抗微生物药物(英文PPT)Antimicrobial Agents
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抗生素英文课件精品 Antimicrobial Agents
Str
Tet
Ery
Chl
Amp
Susceptibility vs. Resistance (cont.)
• Plasma concentration above 6-10 ug/ml may result in ototoxicity or nephrotoxicity
• Ration of toxic to therapeutic concentration is very low –agents difficult to use.
Susceptibility vs. Resistance of microorganisms to Antimicrobial Agents
• Success of therapeutic outcome depends on: • Achieving concentration of ATB at the site of
infection that is sufficient to inhibit bacterial growth. • Host defenses maximally effective –MI effect is sufficient – bacteriostatic agents (slow protein synthesis, prevent bacterial division) • Host defenses impaired- bactericidal agents • Complete ATB-mediated killing is necessary
Antimicrobial Agents
Martin Votava Olga Kroftová
Antibiotics
抗菌药(英文PPT)Antimicrobials
•G(+): either inducible or constitutive and are ofter plasmid mediated
(2) Change permeability of outer membrane (3) Altering their PBP
β-Lactams
Penicillin groups: penicillin ring Cephalosporin groups: cephalosporin ring Monobactams: Aztreonam Carbapenems: (1) Imipenem-Cilastatin (Tienam) (2) meropenem (Mepem)
Chapter Outline
◇ Learning objectives ◇ Antibacterial Antibiotics
• Mechanisms of action and resistance • Spectrum of coverage • Pharmacology and adverse effects
抗菌药（英文PPT）Antimicrobials
Learning Objectives
Recognize the different classes of antimicrobials and their mechanisms of action. Identify the spectrum of coverage for specific antimicrobials. Describe possible adverse effects and drug interactions caused by antimicrobials. Select appropriate antimicrobials for various pathogens.
(2) Change permeability of outer membrane (3) Altering their PBP
β-Lactams
Penicillin groups: penicillin ring Cephalosporin groups: cephalosporin ring Monobactams: Aztreonam Carbapenems: (1) Imipenem-Cilastatin (Tienam) (2) meropenem (Mepem)
Chapter Outline
◇ Learning objectives ◇ Antibacterial Antibiotics
• Mechanisms of action and resistance • Spectrum of coverage • Pharmacology and adverse effects
抗菌药（英文PPT）Antimicrobials
Learning Objectives
Recognize the different classes of antimicrobials and their mechanisms of action. Identify the spectrum of coverage for specific antimicrobials. Describe possible adverse effects and drug interactions caused by antimicrobials. Select appropriate antimicrobials for various pathogens.
细菌耐药性英文PPTAntimicrobial课件
Gentamicin
1967
1969
Vancomycin
1972
1987
Cefotaxime
1981
1981 (AmpC -lactamase)
1983 (ESBL)
Linezolid
2000
1999
一是作为领导干部一定要树立正确的 权力观 和科学 的发展 观，权 力必须 为职工 群众谋 利益， 绝不能 为个人 或少数 人谋取 私利
Antibiotics in the Sudan
CID 2003;37:1582
Nasopharyngeal swabs from outpatients in Sudan during the Civil War with no access to health care revealed:
- Strep pneumoniae - Strep pyogenes - H. influenzae
一是作为领导干部一定要树立正确的 权力观 和科学 的发展 观，权 力必须 为职工 群众谋 利益， 绝不能 为个人 或少数 人谋取 私利
Premise
If misuse of antibiotics causes drug resistance, the solution is to use antibiotics only when truly indicatric Tons
5 x 1016
3 x 108
Replicate 20-30 minutes
20-30 years
Microbiology in the 21st century: Where are we and where are we going? Washington, DC. American Society for Microbiology;2004.
抗微生物药物(英文PPT)Antimicrobial Drugs
– Gram-positives
• Binds 50S, prevents translocation
• Oxazolidinones
– Linezolid
• Gram-positives
– Binds 50S subunit, prevents formation of 70S ribosome
Figure 20.12
– Vancomycin
• Glycopeptide • Important "last line" against antibiotic resistant
S. aureus
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Antimycobacterial antibiotics
• 1928: Fleming discovered penicillin, produced by Penicillium.
• 1940: Howard Florey and Ernst Chain performed first clinical trials of penicillin.
