Penicillins and Cephalosporins

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Questions and Answers

What is the reason for using Cefazolin in surgical prophylaxis?

  • Bile excretion
  • Good tissue and fluid penetration (correct)
  • Broad spectrum activity
  • Minimal allergic reactions

How is Ceftriaxone primarily excreted from the body?

  • Metabolism in the liver
  • Glomerular filtration
  • Bile excretion (correct)
  • Tubular secretion

What is the primary adverse reaction profile of cephalosporins compared to penicillins?

  • Neurotoxicity
  • Hepatotoxicity
  • Well-tolerated (correct)
  • High incidence of diarrhea

What is the cross-reactivity rate between penicillin and cephalosporins?

<p>3% to 5% (C)</p> Signup and view all the answers

Which organisms are covered by carbapenems?

<p>β-lactamase-producing G +ve and G –ve organisms, anaerobes, and P. aeruginosa (D)</p> Signup and view all the answers

Which carbapenem has coverage different from the others?

<p>Ertapenem (C)</p> Signup and view all the answers

What factors affect the selection of antimicrobial agents?

<p>Patient factors, safety and efficacy, and cost of therapy (A)</p> Signup and view all the answers

What are the properties influencing the frequency of dosing of antimicrobial agents?

<p>Concentration-dependent killing and time-dependent killing (B)</p> Signup and view all the answers

What are the chemotherapeutic spectra of antimicrobial drugs?

<p>Narrow-spectrum and extended/broad-spectrum (B)</p> Signup and view all the answers

What are the mechanisms of acquired resistance in drug-resistant organisms?

<p>Altered expression of proteins, modification of target sites, decreased accumulation, and enzymatic inactivation (D)</p> Signup and view all the answers

What can combinations of antimicrobial drugs lead to?

<p>Advantages such as synergism, but also disadvantages like risk of antibiotic resistance (D)</p> Signup and view all the answers

What can capillaries in certain tissues act as, impacting penetration and concentration of antimicrobial agents?

<p>Natural barriers to drug delivery (A)</p> Signup and view all the answers

What is the primary mechanism of action of penicillins?

<p>Interfering with the transpeptidation process (C)</p> Signup and view all the answers

Which type of penicillin is effective against Pseudomonas aeruginosa when combined with a β-lactamase inhibitor?

<p>Antipseudomonal penicillins (B)</p> Signup and view all the answers

What is a common cause of resistance to penicillins?

<p>β-lactamase production (B)</p> Signup and view all the answers

Which type of penicillin is used for treating infections caused by penicillinase-producing staphylococci?

<p>Antistaphylococcal penicillins (B)</p> Signup and view all the answers

What is the primary function of cell wall inhibitors as antimicrobial drugs?

<p>Interfere with bacterial cell wall synthesis (A)</p> Signup and view all the answers

What is the main advantage of semisynthetic penicillins like ampicillin and amoxicillin?

<p>Extended Gram-negative antimicrobial activity (C)</p> Signup and view all the answers

Which adverse reaction is associated with penicillins?

<p>Hypersensitivity (C)</p> Signup and view all the answers

Which cephalosporin can cross the blood-brain barrier?

<p>Cefuroxime sodium (C)</p> Signup and view all the answers

Which penicillin shows poor oral bioavailability?

<p>Penicillin V (A)</p> Signup and view all the answers

Which generation of cephalosporins is effective against Pseudomonas aeruginosa?

<p>Fourth-generation (C)</p> Signup and view all the answers

Which cephalosporin is used for treating meningitis and has good penetration into bone?

<p>Ceftriaxone (B)</p> Signup and view all the answers

Which body organ does penicillin have insufficient penetration into?

<p>Bone (B)</p> Signup and view all the answers

What are the topics covered in Pharmacology (3)?

<p>Antimicrobial Drugs, Anticancer Drugs, Thyroid Hormones, Estrogens and Androgens (D)</p> Signup and view all the answers

What is the principle behind antimicrobial therapy?

