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Reboxetine mesylate is a selective and potent norepinephrine reuptake inhibitor. The chemical name is (±)-(2RS)-2-[(RS)-(2-ethoxyphenoxy)phenylmethyl]morpholine methanesulfonate, it exerts antidepressant effects by inhibiting the reuptake of norepinephrine at the presynaptic membrane of neurons, and by increasing the concentration of norepinephrine at synaptic gaps.
It is primarily used for the treatment of depression in adults, including major depression, fluoxetine-refractory depression, and atypical depression. Its clinical application suggests that switching to it may be effective in depressed patients whose fluoxetine is ineffective at adequate doses. It also enhances NE energy to suppress appetite and treat hyperphagia, increases arousal to treat hypersomnia and lassitude, and has a marked improvement in anxiety depression.
It is primarily metabolized by CYP3A4 isoenzymes and therefore may interact with drugs that reduce CYP3A4 activity (e.g., the antifungal agents ketoconazole and fluconazole), potentially increasing their blood levels. In addition, it has synergistic effects with certain drugs (e.g., monoamine oxidase inhibitors, selective 5-hydroxytryptamine reuptake inhibitors, tricyclic antidepressants, etc.), and concomitant use should be avoided.
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| Chemical Formula | C20H27NO6S |
| Molecular Weight | 409.16 |
| Exact Mass | 409.50 |
| m/z | 409.16 (100.0%), 410.16 (21.6%), 411.15 (4.5%), 411.16 (2.2%), 411.16 (1.2%) |
| Elemental Analysis | C, 58.66; H, 6.65; N, 3.42; O, 23.44; S, 7.83 |
| Melting Point | 170-171°C |
| Storage Conditions | Inert atmosphere,2-8°C |
| Solubility | H2O: ~8 mg/mL at ≤60 °C |
| Form | amorphous semi-solid |
| Color | tan or off-white |
Reboxetine mesylate is marketed primarily for the treatment of adult depression, specifically the following types of depression:
Fluoxetine-refractory depression
for adult patients with major depressive disorder who have already tried fluoxetine treatment with poor results, reboxetine may be an effective alternative option. One study showed that patients with depression who switched to reboxetine after fluoxetine was ineffective experienced significant improvement in their depressive symptoms.
Atypical Depression
Atypical depression usually presents with symptoms such as excessive eating and sleeping and sluggishness and paralysis. Reboxetine enhances norepinephrine (NE) function, suppresses appetite, and increases arousal, so it may theoretically be effective in atypical depression.
Anxiety Depression
Reboxetine has also shown positive results in the treatment of anxiety depression. Compared to the placebo group, Reboxetine significantly improved patients' symptoms of agitation, anxiety, and insomnia while having a relatively low incidence of adverse effects.
Overall, it has a wide range of application prospects in the field of depression treatment, but its specific use still needs to be carried out according to the specific conditions of the patient and the doctor's advice.
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The mechanism of action in the treatment of depression is mainly based on its properties as a selective norepinephrine (NA) reuptake inhibitor.
Inhibition of norepinephrine reuptake
It is able to inhibit the reuptake process of norepinephrine at the presynaptic membrane of neurons. This leads to an increase in the concentration of norepinephrine in the synaptic gap, which enhances the role of norepinephrine in neurotransmission.
Enhancement of norepinephrine activity in the CNS
By inhibiting the reuptake of norepinephrine, it is able to enhance the activity of norepinephrine in the CNS. Norepinephrine is an important neurotransmitter that has a significant impact on the regulation of mood, attention, learning and memory.
HImprovement of Mood State
Since norepinephrine plays an important role in mood regulation, it can improve patients' mood state and alleviate depressive symptoms by increasing the activity of norepinephrine.
In addition, it has an important role in the inhibition of neurons in the nucleus accumbens. The nucleus accumbens is an important region in the brain involved in mood regulation, which is closely related to the occurrence of depression, and it can dose-dependently inhibit the firing of neurons in the nucleus accumbens, which may be related to its antidepressant effect.
research history
Reboxetine mesylate, also known as EDRONAX, is a selective norepinephrine reuptake inhibitor. It has been developed as a treatment for major depressive disorder, particularly unipolar depression. Since its introduction, it has demonstrated its efficacy in preventing relapse and recurrence in long-term treatment.
Development background
Depression, as a common mental disorder, has a tendency to increase in incidence year by year. In the treatment of depression, the search for drugs with good efficacy and low side effects has been the focus of research, and as a novel antidepressant drug, has emerged.
01
First marketed
Developed by Pharmacia & Upjohn and first approved for marketing in August 1997 in the UK. Its launch provided a new treatment option for people with depression.
