抗生素抑制蛋白合成(英文PPT)Antibiotics That Inhibit Protein Synthesis
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抗生素处方(英文PPT)Antibiotic Prescribing
crosstransmission
resistance
SELECTION
dosage duration
BROAD-SPECTRUM EMPIRIC THERAPY
Adapted from: J. Carlet.
CONCERN
new antibiotics
(promotion from pharmaceutical
Surg) Tigecycline
Voriconazole
“Other” – Don’t put “registrar wants it!”
Write number on medication chart
Restricted antibiotic indications
See Sheet (available via AIR link) Note dosages Where in doubt, please contact ID Registrar, ID
Requires direct approval from Infectious Diseases:
Caspofungin Ciprofloxacin IV Flucytosine Linezolid Liposomal amphotericin Meropenem (except CF) Moxifloxacin Posaconazole Teicoplanin (except cardiac
Outer cell membrane disruption Inhibit protein synthesis (binding to ribosome)
Rapidly bactericidal: main value is as empiric agents (1 or 2 doses) for potential aerobic Gram negative sepsis
resistance
SELECTION
dosage duration
BROAD-SPECTRUM EMPIRIC THERAPY
Adapted from: J. Carlet.
CONCERN
new antibiotics
(promotion from pharmaceutical
Surg) Tigecycline
Voriconazole
“Other” – Don’t put “registrar wants it!”
Write number on medication chart
Restricted antibiotic indications
See Sheet (available via AIR link) Note dosages Where in doubt, please contact ID Registrar, ID
Requires direct approval from Infectious Diseases:
Caspofungin Ciprofloxacin IV Flucytosine Linezolid Liposomal amphotericin Meropenem (except CF) Moxifloxacin Posaconazole Teicoplanin (except cardiac
Outer cell membrane disruption Inhibit protein synthesis (binding to ribosome)
Rapidly bactericidal: main value is as empiric agents (1 or 2 doses) for potential aerobic Gram negative sepsis
抗生素英文课件精品ANTIBIOTICS(33p)
killed the bacteria that causes syphilis • Compound was called salvarsan but was
quite toxic to the host
Antibiotics
• Natural compounds produced by microorganisms that inhibit the growth of other microbes
class of antibiotics
Penicillin
• Wonder drug
• Killed bacteria with few side effects on the patient
• SELECTIVE TOXICITY
• Penicillin was NOT the first anti-bacterial compound
• Chloramphenicol, erythromycin (G+), streptomycin, tetracyclines
Injury to plasma membrane
• Changes to permeability of membrane causes loss of metabolites
ANTIBIOTICS
From the Greek: anti - against bios - life
Chemotherapy
• Paul Ehrlich • Use of chemical agent to kill bacteria and
not harm the host • Search for the “Magic bullet” • Developed an arsenic compound that
quite toxic to the host
Antibiotics
• Natural compounds produced by microorganisms that inhibit the growth of other microbes
class of antibiotics
Penicillin
• Wonder drug
• Killed bacteria with few side effects on the patient
• SELECTIVE TOXICITY
• Penicillin was NOT the first anti-bacterial compound
• Chloramphenicol, erythromycin (G+), streptomycin, tetracyclines
Injury to plasma membrane
• Changes to permeability of membrane causes loss of metabolites
ANTIBIOTICS
From the Greek: anti - against bios - life
Chemotherapy
• Paul Ehrlich • Use of chemical agent to kill bacteria and
not harm the host • Search for the “Magic bullet” • Developed an arsenic compound that
抗生素作用机制(英文PPT)Antibiotics that Inhibit Cell Wall S
1 They are the number most prescribed group of drugs.
Antibiotics and their Targets
DNA RNA Protein
Replication RNA Polymerase
Ribosome
Cell Wall Synthesis Proteins
Bacterial Cell Wall
Peptidoglycan wall = linear polymers alternating N-acglucosamine and N-ac-muramic acid, cross linked by short peptides. Three stages of synthesis: monomer synthesis, glycan chain formation, cross linking of peptidoglycan chains. ß-Lactams = penicillins and cephalosporins are most important Vancomycin = Blocks cell wall synthesis by other mechanisms and so helps handle resistance to ß-Lactams. Resistance = an alarming problem.
