Metronidazole


Description

Metronidazole is a commonly used antibiotic, belonging to the nitroimidazole class of antibiotics.[14] It is frequently used to treat gastrointestinal infec...

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Pharmacology

Indication

Metronidazole is indicated for the treatment of confirmed trichomoniasis caused by Trichomonas vagin... Read more

Pharmacodynamic

Metronidazole treats amebiasis, trichomoniasis, and giardiasis, exerting both antibacterial and anti... Read more

Mechanism of action

The exact mechanism of action of metronidazole has not been fully established, however, it is possib... Read more

Absorption

After the intravenous infusion of a 1.5g dose, peak concentration was reached within 1 hour and was... Read more

Protein binding

Metronidazole is less than 20% bound to plasma proteins.[ Read more

Volume of distribution

Metronidazole is widely distributed throughout the body[ Read more

Clearance

Dose adjustments may be required in patients with hepatic impairment, as clearance is impaired in th... Read more

Half life

The elimination half-life of metronidazole is 7.3 ± 1.0 after a single 500mg IV dose in healthy subj... Read more

Route of elimination

Metronidazole and metabolites are 60 to 80% eliminated in the urine, and 6-15% excreted in the feces... Read more

Toxicity

LD50 information

The oral LD50 of metronidazole in rats is 5000 mg/kg [
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Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Fungal Infection US
  • Kind: experimental
    • Percent: 12%
  • Clinical Trial
    Candida vaginitis US
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 7%
  • Clinical Trial
    Erythema US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Vulvovaginal Candidiasis US
  • Kind: experimental
    • Percent: 5.6%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Worsening of rosacea US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Contact Dermatitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Local allergic reaction US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Skin stinging US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Skin burning US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Skin Irritation US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Erythema US
  • Kind: experimental
    • Percent: <3%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 2.2%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1.6%
  • Clinical Trial
    Vulvovaginal pruritus US
  • Kind: experimental
    • Percent: 1.6%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1.2%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 1.2%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Mucous membrane disorder US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Flu syndrome US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Breast Pain US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Allergic Reaction US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Metrorrhagia US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Vaginitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urinary Frequency US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Salpingitis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pyleonephritis US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Menorrhagia US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Leucorrhea US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Labial edema US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Female Lactation US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dysuria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Breast enlargement US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Pregnancy Trimester, First
        • Drugbank Id: DBCOND0006255
    • Regions: US
    • Patient Conditions:
        • Name: Hypersensitivity to nitroimidazoles
        • Drugbank Id: DBCOND0121375
    • Regions: US
    • Patient Conditions:
        • Name: Hypersensitivity to metronidazole
        • Drugbank Id: DBCOND0121374

    Food Interactions

    • Avoid alcohol.
    • Take with food to reduce irritation.

    Interactions

    Type in a drug name to check for interaction with Metronidazole

    The serum concentration of (R)-warfarin can be increased when it is combined with Metronidazole.
    The serum concentration of (S)-Warfarin can be increased when it is combined with Metronidazole.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Metronidazole.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Metronidazole.
    The metabolism of 5-androstenedione can be decreased when combined with Metronidazole.
    The serum concentration of 5-fluorouridine can be increased when it is combined with Metronidazole.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Metronidazole.
    The metabolism of 7-ethyl-10-hydroxycamptothecin can be decreased when combined with Metronidazole.
    The therapeutic efficacy of 7-Nitroindazole can be decreased when used in combination with Metronidazole.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Metronidazole.
    The metabolism of Metronidazole can be increased when combined with Abatacept.
    The serum concentration of Abemaciclib can be increased when it is combined with Metronidazole.
    The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Abexinostat.
    The metabolism of Abiraterone can be decreased when combined with Metronidazole.
    The metabolism of Metronidazole can be decreased when combined with Acalabrutinib.
    The serum concentration of Acebutolol can be increased when it is combined with Metronidazole.
    The serum concentration of Acenocoumarol can be increased when it is combined with Metronidazole.
    The risk or severity of QTc prolongation can be increased when Metronidazole is combined with Aceprometazine.
    The serum concentration of Acetaminophen can be increased when it is combined with Metronidazole.
    The therapeutic efficacy of Acetazolamide can be decreased when used in combination with Metronidazole.

