抗生素英文课件精品Antibiotics(70p)
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【医学精品课件之抗生素】Antibiotics
Classification (According to their mechanism of actions
1. Inhibit the biosynthesis of bacterial cell walls (β –Lactam) 2. React with cell membrances (Polymycin) 3. Disturber with the biosynthesis of protein (Aminoglycosides) 4. Inhibit the replication and transcription of nucleonic acidC H 3 S H 青霉胺
青霉醛
R N H S
N R
S
C O O H S
N
O
N
N
O O HC O O H
OHC O O H R
N
C O O H
青霉二胺
青霉酸
Semi- Synthetic Penicillins
O
HH
R C NH
S
N
O
H COOH
P ( 青 e n 霉 i c i 素 l l i n G G ) R =
"One sometimes finds what one is not looking for."
Because of its cheapness, efficacy, and remarkable lack of toxicity (except for acutely allergic patients). Peniciline G remains a remarkably useful agent for treatment of disease caused by susceptible microorganisms. It is the drug of choice for more infections than any other antibiotics. “ Fist is best”
抗生素(Antibiotics)ppt课件
• 抗病毒：抗原虫
• 抗结核分枝杆菌： 链霉素、环丝氨酸、利福霉素等。
根据化学结构分类
• β -内酰胺：青霉素类、头孢类、棒酸类、单环β -内酰胺类
• 四环素类：四环素、金霉素、强力霉素等。
• 氨糖类：卡那霉素、链霉素、庆大霉素、西素米星等 • 大环内酯类：红霉素、麦迪霉素、螺旋霉素等。 • 多烯大环类：制霉菌素、两性霉素B等。 • 聚醚多肽类：多肽菌素、放线菌素、杆菌肽等。 • 苯烃基胺类：氯霉素、甲砜霉素等。 • 蒽环类及其它：阿霉素、磷霉素、环丝氨酸等。
抗生素 (Antibiotics)
分类——不同的目的和需要
• 根据抗生素的生物来源
• 根据抗生素作用对象分类 • 根据抗生素化学结构分类 • 根据抗生素作用机制分类
根据抗生素的生物来源
• 细菌： 多肽类抗生素、多粘菌素、（短）杆菌肽。
•
•
真菌：
青霉素、头孢菌素、灰黄霉素。
放线菌： 数量多范围广，四环素类，大环内酯类，
• 细菌细胞膜渗透性的改变，或其他有关特性 如细菌菌膜（biofilm）的形成，使抗生素无 法进入胞内；
• 依赖于能量的主动转运（主动外排，active efflix）机制，即能够将已经进入胞内的药 物泵出胞外。
β -内酰胺类抗生素（β -Lactam Antibiotics）
定义——分子中含有β -内酰胺环的抗生素
耐药机制
1. -内酰胺酶的水解机制
2. -内酰胺酶的牵制机制
3. PBPs发生改变
4. 细菌细胞壁或外膜通透性改变
5. 细菌自溶酶减少
抗菌作用影响因素
1. 穿透屏障 2. 酶水解屏障 3. 和PBPs 的亲和力
一、青霉素类
抗生素 (英文PPT)ANTIBIOTICS
*Treatment of chronic adult periodontitis almost totally amenable to mechanical therapy.
*Administration instead of mechanical therapy for periodontitis.
✓ Unwanted effects ✓ Precautions ✓ Contraindications ✓ Patient’s point if view ✓ Patient
PATTERNS OF MISUSE
➢ They are used as “drugs of fear” to cover for potential errors of omission or commission & thereby prevent a claim of negligence.
PERIOD OF EMPIRICAL USE • Use of mouldy curd by chinese on boils •Chaulmoogra oil by hindus in leprosy •Chenopodium by aztecs for intestinal worms •Mercury by paracelsus for syphilis •Cinchona bark for fevers
•NON-EFFECTIVE CONDITIONS IN DENTISTRY
•NEWER ANTI-MICROBIAL APPROACHES
•MACROLIDES
•ANTIBIOMA
•MISCELLANEOUS ANTIBIOTICS
•ANTI FUNGALS &ANTI VIRAL DRUGS
*Administration instead of mechanical therapy for periodontitis.
✓ Unwanted effects ✓ Precautions ✓ Contraindications ✓ Patient’s point if view ✓ Patient
PATTERNS OF MISUSE
➢ They are used as “drugs of fear” to cover for potential errors of omission or commission & thereby prevent a claim of negligence.