Figure 20.1
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
Figure 20.8
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Cephalosporins
– 2nd, 3rd, and 4th generations more effective against gramnegatives
抗微生物药概论_PPT幻灯片
4、抗菌活性 是指抗菌药抑制或杀灭病原微生物 的能力。
最低抑菌浓度：能够抑制细菌生长的最低浓度
最低杀菌浓度：能够杀灭细菌的最低浓度
5、抗生素后效应：抗生素发挥抗菌作用后，血药 浓度低于最低抑菌浓度或被消除之后，细菌生长 仍受到持续抑制的效应。
二、抗菌药作用机制
1. 抑制细菌细胞壁的合成 2. 抑制菌体蛋白质合成 3. 影响细胞膜通透性 4. 影响核酸和叶酸代谢
① 病原体不明的严重感染 ② 单一药物不能有效控制混合感染 ③ 单一药物不能有效控制严重感染 ④ 结核
Thanks!
三、细菌耐药性
❖ 病原菌与抗菌药多次接触后，对抗菌药的敏 感性降低乃至消失的现象。
❖ 分为天然耐药性和获得性菌胞浆膜 改变靶蛋白对药物 的通透性 的亲和力
灭活酶产生
四、抗菌药的合理应用
1. 严格按适应症选药 2. 选用适当的剂量和疗程 3. 抗菌药的预防性应用 4. 抗菌药物的联合应用
抗菌药物概论 Introduction to antibacterial drugs
内容
一、基本概念 二、抗菌药作用机制
三、细菌耐药性 四、抗菌药合理应用
一、基本概念
抗微生物药：是一类能抑制或杀灭病原微生物的药物 化学治疗：指对体内微生物、寄生虫及癌细胞等所 致疾病的药物治疗。
机体
抗微生物药
抑制或杀灭 耐药性
病原微生物
1.抗生素 是指某些微生物（细菌、真菌、 放线菌等）在代谢过程中产生的具有抑制 或杀灭其它微生物作用的化学物质。
❖ 举例：青霉素、链霉素、氯霉素、土霉 素、四环素等。
3、抑菌药：是指仅有抑制微生物的生长繁殖而无 杀灭作用的药物。如红霉素。
杀菌药：不仅能抑制微生物生长繁殖，而且具有杀 灭作用的药物。如青霉素。
最低抑菌浓度：能够抑制细菌生长的最低浓度
最低杀菌浓度：能够杀灭细菌的最低浓度
5、抗生素后效应：抗生素发挥抗菌作用后，血药 浓度低于最低抑菌浓度或被消除之后，细菌生长 仍受到持续抑制的效应。
二、抗菌药作用机制
1. 抑制细菌细胞壁的合成 2. 抑制菌体蛋白质合成 3. 影响细胞膜通透性 4. 影响核酸和叶酸代谢
① 病原体不明的严重感染 ② 单一药物不能有效控制混合感染 ③ 单一药物不能有效控制严重感染 ④ 结核
Thanks!
三、细菌耐药性
❖ 病原菌与抗菌药多次接触后，对抗菌药的敏 感性降低乃至消失的现象。
❖ 分为天然耐药性和获得性菌胞浆膜 改变靶蛋白对药物 的通透性 的亲和力
灭活酶产生
四、抗菌药的合理应用
1. 严格按适应症选药 2. 选用适当的剂量和疗程 3. 抗菌药的预防性应用 4. 抗菌药物的联合应用
抗菌药物概论 Introduction to antibacterial drugs
内容
一、基本概念 二、抗菌药作用机制
三、细菌耐药性 四、抗菌药合理应用
一、基本概念
抗微生物药：是一类能抑制或杀灭病原微生物的药物 化学治疗：指对体内微生物、寄生虫及癌细胞等所 致疾病的药物治疗。
机体
抗微生物药
抑制或杀灭 耐药性
病原微生物
1.抗生素 是指某些微生物（细菌、真菌、 放线菌等）在代谢过程中产生的具有抑制 或杀灭其它微生物作用的化学物质。
❖ 举例：青霉素、链霉素、氯霉素、土霉 素、四环素等。
3、抑菌药：是指仅有抑制微生物的生长繁殖而无 杀灭作用的药物。如红霉素。
杀菌药：不仅能抑制微生物生长繁殖，而且具有杀 灭作用的药物。如青霉素。
抗微生物药物英文PPTAntimicrobial
Figure 20.9
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Polypeptide antibiotics
– Bacitracin
• Topical application • Against gram-positives
– Gram-positives
• Binds 50S, prevents translocation
• Oxazolidinones
– Linezolid
• Gram-positives
– Binds 50S subunit, prevents formation of 70S ribosome
Figure 20.12
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
Figure 20.8
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Cephalosporins
– 2nd, 3rd, and 4th generations more effective against gramnegatives
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B
– Topical – Combined with bacitracin and neomycin in
– Changes shape of 30S subunit
Antibacterial Antibiotics Inhibitors of Protein Synthesis
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Polypeptide antibiotics
– Bacitracin
• Topical application • Against gram-positives
– Gram-positives
• Binds 50S, prevents translocation
• Oxazolidinones
– Linezolid
• Gram-positives
– Binds 50S subunit, prevents formation of 70S ribosome
Figure 20.12
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
Figure 20.8
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Cephalosporins
– 2nd, 3rd, and 4th generations more effective against gramnegatives
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B
– Topical – Combined with bacitracin and neomycin in
– Changes shape of 30S subunit
Antibacterial Antibiotics Inhibitors of Protein Synthesis
--抗微生物药物(英文PPT)Antimicrobial_1
What is an Antibiotic?
