Non-β-Lactam Antibiotics: Tetracyclines Overview
42 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which enzyme is responsible for O-adenylation?

  • Adenyl synthetase (correct)
  • Streptidine synthetase
  • Phosphoryl transferase
  • Glucosamine transferase

    • The primary functional group in aminoglycosides is a hydroxyl group.

    False

    What is the pharmacophoric unit mentioned in the content?

    1,3-Diamino inositol

    Adenyl synthetase makes __________.

    <p>O-adenylation</p> Signup and view all the answers

    Match the following compounds with their associated components:

    <p>Streptidine = An aminoglycoside component 2-deoxy streptamine = Building block in aminoglycosides N-methyl glucosamine = Variation in glucosamine structure Aminocyclitol = Core structure in many antibiotics</p> Signup and view all the answers

    What is one reason why tetracycline is not recommended for pregnant women?

    <p>It causes discoloration of teeth in the fetus.</p> Signup and view all the answers

    Outdated tetracycline can cause super infections in the intestine.

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

    What condition can arise from the overgrowth of Candida due to tetracycline use?

    <p>Vaginal infections</p> Signup and view all the answers

    Tetracycline causes __________ discoloration and hypoplasia of teeth in growing children.

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

    Match the following effects of tetracycline with their descriptions:

    <p>Discoloration of teeth = Caused by chelation with Ca2+ Renal damage = A risk of using outdated tetracycline Super infections = Overgrowth of Candida or resistant bacteria Photosensitive reactions = Allergic reactions to sunlight exposure</p> Signup and view all the answers

    What is the primary pharmacophore of the tetracycline group mentioned?

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

    Tetracycline is not recommended for children younger than 8 years due to possible tooth damage.

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

    What is a degradation product mentioned in the content?

    <p>4-epianhydrotetracyclines</p> Signup and view all the answers

    The 4-epianhydrotetracyclines are known to be beneficial for kidney health.

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

    At which pH range does epimerization occur?

    <p>pH 2-6</p> Signup and view all the answers

    The formation of _______ leads to an inactive configuration.

    <p>4-Epimertetracycline</p> Signup and view all the answers

    Match the compound with its characteristic:

    <p>4-epianhydrotetracyclines = Toxic to kidneys 4-Epimertetracycline = Inactive configuration Epimerization = Occurs between pH 2-6 Tetracyclines = Degradation product</p> Signup and view all the answers

    Which of the following statements about tetracyclines is true?

    <p>They can undergo epimerization.</p> Signup and view all the answers

    4-epianhydrotetracyclines are formed when tetracyclines lose their effectiveness.

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

    What configuration do 4-Epimertetracyclines have?

    <p>Beta configuration</p> Signup and view all the answers

    The chemical structure CH3 N(CH3)2 represents a compound with a _______ group.

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

    Which of the following antibiotics is a tetracycline analogue?

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

    Tigecycline is active against Pseudomonas infections.

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

    What mechanisms of resistance do tetracycline analogues overcome?

    <p>Acquired efflux pumps and ribosomal protection</p> Signup and view all the answers

    The prototype aminoglycoside antibiotic is __________.

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

    Match the following aminoglycosides with their characteristics:

    <p>Neomycin = Must not be given parenterally due to high toxicity Streptomycin = First used prototype of this class Aminoglycosides = Broad spectrum but limited use for severe G-ve infections</p> Signup and view all the answers

    Which of the following is NOT a characteristic of aminoglycosides?

    <p>Can be taken orally for systemic infections</p> Signup and view all the answers

    Aminoglycosides are effective against anaerobic bacteria.

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

    What is one major side effect associated with aminoglycosides?

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

    Due to their high toxicity, neomycin is used __________ or __________.

    <p>topically, orally</p> Signup and view all the answers

    Match the source with the aminoglycosides:

    <p>Streptomyces = Ends with suffix 'mycin' Micromonospora = Ends with suffix 'micin' Aminoglycosides = Obtained from microorganisms in soil</p> Signup and view all the answers

    What is the primary reason aminoglycosides are not absorbed from the gastrointestinal tract?

    <p>Their polar structure prevents absorption.</p> Signup and view all the answers

    Aminoglycosides can be mixed with β-lactam antibiotics in the same solution without any issue.

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

    What type of bacteria do aminoglycosides target?

