Podcast
Questions and Answers
What structural feature distinguishes cephalosporins from penicillins?
What structural feature distinguishes cephalosporins from penicillins?
Which of the following best describes the mechanism of resistance for bacteria against cephalosporins?
Which of the following best describes the mechanism of resistance for bacteria against cephalosporins?
What characteristic is used to classify cephalosporins into different generations?
What characteristic is used to classify cephalosporins into different generations?
Which of the following bacterial species is generally considered resistant to cephalosporins?
Which of the following bacterial species is generally considered resistant to cephalosporins?
Signup and view all the answers
What effect does probenecid have on the pharmacokinetics of cephalosporins?
What effect does probenecid have on the pharmacokinetics of cephalosporins?
Signup and view all the answers
Which of the following infections is NOT typically treated with cephalosporins?
Which of the following infections is NOT typically treated with cephalosporins?
Signup and view all the answers
Besides gram-positive cocci, which of the following additional group of bacteria exhibits sensitivity to cephalosporins, according to the content?
Besides gram-positive cocci, which of the following additional group of bacteria exhibits sensitivity to cephalosporins, according to the content?
Signup and view all the answers
Which of the following statements correctly describes the route of excretion for most cephalosporins?
Which of the following statements correctly describes the route of excretion for most cephalosporins?
Signup and view all the answers
Which of the following best describes the primary use of first-generation cephalosporins?
Which of the following best describes the primary use of first-generation cephalosporins?
Signup and view all the answers
Which bacterial groups are generally NOT susceptible to first and second-generation cephalosporins?
Which bacterial groups are generally NOT susceptible to first and second-generation cephalosporins?
Signup and view all the answers
What is the main distinction of third-generation cephalosporins compared to first and second-generation drugs?
What is the main distinction of third-generation cephalosporins compared to first and second-generation drugs?
Signup and view all the answers
Which of the following second-generation cephalosporin has diminished use because of its high susceptibility to beta-lactamase?
Which of the following second-generation cephalosporin has diminished use because of its high susceptibility to beta-lactamase?
Signup and view all the answers
What is a key consideration when selecting a second-generation cephalosporin for a specific infection?
What is a key consideration when selecting a second-generation cephalosporin for a specific infection?
Signup and view all the answers
Which of the following organisms are classified as PEcK bacteria, targeted by first-generation cephalosporins?
Which of the following organisms are classified as PEcK bacteria, targeted by first-generation cephalosporins?
Signup and view all the answers
Which cephalosporin is considered the drug of choice for surgical prophylaxis?
Which cephalosporin is considered the drug of choice for surgical prophylaxis?
Signup and view all the answers
Why are second generation cephalosporins not recommended against Enterobacter?
Why are second generation cephalosporins not recommended against Enterobacter?
Signup and view all the answers
Which of the following third generation cephalosporins is primarily excreted through the biliary tract, requiring no dosage adjustment in cases of renal insufficiency?
Which of the following third generation cephalosporins is primarily excreted through the biliary tract, requiring no dosage adjustment in cases of renal insufficiency?
Signup and view all the answers
Which of the following best describes the mechanism of action for fosfomycin?
Which of the following best describes the mechanism of action for fosfomycin?
Signup and view all the answers
A patient presents with a severe cephalosporin allergy. According to the guidelines, which of these would be the recommended treatment for uncomplicated gonorrhea?
A patient presents with a severe cephalosporin allergy. According to the guidelines, which of these would be the recommended treatment for uncomplicated gonorrhea?
Signup and view all the answers
For which of the following infections is oral vancomycin the preferred treatment according to the text?
For which of the following infections is oral vancomycin the preferred treatment according to the text?
Signup and view all the answers
Which of the following is a characteristic of Cefditoren?
Which of the following is a characteristic of Cefditoren?
Signup and view all the answers
Which of these third generation cephalosporins exhibits activity against Bacteroides fragilis?
Which of these third generation cephalosporins exhibits activity against Bacteroides fragilis?
Signup and view all the answers
What is the primary mechanism of bacitracin's antibacterial action?
