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【医学ppt课件】人工合成抗菌药

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医学ppt课件 人工合成抗菌药 人工合成抗菌药PPT课件 抗菌药物ppt课件 合成抗菌药PPT课件 人工合成 抗菌药 抗菌药物抗菌药物 人工合成抗菌药物 PPT医学课件
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单击此处编辑母版标题样式 单击此处编辑母版副标题样式 *1 第四十三章 人工合成抗菌药 喹诺酮类药物 磺胺类药物 其他合成抗菌药物 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 第一节 喹诺酮类药物(quinolones) 基本要求 1.掌握喹诺酮类抗菌作用、机制、应用和不良反应。 2.掌握第三代喹诺酮类主要代表药及作用特点。 3.了解喹诺酮类药物的分类、共同特性、耐药性机制 、禁忌症和药物相互作用。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 第一代 萘啶酸 第二代 吡哌酸 第三代 氟喹诺酮类 一、一、药物发展史药物发展史 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 第三代 氟喹诺酮类 以4-喹诺酮为基本结构,N1、C3、C6、C7、C8引入不 同基团,形成各具特点的喹诺酮类 环丙沙星 (ciprofloxacin)氧氟沙星 (ofloxacin) 依诺沙星 (enoxacin)洛美沙星 (lomefloxacin) 培氟沙星 (pefloxacin)氟罗沙星 (fleroxacin) 诺氟沙星 (norfloxacin)托氟沙星 (tosufloxacin) 芦氟沙星 (rufloxacin)司氟沙星 (sparfloxacin) 格帕沙星 (grepafloxacin) 曲伐沙星 (trovafloxacin) 那氟沙星 (nadifloxacin) 左氧氟沙星 (levofloxacin) Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 抗菌谱 广谱杀菌药 G+、G-、绿脓杆菌、支原体、衣原体 、军团菌、结核菌、厌氧菌等 机 制 抑制G- 菌DNA回旋酶, 抑制G+ 菌拓扑异构酶Ⅳ 阻碍DNA复制而杀菌 可能的机制:抑制RNA及蛋白质合成;诱导菌体DNA错 误复制;抗菌后效应 二、抗菌作用及作用机制二、抗菌作用及作用机制 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. u大肠杆菌的DNA螺旋酶: u2个A亚单位 + 2个B亚单位 uA亚单位:双链断开。 uB亚单位:催化ATP水解,提供能量 ,前链后移。 uA亚单位:封口 负超螺旋。 u药物-DNA-酶 复合物。 u u抑制断裂、再接功能 阻碍 DNA复制 细菌死亡。 u对人体拓朴异构酶Ⅱ影响很小 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 口服吸收较好,血药浓度较高 t 1/2 较长,3.5 ~ 7 h 血浆蛋白结合率低,组织穿透性好,分布广。 可进入骨、关节、前列腺、脑(氧氟、环丙、培 氟)达治疗浓度 主要经肝代谢,肾排泄差异较大 四、体内过程四、体内过程 三、耐药机制三、耐药机制 交叉耐药,常见金、肠、大、铜交叉耐药,常见金、肠、大、铜 高浓下,DNA回旋酶染色体突变,与药亲和力 低浓下,膜结构改变,通透性降低 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 五、临床应用五、临床应用 u1. 泌尿生殖道感染: 环丙沙星、加替沙星、氧氟沙星与-内酰胺类同 为首选药。用于前列腺炎、单纯性淋球菌性尿道 炎或宫颈炎。铜绿假单胞菌性尿道炎---首选环丙 沙星 u2. 呼吸系统感染: 左氧氟沙星、莫西沙星或加替沙星与万古霉素合 用首选用于高度耐青霉素的肺炎链球菌感染。 氟喹诺酮类替代大环内酯类用于支原体/衣原体/ 军团菌肺感染 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 五、临床应用五、临床应用 3. 肠道感染与伤寒 首选用于志贺菌引起的菌痢、沙门菌引 起的胃肠炎 伤寒或副伤寒---首选氟喹诺酮类或头孢 曲松 4、用于脑膜炎奈瑟菌鼻烟部带菌者的根除 治疗 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 六、不良反应六、不良反应 1. 