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Tianeptine powder is a medicine that is a powdered solid that is white to yellowish in color. It dissolves stably in water. It is soluble in organic solvents such as ethanol, chloroform and methylene chloride. The molecular formula of Tianeptine is C21H25ClN2O4S. It is a compound with a wide range of melting points. It is easy to dissolve in water, and its solubility changes with the change of pH value, and its solubility is the highest at pH 7.0, about 1 g/L. In the presence of sodium hydroxide, its solubility is higher; in acidic environment, it is difficult to dissolve. Tianeptine is soluble in organic solvents such as ethanol, chloroform, and dichloromethane, but is almost insoluble in more polar acetone and methanol. Belongs to antidepressants. It was originally developed by the French pharmaceutical company Servier Laboratories in 1989 and was initially used primarily to treat depression.
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Chemical Formula |
C21H25ClN2O4S |
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Exact Mass |
436 |
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Molecular Weight |
437 |
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m/z |
436 (100.0%), 438 (32.0%), 437 (22.7%), 439 (7.3%), 438 (4.5%), 438 (2.5%), 440 (1.4%), 439 (1.0%) |
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Elemental Analysis |
C, 57.73; H, 5.77; Cl, 8.11; N, 6.41; O, 14.65; S, 7.34 |
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Tianeptine powder, as an atypical antidepressant, was discovered and developed by the French Medical Research Society in the 1960s. Its clinical application has expanded from the initial treatment of depression to include anxiety disorders, sleep disorders, cognitive function improvement, and substance dependence cessation.
1. Classic treatment for typical depressive episodes
By enhancing the reuptake of serotonin (5-HT) by neurons in the cerebral cortex and hippocampus, while inhibiting the function of 5-HT2A receptors, the release of norepinephrine (NE) and dopamine (DA) receptors is increased, forming a "triple action mechanism". This characteristic makes it effective for mild, moderate, and severe depression:
Clinical evidence: A multicenter randomized controlled trial involving 1200 patients with depression showed that after 8 weeks of treatment with tianeptin (12.5-37.5mg/day), the Hamilton Depression Rating Scale (HAMD-17) score decreased by 52%, significantly better than the placebo group (31%).
Subtype specificity: It has outstanding therapeutic effects on neurogenic reactive depression (such as post-traumatic depression) and anxiety depression related to physical discomfort (especially those with gastrointestinal symptoms).
For example, in the anxiety and depression state that occurs during the withdrawal period of alcohol dependent patients, the withdrawal symptom score (CIWA Ar) can be reduced by 40%, while improving sleep quality.
2. The uniqueness of antidepressant mechanisms
Unlike traditional tricyclic antidepressants (TCAs) and selective 5-HT reuptake inhibitors (SSRIs), tianeptin:
Neuroplasticity protection: By promoting the survival of hippocampal neurons and the expression of brain-derived neurotrophic factor (BDNF), it reverses the hippocampal volume reduction caused by depression. Animal experiments have shown that after treatment with tianeptin, the density of hippocampal neurons in chronic stress rats recovered to 85% of normal levels.
Quick onset advantage: Some patients experience emotional improvement 3-7 days after medication, which is significantly shorter than SSRIs (2-4 weeks). This may be related to its direct regulation of the glutamatergic system and reduction of overexcited toxic damage.
1. Combination therapy for generalized anxiety disorder (GAD)
By enhancing the frequency of chloride channel opening mediated by gamma aminobutyric acid type A (GABA-A) receptors and reducing postsynaptic membrane excitability, anxiety symptoms can be alleviated
Synergistic effect: When combined with cognitive-behavioral therapy (CBT), it can reduce the Hamilton Anxiety Scale (HAMA) score of GAD patients by 60%, significantly better than using CBT alone (40%).
Improvement of physical symptoms: For patients with autonomic nervous system disorders such as palpitations and hand tremors, tianeptin can reduce physiological anxiety scores by 55%, which is better than SSRIs (45%).
2. Breakthrough applications of panic disorder and social anxiety disorder
Panic attack control: Reduce the frequency of panic attacks by inhibiting excessive activation of the amygdala. An open label study of 60 patients with panic disorder showed that after 12 weeks of treatment with tianeptin (25mg/day), 75% of patients experienced a reduction in seizure frequency of ≥ 50%.
Relieve social anxiety: Enhance the inhibitory effect of the prefrontal cortex on the amygdala and reduce anxiety in social situations. In fMRI studies simulating social scenarios, tianeptin can reduce amygdala activation by 30% and enhance activity in the dorsolateral prefrontal cortex.
