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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 22 of 22. This is the beginning of the thread.
Posted by jasmineneroli on December 10, 2004, at 18:39:45
I know it's only available in UK/Europe, but has anyone tried Stablon (Tianeptine) with success?
I read that is was good for anxiety/depression. It apparently is unique in that it's a Serotonin reuptake ACCELERATOR and works on 5HT1A only. Therefore, it works on the "calming" receptor, and does not involve 5HT2A/B, the sexual dysfunction related receptors.
I was hoping that it might be an appropriate med for GAD (with some depression).
Anyone know which CytP450 enzyme(s) are needed to metabolize this drug? Or is it metabolised in a way other than hepatically? Therapeutic dosage range??
Thanks
Jas
Posted by Franz on December 11, 2004, at 21:15:50
In reply to Tianeptine-anyone tried/info plse????, posted by jasmineneroli on December 10, 2004, at 18:39:45
Hi jasmineneroli
tianeptine is metabolized by beta oxidation not by the P450
Posted by jasmineneroli on December 11, 2004, at 23:52:17
In reply to metabolism, posted by Franz on December 11, 2004, at 21:15:50
Hi FranzL
Thanks for your response. I had found that P450 not involved in tianeptine metabolism, but not the site your noted. More good info there.
Makes me really want to try it.
Would love to know of others who have.
Jas
Posted by jasmineneroli on December 11, 2004, at 23:54:04
In reply to Tianeptine-anyone tried/info plse????, posted by jasmineneroli on December 10, 2004, at 18:39:45
Posted by sabre on December 12, 2004, at 0:27:57
In reply to STABLON/TIANEPTINE EXPERIENCES PLSE!!!!! (nm), posted by jasmineneroli on December 11, 2004, at 23:54:04
Hi Jas
Yes, I'd like to know about this drug too.I emailed Servier a few months ago to find out about its availability in Australia.
The project manager said there were no plans for it to be registered here. Pity.
I think anyone who has a very strong and negative effect from SSRIs would be curious about trying Tianeptine.sabre
Posted by Pluto on December 12, 2004, at 23:15:05
In reply to Re: STABLON/TIANEPTINE EXPERIENCES PLSE!!!!!, posted by sabre on December 12, 2004, at 0:27:57
Stablon is nothing but alcohol in a pill if you take two 12.5mg tablets together. It produces severe akathisia in some patients.
I tried it once in hope, it may be an effective substitute to SSRIs without sexual side efects. But it did nothing to me. Sex was also bad on this medicine.
It is an intoxicating, and is a controlled substance in many countries including Singapore.
However it is available online if you have a prescription. Manufacturer claims are a lot, but I don't think it is cost effective. But every individual is different.
May be I am one among those who don't like and respond to Stablon.
PLS
Posted by Franz on December 12, 2004, at 23:15:35
In reply to Re: STABLON/TIANEPTINE EXPERIENCES PLSE!!!!!, posted by sabre on December 12, 2004, at 0:27:57
> Hi Jas
> Yes, I'd like to know about this drug too.
>
> I emailed Servier a few months ago to find out about its availability in Australia.
> The project manager said there were no plans for it to be registered here. Pity.
> I think anyone who has a very strong and negative effect from SSRIs would be curious about trying Tianeptine.
>
> sabre
>Hi sabre,
Where you wrote?. I used the form at servier.com with no response.
Thanks
Posted by sabre on December 13, 2004, at 1:09:30
In reply to servier » sabre, posted by Franz on December 12, 2004, at 23:15:35
Franz, this was about 5 weeks ago.
I don't think I went through the form on the Servier site.
I contacted the Servier Labs in Australia
It has a new web site under construction:
http://www.servier.com.au/The Associate Project Manager replied and the email was marissa.lim@au.netgrs.com
In any case, I don't think it is coming here in a hurry.
I also enquired about Duloxetine through Boehringer and they said it wasn't available in Australia and said they would provide a list of international pharmacies if I had a script for it.
sabre
Posted by ed_uk on December 13, 2004, at 8:31:12
In reply to Re: servier, posted by sabre on December 13, 2004, at 1:09:30
Some info about tianeptine...
.......In Singapore the National Pharmaceutical Administration in the Ministry of
Health has restricted the use of tianeptine sodium to psychiatrists due to its abuse potential.....
[Misuse of tianeptine: five cases of abuse][Article in French]
Leterme L, Singlan YS, Auclair V, Le Boisselier R, Frimas V.
Service du Controle Medical, CPAM de Quimper, Cite du Guerlach, BP 1723, 29107 Quimper Cedex.