PERIOD OF EMPIRICAL USE • Use of mouldy curd by chinese on boils •Chaulmoogra oil by hindus in leprosy •Chenopodium by aztecs for intestinal worms •Mercury by paracelsus for syphilis •Cinchona bark for fevers
•NON-EFFECTIVE CONDITIONS IN DENTISTRY
•NEWER ANTI-MICROBIAL APPROACHES
•MACROLIDES
•ANTIBIOMA
•MISCELLANEOUS ANTIBIOTICS
•ANTI FUNGALS &ANTI VIRAL DRUGS
抗生素概论(英文PPT)Review of Antibiotics
Relationship of Quinolone Structure to Adverse Events and Drug Interactions
R5 F
OO C OH
Affects: CNS toxicity through GABA
binding; NSAID and theophylline
Oxazine ring facilitates:
• Increased gram-negative coverage
• Increased half-life
Gatifloxacin
O
F
CO2H
N
N
O
HN
Ciprofloxacin
F
CH3 HN
N
N
OCH3
methoxy
CO2H
Quinolone Generations
interactions; genetic toxicity
R7 X8 N R1
Affects phototoxicity and
genetic toxicity
Adapted from Lipsky and Baker: Clin Infect Dis 28:352-364, 1999.
R2
Affects theophylline interactions and genetic toxicity; difluorophenyl at R1 may relate to hepatotoxicity
Resistant (N=476)
Gatifloxacin
0.5
0.5
0.5
Levofloxacin
2.0
2.0
抗生素PPT课件(英文精品) Antibiotics and Pain Control
– Fullen, et al.
• Both the timing and the choice are important.
– Thadepalli, et al.
What Bugs?
• Yom Kippur War
– Pseudomonas – 25.6% isolates – Gm Neg bacilli – 70% isolates overall
General Preventive Measures
• Adequate and Timely Resuscitation
• Early Wound Care • Antibiotics • Tetanus Immune Prophylaxis
Adequate and Timely Resuscitation
Why not?!
• Antibiotics not routinely given in the field by civilian pre-hospital personnel (EMT/paramedic model for
medic training).
• Combat medics don’t typically see wound infections during the time they care for them – may not appreciate their devastating effect.
• Debridement
– excise devitalized tissue
• Irrigation
– high pressure, solution
• Eliminate Dead Space
– fluid, blood
• Both the timing and the choice are important.
– Thadepalli, et al.
What Bugs?
• Yom Kippur War
– Pseudomonas – 25.6% isolates – Gm Neg bacilli – 70% isolates overall
General Preventive Measures
• Adequate and Timely Resuscitation
• Early Wound Care • Antibiotics • Tetanus Immune Prophylaxis
Adequate and Timely Resuscitation
Why not?!
• Antibiotics not routinely given in the field by civilian pre-hospital personnel (EMT/paramedic model for
medic training).
• Combat medics don’t typically see wound infections during the time they care for them – may not appreciate their devastating effect.
• Debridement
– excise devitalized tissue
• Irrigation
– high pressure, solution
• Eliminate Dead Space
– fluid, blood
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fluids
• levels of active drug sustained long enough to kill the invading agent
• Long “Shelf” life
10/21/2020
10
Still More Characteristics
• Low probability of resistance • Microbial drug resistance develops slowly • microbicidal rather than microbistatic • Not inactivated by organic material • Assists the host in eliminating the infecting
microbe • Not a powerful allergen
10/21/2020
11
Sources of Antibiotics
Most spore-forming microorganisms • Fungi
– Penicillium penicillin, – Cephalosporium griseofulvin • Bacteria – Bacillus bacitracin, polymyxin, tyrothricin,
– no adverse side reactions – non allergenic
• High toxicity for microbe
– bactericidal not bacteriostatic – broad spectrum
• Low risk of other infections
Sulfonamide Dihydropteroic acid
• 1928, Alexander Fleming
– antibacterial activity in Penicillium mold (called it Penicillin)
• 1938, Howard Florey and Ernst Chain
– developed Penicillin as an effective antibiotic
10/21/2020
7
Antimicrobial Therapy
• Antimicrobics – substances produced by microbes that inhibit other microbes
• Semi-synthetic antibiotics – naturally produced but altered
• Synthetic antibiotics: – derived from chemicals
10/21/2020
8
Ideal Properties of an Antibiotic
• Low toxicity for patient
– kills the invading microorganism without damaging the host
10/21/2020
Sulfa Drugs
14
Sulfa vs PABA
NH2SO2
NH2
Sulfanilamide
HOOC
NH2
PABA
10/21/2020
15
Structure of Sulfa Drugs
Sulfanilamide
Sulfisoxazole
Prontosil
10/21/2020
10/21/2020
9
More Characteristics
• drug can be administered orally or parenterally (by injection)
– Soluble in tissue fluids – absorbed by and dissolved in tissues or body
2 NADP+
Dihydrofolate synthetase
Tetrahydrofolic Acid
Thymidine DNA
Purines DNA, RNA
Methionine tRNa1, 0P/r2o1t/e2in02s0
17
Folic Acid Inhibition
PABA + pteridine
• Major Groups of antibiotics • Mechanisms of action
10/21/2020
3
History
• Salvarsan 606 • Prontosil • Penicillin
10/21/2020
4 10/21/2020
5 10/21/2020
6
Penicillin
colimycin, gramicidin – Streptomycetes Aminoglycosides, nystatin,
chloramphenicol, erythromycin, tetracylcine...
