Stablon Articles
Stablon - calmness with fewer side effects
Stablon - Address anxiety and depression without feeling sedated.
Stablon – A well-tolerated, stand-out anti-depressant therapy

Stablon – A well-tolerated, stand-out anti-depressant therapy

Stablon (the brand name for Tianeptine) is one such anti-depressant drug. It forms part of a family of anti-depressants known as tricyclic anti-depressants. Whilst regarded by many as “old fashioned”, tricyclic anti-depressants still hold an important place in the medical armoury used to combat depression. Indeed, Stablon is one of a newer breed of tricyclics having been brought to the market in the late 1980s (older style tricyclics have been around since the 1950s).

And, as we shall see below, Stablon in particular has a number of key advantages over other anti-depressants that make it a drug well worthy of consideration when trying to decide upon the most appropriate drug regime to adopt.

The Medical Treatment of Depression

Over recent years a family of medications known as Selective Serotonin Reuptake Inhibitors (SSRIs) have become the first choice of treatment for many patients suffering from depression. They work on the theory that certain types of depression are due to a chemical imbalance in the brain signified by low levels of the neurotransmitter serotonin (a hormone that is also known by the name 5-hydroxytryptamine).

Neurotransmitters act as the brain’s messenger service. The majority of neurons (as cells of the nervous system are called) in the human brain do not actually touch each other but are separated by minute gaps known as synaptic gaps. In order to communicate with one another, neurons use nerve impulses that are fired along defined pathways. When one neuron wants to communicate with another neuron and pass on a nerve impulse, it does so by releasing specialised chemicals - these chemicals are the neurotransmitters. The neurotransmitters enable a nerve impulse to safely cross over a synaptic gap where it may be accepted at specialized receptor sites on the next neuron.

Once the appropriate receptor site on the next neuron has been activated, the neurotransmitter either promotes an excitatory response (which makes it more likely that the nerve impulse will be passed on again) or an inhibitory response (which makes it less likely that the nerve impulse will be passed on, so blocking further movement of that particular nerve impulse along that particular pathway).

There are a number of different neurotransmitters. They are responsible for different actions and are classed in a number of different ways. Serotonin belongs to a group known as ‘monoamine neurotransmitters’ and is implicated in mood, emotion, sleep and appetite. Researchers have discovered that when someone is clinically depressed, they are deficient in monoamine neurotransmitters - this discovery has given rise to the term ‘the monoamine hypothesis of depression’. By boosting levels of these neurotransmitters, a patient’s symptoms of depression may be relieved and ‘normal function’ restored.

SSRIs such as Prozac work by preventing the re-uptake (re-absorption) of serotonin which allows more serotonin to remain at the synapse thereby boosting serotonin levels and in turn alleviating depressive symptoms. This all seems to make a good deal of sense so why would a medication that works in a directly opposite fashion and actually enhances the re-uptake of serotonin (and thereby reduces serotonin levels) also have an anti- depressive effect?

The answer to this is not yet fully understood but this is what Stablon does. Its actions appear to fly in the face of accepted theories but there can be no denying the results of Stablon therapy - it is an effective anti-depressant and what’s more it does not appear to carry with it some of the more negative side effects of SSRIs (something which we will look at in more detail below).

What do we know about how Stablon works?

There can be little doubt that Stablon acts in a novel way when compared with many other anti-depressants.

Stablon is what is known as a selective serotonin reuptake enhancer (SSRE). This means that instead of blocking serotonin receptors to prevent re-absorption (reuptake) and so allow as much serotonin as possible to be available, Stablon does the exact opposite. Although lacking any significant action upon monoamine transporters (such as serotonin) and upon neurotransmitter receptor sites (unlike drugs such as Prozac), Stablon actively stimulates and accelerates the reuptake of serotonin into serotonergic terminals in the brain’s hippocampus and cortex. The result is that more serotonin is taken out of circulation and serotonin levels are lowered.