Five cases of excessive consumption of tianeptine suggest possible drug-abuse of this substance. This side effect is unknown in animals and humans. According to DSM IV, CIM 10 criteria and the French public health code, these five patients had pathological profiles of psychoactive drug abusers. Tianeptine dosage was always used higher than recommended and the drug was taken in association with other psychotropes. Withdrawal was difficult and induced anxiety and other disorders which led to relapse in most of the patients.
[Does addiction to antidepressants exist? About a case of one addiction to tianeptine][Article in French]
Guillem E, Lepine JP.
Espace Murger, Centre de Soins Specialise aux Toxicomanes, Service de Psychiatrie, Hopital Fernand-Widal (AP-HP), 200, rue du faubourg Saint-Denis, 75010 Paris.
We report on a tianeptine dependence lasting for eighteen months in a 42 year old patient. The patient had a previous history of addiction to opiates, amineptine, cocaine and alcohol. He also had a family history of addiction to alcohol and opiates. Tianeptine was prescribed for a major depressive disorder. The patient alleged a "flash sensation" like with heroin since the very first doses with a physical and psychological well-being sensation, better psychomotor performances and transient mood elation. His addiction to tianeptine was immediate and heavy. The positive reinforcement faded away after one month and a total dependance took over, with physical and psychological withdrawal symptoms when doses were not renewed. After two months of treatment, the daily consumption of tianeptine was of 90 tablets. The patient was hospitalised to treat both the addiction to tianeptine and the ongoing major depressive disorder. He was taking 240 tablets daily. In the literature, reports of addictions to antidepressants are scarce and most of them involve agents with amphetamine-like properties, including amineptine and tranylcypromine. Other reports involving other antidepressant agents, including amitriptyline, fluoxetine and tianeptine remain exceptional. Addictions to antidepressants almost exclusively concern patients with a diagnosis of personality disorder and a previous history of drug or alcohol abuse and who are treated for a depressive disorder. Tianeptine, which is devoid of any psychostimulating effect in human, does not seem to have addictive properties apart from the reports of scarce cases.
Encephale. 1999 Nov-Dec;25(6):672-3. Related Articles, Links
[Abuse of tianeptine. A case report][Article in French]
Vandel P, Regina W, Bonin B, Sechter D, Bizouard P.
Service de Psychiatrie et Psychologie Medicale, CHU Saint-Jacques, Besancon.
The authors report a case of tianeptine abuse in a 30 year-old woman. After a medical prescription of the recommended dosage of 12.5 mg 3 times daily of oral tianeptine for a depressive illness, the patient spontaneously increased the dosage which after two months reached 150 tablets per day. No severe toxic effects were observed. As adverse effects, the patient, in the beginning of this high treatment period suffered from nausea, vomiting, abdominal pain, anorexia with weight loss, constipation. These side effects progressively disappeared. The biological tolerance was excellent, and hepatic parameters were not affected. The patient experienced and seek a psychostimulant effect. After seven months of such a therapy, she was hospitalized to undergo a withdrawal. The discontinuation of the tianeptine treatment occurs in four days. A withdrawal syndrome marked by myalgia, and cold feeling was transient, and alleviated by sedative phenothiazine (cyamemazine) and myorelaxant benzodiazepine (tetrazepam).
Pharmacol Biochem Behav. 1999 Jun;63(2):285-90. Related Articles, Links
Although chemically related to amineptine, the antidepressant tianeptine is not a dopamine uptake inhibitor.Vaugeois JM, Corera AT, Deslandes A, Costentin J.
Unite de Neuropsychopharmacologie Experimentale, UPRES-A 6036 CNRS, IFRMP, UFR de Medecine et Pharmacie de Rouen, Saint Etienne du Rouvray, France.
We investigated whether the antidepressant tianeptine shares the dopamine uptake inhibitory properties of the chemically related antidepressant amineptine. Tianeptine dose dependently (5, 10, 20, 40 mg/kg IP) increased locomotor activity in mice. This stimulant effect (20 mg/kg IP) was dose dependently prevented not only by the D1 dopamine receptor antagonist SCH 23390 (7.5. 15, 30 microg/kg SC), but also by the D2 dopamine receptor antagonist haloperidol (50, 100, 200 microg/kg IP), in contrast to that elicited by dopamine uptake inhibitors. Where the latter prevent dexamphetamine-induced (3 mg/kg SC) reversion of akinesia in mice pretreated with reserpine (4 mg/kg SC, 5 h before test), tianeptine (20 mg/kg IP, 30 min before test) did not. Tested up to a concentration of 10-4 M, tianeptine did neither inhibit the [3H]dopamine uptake into mouse striatal synaptosomes nor compete in vitro with the specific binding of [3H]WIN 35,428 at dopamine transporters from striatal membranes. Finally, in mice injected IV with a tracer dose of [3H]WIN 35,428 (1 microCi), the highest tested dose of tianeptine (40 mg/kg IP) did not reduce the specific binding of the radioligand to striatal dopamine transporters. It is concluded that the antidepressant effect of tianeptine does not depend upon a blockade of the neuronal dopamine transporter.