10/21/2020
12
Mechanisms of Drug Action
• inhibit cell wall synthesis • inhibit nucleic acid synthesis • inhibit protein synthesis • interfere with cell membrane function
1
Antibiotics
• Hugh B. Fackrell • Filename: antibiot.ppt
10/21/2020
2
Outline
• History • Ideal properties ห้องสมุดไป่ตู้ Sources • “Sulfas”
– Antimetabolites – antibiotic synergism
16
Folic Acid Metabolism
Sulfonamide
PABA + pteridine
[GTP]
Pteridine synthetase
Dihydropteroic acid
L- Glutamine
Dihydrofolate
Synthetase
Dihydrofolic Acid
2 NADPH Trimethoprim
• levels of active drug sustained long enough to kill the invading agent
• Long “Shelf” life
10/21/2020
10
Still More Characteristics
• Low probability of resistance • Microbial drug resistance develops slowly • microbicidal rather than microbistatic • Not inactivated by organic material • Assists the host in eliminating the infecting
microbe • Not a powerful allergen
10/21/2020
11
Sources of Antibiotics
Most spore-forming microorganisms • Fungi
– Penicillium penicillin, – Cephalosporium griseofulvin • Bacteria – Bacillus bacitracin, polymyxin, tyrothricin,
– no adverse side reactions – non allergenic
• High toxicity for microbe
– bactericidal not bacteriostatic – broad spectrum
• Low risk of other infections
Sulfonamide Dihydropteroic acid
• 1928, Alexander Fleming
– antibacterial activity in Penicillium mold (called it Penicillin)
• 1938, Howard Florey and Ernst Chain
– developed Penicillin as an effective antibiotic
10/21/2020
7
Antimicrobial Therapy
• Antimicrobics – substances produced by microbes that inhibit other microbes
• Semi-synthetic antibiotics – naturally produced but altered
• Synthetic antibiotics: – derived from chemicals
10/21/2020
8
Ideal Properties of an Antibiotic
• Low toxicity for patient
– kills the invading microorganism without damaging the host
10/21/2020
Sulfa Drugs
14
Sulfa vs PABA
NH2SO2
NH2
Sulfanilamide
HOOC
NH2
PABA
10/21/2020
15
Structure of Sulfa Drugs
Sulfanilamide
Sulfisoxazole
Prontosil
10/21/2020
10/21/2020
9
More Characteristics
• drug can be administered orally or parenterally (by injection)
– Soluble in tissue fluids – absorbed by and dissolved in tissues or body
2 NADP+
Dihydrofolate synthetase
Tetrahydrofolic Acid
Thymidine DNA
Purines DNA, RNA
Methionine tRNa1, 0P/r2o1t/e2in02s0
17
Folic Acid Inhibition
PABA + pteridine
• Major Groups of antibiotics • Mechanisms of action
10/21/2020
3
History
• Salvarsan 606 • Prontosil • Penicillin
10/21/2020
4 10/21/2020
5 10/21/2020
6
Penicillin
colimycin, gramicidin – Streptomycetes Aminoglycosides, nystatin,
chloramphenicol, erythromycin, tetracylcine...
10/21/2020
12
Mechanisms of Drug Action
• inhibit cell wall synthesis • inhibit nucleic acid synthesis • inhibit protein synthesis • interfere with cell membrane function
1
Antibiotics
• Hugh B. Fackrell • Filename: antibiot.ppt
10/21/2020
2
Outline
• History • Ideal properties ห้องสมุดไป่ตู้ Sources • “Sulfas”
– Antimetabolites – antibiotic synergism
16
Folic Acid Metabolism
Sulfonamide
PABA + pteridine
[GTP]
Pteridine synthetase
Dihydropteroic acid
L- Glutamine
Dihydrofolate
Synthetase
Dihydrofolic Acid
2 NADPH Trimethoprim