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 from the good drug guide depressive illness devastates millions of lives. tianeptine (stablon, coaxil, tatinol) is a neuroprotective antidepressant that reverses the neuronal damage and lasting misery caused by chronic, uncontrolled stress . tianeptine acts both as a non-sedating anti-anxiety agent and a non-stimulating mood-brightener . uniquely in clinical medicine, tianeptine acts as a selective serotonin reuptake enhancer . its puzzling efficacy as an antidepressant illustrates how little modern psychiatric medicine really understands about mind, mood and depression. a breakthrough in tianeptine research was announced in july 2014 with the unexpected discovery that tianeptine is a full agonist at the mu and delta opioid receptors with negligible effect at the kappa opioid receptors. selective mu opioid agonists in the brain's "hedonic hotspots" typically induce euphoria. selective kappa agonists typically induce dysphoria. the role of central delta opioid receptors is poorly understood. dual activation of the mu and, less potently, delta opioid receptors may be critical to tianeptine's mood-brightening and anxiolytic effect - a therapeutic action seemingly unaccompanied by the physiological tolerance and dependence that have plagued traditional opioids . all previous research into tianeptine may need to be re-evaluated in this light. neonatal abstinence syndrome following heavy use of tianeptine during pregnancy has been reported . the recently popular sulfate salt ( tianeptine sulphate ) is less readily absorbed and excreted from the body than the sodium salt, allowing one-per-day dosing, smoother plasma concentrations, and minimal risk of abuse. more research is urgently needed. an inverse correlation exists between the suicide rate and dietary intake of the essential amino acid l-tryptophan, the rate-limiting precursor of serotonin synthesis. the widely prescribed selective serotonin reuptake inhibitors [i.e. the ssris fluoxetine (prozac), sertraline (zoloft), fluvoxamine (luvox), paroxetine (paxil) and citalopram (celexa)] block the reuptake of the neurotransmitter serotonin into the presynaptic nerve cells by interfering with the serotonin transporter. they thereby increase the availability of serotonin in the synapse. ssris are marketed primarily as antidepressants. they are prescribed for a host of off-label indications too. in contrast to ssris, tianeptine facilitates the reuptake of serotonin into serotonergic terminals both in the cortex and hippocampus - confounding simplistic "low serotonin" theories of depression. tianeptine lacks any significant activity at monoamine transporters or neurotransmitter receptors. how it actually accelerates serotonin reuptake, both acutely and chronically, is unclear. like other contemporary antidepressants , its therapeutic action presumably depends on downstream adaptations both between and within neurons occurring over a period of several weeks. but again the precise molecular mechanisms are obscure . tianeptine was first synthesised in 1981[?] by french researchers antoine deslandes and michael spedding. it has been developed and marketed since the late 1980s as the antidepressant stablon by secretive, privately-owned servier , the innovative french drug giant. tianeptine is sold in europe, latin america and asia. it is not marketed in north america because its patent has expired. to gain a us product license, a raft of costly new clinical trials would be needed by the fda . unfortunately, american regulators are habitually sceptical of the calibre of european medical science. even after fda approval, tianeptine/stablon could be sold only cheaply due to generic competitors. commercially, this might not seem an insoluble problem: structurally, tianeptine may be considered a modified tricyclic, and patentable analogues of tianeptine do exist, notably hetero[2,1]benzothiazepine derivatives. but if and when any such analogues will be commercialised is uncertain. no evidence exists that they are therapeutically superior to tianeptine. another option might exploit how tianeptine sold as stablon (etc) is a racemate; the l-isomer is more therapeutically active than its molecular sister. the design of single-isomer "chiral" drugs allows corporate patent lawyers to extend the patent life of old medicines. thus tired ssri antidepressant citalopram/ celexa was relaunched in 2002 as expensive new s-citalopram/ lexapro ; and patent-expired modafinil/ provigil will soon be relaunched as expensive new r-modafinil/ nuvigil . this route hasn't been pursued yet with stablon. in fact tianeptine may finally reach the usa branded not as an antidepressant, but in the guise of a treatment of irritable bowel syndrome ( ibs ). for in 2004 vela pharmaceuticals registered a patent for the use of tianeptine to treat ibs. in march 2006 pharmos corporation acquired vela. tianeptine for ibs is now in "late-preclinical development". if and when a medicine gains a us product license, physicians can then prescribe it "off-label" for whatever they see fit, including depression. but this prospect is several years away at best. some indication of tianeptine's potential range of application can be gleaned from its various patents. thus patent us6599896 proposes "...use of tianeptine in the production of medicaments to treat neurodegenerative pathologies...cerebral ischaemia, cerebral traumatism, cerebral aging, alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis, demyelating pathologies, encephalopathies, chronic fatigue syndrome, myalgic encephalomyelitis post-viral fatigue syndrome, the state of fatigue following a bacterial or viral infection, and the dementia syndrome of aids”. a prospective, double-blind, randomised, placebo-controlled trial of tianeptine for fibromyalgia is currently under way in spain. regular tianeptine use may even be good for one's teeth , though it's unlikely to become a staple of orthodox dentistry. despite this cornucopia of possibilities, tianeptine is not well known in anglo-american psychiatry or among the english-speaking lay public. much of the early literature was published only in french. servier's present focus is not on tianeptine but the novel melatonin receptor agonist and serotonin 5-ht2c receptor antagonist agomelatine (valdoxan), ec-licensed from february 2009 as an antidepressant. unlike tianeptine, agomelatine is comprehensively patent-protected. how does tianeptine/stablon work? no one really knows. so the story below will soon be superseded. tianeptine is neuroprotective via multiple neurochemical and cellular mechanisms. when an organism is under stress, or perceives itself under stress, the hypothalamus secretes corticotropin-releasing hormone/factor (crh/crf). crh/crf in turn increases secretion of adrenocorticotrophic hormone (acth) from the anterior pituitary. acth in turn stimulates the release of glucocorticoids from the adrenal cortex. persistent, uncontrolled physical and psychosocial stress causes excess cortisol secretion from the adrenal glands. excess cortisol causes dendritic shrinkage in the hippocampus and a contrasting growth of dendrites in the lateral amygdala . these stress-induced changes tend to lower mood; they can cause clinical depression in the genetically vulnerable. current evidence suggests that tianeptine acts to prevent and even reverse stress-induced neural damage, promoting both neuronal survival and synaptic plasticity . sustained use of tianeptine tends to "normalise" the hypothalamic-pituitary-adrenal ( hpa ) system. tianeptine reduces basal and stress-evoked activity of the hpa, helping its users cope in a stressful environment. treatment with tianeptine inhibits corticosterone-induced gene transcription . stress-induced increases in plasma acth , and corticosterone levels are diminished. so too is basal activity of corticotropin-releasing factor ( crf ) neurons and their sensitivity to stress. prolonged tianeptine use also reduce

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Domain Name: TIANEPTINE.COM
Registry Domain ID: 25779931_DOMAIN_COM-VRSN
Registrar WHOIS Server: whois.godaddy.com
Registrar URL: http://www.godaddy.com
Updated Date: 2017-10-01T17:04:24Z
Creation Date: 2000-04-27T11:55:01Z
Registry Expiry Date: 2027-04-27T11:55:01Z
Registrar: GoDaddy.com, LLC
Registrar IANA ID: 146
Registrar Abuse Contact Email: [email protected]
Registrar Abuse Contact Phone: 480-624-2505
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Name Server: NS3.BLTC.NET
Name Server: NS4.BLTC.NET
DNSSEC: unsigned
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  REGISTRAR GoDaddy.com, LLC

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  SERVER com.whois-servers.net

  ARGS domain =tianeptine.com

  PORT 43

  TYPE domain

DOMAIN

  NAME tianeptine.com

  CHANGED 2017-10-01

  CREATED 2000-04-27

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