02
Pharmacological effects
Highly selective norepinephrine reuptake inhibitor, which exerts antidepressant effects by inhibiting the reuptake of norepinephrine at the presynaptic membrane of neurons and increasing the concentration of norepinephrine in the synaptic gap.
03
Clinical Studies
Demonstrated excellent efficacy and high tolerability in clinical trials. Studies have shown that it has good therapeutic effects on major depressive disorder, fluoxetine-refractory depression and atypical depression. It also has relatively few side effects and a high safety profile.
04
Follow-up studies
Since it has been on the market, researchers have conducted in-depth studies on its pharmacological effects, mechanism of action, efficacy and safety. These studies provide more basis and support for the clinical application.
05
development prospect
Regarding its future prospects, reboxetine mesylate holds potential due to its specific mechanism of action. With further research and clinical trials, it may expand its application in other mood disorders or even in neurodegenerative diseases. However, its market availability and acceptance will depend on ongoing clinical evaluations and regulatory approvals.
- First, as a norepinephrine reuptake inhibitor, has shown significant efficacy in the treatment of depression. With a deeper understanding of the pathogenesis of depression, this class of drugs is likely to receive more attention and application.
- Second, although there are a variety of antidepressants already on the market, each has its own specific mechanism of action and indications. As a highly selective norepinephrine reuptake inhibitor, may have unique advantages in some specific types of depression or symptoms. For example, it may have better efficacy in major depression, fluoxetine-refractory depression, and atypical depression.
- In addition, as medical technology continues to advance and clinical studies intensify, the dosing regimen, side effect management and drug interactions may be more thoroughly explored and optimized. This will help improve the safety and efficacy of the drug and further expand its application scope.
What are the side effects of this compound?
This compound, also known as reboxetine mesylate, is an antidepressant drug that primarily exerts its antidepressant effects by inhibiting the reuptake of norepinephrine (NE). However, there may be some side effects when using this medication. The following is a detailed summary of its side effects:
1.Common side effects
Neurological response:
- Headache: Medications may dilate blood vessels in the head or cause neurotransmitter imbalances, leading to headaches.
- Dizziness: There may be a feeling of dizziness that affects balance.
- Insomnia: Medications may affect the balance of neurotransmitters in the brain, especially changes in norepinephrine and dopamine levels, leading to difficulty falling asleep, shallow sleep, or early awakening.
Autonomic nervous system response:
- Dry mouth: Drugs inhibit adrenergic receptors, reduce saliva secretion, and cause dry oral mucosa.
- Excessive sweating: Abnormal sweating may occur.
Digestive system reactions:
- Nausea: Medications may stimulate smooth muscle in the gastrointestinal tract or affect the central nervous system, leading to a feeling of nausea.
- Vomiting: Severe nausea may cause vomiting.
- Constipation: Medication inhibits serotonin reuptake, reduces intestinal peristalsis frequency, and leads to difficulty in defecation.
- Loss of appetite: Anorexia or loss of appetite may occur.
Cardiovascular system response:
- Increased heart rate and palpitations: Medications may cause the heart to beat faster, resulting in palpitations.
- Vascular dilation: Medications may cause vascular dilation, leading to related symptoms.
- Orthostatic hypotension: When standing rapidly from a lying or sitting position, there may be a decrease in blood pressure, leading to symptoms such as dizziness and darkening of the eyes.
Urinary system reactions:
- Difficulty urinating: Medications may affect bladder function, leading to difficulty urinating.
- Urinary retention: urine is retained in the bladder and cannot be discharged smoothly.
- Urinary tract infection: Due to poor urination, there may be an increased risk of urinary tract infection.
2.Serious side effects
- Allergic reactions: Symptoms such as redness, swelling, blistering, peeling, itching, and rash may occur with or without fever; In severe cases, there may be difficulty breathing, swallowing, or speaking; Allergic reactions that endanger life, such as swelling of the skin surface, tongue, or throat.
- Hyponatremia: Symptoms such as headache, lack of concentration, memory impairment, confusion, weakness, epilepsy, or changes in balance may occur. Hyponatremia may be caused by drugs affecting the balance of sodium ions in the body.
- Hypertension: Symptoms such as severe headaches, dizziness, fainting, or changes in vision may occur. Hypertension may be caused by medication affecting vascular tone or neurotransmitter balance.
- Psychological symptoms: may include restlessness, anxiety, irritability, aggressive behavior, hallucinations, and other symptoms. These symptoms may be related to the medication affecting the balance of neurotransmitters in the brain.
- Reproductive system response: Male patients may experience symptoms such as testicular swelling and pain, erectile dysfunction, painful or delayed ejaculation.
3.Other precautions
- Drug interactions: This compound may interact with various drugs, such as antifungal agents (fluconazole, ketoconazole), antibiotics (erythromycin), monoamine oxidase inhibitors (moclobemide, phenethylamine), etc. Therefore, it is advisable to avoid using these medications together or consult a doctor when using them.