1.胃肠道反应 较常见,厌食、恶心、呕吐 、胃部不适(发生率3~5%) 2.中枢神经系统毒性 兴奋症状:轻者头痛 、失眠,重者精神异常抽搐、惊厥。可能 是药物抑制GABA与其受体的结合所致 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 3、皮肤反应及光敏反应 水肿、皮肤瘙痒 、光照部位皮肤出现瘙痒性红斑,严重 者皮肤糜烂、脱落,停药可恢复。(尤 为皮肤蓄积者,如洛美沙星、司氟沙星 ) 4、其他 可能引起负重关节软骨损伤(动 物实验),儿童可致关节痛和关节水肿 。孕妇、乳母避免用。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 八、药物相互作用八、药物相互作用 u抗酸药、含金属离子的药物可减少其生物利用 度,避免同服 u慎与茶碱或非甾体类抗炎药(NSAID)合用,增 加其中枢毒性反应。依诺沙星、环丙沙星抑制 茶碱代谢。 u环丙沙星、洛美沙星、司氟沙星避免日照保存 、应用,患者用上述药期间避免日照。 七、禁忌症七、禁忌症 过敏者;过敏者;精神病精神病/ /癫痫病史癫痫病史;; 儿童、孕妇儿童、孕妇/ /授乳妇女授乳妇女 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 诺氟沙星 (norfloxacin氟哌酸) 第一个 用于临床。用于泌尿系、肠道感染和淋病。 支原体、衣原体、军团菌感染无临床价值。 环丙沙星(ciprofloxacin) 抗菌活性强。 厌氧菌不敏感。应用于对其他抗菌药耐药的 G-杆菌所致的呼吸道、泌尿生殖道、消化道 、骨关节及皮肤软组织感染。老年人、运动 员慎用(诱发跟腱炎和跟腱撕裂) 九、常用药物特点九、常用药物特点 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 氧氟沙星(ofloxacin)抗菌活性强而广, 包括沙眼衣原体、部分厌氧菌结核菌等 。用于呼吸道、泌尿生殖道、胆道、皮 肤软组织、盆腔感染等。抗TB杆菌第二 线药。 左氧氟沙星(levofloxacin) 抗菌活性为 氧氟沙星2倍, G+和G-菌、支原体、衣原 体、军团菌、厌氧菌等均有较强杀灭作 用。不良反应最低。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 洛美沙星(lomefloxacin) 和氟罗沙星(fleroxacin) 抗菌谱广、抗菌活性强、口服吸收好,作用与氧 氟沙星接近。用药期间应避免日光。 司氟沙星(sparfloxacin) 主要对G- 、G+ 、支原体、衣原体、军团菌、结核 菌、厌氧菌等作用强,等同或优于氧氟沙星和环 丙沙星,用于全身感染。 莫西沙星(moxifloxacin) 第四代,广谱、高效、低毒,用于全身感染, 无光敏反应。 九、常用药物特点九、常用药物特点 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 第二节第二节 磺胺类抗菌药磺胺类抗菌药 基本要求 1.掌握磺胺类的抗菌作用机制和不良反应。 2.掌握磺胺甲恶唑、磺胺嘧啶的抗菌作用特点和临床 应用。 3. 掌握甲氧苄啶的作用机制、与磺胺合用的理由。 4.了解磺胺类药物的分类、柳氮磺胺吡啶、磺胺嘧啶 银、磺胺米隆、磺胺醋酰钠的作用特点和应用。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 一、化学及分类一、化学及分类 对氨基苯磺酰胺衍生物对氨基苯磺酰胺衍生物 分类: 肠道易吸收类,肠道难吸收类,外用类 短效(SIZ) 中效(SD、SMZ) 长效(磺胺多辛) 二、抗菌作用与机制二、抗菌作用与机制 广谱抑菌药广谱抑菌药 抗菌谱抗菌谱 G+、G-、沙眼衣原体、疟原虫等及绿脓杆菌。 但对支原体、立克次体、螺旋体无效 抗菌机制抗菌机制 影响叶酸代谢 三、耐药性三、耐药性 同类有交叉耐药 异类无交叉耐药 机制:合成过量的PABA;降低膜通透性;改变代谢途径 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 谷氨酸谷氨酸 食物食物 + + 二氢蝶酸合成酶二氢蝶酸合成酶 二氢叶酸还原酶二氢叶酸还原酶 蝶啶蝶啶 二氢叶酸二氢叶酸 四氢叶酸四氢叶酸 + + 对氨苯甲酸对氨苯甲酸 一碳单位一碳单位 ((PABA) PABA) 核酸合成核酸合成 ↑ ↑ 磺胺类磺胺类 ↑ ↑ 甲氧苄啶甲氧苄啶 ((TMP)TMP) 磺胺类药物能否与甲氧苄啶合用?能磺胺类药物能否与甲氧苄啶合用?