雷沙吉兰Rasagiline杂质汇总列表
甲磺酸雷沙吉兰片说明书
核准日期：2017年6月16日修订日期：2018年11月01日；2020年06月29日；2021年07月17日；2021年11月03日；2022年03月01日；2022年03月18日甲磺酸雷沙吉兰片说明书请仔细阅读说明书并在医师指导下使用【药品名称】通用名称：甲磺酸雷沙吉兰片商品名称：安齐来®（Azilect®）英文名称：Rasagiline Mesylate Tablets汉语拼音：Jiahuangsuan Leishajilan Pian【成份】化学名称：(R)-N-2-丙炔基-1-茚胺甲磺酸盐化学结构式：分子式：(C12H13N)·CH4SO3分子量：267.34辅料：甘露醇、玉米淀粉、预胶化玉米淀粉、无水胶态二氧化硅、硬脂酸、滑石粉【性状】本品为白色或类白色片。
【适应症】本品适用于原发性帕金森病患者的单药治疗，以及伴有剂末波动患者的联合治疗（与左旋多巴合用）。
【规格】1mg(以雷沙吉兰计)【用法用量】口服给药。
无论是否与左旋多巴合用，用量均为1mg每日一次。
服用本品不受进食影响。
老年人：无需调整剂量。
儿童：由于本品用于儿童和青少年的安全性和有效性尚未建立，本品不推荐用于儿童和青少年。
肝功能损害患者：本品禁用于重度肝功能损害患者（参见【禁忌】）。
雷沙吉兰应避免用于中度肝功能损害患者。
轻度肝功能损害患者开始服用本品时应谨慎。
如果患者的肝功能损害由轻度进展为中度时，应停止服用雷沙吉兰（参见【注意事项】）。
肾功能损害患者：无需调整剂量。
【不良反应】安全性特征概述在帕金森病患者的临床研究中，最常报告的不良反应为：单药治疗中出现的头痛、抑郁、眩晕和流感（流行性感冒和鼻炎）；左旋多巴联合治疗中出现的异动症、直立性低血压、跌倒、腹痛、恶心呕吐和口干；两种疗法中出现的肌肉骨骼疼痛、背部和颈部疼痛以及关节痛。
这些不良反应与药物停药率升高无关。
不良反应列表不良反应采用如下惯例按照系统器官和发生频率分类，如下表1和2中所示：很常见（≥1/10）、常见（≥1/100，<1/10）、少见（≥1/1000，<1/100），罕见（≥1/10000，<1/1000）、极罕见（<1/10000），未知（无法根据现有数据估算）。
雷沙吉兰相关杂质
相关杂质整理列表中文名英文名CAS号规格纯度结构式雷沙吉兰杂质1（（S）-甲磺酸雷沙吉兰）RasagilineImpurity 1（(S)-Rasagiline Mesylate）202464-88-810mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质2 RasagilineImpurity 21179031-47-010mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质3 RasagilineImpurity 3N/A 10mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质4 RasagilineImpurity 41175018-73-110mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质5 RasagilineImpurity 510277-74-4 10mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质6 RasagilineImpurity 6N/A 10mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质7 RasagilineImpurity 7N/A 10mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质8 RasagilineImpurity 8N/A 10mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质9 RasagilineImpurity 91312077-04-510mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质10RasagilineImpurity 101175018-74-210mg-25mg-50mg-100mg ≥99%雷沙吉兰杂质11RasagilineImpurity 111312077-05-6（freebase）10mg-25mg-50mg-100mg ≥99%湖北扬信医药科技有限公司经营上万种杂质对照品（优势供应硫酸羟氯喹杂质、硝苯地平杂质、沙丁胺醇杂质、达格列净杂质、厄贝沙坦杂质、阿莫西林克拉维酸钾杂质、利伐沙班杂质、阿托伐他汀钙杂质、西格列汀杂质、利格列汀杂质等），并代理销售中检所、STD、LGC、TLC、EP、USP、TRC等多个品牌产品，提供上万种标准品对照品，真诚为您服务。
雷沙吉兰溶解度
雷沙吉兰溶解度一、简介雷沙吉兰（Rasagiline）是一种单胺氧化酶A抑制剂，被广泛用于治疗帕金森病和路易体痴呆等疾病。
了解雷沙吉兰的溶解度对于药物制剂的开发、生产和质量控制具有重要意义。
本篇文档将全面介绍雷沙吉兰的溶解度特性。
二、溶解度影响因素影响雷沙吉兰溶解度的因素主要有温度、pH值、溶剂类型和固体粒径等。
温度升高通常会提高溶解度，但也可能导致药物稳定性下降；在不同pH值条件下，雷沙吉兰的溶解度会有所不同；不同类型的溶剂对溶解度也有显著影响；固体粒径越小，比表面积越大，溶解度通常越高。
三、溶解度数据以下是雷沙吉兰在不同条件下的溶解度数据：1.温度：在常温下，雷沙吉兰在水中的溶解度约为1.5mg/mL；在pH值为7.4的磷酸盐缓冲液中，溶解度约为2.0mg/mL；在pH值为1.2的盐酸溶液中，溶解度约为1.0mg/mL。
随着温度的升高，溶解度也会相应提高。
2.pH值：在pH值为 1.2的盐酸溶液中，雷沙吉兰的溶解度最低，为1.0mg/mL；在pH值为7.4的磷酸盐缓冲液中，溶解度为2.0mg/mL；在pH值为9.0的碳酸盐缓冲液中，溶解度最高，可达到约3.5mg/mL。
3.溶剂类型：在不同溶剂中，雷沙吉兰的溶解度有很大差异。
例如，在纯水中，溶解度约为1.5mg/mL；而在乙醇、甲醇或丙酮等有机溶剂中，溶解度会显著提高。
4.固体粒径：雷沙吉兰的固体粒径对其溶解度也有影响。
减小固体粒径可以使比表面积增大，从而提高溶解度。
然而，过小的粒径可能导致药物在溶液中的稳定性下降。
四、结论通过对雷沙吉兰溶解度的研究，可以发现温度、pH值、溶剂类型和固体粒径等因素对溶解度具有显著影响。
在实际应用中，应充分考虑这些因素以优化药物制剂的开发和制备过程。
同时，了解溶解度数据对于药物剂量的确定和给药方案的制定也具有重要意义。
通过对雷沙吉兰溶解度的深入研究，有助于提高药物制剂的质量和治疗效果。
阿塞那平杂质汇总
项目报批 纯度高于98%
阿塞那平杂质7 Asenapine Impurity 7 128949-51-9
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项目报批 纯度高于98%
Asenapine Impurity 8
阿塞那平杂质8
（Asenapine-N-
N/A
Glucuronide (Mixture
阿塞那平杂质列表集
中文名称
英文名称
CAS
阿塞那平杂质1 Asenapine Impurity 1 129385-59-7
规格
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用途
项目报批 纯度高于98%
结构式
阿塞那平杂质3 Asenapine Impurity 3 128915-56-0
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红霉素杂质，克拉霉素杂质，林可霉素杂质，罗红霉素杂质，克林霉素杂质，恩曲他滨杂质，艾地那非杂质，瑞卢戈利杂质，艾氟康唑
杂质等；并提供COA、NMR、HPLC、MS等结构确证图谱;详情请点用户名，谢谢！
企 鹅 号：
专业<杂质对照品>解决方案，代理中检所/EP/BP/USP/LGC/TRC/DR/TLC/MC/SIGMA/BACHEM/STD等品牌。
of Diastereomers)）
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项目报批 纯度高于98%
阿塞那平杂质9 Asenapine Impurity 9 912356-09-3
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项目报批 纯度高于98%
扬信医药代理各品种杂质对照品:舒更葡糖钠杂质，达托霉素杂质，依维莫司杂质，他克莫司杂质，阿奇霉素杂质，克拉维酸钾杂质，
雷沙吉兰合成研究进展
雷沙吉兰合成研究进展作者：郑欣钟日英蔡彦来源：《中国医药导报》2012年第19期[摘要] 雷沙吉兰（Rasagiline）为不可逆选择性单胺氧化酶-B（MAO-B）抑制剂，可增强多巴胺的传递信号，有效缓解帕金森症的诸如静止性震颤、肌肉僵直等症状。
本文通过系统地查阅国内外近年来雷沙吉兰合成的相关文献，旨在为科研工作者全面而系统地了解雷沙吉兰的合成路线、进一步深入研究提供参考。
[关键词] 雷沙吉兰；帕金森症；合成研究[中图分类号] R971.5 [文献标识码] A [文章编号] 1673-7210（2012）07（a）-0013-03Research progress on synthesis of RasagilineZHENG Xin ZHONG Riying CAI YanXiashan Maternal and Child Health Hospital in Zhanjiang City, Guangdong Province, Zhanjiang 524013, China[Abstract] Rasagiline is a irreversible selectivity antagonist of monoamine oxidase-B(MAO-B), it can enhance the transmission of dopamine which can mitigate the symptom of Parkinson's disease such as static tremor and stiffen muscle. In this paper, research literatures on rasagiline synthesis at home and abroad are collated. Its purpose is to make scientific research workers systemly understanding synthesis route of rasagiline and provide the reference for its further research.[Key words] Rasagiline; Parkinson's disease; Synthesis甲磺酸雷沙吉兰（Rasagiline mesylate，Agilect），商品名为：Azilect，化学名为：R-（+）-N-炔丙基-1-氨基茚甲磺酸盐，化学结构见图1中结构式Ⅰ。
雷沙吉兰fda
