抗生素药理学(英文PPT) Pharmacology of the Antibiotics
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抗生素PPT课件(英文精品) Chemotherapeutic Agents Antibiotics
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Chemotherapeutic Agents / Antibiotics, chapter 34-39
•Antibacterial compounds (procaryotes)
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Vorikonazol Flukonazol (Racemate)
M a c iIntratkoonaszol:h P I C T im a g e fo rm a t
is n o t s u p p o rte d
SAR: -Weakly basic azole ring, imidazol / 1,2,4-triazol (less tox. humans), pKa 6.5-6.8 -2 or 3 other aromatic rings -Cl (or F) on at least one aromatic ring (F i flukonazol) -Lipophilic structures (as lanosterol)
is n o t su p p o rted
Proad spectrum. Some effect on certain protozoa.
Isolated, Streptomyces sp.
M acintosh P IC T im age form at
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Chemotherapeutic Agents / Antibiotics, chapter 34-39
•Antibacterial compounds (procaryotes)
is not supported
M acintosh P IC T im age form at
is not supported
M acintosh P IC T im age form at
is not supported
M acintosh PICT im age form at
is not supported
Vorikonazol Flukonazol (Racemate)
M a c iIntratkoonaszol:h P I C T im a g e fo rm a t
is n o t s u p p o rte d
SAR: -Weakly basic azole ring, imidazol / 1,2,4-triazol (less tox. humans), pKa 6.5-6.8 -2 or 3 other aromatic rings -Cl (or F) on at least one aromatic ring (F i flukonazol) -Lipophilic structures (as lanosterol)
is n o t su p p o rted
Proad spectrum. Some effect on certain protozoa.
Isolated, Streptomyces sp.
抗生素英文课件精品——Introduction to Antibacterial Therapy
(1994 - 2000)
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Coagulase Negative Staph
Many species – S. epidermidis most common
Mostly methicillin resistant (65%) Often contaminants or colonizers – use
– Associated with carcinoma of colon
At PHD ~50% of SA are hetero (methicillin) resistant = MRSA
Glycopeptide (vancomycin) intermediate (GISA)
– MIC 8-16 – Eight nationwide (one at PHD)
VRSA reported July 5, 2002 MMWR
Gram Positive Cocci Gram Negative Rods Fastidious GNR Anaerobes
Gram Positive Cocci
Gram stain: clusters Catalase pos = Staph Coag pos = S aureus Coag neg = variety of
streptococci
Coagulase-
im a g e f o r m a t (1%)
negative staphylococci
i s n o t Candida s u p p o r t e d(32%)
(8%)
Enterococci (11%)
M acintosh P IC T im age form at
is not supported
Coagulase Negative Staph
Many species – S. epidermidis most common
Mostly methicillin resistant (65%) Often contaminants or colonizers – use
– Associated with carcinoma of colon
At PHD ~50% of SA are hetero (methicillin) resistant = MRSA
Glycopeptide (vancomycin) intermediate (GISA)
– MIC 8-16 – Eight nationwide (one at PHD)
VRSA reported July 5, 2002 MMWR
Gram Positive Cocci Gram Negative Rods Fastidious GNR Anaerobes
Gram Positive Cocci
Gram stain: clusters Catalase pos = Staph Coag pos = S aureus Coag neg = variety of
streptococci
Coagulase-
im a g e f o r m a t (1%)
negative staphylococci
i s n o t Candida s u p p o r t e d(32%)
(8%)
Enterococci (11%)
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ANTIBIOTICRESISTANTPATHOGENSIMPACTANDCONTROL104p
Systemic: Sepsis, bacteremia, endocarditis Organ system: Meningitis, osteomyelitis, septic arthritis, paratitis,
myositis
Evolution of Antimicrobial Resistance in Gram-positive Cocci
Deaths: 20,000
Source: Centers for Disease Control. MMWR 1997;46(RR-8)
% of Isolates Resistant to Penicillin
Trend for Penicillin-Resistant (MIC 2 mg/ml) S. pneumoniae in the US (1988-2002)
