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Metronidazole and Tinidazole

By

Brian J. Werth

, PharmD, University of Washington School of Pharmacy

Last full review/revision May 2020| Content last modified May 2020
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Metronidazole is a bactericidal antibiotic. It enters bacterial cell walls and disrupts DNA and inhibits DNA synthesis in certain microorganisms. Tinidazole is a related nitroimidazole with similar mechanism of action but more limited clinical use.

Pharmacokinetics

Oral metronidazole is absorbed well. It is usually given IV only if patients cannot be treated orally. It is distributed widely in body fluids and penetrates into cerebrospinal fluid, resulting in high concentrations.

Metronidazole is metabolized presumably in the liver and excreted mainly in urine, but elimination is not decreased in patients with renal insufficiency. However, because metronidazole metabolites may accumulate in patients with end-stage renal disease, these patients should be monitored for metronidazole-associated adverse effects such as central nervous system effects, including headaches, convulsions, and peripheral neuropathy (mainly numbness or paresthesias in an extremity).

Tinidazole has a slightly longer half-life than metronidazole, allowing for less frequent dosing.

Indications

Metronidazole is active against

Metronidazole is used primarily for infections caused by obligate anaerobes, often with other antimicrobials. Metronidazole is the drug of choice for bacterial vaginosis. The drug has other clinical uses (see table Some Clinical Uses of Metronidazole).

Tinidazole is used primarily for the protozoan parasites mentioned above. It is not used for systemic anaerobic bacterial infections.

Table
icon

Some Clinical Uses of Metronidazole

Indication

Comments

Infections due to obligate anaerobes (eg, intra-abdominal, pelvic, soft-tissue, periodontal, and odontogenic infections; lung abscess)

Often used with other antimicrobials

Drug of choice

Central nervous system infections (meningitis, brain abscess)

Septicemia

Prophylaxis before intestinal surgery

No longer recommended as a first-line drug

Should be considered only for mild cases when vancomycin or fidaxomicin are unavailable or for severe systemic cases given in combination with vancomycin

Peptic ulcers due to Helicobacter pylori

For treatment and prevention of relapses

Used with other drugs

Topical or oral use

Contraindications

Metronidazole and tinidazole are contraindicated in patients who have had an allergic reaction to it.

Use During Pregnancy and Breastfeeding

Reproduction studies with metronidazole in some animal species showed increased risk of carcinogenic activity. No adequate and well-controlled studies have been done in pregnant women. Most human studies have not shown increased risk of cancer, birth defects, or other fetal adverse effects after use of metronidazole during pregnancy; however, in some studies, cleft lip (with or without cleft palate) was reported in neonates of women who took metronidazole during the 1st trimester. Some experts advise avoiding metronidazole during the 1st trimester, although the Centers for Disease Control and Prevention's (CDC) 2015 sexually transmitted diseases treatment guidelines indicate that a single 2-g dose can be used at any stage of pregnancy to treat trichomoniasis.

Metronidazole enters breast milk; use during breastfeeding is not recommended.

There are limited data on use of tinidazole during pregnancy, but because animal studies suggest moderate risk, tinidazole is avoided during pregnancy.

Adverse Effects

Adverse effects of metronidazole and tinidazole include

  • Gastrointestinal disturbances

  • Central nervous system effects and peripheral neuropathy

  • Disulfiram-like reaction

Nausea, vomiting, headache, seizures, syncope, other central nervous system effects, and peripheral neuropathy can occur; rash, fever, and reversible neutropenia have been reported. Metronidazole can cause a metallic taste and dark urine. A disulfiram-like reaction (including flushing, headache, nausea, and vomiting) may occur if alcohol is ingested within 7 days of use.

Tinidazole may have a slightly lower incidence of gastrointestinal disturbance.

Dosing Considerations

Metronidazole and tinidazole doses are not decreased in patients with renal failure. Metronidazole doses are usually decreased 50% in patients with significant liver disease; tinidazole has not been studied in liver disease and should be used with caution if at all.

Metronidazole and tinidazole inhibit metabolism of warfarin and may increase its anticoagulant effect.

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