Ed.
Posted by jakeman on December 13, 2004, at 20:39:16
In reply to Re: Abuse potential of tianeptine, posted by ed_uk on December 13, 2004, at 8:31:12
> Some info about tianeptine...
>
> .......In Singapore the National Pharmaceutical Administration in the Ministry of
> Health has restricted the use of tianeptine sodium to psychiatrists due to its abuse potential.....>He was taking 240 tablets daily.
I took 2 tablets a day for about a month with no effect whatsoever. Apparently 240 a day does have an effect...
Posted by Iansf on December 14, 2004, at 16:20:57
In reply to Re: Abuse potential of tianeptine, posted by ed_uk on December 13, 2004, at 8:31:12
> His addiction to tianeptine was immediate and heavy... After two months of treatment, the daily consumption of tianeptine was of 90 tablets. The patient was hospitalised to treat both the addiction to tianeptine and the ongoing major depressive disorder. He was taking 240 tablets daily. >
240 TABLETS A DAY? Whoa! Where did the poor guy find room for food in his stomach?
Posted by Michael Bell on December 14, 2004, at 21:18:38
In reply to Tianeptine-anyone tried/info plse????, posted by jasmineneroli on December 10, 2004, at 18:39:45
I don't have depression, but for anxiety Tianeptine was SOMEWHAT helpful. However, I wouldn't recommend it as monotherapy. SOmetimes it seems to work, other times its like a sugar pill. On the bright side, it had absolutely no negative side effects that I am aware of.
Posted by jasmineneroli on December 14, 2004, at 21:55:40
In reply to Re: Abuse potential of tianeptine, posted by Iansf on December 14, 2004, at 16:20:57
> > His addiction to tianeptine was immediate and heavy... After two months of treatment, the daily consumption of tianeptine was of 90 tablets. The patient was hospitalised to treat both the addiction to tianeptine and the ongoing major depressive disorder. He was taking 240 tablets daily. >
>
> 240 TABLETS A DAY? Whoa! Where did the poor guy find room for food in his stomach?*LOL, not to mention money to buy them all!!! I think we're talking about a few rare indiviuals here.
Jas
Posted by jasmineneroli on December 14, 2004, at 22:07:27
In reply to Re: Abuse potential of tianeptine, posted by Iansf on December 14, 2004, at 16:20:57
that was an interesting series of responses!
I think the abuse potential is directly linked to the type of person involved.
I have GAD....and am notorious (as most anxiety-types are) for being leery of all meds/supps. Only want to try small amounts and titrate slowly, and obsessively observe myself for side effects!!!! My Pdoc would probably laugh at the idea that I would knowingly abuse a drug :). I've refused many of his drug suggestions, based on the bad withdrawal symptoms I've read here! So I feel safe trying it, myself.Seems that it might be worth trying for anxiety, perhaps alongside the tryptophan I'm already taking, or with Klonopin. I'd have to get my Pdoc to order it from the UK for me. Especially since the side-effect profile is so clean.
Thanks again for your input.
I'll update here if I end up taking it.
Regards,
Jas
Posted by Franz on December 15, 2004, at 15:25:17
In reply to Tianeptine - thanks all......................., posted by jasmineneroli on December 14, 2004, at 22:07:27
Hello,
All the articles I read show very mild side effects (if any) and discontinuation problems for tianeptine.
Some caught my attention, but I do not have the knowledge to completely understand the clinical significance.
e.g.
Tianeptine, a new tricyclic antidepressant metabolized by beta-oxidation of its heptanoic side chain, inhibits the mitochondrial oxidation of medium and short chain fatty acids in mice.
Fromenty B, Freneaux E, Labbe G, Deschamps D, Larrey D, Letteron P, Pessayre D.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&list_uids=2597170&dopt=Citation
I do not know if this inhibition take splace in humans at therapeutic doses and if this is too bad or what.
Anyone can help?.
Thanks
p.s. if someone was taking 240 tablets daily and survived, that is good!
Posted by ed_uk on December 16, 2004, at 6:10:22
In reply to more on metabolism, side effects (chemist?), posted by Franz on December 15, 2004, at 15:25:17
Hi Jas,
Tianeptine isn't used in the UK.
Ed.