How Stablon actually achieves this is unclear. However, it is known to be neuroprotective via multiple neuro-chemical and cellular mechanisms. As with other modern anti-depressants, its therapeutic actions presumably lie within adaptations that occur both between and within neurons, as a result of therapy over a period of several weeks. But the exact molecular mechanisms at work are still obscure.

What are the effects of taking Stablon?

The aim of Stablon is to reduce the body’s brain and hormonal response to stress. If we find ourselves under persistent physical and psychosocial stress, our adrenal glands secrete excessive amounts of the corticosteroid hormone cortisol. Excess cortisol is not good for us and can induce changes in the brain’s hippocampus. If you are genetically susceptible these changes may not just result in lowering of your mood but can cause clinical depression.

Current evidence suggests that one of the ways in which Stablon achieves a reduced response to stress is by preventing, and possibly even reversing, stress-induced neural damage. Sustained use of Stablon appears to ‘normalise’ the hypothalamic-pituitary-adrenal (HPA) axis. The HPA axis is a complex set of direct influences and feedback interactions that exist between the hypothalamus, the pituitary gland and the adrenal glands. They represent a major part of the neuro-endocrine system which is responsible for controlling the body’s reaction to stress and which regulates many body processes, including energy storage and expenditure, the immune system, digestion, sexuality, moods and emotions. By reducing stress- evoked activity of the HPA, the patient is better able to cope in a stressful environment.

Taking Stablon over a period of time may also help to reduce some stress induced programmed cell death (apoptosis).

At a molecular level, Stablon exerts its actions on the glutamate system. Glutamate is the most abundant excitatory neurotransmitter in the human nervous system. It is involved in a number of functions including memory and learning. Stablon appears to prevent the overstimulation of certain types of glutamate receptors in the brain’s hippocampus. It also modulates what are known as NMDA glutamate receptors. These particular receptors play a crucial role in mediating both the functional and intracellular effects of stress.

And it is because it has both antidepressant and anxiolytic (anxiety reducing) properties that Stablon is particularly suitable for the treatment of an entire range of depressive conditions.

How effective is Stablon?

As with all of today's psychoactive medicines, Stablon won’t work for everybody but around two thirds of those who take Stablon will appreciably respond to it. This response level is similar for all drugs commonly prescribed for depression including such well known therapies as Prozac.

The safety and effectiveness of Stablon have been the subject of numerous research studies and clinical trials. For example in 1989 French researchers reported that in a multi-centre, double blind randomized trial, 64% of the 265 adult outpatients with dysthymic disorder associated with clinically manifest anxiety enrolled into the study, demonstrated decreased symptoms after a 6 week treatment period¹. In another study in Brazil 126 depressed patients were treated with Stablon over a 42 day period and again the study confirmed Stablon’s efficacy (and Safety) as a treatment for major depression².

On an anecdotal level, eminent New York psychiatrist Richard Brown MD has reported encouraging results using Stablon with his patients. He has found Stablon to be useful across a whole range of depressive conditions from anxiety to major depression. For many of his patients the lack of side effects such as weight gain and sexual dysfunction makes Stablon a particularly acceptable form of medical treatment.

What are the advantages of Stablon?

Apart from its novel way of actually chemically tackling depression, Stablon stands out from the crowd because it appears to have fewer of the unpleasant side effects that can make treatment with other forms of anti-depressants particularly troubling.

As mentioned above, these days SSRIs tend to be the first line of attack when it comes to prescribing medication for depression. But one of the main side effects of SSRIs and other ‘serotonergic’ anti-depressants is that they can lead to sexual dysfunction. Such difficulties are not only an issue for the patient but can also cause real problems within their relationships with their partners. Stablon does not carry with it the risk of developing such problems. In fact, rather than having a dampening effect on libido and sexual performance, Stablon may even enhance sexual function.

People taking SSRIs on a long term basis may also find that that their medications induce feelings of apathy and emptiness. They may feel that their emotions have in some way been dulled or blunted. Stablon does not give rise to such feelings. Nor does Stablon appear to give rise to inner tension which may be induced by other antidepressants such as bupropion (a noradrenergic/dopaminergic antidepressant). Patients taking Stablon are more likely to be mellow with both irritability and impulsiveness reduced.

