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What is the primary mechanism of action for beta-lactam antibiotics?
What is the primary mechanism of action for beta-lactam antibiotics?
Beta-lactam antibiotics inhibit cell wall synthesis.
Why are beta-lactam antibiotics considered bactericidal?
Why are beta-lactam antibiotics considered bactericidal?
They lead to bacterial lysis by damaging cell wall integrity.
Which types of bacteria lack activity against beta-lactam antibiotics?
Which types of bacteria lack activity against beta-lactam antibiotics?
Beta-lactam antibiotics lack activity against atypical organisms like Mycoplasma pneumoniae and Chlamydophila pneumoniae.
What role do Penicillin Binding Proteins (PBPs) play in bacterial cell wall synthesis?
What role do Penicillin Binding Proteins (PBPs) play in bacterial cell wall synthesis?
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Explain why beta-lactam antibiotics are classified as time-dependent killers.
Explain why beta-lactam antibiotics are classified as time-dependent killers.
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What happens to bacteria when beta-lactam antibiotics inhibit transpeptidase?
What happens to bacteria when beta-lactam antibiotics inhibit transpeptidase?
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What types of hypersensitivity reactions are associated with beta-lactam antibiotics?
What types of hypersensitivity reactions are associated with beta-lactam antibiotics?
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What additional mechanism enhances the lethality of beta-lactam antibiotics during bacterial multiplication?
What additional mechanism enhances the lethality of beta-lactam antibiotics during bacterial multiplication?
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What are the major allergic reactions associated with penicillin use?
What are the major allergic reactions associated with penicillin use?
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What role does the β-lactam ring play in penicillin allergies?
What role does the β-lactam ring play in penicillin allergies?
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What is the percentage of cross-allergy likelihood between penicillins and cephalosporins?
What is the percentage of cross-allergy likelihood between penicillins and cephalosporins?
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What non-allergic side effect is associated with broad-spectrum penicillins?
What non-allergic side effect is associated with broad-spectrum penicillins?
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Name a narrow spectrum penicillin used for treating infections caused by Streptococcus species.
Name a narrow spectrum penicillin used for treating infections caused by Streptococcus species.
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What may occur when penicillins are administered in extremely high plasma concentrations?
What may occur when penicillins are administered in extremely high plasma concentrations?
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Which types of penicillin are classified as broad spectrum?
Which types of penicillin are classified as broad spectrum?
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What is a potential risk of using high dose penicillins for longer than 10 days?
What is a potential risk of using high dose penicillins for longer than 10 days?
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What is the primary advantage of combining extended-spectrum penicillins with β-lactamase inhibitors?
What is the primary advantage of combining extended-spectrum penicillins with β-lactamase inhibitors?
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Name two examples of ureidopenicillins.
Name two examples of ureidopenicillins.
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Which bacteria are specifically mentioned as being more active against by extended-spectrum penicillins?
Which bacteria are specifically mentioned as being more active against by extended-spectrum penicillins?
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Identify one mechanism by which bacteria develop resistance to penicillins.
Identify one mechanism by which bacteria develop resistance to penicillins.
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What is a key characteristic of carbapenems compared to other beta-lactams?
What is a key characteristic of carbapenems compared to other beta-lactams?
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What are the roles of different beta-lactamases produced by bacteria like Staphylococcus aureus?
What are the roles of different beta-lactamases produced by bacteria like Staphylococcus aureus?
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List one narrow-spectrum penicillin and its primary use.
List one narrow-spectrum penicillin and its primary use.
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Which two gram-negative bacteria are mentioned as targets of treatment with penicillin combinations?
Which two gram-negative bacteria are mentioned as targets of treatment with penicillin combinations?
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What role do cross-linking and septum formation play in bacterial cell division?
What role do cross-linking and septum formation play in bacterial cell division?
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Why is penicillin more effective against Gram-positive bacteria?
Why is penicillin more effective against Gram-positive bacteria?
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Explain the barrier that the outer membrane of Gram-negative bacteria presents to antibiotics.
Explain the barrier that the outer membrane of Gram-negative bacteria presents to antibiotics.
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How do hydrophilic penicillins like Ampicillin and Amoxicillin demonstrate activity against Gram-negative bacteria?
How do hydrophilic penicillins like Ampicillin and Amoxicillin demonstrate activity against Gram-negative bacteria?
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What makes peptidoglycan a unique target for antibiotics like penicillin?
What makes peptidoglycan a unique target for antibiotics like penicillin?
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Discuss how natural resistance to penicillin occurs in some Gram-negative bacteria.
Discuss how natural resistance to penicillin occurs in some Gram-negative bacteria.
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What are the mechanisms of acquired resistance to penicillin?
What are the mechanisms of acquired resistance to penicillin?
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Name a few common organisms known to produce beta-lactamase.
Name a few common organisms known to produce beta-lactamase.
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What is the primary indication for Phenoxymethylpenicillin Potassium?
What is the primary indication for Phenoxymethylpenicillin Potassium?
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What is the advantage of using Benzathine benzylpenicillin G (BPG) in treatment?
What is the advantage of using Benzathine benzylpenicillin G (BPG) in treatment?
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For what type of infections are antistaphylococcal penicillins indicated?
For what type of infections are antistaphylococcal penicillins indicated?
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How do aminopenicillins like ampicillin and amoxicillin differ from natural penicillins?
How do aminopenicillins like ampicillin and amoxicillin differ from natural penicillins?
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What is a common vulnerability shared by aminopenicillins and natural penicillins?