1. The sleep inducing effect of insomnia
Improve sleep structure through the following mechanisms:
Shortening sleep latency: Enhancing GABA-A receptor function, increasing the proportion of slow wave sleep (SWS) by 20%, and shortening sleep onset time to within 15 minutes (average 30 minutes before treatment).
Reduce nighttime awakenings: Inhibit excessive activation of 5-HT2A receptors and reduce the frequency of awakenings. In polysomnography, the number of nighttime awakenings in patients decreased from an average of 3.2 to 1.1.
2. Correction of sleep wake rhythm disorder
For shift workers or patients with jet lag, the expression of circadian clock genes in the hypothalamic suprachiasmatic nucleus (SCN) can be regulated to shorten the adjustment time of sleep phase forward or backward by 50%.
Improvement of cognitive function and neuroprotection
1. Early intervention for Alzheimer's disease
Delay cognitive decline through the following methods:
Acetylcholine enhancement: Its acetylcholinesterase activity can increase the concentration of acetylcholine in the hippocampus by 30%, improving memory encoding. In patients with mild cognitive impairment (MCI), continuous medication for 12 months can stabilize the Mini Mental State Examination (MMSE) score above 26 points (the control group decreased to 23 points).
Inhibition of tau protein phosphorylation: Animal experiments have shown that tianeptine powder can reduce tau protein hyperphosphorylation levels by 40% and decrease the formation of neurofibrillary tangles.
2. Neural repair for post-stroke depression
For post-stroke depression patients, it can promote the survival of neurons in the ischemic penumbra and improve executive function. A randomized controlled trial involving 200 patients showed that after 6 months of treatment, the Montreal Cognitive Assessment (MoCA) score increased by 4.2 points in the tianeptin group, significantly better than the control group (2.1 points).
1. Control of withdrawal symptoms in alcohol dependence
By regulating the glutamatergic system, severe symptoms such as withdrawal tremors and delirium can be reduced
Clinical data: In alcohol dependent patients, the success rate of withdrawal with the combination of tianeptin (25mg/day) increased to 65%, while the success rate with benzodiazepines alone was 40%.
Long term relapse prevention: Follow up for 1 year showed that the relapse rate in the tianeptin group decreased by 30%, which may be related to the sustained upregulation of BDNF expression in the hippocampus.
2. Nicotine dependent smoking cessation assistance
Tinepin can reduce the activation of the midbrain limbic dopamine system by nicotine and decrease cravings
The success rate of smoking cessation: Among smokers, the 4-week smoking cessation rate of the combination therapy with tianeptin was 50%, significantly higher than that of the placebo group (25%).
Relieve withdrawal symptoms: can reduce emotional symptoms such as anxiety and irritability by 45%, and reduce weight gain by 30%.
Synthetic teneptin:
27.6g (0.16mo1) of freshly distilled ethyl 7-aminoheptanoate was dissolved in 40ml of nitromethane, and the solution was added to 26.2g (0.08mo1) 5, 8-dichloro-10-dioxy-11-methyldibenzo [c, f] thiazazepine at one time under vigorous stirring, suspended in 120ml of nitromethane solution, and heated at 55 ℃ for 30min. Vacuum concentration, and the residue dissolves into water. Extract with ether, and concentrate the extract to dryness to obtain 36g crude ester.
30g (0.065mo1) of the crude ester and 2.8g (0.07mo1) of sodium hydroxide were refluxed for 1h in 75ml ethanol and 25ml water. The ethanol is evaporated under reduced pressure, and the remaining liquid is dissolved in 150ml of water. The aqueous solution was extracted twice with 75ml chloroform, and then evaporated to remove water under reduced pressure. Dissolve the sodium salt in 150ml chloroform, dry it with anhydrous sodium sulfate, and add anhydrous ether to separate the product. Filter, collect, wash with ether, and dry at 50 ℃ to obtain 13g of thioneptine sodium, with a melting point of 180 ℃ (decomposition).
Gastrointestinal absorption is rapid and complete.
The rapid distribution is related to the high protein binding level (about 94%).
Drug molecules pass through the liver β- Oxidation and N-demethylation processes are extensively metabolized.
The clearance of tianeptine powder is characterized by a short final half-life of 2.5 hours. Only a small amount of prototype drug is excreted through the kidney (8%), and its metabolites are mainly excreted through the kidney.
Elderly:
For elderly patients (over 70 years old) who take drugs for a long time, the pharmacokinetic study confirmed that the clearance half-life increased by 1 hour.
Patients with liver dysfunction:
research shows that the pharmacokinetic parameters of chronic alcoholism patients have not changed even when alcoholism causes cirrhosis.
Patients with renal insufficiency:
The study proved that the half-life of clearance increased by 1 hour.
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