- Special populations should use with caution: pregnant women, lactating women, patients with liver and kidney dysfunction, those with a history of seizures (such as epilepsy), patients with elevated intraocular pressure (glaucoma), patients with difficulty urinating caused by prostate hyperplasia, patients with low blood pressure (hypotension) or taking antihypertensive drugs, and patients with heart disease should use this drug with caution.
- Overdosing: Overdosing may lead to symptoms such as low blood pressure, anxiety, and high blood pressure. If there is an overdose, please seek medical attention immediately and follow the general treatment principles for drug overdose.
Reboxetine Mesylate (methylsulfate of reboxetine) is a selective norepinephrine reuptake inhibitor (NRI), and is mainly used for the treatment of depression. The following provides an overview of its chemical properties from multiple aspects:
Molecular structure and composition
Molecular formula and molecular weight
The chemical formula of rivotinib mesylate is relatively complex. It is formed by combining the rivotinib base part with mesylic acid. Its molecular weight is relatively large, and the precise molecular weight data is of great significance for the analysis, purification, and pharmacokinetic studies of the drug, as it can affect the absorption, distribution, metabolism, and excretion processes of the drug in the body.
Structural characteristics
The rivotinib base has a specific chiral center and exists in two enantiomers, namely the S-enantiomer and the R-enantiomer. In rivotinib mesylate, it usually exists in a racemic form or a specific enantiomer form. Different enantiomers may have differences in pharmacological activity and pharmacokinetic properties. The mesylate ion bond with the rivotinib base to form a stable salt structure, which helps to improve the solubility and stability of the drug.
Physical properties
Appearance: Rivotinib mesylate is generally a white or off-white crystalline powder. This appearance characteristic is one of the important bases for judging the purity and quality of the drug. Pure drugs usually have a regular crystalline form and uniform color.
Solubility: It has certain solubility in water, which is very important for the preparation of drug formulations. Good water solubility enables the drug to be conveniently prepared into various oral formulations, such as tablets and capsules, ensuring that the drug can dissolve rapidly in the gastrointestinal tract and release the active ingredients, thereby being absorbed by the body. At the same time, it is also soluble in some polar organic solvents, such as methanol and ethanol, and can be used to dissolve drug samples in the analysis and research of the drug, for various chemical and physical property determinations.
Melting point: It has a certain melting point range. The melting point is the temperature at which a substance changes from a solid state to a liquid state and is an important physical constant of the substance. By determining the melting point of rivotinib mesylate, the purity of the drug can be preliminarily judged. The higher the purity, the narrower the melting point range and the closer it is to the theoretical value.
Chemical stability
Stability to light and heat
Rivotinib mesylate is relatively sensitive to light and heat. Under light conditions, the drug molecules may undergo photochemical reactions, resulting in changes in the molecular structure and the formation of some inactive or toxic degradation products. High-temperature environments will also accelerate the decomposition reaction of the drug, reducing the drug content and efficacy. Therefore, during the storage and transportation of the drug, it is necessary to adopt conditions of avoiding light and low temperature, such as storing the drug in brown bottles and placing them in a cool and dry place to extend the shelf life of the drug.
Stability to acids and bases
In different acid-base environments, the stability of rivotinib mesylate also varies. In acidic conditions, the drug may undergo hydrolysis reactions, resulting in the destruction of the molecular structure; while in alkaline conditions, some chemical reactions may occur, affecting the stability of the drug. In the preparation of formulations, appropriate pH conditions need to be selected to ensure the stability of the drug. For example, the pH value of oral formulations is usually controlled within a certain range to avoid excessive influence of the acid-base environment on the drug in the gastrointestinal tract.
Chemical reaction activity
Functional group reactions
The rivotinib mesylate molecule contains some specific functional groups, such as amino groups and ether bonds. These functional groups have certain chemical reaction activity and can participate in some chemical reactions. For example, the amino group can react with some acid anhydrides, acyl chlorides, etc., to form corresponding amide compounds; the ether bond can undergo cleavage reactions under certain conditions. These chemical reaction characteristics have important application values in the structural modification of drugs, the synthesis of analogues, and the study of drug metabolism.
Metabolic reactions
In the human body, rivotinib mesylate undergoes a series of metabolic reactions. It is mainly oxidized by the cytochrome P450 enzyme system in the liver to generate some metabolites. These metabolites may have different pharmacological activities and toxicity. Some of the metabolites may still possess certain antidepressant activity, while others may lose their activity or cause adverse reactions. Studying the metabolic reactions of drugs is of great significance for understanding the mechanism of drug action, optimizing drug treatment plans, and predicting adverse drug reactions.
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