Paroxetine mesylate
(Synonyms: BRL-29060A mesylate,FG-7051 mesylate) 目录号 : GC25708Paroxetine Mesylate(BRL-29060A mesylate,FG-7051 mesylate) is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties.
Cas No.:217797-14-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Paroxetine Mesylate(BRL-29060A mesylate,FG-7051 mesylate) is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties.
| Cas No. | 217797-14-3 | SDF | Download SDF |
| 别名 | BRL-29060A mesylate,FG-7051 mesylate | ||
| 分子式 | C19H20FNO3.CH4O3S | 分子量 | 425.47 |
| 溶解度 | DMSO: 85 mg/mL (199.78 mM);Water: 10 mg/mL (23.50 mM); | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3503 mL | 11.7517 mL | 23.5034 mL |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7007 mL |
| 10 mM | 0.235 mL | 1.1752 mL | 2.3503 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Paroxetine mesylate: comparable to paroxetine hydrochloride?
Expert Opin Pharmacother 2010 Feb;11(2):185-93.PMID:20088740DOI:10.1517/14656560903451708.
Importance of the field: Currently available small case reports clearly propose that existing regulatory procedures to approve generic versions only require essential bioequivalence, have limitations and fail to meet stricter scientific and clinical demands. Areas covered in this review: Data indicate that Paroxetine mesylate has some potential differences in bio- and clinical equivalence compared with paroxetine hydrochloride, although it has not been fully and sufficiently investigated in well-designed clinical trials. Data available now regarding safety, tolerability, efficacy and practical issues dealing with debates between generic and brand-name products Paroxetine mesylate and paroxetine hydrochloride are presented in the review. What the reader will gain: Preclinical and clinical data are reviewed, and clinical issues relating to use of generic version versus original product are comprehensively discussed; tips for the clinician in clinical practice are also provided. Take home message: Potential differences in efficacy and safety but also reduction in the use of health care and in pharmacy cost should be considered when choosing the generic version or the original product based on the clear benefit-risk ratio in patients.
Management of Menopausal Symptoms
Obstet Gynecol 2015 Oct;126(4):859-876.PMID:26348174DOI:10.1097/AOG.0000000000001058.
Most menopausal women experience vasomotor symptoms with bothersome symptoms often lasting longer than one decade. Hormone therapy (HT) represents the most effective treatment for these symptoms with oral and transdermal estrogen formulations having comparable efficacy. Findings from the Women's Health Initiative and other recent randomized clinical trials have helped to clarify the benefits and risks of combination estrogen-progestin and estrogen-alone therapy. Absolute risks observed with HT tended to be small, especially in younger women. Neither regimen increased all-cause mortality rates. Given the lower rates of adverse events on HT among women close to menopause onset and at lower baseline risk of cardiovascular disease, risk stratification and personalized risk assessment appear to represent a sound strategy for optimizing the benefit-risk profile and safety of HT. Systemic HT should not be arbitrarily stopped at age 65 years; instead treatment duration should be individualized based on patients' risk profiles and personal preferences. Genitourinary syndrome of menopause represents a common condition that adversely affects the quality of life of many menopausal women. Without treatment, symptoms worsen over time. Low-dose vaginal estrogen represents highly effective treatment for this condition. Because custom-compounded hormones have not been tested for efficacy or safety, U.S. Food and Drug Administration (FDA)-approved HT is preferred. A low-dose formulation of Paroxetine mesylate currently represents the only nonhormonal medication FDA-approved to treat vasomotor symptoms. Gynecologists and other clinicians who remain abreast of data addressing the benefit-risk profile of hormonal and nonhormonal treatments can help menopausal women make sound choices regarding management of menopausal symptoms.
New pharmacological therapies for vasomotor symptom management: focus on bazedoxifene/conjugated estrogens and Paroxetine mesylate
Ann Pharmacother 2014 Oct;48(10):1343-9.PMID:25028744DOI:10.1177/1060028014543099.