    References

    • 1 . Shennan A, Crawshaw S, Briley A, Hawken J, Seed P, Jones G, Poston L: A randomised controlled trial of metronidazole for the prevention of preterm birth in women positive for cervicovaginal fetal fibronectin: the PREMET Study. BJOG. 2006 Jan;113(1):65-74. [PubMed: 16398774]
    • 2 . Williams CS, Woodcock KR: Do ethanol and metronidazole interact to produce a disulfiram-like reaction? Ann Pharmacother. 2000 Feb;34(2):255-7. [PubMed: 10676835]
    • 3 . Visapaa JP, Tillonen JS, Kaihovaara PS, Salaspuro MP: Lack of disulfiram-like reaction with metronidazole and ethanol. Ann Pharmacother. 2002 Jun;36(6):971-4. [PubMed: 12022894]
    • 4 . Dingsdag SA, Hunter N: Metronidazole: an update on metabolism, structure-cytotoxicity and resistance mechanisms. J Antimicrob Chemother. 2018 Feb 1;73(2):265-279. doi: 10.1093/jac/dkx351. [PubMed: 29077920]
    • 5 . Hernandez Ceruelos A, Romero-Quezada LC, Ruvalcaba Ledezma JC, Lopez Contreras L: Therapeutic uses of metronidazole and its side effects: an update. Eur Rev Med Pharmacol Sci. 2019 Jan;23(1):397-401. doi: 10.26355/eurrev_201901_16788. [PubMed: 30657582]
    • 6 . Sprandel KA, Schriever CA, Pendland SL, Quinn JP, Gotfried MH, Hackett S, Graham MB, Danziger LH, Rodvold KA: Pharmacokinetics and pharmacodynamics of intravenous levofloxacin at 750 milligrams and various doses of metronidazole in healthy adult subjects. Antimicrob Agents Chemother. 2004 Dec;48(12):4597-605. doi: 10.1128/AAC.48.12.4597-4605.2004. [PubMed: 15561831]
    • 7 . Lamp KC, Freeman CD, Klutman NE, Lacy MK: Pharmacokinetics and pharmacodynamics of the nitroimidazole antimicrobials. Clin Pharmacokinet. 1999 May;36(5):353-73. doi: 10.2165/00003088-199936050-00004. [PubMed: 10384859]
    • 8 . Morales-Leon F, von Plessing-Rossel C, Villa-Zapata L, Fernandez-Rocca P, Sanhueza-Sanhueza C, Bello-Toledo H, Mella-Montecinos S: [Pharmacokinetics/pharmacodinamic (PK/PD) evaluation of a short course of oral administration of metronidazole for the management of infections caused by Bacteroides fragilis]. Rev Chilena Infectol. 2015 Apr;32(2):135-41. doi: 10.4067/S0716-10182015000300001. [PubMed: 26065445]
    • 9 . Lau AH, Lam NP, Piscitelli SC, Wilkes L, Danziger LH: Clinical pharmacokinetics of metronidazole and other nitroimidazole anti-infectives. Clin Pharmacokinet. 1992 Nov;23(5):328-64. doi: 10.2165/00003088-199223050-00002. [PubMed: 1478003]
    • 10 . Kapoor K, Chandra M, Nag D, Paliwal JK, Gupta RC, Saxena RC: Evaluation of metronidazole toxicity: a prospective study. Int J Clin Pharmacol Res. 1999;19(3):83-8. [PubMed: 10761537]
    • 11 . Lofmark S, Edlund C, Nord CE: Metronidazole is still the drug of choice for treatment of anaerobic infections. Clin Infect Dis. 2010 Jan 1;50 Suppl 1:S16-23. doi: 10.1086/647939. [PubMed: 20067388]
    • 12 . Loesche WJ, Schmidt E, Smith BA, Morrison EC, Caffesse R, Hujoel PP: Effects of metronidazole on periodontal treatment needs. J Periodontol. 1991 Apr;62(4):247-57. doi: 10.1902/jop.1991.62.4.247. [PubMed: 2037955]
    • 13 . Pearce RE, Cohen-Wolkowiez M, Sampson MR, Kearns GL: The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94. doi: 10.1124/dmd.113.052548. Epub 2013 Jun 27. [PubMed: 23813797]
    • 14 . Flagyl (Metronidazole) FDA Label [Link]
    • 15 . FDA approvals, Metronidazole [Link]
    • 16 . Canadian monograph, Flagyl [Link]
    • 17 . Flagyl [Link]

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