    <p>Bacteria that synthesize proteins.</p> Signup and view all the answers

    Aminoglycosides exert a synergistic action with β-lactam antibiotics when given into different tissue ________.

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

    Match the following mechanisms with their descriptions:

    <p>Permeability defect = Outer membrane change prevents active transport into cell Lack of receptor = Lower binding affinity on the 30 S subunit R-factor enzymes = Enzymes that destroy drugs through acetylation</p> Signup and view all the answers

    Which of the following describes the action of aminoglycosides?

    <p>Inhibition of protein synthesis.</p> Signup and view all the answers

    Aminoglycosides can be excreted in urine in an inactive form after injection.

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

    What type of structure allows aminoglycosides to exist as polycations at physiological pH?

    <p>Strongly basic compounds</p> Signup and view all the answers

    The enzyme ________ is involved in acetylation of aminoglycosides, leading to drug inactivation.

    <p>Acetyl transferase</p> Signup and view all the answers

    What is required for aminoglycosides to effectively bind to the ribosome?

    <p>Presence of a specific receptor protein.</p> Signup and view all the answers

    Signup and view all the answers

    Study Notes

    Non-β-Lactam Antibiotics

    • Tetracyclines are obtained from fermentation procedures from Streptomyces species, natural sources.
    • Tetracyclines are bacteriostatic, highly lipophilic, and effective against Gram-positive and Gram-negative bacteria, Rickettsiae, Mycoplasma, Chlamydia and Cholera.
    • Tetracyclines are used to treat acute intestinal amoebiasis, malaria infections, and bacillary dysentery.
    • Appropriate tetracyclines are used to treat acne, promote inflammatory changes, and treat eye infections, pneumonia, and urinary tract infections.
    • Tetracyclines bind to the 30S ribosomal subunit of bacteria, blocking access of aminoacyl-tRNA to the acceptor site, inhibiting protein synthesis.
    • The mechanism of action involves forming a chelate compound with magnesium ions present at the binding site, blocking aminoacyl-tRNA from bringing another amino acid, which results in inhibition of protein synthesis.
    • Tetracyclines are strong metal-binders and remove essential metal ions as chelated compounds.
    • Adverse effects include gastric discomfort, deposition in bones and teeth during calcification in growing children, super infections, outdated tetracyclines can produce renal damage and photosensitivity.

    Aminoglycosides

    • Aminoglycosides are obtained from Streptomyces or Micromonospora.

    • Aminoglycosides are bactericidal against aerobic gram-negatives.

    • Aminoglycosides inhibit protein synthesis at the 30S ribosomal subunit.

    • Aminoglycosides have nephrotoxicity and ototoxicity.

    • Aminoglycosides include Tobramycin, Amikacin, Neomycin, Gentamicin, and Streptomycin.

    • Aminoglycosides have side effects such as neurotoxicity, allergic reactions, nephrotoxicity, and ototoxicity.

    • The properties of aminoglycosides are due to highly polar structure.

    • Aminoglycosides cannot be absorbed through the GIT due to their highly polar structure.

    • Aminoglycosides are excreted through the urine following injection.

    • Aminoglycosides are incompatible and must not be combined with other antibiotics in the same solution.

    • Aminoglycosides inhibit protein synthesis.

      • Binding to the 30S ribosomal subunit of bacteria.
      • Inhibiting initiation of protein synthesis.

    • Aminoglycosides show bacterial resistance:

      • Permeability defect by outer membrane change.
      • Lack of specific receptor on 30S subunit
        • Decreased affinity for binding sites of aminoglycosides. -Production of enzymes (R-factor enzymes) that destroy drugs.

    • Examples of enzymes are:

      • Acetyl transferase enzyme,
      • Phosphoryl transferase enzyme,
      • Adenyl synthetase enzyme.

    • Spectinomycin is the drug of choice for treating gonorrhea caused by penicillinase-producing N. gonorrhea.

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Medicinal Chemistry I PDF

    Description

    Explore the properties, uses, and mechanisms of tetracyclines, a critical subclass of non-β-lactam antibiotics. This quiz covers their bacteriostatic action, effectiveness against various bacteria, and clinical applications in treating infections. Test your knowledge on this important antibiotic class and its role in healthcare.

    More Like This

    Use Quizgecko on...
    Browser
    Open
    Browser
    Browser