• An antibiotic is a selective poison.
• It has been chosen so that it will kill the desired bacteria, but not the cells in your body. Each different type of antibiotic affects different bacteria in different ways.
• For example, an antibiotic might inhibit a bacteria's ability to turn glucose into energy, or the bacteria's ability to construct its cell wall. Therefore the bacteria dies instead of reproducing.
• In 1928, Sir Alexander Fleming, a Scottish biologist, observed that Penicillium notatum, a common mold, had destroyed staphylococcus bacteria in culture.
Susceptibility vs. Resistance of microorganisms to Antimicrobial Agents
• Success of therapeutic outcome depends on: • Achieving concentration of ATB at the site of
抗微生物药物PPT课件
三、细菌对抗菌药物的耐药性
No （一）耐药性（drug resistance）的概念
耐药性是指病原体或肿瘤细胞对反复应用 的化学治疗药物敏感性降低或消失的现象。
耐药性的分类： 固有耐药性：
Image 是由细菌染色体基因决定而代代相传的
耐药性，如肠道杆菌对青霉素的耐药； 获得耐药性：
大多由质粒介导，但亦可由染色体介导
抑制DNA、RNA的合成
如：喹诺酮类 —（-）DNA回旋酶 RFP —（-）依赖DNA的RNA多聚酶
4.抑制蛋白的合成
氨基苷类
蛋白质合成全过程抑制药
四环素类
30S 亚基抑制药
氯霉素
林可霉素类 50S 亚基抑制药
大环内酯类
︱
抑
制
细
菌
蛋 白
氨基苷类
氨基苷类
质
合
成
︱
氨基苷类
四环素类
大环内酯类
氯霉素类 林可霉素类
结构改变造成的耐药。 （2）增加靶蛋白数量 如：金葡菌对甲氧西林的耐药 （3）生成耐药靶蛋白 如：金葡菌产生青霉素结合蛋白PBP2A， 与β-内酰胺类抗生素亲和力极低导致耐药
3.降低细胞膜的通透性使药物不易进入菌体内 如：细菌对-内酰胺类、四环素的耐药
4.改变代谢途径 如：耐磺胺药的细菌自身产生PABA /直接利用叶酸转化为二氢叶酸
4.抗菌谱（antibacterial spectrum）：抗菌范围 窄谱：仅对单一菌种\单一菌属有抗菌作用 广谱：不仅对细菌有作用，而且对衣原体、 支原体、立克次体、螺旋体及原虫抑制作用。
5.抗菌活性（antibacterial activity）： 是指抗菌药抑制/杀灭细菌的能力。 抑菌药：仅抑菌的生繁而无杀灭作用的药物 杀菌药：既能抑菌,又能灭菌的药物
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• Limitation of in vitro tests • In vitro sensitivity tests are based on non-toxic
plasma concentrations –cut off • Do not reflect concentration at the site of infection • E.g.: G- aer.bacilli like Ps.aeruginosa inhibited by
Antimicrobial Agents
Martin Votava Olga Kroftová
Antibiotics
• Substances produced by various species of microorganisms: bacteria, fungi, actinomycetes- to suppress the growth of other microorganisms and to destroy them.
Susceptibility vs. Resistance of microorganisms to Antimicrobial Agents
• Success of therapeutic outcome depends on: • Achieving concentration of ATB at the site of
2 – 4 ug/ml of gentamycin or tobramycin. Susceptible !?