<p>Selective toxicity due to biochemical differences between microorganisms and human beings (C)</p> Signup and view all the answers

What factors are considered for selecting the most appropriate antimicrobial agent?

<p>The identity of the organism, the susceptibility of the organism to a particular agent, the site of infection (B)</p> Signup and view all the answers

What is the purpose of Gram stain and sample culture in antimicrobial therapy?

<p>To identify the organism causing the infection (B)</p> Signup and view all the answers

What does MIC stand for in the context of antimicrobial therapy?

<p>Minimum Inhibitory Concentration (A)</p> Signup and view all the answers

What is the significance of selective toxicity in antimicrobial therapy?

<p>It allows for targeting the microorganism without harming the host (B)</p> Signup and view all the answers

What is the primary route of excretion for Ceftriaxone?

<p>Biliary excretion (A)</p> Signup and view all the answers

What is the main reason for avoiding or using caution with 1st generation cephalosporins in individuals with penicillin allergy?

<p>Potential for cross-reactivity with penicillin (A)</p> Signup and view all the answers

Which cephalosporin is preferred for surgical prophylaxis due to its good tissue and fluid penetration and activity against penicillinase-producing S. aureus?

<p>Cefazolin (C)</p> Signup and view all the answers

What is the primary mechanism of action of carbapenems?

<p>Disruption of cell wall synthesis (B)</p> Signup and view all the answers

What is the primary adverse reaction profile of cephalosporins compared to penicillins?

<p>Greater likelihood of inducing anaphylactic shock (D)</p> Signup and view all the answers

How are carbapenems primarily eliminated from the body?

<p>Renal excretion (C)</p> Signup and view all the answers

Which penicillin has poor oral bioavailability?

<p>Penicillin V (B)</p> Signup and view all the answers

Which cephalosporin has the longest half-life?

<p>Ceftriaxone (D)</p> Signup and view all the answers

Which cephalosporin is active against MRSA?

<p>Ceftaroline (C)</p> Signup and view all the answers

Which cephalosporin has greater stability against beta-lactamases?

<p>Cefepime (C)</p> Signup and view all the answers

Which cephalosporin is effective in treating meningitis and has good penetration into bone?

<p>Ceftriaxone (B)</p> Signup and view all the answers

Which penicillin is primarily excreted through the kidneys?

<p>Penicillin V (C)</p> Signup and view all the answers

What influences the selection of the most appropriate antimicrobial agent?

<p>The identity of the organism (B)</p> Signup and view all the answers

What is the primary factor considered when selecting the most appropriate antimicrobial agent?

<p>The site of infection (A)</p> Signup and view all the answers

What is the significance of selective toxicity in antimicrobial therapy?

<p>It allows for preferential harm to the microorganism over the host (C)</p> Signup and view all the answers

What does MIC stand for in the context of antimicrobial therapy?

<p>Minimum Inhibitory Concentration (D)</p> Signup and view all the answers

What is the primary function of cell wall inhibitors as antimicrobial drugs?

<p>Disrupting the formation of the bacterial cell wall (B)</p> Signup and view all the answers

What can capillaries in certain tissues act as, impacting penetration and concentration of antimicrobial agents?

<p>A barrier to antimicrobial penetration (C)</p> Signup and view all the answers

Which type of penicillin has extended Gram-negative antimicrobial activity and is commonly used for respiratory infections?

<p>Ampicillin (D)</p> Signup and view all the answers

What is the primary reason for the increasing resistance of natural penicillins like penicillin G and penicillin V?

<p>β-lactamase production in many bacteria (B)</p> Signup and view all the answers

Which mechanism can lead to resistance to penicillins?

<p>Altered penicillin-binding proteins (C)</p> Signup and view all the answers

What is the primary mode of administration for penicillins?

<p>Intravenously (B)</p> Signup and view all the answers

Which type of penicillin is used to treat infections caused by penicillinase-producing staphylococci?

<p>Methicillin (A)</p> Signup and view all the answers

What is the primary target of cell wall inhibitors as antimicrobial drugs?

<p>Bacterial cell wall synthesis (B)</p> Signup and view all the answers

What factors affect the selection of antimicrobial agents?