_________________ __________________ ______________ _____________ ___________________ _______________________________________________________________________________________________________________________________________ HIGHLIGHTS OF PRESCRIBING INFORMATION These highlights do not include all the information needed to use AZILECT ®safely and effectively. See full prescribing information for AZILECT. AZILECT (rasagiline mesylate) Tablets for Oral Use Initial U.S. Approval: 2006 RECENT MAJOR CHANGES • Indications and Usage (1) 05/2014 • Dosage and Administration (2.1) 05/2014 • Warnings and Precautions (5.2, 5.3, 5.6, 5.8, 5.9) 05/2014 INDICATIONS AND USAGEAZILECT, a monoamine oxidase (MAO)-B inhibitor (MAOI), is indicated for the treatment of Parkinson’s disease (1) _______________DOSAGE AND ADMINISTRATION • Monotherapy: AZILECT 1 mg once daily (2.1) • As adjunct without levodopa: AZILECT 1 mg once daily (2.1) • As adjunct to levodopa: AZILECT 0.5 mg once daily. Increase dose to 1 mg daily as needed for sufficient clinical response (2.1) • Patients taking ciprofloxacin or other CYP1A2 inhibitors: AZILECT 0.5 mg once daily (2.2, 5.4) • Patients with mild hepatic impairment: AZILECT 0.5 mg once daily. AZILECT should not be used in patients with moderate or severe hepatic impairment (2.3, 5.5) DOSAGE FORMS AND STRENGTHS • AZILECT 0.5 mg tablets (containing, as the active ingredient, rasagiline mesylate equivalent to 0.5 mg of rasagiline base) (3) • AZILECT 1 mg tablets (containing, as the active ingredient, rasagiline mesylate equivalent to 1 mg of rasagiline base) (3) CONTRAINDICATIONS Concomitant use of meperidine, tramadol, methadone, propoxyphene dextromethorphan, St. John’s wort, cyclobenzaprine, or another (selective or non-selective) MAO inhibitor (4) _______________ WARNINGS AND PRECAUTIONS _______________ • May cause hypertension (including severe hypertensive syndromes) at recommended doses (5.1) • May cause serotonin syndrome when used with antidepressants (5.2) • May cause falling asleep during activities of daily living, daytime drowsiness, and somnolence (5.3) • May cause hypotension, especially orthostatic (5.6) • May cause or exacerbate dyskinesia. Decreasing the levodopa dose may lessen or eliminate this side effect (5.7) • May cause hallucinations and psychotic-like behavior (5.8) • May cause impulse control/compulsive behaviors (5.9) • May cause withdrawal-emergent hyperpyrexia and confusion (5.10) • Increased risk of melanoma: monitor patients for melanoma on a regular basis (5.11) ___________________ ADVERSE REACTIONS ___________________ Most common adverse reactions (incidence 3% or greater than placebo): • AZILECT monotherapy: flu syndrome, arthralgia, depression, dyspepsia (6.1) • AZILECT used as adjunct without levodopa: peripheral edema, fall, arthralgia, cough, and insomnia (6.1) • AZILECT used as adjunct to levodopa: dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, abnormal dreams, fall, and tenosynovitis (6.1) To report SUSPECTED ADVERSE REACTIONS, contact TEVA at 1800-221-4026 or FDA at 1-800-FDA-1088 or /medwatch . ___________________ DRUG INTERACTIONS ____________________ • Meperidine: Risk of serotonin syndrome (4, 7.1) • Dextromethorphan: Risk of psychosis or bizarre behavior (4, 7.2) • MAO inhibitors: Risk of non-selective MAO inhibition and hypertensive crisis (4, 7.3) USE IN SPECIFIC POPULATIONS • Pregnancy: Based on animal data, may cause fetal harm. Do not use AZILECT unless the potential benefit justifies the potential risk to the fetus (8.1) See 17 for PATIENT COUNSELING INFORMATION Revised: 05/2014 FULL PRESCRIBING INFORMATION: CONTENTS* 1. INDICATIONS AND USAGE 2. DOSAGE AND ADMINISTRATION 2.1 General Dosing Recommendations 2.2 Patients Taking Ciprofloxacin or Other CYP1A2 Inhibitors 2.3 Patients with Hepatic Impairment 3. DOSAGE FORMS AND STRENGTHS 4. CONTRAINDICATIONS 5. WARNINGS AND PRECAUTIONS 5.1 Hypertension 5.2 Serotonin Syndrome 5.3 Falling Asleep During Activities of Daily Living and Somnolence 5.4 Ciprofloxacin or Other CYP1A2 Inhibitors 5.5 Hepatic Impairment 5.6 Hypotension / Orthostatic Hypotension 5.7 Dyskinesia 5.8 Hallucinations / Psychotic-Like Behavior 5.9 Impulse Control / Compulsive Behaviors 5.10 Withdrawal-Emergent Hyperpyrexia and Confusion 5.11 Melanoma 6. ADVERSE REACTIONS 6.1 Clinical Trials Experience7. DRUG INTERACTIONS 7.1 Meperidine 7.2 Dextromethorphan 7.3 MAO Inhibitors 7.4 Sympathomimetic Medications 7.5 Antidepressants 7.6 Ciprofloxacin or Other CYP1A2 Inhibitors 7.7 Tyramine/Rasagiline Interaction 7.8 Dopaminergic Antagonists 8. USE IN SPECIFIC POPULATIONS 8.1. Pregnancy 8.3. Nursing Mothers 8.4. Pediatric Use 8.5. Geriatric Use 8.6 Hepatic Impairment 8.7 Renal Impairment 9. DRUG ABUSE AND DEPENDENCE 9.1. Controlled Substance 9.2. Abuse 9.3. Dependence 10. OVERDOSAGE 11. DESCRIPTION 12. CLINICAL PHARMACOLOGY 12.1. Mechanism of Action 12.2. Pharmacodynamics 12.3. Pharmacokinetics 13. NONCLINICAL TOXICOLOGY 13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility 14. CLINICAL STUDIES 14.1 Monotherapy Use of AZILECT 14.2 Adjunct Use of AZILECT 16. HOW SUPPLIED/STORAGE AND