Antibiotic Susceptibility Testing
Determination of MIC
8
4
2ቤተ መጻሕፍቲ ባይዱ
1
0
Tetracycline (μg/ml)
MIC = 2 μg/ml
Disk Diffusion Test
• If can be achieved – microorganism susceptible to the ATB
• If effective concentration is higher than toxicmicroorganism is resistant
Susceptibility vs. Resistance (cont.)
infection that is sufficient to inhibit bacterial growth. • Host defenses maximally effective –MI effect is sufficient – bacteriostatic agents (slow protein synthesis, prevent bacterial division) • Host defenses impaired- bactericidal agents • Complete ATB-mediated killing is necessary
Sir Alexander Fleming
Fleming’s Petri Dish
Zone of Inhibition
• Around the fungal colony is a clear zone where no bacteria are growing
• Zone of inhibition due to the diffusion of a substance with antibiotic properties from the fungus
History
• Penicillin was isolated in 1939, and in 1944 Selman Waksman and Albert Schatz, American microbiologists, isolated streptomycin and a number of other antibiotics from Streptomyces griseus.
Susceptibility vs. Resistance (cont.)
• Dose of drug has to be sufficient to produce effect inhibit or kill the microorganism:
• However concentration of the drug must remain below those that are toxic to human cells –
Today the term ATB extends to include synthetic antibacterial agents: sulfonamides and quinolones.
History
• The German chemist Paul Ehrlich developed the idea of selective toxicity: that certain chemicals that would be toxic to some organisms, e.g., infectious bacteria, would be harmless to other organisms, e.g., humans.
• In 1928, Sir Alexander Fleming, a Scottish biologist, observed that Penicillium notatum, a common mold, had destroyed staphylococcus bacteria in culture.
Str
Tet
Ery
Chl
Amp
Susceptibility vs. Resistance (cont.)
• Plasma concentration above 6-10 ug/ml may result in ototoxicity or nephrotoxicity
• Ration of toxic to therapeutic concentration is very low –agents difficult to use.
plasma concentrations –cut off • Do not reflect concentration at the site of infection • E.g.: G- aer.bacilli like Ps.aeruginosa inhibited by
Antimicrobial Agents
Martin Votava Olga Kroftová
Antibiotics
• Substances produced by various species of microorganisms: bacteria, fungi, actinomycetes- to suppress the growth of other microorganisms and to destroy them.
Susceptibility vs. Resistance of microorganisms to Antimicrobial Agents
• Success of therapeutic outcome depends on: • Achieving concentration of ATB at the site of
2 – 4 ug/ml of gentamycin or tobramycin. Susceptible !?
Antibiotic Susceptibility Testing
Determination of MIC
8
4
2ቤተ መጻሕፍቲ ባይዱ
1
0
Tetracycline (μg/ml)
MIC = 2 μg/ml
Disk Diffusion Test
• If can be achieved – microorganism susceptible to the ATB
• If effective concentration is higher than toxicmicroorganism is resistant
Susceptibility vs. Resistance (cont.)
infection that is sufficient to inhibit bacterial growth. • Host defenses maximally effective –MI effect is sufficient – bacteriostatic agents (slow protein synthesis, prevent bacterial division) • Host defenses impaired- bactericidal agents • Complete ATB-mediated killing is necessary
Sir Alexander Fleming
Fleming’s Petri Dish
Zone of Inhibition
• Around the fungal colony is a clear zone where no bacteria are growing
• Zone of inhibition due to the diffusion of a substance with antibiotic properties from the fungus
History
• Penicillin was isolated in 1939, and in 1944 Selman Waksman and Albert Schatz, American microbiologists, isolated streptomycin and a number of other antibiotics from Streptomyces griseus.
Susceptibility vs. Resistance (cont.)
• Dose of drug has to be sufficient to produce effect inhibit or kill the microorganism:
• However concentration of the drug must remain below those that are toxic to human cells –
Today the term ATB extends to include synthetic antibacterial agents: sulfonamides and quinolones.
History
• The German chemist Paul Ehrlich developed the idea of selective toxicity: that certain chemicals that would be toxic to some organisms, e.g., infectious bacteria, would be harmless to other organisms, e.g., humans.
• In 1928, Sir Alexander Fleming, a Scottish biologist, observed that Penicillium notatum, a common mold, had destroyed staphylococcus bacteria in culture.
Str
Tet
Ery
Chl
Amp
Susceptibility vs. Resistance (cont.)
• Plasma concentration above 6-10 ug/ml may result in ototoxicity or nephrotoxicity
• Ration of toxic to therapeutic concentration is very low –agents difficult to use.