What is the primary mechanism of bacitracin's antibacterial action?
Signup and view all the answers
Which of the following is NOT a typical route of administration for aztreonam?
Which of the following is NOT a typical route of administration for aztreonam?
Signup and view all the answers
For the treatment of uncomplicated gonorrhea in a patient who cannot be administered ceftriaxone, which of the following is recommended?
For the treatment of uncomplicated gonorrhea in a patient who cannot be administered ceftriaxone, which of the following is recommended?
Signup and view all the answers
Which of these statements best describes the use of third generation cephalosporins regarding meningitis?
Which of these statements best describes the use of third generation cephalosporins regarding meningitis?
Signup and view all the answers
Which of the following best describes the role of clavulanic acid, sulbactam, and tazobactam?
Which of the following best describes the role of clavulanic acid, sulbactam, and tazobactam?
Signup and view all the answers
Which bacterial species is targeted by vancomycin with an oral administration?
Which bacterial species is targeted by vancomycin with an oral administration?
Signup and view all the answers
Which of the following third generation cephalosporins are recognized for their activity against P.aeruginosa?
Which of the following third generation cephalosporins are recognized for their activity against P.aeruginosa?
Signup and view all the answers
What is the primary concern associated with combining vancomycin with aminoglycosides?
What is the primary concern associated with combining vancomycin with aminoglycosides?
Signup and view all the answers
Why might third generation cephalosporins not be effective against certain Enterobacter infections?
Why might third generation cephalosporins not be effective against certain Enterobacter infections?
Signup and view all the answers
What is the proposed mechanism of action for vancomycin according to the text?
What is the proposed mechanism of action for vancomycin according to the text?
Signup and view all the answers
Which statement is NOT accurate regarding cycloserine?
Which statement is NOT accurate regarding cycloserine?
Signup and view all the answers
What is a key distinction in the mechanism of action between daptomycin and telavancin?
What is a key distinction in the mechanism of action between daptomycin and telavancin?
Signup and view all the answers
Why is daptomycin not suitable for the treatment of pneumonia?
Why is daptomycin not suitable for the treatment of pneumonia?
Signup and view all the answers
Which of the following is NOT a feature of telavancin?
Which of the following is NOT a feature of telavancin?
Signup and view all the answers
What does the content imply regarding the effectiveness of the drugs against resistant gram-positive bacteria?
What does the content imply regarding the effectiveness of the drugs against resistant gram-positive bacteria?
Signup and view all the answers
Which of the following best explains why bacitracin is primarily used topically?
Which of the following best explains why bacitracin is primarily used topically?
Signup and view all the answers
What is the primary mechanism of action of polymyxins against bacteria?
What is the primary mechanism of action of polymyxins against bacteria?
Signup and view all the answers
Why are polymyxins not a first-line treatment for systemic infections?
Why are polymyxins not a first-line treatment for systemic infections?
Signup and view all the answers
Cycloserine's mechanism of action involves the inhibition of which process?
Cycloserine's mechanism of action involves the inhibition of which process?
Signup and view all the answers
Which of the following statements is true regarding the use of polymyxins?
Which of the following statements is true regarding the use of polymyxins?
Signup and view all the answers
Which of the following is a key characteristic of Bacitracin?
Which of the following is a key characteristic of Bacitracin?
Signup and view all the answers
How does Cycloserine exert its antibacterial effect?
How does Cycloserine exert its antibacterial effect?
Signup and view all the answers
Which of the following is a typical combination for treating skin infections?
Which of the following is a typical combination for treating skin infections?
Signup and view all the answers
Flashcards
First-generation cephalosporins: What are they effective against?
First-generation cephalosporins: What are they effective against?
First-generation cephalosporins are effective against a range of gram-positive bacteria, including Staphylococcus aureus, and some gram-negative bacteria like Proteus, E. coli, and Klebsiella pneumoniae.
What bacteria are first-generation cephalosporins NOT effective against?
What bacteria are first-generation cephalosporins NOT effective against?
First-generation cephalosporins are generally not effective against enterococci or Pseudomonas aeruginosa.
Which first-generation cephalosporin is often used for surgical prophylaxis?