<p>Patient factors, safety and efficacy, and cost of therapy (A)</p> Signup and view all the answers

What are the mechanisms of acquired resistance in drug-resistant organisms?

<p>Altered expression of proteins, modification of target sites, decreased accumulation, and enzymatic inactivation (A)</p> Signup and view all the answers

What is the primary function of cell wall inhibitors as antimicrobial drugs?

<p>Inhibit the synthesis of bacterial cell walls (D)</p> Signup and view all the answers

What can combinations of antimicrobial drugs lead to?

<p>Advantages such as synergism and disadvantages like risk of antibiotic resistance (D)</p> Signup and view all the answers

What is the significance of selective toxicity in antimicrobial therapy?

<p>It allows the drug to target the pathogen without harming the host (D)</p> Signup and view all the answers

What is the reason for using Cefazolin in surgical prophylaxis?

<p>It covers most skin flora and has a long half-life (A)</p> Signup and view all the answers

What is the primary factor considered when selecting the most appropriate antimicrobial agent?

<p>The identity of the organism (B)</p> Signup and view all the answers

What is the significance of selective toxicity in antimicrobial therapy?

<p>It ensures absolute toxicity to microorganisms only (B)</p> Signup and view all the answers

What is the primary route of excretion for Ceftriaxone?

<p>Bile (D)</p> Signup and view all the answers

What can capillaries in certain tissues act as, impacting penetration and concentration of antimicrobial agents?

<p>Barriers (D)</p> Signup and view all the answers

What is the reason for using Cefazolin in surgical prophylaxis?

<p>To prevent surgical site infections (D)</p> Signup and view all the answers

What are the topics covered in Pharmacology (3)?

<p>Antimicrobial Drugs, Anticancer Drugs, Thyroid Hormones, Estrogens and Androgens (A)</p> Signup and view all the answers

What is the primary reason for the increasing resistance of natural penicillins like penicillin G and penicillin V?

<p>Altered penicillin-binding proteins (B)</p> Signup and view all the answers

Which penicillin shows poor oral bioavailability?

<p>Penicillin G (C)</p> Signup and view all the answers

What is the primary route of excretion for Ceftriaxone?

<p>Biliary excretion (C)</p> Signup and view all the answers

Which body organ does penicillin have insufficient penetration into?

<p>Central nervous system (C)</p> Signup and view all the answers

What can capillaries in certain tissues act as, impacting penetration and concentration of antimicrobial agents?

<p>Selective barrier (A)</p> Signup and view all the answers

What is the primary mechanism of action of carbapenems?

<p>Inhibition of folic acid synthesis (D)</p> Signup and view all the answers

What are the two properties influencing the frequency of dosing of antimicrobial agents?

<p>Concentration-dependent killing and time-dependent killing (D)</p> Signup and view all the answers

What are the mechanisms of acquired resistance in drug-resistant organisms?

<p>Altered expression of proteins, modification of target sites, decreased accumulation (C)</p> Signup and view all the answers

What are the chemotherapeutic spectra of antimicrobial drugs?

<p>Narrow-spectrum and extended/broad-spectrum antimicrobial drugs (B)</p> Signup and view all the answers

What can combinations of antimicrobial drugs lead to?

<p>Advantages such as synergism, but also disadvantages like risk of antibiotic resistance (B)</p> Signup and view all the answers

What can capillaries in certain tissues act as, impacting penetration and concentration of antimicrobial agents?

<p>Natural barriers to drug delivery (C)</p> Signup and view all the answers

What is the primary cause of drug resistance in antimicrobial therapy?

<p>Acquired resistance through genetic alterations (D)</p> Signup and view all the answers

Which adverse reactions are associated with penicillins?

<p>Hypersensitivity and diarrhea (B)</p> Signup and view all the answers

Which cephalosporin is primarily used for treating complicated skin infections and community-acquired pneumonia?

<p>Ceftaroline (D)</p> Signup and view all the answers

What is the primary route of excretion for penicillins?