CHALLENGES IN THE PREVENTION AND MANAGEMENT OF HEALTHCARE-ASSOCIATED INFECTIONS
Changing population of hospital patients
Increased severity of illness Increased numbers of immunocompromised patients Shorter duration of hospitalization More and larger intensive care units
Pneumonia: 967 (46.9%) Other lower respiratory tract: 368 (17.8%) Urinary tract: 363 (17.6%) Bloodstream: 247 (12.0%)
myositis
Evolution of Antimicrobial Resistance in Gram-positive Cocci
Deaths: 20,000
Source: Centers for Disease Control. MMWR 1997;46(RR-8)
% of Isolates Resistant to Penicillin
Trend for Penicillin-Resistant (MIC 2 mg/ml) S. pneumoniae in the US (1988-2002)
CHALLENGES IN THE PREVENTION AND MANAGEMENT OF HEALTHCARE-ASSOCIATED INFECTIONS
Changing population of hospital patients
Increased severity of illness Increased numbers of immunocompromised patients Shorter duration of hospitalization More and larger intensive care units
Pneumonia: 967 (46.9%) Other lower respiratory tract: 368 (17.8%) Urinary tract: 363 (17.6%) Bloodstream: 247 (12.0%)
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Spectrum of Activity of Antiinfectives
Anti-infectives that interfere with the ability of the cell to reproduce/replicate without killing them are called BACTERIOSTATIC drugs.
- Bacteriodes gingivalis - B. intermedius - Fusobacterium nucleatum - Veillonella parvula - Actinomyces (naestundii, israelli, viscosus)
Localized Juvenile Periodontitis
1. Virulence of the microorganism 2. Number of the microorganism present 3. Resistance of the host
Potentially Periodontopathic Bacteria:
Adult peiodontitis
The early penicillin drugs are examples.
Spectrum of Activity of Anti-infectives
Broad-spectrum anti-infectives affect many bacteria.
Meropenem is an example. Because narrow spectrum antibiotics
Tetracycline is an example.
Spectrum of Activity of Antiinfectives
Antibiotics that can aggressively cause bacterial death are called BACTERICIDAL.
These properties (-cidal and –static) can also depend on the antibiotic concentration in the blood.
- Actinobacillus actinomycetemcomitans - Capnocytophaga sp.
Streptococcus mutans – causing dental
caries ( most common dental infection)
treatment of choice: local physical removal of microbial plaque on a regular basis( good oral hygiene)
(e.g. Erythromycin and Clindamycin may be bactericidal at higher blood levels)
Factors That Determine the Likehood Of a microorganism Causing an Infection:
Pharmacology of the Antibiotics
PAUL E. MANAIG,M.D.
General Mechanisms of Action of anti-infective agents
The mechanisms are: Inhibition the biosynthesis of
PROTEIN SYNTHESIS INHIBITORS
CELL WALL Permeability DNA SYNTHESIS INHIBITORS
penicillin, cephalosporin, vancomycin Macrolides, aminogylcosides Ketoconazole
Bacteriostatic Erythromycin, tetracyclines, clindamycin, chloramphenicol, spectinomycin, sulfonamides
Bactericidal - Penicillins, Cephalosphorins, Metronidazole, Aminoglycosides, Vancomycin, Polymyxin
Antimicrobial use in dentistry
Infection/Situation
Drug tal Disease ANUG (Vincent)
Penicillin V
Metronidazole Tetracycline
are selective, they are more active against single organisms than the
broad spectrum antibiotics.
Spectrum of Activity of Anti-infectives Anti-infective agents can also be:
Quinolones
Spectrum of Activity of Anti-infectives
Narrow spectrum
Broad-spectrum
Spectrum of Activity of Anti-infectives
Narrow spectrum anti-infectives affect only a few bacterial types
bacterial cell WALL Inhibition of protein synthesis Some change the cell membrane
permeability Some inhibit DNA synthesis
Examples
CELL WALL INHIBITORS