HANDLING 17. PATIENT COUNSELING INFORMATION *Sections or subsections omitted from the full prescribing information are not listed.FULL PRESCRIBING INFORMATIONAZILECT® (rasagiline tablets)1. INDICATIONS AND USAGEAZILECT (rasagiline tablets) is indicated for the treatment of Parkinson’s disease (PD).2. DOSAGE AND ADMINISTRATION2.1 General Dosing RecommendationsWhen AZILECT is prescribed as monotherapy or as adjunct therapy in patients not taking levodopa, patients may start AZILECT at the recommended dose of 1 mg administered orally once daily.In patients taking levodopa, with or without other PD drugs (e.g., dopamine agonist, amantadine, anticholinergics), the recommended initial dose of AZILECT is 0.5 mg once daily. If the patient tolerates the daily 0.5 mg dose, but a sufficient clinical response is not achieved, the dose may be increased to 1 mg once daily. When AZILECT is used in combination with levodopa, a reduction of the levodopa dose may be considered, based upon individual response.The recommended doses of AZILECT should not be exceeded because of risk of hypertension [see Warnings and Precautions (5.1)].2.2 Patients Taking Ciprofloxacin or Other CYP1A2 InhibitorsPatients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should not exceed a dose of AZILECT 0.5 mg once daily [see Warnings and Precautions (5.4), Drug Interactions (7.6), and Clinical Pharmacology (12.3)].2.3 Patients with Hepatic ImpairmentPatients with mild hepatic impairment should not exceed a dose of AZILECT 0.5 mg once daily. AZILECT should not be used in patients with moderate or severe hepatic impairment [see Warnings and Precautions (5.5), Use in Specific Populations (8.6), and Clinical Pharmacology (12.3)].3. DOSAGE FORMS AND STRENGTHSAZILECT 0.5 mg Tablets: White to off-white, round, flat, beveled tablets, debossed with “GIL 0.5” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 0.5 mg of rasagiline base.AZILECT 1 mg Tablets: White to off-white, round, flat, beveled tablets, debossed with “GIL 1” on one side and plain on the other side containing, as the active ingredient, rasagiline mesylate equivalent to 1 mg of rasagiline base.4. CONTRAINDICATIONSAZILECT is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors, because of risk of serotonin syndrome [See Warnings and Precautions (5.2)]. At least 14 days should elapse between discontinuation of AZILECT and initiation of treatment with these medications. AZILECT is contraindicated for use with St. John’s wort and with cyclobenzaprine.AZILECT is contraindicated for use with dextromethorphan because of risk of episode of psychosis or bizarre behavior.5. WARNINGS AND PRECAUTIONS5.1 HypertensionExacerbation of hypertension may occur during treatment with AZILECT. Medication adjustment may be necessary if elevation of blood pressure is sustained. Monitor patients for new onset hypertension or hypertension that is not adequately controlled after starting AZILECT.In Study 3, AZILECT (1 mg/day) given in conjunction with levodopa, produced an increased incidence of significant blood pressure elevation (systolic > 180 or diastolic > 100 mm Hg) of 4% compared to 3% for placebo [see Adverse Reactions (6.1)].When used as an adjunct to levodopa (Studies 3 and 4), the risk for developing post-treatment high blood pressure (e.g., systolic > 180 or diastolic >100 mm Hg) combined with a significant increase from baseline (e.g., systolic > 30 or diastolic > 20 mm Hg) was higher for AZILECT (2%) compared to placebo (1%).Dietary tyramine restriction is not required during treatment with recommended doses of AZILECT. However, certain foods that may contain very high amounts (i.e., more than 150 mg) of tyramine that could potentially cause severe hypertension because of tyramine interaction (including various clinical syndromes referred to as hypertensive urgency, crisis, or emergency) in patients taking AZILECT, even at the recommended doses, due to increased sensitivity to tyramine. Patients should be advised to avoid foods containing a very large amount of tyramine while taking recommended doses of AZILECT because of the potential for large increases in blood pressure including clinical syndromes referred to as hypertensive urgency, crisis, or emergency. AZILECT is a selective inhibitor of MAO-B at the recommended doses of 0.5 or 1 mg daily. Selectivity for inhibiting MAO-B diminishes in a dose-related manner as the dose is progressively increased above the recommended daily doses.5.2 Serotonin SyndromeSerotonin syndrome has been reported with concomitant use of an antidepressant (e.g., selective serotonin reuptake inhibitors-SSRIs, serotonin-norepinephrine reuptake inhibitors-SNRIs, tricyclic antidepressants, tetracyclic antidepressants, triazolopyridine antidepressants) and a nonselective MAOI (e.g., phenelzine, tranylcypromine) or selective MAO-B inhibitors, such as selegiline (Eldepryl) and rasagiline (AZILECT). Serotonin syndrome has also been reported withconcomitant use of AZILECT with meperidine, tramadol, methadone, or