第二章 药代动力学
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">第二章 药代动力学</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic4.zhimg.com/80/v2-ecae69332aaf9e618ccb8cc84828859b_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">药理学:药动学+药效学</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">药动学(<span style="color: black;">药品</span>在<span style="color: black;">身体</span>的吸收 代谢 分布 排泄ADME; 血药浓度随时间的变化规律)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">代谢=生物转化</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"><span style="color: black;">第1</span>节: <span style="color: black;">药品</span>在<span style="color: black;">身体</span>的过程</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic2.zhimg.com/80/v2-24be372381b5af5291e132f1aedf6a6d_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">*肝脏——代谢; 肾脏——排泄</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">一。<span style="color: black;">药品</span>的跨膜转运</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic4.zhimg.com/80/v2-c836546fa69b2d77e9e59d5dbf1c0673_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">离子障: 解离性<span style="color: black;">药品</span>极性大,难以扩散;非解离性<span style="color: black;">药品</span>极性小,容易扩散</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">(离子障原理)→弱酸性<span style="color: black;">药品</span><span style="color: black;">重点</span>在胃中被吸收;弱碱性<span style="color: black;">药品</span><span style="color: black;">重点</span>在小肠中被吸收</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"> 神经垂体(垂体后叶)血管加压素(抗利尿激素)+催产素</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">腺垂体(垂体前叶):</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">二。影响<span style="color: black;">药品</span>通透细胞膜的<span style="color: black;">原因</span></p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"><span style="color: black;">药品</span>的吸收:<span style="color: black;">药品</span><span style="color: black;">经过</span>给药的部位进入血液循环的过程)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">首过消除:口服<span style="color: black;">药品</span>在胃肠道吸收后,<span style="color: black;">首要</span>要经过门静脉到 肝,再进入体循环。有些<span style="color: black;">药品</span>在<span style="color: black;">经过</span>肝脏时被部分代谢灭活, 进入体循环量减少</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">给药方式</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic3.zhimg.com/80/v2-56da62420b5e9a746165a9e89aa79b92_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">*治疗心绞痛(硝酸甘油片+速效救心丸(中药))</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">三。分布(<span style="color: black;">药品</span>经血液转运到组织器官的过程)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">影响<span style="color: black;">药品</span>分布的<span style="color: black;">原因</span></p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic1.zhimg.com/80/v2-3e1151275b68f6aa48df612134594cc4_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">*红细胞血红素→胆红素→决定胆汁的颜色</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">*基底神经核被胆红素沉积(核黄疸)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">四。代谢(生物转化)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">肝脏将<span style="color: black;">身体</span><span style="color: black;">药品</span>灭活,并转化为极性高的水溶性代谢物而利排出体外的过程。<span style="color: black;">药品</span><span style="color: black;">出现</span>化学结构和性质上的变化,<span style="color: black;">叫作</span>为生物转化(biotransformation</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">MFO=肝脏微粒体混合功能酶系统/肝药酶/单加氧酶</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"> <span style="color: black;">包含</span>(细胞色素P-450 ; 电子供体NADPH ; 电子传递<span style="color: black;">触及</span>的一种黄素蛋白)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">肝药酶特点: ①专一性低 ②活性有限 ③个体差异大 ④<span style="color: black;">能够</span>受到某些<span style="color: black;">药品</span>诱导</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">五。排泄(<span style="color: black;">药品</span>的原型或其代谢产物<span style="color: black;">经过</span>排泄器官排出体外的过程)</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic1.zhimg.com/80/v2-b5bfaa7045af77d604d95eb3c7047d80_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"> *促进尿酸排泄药——丙磺舒,苯溴马隆(竞争性<span style="color: black;">控制</span>肾小管对有机酸的转运,<span style="color: black;">控制</span>肾小管对尿酸的再吸收,<span style="color: black;">增多</span>尿酸排泄)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">第二节 <span style="color: black;">药品</span>代谢动力学基本概念</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"> <span style="color: black;">药品</span>:时量曲线(药量随时间变化的规律)</p>
<div style="color: black; text-align: left; margin-bottom: 10px;"><img src="https://pic4.zhimg.com/80/v2-e67476d0cd0cc5c3074367ae504fa8d7_720w.webp" style="width: 50%; margin-bottom: 20px;"></div>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;"><span style="color: black;">药品</span>有效血浓度=最低中毒浓度MTC-最低有效浓度MEC</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">生物利用度(F) 指血管外给药后<span style="color: black;">药品</span>被吸收进入体循环的相对数量和速度,</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">F=A/D*100% (A-进入体循环的药量; D-服药量)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">生物利用度的吸收程度=时量曲线下面积(area under curve AUC)单位为mg*h/L</p>相对生物利用度同一给药途径下<span style="color: black;">区别</span>制剂进行AUC比较绝对生物利用度静脉注射和血管外途径给药时的AUC值进行比较<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">二。房室模型(<span style="color: black;">一般</span>-二室模型)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">便于药动学分析的一个概念,假设人体<span style="color: black;">做为</span>一个系统,内分成若干房室</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">三。<span style="color: black;">药品</span>消除动力学</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">一级动力学消除(大部分<span style="color: black;">药品</span>符合此规律)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">消除速率与<span style="color: black;">药品</span>浓度<span style="color: black;">相关</span>,dc/dt=KC</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">恒比消除:单位时间内消除恒定比例的药量</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">半衰期恒定 T1/2=0.693/k</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">零级动力学消除(机体<span style="color: black;">处在</span>中毒状态,超过机体的消除能力)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">消除速率与药量或浓度<span style="color: black;">没</span>关dc/dt=k</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">恒量消除:单位时间消除恒量的药</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">半衰期不恒定</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">四。连续恒速给药</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">预测多次给药达到稳态血药水平,即css稳态浓度(<span style="color: black;">通常</span>4~5个t1/2<span style="color: black;">才可</span>达到)</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">负荷剂量:病情<span style="color: black;">严重</span><span style="color: black;">必须</span>立即达到有效血药浓度时,一<span style="color: black;">起始</span>就<span style="color: black;">能够</span>给与负荷剂量</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">(<span style="color: black;">药品</span>的特异性和<span style="color: black;">选取</span>性并不平行)阿托品M胆碱受体特异性的阻断剂,<span style="color: black;">然则</span><span style="color: black;">选取</span>性并不高</p>
<p style="font-size: 16px; color: black; line-height: 40px; text-align: left; margin-bottom: 15px;">这是我本科<span style="color: black;">时期</span>的笔记,觉得自己整理的还是很用心的,不拿出来怪可惜的 搬运到知乎上进行分享,药理学是我学的最开心的一门课之一,当然考前背诵还是很头秃的,<span style="color: black;">倘若</span>有任何问题欢迎留言~ <span style="color: black;">另一</span>,我学的是生物专业开设的药理学,跟医学专业的<span style="color: black;">需求</span>应该差别蛮大的。</p>
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