What is the clinical evidence available for twice daily metronidazole IV dosing compared to three times daily dosing? Is there any difference in efficacy based on clinical indications?

Comment by InpharmD Researcher

Limited data are available to compare the clinical outcomes of using metronidazole twice daily versus the standard dosing of three times daily. The existing evidence consists mainly of single-center cohort studies with small sample sizes, as well as pharmacokinetics/pharmacodynamics studies demonstrating in-vitro antimicrobial activities against common anaerobes. However, a more recent meta-analysis, published in July 2023, investigated metronidazole administration at 8-hour versus 12-hour intervals and found no significant differences in clinical outcomes for anaerobic infections.

Background

A recently published meta-analysis compared the efficacy of intravenous or oral metronidazole administration at every 8-hour versus every 12-hour intervals. The study highlighted that metronidazole's long elimination half-life, favorable ratio of steady-state serum levels to minimum inhibitory concentration (MIC), and presence of active metabolites suggest the consideration of using metronidazole at 12-hour dosage intervals. The final analysis incorporated two prospective cohort studies: one involving 200 patients at a single site (Table 1) and another multisite study with 85 patients (Table 2). The findings from the single-site study conducted by Soule et al. revealed no statistically significant between-group differences in primary outcomes, including clinical cure (8-hour: 83% vs. 12-hour: 83%, p= 1.00) and mortality (8-hour: 2% vs. 12-hour: 3%, p= 0.651). Additionally, there were no statistically significant differences in secondary clinical outcomes, such as the duration of antibiotic therapy (8-hour: 5.8 ± 4 vs. 12-hour: 5.9 ± 4.3, p= 0.891), duration of metronidazole use (8-hour: 4.8 ± 2.8 vs. 12-hour: 4.9 ± 2.4, p= 0.827), or hospital length of stay (LOS) in days (8-hour: 6.7 ± 5.2 vs. 12-hour: 8.1 ± 7, p= 0.110). Similarly, the multisite study conducted by Shah et al. indicated that patients who received metronidazole every 8 hours, compared to those who received it every 12 hours, had no statistically significant differences in all-cause 30-day mortality (8-hour: 15.6% vs. 12-hour: 9.4%, p= 0.492), median post-infection days of hospitalization (8-hour: 9 days, interquartile range [IQR]: 6 to 12.8 days vs. 12-hour: 8 days, IQR: 4 to 10 days, p= 0.271), or 30-day readmission due to infection (8-hour: 3.1% vs. 12-hour: 1.9%, p= 0.999). All patients who had repeat blood cultures showed sterile results (8-hour: 56% vs. 12-hour: 88.7%, p= 0.999). The meta-analysis concerning the need to escalate antibiotic therapy revealed no statistically significant difference (95% confidence interval [CI] 47.6% lower to 6.4 times higher risk; p = 0.342). These findings collectively suggest that dosing metronidazole every 12 hours is as effective as dosing every 8 hours for anaerobic infections. As a result, healthcare systems may consider adopting the every 12-hour metronidazole dosing regimen while continuing to evaluate patient outcomes. [1]

A 2016 poster abstract details a retrospective chart review (N= 81) comparing metronidazole 500 mg twice daily (BID) versus three times daily (TID) for appendicitis or diverticulitis. Clinical outcomes and readmission rates were assessed at 30 days follow-up. Patients were excluded if they had concomitant infection, fistula, or chronic appendicitis. The authors did not find a statistical difference in resolution rates (values unspecified). The 30-day readmission rates were similarly nonsignificant, with only 1 or 0 patients in the appendicitis or diverticulitis BID and TID groups being readmitted (p= 1 when comparing appendicitis and p= 0.417 when comparing diverticulitis). Yet, due to the small sample size and retrospective nature of the study, stronger evidence is needed to confirm these findings. [2]