propoxyphene. AZILECT is contraindicated for use with meperidine, tramadol, methadone, propoxyphene and MAO inhibitors (MAOIs), including other selective MAO-B inhibitors [see Contraindications (4) and Drug Interactions (7.1, 7.2, 7.3)].In the postmarketing period, potentially life-threatening serotonin syndrome has been reported in patients treated with antidepressants concomitantly with AZILECT. Concomitant use of AZILECT with one of many classes of antidepressants (e.g., SSRIs, SNRIs, triazolopyridine, tricyclic or tetracyclic antidepressants) is not recommended [see Drug Interactions (7.5)].The symptoms of serotonin syndrome have included behavioral and cognitive/mental status changes (e.g., confusion, hypomania, hallucinations, agitation, delirium, headache, and coma), autonomic effects (e.g., syncope, shivering, sweating, high fever/hyperthermia, hypertension, tachycardia, nausea, diarrhea), and somatic effects (e.g., muscular rigidity, myoclonus, muscle twitching, hyperreflexia manifested by clonus, and tremor). Serotonin syndrome can result in death.AZILECT clinical trials did not allow concomitant use of fluoxetine or fluvoxamine with AZILECT, and the potential drug interaction between AZILECT and antidepressants has not been studied systematically. Although a small number of AZILECT-treated patients were concomitantly exposed to antidepressants (tricyclics n=115; SSRIs n=141), the exposure, both in dose and number of subjects, was not adequate to rule out the possibility of an untoward reaction from combining these agents. At least 14 days should elapse between discontinuation of AZILECT and initiation of treatment with a SSRI, SNRI, tricyclic, tetracyclic, or triazolopyridine antidepressant. Because of the long half-lives of certain antidepressants (e.g., fluoxetine and its active metabolite), at least five weeks (perhaps longer, especially if fluoxetine has been prescribed chronically and/or at higher doses) should elapse between discontinuation of fluoxetine and initiation of AZILECT [see Drug Interactions (7.5)].5.3 Falling Asleep During Activities of Daily Living and SomnolenceIt has been reported that falling asleep while engaged in activities of daily living always occurs in a setting of preexisting somnolence, although patients may not give such a history. For this reason, prescribers should monitor patients for drowsiness or sleepiness, because some of the events occur well after initiation of treatment with dopaminergic medication. Prescribers should also be aware that patients may not acknowledge drowsiness or sleepiness until directly questioned about drowsiness or sleepiness during specific activities.Cases of patients treated with AZILECT and other dopaminergic medications have reported falling asleep while engaged in activities of daily living including the operation of motor vehicles, which sometimes resulted in accidents. Although many of these patients reported somnolence while on AZILECT with other dopaminergic medications, some perceived that they had no warning signs, such as excessive drowsiness, and believed that they were alert immediately prior to the event. Some of these events have been reported more than 1-year after initiation of treatment.In Study 3, somnolence was a common occurrence in patients receiving AZILECT and was more frequent in patients with Parkinson’s disease receiving AZILECT than in respective patients receiving placebo (6% AZILECT compared to 4% Placebo) [see Adverse Reactions (6.1].Before initiating treatment with AZILECT, patients should be advised of the potential to develop drowsiness and specifically asked about factors that may increase the risk with AZILECT such as concomitant sedating medications, the presence of sleep disorders, and concomitant medications that increase rasagiline plasma levels (e.g., ciprofloxacin) [see Drug Interactions (7.6)]. If a patient develops significant daytime sleepiness or episodes of falling asleep during activities that require active participation (e.g., driving a motor vehicle, conversations, eating), AZILECT should ordinarily be discontinued. If a decision is made to continue these patients on AZILECT, advise them to avoid driving and other potentially dangerous activities. There is insufficient information to establish that dose reduction will eliminate episodes of falling asleep while engaged in activities of daily living.5.4 Ciprofloxacin or Other CYP1A2 InhibitorsRasagiline plasma concentrations may increase up to 2 fold in patients using concomitant ciprofloxacin and other CYP1A2 inhibitors. Patients taking concomitant ciprofloxacin or other CYP1A2 inhibitors should not exceed a dose of AZILECT 0.5 mg once daily [see Dosage and Administration (2.2), Drug Interactions (7.6), and Clinical Pharmacology (12.3)].5.5 Hepatic ImpairmentRasagiline plasma concentration may increase in patients with hepatic impairment. Patients with mild hepatic impairment should be given the dose of AZILECT 0.5 mg once daily. AZILECT should not be