Posted by jasmineneroli on December 17, 2004, at 0:18:28
In reply to Re: To Jasmineneroli, posted by ed_uk on December 16, 2004, at 6:10:22
O, I thought it was available in the whole of Europe. I will have to get it from France, I guess, if I decide to try it. Do you know why it's not available in the UK?
Thanks.
Jas
Posted by ed_uk on December 17, 2004, at 4:06:41
In reply to Re: To Jasmineneroli » ed_uk, posted by jasmineneroli on December 17, 2004, at 0:18:28
Hi,
I don't know whether the manufacturer ever applied for a license for tianeptine in the UK.
Tianepine seems to be available as...
'Coaxil' in Poland, Slovakia, Hungary, Latvia and Lithuania.
'Stablon' in France, Turkey, Austria, Argentina, Brazil, India, Malaysia, Portugal, Singapore and Thailand.
PS. This information may be out of date!!!
Ed.
Posted by Franz on December 19, 2004, at 17:41:06
In reply to Re: To Jasmineneroli, posted by ed_uk on December 17, 2004, at 4:06:41
Hi, is there any problem to take some melatonin with tianeptine?. I read SSRI drugs and melatonin elevate the level of melatonin.
Anyone know better?
Thanks
Posted by jasmineneroli on December 20, 2004, at 21:03:59
In reply to tianeptine -Stablon- and melatonin, posted by Franz on December 19, 2004, at 17:41:06
Tianeptine ACCELERATES the uptake of serotonin, rather than inhibits its re-uptake, like the SSRI's. So I'm not sure if that mechanism means that the serotonin would then be rapidly further metabolized to melatonin. Thus resulting in more melatonin. I'd be concerned about adding melatonin, without more info from the manufacturer, Servier, in France.
I've heard, however, that small doses of melatonin (1 - 1.5mg) can be used to good effect with most regular SSRI'S.
Ed-UK or Larry Hoover may know more.
Jas
Posted by Franz on December 23, 2004, at 22:11:54
In reply to Re: tianeptine -Stablon- and melatonin » Franz, posted by jasmineneroli on December 20, 2004, at 21:03:59
> Tianeptine ACCELERATES the uptake of serotonin, rather than inhibits its re-uptake, like the SSRI's. So I'm not sure if that mechanism means that the serotonin would then be rapidly further metabolized to melatonin. Thus resulting in more melatonin. I'd be concerned about adding melatonin, without more info from the manufacturer, Servier, in France.
> I've heard, however, that small doses of melatonin (1 - 1.5mg) can be used to good effect with most regular SSRI'S.
> Ed-UK or Larry Hoover may know more.
> Jas
Thanks Jas, yes it is difficult to know. I think I will try 1.5mg or less.I hope Ed-UK or Larry Hoover can read and reply.
Posted by Larry Hoover on December 24, 2004, at 8:53:12
In reply to Re: tianeptine and melatonin Ed-UK or Larry Hoove » jasmineneroli, posted by Franz on December 23, 2004, at 22:11:54
> > Tianeptine ACCELERATES the uptake of serotonin, rather than inhibits its re-uptake, like the SSRI's. So I'm not sure if that mechanism means that the serotonin would then be rapidly further metabolized to melatonin. Thus resulting in more melatonin. I'd be concerned about adding melatonin, without more info from the manufacturer, Servier, in France.
> > I've heard, however, that small doses of melatonin (1 - 1.5mg) can be used to good effect with most regular SSRI'S.
> > Ed-UK or Larry Hoover may know more.
> > Jas
>
>
> Thanks Jas, yes it is difficult to know. I think I will try 1.5mg or less.
>
> I hope Ed-UK or Larry Hoover can read and reply.I'll give you my take on it, but I don't know if there's a flaw in my reasoning or not.
When a neurotransmitter is pumped back into the neuron that released it into the synapse, it is taken into a storage vescicle for re-use. In other words, it doesn't move off to a different part of the brain. It is an efficiency process, one which recycles the neurotransmitter, rather than permitting it to be destroyed by enzymes like MAO or COMT.
The melatonin produced in e.g. the pineal gland is almost certainly produced in situ, in that gland, taking tryptophan past serotonin and on to melatonin. In that synthesis, serotonin is not a product but is instead an intermediate.
By supplying melatonin, you may take some pressure off the mutual demand for tryptophan. You may also prevent the adverse sequelae coming from antidepressant-induced insomnia.
I can't think of a mechanistic reason not to consider the combination, but that doesn't mean that there isn't one.
Starting at a low dose of melatonin still makes sense, as adverse effects of combinations usually are dose-responsive. I'd start at 0.5 mg melatonin, and work up from that. Some people only need such a small dose of melatonin, anyway, and taking too much actually inhibits sleep, via saturation of the receptors.
Lar
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