<p>Kidneys (D)</p> Signup and view all the answers

Which cephalosporin has the longest half-life among all cephalosporins?

<p>Ceftriaxone (B)</p> Signup and view all the answers

What is the main reason for avoiding or using caution with 1st generation cephalosporins in individuals with penicillin allergy?

<p>Cross-reactivity (C)</p> Signup and view all the answers

What is the primary mechanism of action shared by cephalosporins and penicillins?

<p>Disruption of cell wall synthesis (D)</p> Signup and view all the answers

What is the primary route of excretion for Ceftriaxone?

<p>Biliary excretion (C)</p> Signup and view all the answers

What is the highest rate of allergic cross-sensitivity between penicillin and 1st generation cephalosporins?

<p>5%-10% (C)</p> Signup and view all the answers

What is the primary mechanism of action of carbapenems?

<p>Inhibition of cell wall synthesis (A)</p> Signup and view all the answers

What is the primary adverse reaction profile of cephalosporins compared to penicillins?

<p>Higher incidence of allergic reactions (B)</p> Signup and view all the answers

Which cephalosporin is preferred for surgical prophylaxis due to its good tissue and fluid penetration and activity against penicillinase-producing S. aureus?

<p>Cefazolin (B)</p> Signup and view all the answers

Which carbapenem has coverage different from the others?

<p>Ertapenem (B)</p> Signup and view all the answers

Antimicrobial therapy takes advantage of the biochemical differences that exist between microorganisms and human beings resulting in absolute toxicity.

<p>False (B)</p> Signup and view all the answers

The selection of the most appropriate antimicrobial agent considers the identity of the organism, the susceptibility of the organism to a particular agent, and the site of infection.

<p>True (A)</p> Signup and view all the answers

Cefazolin is primarily used for treating complicated skin infections and community-acquired pneumonia.

<p>False (B)</p> Signup and view all the answers

Natural penicillins like penicillin G and penicillin V show increasing resistance.

<p>True (A)</p> Signup and view all the answers

Cell wall inhibitors are primarily targeting the ribosomes of microorganisms.

<p>False (B)</p> Signup and view all the answers

Ceftriaxone is primarily excreted through the kidneys.

<p>True (A)</p> Signup and view all the answers

Is Cefazolin preferred for surgical prophylaxis due to its good tissue and fluid penetration and activity against penicillinase-producing S. aureus?

<p>True (A)</p> Signup and view all the answers

Ceftriaxone is primarily excreted through the urine

<p>False (B)</p> Signup and view all the answers

The cross-reactivity rate between penicillin and cephalosporins is around 3% to 5%

<p>True (A)</p> Signup and view all the answers

Carbapenems have the same mechanism of action as penicillins

<p>True (A)</p> Signup and view all the answers

Carbapenems have a narrow spectrum of activity

<p>False (B)</p> Signup and view all the answers

Cephalosporins have a higher rate of allergic cross-sensitivity with 1st generation cephalosporins than with penicillin

<p>False (B)</p> Signup and view all the answers

Penicillins are primarily excreted through the liver.

<p>False (B)</p> Signup and view all the answers

Cephalosporins share the same mechanism of action as penicillins.

<p>True (A)</p> Signup and view all the answers

First-generation cephalosporins act on Gram-positive and some Gram-negative bacteria.

<p>True (A)</p> Signup and view all the answers

Third-generation cephalosporins like ceftriaxone have the longest half-life.

<p>True (A)</p> Signup and view all the answers

Ceftaroline is the only beta-lactam active against MRSA.

<p>True (A)</p> Signup and view all the answers

Cephalosporins are not effective in treating meningitis.