Cell wall
Lecture Plan
Bacterial Cell Wall Synthesis Inhibitors RNA Polymerase Inhibition DNA Replication Inhibitors Translation Inhibitors Metronidazole
Antibiotics and their Targets
DNA RNA Protein
Replication RNA Polymerase
Ribosome
Cell Wall Synthesis Proteins
Bacterial Cell Wall
Peptidoglycan wall = linear polymers alternating N-acglucosamine and N-ac-muramic acid, cross linked by short peptides. Three stages of synthesis: monomer synthesis, glycan chain formation, cross linking of peptidoglycan chains. ß-Lactams = penicillins and cephalosporins are most important Vancomycin = Blocks cell wall synthesis by other mechanisms and so helps handle resistance to ß-Lactams. Resistance = an alarming problem.
Cell wall
Lecture Plan
Bacterial Cell Wall Synthesis Inhibitors RNA Polymerase Inhibition DNA Replication Inhibitors Translation Inhibitors Metronidazole
抗生素英文课件精品—— Anti-bacteria Medicine
Selection of a potential product
1、efficacy 2、metabolic characterization 3、toxicity and adverse effect 4、Potentiality of industrial production
Antibiotics: from strain isolation to clinical application
! Rifampicin must be given by a “cocktail” of drugs.
Problem of antibiotics which inhibit
protein synthesis
Antibiotics: From isolation of strain to clinical application
Antibiotics and drugs targeting nucleic acid biosynthesis and functions
3. Rifampicin (from rifamycin) subunit of DNA-primed RNA polymease
Antibiotics and drugs targeting nucleic acid biosynthesis and functions
Mechanism of resistance
Selection pressure ( not only in health institutions)
Genetic recombination ( especially conjugation mediated by plasmid)
Improper prescription of antibiotics
1、efficacy 2、metabolic characterization 3、toxicity and adverse effect 4、Potentiality of industrial production
Antibiotics: from strain isolation to clinical application
! Rifampicin must be given by a “cocktail” of drugs.
Problem of antibiotics which inhibit
protein synthesis
Antibiotics: From isolation of strain to clinical application
Antibiotics and drugs targeting nucleic acid biosynthesis and functions
3. Rifampicin (from rifamycin) subunit of DNA-primed RNA polymease
Antibiotics and drugs targeting nucleic acid biosynthesis and functions
Mechanism of resistance
Selection pressure ( not only in health institutions)
Genetic recombination ( especially conjugation mediated by plasmid)
Improper prescription of antibiotics
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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• Also effective against mycoplasma, chlamydia, spirochetes.
TETRACYCLINES: Therapeutic Uses *
• Infectious diseases: - Rickettesial diseases (eg. Typhus fever) - Trachoma, urethritis, cervisitis - Brucellosis - Cholera - Pneumonia (M. pneumoniae) - Lyme disease -Anthrax
• The use of antacids is not advised when taking tetracycline
• Widely distributed. Poor CNS penetration
• Cross placenta and enter fetal circulation
• Elimination through liver and kidney
Precautions of tetracyclines
Tetracyclines should not be used in: Patients with renal impairment (except doxycycline,
minocycline). Pregnant or breast-feeding women. Children under 8 years old. Diarrhea (alert!!)
Other adverse effects include:
- Gastric discomfort: take with non-dairy food. - photoxicity: severe sunburn. - Vestibular problems (minocycline mainly): nausea, dizziness and
Antibiotics That Inhibit Protein Synthesis
Dr Khalid AlBalushi PHAR4010
Protein Synthesis Inhibitors
TETRACYCLINES
• Bind reversibly to the 30S ribosomal subunit and interferes with the attachment of tRNA with mRNA-ribosome complex.
