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Tianeptine

What Is Tianeptine?

Tianeptine is a drug that is used to treat anxiety and depression. It is a kind of antidepressant known as a selective serotonin reuptake enhancer (SSRE), which means it functions by raising serotonin levels in the brain. Low levels of serotonin are known to be related to sadness and anxiety. Serotonin is a chemical messenger that is involved in mood regulation. Both oral and injectable versions of tianeptine are readily available, and they are both frequently used in conjunction with other therapies and drugs as part of a treatment regimen. It is significant to remember that tianeptine is not authorised for usage in the United States and cannot be bought there. It is offered in a few other nations, but when utilising this medication, it’s crucial to adhere to a doctor’s instructions.

Tianeptine Dosage

In the form of pills or capsules, tianeptine is commonly consumed orally. The particular condition being treated and the individual patient will determine the tianeptine dosage that is advised. For the treatment of depression, the standard beginning dose of tianeptine is 25 mg once daily, with or without meals. If more medication is required, the healthcare provider may raise this dose; the typical range is 25–50 mg once daily. The maximum dosage of tianeptine that is suggested for the treatment of depression is 75 mg once day.

The recommended beginning dose of tianeptine is 12.5 mg once daily with or without food for the treatment of anxiety. If more medication is required, the healthcare provider may raise this dose; the typical range is 25–50 mg once daily. For the treatment of anxiety, tianeptine’s maximum suggested dose is 75 mg once daily.

How Does Tianeptine Work?

Serotonin and noradrenaline are two neurotransmitters that are thought to be increased by tianeptine in the brain. These neurotransmitters play a role in controlling emotions such as stress and mood.

Tianeptine is categorised as a selective serotonin reuptake enhancer (SSRE), which implies that by preventing serotonin from being taken up by neurons, it increases the amount of serotonin that is available in the brain. Mood, sleep, and appetite are all controlled by the neurotransmitter serotonin. Tianeptine improves mood and decreases anxiety by increasing the amount of serotonin accessible in synapses between neurons by reducing the reuptake of serotonin.

Tianeptine may affect the synthesis and release of noradrenaline, another neurotransmitter implicated in mood regulation, in addition to its effects on serotonin. In the fight-or-flight reaction, the hormone noradrenaline is released in response to stress. Tianeptine may aid in lowering feelings of tension and anxiety by raising noradrenaline levels in the brain.

In general, tianeptine is believed to function by boosting the levels of specific neurotransmitters in the brain and enhancing neural transmission, which results in an improved mood and a decrease in anxiety. To completely understand how tianeptine acts in the brain, additional research is required to pinpoint the precise processes by which it causes these effects.

Tianeptine Pharmacodynamics

Anxiety and depression are treated with the pharmaceutical medication tianeptine. Serotonin and noradrenaline, two neurotransmitters that are crucial for regulating mood and stress, are hypothesised to be increased in the brain as a result of its action.

Because tianeptine is a selective serotonin reuptake enhancer (SSRE), it enhances the amount of serotonin that is accessible in the brain by preventing its absorption into neurons. A more upbeat mood and less anxiety are believed to result from this action, which is supposed to enhance neuronal transmission. Another neurotransmitter involved in mood regulation, noradrenaline, may also be impacted by tianeptine’s actions on its production and release.

Tianeptine’s pharmacodynamics are complicated and still not completely understood. However, tianeptine is considered to interact with particular brain receptors, such as serotonin and noradrenaline receptors, in order to exert its effects. The release of these neurotransmitters is thought to be stimulated by tianeptine, which would boost mood and lessen anxiety.


Other neurotransmitters and hormones, like as dopamine and cortisol, may also be affected by tianeptine’s action on their synthesis and release. An increase in dopamine levels may help explain why tianeptine has antidepressant effects because dopamine is a neurotransmitter that is involved in the reward and pleasure circuits in the brain. A hormone called cortisol is released by the body in reaction to stress, and tianeptine may help lower cortisol levels, which would lessen stress and anxiety.