Which first-generation cephalosporin is often used for surgical prophylaxis?
Cefazolin is a first-generation cephalosporin that is often used for surgical prophylaxis due to its effectiveness against common surgical site infections.
How do second-generation cephalosporins differ from first-generation cephalosporins in terms of their activity?
How do second-generation cephalosporins differ from first-generation cephalosporins in terms of their activity?
Signup and view all the flashcards
What bacteria are second-generation cephalosporins NOT effective against?
What bacteria are second-generation cephalosporins NOT effective against?
Signup and view all the flashcards
What are the key features of third-generation cephalosporins?
What are the key features of third-generation cephalosporins?
Signup and view all the flashcards
Which second-generation cephalosporin is susceptible to beta-lactamase?
Which second-generation cephalosporin is susceptible to beta-lactamase?
Signup and view all the flashcards
What factors should guide the choice of a cephalosporin?
What factors should guide the choice of a cephalosporin?
Signup and view all the flashcards
What are cephalosporins?
What are cephalosporins?
Signup and view all the flashcards
How are cephalosporins classified?
How are cephalosporins classified?
Signup and view all the flashcards
What kind of bacteria are cephalosporins ineffective against?
What kind of bacteria are cephalosporins ineffective against?
Signup and view all the flashcards
How are cephalosporins administered?
How are cephalosporins administered?
Signup and view all the flashcards
How are cephalosporins eliminated?
How are cephalosporins eliminated?
Signup and view all the flashcards
What kind of bacteria are cephalosporins effective against?
What kind of bacteria are cephalosporins effective against?
Signup and view all the flashcards
What are some specific infections that cephalosporins are used for?
What are some specific infections that cephalosporins are used for?
Signup and view all the flashcards
What is the expanded spectrum activity of cephalosporins?
What is the expanded spectrum activity of cephalosporins?
Signup and view all the flashcards
Cefixime (Suprax)
Cefixime (Suprax)
Signup and view all the flashcards
Ceftriaxone (Rocephin)
Ceftriaxone (Rocephin)
Signup and view all the flashcards
Third Generation Cephalosporins
Third Generation Cephalosporins
Signup and view all the flashcards
Ceftazidime and Cefoperazone
Ceftazidime and Cefoperazone
Signup and view all the flashcards
Biliary Excretion of Ceftriaxone and Cefoperazone
Biliary Excretion of Ceftriaxone and Cefoperazone
Signup and view all the flashcards
CNS Penetration of Third Generation Cephalosporins
CNS Penetration of Third Generation Cephalosporins
Signup and view all the flashcards
Cefditoren (Spectracef)
Cefditoren (Spectracef)
Signup and view all the flashcards
Meningitis Caused by Resistant Pneumococci
Meningitis Caused by Resistant Pneumococci
Signup and view all the flashcards
Cycloserine
Cycloserine
Signup and view all the flashcards
Daptomycin
Daptomycin
Signup and view all the flashcards
Telavancin
Telavancin
Signup and view all the flashcards
What are the side effects of Cycloserine?
What are the side effects of Cycloserine?
Signup and view all the flashcards
Why is Daptomycin not used for treating pneumonia?
Why is Daptomycin not used for treating pneumonia?
Signup and view all the flashcards
Vancomycin
Vancomycin
Signup and view all the flashcards
Aztreonam
Aztreonam
Signup and view all the flashcards
Beta- Lactamase Inhibitors
Beta- Lactamase Inhibitors
Signup and view all the flashcards
Vancomycin's Mechanism of Action
Vancomycin's Mechanism of Action
Signup and view all the flashcards
Red Man Syndrome
Red Man Syndrome
Signup and view all the flashcards
Fosfomycin
Fosfomycin
Signup and view all the flashcards
Bacitracin
Bacitracin
Signup and view all the flashcards
Indications for Vancomycin
Indications for Vancomycin
Signup and view all the flashcards
Polymyxins
Polymyxins
Signup and view all the flashcards
Polymyxin B
Polymyxin B
Signup and view all the flashcards
Colistin (Polymyxin E)
Colistin (Polymyxin E)
Signup and view all the flashcards
Cycloserine's Mechanism of Action
Cycloserine's Mechanism of Action
Signup and view all the flashcards
Study Notes
Cell Wall Synthesis Inhibitors II
- Telavancin and daptomycin are included in this category.