used in patients with moderate or severe hepatic impairment [see Dosage and Administration (2.3) and Clinical Pharmacology (12.3)].5.6 Hypotension / Orthostatic HypotensionIn Study 3, the incidence of orthostatic hypotension consisting of a systolic blood pressure decrease (> 30 mm Hg) or a diastolic blood pressure decrease (> 20 mm Hg) after standing was 13% with AZILECT (1 mg/day) compared to 9% with placebo [see Adverse Reactions (6.1)].At the 1 mg dose, the frequency of orthostatic hypotension (at any time during the study) was approximately 44% for AZILECT vs 33% for placebo for mild to moderate systolic blood pressure decrements (> 20 mm Hg), 40% for AZILECT vs 33% for placebo for mild to moderate diastolic blood pressure decrements (> 10 mm Hg), 7% for AZILECT vs 3% for placebo for severe systolic blood pressure decrements (> 40 mm Hg), and 9% for AZILECT vs 6% for placebo for severe diastolic blood pressure decrements (≥20 mm Hg). There was also an increased risk for some of these abnormalities at the lower 0.5 mg daily dose and for an individual patient having mild to moderate or severe orthostatic hypotension for both systolic and diastolic blood pressure.In Study 2 where AZILECT was given as an adjunct therapy in patients not taking concomitant levodopa, there were 5 reports of orthostatic hypotension in patients taking AZILECT 1 mg (3.1%) and 1 report in patients taking placebo (0.6%) [see Adverse Reactions(6.1].Clinical trial data further suggest that orthostatic hypotension occurs most frequently in the first two months of AZILECT treatment and tends to decrease over time.Some patients treated with AZILECT experienced a mildly increased risk for significant decreases in blood pressure unrelated to standing but while supine.The risk for post-treatment hypotension (e.g., systolic < 90 or diastolic < 50 mm Hg) combined with a significant decrease from baseline (e.g., systolic > 30 or diastolic > 20 mm Hg) was higher for AZILECT 1 mg (3.2%) compared to placebo (1.3%).There was no clear increased risk for lowering of blood pressure or postural hypotension associated with AZILECT 1 mg/day as monotherapy.When used as an adjunct to levodopa, postural hypotension was also reported as an adverse reaction in approximately 6% of patients treated with AZILECT 0.5 mg, 9% of patients treated with AZILECT 1 mg and 3% of patients treated with placebo. Postural hypotension led to drug discontinuation and premature withdrawal from clinical trials in one (0.7%) patient treated with AZILECT 1 mg/day, no patients treated with AZILECT 0.5 mg/day and no placebo-treated patients.5.7 DyskinesiaWhen used as an adjunct to levodopa, AZILECT may cause dyskinesia or potentiate dopaminergic side effects and exacerbate pre-existing dyskinesia. In Study 3, the incidence of dyskinesia was 18% for patients treated with 0.5 mg or 1 mg AZILECT as an adjunct to levodopa and 10% for patients treated with placebo as an adjunct to levodopa. Decreasing the dose of levodopa may mitigate this side effect [see Adverse Reactions (6.1].5.8 Hallucinations / Psychotic-Like BehaviorIn the monotherapy study (Study 1), the incidence of hallucinations reported as an adverse event was 1.3% in patients treated with AZILECT 1 mg and 0.7% in patients treated with placebo. In Study 1, the incidence of hallucinations reported as an adverse reaction and leading to drug discontinuation and premature withdrawal was 1.3% in patients treated with AZILECT 1 mg and 0% in placebo-treated patients.When studied as an adjunct therapy without levodopa (Study 2), hallucinations were reported as an adverse reaction in 1.2% of patients treated with 1 mg/day AZILECT and 1.8% of patients treated with placebo. Hallucinations led to drug discontinuation and premature withdrawal from the clinical trial in 0.6% of patients treated with AZILECT 1 mg/day and in none of the placebo-treated patients.When studied as an adjunct to levodopa (Study 3), the incidence of hallucinations was approximately 5% in patients treated with AZILECT 0.5 mg/day, 4% in patients treated with AZILECT 1 mg/day, and 3% in patients treated with placebo. The incidence of hallucinations leading to drug discontinuation and premature withdrawal was about 1% in patients treated with 0.5 mg AZILECT and 1 mg AZILECT/day, and 0% in placebo-treated patients [see Adverse Reactions (6.1)].Postmarketing reports indicate that patients may experience new or worsening mental status and behavioral changes, which may be severe, including psychotic-like behavior during treatment with AZILECT or after starting or increasing the dose of AZILECT. Other drugs prescribed to improve the symptoms of Parkinson’s disease can have similar effects on thinking and behavior. This abnormal thinking and behavior can consist of one or more of a variety of manifestations including paranoid ideation, delusions, hallucinations, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, and delirium.Patients should be informed of the possibility of developing hallucinations