenaline sensation which Sukarno describes.
Posted by Conundrum on November 15, 2010, at 8:15:32
In reply to Re: tianeptine » Conundrum, posted by g_g_g_unit on November 14, 2010, at 21:49:20
No, not at all. I didn't think tianeptine had any effect on adrenaline. I wouldn't be surprised if that goes away with time.
>
> >
> > Thats what the first we was like for me. It got better thought, and I returned to my baseline depression.
> >
> > I have about 4 days left of pills. Hopefully it kicks in or I"m done with it.
>
> Did it also make you more anxious at first? I'm getting this horrible adrenaline sensation which Sukarno describes.
>
>
Posted by hyperfocus on November 15, 2010, at 9:27:00
In reply to tianeptine might become scheduled/controlled, posted by sukarno on November 13, 2010, at 15:23:23
In Russia junkies crush and inject Stablon into their veins. There was a pretty graphic video making the rounds on the net showing the consequences of this - people with various stages of necrosis i.e the flesh was rotting off their limbs. Some people you could see their bones from the holes in their arms. It's no wonder it's controlled there. I really hope that Stablon doesn't go the way of Survector because of this.
Posted by sukarno on November 15, 2010, at 11:26:16
In reply to Re: tianeptine » Conundrum, posted by g_g_g_unit on November 14, 2010, at 21:49:20
>
> >
> > Thats what the first we was like for me. It got better thought, and I returned to my baseline depression.
> >
> > I have about 4 days left of pills. Hopefully it kicks in or I"m done with it.
>
> Did it also make you more anxious at first? I'm getting this horrible adrenaline sensation which Sukarno describes.
>
>The alleged adrenaline sensation finally went away 2 or 3 days ago with me and now I haven't used my lightbox in almost a week, but the majority (75 to 90% if I had to put a number on it) of the depression is gone. Usually if I skip just 1 day of light therapy my depression returns and if I miss 2 days it is horrible.
I feel relaxed now even though I'm in an adverse situation. I really dislike (hate is a better word even though I don't like to use it) Indonesia. I can't wait to go back to the US as I've been trapped here for nearly 10 years. I can imagine how effective Stablon would be if I was in the US again. Heck, I probably wouldn't even need an antidepressant. Light therapy would probably be enough.
I'm still taking 1/2 tablet 4x/day and only needed to take Valium once to counter the adrenaline-like effects.
I hope it works out for you! :-)
Regards,
Paul
Posted by g_g_g_unit on November 15, 2010, at 23:07:49
In reply to Re: tianeptine, posted by sukarno on November 15, 2010, at 11:26:16
Thanks for your response sukarno. A couple of questions, if you don't mind -
a) What does the anti-depressant effect actually feel when it manifests? So far, after 4 days on the drug, I don't feel particularly depressed, but my hopeless mood has been replaced by a kind of serene apathy, similar to that induced by SSRIs (as conundrum has stated). There have been moments where I get a little, mildly euphoric buzz and feel really connected to people/my surroundings, which is great, but I take it that's not what I should be looking for . .?
Unfortunately, it's that stimulating effect which is most beneficial for my motivation and concentration. I see some people taking 4-6 tabs and wonder if I may be underdosing (though obviously it's too early to tell), or if they're just chasing a certain effect?
and b) do you find that the anxiolytic effects build over time? My hypervigilance has completely died down, and like I say I feel really calm and serene, but unfortunately there has been no positive effect on my worrying and OCD-related intrusive thoughts. I'm not sure if you're prone to GAD or anxiety outside of your panic disorder, but do the benefits in that respect take time, as with SSRIs?
thanks :)
Posted by g_g_g_unit on November 16, 2010, at 7:02:03
In reply to Re: tianeptine » sukarno, posted by g_g_g_unit on November 15, 2010, at 23:07:49
To make things even more confusing - when I tried sri drugs in the past year (fluoxetine and clomipramine) they actually improved the strength of my erections (though not sensation) where as on stablon I see no pro-sexual benefits whatsoever.
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