The use of SSRIs also carries with it the risk of gaining weight. Again this is not a problem for those using Stablon.

Classed as a tricyclic anti-depressant, one would expect that a major down side to Stablon therapy would be the risk of it having a sedating effect. However, this is not the case because Stablon has no affinity for the histamine receptors. Stablon is therefore a non-drowsy medication. Also unlike classic tricyclic antidepressants, Stablon does not normally impair cognitive function.

Given these impressive advantages, it’s clear that Stablon is a very useful weapon to have in the fight against depression.

Other roles for Stablon

As with many medications, Stablon has been found useful for treating a number of other conditions apart from depression.

With its anxiolytic properties those suffering from panic and anxiety disorders and social phobias may respond particularly well to Stablon. This is probably because Stablon is known to reduce acute stress-induced noradrenaline release in the frontal cortex of the brain. Noradrenaline causes blood pressure to rise, the heart to beat faster, metabolism and blood glucose levels to increase metabolism and energy production and blood flow to the extremities to rise. Stablon may also be effective against posttraumatic stress disorder (PTSD).

Stablon has been reported to be moderately helpful in treating Attention Deficit Hyperactivity Disorder (ADHD) and may offer an alternative to amphetamines and medicines such as Ritalin.

Stablon is also known to be useful in alleviating the signs and symptoms of alcohol withdrawal and for helping people to drink less. Stablon can induce a similar degree of well-being as that brought about by alcohol without the intoxication and hangover effects brought about by drinking. Stablon also tends to reduce aggression.

Away from neurological conditions, Stablon has been shown to be useful for a number health issues:

• Stablon is known to improve the cardio-vascular status of those with ischemic heart disease. There is known to be some sort of association between heart disease and depression although this link is only poorly understood at present
• Stablon is also useful for asthmatics because it is a fast acting bronchodilator
• Stablon can help in the treatment of Irritable Bowel Syndrome (IBS)
• Stablon may be used for treating those with depression and erectile dysfunction. Participants in the Elixir study (which was carried out in 2006 that involved younger men with a mean age of 36) reported that not only had Stablon lowered their levels of anxiety and depression but that it had also improved erectile dysfunction issues. Almost 90% of the participants stated that their ability to have sex had improved

Availability

Stablon was developed by the innovative French drug giant Laboratories Servier and has been marketed since 1988. It is not marketed in US as the patent has expired. To bring Stablon to the US market now would require a whole new range of expensive drug trials to be undertaken. However despite Stablon’s unlicensed status, North Americans (and UK) residents can lawfully order Stablon from overseas if it is for personal use.

Dosage

A typical dosage for Stablon is 12.5 mg, taken two or three times a day.

Side effects

The side effect profile of Stablon is one of the main reasons that it stands out when compared with other anti-depressants. Indeed, it is certainly a contender for being the most well tolerated anti-depressant available.

Having said that, all medications do carry with them the possibility of side effects occurring. In the case of Stablon any side effects are rare and usually mild and temporary in nature. They include:

• Gastric problems such as stomach pains, abdominal pain, flatulence, nausea and vomiting
• Anorexia
• Dryness of the mouth
• Insomnia (if this occurs it usually happens when starting Stablon but quickly subsides), drowsiness and nightmares
• Headaches
• Dizziness and faintness
• Respiratory discomfort

Although not intended to be a complete list, this list is very short when compared with other standard anti-depressants. As discussed above, two of the most distressing side effects for many that arise with SSRIs (weight gain and sexual dysfunction) do not apply to Stablon.

Warnings

Like most anti-depressants, Stablon may interfere with other anti-depressant medications, particularly Monoamine Oxidase (MAO) inhibitors and other serotonin inhibitors (SSRIs) such as Prozac. You should not use MAO inhibitors at the same time as Stablon and as a rule of thumb you should allow an interval of 15 days between MAOI and Stablon treatments. If for any reason you do decide to combine Stablon with other anti-depressants, including MAO inhibitors, you must only do so under the guidance of your doctor.

