Cephalosporins: Structure and Classification
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Questions and Answers

What is the main difference between cephalosporins and penicillins?

  • Cephalosporins are more resistant to beta lactamase inactivation (correct)
  • Cephalosporins have a six-membered dihydrothiazine ring
  • Cephalosporins are more prone to hydrolytic degradation
  • Cephalosporins have a narrower spectrum of activity
  • Which generation of cephalosporins is active against E. coli, Klebsiella, and Proteus?

  • 1st Generation
  • 2nd Generation (correct)
  • 3rd Generation
  • All of the above
  • What is the primary use of 1st Generation cephalosporins?

  • Treat URTI, LRTI, sinusitis, and otitis media
  • Treat gram-negative infections
  • Treat skin and soft-tissue infections, as well as streptococcal pharyngitis (correct)
  • Treat anaerobic infections
  • What is the main advantage of 3rd Generation cephalosporins?

    <p>Better activity against gram-negative organisms</p> Signup and view all the answers

    Which of the following is a characteristic of cephalosporins?

    <p>They consist of a six-membered dihydrothiazine ring fused to a beta lactam ring</p> Signup and view all the answers

    What is the primary limitation of cephalosporins?

    <p>They are prone to hydrolytic degradation</p> Signup and view all the answers

    What is the mechanism of action of Aminoglycosides?

    <p>They inhibit bacterial protein synthesis by binding to the 30s subunit and blocking tRNA binding to the A site.</p> Signup and view all the answers

    Which of the following is NOT a use of Streptomycin?

    <p>Urinary tract infections</p> Signup and view all the answers

    What is a unique property of Meropenem?

    <p>It is resistant to dehydropeptidase enzyme.</p> Signup and view all the answers

    Which Aminoglycoside is most active among the Nebramycins?

    <p>Tobramycin</p> Signup and view all the answers

    What is a characteristic of Macrolides?

    <p>They contain a many-membered lactone ring.</p> Signup and view all the answers

    What is the mechanism of action of Ertapenem?

    <p>It inhibits bacterial cell wall formation.</p> Signup and view all the answers

    What happens when Azithromycin is administered with food?

    <p>Food has no significant effect on absorption</p> Signup and view all the answers

    Which antibiotic is a derivative of dichloroacetic acid?

    <p>Chloramphenicol</p> Signup and view all the answers

    Which antibiotic is a reversible inhibitor of CYP3A4 enzyme?

    <p>Telithromycin</p> Signup and view all the answers

    What is the mechanism of action of Clindamycin?

    <p>Binds exclusively to the 50S subunit of bacterial cell</p> Signup and view all the answers

    Which antibiotic is effective against macrolide-resistant G(+)?

    <p>Telithromycin</p> Signup and view all the answers

    What is the spectrum of activity of Clindamycin?

    <p>Bacteriostatic against S.epidermidis, S.aureus, M.pneumonia, and bactericidal against H.influenzae, N.meningitides, B</p> Signup and view all the answers

    What is the primary mechanism of action of Cephalosporins against bacteria?

    <p>Inhibition of cell wall formation</p> Signup and view all the answers

    What is the main adverse effect of Cephalosporins due to inhibition of Vitamin K?

    <p>Hypoprothrombinemia</p> Signup and view all the answers

    Which of the following bacteria is NOT typically treated with Aztreonam?

    <p>Staphylococcus aureus</p> Signup and view all the answers

    What is the main characteristic of Carbapenems?

    <p>Broad spectrum of activity</p> Signup and view all the answers

    What is the primary mechanism of action of Olivanic acids?

    <p>Inhibition of beta-lactamases</p> Signup and view all the answers

    What is the main characteristic of Imipenem?

    <p>High beta-lactamase resistance</p> Signup and view all the answers

    What is the mechanism of action of quinolones?

    <p>Inhibition of Topoisomerase IV and DNA gyrase enzymes</p> Signup and view all the answers

    Which of the following quinolones is NOT mentioned in the text?

    <p>Cinafloxacin</p> Signup and view all the answers

    What is the adverse effect of quinolones that is associated with Hepatotoxicity?

    <p>Trovafloxacin</p> Signup and view all the answers

    What type of organisms are Polypeptides effective against?

