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Questions and Answers
Which statement accurately describes why penicillins and aminoglycosides cannot be administered simultaneously in the same IV fluid?
Which statement accurately describes why penicillins and aminoglycosides cannot be administered simultaneously in the same IV fluid?
Which of the following beta-lactam antibiotics is primarily administered orally due to its acid stability?
Which of the following beta-lactam antibiotics is primarily administered orally due to its acid stability?
Which of the following represents a mechanism of bacterial resistance to penicillins that does not involve beta-lactamase activity?
Which of the following represents a mechanism of bacterial resistance to penicillins that does not involve beta-lactamase activity?
Which of the following is a characteristic unique to piperacillin among the listed ureido-penicillins?
Which of the following is a characteristic unique to piperacillin among the listed ureido-penicillins?
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Which of the following is the primary role of beta-lactamase inhibitors when co-administered with penicillins?
Which of the following is the primary role of beta-lactamase inhibitors when co-administered with penicillins?
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Which statement regarding the use of carbenicillin in the US is correct?
Which statement regarding the use of carbenicillin in the US is correct?
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What is the primary purpose of using procaine penicillin G and benzathine penicillin G?
What is the primary purpose of using procaine penicillin G and benzathine penicillin G?
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A patient with a confirmed Pseudomonas infection requires intravenous antibiotic therapy. Based on information from the provided text, which antibiotic would be the most appropriate choice?
A patient with a confirmed Pseudomonas infection requires intravenous antibiotic therapy. Based on information from the provided text, which antibiotic would be the most appropriate choice?
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Which penicillin is specifically effective against aerobic gram positive bacilli, specifically Listeria?
Which penicillin is specifically effective against aerobic gram positive bacilli, specifically Listeria?
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Which of the following penicillins can be administered via all routes, including intravenous?
Which of the following penicillins can be administered via all routes, including intravenous?
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Ampicillin and Amoxicillin are classified as extended spectrum penicillins because they are effective against which type of bacteria?
Ampicillin and Amoxicillin are classified as extended spectrum penicillins because they are effective against which type of bacteria?
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What is a common method to protect penicillins from hydrolysis by beta-lactamases?
What is a common method to protect penicillins from hydrolysis by beta-lactamases?
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Which penicillin is known to cause neutropenia and phlebitis as common side effects?
Which penicillin is known to cause neutropenia and phlebitis as common side effects?
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For which specific setting are resistant strains of bacteria often susceptible to vancomycin?
For which specific setting are resistant strains of bacteria often susceptible to vancomycin?
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Which combination includes amoxicillin and a beta-lactamase inhibitor?
Which combination includes amoxicillin and a beta-lactamase inhibitor?
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Which of the following statements is true regarding dicloxacillin?
Which of the following statements is true regarding dicloxacillin?
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Which antibiotic class contains a structure characterized by a 4-membered ring attached to a thiazolidine ring?
Which antibiotic class contains a structure characterized by a 4-membered ring attached to a thiazolidine ring?
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Which of the following mechanisms do penicillins utilize to exert their antibacterial effects?
Which of the following mechanisms do penicillins utilize to exert their antibacterial effects?
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What characteristic feature distinguishes cephalosporins from penicillins?
What characteristic feature distinguishes cephalosporins from penicillins?
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Which of the following types of bacteria are expected to be resistant to beta-lactam antibiotics?
Which of the following types of bacteria are expected to be resistant to beta-lactam antibiotics?
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The extended spectrum penicillins are known to effectively target which type of bacteria?
The extended spectrum penicillins are known to effectively target which type of bacteria?
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In the process of bacterial cell wall disruption by penicillins, which of the following proteins do penicillins bind to?
In the process of bacterial cell wall disruption by penicillins, which of the following proteins do penicillins bind to?
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Which class of penicillins is primarily designed to combat staphylococcal infections?
Which class of penicillins is primarily designed to combat staphylococcal infections?
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Which of the following is NOT classified as an inhibitor of cell wall synthesis?
Which of the following is NOT classified as an inhibitor of cell wall synthesis?
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Flashcards
Carbenicillin
Carbenicillin
A type of penicillin effective against indole-positive Proteus and Pseudomonas.
Ticarcillin
Ticarcillin
A type of penicillin that is similar to Carbenicillin and also effective against indole-positive Proteus and Pseudomonas.
Piperacillin
Piperacillin
A type of penicillin that is active against Klebsiella pneumoniae and is considered the most potent penicillin.
Clavulanic acid
Clavulanic acid
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Beta-Lactamase Inhibitors
Beta-Lactamase Inhibitors
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Synergism
Synergism
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Resistance to Penicillins
Resistance to Penicillins
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Depot Penicillins
Depot Penicillins
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Beta-lactam antibiotics
Beta-lactam antibiotics
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Beta-lactam ring
Beta-lactam ring
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Cephalosporins
Cephalosporins
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Natural penicillins
Natural penicillins
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Antistaphylococcal penicillins
Antistaphylococcal penicillins
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Extended spectrum penicillins
Extended spectrum penicillins
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Mechanism of action of beta-lactam antibiotics
Mechanism of action of beta-lactam antibiotics
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Transpeptidases
Transpeptidases
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Anti-Pseudomonal Penicillins
Anti-Pseudomonal Penicillins
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Oxacillin: Acid Stability
Oxacillin: Acid Stability
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Nafcillin: Treatment of Serious Staphylococcal Infections
Nafcillin: Treatment of Serious Staphylococcal Infections
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Dicloxacillin: Resistance to Penicillinase
Dicloxacillin: Resistance to Penicillinase
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Ampicillin: Treatment of Listeria Infections
Ampicillin: Treatment of Listeria Infections
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Amoxicillin: Prophylactic Use in Heart Valve Patients
Amoxicillin: Prophylactic Use in Heart Valve Patients
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Study Notes
Antibacterial Cell Wall Synthesis and Disruption Drugs
- Beta-lactam antibiotics include Penicillins, Cephalosporins, Carbapenems, and Monobactams.