AMINOGLYCOSIDES *
• Acne: topical or oral for severe acne vulgaris
• Peptic ulcer disease: H. pylori
• Periodontal disease: (doxycycline, minocycline)
Tetracyclve toxicity results from inability to cross mammalian cell membrane and they enter bacteria by energy-dependent transport system
• Broad-spectrum, bacteriostatic antibiotics [gm +ve, gm –ve].
renal renal
Long acting
Doxycycline minocycline
No change
hepatic
TETRACYCLINES: PK
• Food impairs the absorption of tetracyclines (not doxyclycline and minocycline) because they form insoluble chelates with calcium, magnesium, Aluminum and other metals.
TETRACYCLINES: resistance
• Reduced drug accumulation: - decrease uptake - increased efflux
• increased enzymatic drug inactivation: (rarest) • Decreased access to ribosomes: protective proteins
TETRACYCLINES: PK
Class
Drug
Effect on Food Route of on absorption Elimination
Short acting
Tetracycline
decrease
Oxytetracycline
Intermediate acting
demeclocycline decrease
TETRACYCLINES: resistance
Adverse effects of tetracyclines *
The major adverse effects of tetracyclines are discoloration of teeth and retardation of bone growth (not recommended for use in children and pregnant women).
vomiting. - Fatal hepatotoixty: very rare and occur in pregnant women receiving high doses of the drug (more likely with high dose IV administration, >2gm/day,). - suprainfections: overgrowth fungi, resistant staphylococci and C. difficile.
TETRACYCLINES: Therapeutic Uses *
• Infectious diseases: - Rickettesial diseases (eg. Typhus fever) - Trachoma, urethritis, cervisitis - Brucellosis - Cholera - Pneumonia (M. pneumoniae) - Lyme disease -Anthrax
• The use of antacids is not advised when taking tetracycline
• Widely distributed. Poor CNS penetration
• Cross placenta and enter fetal circulation
• Elimination through liver and kidney
Precautions of tetracyclines
Tetracyclines should not be used in: Patients with renal impairment (except doxycycline,
minocycline). Pregnant or breast-feeding women. Children under 8 years old. Diarrhea (alert!!)
Other adverse effects include:
- Gastric discomfort: take with non-dairy food. - photoxicity: severe sunburn. - Vestibular problems (minocycline mainly): nausea, dizziness and
Antibiotics That Inhibit Protein Synthesis
Dr Khalid AlBalushi PHAR4010
Protein Synthesis Inhibitors
TETRACYCLINES
• Bind reversibly to the 30S ribosomal subunit and interferes with the attachment of tRNA with mRNA-ribosome complex.
AMINOGLYCOSIDES *
• Acne: topical or oral for severe acne vulgaris
• Peptic ulcer disease: H. pylori
• Periodontal disease: (doxycycline, minocycline)
Tetracyclve toxicity results from inability to cross mammalian cell membrane and they enter bacteria by energy-dependent transport system
• Broad-spectrum, bacteriostatic antibiotics [gm +ve, gm –ve].
renal renal
Long acting
Doxycycline minocycline
No change
hepatic
TETRACYCLINES: PK
• Food impairs the absorption of tetracyclines (not doxyclycline and minocycline) because they form insoluble chelates with calcium, magnesium, Aluminum and other metals.
TETRACYCLINES: resistance
• Reduced drug accumulation: - decrease uptake - increased efflux
• increased enzymatic drug inactivation: (rarest) • Decreased access to ribosomes: protective proteins
TETRACYCLINES: PK
Class
Drug
Effect on Food Route of on absorption Elimination
Short acting
Tetracycline
decrease
Oxytetracycline
Intermediate acting
demeclocycline decrease
TETRACYCLINES: resistance
Adverse effects of tetracyclines *
The major adverse effects of tetracyclines are discoloration of teeth and retardation of bone growth (not recommended for use in children and pregnant women).
vomiting. - Fatal hepatotoixty: very rare and occur in pregnant women receiving high doses of the drug (more likely with high dose IV administration, >2gm/day,). - suprainfections: overgrowth fungi, resistant staphylococci and C. difficile.