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抗高血压药物的研究进展[论文摘要] 高血压是最常见的心血管病，我国人群高血压患病率高达19.88%，就意味着我国13亿人口中，患高血压者达两亿之多，而高血压又是心、脑血管及心、肾功能衰竭等病变的主要危险因素。
近年来，随着高血压基础研究和治疗学等方面不断深入，国内外诸多大规模临床治疗试验均已取得丰厚的成果，同时对各种常用抗高血压药物的优缺点也有了较全面的认识，这就使得高血压治疗能更好地纠正和改善高血压的各种病理生理状态，从而明显减轻靶器官损害，降低高血压并发症的发生率和死亡率，提高患者的生活质量。
本文主要就临床中常用抗高血压药物的发展和临床应用进行深入评价。
关键词：高血压治疗药物发展目录引言 (1)一、对高血压的基本认识 (1)（一）高血压的发病原因 (1)1、同所处环境成正比 (1)2、与遗传因素相关 (1)3、不能排除饮食等因素影响 (1)（二）高血压治疗范围的界定 (1)二、抗高血压药物的发展历程 (2)（一）上世纪60年代（利尿降压药） (2)1、降压机制 (2)2、临床应用 (2)3、不良反应 (2)（二）上世纪70年代（β- 受体阻滞剂） (2)1、作用机制 (2)2、临床应用 (2)3、不良反应 (3)（三）上世纪80年代（血管紧张素转换酶抑制剂） (3)1、作用机制 (3)2、临床应用 (4)3、不良反应 (4)（四）上世纪90年代（长效钙拮抗剂） (4)1、作用机制 (4)2、临床应用 (4)3、不良反应 (5)三、抗高血压新药的研究 (5)（一）血管紧张素Ⅱ受体拮抗剂 (5)1、作用机制 (5)2、临床应用 (5)（二）α-受体阻滞剂 (6)1、作用机制 (6)2、临床应用 (6)3、不良反应 (6)四、抗高血压药物的使用原则 (6)（一）小剂量用药的原则 (6)（二）高血压分级诊断的原则 (7)结束语 (7)谢辞 (8)参考文献 (9)引言近年来，随着人民生活水平的提高，高血压的发病率也呈现出上升的态势，成为危害人民健康的常见病，严重威胁国民的身体健康。
核准日期：2007年3月10日修订日期：2020年3月25日【通用名称】盐酸胺碘酮片[药典]【商品名称】可达龙® Cordarone【英文名称】Amiodarone Hydrochloride Tablets[药典]【汉语拼音】Yan Suan An Dian Tong Pian【成份】本品要紧成份为：盐酸胺碘酮化学名称：(2-丁基-3-苯并呋喃基)［4-［2-(二乙氨基)乙氧基］-3，5-二碘苯基］甲酮盐酸盐化学结构式：点击放大分子式：C25H29I2NO3·HCl分子量：681.78要紧成份相关链接：盐酸胺碘酮D 【性状】本品为类白色片。
【适应症】1.房性心律失常（心房扑动，心房纤颤转律和转律后窦性心律的维持）。
2.结性心律失常。
3.室性心律失常（医治危及生命的室性期前收缩和室性心动过速和室性心律过速或心室纤颤的预防）。
4.伴W-P-W综合征的心律失常。
依据其药理学特点，胺碘酮适用于上述心律失常，尤其归并器质性心脏病的患者（冠状动脉供血不足及心力衰竭）。
【规格】0.2g【用法用量】- 负荷量：通常一日600mg（3片），能够持续应用8-10日- 维持量：宜应用最小有效剂量。
依照个体反映，可给予一日100-400mg.由于胺碘酮的延长医治作用，可给予隔日200mg或一日100mg。
已有推荐每周停药二日的间隙性医治方式。
【不良反映】依照系统器官和发生率，对不良反映进行了分类，其中发生频率的分类类别为：超级常见(≥10%)；常见(≥1%，<10%)；不常见(≥0.1%，<1%)；罕有(≥0.01%，<0.1%)，超级罕有(<0.01%)。
眼睛的征象：●超级常见：角膜微沉淀，在成人中几乎会普遍地显现，通常局限于瞳孔下面的区域，并非提示为医治的禁忌。
在例外情形下，它们可能伴有有色的耀眼的晕轮或视力模糊。
这种角膜微沉淀由复合的脂质沉积组成，在停止胺碘酮医治后通常完全可逆。
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jun.-27-2017Print Date:Jun.-27-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :NPS-2143 (hydrochloride)Catalog No. :HY-10171CAS No. :324523-20-81.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:NPS2143 hydrochloride; NPS 2143 hydrochlorideFormula:C24H26Cl2N2O2Molecular Weight:445.38CAS No. :324523-20-84. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
