Metronidazole

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

Hydrophilic metronidazole cream 2% (NRF 11.91.); Metronidazole facial fluid 1-2%

Definition
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Nitroimidazole derivative, chemotherapeutic agent. Metronidazole is one of the most frequently prescribed active substances. It is extremely well tolerated by topical application.

Half-life
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7-8 h or 10 h (metabolites).

Pharmacodynamics (Effect)
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Intracellular metabolism under anaerobic conditions, attachment of the metabolites to the DNA and fragmentation. For efficacy in rosacea it is assumed that metronidazole acts as a catalyst for the oxidation of palmitoleic acid to azelaic acid.

Spectrum of action
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Bacteroides spp., Balantidium coli, Chilomastix mesnii, Clostridium spp., Dientamoeba fragilis, Dracunculus medinensis, Entamoeba histolytica, Fusobacterium spp., Gardnerella vaginalis, Giardia lamblia, Prevotella spp.

Indication
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  • Systemic: Infections of the mucous membranes by anaerobes and Gardnerella vaginalis; aerobic-anaerobic mixed infections
  • Topical: in rosacea.

Limited indication
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Liver damage, chron. liver damage, chronic alcohol abuse, hematopoiesis disorders, diseases of the CNS and peripheral nervous system.

Dosage and method of use
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Topical: Solutions/Creams: In case of rosacea apply thinly once a day. 10% vaginal tablets for bacterial vaginal inflammation in the evening over 6 days, 10% vaginal tablets in addition to oral therapy for trichomoniasis over 6 days (partner treatment!). Systemic use: see table 1.

Standard concentration
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Solutions: 0.5%, creams: 1-2%; the upper indicative concentration of cutaneously applied metronidazole is 3%. Vaginal tablets: 10%.

Undesirable effects
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Allergic reactions, fixed drug reactions, CNS disorders, peripheral neuropathies, gastrointestinal disorders, leukopenia, vulvovaginal candidosis.

Interactions
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Alcohol (antabuse reaction), bleeding tendency when taking oral anticoagulants, disulfiram (psychosis), fluorouracil (neutropenia), phenobarbital (metronidazole effect), phenytoin (metronidazole effect), calcitabine (peripheral neuropathy).

Contraindication
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Pregnancy 1st trimester (trichomoniasis), lactation.

A combination with classic sun protection products is not recommended.

Recipe(s)
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In formulations Metronidazole has an optimum stability at pH5, in neutral and basic milieu hydrolysis occurs. In the 2% hydrophilic metronidazole cream (NRF 11.91.) metronidazole is mixed with non-ionic liniment DAC (NRFS.39.):

  • Rp (Hydrophilic metronidazole cream 2%)
  • metronidazole 1,0
  • Nonionic liniment DAC (NRF p.39.) 50,0

S. 2% Metronidazole cream (use-by period: 6 months; tube, dispenser) .

Other standardised magistral recipes:

Metronidazole gel, hydrophilic 0.75% (NRF 11.65.)

Metronidazole facial fluid 1-2% (O/W)

Metronidazole cream, tinted 1-2%

Metronidazole cream, hydrophilic 1/2% (NRF 11.91.) - combinations with 2% erythromycin or with 5% permethrin are possible

Preparations
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Metrogel, Clont, Flagyl

Note(s)
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  • Metronidazole is said to be more effective in HIV-associated eosinophilic pustular folliculitis than indomethacin.
  • Treatment duration: max. 10 days
  • Ineffective against propionibacteria and actinomycetes
  • Increasing resistance problems with Helicobacter pylori.

Literature
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  1. Ellis E et al (2004) Eosinophilic pustular folliculitis: a comprehensive review of treatment options. At J Clin Dermatol 5: 189-197
  2. Khan S et al (2007) Metronidazole-induced aseptic meningitis during Helicobacter pylori eradication therapy. Ann Intern Med 146: 395-396
  3. Meehlhorn A (2016) Metronidazole in magistral retinas. dermatologist 67: 503-505
  4. Wolf G (2011) Auxiliary tax for pharmacists. Dermatologist 62: 174-175.

Tables
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Dosage of Metronidazole depending on the indication

Indication

Therapy regime/dosage

histolytic entamoeba

Intestinal form: 750 mg/day p.o. for 5-10 days or 2.4 g/day p.o. for 2-3 days, plus 15-100 mg/kg bw paromomomycin or 500 mg diloxanide furoate (furamide)

Liver abscess: 30 mg/kg bw/day i.v. in 3 single doses for 8-10 days or 750 mg/day p.o. over 5-10 days, additionally as above

Anaerobic infections

Adults: 2-3 times/day 400-500 mg p.o.

Children < 12 years: 2-3 times/day 7 mg/kg bw

Giardia lamblia

adults: 2 g/day for 3 days or 750 mg/day for 5-7 days

Children: 15 mg/kg bw over 5-10 days

Leishmania

5 mg/kg bw/day for 30-60 days

Pseudomembranous colitis (in AI against vancomycin)

3 times/day 500 mg p.o. over 7-10 days

Trichomoniasis

2 times 1 g at intervals of 6 hours, the next morning 1 g as a single dose, additionally 1 vaginal suppository/day (partner treatment!). Alternatively 250-400 mg twice a day for 6 days, 1 vaginal suppository in the evening. Partner treatment!

Trypanosomes

5 mg/kg bw/day for 30-60 days

Authors

Last updated on: 29.10.2020