<p>False (B)</p> Signup and view all the answers

Capillaries in certain tissues act as natural barriers to drug delivery, impacting penetration and concentration of antimicrobial agents

<p>True (A)</p> Signup and view all the answers

Factors affecting selection of antimicrobial agents include patient factors, safety and efficacy, and cost of therapy

<p>True (A)</p> Signup and view all the answers

Concentration-dependent killing and time-dependent killing are properties influencing the frequency of dosing

<p>True (A)</p> Signup and view all the answers

Combinations of antimicrobial drugs have advantages such as synergism, but also disadvantages like risk of antibiotic resistance

<p>True (A)</p> Signup and view all the answers

Drug resistance can be caused by naturally inherent resistance or acquired resistance through genetic alterations

<p>True (A)</p> Signup and view all the answers

Altered expression of proteins in drug-resistant organisms cannot lead to drug resistance

<p>False (B)</p> Signup and view all the answers

Prophylactic use of antibiotics is necessary in all clinical situations to prevent infections.

<p>False (B)</p> Signup and view all the answers

Penicillins weaken the bacterial cell wall by interfering with the transpeptidation process, leading to cell death.

<p>True (A)</p> Signup and view all the answers

Resistance to penicillins can occur through β-lactamase production, decreased drug permeability, and altered penicillin-binding proteins.

<p>True (A)</p> Signup and view all the answers

Natural penicillins like penicillin G and penicillin V have a narrow spectrum and are not facing increasing resistance.

<p>False (B)</p> Signup and view all the answers

Semisynthetic penicillins such as ampicillin and amoxicillin have extended Gram-negative antimicrobial activity.

<p>True (A)</p> Signup and view all the answers

Antistaphylococcal penicillins like methicillin and nafcillin are used to treat infections caused by penicillinase-producing staphylococci.

<p>True (A)</p> Signup and view all the answers

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Study Notes

Cell Wall Inhibitors: Penicillins and Cephalosporins

  • Oral absorption of some penicillins is hindered by stomach acids, with penicillin V showing poor oral bioavailability and amoxicillin being readily absorbed from the GI tract.
  • Penicillins are distributed well throughout the body, but have insufficient penetration of bone, CSF, and the prostate, and no teratogenic effects when crossing the placental barrier.
  • Penicillins are primarily excreted through the kidneys, and nafcillin and oxacillin are metabolized in the liver.
  • Adverse reactions to penicillins include hypersensitivity, diarrhea, nephritis, neurotoxicity, and hematologic toxicities.
  • Cephalosporins share the same mechanism of action as penicillins and face resistance due to the hydrolysis of the beta-lactam ring by beta-lactamases.
  • The antibacterial spectrum of cephalosporins varies across different generations, with first-generation cephalosporins acting on Gram-positive and some Gram-negative bacteria, and showing resistance to staphylococcal penicillinase.
  • Second-generation cephalosporins like cefuroxime sodium have a longer half-life and can cross the blood-brain barrier, with cefoxitin showing greater activity on Gram-negative bacteria.
  • Third-generation cephalosporins like cefotaxime and ceftriaxone are effective in treating meningitis and have good penetration into bone, with ceftriaxone having the longest half-life of all cephalosporins.
  • Fourth-generation cephalosporins like cefepime are active against Pseudomonas aeruginosa and show greater stability against beta-lactamases.
  • Advanced generation cephalosporins like ceftaroline are the only beta-lactams active against MRSA and are used for treating complicated skin infections and community-acquired pneumonia.
  • Cephalosporins can be administered orally or parenterally and distribute well into body fluids, with ceftriaxone and cefotaxime being used for CSF infections and childhood meningitis.
  • Overall, both penicillins and cephalosporins have unique characteristics and varying antibacterial spectra, making them important in the treatment of bacterial infections.