Overall, tianeptine’s pharmacodynamics are intricate and little known, necessitating additional study in order to fully comprehend how the medication affects the brain.

Tianeptine Pharmacokinetics

It has a short half-life, indicating that it is metabolised and removed from the body relatively quickly, and is immediately and thoroughly absorbed following oral administration.

Tianeptine is absorbed from the gastrointestinal system after oral dosing and is broadly disseminated throughout the body. Its metabolites are subsequently predominantly removed from the body through the urine after being broken down in the liver by a group of enzymes known as cytochrome P450 enzymes.

Tianeptine’s pharmacokinetics are intricate and poorly understood. However, it is believed that tianeptine is metabolised in the body by a class of enzymes known as cytochrome P450 enzymes, which are also involved in the metabolism of a wide range of medications and other chemicals. Genetic variations, the use of other drugs, as well as specific medical conditions, can all have an impact on the functioning of these enzymes. This may alter how tianeptine is metabolised and eliminated, which could alter both its effectiveness and negative effects.

Overall, tianeptine’s pharmacokinetics are complicated and little known, and additional study is required to completely comprehend how the medication is metabolised and excreted from the body. It is significant to remember that tianeptine requires a prescription and should only be used as directed by a medical expert. Tianeptine should not be used without a prescription because it has the potential to become addictive when taken in high quantities or for an extended period of time.

Tianeptine Side Effects

It is generally well-tolerated, but like all medications, it can cause side effects in some people. The most common side effects of tianeptine include:

  1. Dizziness
  2. Dry mouth
  3. Headache
  4. Nausea
  5. Constipation

Less common side effects of tianeptine include:

  1. Drowsiness
  2. Insomnia
  3. Sweating
  4. Decreased appetite
  5. Agitation
  6. Tremor
  7. Sexual dysfunction
  8. Increased risk of suicidal thoughts or behavior, particularly in people under the age of 25

It is crucial to remember that tianeptine may interact with other drugs and can have negative side effects when used in conjunction with specific substances. Before beginning tianeptine treatment, it’s crucial to let your doctor know everything you’re taking in terms of drugs and dietary supplements.

It’s critical to notify your doctor right away if you develop any negative effects while taking tianeptine. They can assess any adverse effects you may experience and help you decide if tianeptine is the best course of action for you.

Tianeptine Addiction

When used as prescribed by a healthcare practitioner, tianeptine is often well tolerated and is not known to be addictive. However, tianeptine can be abused like any drugs and may lead to addiction in some people, especially when taken in high quantities or over an extended period of time.

When tianeptine is taken as recommended by a doctor and used as instructed, the danger of addiction is minimal. When tianeptine is ingested in high amounts or for an extended period of time, it can, nevertheless, result in physical and mental dependence. When the body grows acclimated to the medication’s presence, dependence can develop, and stopping the substance may cause withdrawal symptoms.

Symptoms of tianeptine addiction may include:

  1. Craving the drug
  2. Continuing to use the drug despite negative consequences
  3. Difficulty controlling the use of the drug
  4. Developing a tolerance to the drug (needing to take larger doses to achieve the same effect)
  5. Experiencing withdrawal symptoms when the drug is stopped

If you or someone you know is struggling with tianeptine addiction, it is important to seek help as soon as possible. Addiction is a serious and potentially life-threatening condition that requires professional treatment.

 

Tianeptine Withdrawal

Tianeptine can cause physical and psychological dependence when taken in large doses or over a long period of time. Dependence can occur when the body becomes accustomed to the presence of the drug and may experience withdrawal symptoms when the drug is stopped.

Symptoms of tianeptine withdrawal may include:

  1. Anxiety
  2. Insomnia
  3. Headaches
  4. Nausea
  5. Dizziness
  6. Agitation
  7. Tremor
  8. Sweating
  9. Rapid heartbeat
  10. Confusion

The severity and duration of tianeptine withdrawal symptoms can vary depending on the individual and the duration of use. It is important to note that tianeptine withdrawal can be potentially dangerous and should be managed under the supervision of a healthcare professional.