Despite the limited clinical outcomes regarding Q12H vs Q8H metronidazole dosing, relatively dated pharmacokinetic (PK)/pharmacodynamic (PD) studies have observed efficient blood levels at 12 h post-administration. In 18 healthy volunteers who were randomly assigned to 3 doses of intravenous (IV) metronidazole (500 mg Q8H, 1,000 mg/day, 1,500 mg/day) and 8 critically ill patients who received 500 mg Q8H, the researchers observed attainment of the target pharmacodynamic parameter (AUC/MIC ratio ≥ 70) against B. fragilis isolates is > 99% when MICs are <2 mg/L, irrespective of the dosing interval of 24 h. In multiple PK/PD studies, the elimination half-life ranges from 6 to 10 h for metronidazole and from 8.5 to 19.2 h for its active hydroxy metabolite (antimicrobial activity ~30 to 65% that of metronidazole) in patients with normal renal function. [3], [4]

A 1983 review of metronidazole PK profile also discusses that Q12H dosing interval would generate corresponding concentrations of ~ 5 to 20 mcg/mL, which should be sufficient against most of the anaerobes and infections caused by Bacteroides, Fusobacteria, and Clostridia species. However, these MICs and susceptibility may not reflect antibiograms in current practice. [5]

According to an institutional therapeutic policy, a Canadian health system (Northern Health) advocates a transition from Q8H to Q12H metronidazole dosing for non-C. difficile infections, non-pseudomembranous colitis and non-CNS indications. This recommendation is mainly based on the presence of active metabolites and favorable ratio of serum levels to MIC without clearly referenced efficacy data regarding patient outcomes. [6]

Two randomized, controlled trials published in 2022 evaluated the efficacy of metronidazole twice daily as part of combination regimens for treating Helicobacter pylori infections. The first study compared esomeprazole 20 mg QID and amoxicillin 750 mg QID versus esomeprazole 20 mg BID, amoxicillin 1000 mg BID, and either clarithromycin 500 mg BID, metronidazole 400 mg BID, or levofloxacin 500 mg daily. All regimens were given for 14 days. Eradication of H. pylori with the two-drug regimen was found to be 84.9% compared to 83.6% in the patients that received triple therapy. There was no mention of how many patients in the triple therapy group received metronidazole, but 50% of specimens were found to be resistant to metronidazole therapy. [7]

Another randomized, controlled trial compared quadruple therapy (pantoprazole 40 mg, amoxicillin 1 g, clarithromycin 500 mg, and metronidazole 500 mg every 12 hours) for 14 days versus 14 days of high-dose dual therapy consisting of esomeprazole 40 mg BID and amoxicillin 1g TID. Eight weeks after the end of treatment, H. pylori eradication was found to be 88.6% in the quadruple therapy group compared to 82.2% in the dual therapy group (p= 0.19). [8]

A 2010 review indicates metronidazole is effective for the management of anaerobic infections, such as intra-abdominal infections, gynecologic infections, septicemia, endocarditis, bone and joint infections, central nervous system infections, and oral/dental infections. Metronidazole is also commonly used for prophylaxis before abdominal and gynecological surgical procedures to reduce the risk of postoperative anaerobic infection. For the treatment of severe intra-abdominal and pelvic infections, a retrospective chart review published in 2007 observed 1 g of metronidazole given intravenously once daily to have pharmacokinetic and pharmacoeconomic advantages over treatment administered every 6 to 8 hours. There is noted to be an increasing number of clinical failures reported with metronidazole treatment of Clostridioides difficile (C. diff). However, the appropriate frequency of metronidazole administration for the treatment of C. diff is not addressed. [9]

References:

