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

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

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

Which of the following protozoa is sensitive to Nitroimidazoles?

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

Nitroimidazoles have a significant action on Fungi.

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

Nitroimidazoles have a significant action on Viruses.

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

Tinidazole has a shorter half-life than Metronidazole.

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

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

<p>All of the above (E)</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 (H)</p> Signup and view all the answers

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

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

What is a special precaution to take when using Metronidazole?

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

Metronidazole is the drug of choice for Amoebiasis.

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

Metronidazole is the drug of choice for Trichomoniasis.

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

Metronidazole is the drug of choice for Giardiasis.

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

Metronidazole can be used to treat Pseudomembranous enterocolitis.

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

Metronidazole is effective against Helicobacter pylori infections when used alone.

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

Metronidazole can be used to treat Guinea worm infestation.

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

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

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

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

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

Tinidazole has a long half-life.

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

Tinidazole can be administered intravenously.

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

Flashcards

Nitroimidazoles

A group of drugs containing a nitroimidazole ring, effective against anaerobic bacteria and protozoa, and also show some activity against helminths.

Metronidazole

The most commonly used nitroimidazole drug, available in various forms for oral, intravenous, topical, and rectal administration.

Tinidazole

Another nitroimidazole drug similar to metronidazole, but with a longer half-life, requiring less frequent dosing.

Ornidazole

A nitroimidazole drug with oral and intravenous administration routes, known for its potent activity.

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Secnidazole

A nitroimidazole drug primarily for oral administration, commonly used for various infections.

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Satraconazole

A nitroimidazole drug available orally, known for its broad spectrum of activity.

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Antimicrobial Spectrum

The ability of a drug to inhibit the growth of or kill microorganisms.

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Anaerobic bacteria

Different bacterial groups that lack the ability to survive in the presence of oxygen.

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Aerobic bacteria

A group of bacteria that can survive in the presence or absence of oxygen.

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Protozoa

Single-celled eukaryotic organisms that are often invisible without a microscope, some of which cause infections.

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Helminth

Multicellular parasitic worms that can infect humans and animals.

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Hormone

A specific molecule produced by an organism that acts as a signaling molecule.

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Pharmacokinetics

The process by which a drug is absorbed, distributed, metabolized, and eliminated from the body.

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Pharmacology

The study of how drugs interact with living organisms, focusing on their effects and mechanisms of action.

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Mechanism of action

The specific way that a drug interacts with its target to produce its effects.

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Prodrug

A drug that is inactive in its original form and must be metabolized in the body to become active.

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Metabolism

The process by which a drug is broken down into smaller molecules in the body.

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Adverse drug effect

An unwanted or harmful effect that occurs during drug use.

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Drug interaction

A situation where two or more drugs interact within the body, potentially changing their effects.

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Hypersensitivity

A condition where an individual develops excessive sensitivity to a drug, leading to exaggerated or unexpected reactions.

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Cellular penetration

The ability of a drug to pass through biological barriers, such as cell membranes, to reach its target site.

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Plasma concentration

The concentration of a drug in the blood or other bodily fluids.

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Half-life

The length of time it takes for the concentration of a drug in the body to decrease by half.

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Blood brain barrier penetration

The ability of a drug to pass through the barrier between the bloodstream and the central nervous system.

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Intravenous infusion

When a drug is administered directly into the bloodstream.

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Infected site

An area of the body that is inflamed or infected.

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Periodontitis

A condition involving inflammation of the gums, typically caused by various bacteria.

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CNS infections

A condition affecting the brain where bacteria or other pathogens have invaded the brain tissue.

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Candida infection

A condition characterized by an excessive growth of the Candida fungus, often causing oral thrush.

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Pseudomembranous colitis

A severe complication of diarrhea caused by an overgrowth of Clostridium difficile bacteria.

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Irritable bowel syndrome

A complex condition involving inflammation of the intestines, often associated with abdominal pain and changes in bowel habits.

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Helicobacter pylori infection

An infection caused by the Helicobacter pylori bacteria, commonly residing in the stomach and duodenum.

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Protein synthesis inhibitor

A type of drug that works by inhibiting the synthesis of proteins within a cell.

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Pericoronitis

A condition involving inflammation of the gums near a partially erupted tooth.

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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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