Nitroimidazoles Overview
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Questions and Answers

What are the routes of administration for Metronidazole?

  • Oral, IV Infusion, Vaginal Gel
  • Oral, IV Infusion
  • Oral
  • Oral, IV Infusion, Dental Gel, Rectal Suppository, Vaginal Gel (correct)

    • Which of the following is NOT primarily active against anaerobic bacteria?

  • Anaerobic bacteria
  • Aerobic bacteria (correct)
  • Helminth
  • Protozoa

    • Which of the following is a gram-positive anaerobic bacillus?

  • Bacteroides fragilis
  • Clostridium tetani (correct)
  • Helicobacter pylori
  • Fusobacterium

    • Nitroimidazoles have significant action against anaerobic gram-negative cocci.

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

    Nitroimidazoles have a significant action on aerobic gram-positive bacilli.

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

    Which of the following protozoa is sensitive to Nitroimidazoles?

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

    Nitroimidazoles have a significant action on Fungi.

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

    Nitroimidazoles have a significant action on Viruses.

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

    What is the mechanism of action for Metronidazole?

    <p>Metronidazole is a prodrug that requires activation by nitroreductases present in anaerobic bacteria. The activated form of metronidazole binds to DNA and fragments it, inhibiting protein synthesis.</p> Signup and view all the answers

    Tinidazole is more potent than Metronidazole.

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

    Tinidazole has a shorter half-life than Metronidazole.

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

    Which of the following is a common adverse drug effect of Metronidazole?

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

    Which of the following is a less frequent adverse drug effect of Metronidazole?

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

    Metronidazole can cause a disulfiram-like reaction when taken with alcohol.

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

    What is a special precaution to take when using Metronidazole?

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

    Metronidazole is the drug of choice for Amoebiasis.

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

    Metronidazole is the drug of choice for Trichomoniasis.

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

    Metronidazole is the drug of choice for Giardiasis.

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

    Metronidazole can be used to treat Pseudomembranous enterocolitis.

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

    Metronidazole is effective against Helicobacter pylori infections when used alone.

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

    Metronidazole can be used to treat Guinea worm infestation.

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

    Metronidazole is used to treat Antibiotic-associated diarrhea in pregnancy.

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

    Metronidazole can be used to relieve symptoms in Irritable Bowel Syndrome (IBS).

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

    Tinidazole has a long half-life.

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

    Tinidazole can be administered intravenously.

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

    Study Notes

    Nitroimidazoles

    • Nitroimidazoles are a group of drugs that include Metronidazole, Tinidazole, Ornidazole, Secnidazole, and Satranidazole.

    Routes of Administration

    • Metronidazole: Oral, IV infusion, dental gel, rectal suppository, vaginal gel
    • Tinidazole: Oral, IV infusion, vaginal gel
    • Ornidazole: Oral, IV infusion
    • Secnidazole: Oral
    • Satranidazole: Oral

    Antimicrobial Spectrum

    • Primarily active against anaerobic bacteria
    • Bacteria:
      • Anaerobic gram-positive bacilli (e.g., Clostridium tetani, Clostridium perfringens, Clostridium difficile, Clostridium septicum, Clostridium novyi, Clostridium histolyticum, Mobiluncus, Eubacterium)
      • Anaerobic gram-negative bacilli (e.g., Fusobacterium, Helicobacter pylori, Bacteroides fragilis, Prevotella)
      • Anaerobic gram-positive cocci (e.g., Peptococcus, Peptostreptococcus)
      • Anaerobic gram-negative cocci (no significant action)
    • Protozoa: Entamoeba histolytica, Giardia intestinalis, Trichomonas vaginalis, Balantidium coli, Blastocystis hominis
    • Helminth: Dracunculus medinensis (Guinea worm)
    • No significant action on: Fungi, Viruses

    Metronidazole Mechanism of Action

    • Pro drug requiring activation of the nitro group
    • Nitroreductase (enzyme) reduces ferredoxin and oxidizes ferredoxin
    • Active metabolite binds to DNA causing DNA fragmentation and inhibits protein synthesis

    Metronidazole Pharmacokinetics

    • Completely absorbed by the body
    • Widely distributed in saliva, semen, liver, vaginal fluids, CSF
    • High penetration across the breast milk and placenta
    • Gastrointestinal irritation can be minimized by taking with food

    Metronidazole Therapeutic Uses

    • Dental uses: Anaerobic oral infections (e.g., ANUG, cellulitis, pericoronitis, Vincent's stomatitis, periodontitis, acute apical infections, endodontic infections)
    • Aerobic and Facultative bacterial infections: Used with other antibiotics (penicillin, cephalosporins, aminoglycosides, or macrolides)
    • Other uses: Amoebiasis, Trichomoniasis, Giardiasis, anaerobic bacterial infections (intraabdominal, gynecologic, dermal, CNS, bones & joints, bacterial septicemia, and endocarditis), tetanus, mixed aerobic and anaerobic infections, pseudomembranous enterocolitis, Helicobacter pylori (triple drug regimen), Dracunculiasis (Guinea worm infestation), HIV seronegative eosinophilic pustular folliculitis, antibiotic-associated diarrhea in pregnancy, irritable bowel syndrome

    Tinidazole

    • Long half-life, single daily dose
    • Oral and IV infusion
    • More potent than metronidazole
    • More rapid cellular penetration and inhibition of DNA
    • Higher and persistent plasma concentrations

    Metronidazole Adverse Drug Effects

    • Common: Headache, nausea, dry mouth, metallic taste
    • Less frequent: Dizziness, vertigo, dark urine, stomatitis, paresthesias, furred tongue (due to candidiasis), neutropenia
    • Urticaria, flushing, pruritis
    • Prolonged treatment: Peripheral neuritis, seizures
    • Drug interactions: Disulfiram-like effects, decrease metabolism/excretion of drugs like warfarin, lithium, phenytoin, cyclosporin, and 5-fluorouracil
    • Special precaution: Mutagenicity, carcinogenicity, and teratogenicity in animal studies

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    Related Documents

    Nitroimidazoles: Pharmacology and Therapeutics PDF

    Description

    This quiz covers Nitroimidazoles, a group of drugs including Metronidazole and Tinidazole. It discusses their routes of administration, antimicrobial spectrum, and the types of bacteria and protozoa they target. Test your knowledge on these important medications!

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