[1] Jizba T, Ahmad F, Walters RW, Foral P, Destache CJ, Velagapudi M. A Comparison of Clinical Outcomes Associated with Dosing Metronidazole Every 8 Hours versus Every 12-Hours: A Systematic Review and Meta-Analysis. Medicine and Pharmacology; 2023.
[2] Béïque L, Tsang C, Geertsema S, et al. Comparison of metronidazole q12h to q8h in combination with other antibiotics on the clinical outcome and readmission rate of patients with appendicitis and diverticulitis. Open Forum Infectious Diseases. 2016;3(suppl_1):1037.
[3] Lamp KC, Freeman CD, Klutman NE, Lacy MK. Pharmacokinetics and pharmacodynamics of the nitroimidazole antimicrobials. Clin Pharmacokinet. 1999;36(5):353-373. doi:10.2165/00003088-199936050-00004
[4] Sprandel KA, Drusano GL, Hecht DW, Rotschafer JC, Danziger LH, Rodvold KA. Population pharmacokinetic modeling and Monte Carlo simulation of varying doses of intravenous metronidazole. Diagn Microbiol Infect Dis. 2006;55(4):303-309. doi:10.1016/j.diagmicrobio.2006.06.013
[5] Ralph ED. Clinical pharmacokinetics of metronidazole. Clin Pharmacokinet. 1983;8(1):43-62. doi:10.2165/00003088-198308010-00003
[6] Northern Health. New NH Therapeutic Interchange Metronidazole dose to dose TIP. Posted May 7, 2019. Accessed April 29, 2022.
[7] Zhao Z, Zou PY, Su NY, et al. High-dose dual therapy versus culture-based susceptibility-guided therapy as a rescue regimen for Helicobacter pylori infection: a randomized controlled trial. Therap Adv Gastroenterol. 2022;15:17562848221145566. Published 2022 Dec 26. doi:10.1177/17562848221145566
[8] Yadollahi B, Valizadeh Toosi SM, Bari Z, et al. Efficacy of 14-day concomitant quadruple therapy and 14-day high-dose dual therapy on H. pylori eradication. Gastroenterol Hepatol Bed Bench. 2022;15(2):172-178.
[9] Löfmark S, Edlund C, Nord CE. Metronidazole is still the drug of choice for treatment of anaerobic infections. Clin Infect Dis. 2010;50 Suppl 1:S16-S23. doi:10.1086/647939

Literature Review

A search of the published medical literature revealed 4 studies investigating the researchable question:

What is the clinical evidence available for twice daily metronidazole IV dosing compared to three times daily dosing? Is there any difference in efficacy based on clinical indications?

Level of evidence

C - Multiple studies with limitations or conflicting results  Read more→



Please see Tables 1-4 for your response.


Clinical efficacy of 12-h metronidazole dosing regimens in patients with anaerobic or mixed anaerobic infections

Design

Retrospective, single-center, pre–post-intervention study

N= 200

Objective

To evaluate the frequency of clinical cure among patients who received metronidazole every 12 h compared with those who received an every 8 h frequency

Study Groups

Q8h (n= 100)

Q12h (n= 100)

Inclusion Criteria

Aged ≥ 18 years; received metronidazole for at least 3 days for a presumed anaerobic or mixed anaerobic infection

Exclusion Criteria

C. difficile infection; central nervous system (CNS) infection; parasitic/amoebic infection; use of metronidazole for surgical prophylaxis; receipt of antibiotics with anaerobic coverage for greater than 24 h before the initiation of metronidazole; use of a concurrent medication with anaerobic coverage; those with an organism not susceptible to initial antibiotic selection; pregnant

Methods

All patients received metronidazole from June 2014 to June 2015 using the traditional 8-h dosing frequency. In July 2015, an every 12-h dosing was utilized for all indications except for C. difficile, CNS, or parasitic/amoebic infections. Clinical cure was defined as improvement or resolution of the principal sign/symptom of infection with normalization of white blood cells (WBCs > 4,000 and < 12,000 cells/µL) and temperature (> 96.8°F and < 100.4°F) at the end of therapy or discharge. Clinical failure was defined by the presence of any of the following parameters: no resolution of the principle sign/symptom, escalation of antibiotics, or no microbiological cure.