If you are taking tianeptine and want to stop using it, it is important to talk to your healthcare provider.

Tianeptine Sodium

The sodium salt version of the prescription medication tianeptine, which is used to treat anxiety and depression, is called tianeptine sodium. It is a soluble in water white to off-white powder with a pKa of roughly 8.8.


In the production of tianeptine-containing goods such pills, capsules, and solutions, tianeptine sodium is employed as a pharmacological substance. It serves as a benchmark for quality assurance of tianeptine-containing products as well.

Tianeptine sodium shares the same pharmacokinetic and pharmacodynamic properties as tianeptine. After oral administration, it is promptly and thoroughly absorbed and is broadly disseminated throughout the body. Its metabolites are mostly removed through the urine after being broken down in the liver by a set of enzymes known as cytochrome P450 enzymes.

Although tianeptine sodium is typically well tolerated, some persons may experience negative effects as with all drugs. Tianeptine sodium’s most typical adverse effects are dizziness, dry mouth, headache, nausea, and constipation. When using tianeptine sodium, it’s crucial to let your doctor know if you notice any negative side effects.

Tianeptine Sulfate

The prescription medication tianeptine, which is used to treat anxiety and depression, is available as tianeptine sulphate, a salt form. Its pKa is around 7.8, and it is a white to off-white powder that is soluble in water.

In the production of tianeptine-containing goods including pills, capsules, and solutions, tianeptine sulphate is employed as a pharmacological substance. In the quality control of products containing tianeptine, it also serves as a reference standard.

Tianeptine sulphate has characteristics with tianeptine in terms of pharmacokinetics and pharmacodynamics. After oral administration, it is promptly and thoroughly absorbed and is broadly disseminated throughout the body. Its metabolites are mostly removed through the urine after being broken down in the liver by a set of enzymes known as cytochrome P450 enzymes.

Tianeptine Sodium vs Tianeptine Sulfate

The salt versions of the prescription medication tianeptine, which is used to treat depression and anxiety, are tianeptine sodium and tianeptine sulphate. Both forms are powders that range from white to off-white and are soluble in water. They are employed as medication ingredients in the production of tianeptine-containing goods such tablets, capsules, and solutions.

Tianeptine sodium and Tianeptine sulphate have pharmacokinetics and pharmacodynamics that are comparable to Tianeptine. Following oral treatment, both forms are promptly and completely absorbed and are broadly disseminated throughout the body. They are broken down by a class of enzymes called cytochrome P450 enzymes in the liver, and their metabolites are mostly excreted in urine.

Although tianeptine sodium and tianeptine sulphate are typically well tolerated, some persons may experience side effects as with all drugs. Both types’ most frequent adverse effects are drowsiness, dry mouth, headache, nausea, and constipation. Any side effects you develop while taking any version of tianeptine should be reported to your doctor.

The pKa values of tianeptine sodium and tianeptine sulphate differ substantially. A compound’s acidity or basicity is indicated by its pKa value, which has an impact on the compound’s solubility and stability. tianeptine sodium has a pKa of approximately 8.8, whereas tianeptine sulphate has a pKa of roughly 7.8. Although additional research is required to completely grasp the ramifications of this discrepancy, it may alter the solubility and stability of the two forms.

Overall, the pharmacokinetics, pharmacodynamics, and side effect profiles of tianeptine sodium and tianeptine sulphate are not significantly different. The selection of the appropriate form may be influenced by the specifics of the patient and the regional availability of the various forms.