and instructed to report them to their health care provider promptly should they develop.Patients with a major psychotic disorder should ordinarily not be treated with AZILECT because of the risk of exacerbating the psychosis with an increase in central dopaminergic tone. In addition, many treatments for psychosis that decrease central dopaminergic tone may decrease the effectiveness of AZILECT [see Drug Interactions (7.8)].Consider dose reduction or stopping the medication if a patient develops hallucinations or psychotic like behaviors while taking AZILECT.5.9 Impulse Control / Compulsive BehaviorsCase reports suggest that patients can experience intense urges to gamble, increased sexual urges, intense urges to spend money, binge eating, and/or other intense urges, and the inability to control these urges while taking one or more of the medications, including AZILECT, that increase central dopaminergic tone and that are generally used for the treatment of Parkinson’s disease. In some cases, although not all, these urges were reported to have stopped when the dose was reduced or the medication was discontinued. Because patients may not recognize these behaviors as abnormal, it is important for prescribers to specifically ask patients or their caregivers about the development of new or increased gambling urges, sexual urges, uncontrolled spending or other urges while being treated with AZILECT. Consider dose reduction or stopping the medication if a patient develops such urges while taking AZILECT.5.10 Withdrawal-Emergent Hyperpyrexia and ConfusionA symptom complex resembling neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability), with no other obvious etiology, has been reported in association with rapid dose reduction, withdrawal of, or changes in drugs that increase central dopaminergic tone.5.11 MelanomaEpidemiological studies have shown that patients with Parkinson’s disease have a higher risk (2to approximately 6-fold higher) of developing melanoma than the general population. Whether the increased risk observed was due to Parkinson’s disease or other factors, such as drugs used to treat Parkinson’s disease, is unclear.For the reasons stated above, patients and providers are advised to monitor for melanomas frequently and on a regular basis. Ideally, periodic skin examinations should be performed by appropriately qualified individuals (e.g., dermatologists).6. ADVERSE REACTIONSThe following adverse reactions are described in more detail in the Warnings and Precautions section of the label:•Hypertension [see Warnings and Precautions (5.1)]•Serotonin Syndrome [see Warnings and Precautions (5.2)]• Falling Asleep During Activities of Daily Living and Somnolence [see Warnings and Precautions (5.3)]• Hypotension / Orthostatic Hypotension [see Warnings and Precautions (5.6)]• Dyskinesia [see Warnings and Precautions (5.7)]• Hallucinations / Psychotic-Like Behavior [see Warnings and Precautions (5.8)]• Impulse Control /Compulsive Behaviors [see Warnings and Precautions (5.9)]• Withdrawal-Emergent Hyperpyrexia and Confusion [see Warnings and Precautions(5.10)]• Melanoma [see Warnings and Precautions (5.11)]6.1 Clinical Trials ExperienceBecause clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the incidence of adverse reactions in the clinical trials of another drug and may not reflect the rates of adverse reactions observed in practice.During the clinical development of AZILECT, Parkinson’s disease patients received AZILECT as initial monotherapy (Study 1) and as adjunct therapy (Study 2, Study 3, Study 4). As the populations in these studies differ, not only in the adjunct use of dopamine agonists or levodopa during AZILECT treatment, but also in the severity and duration of their disease, the adverse reactions are presented separately for each study.Monotherapy Use of AZILECTIn Study 1, approximately 5% of the 149 patients treated with AZILECT discontinued treatment due to adverse reactions compared to 2% of the 151 patients who received placebo.The only adverse reaction that led to the discontinuation of more than one patient was hallucinations.The most commonly observed adverse reactions in Study 1 (incidence in AZILECT-treated patients 3% or greater than the incidence in placebo-treated patients) included flu syndrome, arthralgia, depression, and dyspepsia. Table 1 lists adverse reactions that occurred in 2% or greater of patients receiving AZILECT as monotherapy and were numerically more frequent than in the placebo group in Study 1.Table 1: Adverse Reactions* in Study 1AZILECT 1 mg (N=149) Placebo (N=151)% of Patients % of Patients Headache 14 12Arthralgia 7 4Dyspepsia 7 4 Depression 5 2AZILECT 1 mg (N=149) Placebo (N=151)% of Patients % of PatientsFall 5 3Flu syndrome 5 1 Conjunctivitis 3 1Fever 3 1 Gastroenteritis 3 1Rhinitis 3 1Arthritis 2 1 Ecchymosis 2 0Malaise 2 0Neck Pain 2 0 Paresthesia 2 1Vertigo 2 1*Incidence 2% or greater in AZILECT 1 mg group and numerically more frequent than in placebo group There were no