What is a common vulnerability shared by aminopenicillins and natural penicillins?
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What is the recommended dosage of Benzathine benzylpenicillin G for treating β-hemolytic streptococcal pharyngitis?
What is the recommended dosage of Benzathine benzylpenicillin G for treating β-hemolytic streptococcal pharyngitis?
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Why might food interfere with the absorption of isoxazolyl penicillins?
Why might food interfere with the absorption of isoxazolyl penicillins?
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What structural modification increases the acid stability of amoxicillin compared to ampicillin?
What structural modification increases the acid stability of amoxicillin compared to ampicillin?
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Study Notes
Beta-Lactam Antibiotics
- Beta-lactam antibiotics inhibit cell wall synthesis in bacteria
- These antibiotics contain a beta-lactam ring in their structure.
- The major subdivisions of beta-lactam antibiotics are: penicillins, cephalosporins, carbapenems, and monobactams and beta-lactamase inhibitors.
Classification of Antibiotics
- Inhibitors of cell wall synthesis: Penicillins, Cephalosporins, Carbapenems, Monobactams, Glycopeptides
- Protein synthesis inhibitors acting on ribosomal subunits 30S: Aminoglycosides, Tetracyclines
- Protein synthesis inhibitors acting on ribosomal subunits 50S: Macrolides, Azalides, Chloramphenicols, Lincosamides
- Antibiotics which disturb functions of nucleic acids: Rifampicins
- Antibiotics which disturb structure and functions of cell membranes: Polyenes, Cyclic polypeptides (polymyxins)
Beta-Lactam Antibiotics (Inhibitors of Cell Wall Synthesis)
- Their structure contains a beta-lactam ring.
- Major subdivisions:
- Penicillins: Official names usually end in "cillin"
- Cephalosporins: Recognized by "cef" or "ceph" in their names
- Carbapenems (e.g., meropenem, imipenem):
- Monobactams (e.g., aztreonam):
- Beta-lactamase inhibitors (e.g., clavulanic acid, sulbactam):
Characteristics of Beta-Lactam Antibiotics
- All beta-lactams have the same mode of action (inhibit cell wall synthesis)
- Bactericidal (except against Enterococcus sp.)
- Time-dependent killers
- Cross-hypersensitivity
- Lack activity against atypical organisms (Mycoplasma pneumoniae, Chlamydophila pneumoniae)
- Lack activity against MRSA
Mechanism of Action (MOA)
- Bacteria lack osmotic regulating mechanisms; cell wall controls osmotic changes.
- The cell wall is composed of peptidoglycans.
- Cross-linked by peptide chains
- NAM-NAG (N-acetyl muramic acid and N-acetyl glucosamine)
- Cross-linked by a pentaglycine cross-bridge (extending from L-lysine to D-alanine)
- Transpeptidation reaction, cross-bridging
- Transpeptidase (PBPs): used for cross-linking; cross-linking provides stability and strength
- Beta-lactams inhibit transpeptidases, leading to damage of cross-linking, weakening of the cell wall, swelling due to endosmosis, bacterial membrane bursts, and bacterial lysis
- Additional mechanisms: activation of autolysins (murein hydrolase and autolysins); more lethal during active multiplication
Gram-Positive vs Gram-Negative Bacteria
- Gram-positive: Thick peptidoglycan layer, teichoic acid; peptidoglycan layer is easily accessible to beta-lactams.
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Gram-negative: Two membranes; thin peptidoglycan layer; lipopolysaccharides; porin channels act as a permeability barrier; hydrophilic penicillins (ampicillin, amoxicillin) can diffuse through these channels.
- Pseudomonas lacks porins, so ampicillin and amoxicillin are ineffective.
Resistance to Penicillins
- Natural: Target enzymes and PBPs are deep located, lipoproteins barrier in -ve, low affinity
- Acquired: Production of penicillinase/beta-lactamase enzyme, common organisms include Staph, Bacillus, Gonococci, E. coli, Enterococci and Haemophilus; loss or alteration of porin channels in gram-negative; modification of PBPs; activation of antibiotic efflux mechanisms.
Side Effects of Penicillins
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Allergic reactions: itching, rashes, fever, angioedema, anaphylaxis
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Allergies are less common with oral administration.
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Metabolic opening of beta-lactam ring creates a highly reactive penicilloyl group.
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Cross-allergy between penicillins and cephalosporins (maximum 10%).
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Carbapenems and monobactams have a lower risk of cross-reactivity.
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Intradermal test for allergy.
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Only ~10% of patients with a "penicillin allergy" respond positively.
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Non-allergic side effects: Diarrhea, neutropenia, anemia, thrombocytopenia, interstitial nephritis, convulsions, hepatic toxicity.
Classification of Penicillins:
- Narrow spectrum: Biosynthetic (natural), Anti-staphylococcal
- Broad spectrum: Aminopenicillins, Anti-pseudomonal, Carboxypenicillins, Ureidopenicillins
Beta-Lactamase Inhibitors
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Clavulanic acid
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Sulbactam
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Tazobactam
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Combination with beta-lactams extends activity against beta-lactamase-producing bacteria (S. aureus, E. coli, Pseudomonas, H. influenza).
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Description
This quiz explores beta-lactam antibiotics, focusing on their role in inhibiting cell wall synthesis in bacteria. It covers the major subdivisions, including penicillins, cephalosporins, and more. Additionally, the quiz examines various classifications of antibiotics based on their mechanisms of action.