Cephalosporins
- Structurally and functionally similar to penicillins, with variable R1 and R2 groups.
- Contain a 6-membered sulfur ring attached to a beta-lactam ring.
- Show high resistance to penicillinases (e.g., cephalosporinase).
- Classified into generations (first, second, third, fourth) based on bacterial susceptibility and resistance to beta-lactamases.
- Commonly ineffective against methicillin-resistant Staphylococcus aureus (MRSA), Listeria monocytogenes, Clostridium difficile, and Enterococci.
First-Generation Cephalosporins
- Examples include Cefazolin (Ancef, Kefzol), Cefadroxil (Duricef), Cephalexin (Keflex), Cephradine (Anspor, Velosef), Cephalothin (Keflin), and Cephapirin (Cefadyl).
- Substitute for penicillin G, resistant to staphylococcal penicillinase.
- Active against Proteus, E. coli, and Klebsiella pneumoniae (PEcK drugs).
- Not active against enterococci or Pseudomonas aeruginosa.
- Primarily excreted via glomerular filtration and tubular secretion.
- Cefazolin is the common parenteral first-generation cephalosporin in use.
- Alternative option for penicillin-allergic patients.
Second-Generation Cephalosporins
- Examples include Cefaclor (oral av. Ceclor), Cefamandole (Mandol), Cefmetazole (Zefazone), Cefprozil (oral av. Cefzil), Cefoxitin (Mefoxin), Cefonicid (Monocid), Cefotetan (Cefotan), Cefuroxime (oral av. Ceftin, Kefurox, Zinacef), and Loracarbef (oral av. Lorabid).
- Greater activity against gram-negative organisms (e.g., Haemophilus influenzae, Enterobacter aerogenes, Neisseria) as well as PEcK drugs.
- Not recommended for Enterobacter due to chromosome-mediated beta-lactamase.
- Not effective against Gram-positive organisms.
- Cefaclor's use is diminished due to high beta-lactamase susceptibility.
- IM injections may be painful.
Third-Generation Cephalosporins (Broad Spectrum)
- Examples include Cefdinir (Omnicef), Cefixime (Suprax), Cefoperazone (Cefobid), Cefotaxime (Claforan), Ceftazidime (Fortaz, Tazidime), Ceftizoxime (Cefizox), Ceftriaxone (Rocephin), Ceftibuten (Cedax), Cefditoren (Spectracef), and Cefpodoxime (Banan, Vantin).
- Increased gram-negative coverage and some ability to cross the blood-brain barrier.
- Ceftriaxone and Cefixime are first-line drugs against Neisseria gonorrhoeae.
- Cefoperazone and Ceftriaxone are excreted through the biliary tract, thus dosage adjustment isn't needed for renal insufficiency.
- These are helpful in treating meningitis as they have good CNS penetration.
Fourth-Generation Cephalosporins
- Cefepime (Maxipime) is a fourth-generation cephalosporin.
- Similar to third-generation drugs, but with more resistance to hydrolysis by chromosomal beta-lactamases produced by Enterobacter.
- High activity against Pseudomonas aeruginosa, Enterobacteriaceae, S. aureus, S. pneumoniae, and Hemophilus and Neisseria.
- Primarily renally eliminated, 100%.
Fifth or Advanced Generation Cephalosporins: Ceftaroline
- Ceftaroline (Teflaro) is a fifth-generation cephalosporin approved for treating complicated skin and skin structure infections and community-acquired pneumonia.
- Has extended activity against Gram-positive organisms and activity against Gram-negative organisms.
- Intravenous drug
- Effective against methicillin-resistant S. aureus (MRSA), vancomycin-resistant S. aureus (VRSA), vancomycin-insensitive S. aureus (VISA), and hetero-resistant vancomycin-insensitive S. aureus (hVISA).