    <p>Bacteria</p> Signup and view all the answers

    What is the source of Polypeptides?

    <p>Bacillus and Streptomyces spp.</p> Signup and view all the answers

    What is the therapeutic use of quinolones mentioned in the text?

    <p>All of the above</p> Signup and view all the answers

    What is the unique property of 4th generation cephalosporins?

    <p>Increased stability to hydrolysis by inducible chromosomal β-lactamases</p> Signup and view all the answers

    What is the primary adverse effect of cephalosporins due to inhibition of Vitamin K?

    <p>Hypoprothrombinemia, leading to an increased tendency to bleed</p> Signup and view all the answers

    What is the mechanism of action of Aztreonam?

    <p>Inhibition of cell wall formation by binding to PBP3 in Gram-negative bacteria</p> Signup and view all the answers

    What is the characteristic of Carbapenems?

    <p>Fused β-lactam rings with a broad antimicrobial spectrum</p> Signup and view all the answers

    What is the source of Olivanic acids?

    <p>Streptomyces olivaceus</p> Signup and view all the answers

    What is the characteristic of Thienamycins?

    <p>Broad-spectrum antibiotic activity with high β-lactamase resistance</p> Signup and view all the answers

    What is the primary use of Aztreonam?

    <p>Treatment of Gram-negative bacterial infections, including UTI, LRTI, intra-abdominal infection, gynecological infection, and septicemia</p> Signup and view all the answers

    What is the primary characteristic of Monobactams?

    <p>Binding to PBP3 in Gram-negative bacteria</p> Signup and view all the answers

    Which type of organisms is Lledo effective against?

    <p>G(+) and nonspore forming anaerobes</p> Signup and view all the answers

    What is the mechanism of action of Quinolones?

    <p>Inhibition of Topoisomerase IV and DNA gyrase enzymes</p> Signup and view all the answers

    What is a common adverse effect of Quinolones?

    <p>GI disturbances</p> Signup and view all the answers

    Which of the following Quinolones is NOT mentioned in the text?

    <p>Clinafloxacin</p> Signup and view all the answers

    What is a therapeutic use of Quinolones mentioned in the text?

    <p>UTI</p> Signup and view all the answers

    What is the source of Polypeptides?

    <p>Bacillus and Streptomyces spp.</p> Signup and view all the answers

    What is a characteristic of Polypeptides?

    <p>Most powerful antibiotics</p> Signup and view all the answers

    What is an adverse effect of Quinolones associated with Tendon Rupture?

    <p>Tendon Rupture</p> Signup and view all the answers

    What is the primary site of action of Bacitracin?

    <p>Cell wall</p> Signup and view all the answers

    Which type of leprosy is associated with a malignant course?

    <p>Lepromatous leprosy</p> Signup and view all the answers

    What is the primary mechanism of action of Amphotericin B?

    <p>Interfering with cell membrane function</p> Signup and view all the answers

    What is the characteristic shape of Mycoplasma pneumoniae?

    <p>Pleomorphic</p> Signup and view all the answers

    What is the primary treatment for leprosy?

    <p>Dapsone</p> Signup and view all the answers

    What is the unique feature of Mycoplasma pneumoniae?

    <p>It lacks a peptidoglycan cell wall</p> Signup and view all the answers

    What is the primary source of Bacitracin?

    <p>Bacillus</p> Signup and view all the answers

    What is the term for the treatment of tuberculosis?

    <p>TB-DOTS</p> Signup and view all the answers

    Which antibiotic binds exclusively to the 50S subunit of bacterial cell?

    <p>Clindamycin</p> Signup and view all the answers

    What is the main advantage of Clindamycin over Lincomycin?

    <p>Improved absorption and distribution</p> Signup and view all the answers

    Which of the following antibiotics is a CYP3A4 inhibitor?

    <p>Telithromycin</p> Signup and view all the answers

    Which antibiotic is produced from Streptomyces venezuelae?

    <p>Chloramphenicol</p> Signup and view all the answers

    What is the primary use of Clindamycin?

    <p>Staph infections, cellulitis, and osteomyelitis</p> Signup and view all the answers

    Which antibiotic is not administered with food?