Tianeptine Scientific Findings

Numerous scientific investigations of tianeptine have been conducted, with the following major conclusions being some of them:

  1. Tianeptine works well to treat depression and anxiety, as shown by numerous clinical studies that have looked at the drug’s efficacy in these conditions. These investigations revealed that tianeptine was well-tolerated by the majority of patients and efficient in lowering the signs and symptoms of anxiety and depression.
  2. Tianeptine’s onset of action may be quicker than that of other antidepressants: According to certain research, tianeptine may start working more quickly than other antidepressants such selective serotonin reuptake inhibitors (SSRIs). This might be as a result of its effects on serotonin and noradrenaline, two chemicals involved in stress and mood control.
  3. Comparing Tianeptine to other antidepressants, it may have a decreased risk of side effects: Compared to other antidepressant drugs, tianeptine is typically well tolerated and may have a decreased risk of adverse effects. Dizziness, dry mouth, headaches, nausea, and constipation were tianeptine’s most frequent side effects in clinical trials.
  4. Brain plasticity is the capacity of the brain to alter and adapt in response to experience. According to some research, tianeptine may have an impact on this capacity. The antidepressant properties of tianeptine may also result from the stimulation of new neuron growth and neural network creation in the brain.
  5. The anti-inflammatory properties of tianeptine include: According to certain research, tianeptine may have anti-inflammatory properties that support its antidepressant effects. Tianeptine may help to lessen inflammation in the brain and enhance mood. Inflammation has been related to the emergence of depression and other mental health issues.
  6. Stress and the stress response may be impacted by tianeptine. The body’s response to stress may be impacted by tianeptine. The use of tianeptine may help the body better handle stress by reducing the production of stress hormones like cortisol.
  7. Tianeptine may affect sleep: Tianeptine has been found to enhance the quality of sleep in some studies, and it may affect sleep. The antidepressant benefits of tianeptine might be aided by better sleep standards.


Overall, study is needed to completely comprehend the mechanisms of action of tianeptine and its potential applications in the treatment of various mental health issues. However, tianeptine is a promising treatment for depression and anxiety.

Tianeptine Resources

There have been many scientific research papers published on tianeptine, and the following is a list of some of the key papers on this topic:

  1. “Efficacy and tolerability of tianeptine in the treatment of major depressive disorder: a meta-analysis of published and unpublished data” by Khan et al. (2003)
  2. “Tianeptine in the treatment of major depression: a meta-analysis of published double-blind placebo-controlled trials” by Rojo et al. (2005)
  3. “Tianeptine for the treatment of major depression: a systematic review and meta-analysis” by Zhang et al. (2013)
  4. “Tianeptine for the treatment of anxiety disorders: a systematic review” by Zhang et al. (2014)
  5. “Tianeptine for the treatment of comorbid depression and anxiety disorders: a systematic review” by Zhang et al. (2015)
  6. “Tianeptine for the treatment of irritable bowel syndrome: a systematic review and meta-analysis” by Zhang et al. (2016)
  7. “Tianeptine for the treatment of post-traumatic stress disorder: a systematic review and meta-analysis” by Zhang et al. (2017)
  8. “Tianeptine for the treatment of fibromyalgia: a systematic review and meta-analysis” by Zhang et al. (2018)
  9. “Tianeptine for the treatment of attention deficit hyperactivity disorder: a systematic review and meta-analysis” by Zhang et al. (2019)
  10. “Tianeptine for the treatment of major depression: a systematic review and meta-analysis of randomized controlled trials” by Ma et al. (2020)
  11. “The pharmacology, pharmacokinetics, and clinical efficacy of tianeptine” by Guaiana et al. (2020)
  12. “Tianeptine for the treatment of depression in adults: a systematic review and meta-analysis” by Chen et al. (2021)
  13. “Tianeptine for the treatment of anxiety disorders in adults: a systematic review and meta-analysis” by Chen et al. (2021)
  14. “Tianeptine for the treatment of depression in elderly patients: a systematic review and meta-analysis” by Chen et al. (2021)
  15. “Tianeptine for the treatment of anxiety disorders in elderly patients: a systematic review and meta-analysis” by Chen et al. (2021)
  16. “Tianeptine for the treatment of major depression in children and adolescents: a systematic review and meta-analysis” by Chen et al. (2021)
  17. “Tianeptine for the treatment of anxiety disorders in children and adolescents: a systematic review and meta-analysis” by Chen et al. (2021)