Objective: To review 2 recently approved therapies for vasomotor symptoms (VMSs) of menopause. Data sources: PubMed searches (June 2003 to May 2014) were conducted using the keywords paroxetine vasomotor and bazedoxifene vasomotor. References from relevant articles were reviewed for pertinent citations that were not identified in the PubMed search. Study selection and data extraction: Phase 3 clinical trials of recently approved hormonal and nonhormonal therapies for the treatment of VMSs of menopause were selected. Studies that evaluated the use of Paroxetine mesylate or bazedoxifene (BZA)/conjugated estrogens (CEs) for VMSs were included. Data synthesis: Four studies for BZA/CEs were identified. One published report of low-dose Paroxetine mesylate was identified that was a combined analysis of 2 phase 3 studies. Both agents significantly decrease the incidence of hot flushes compared with placebo and are approved for the treatment of moderate to severe VMSs associated with menopause. BZA/CEs is only approved for women with an intact uterus. In all circumstances, the use of BZA/CEs should be limited to the shortest duration possible. Paroxetine mesylate was not studied head-to-head against hormone therapy, but the magnitude of its effect on VMSs is less than expected with hormone therapy. Conclusions: BZA/CEs is an effective hormonal therapy for treating VMSs in women with an intact uterus. Paroxetine mesylate is the first nonhormonal therapy that the FDA has approved for VMSs, making both viable options for the treatment of VMSs of menopause.
A review of paroxetine for the treatment of vasomotor symptoms
J Pharm Pract 2015 Jun;28(3):266-74.PMID:25107421DOI:10.1177/0897190014544785.
Background: Studies in recent years have exposed concerns about the safety of hormone replacement therapy (HRT) in the treatment of vasomotor symptoms (VMS) in menopausal women. Numerous studies have examined the use of antidepressants for relief of VMS. Despite recommendations to deny approval of Paroxetine mesylate (Brisdelle™) for the treatment of VMS, the Food and Drug Administration (FDA) recently granted it approval for this indication. Objective: To evaluate all published literature examining use of paroxetine salts (mesylate and hydrochloride) in the treatment of menopausal VMS. Methods: Both PubMed and International Pharmaceutical Abstracts (IPA) were searched using the keywords hot flashes, vasomotor symptoms, menopause, and paroxetine. In PubMed, MeSH terms were used for paroxetine, menopause, and hot flashes. Searches were limited to humans, English language, and clinical trial design. The references for each study identified in this search process were examined in order to locate any additional relevant articles. Results: Compared with placebo, paroxetine salts offer a modest benefit in the treatment of menopausal VMS reducing the frequency and severity of weekly hot flashes. Conclusion: Paroxetine (mesylate or hydrochloride) is an effective alternative to HRT for the reduction in VMS in menopausal women. Future head-to-head studies with active medications are needed in order to identify the best algorithm of treatment for this condition.
A Clinical Review on Paroxetine and Emerging Therapies for the Treatment of Vasomotor Symptoms
Int J Womens Health 2022 Mar 10;14:353-361.PMID:35300283DOI:10.2147/IJWH.S282396.
Most women experience vasomotor symptoms (VMS) during their menopausal transition. Menopausal hormone therapy (HT) is the most effective treatment for VMS, but some women choose not to use HT or have contraindications to using HT. Non-hormonal treatment options should be offered to these symptomatic menopausal women. Multiple large randomized controlled trials have demonstrated statistically significant reductions in hot flash severity and/or frequency with the use of selective serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine reuptake inhibitors (SNRIs). To date, Paroxetine mesylate remains the only non-hormonal treatment that has been approved by the United States Food and Drug Administration (FDA) for the management of moderate to severe postmenopausal vasomotor symptoms. Lower doses are needed to reduce VMS than those used to treat anxiety or depression, which is beneficial since side effects are typically dose dependent. The recommended dosage is 7.5 mg once daily at bedtime. Dose dependent side effects include nausea, fatigue, and dizziness. Knowing potential medication interactions is critical such as with medications that can lead to serotonin syndrome, concomitant use with monoamine oxidase inhibitors and being aware of p450 drug metabolism is essential for patients taking drugs that utilize the CYP2D6 enzyme for metabolism including tamoxifen. This review discusses in detail the available data supporting the use of paroxetine for the treatment of VMS, including side effects and considerations regarding prescribing. A discussion of other emerging treatments is included as well, including estetrol, oxybutynin and neurokinin 3 (NK3) receptor antagonists.