    <p>Clindamycin</p> Signup and view all the answers

    What is the spectrum of activity of Clindamycin?

    <p>Anaerobes, S.epidermidis, S.aureus, and others</p> Signup and view all the answers

    What is a unique chemical feature of Chloramphenicol?

    <p>Contains a nitrobenzene moiety</p> Signup and view all the answers

    What is the mechanism of action of Vancomycin?

    <p>Interferes with bacterial cell wall synthesis</p> Signup and view all the answers

    What is the primary route of administration for Vancomycin?

    <p>Intravenous</p> Signup and view all the answers

    Which of the following antibiotics is derived from Streptomyces orientalis?

    <p>Vancomycin</p> Signup and view all the answers

    What is the spectrum of activity of Polymyxin B and Colistin?

    <p>G(-) bacteria</p> Signup and view all the answers

    What is the mechanism of action of Mupirocin?

    <p>Reversibly binds to isoleucyl transfer-RNA synthetase</p> Signup and view all the answers

    What is the primary use of Mupirocin?

    <p>Topical use</p> Signup and view all the answers

    What is the adverse effect associated with Vancomycin's 'Red Man or Red Neck Syndrome'?

    <p>Decreased auditory acuity</p> Signup and view all the answers

    Which of the following antibiotics is derived from Pseudomonas fluorescens?

    <p>Mupirocin</p> Signup and view all the answers

    Study Notes

    Cephalosporins

    • Structure: consist of a six-membered dihydrothiazine ring fused to a beta lactam ring
    • Broad spectrum and resistant to beta lactamase inactivation
    • Classified into generations, each with its own spectrum of activity:
      • 1st Generation: excellent gram-positive and modest gram-negative activity, alternatives for skin and soft-tissue infections, and for streptococcal pharyngitis
      • 2nd Generation: better activity against gram-negative organisms with some gram-positive action, treats URTI, LRTI, sinusitis, and otitis media
      • 3rd Generation: activity against gram-positive organisms and much more activity against Enterobacteriaceae
      • 4th Generation: encompasses the antimicrobial spectrum of all the third-generation agents and has increased stability to hydrolysis by inducible chromosomal -lactamases

    Carbapenems

    • Comprise a family of fused beta lactam rings
    • Has broadest antimicrobial spectrum of any antibiotic
    • Analogues of penicillins or clavams, the sulfur or oxygen being replaced with carbon
    • Examples: Olivanic acids, Thienamycin, Imipenem, Meropenem, Ertapenem

    Aminoglycosides

    • Natural products or semi-synthetic derivatives of compounds produced by a variety of soil actinomycetes
    • Mechanism of Action: binds to 30s ribosomal subunit and interferes with initiation of protein synthesis
    • Examples: Streptomycin, Tobramycin, Neomycin, Spectinomycin, Netilmicin, Amikacin

    Macrolides

    • Contain a many-membered lactone ring (14-membered ring: Erythromycin and Clarithromycin, 15-membered ring: Azithromycin)
    • Basic in nature due to the presence of a glycosidically linked amino sugar
    • Spectrum of Activity: resembles that of Penicillin, used as an alternative to PCN
    • Examples: Erythromycin, Clarithromycin, Azithromycin

    Chloramphenicol

    • Produced from Streptomyces venezuelae
    • May cause blood dyscrasias
    • Contains a nitrobenzene moiety and is a derivative of dichloroacetic acid
    • Clindamycin: a congener of Lincomycin, improved absorption and distribution than Lincomycin

    Monobactams

    • Binds with PBP3 in gram-negative bacteria only
    • Treats UTI, LRTI, intra-abdominal infection, gynecological infection, and septicemia
    • Examples: Aztreonam

    Quinolones

    • Mechanism of Action: inhibition of Topoisomerase IV and DNA gyrase enzymes
    • Spectrum of Activity: specific agents with activity against Streptococci, active against Chlamydia, Mycoplasma, Legionella, Brucella, and Mycobacterium
    • Examples: Levofloxacin, Gatifloxacin, Moxifloxacin, Ofloxacin, Ciprofloxacin

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    Description

    This quiz covers the structure and classification of cephalosporins, a type of broad-spectrum antibiotic. Learn about their characteristics, generations, and uses in treating various infections.

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