Fifth or Advanced Generation Cephalosporins: Ceftobiprole
- Ceftobiprole medocaril (ZEVTERA) is a fifth-generation cephalosporin effective against Gram-positives and Gram-negatives.
- Administered by infusion.
- Useful in community-acquired pneumonia and nosocomial pneumonia, excluding ventilator-associated pneumonia.
Other Facts
- Available oral formulations: Cefadroxil, Cephalexin, Cephradine, Cefaclor, Cefprozil, Cefuroxime axetil, Cefdinir, Cefixime, Cefpodoxime, and Ceftibuten.
- Similar resistance mechanisms as penicillins.
- Similar elimination mechanisms as penicillins (with two exceptions).
Cephalosporin Adverse Effects
- Hypersensitivity (5% of patients)
- Cross-reactivity with penicillin allergies.
- Disulfiram-like reactions with methyl-thiotetrazole group cephalosporins and alcohol.
- Superinfections, renal damage, and local reactions (e.g., thrombophlebitis).
Carbapenems
- Synthesized from thienamycin.
- Imipenem is metabolized to potentially nephrotoxic compounds in the kidneys.
- Often combined with cilastatin to inhibit the dehydropeptidase enzyme.
- Imipenem/cilastatin (Primaxin) is a broad-spectrum antibiotic effective against gram-positive and gram-negative cocci (except methicillin-resistant S. aureus).
- Other carbapenems include meropenem, ertapenem, and doripenem.
Monobactams
- Aztreonam (Azactam) is a monobactam.
- Specifically targets gram-negative rods, such as Pseudomonas and Serratia.
- Little/no activity against Gram-positive cocci or anaerobic bacteria.
- Administered intravenously or intramuscularly.
Beta-Lactamase Inhibitors
- Clavulanic acid, Sulbactam, and Tazobactam inhibit beta-lactamases protecting penicillins.
Vancomycin
- Tricyclic glycopeptide used orally and parenterally.
- Effective against methicillin-resistant Staphylococcus aureus (MRSA) infections.
- Inhibits cell wall synthesis.
- Used to treat enterococcal and Clostridium difficile colitis.
- Possible side effects include "red man" syndrome, kidney damage, and allergy.
Fosfomycin
- Inhibits early stages of cell wall synthesis.
- Analogue of N-acetyl muramic acid.
- Effective against gram-positive and gram-negative organisms.
- Oral administration, 3g dose suitable in uncomplicated UTI's in women.
- Safe for use during pregnancy.
Bacitracin
- Mixture of polypeptides that inhibit cell wall synthesis.
- Active against Gram-positive cocci and bacilli, but typically used topically due to nephrotoxicity.
- Can be combined with other antibiotics like neomycin and polymyxin.
Polymyxins
- Peptides primarily used against gram-negative bacteria.
- Nephrotoxic and limited to topical or ophthalmic use.
- Effective against Pseudomonas and other gram-negative bacteria.
Cycloserine
- Water-soluble antibiotic useful for treating tuberculosis resistant to first-line drugs.
- Inhibits the enzymes involved in D-alanine synthesis which is essential in cell wall synthesis.
- Has adverse effects, such as neurotoxicity (headaches, tremors, psychosis, convulsions).
Daptomycin
- Bactericidal lipopeptide antibiotic.
- Disrupts cell membranes.
- Effective in complicated skin infections and bacteremia caused by S. aureus, including infective endocarditis.
- Inactivates in pulmonary tissue and not suitable for pneumonia.
Telavancin
- Lipoglycopeptide antibiotic similar in structure to vancomycin.
- Dual mechanism of action similar to daptomycin.
- Effective in complicated skin and skin-structure infections caused by MRSA, and in nosocomial and ventilator-associated bacterial pneumonia.
- Contraindicated in pregnancy due to renal impairment and anticoagulation test interference. Cardiac abnormalities may occur.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Test your knowledge on cephalosporins, their structural features, resistance mechanisms, and classifications. This quiz will cover various aspects, including their pharmacokinetics and treatment uses. Dive into the complexities of this important antibiotic class and challenge your understanding!