Principles of Antimicrobial Therapy by Dr. Osama Abusara

  • Capillaries in certain tissues act as natural barriers to drug delivery, impacting penetration and concentration of antimicrobial agents
  • Factors affecting selection of antimicrobial agents include patient factors, safety and efficacy, and cost of therapy
  • Route of drug administration and rational dosing are determined based on pharmacodynamics and pharmacokinetics of antimicrobial agents
  • Concentration-dependent killing and time-dependent killing are properties influencing the frequency of dosing
  • Properties affecting dosing frequency include concentration-dependent killing, time-dependent killing, and postantibiotic effect
  • Chemotherapeutic spectra include narrow-spectrum and extended/broad-spectrum antimicrobial drugs
  • Combinations of antimicrobial drugs have advantages such as synergism, but also disadvantages like risk of antibiotic resistance
  • Drug resistance can be caused by naturally inherent resistance or acquired resistance through genetic alterations
  • Acquired resistance can result from altered expression of proteins, modification of target sites, decreased accumulation, and enzymatic inactivation
  • Altered expression of proteins in drug-resistant organisms can lead to drug resistance
  • Modification of target sites, decreased accumulation, and enzymatic inactivation are mechanisms of acquired resistance
  • Drug resistance can be caused by genetic alterations and altered expression of proteins in drug-resistant organisms

Cell Wall Inhibitors: Penicillins and Cephalosporins

  • Oral absorption of some penicillins is hindered by stomach acids, with penicillin V showing poor oral bioavailability and amoxicillin being readily absorbed from the GI tract.
  • Penicillins are distributed well throughout the body, but have insufficient penetration of bone, CSF, and the prostate, and no teratogenic effects when crossing the placental barrier.
  • Penicillins are primarily excreted through the kidneys, and nafcillin and oxacillin are metabolized in the liver.
  • Adverse reactions to penicillins include hypersensitivity, diarrhea, nephritis, neurotoxicity, and hematologic toxicities.
  • Cephalosporins share the same mechanism of action as penicillins and face resistance due to the hydrolysis of the beta-lactam ring by beta-lactamases.
  • The antibacterial spectrum of cephalosporins varies across different generations, with first-generation cephalosporins acting on Gram-positive and some Gram-negative bacteria, and showing resistance to staphylococcal penicillinase.
  • Second-generation cephalosporins like cefuroxime sodium have a longer half-life and can cross the blood-brain barrier, with cefoxitin showing greater activity on Gram-negative bacteria.
  • Third-generation cephalosporins like cefotaxime and ceftriaxone are effective in treating meningitis and have good penetration into bone, with ceftriaxone having the longest half-life of all cephalosporins.
  • Fourth-generation cephalosporins like cefepime are active against Pseudomonas aeruginosa and show greater stability against beta-lactamases.
  • Advanced generation cephalosporins like ceftaroline are the only beta-lactams active against MRSA and are used for treating complicated skin infections and community-acquired pneumonia.
  • Cephalosporins can be administered orally or parenterally and distribute well into body fluids, with ceftriaxone and cefotaxime being used for CSF infections and childhood meningitis.
  • Overall, both penicillins and cephalosporins have unique characteristics and varying antibacterial spectra, making them important in the treatment of bacterial infections.

Principles of Antimicrobial Therapy and Cell Wall Inhibitors

  • Prophylactic use of antibiotics is necessary in certain clinical situations to prevent infections when benefits outweigh potential risks.
  • Cell wall inhibitors are antimicrobial drugs that interfere with bacterial cell wall synthesis.
  • Penicillins, cephalosporins, carbapenems, monobactams, and β-lactam antibiotics are examples of cell wall inhibitors.
  • Penicillins weaken the cell wall by interfering with the transpeptidation process, leading to cell death.
  • Natural penicillins like penicillin G and penicillin V have a broad spectrum but are facing increasing resistance due to β-lactamases production in many bacteria.
  • Semisynthetic penicillins such as ampicillin and amoxicillin have extended Gram-negative antimicrobial activity and are used for respiratory infections.
  • Antistaphylococcal penicillins like methicillin and nafcillin are used to treat infections caused by penicillinase-producing staphylococci.
  • Antipseudomonal penicillins like piperacillin are effective against Pseudomonas aeruginosa when combined with a β-lactamase inhibitor.
  • Resistance to penicillins can occur through β-lactamase production, decreased drug permeability, and altered penicillin-binding proteins.
  • Penicillins can be administered orally or parenterally, with some forms having a long period of absorption.
  • Resistance to penicillins can also occur through decreased permeability to the drug and altered penicillin-binding proteins.
  • Penicillins are administered orally or parenterally, with some forms having a long period of absorption.

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