- Other inhibitors of cell wall synthesis and disrupting agents (non-beta-lactams) include Vancomycin, Bacitracin, Cycloserine, Polymyxins, Fosfomycin (Phosphonomycin), etc.
Beta-Lactam Antibiotics: Structure
- Beta-lactam antibiotics have a unique 4-membered ring (beta-lactam ring) attached to a thiazolidine ring.
- The beta-lactam ring has a secondary amino group (RNH).
- Substituents can be attached to the amino group.
- Cephalosporins are also beta-lactam antibiotics but have a 6-membered ring instead of a thiazolidine ring.
- R1 and R2 groups determine the antibiotic's therapeutic activity and toxicity.
Penicillin Classes
- Penicillins are divided into three classes:
- Natural penicillins (e.g., penicillin G)
- Gram-positive or antistaphylococcal penicillins (e.g., nafcillin)
- Extended-spectrum penicillins (e.g., ampicillin, amoxicillin, antipseudomonal penicillins)
Mechanism of Action (MOA)
- Penicillins inhibit the cross-linking step in bacterial cell wall synthesis.
- They bind to and inactivate transpeptidases, which are responsible for cross-linking linear glycopeptide strands.
- This action causes bacterial cell lysis and death, making penicillins bactericidal antibiotics.
- Penicillins require rapidly growing organisms with peptidoglycan cell walls for their action. Mycobacteria, fungi, protozoa, and viruses are not affected.
Mechanism of Action (detailed)
- Penicillins bind to penicillin-binding proteins (PBPs), enzymes involved in cell wall synthesis.
- Some PBPs are transpeptidases that cross-link cell wall chains.
- Binding prevents cross-linking.
- Gram-positive cocci have autolysins that aid in cell wall remodeling.
- Penicillins can activate autolysins, leading to cell lysis.
- Gram-positive bacteria easily absorb penicillins.
- Gram-negative bacteria require lipid-filled channels (porins) for penicillin entry.
Penicillin G
- Penicillin G (benzylpenicillin) is used for parenteral treatment of treponemal and clostridium infections.
- It has good activity against Gram-positive organisms.
- It is susceptible to beta-lactamases, unstable in acidic environments, and only 30% absorbed from the duodenum.
- Important drug of choice for gas gangrene (due to Clostridium perfringens).
- Also used in anthrax, actinomycosis, and listeria infections.
Antistaphylococcal Penicillins
- These are resistant to staphylococcal beta-lactamases.
- Effective against staphylococci and streptococci but not against enterococci, anaerobic bacteria, and gram-negative bacteria.
- Methicillin, Nafcillin, Oxacillin, Cloxacillin, and Dicloxacillin are examples.
Extended-Spectrum Penicillins (Ampicillin and Amoxicillin)
- These penicillins retain the spectrum of other penicillins and are effective against gram-negative bacteria but are destroyed by beta lactamases.
- Amoxicillin is orally administered and is often the drug of choice for gram-positive bacilli (e.g., Listeria).
- Used prophylactically in cases of abnormal heart valves and oral surgeries.
- Beta-lactamase inhibitors, like clavulanate, sulbactam, and tazobactam, are used to prevent their breakdown. (Examples: Augmentin, Unasyn, Zosyn).
Anti-pseudomonal Penicillins
- Carbenicillin, ticarcillin, piperacillin, azlocillin, and mezlocillin are effective against Pseudomonas aeruginosa but are sometimes called anti-pseudomonal penicillins.
- Azlocillin, Mezlocillin, and Piperacillin (ureido-penicillins) are more potent than other comparable drugs.
Beta-lactamase Inhibitors
- Clavulanic acid, sulbactam, and tazobactam inactivate beta-lactamases, protecting penicillins from breakdown.
Synergism
- Penicillins and aminoglycosides can work synergistically, but cannot be given in the same IV fluid due to opposite charges.
Causes of Resistance to Penicillins
- Impermeable cell walls lacking peptidoglycan.
- Plasmid or chromosomally mediated beta-lactamases.
- Decreased permeability, and altered penicillin-binding proteins (e.g., methicillin-resistant Staphylococcus).
Kinetics of Penicillins
- Administration routes vary, including intramuscular and oral.
- Penicillin G absorption can be affected by food.
- Some penicillins cross the placental barrier, some have a great oral absorption, and are primarily excreted thorough the kidneys.
- Probenecid can inhibit penicillin secretion by the kidneys.
Adverse Effects of Penicillins
- Hypersensitivity reactions (e.g., skin rashes, Steven-Johnson syndrome) are common, especially with penicilloic acid and ampicillin.
- Other adverse effects include diarrhea; potential interstitial nephritis, neurotoxicity; cation toxicity; Eosinophilia; serum sickness; angioedema; superinfections.
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Description
Test your knowledge on various antibacterial drugs targeting cell wall synthesis and disruption. This quiz covers beta-lactam antibiotics, their structures, and the classes of penicillins. Dive into the details of these essential medications and their mechanisms.