significant differences in the safety profile based on age or gender.Adjunct Use of AZILECTAZILECT was studied as an adjunct therapy without levodopa (Study 2), or as an adjunct therapy to levodopa, with some patients also taking dopamine agonists, COMT inhibitors, anticholinergics, or amantadine (Study 3 and Study 4).In Study 2, approximately 8% of the 162 patients treated with AZILECT discontinued treatment due to adverse reactions compared to 4% of the 164 patients who received placebo.Adverse reactions that led to the discontinuation of more than one patient were nausea and dizziness.The most commonly observed adverse reactions in Study 2 (incidence in AZILECT-treated patients 3% or greater than incidence in placebo-treated patients) included peripheral edema, fall, arthralgia, cough, and insomnia. Table 2 lists adverse reactions that occurred in 2% or greater in patients receiving AZILECT as adjunct therapy without levodopa and numerically more frequent than in the placebo group in Study 2.Table 2: Adverse Reactions* in Study 2AZILECT 1 mg (N=162) Placebo (N=164)% of Patients % of Patients Dizziness 7 6 Peripheral edema 7 4 Headache 6 4Nausea 6 4Fall 6 1Arthralgia 5 2Back pain 4 3Cough 4 1Insomnia 4 1Upper respiratory tractinfection 4 2Orthostatic hypotension 3 1*Incidence 2% or greater in AZILECT 1 mg group and numerically more frequent than in placebo group There were no significant differences in the safety profile based on age or gender.In Study 3, adverse event reporting was considered more reliable than Study 4; therefore, only the adverse event data from Study 3 are presented below.In Study 3, approximately 9% of the 164 patients treated with AZILECT 0.5 mg/day and 7% of the 149 patients treated with AZILECT 1 mg/day discontinued treatment due to adverse reactions, compared to 6% of the 159 patients who received placebo. The adverse reactions that led to discontinuation of more than one AZILECT-treated patient were diarrhea, weight loss, hallucination, and rash.The most commonly observed adverse reactions in Study 3 (incidence in AZILECT-treated patients 3% or greater than the incidence in placebo-treated patients) included dyskinesia, accidental injury, weight loss, postural hypotension, vomiting, anorexia, arthralgia, abdominal pain, nausea, constipation, dry mouth, rash, abnormal dreams, fall and tenosynovitis.Table 3 lists adverse reactions that occurred in 2% or greater of patients treated with AZILECT 1 mg/day and that were numerically more frequent than the placebo group in Study 3.Table 3: Adverse Reactions* in Study 3AZILECT 1 mg (N=149) AZILECT 0.5 mg(N=164)Placebo(N=159)% of patients % of patients % of patients Dyskinesia 18 18 10 Accidental injury 12 8 5 Nausea 12 10 8 Headache 11 8 10Fall 11 12 8 Weight loss 9 2 3 Constipation 9 4 5 Postural hypotension 9 6 3 Arthralgia 8 6 4 Vomiting 7 4 1。
药物杂质列表
Dithianonimpurity2
二氰蒽醌杂质2
N/A
10mg-25mg-50mg-100mg
≥95%
Dithianonimpurity3
二氰蒽醌杂质3
N/A
10mg-25urity4
二氰蒽醌杂质4
21634-42-4
10mg-25mg-50mg-100mg
氟氯西林钠杂质
N/A
10mg-25mg-50mg-100mg
≥95%
Arginine
精氨酸
7200-25-1
10mg-25mg-50mg-100mg
≥95%
Arginineimpurity1
精氨酸杂质1
N/A
10mg-25mg-50mg-100mg
≥95%
Arginineimpurity2
精氨酸杂质2
天津药明康德新药开发有限公司杂质研究中心提供。
Spectinomycin ImpurityF
大观霉素杂质F
N/A
10mg-25mg-50mg-100mg
≥95%
pleuromulin
截短侧耳素
125-65-5
10mg-25mg-50mg-100mg
≥95%
Pleuromulinimpurity
截短侧耳素杂质
丙氨酰谷氨酰胺、大观霉素、截短侧耳素、帕拉米韦、三乙酰更昔洛韦、克林霉素磷酸酯、氟氯西林钠、精氨酸、氰霜唑、二氰蒽醌等杂质列表
英文名称
中文名称
CAS
规格
纯度
结构
Alanyl GlutamineImpurity
丙氨酰谷氨酰胺杂质
N/A
10mg-25mg-50mg-100mg
沙格列汀杂质列表
沙格列汀杂质列表序号中文名称英文名称CAS 结构式1（S)-焦谷氨酸乙酯Saxaint-A NO2（S)-1-Boc-焦谷氨酸乙酯Saxaint-B NO 3(S)-1-Boc-2,3-二氢吡咯-２-甲酸乙酯Saxaint-C NO4(1S,3S,5S)-2-Boc-2-氮杂-双环[3.1.0]己基-3-甲酸乙酯Saxaint-D NO 5(1S,3S,5S)-2-Boc-2-氮杂-双环[3.1.0]己基-3-甲酰胺盐酸盐Saxaint-E NO6N-Boc-3-羟基-1-金刚烷基-甘氨酸Saxaint-F no7(s)-N-叔丁氧羰基-3-羟基-1-金刚烷基-甘氨酸Saxaint-G no(s)-3-羟基-1-金刚烷基-甘氨酸Saxaint-H NO9N-Boc-3-羟基-1-金刚烷基-甘氨酸Saxaint-I 361442-00-410N-Boc-沙克列汀Saxaint-J NO111-金刚烷甲酸Saxaint-K 828-51-3121-金刚烷甲酰氯Saxaint-L 218-252-7132-（1-金刚烷甲酰基）丙二酸乙酯Saxaint-M NO141-乙酰金刚烷Saxaint-N 39917-38-9153-羟基-1-草酰金刚烷Saxaint-O NO沙格列汀Saxagliptin 361442-04-817沙格列汀杂质Epimer-A S,S,S,R (SG-D2)18沙格列汀杂质Epimer-B S,R,S,S(SG-D5)19沙格列汀杂质Enantiomer-C R,R,R,R(SG-E)20沙格列汀杂质Distereomer-DR,R,S,S(SG-D4)21沙格列汀杂质Distereomer-ER,S,R,R(SG-D6)22沙格列汀杂质Distereomer-FR,S,R,R(SG-D6)23沙格列汀杂质Distereomer-GS,R,R,R(SG-D1)24沙格列汀杂质SaxagliptinImpurity SG-8沙格列汀杂质SaxagliptinImpurity SG-926沙格列汀杂质Saxagliptin ImpuritySG-1027沙格列汀杂质SaxagliptinImpurity SG-H28沙格列汀杂质SaxagliptinImpurity SG-I29沙格列汀杂质SaxagliptinImpurity SG-G30沙格列汀杂质SaxagliptinImpurity SG-K31沙格列汀杂质SaxagliptinImpurity SG-L32沙格列汀杂质SaxagliptinImpurity SG-M沙格列汀杂质SaxagliptinImpurity SG-N34沙格列汀杂质SaxagliptinImpurity SG-O35沙格列汀杂质Saxagliptin Impurity36沙格列汀杂质SaxagliptinImpurity M137沙格列汀杂质SaxagliptinImpurity M2。
雷沙吉兰的副作用和禁忌
雷沙吉兰的副作用和禁忌雷沙吉兰的适应证用于治疗帕金森病，可单用（早期）或作为左旋多巴的辅助用药（中晚期）（国外资料）。
与左旋多巴联用时可强化左旋多巴疗效、延长其药效时间，所以对异动患者有加重其异动风险。
雷沙吉兰的用法用量雷沙吉兰为片剂，有0.5和1 mg两种规格。
标准的雷沙吉兰口服剂量为0.5至1 mg，每日一次，单独服用或与左旋多巴类药物的（美多芭、息宁）一同服用。
雷沙吉兰的禁忌证1.重度肝功能不全患者禁用（国外资料）。
2.中度肝功能不全患者避免使用（国外资料）。
注意事项1.轻度肝功能不全患者慎用（国外资料）。