Duration

June 2014 to July 2016

Outcome Measures

Primary: clinical cure

Secondary: duration of antibiotics, hospital length of stay, escalation of antibiotic therapy, microbiologic cure, and mortality

Baseline Characteristics

 

Q8h (n= 100)

Q12h (n= 100)

p-value

Age, years

62.5 ± 18.7

53.9 ± 19.6

0.002

Male

44 40 0.567

Body mass index, kg/m2

Underweight

Normal

Overweight

Obese

Morbidly obese

 

4%

33%

28%

29%

6% 

 

4%

30%

33%

24%

9%

0.804

-

-

-

-

-

Intensive care unit (ICU) admission

5% 10% 0.179

Liver dysfunction*

6% 9% 0.421

Infection type

Abdominal

Skin/soft tissue

Pneumonia

Other

 

89%

4%

0

7%

 

79%

6%

2%

13%

0.187

-

-

-

-

Concurrent antibiotic therapy

Ciprofloxacin

Ceftriaxone

Other

None

93%

67%

17%

9%

7%

95%

46%

32%

17%

5%

0.552

-

-

-

-

Signs of infection

Abdominal pain

Elevated temperature

Elevated white blood cells

Radiographic confirmation

 

73%

18%

51%

77%

 

64%

23%

53%

74%

 

0.171

0.381

0.777

0.622

Underweight, < 18.5; normal, 18.5–24.9; overweight, 25–29.9; obese, 30–39.9; morbidly obese, > 40

*The metabolism of metronidazole is decreased in patients with hepatic impairment. Dose reductions of 50% may be needed for Child-Pugh Class C.

Results

Endpoint

Q8h (n= 100)

Q12h (n= 100)

p-value

Clinical cure

83% 83% 1

Escalation of all antibiotic therapy

Duration of all antibiotic therapy, days

Duration of metronidazole, days

Hospital length of stay, days

1

5.8 ± 4

4.8 ± 2.8

6.7 ± 5.2

1

5.9 ± 4.3

4.9 ± 2.4

8.1 ± 7

1

0.891

0.827

0.11

Death

2% 3% 0.651

Adverse Events

Not disclosed

Study Author Conclusions

No differences in clinical outcomes for patients receiving every 12-h metronidazole dosing interval were identified among patients receiving metronidazole for presumed anaerobic or mixed anaerobic infections. These findings validate existing pharmacokinetic data and add to the limited clinical literature that currently exists for this dosing strategy. In addition to effectively treating infections, utilizing a 12-h dosing interval has the potential to reduce drug costs, adverse drug effects, and antibiotic resistance.

InpharmD Researcher Critique

This study has some limitations, including the single-center and retrospective design; however, given the relatively large sample size, it was powered to detect a difference in clinical cure between the different dosing groups. Since more patients required initial admission to ICU in the 12-h group vs the 8-h group, patients in the 12-h group may have had more severe infections and possible comorbidities upon initial presentation vs the 8-h group. 

References:

Soule AF, Green SB, Blanchette LM. Clinical efficacy of 12-h metronidazole dosing regimens in patients with anaerobic or mixed anaerobic infections. Ther Adv Infect Dis. 2018;5(3):57-62. doi:10.1177/2049936118766462

Three is a crowd: Clinical outcomes of a twice daily versus a thrice daily metronidazole dosing strategy from a multicenter study.

Design

Multicenter, retrospective, chart review

N= 85

Objective

To compare clinical outcomes of metronidazole 500 mg every 8 hours and 500 mg every 12 hours for patients with bloodstream infections due to obligate anaerobes

Study Groups

8-hour interval (n= 32)

12-hour interval (n= 53)

Inclusion Criteria

Patients with anaerobic bacteremia who received 500 mg of the intravenous or oral formulation of metronidazole at a dosing interval of either every 12 hours or every 8 hours

Exclusion Criteria

Received < 72 hours of metronidazole, initially received metronidazole every 8 hours before transition to every 12 hours, initially received of ≥ 72 hours of an anaerobic agent excluding metronidazole, initially received of ≥ 72 hours of an antimicrobial agent suspected to be susceptible to the primary pathogen identified, received metronidazole concomitantly with an antimicrobial that was suspected to be susceptible to the primary pathogen identified, concomitant Clostridoides difficile infection, central nervous system infection, infected with an anaerobe that was likely resistant to metronidazole

Methods

Eligible patients who received metronidazole for anaerobic bacteremia at the specified doses were identified from chart reviews and included for analysis. The decision to use metronidazole at a dosing interval of either 12 or 8 hours was made based solely on the prescriber’s preference. 