Any patient who is about to undergo general anaesthetic should inform the anaesthetist and stop treatment 24 to 48 hours before the medical intervention. Should an emergency operation prove to be necessary, this may be carried out without stopping treatment previously but with the correct operative supervision.

As with other antidepressants, when treatment is to be stopped, reduce the dosage gradually over a period of 7 to 14 days.

Stablon should not be used during pregnancy or during breast-feeding.

Children under 15 years of age should not take Stablon.

Reference

1. Guelfi JD, Pichot P, Dreyfus JF. Efficacy of tianeptine in anxious-depressed patients: results of a controlled multicenter trial versus amitriptyline. Neuropsychobiology. 1989;22(1):41-8.
2. Costa e Silva JA, Ruschel SI, Caetano D, Rocha FL, da Silva Lippi JR, Arruda S, Ozun M. Placebo-controlled study of tianeptine in major depressive episodes. Europsychobiology. 1997;35(1):24-9.

Stablon - calmness with fewer side effects

What is Stablon?

Anti-depressant Stablon has attracted the interest of the medical community for two key reasons – it works in a novel way and appears to produce fewer side effects to common anti-depressants.

Stablon increases our body’s uptake, or absorption, of the important neurotransmitter serotonin – which helps to regulate mood. This contrasts with common anti-depressants such as Prozac and Paxil, which instead work to maximise serotonin levels by blocking their uptake.

Research has yet to establish exactly why Stablon produces the same effect whilst acting in the opposite way to common anti-depressants. However, it is known to act without certain side effects. – in particular loss of libido/sexual appetite, drowsiness and weight gain in the majority of cases.

Stablon was developed in France by Laboratoires Servier and is also known as tianeptine.

How does Stablon work?

In medical terms, Stablon is known as a selective serotonin reuptake enhancer (SSRE), in contrast to the likes of Prozac which are selective serotonin reuptake inhibitors (SSRIs).

Whilst common serotonin reuptake inhibitors like Prozac and Paxil try to keep as much existing serotonin as possible in circulation in the body, Stablon does the opposite. It actually works to take serotonin out of circulation by stimulating the uptake of this important neurotransmitter, with the aim of reducing the body’s brain and hormonal response to stress.

How effective is Stablon?

New York psychiatrist Richard Brown MD, one of the most famous psychiatrists in the US, has reported encouraging results using Stablon with his patients. Dr Brown found that it does not cause sexual dysfunction or weight gain, and can help across a range of depressive conditions – from anxiety to serious depression. Citing the last 20 patients he had treated with the drug, he found that 15 had experienced good responses with virtually no side effects.

Dr.Brown highlighted a number cases to illustrate the type of situations where Stablon had been effective. One case involved a 50 year old married woman with a lifelong history of depression and anxiety, which included extreme anxiety triggered by flying and a fear about having cancer.

Dr.Brown noted that, while the patient responded reasonably well to treatment using serotonin inhibitors (SSRIs) including fluoxetine/Prozac and paroxetine, she found side effects of weight gain and loss of sex drive to be intolerable. Her weight gain continued despite dieting and regular exercise, but using Stablon the patient returned to her normal body weight and reported being far happier on this medication.

Another case highlighted by Dr Brown involved a single woman in her 40s with mood instability and dysthymic disorder (a chronic, long term form of depression), coupled with recurrent major depression. Treatment with all available classes of anti-depressants and mood stabilizers had not been effective. Dr Brown reported that the patient had the first good treatment response in her life to Stablon and was consistently much better using this drug.

Dr.Brown commented: “I must congratulate the French on finding an anti-depressant that would help the serotonin system while allowing patients to enjoy both sex and food freely.”

A French overview of clinical trials into tianeptine/Stablon by Wilde, Benfield and others found that 78 per cent of patients were evaluated as ‘responders’ following treatment with Stablon. The study also examined long term trials involving Stablon and elderly people – including the treatment of anxiety and somatic health complaints (conditions such as insomnia and fatigue which are commonly associated with depression). It found that Stablon was effective in the treatment of these conditions, making it suitable across the entire range of depressive illnesses and symptoms. This led the survey to suggest that Stablon could be placed in a middle position in the bipolar (depressive illness) medical classification, between the sedative and stimulant anti-depressants.