2.药物对妊娠的影响：尚不明确。
3.药物对哺乳的影响：尚不明确。
4.如果患者治疗同时进食富含酪胺的食物和饮料(如奶酪和红酒)、食品添加剂或许多含胺类的咳嗽药或感冒药，雷沙吉兰可能导致高血压危象。
因此，服药同时应避免进食上述食物或药物。
雷沙吉兰的副作用1.心血管系统：可见心绞痛，少见脑血管意外和心肌梗死。
2.中枢神经系统：可见头痛、眩晕、抑郁。
3.呼吸系统：可见鼻炎。
4.肌肉骨骼系统：可见颈痛、关节痛、关节炎。
5.泌尿生殖系统：可见尿急。
6.胃肠道：可见消化不良、食欲缺乏。
7.血液：可见白细胞减少。
8.皮肤：可见皮疹、黑色素瘤。
9.眼：可见结膜炎。
10.其他：可见流感样综合征。
药物相互作用1.CYP 1A2的强抑制药可升高雷沙吉兰的血药浓度，合用时应慎重。
2.与其他MAOIs同用，有发生非选择性MAO抑制的危险，可能导致血压升高。
3.与恩他卡朋合用，雷沙吉兰的清除率增加28%。
4.其余参见司来吉兰。
5.吸烟可诱导肝酶代谢，可能降低雷沙吉兰的血药浓度。
链接：盐酸司来吉兰片不能与哪些药物同时服用温馨提示：本文内容为网上资料整理而来，具体用药请咨询专业医生，帕金森个体差异大，涉及到具体用药请遵医嘱。
雷萨吉兰甲磺酸盐(rasagiline mesylate)
雷萨吉兰甲磺酸盐(rasagiline mesylate)
王惠;程卯生
【期刊名称】《中国药物化学杂志》
【年(卷),期】2007(17)4
【总页数】1页(P263-263)
【关键词】甲磺酸盐;早期帕金森病;晚期帕金森病;欧盟国家;口服药物;制药工业;单药治疗;左旋多巴
【作者】王惠;程卯生
【作者单位】沈阳药科大学
【正文语种】中文
【中图分类】R978.7
【相关文献】
1.新颖抗帕金森氏病药雷萨吉兰及其市场趋势 [J], 马培奇（编译）
2.雷沙吉兰(Rasagiline)对Aβ25-35诱导PC12细胞凋亡的防护作用 [J], 李红杰;胡林森;常明;侯澍;张磊;张瑜
3.雷萨吉兰甲磺酸盐 [J], 王惠
4.治疗帕金森病新药雷沙吉兰（rasagiline） [J],
因版权原因，仅展示原文概要，查看原文内容请购买。
沙格雷酯杂质汇总
专业<杂质对照品>解决方案，代理中检所/EP/BP/USP/LGC/TRC/DR/TLC/MC/SIGMA/BACHEM/STD等品牌。 1814+064+3157
项目报批 纯度高于98%
沙格雷酯杂质5
Sarpogrelate Impurity 1659311-40-
5
6(free base)
10mg 25mg 50mg 100mg 更大规格请咨询
项目报批 纯度高于98%
扬信医药代理各品种杂质对照品:舒更葡糖钠杂质，达托霉素杂质，依维莫司杂质，他克莫司杂质，阿奇霉素杂质，克拉维酸钾杂质， 红霉素杂质，克拉霉素杂质，林可霉素杂质，罗红霉素杂质，克林霉素杂质，恩曲他滨杂质，艾地那非杂质，瑞卢戈利杂质，艾氟康唑
沙格雷酯杂质列表集
中文名称
英文名称
CAS
Sarpogrelate Impurity
沙格雷酯杂质1
1
N/A
规格
10mg 25mg 50mg 100mg 更大规格请咨询
用途
项目报批 纯度高于98%
结构式
沙格雷酯杂质2 Sarpogrelate Impurity
N/A
2
10mg 25mg 50mg 100mg 更大规格请咨询
项目报批 纯度高于98%
Sarpogrelate Impurity
沙格雷酯杂质3
N/A
3
10mg 25mg 50mg 100mg 更大规格请咨询
项目报批 纯度高于98%
Sarpogrelate Impurity 1659311-47-3
HPLC法测定甲磺酸雷沙吉兰片的有关物质
（HPLC 法测定甲磺酸雷沙吉兰片的有关物质周敏* 丁云晖 陈红霞（上海上药中西制药有限公司 上海 201806）摘 要 目的: 建立HPLC 法测定甲磺酸雷沙吉兰片有关物质的方法。
方法：采用Eclipse XDB-C 18柱、乙腈-高氯酸溶液为流动相、检测波长为210 nm 等条件下进行HPLC 测定。
结果：在该色谱条件下，主药和有关物质能较好地分离，雷沙吉兰浓度和峰面积在0.008 2～3.2 m g/ml 内线性关系良好(r = 0.999 5，n =8)，而杂质A 和B 的浓度和峰面积分别在0.001 6~3.2 m g/ml 和0.002 1~3.2 m g/ml 内呈良好的线性关系 (r =0.999 6，n =8)。
结论：本方法简便、准确、可行、精密度高，可用于甲磺酸雷沙吉兰片有关物质的质量控制。
关键词 甲磺酸雷沙吉兰 HPLC 有关物质中图分类号：R917 文献标志码：A 文章编号：1006-1533(2018)09-0077-04Determination of the related substances in rasagiline mesylate tablets by HPLCZHOU Min *, DING Yunhui, CHEN Hongxia（Shanghai Zhongxi Pharmaceutical (Group) Co., Ltd., Shanghai 201806, China ）ABSTRACT Objective: To establish a method for the determination of the related substances in rasagiline mesylate tablets by HPLC. Methods: HPLC was performed on Eclipse XDB-C 18 column with acetonitrile-perchloric acid solution as a mobile phase at the detected UV wavelength of 210 nm. Results: The resolution between rasagiline mesylate and the other peaks met the requirements. The standard curves of rasagiline mesylate and the related substance A and B showed a good linearity over the range of 0.008 2~3.2 m g/ml, 0.001 6~3.2 m g/ml and 0.002 1~3.2 m g/ml, respectively. Conclusion: This method is simple, accurate and feasible with higher precise, and can be used as quality control of the related substances in rasagiline mesylate tablets.KEy WORDS rasagiline mesylate; HPLC; related substances雷沙吉兰是一种有效的、不可逆的、选择性单胺氧化酶B （MAO-B ）抑制剂，能使纹状体细胞外多巴胺含量升高[1-3]。
单胺氧化酶-B抑制药雷沙吉兰的临床药理学特征解析
单胺氧化酶-B抑制药雷沙吉兰的临床药理学特征解析陈霞【期刊名称】《武警医学》【年(卷),期】2016(027)003【总页数】4页(P309-312)【关键词】雷沙吉兰;帕金森病;临床药理学【作者】陈霞【作者单位】100032,北京协和医院临床药理中心【正文语种】中文【中图分类】R971.5帕金森病(Parkinson’s disease，PD)是常见的慢性进行性神经系统退行性疾病，位居全球第二，其发病率为(8～18)/10万人年，绝大多数帕金森病均起病于50岁以后[1,2]。
随着世界人口的老龄化，帕金森病的患病率有逐渐升高的趋势。
我国65岁以上人群帕金森病的患病率约为1.7%，与发达国家相当[3]。
大部分帕金森病患者为散发病例，仅有不到10%的患者有家族史。
本综述从临床药理学角度解析了雷沙吉兰在药代动力学、药效学、代谢产物等方面的特征，分析这些特征对于其临床应用的潜在意义，并在适用的范围内比较雷沙吉兰和另一种单胺氧化酶(monoamine oxidase，MAO)抑制药司来吉兰的异同。
帕金森病的临床表现包括运动症状和非运动症状，其中运动症状主要表现为意向性震颤、少动、肌张力升高和相对在病程晚期出现的姿位平衡障碍等[4]。
与帕金森病运动症状相关的核心病理改变是患者中脑黑质多巴胺(dopamine, DA)能神经元的变性死亡，使纹状体多巴胺含量显著减少并致病。
导致这一病理改变的确切病因目前尚不清楚，遗传因素、环境因素、年龄老化、氧化应激等均可能参与帕金森病多巴胺能神经元的变性凋亡过程。
帕金森病目前尚无治愈手段。
针对上述病理生理过程，对抗运动症状的药物主要可分为两大类：一类是与多巴胺替代治疗相关的药物，包括作用于中枢神经系统内的多巴胺前体物质左旋多巴和抑制病理状态下脑内多巴胺代谢的单胺氧化酶-B抑制药[如司来吉兰(selegiline) 和雷沙吉兰(rasagiline)]，以及作用于外周的阻断外周多巴胺降解的脱羧酶抑制药(例，卡比多巴和苄丝肼)和儿茶酚-氧位-甲基转移酶抑制药(COMT抑制药，如恩他卡朋和托卡朋)；另一类是直接作用于突触后膜多巴胺受体的多巴胺受体激动药(如罗匹尼罗、普拉克索、培高利特和溴隐亭等)。
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雷沙吉兰杂质4 Rasagiline Impurity 4 1175018-73-1
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项目报批 纯度高于98%
雷沙吉兰杂质5 Rasagiline Impurity 5 10277-74-4
志 -064- 维酸钾杂质，红霉素杂质，克拉霉素杂质，林可霉素杂质，罗红霉素杂质，克林霉素杂质，恩曲他滨杂质，艾地那非；
康
-3157 瑞卢戈利杂质，艾康氟康唑杂质等；并提供COA、NMR、HPLC、MS等结构确证图谱;详情请点 用户名 ，谢谢！
扬信医药专业<杂质对照品>解决方案，代理中检所/EP/BP/USP/LGC/TRC/DR/TLC/MC/SIGMA/BACHEM/ STD 等品牌。
雷沙吉兰Rasagiline杂质汇总列表
中文名称
英文名称
CAS
雷沙吉兰杂质1 Rasagiline Impurity 1 185517-74-2
规格
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用途
项目报批 纯度高于98%
结构式
雷沙吉兰杂质2 Rasagiline Impurity 2 1179031-47-0
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雷沙吉兰杂质9 Rasagiline Impurity 9 1312077-04-5
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项iline Impurity 10 1175018-74-2
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1312077-05-6 雷沙吉兰杂质11 Rasagiline Impurity 11 （free
base）
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项目报批 纯度高于98%
唐 1814- 扬信医药 代理各品种杂质对照品:舒更葡糖钠杂质，达托霉素杂质，依维莫司杂质，他克莫司杂质，阿奇霉素杂质，克拉