国家药品监督管理局通告2020年第30号——国家药监局关于发布仿制药参比制剂目录（第二十七批）的
通告
文章属性
•【制定机关】国家药品监督管理局
•【公布日期】2020.04.29
•【文号】国家药品监督管理局通告2020年第30号
•【施行日期】2020.04.29
•【效力等级】部门规范性文件
•【时效性】现行有效
•【主题分类】药政管理
正文
国家药品监督管理局通告
2020年第30号
国家药监局关于发布仿制药参比制剂目录（第二十七批）的
通告
经国家药品监督管理局仿制药质量与疗效一致性评价专家委员会审核确定，现发布仿制药参比制剂目录（第二十七批）。
特此通告。
附件：仿制药参比制剂目录（第二十七批）
国家药监局
2020年4月29日附件
仿制药参比制剂目录（第二十七批）。
一、组胺H1受体拮抗剂的化学结构类型过敏介质：组胺、白三烯、缓激肽
1、乙二胺类
2、哌嗪类
3、氨基醚类：盐酸苯海拉明2-二苯甲氧基-N，N-二甲基乙胺盐酸盐1、有醚键：对碱稳定，酸中水解为二苯甲醇2、对光稳定，曝晒16h 或存放3年不变色。
杂质二苯甲醇(受光氧化)和二甲胺基乙醇3、叔胺结构，类似生物碱沉淀试剂反应。
Mandelin 、Frohde、 Macquis来源：考试资料网
4、丙胺类：氯苯那敏(扑尔敏)：γ-(4-氯苯基)-N，N-二甲基-2-吡啶丙胺马来酸盐1、具有升华性，有特殊晶型右旋体(S)强于左旋用消旋体2、叔胺类反应3、戊烯二醛反应：吡啶环，PH3.5中与溴化氢，吡啶环开环。
5、三环类：盐酸赛庚啶4-[ 5H-二苯并[a，d]环庚三烯-5-亚基]-1-甲基哌啶盐酸盐倍半水合物来源：考试资料网性质：1、含氮碱性化合物，与生物碱显色试剂反应。
2、甲醇溶液滴于纸上风干后紫外照射，显蓝色荧光。
无杂原子应用：抗5-羟色胺及抗胆碱作用(唯一)。
酮替芬：含杂原子S，抗组胺是扑尔敏的10倍，时间长，抗过敏介质释放。
治疗、控制哮喘
6、哌啶类特非那定：几乎无中枢镇静作用的H1受体拮抗剂
7、无嗜睡作用的H1受体拮抗剂：阿司米唑二、组胺H1受体拮抗剂构效关系：来源：考试资料网1、两个芳环R和R不处于同一平面时，具有最大的抗组胺活性。
2、几何异构体有立体选择性，显示不同的活性。
3、光学异构体也显示不同的活性。
血管紧张素受体拮抗剂简介血管紧张素受体拮抗剂（Angiotensin receptor blockers，简称ARBs）也称为血管紧张素II受体拮抗剂，是一类用于治疗高血压和心衰的药物。
ARBs和血管紧张素转换酶抑制剂（ACEI）一样，能够阻断肾素-血管紧张素系统（RAAS）的作用。
RAAS是维持血浆钠浓度和血容量稳定的主要机制，对血压和水盐代谢有着重要的调节作用。
但在某些情况下，RAAS的过度激活会导致高血压等病症的发生。
ARBs通过阻断血管紧张素II（AT2）受体，降低血压和减少水盐的滞留，从而达到治疗高血压和心衰的效果。
作用机制RAAS调节血压和水盐代谢主要依靠血管紧张素II的作用。
血管紧张素II通过与AT1受体结合，引起血管肌收缩，导致血管阻力升高，进而导致高血压的发生。
ARBs通过竞争性与AT1受体结合，从而避免血管紧张素II对AT1受体的刺激作用，阻断紧张素II的生理效应，减少血管阻力，达到降低血压和改善心脏功能的作用。
适应症ARBs适用于以下情况：1.轻度至中度高血压的治疗。
2.对ACEI有禁忌症或无反应的高血压患者。
3.心肌缺血和心肌梗死的治疗。
4.心衰的治疗。
5.糖尿病肾病的治疗。
6.肝硬化门脉高压的治疗。
7.晚期肾脏病的治疗。
如何使用ARBs常规剂量一般为每天口服一次，用于降低血压的常见剂量为40-80mg。
具体用药剂量和使用方法应由医生根据患者情况调整和指导。
ARBs的使用一般需要长期维持，以达到降低血压和改善心脏功能的效果。
常见不良反应ARBs通常不良反应较小，常见副作用包括：1.头痛。
2.头晕和乏力。
3.消化系统不适，如腹泻、恶心和呕吐。
4.低血压和肾功能不全。
5.过敏反应。
如果出现不良反应，应及时停药并咨询医生。
注意事项1.ARBs是一种处方药，需要在医生的指导下使用。
2.ARBs存在与其他药物的相互作用，应特别注意如ACEI、骨钙素拮抗剂、钾保留利尿药等的合并应用和剂量。