Stablon’s wide ranging appeal has also been endorsed by respected US physician Robert Mason. In a review of the new generation of brain drugs and anti-depressants, he concluded that Stablon “is a new and novel serotonin drug – its anti-depressant and anxiolytic [anti-anxiety] properties and its action on somatic complaints makes the drug particularly suitable for the treatment of the entire range of depressive symptomatology [diseases and their symptoms].”

As a further indication of its ability to tackle a range of conditions, Dr Mason noted trials that pointed towards the drug’s effectiveness in the treatment of depressed patients who suffered from anxiety, while Stablon also appeared to aid their sleep.

Research evaluating Stablon against other ‘standard’ anti-depressants, including a study by Loo, Saiz-Ruiz and others comparing it with fluoxetine / Prozac, point towards good levels of effectiveness and safety.

Is Stablon beneficial for anything else?

Research has also shown Stablon’s success in treating depression and erectile dysfunction. The Elixir study, carried out in 2006 and involving younger men with a mean age of 36 taking Stablon for eight weeks, found that more than 72 per cent of the group responded to Stablon treatment.

Respondents reported lower levels of anxiety and depression and improvements in erectional difficulties, with almost 90 per cent of patients stating that it improved their ability to have sex.

What is the dosage for Stablon?

A typical dosage for Stablon is 12.5 mg , taken two or three times a day.

A word of caution

Like most anti-depressants, Stablon could interfere with other anti-depressant medications , particularly Monoamine Oxidase (MAO) inhibitors (including Gerovital-H3) and other serotonin inhibitors (SSRIs) such as Prozac. Therefore, If you intend to combine Stablon with any other anti-depressants, this should only be done under the guidance of a physician.

Does Stablon have any side effects?

It has been reported that the list of side effects for Stablon is very short in comparison to many other standard anti-depressants. Possible side effects include dry mouth, anorexia, nausea, flatulence and gastralgia (stomach ache). In rare cases, where the drug has been taken in the late evening, insomnia and nightmares have been reported. Further rare side effects include feeling dizzy and faint and repertory discomfort.

Stablon - Address anxiety and depression without feeling sedated.

Stablon(chemical name, Tianeptine) was first manufactured in the early 1980s by French researchers Antoine Deslandes and Michael Spedding. Stablon is what is referred to as a selective serotonin re-uptake enhancer (SSRE). It is commonly prescribed as an anti-depressant/anti-anxiety medication, as it improves the availability and uptake of serotonin. It is thought to reverse neuronal damage caused by persistent, uncontrolled stress, and is non-sedating.

While Stablon is believed to have strong anti-depressant properties, fewer side effects have been noted than with the more commonly prescribed anti-depressants. It differs in the way it is metabolized by the body, and as such, there is less likelihood of drug to drug interactions.

Accordingly, it has been suggested that it may be particularly suitable for elderly patients and for those suffering alcohol withdrawal, as these patients tend to be more sensitive to the effects of psychotropic drugs. It is also used for treating major depression and depressed bipolar disorder. Stablon is not known to interfere with the libido and, as is common with other anti-depressant medications, it does not normally impair cognitive function.

Other Benefits

Research now suggests that Stablon is very effective for treating asthma. In 1998, Dr. Fuad Lechin and colleagues from the Central University of Venezuela Institute of Experimental Medicine, published the results of a year long randomized controlled trial involving asthmatic children.

The study confirmed that those children who received Stablon experienced a dramatic decline in clinical rating, and improved lung function. Furthermore, a study undertaken in 2005 illustrated that Stablon was effective in treating men with depression and erectile dysfunction.

More recent research is being undertaken in treating Attention Defecit (Hyperactive) Disorder (ADD/ADHD), and a new clinical trial is underway for treating fibromyalgia.