能 ①①增强抗菌作用增强抗菌作用 ②② 扩大抗菌谱扩大抗菌谱 ③③ 延缓耐药性延缓耐药性 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 四、体内过程四、体内过程 全身给药体内分布广,蛋白结合率低的易 过血脑屏障;主要在肝脏代谢为乙酰化物,在 肾脏排泄(原形、乙酰化物、葡糖酸结合物) ,酸性尿中易析出结晶 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 五、不良反应五、不良反应 1. 肾损害 在尿中结晶析出:结晶尿、血尿、 疼痛、尿闭。 防治措施:① 服等量NaHCO3,以增加溶解度 ②多饮水,加速排泄 ③ 用药超一周者定期 检查尿液 2. 过敏反应:药热、皮疹,偶见剥脱性皮炎。 本类药有交叉过敏,有过敏史者禁用 。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 3. 血液系统反应 久用可抑制骨髓造血 白细胞减少、血小板减少、再障。 用药期间定期查血常规。 4. 神经系统反应 头晕、乏力。 不应从事高空作业和驾驶 5. 其它 消化道反应;肝损害(肝功能受损者免用); 核黄疸:药物竞争血浆白蛋白,血中游离胆红素 ↑→黄疸,进入CNS→核黄疸。 新生儿、早产儿、孕妇、授乳妇女不用。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 1.1.全身性感染全身性感染 短效磺胺异恶唑(SIZ) 尿路感染 长效磺胺甲氧嘧啶(SMD) 少用 中效磺胺嘧啶(SD)和磺胺甲恶唑(SMZ) SD —首选预防、治疗流脑;诺卡菌引 起的肺部感染、脑膜炎、脑脓肿 SMZ —流脑预防。泌尿道、消化道和 呼吸道感染。与甲氧苄啶合用。 四、常用药物及临床应用四、常用药物及临床应用 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 2.2.肠道感染肠道感染 柳氮磺吡啶(sulfasalazine SASP) 分解产物可抗炎、抗菌、免疫抑制,治疗非 特异性结肠炎 3.3.外用药外用药 磺胺嘧啶银(SD-Ag)和磺胺米隆(SML) 抗菌活性不受脓液PABA的影响。用于烧伤、创伤 伴绿脓杆菌感染 磺胺醋酰(SA) 无刺激性、穿透力强,治疗眼 疾:沙眼、角膜炎、结膜炎。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 第三节第三节 其他合成类抗菌药其他合成类抗菌药 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 甲氧苄啶(甲氧苄啶(TMPTMP)) 特点:1、抗菌谱:与磺胺相似,较广 。抑菌药 2、机制:抑制二氢叶酸还原酶 与磺胺药或某些抗生素合用有增效作用 应用:与磺胺合用,不单用(易耐药) (1)呼吸道(2)流脑(3)泌尿道 (4)伤寒、霍乱 SMZco (SMZ:TMP为5:1)复方新诺明 二者主要药代学参数相近;双重阻断四氢叶酸合成 ,呈杀菌作用,抗菌谱扩大,并减少细菌耐药性产 生。 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 硝基呋喃类(抗菌谱广、作用强、不易耐 药、毒性大) 呋喃妥因呋喃妥因(呋喃坦啶,nitrofurantoin) 尿药浓度高,治疗泌尿道感染,酸性环境中 作用增强 呋喃唑酮呋喃唑酮(痢特灵,furazolidone) 口服不吸收,治疗肠炎、痢疾、霍乱等肠 道感染性疾病及抗幽门螺杆菌;栓剂可治 疗阴道滴虫病 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. 硝基咪唑类——甲硝唑、替硝唑、尼莫唑 甲硝唑(灭滴灵)甲硝唑(灭滴灵) 抗厌氧菌、破伤风梭菌、滴虫、阿米巴原 虫。 主要用于治疗厌氧菌感染。 幽门螺杆菌感染的消化性溃疡、艰难梭菌 所致的假膜性肠炎有特效。 与破伤风抗毒素合用治疗破伤风 Through this publicity campaign, further improve the sense of business integrity of tourism enterprises to help tourism consumers and operators to safeguard the legitimate rights and interests, to ensure that our City's tourism sustainable, healthy and coordinated Development. QUESTIONS 1.简述喹诺酮类抗菌作用机制及 应用。 2.简述磺胺类的不良反应。 3.试述复方新诺明的组成及复方 的理由。 4.甲硝唑首选适应症有哪些?
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