Duration

Between August 2016 and July 2020

Outcome Measures

Primary: all-cause 30-day mortality

Secondary: length of stay (time from positive blood culture to hospital discharge), escalation of antimicrobial therapy (antimicrobial therapy was broadened in the setting of clinical decompensation or the metronidazole dosing interval of every 12 hours was increased to every 8 hours), 30-day readmission due to infection, and positive repeat blood cultures following initiation of metronidazole. 

Baseline Characteristics

 

8-hour interval (n= 32)

12-hour interval (n= 53)

p-value

Median age, years (interquartile range [IQR])

71 (58.8 to 79)  65 (50 to 76) 0.08

Female

59.4% 52.4% 0.557 

Median body mass index, kg/m2 (IQR)

25 (22.2 to 31.3)  27.8 (22.4 to 37.3)  0.246

Median Charleson comorbidity index (IQR)

2 (0 to 3.3)  3 (1 to 6)  0.21

Comorbidities

Moderate to severe renal disease

Diabetes with organ damage 

Metastatic tumor 

Leukemia or lymphoma

Moderate to severe liver disease

 

6.2%

18.8%

12.5%

12.5%

6.2%

 

18.9%

17.0%

17.0%

5.7%

3.8%

 

0.197

0.836

0.759

0.417

0.63

Median PITT bacteremia score (IQR)

0 (0 to 1)  1 (0 to 1)  0.162

Concomitant antimicrobial

Ceftriaxone 

Ceftazidime/cefepime 

Cefazolin/cefuroxime 

Ciprofloxacin 

Other 

No concomitant antimicrobials

 

56.3%

12.5%

0

15.6%

9.4%

6.25%

 

35.8%

15.1%

7.5%

20.8%

5.7%

15.1%

0.307

--

--

--

--

--

--

The most common pathogen was B. fragilis, which was identified in 42.4% of cases; 10 (31.3%) in the 8-hour interval group and 26 (49.1%) in the 12-hour interval group.

Results

Endpoint

8-hour interval (n= 32)

12-hour interval (n= 53)

p-value

All-cause 30-day mortality

5 (15.6%) 5 (9.4%) 0.492

Median post-infection hospital length of stay, days (IQR)

9 (6 to 12.8) 8 (4 to 10) 0.271

Escalation of antimicrobial therapy

4 (12.5%) 3 (5.7%) 0.417

30-day readmission due to infection

1 (3.1%) 1 (1.9%) 0.999

Repeat blood cultures were performed for 18 patients in the 8-hour interval group and 47 patients in the 12-hour interval group and were sterile in all cases

Adverse Events

Not disclosed

Study Author Conclusions

In this multicenter study of patients with anaerobic bacteremia who received metronidazole 500 mg every 8 hours, there was no statistically significant difference in clinical outcomes compared to patients who received metronidazole 500 mg every 12 hours. Although further study is needed to confirm these findings, the benefits of using a metronidazole 500 mg dosing interval of every 8 hours should be weighed against the risk of adverse effects with prolonged use.

InpharmD Researcher Critique

The study is inherently limited by its retrospective design and relatively small sample size. Chart review studies are also subject to reporting bias. 

 

References:

Shah S, Adams K, Merwede J, McManus D, Topal J. Three is a crowd: Clinical outcomes of a twice daily versus a thrice daily metronidazole dosing strategy from a multicenter study. Anaerobe. 2021;71:102378. doi:10.1016/j.anaerobe.2021.10237

Metronidazole: two or three times daily-a comparative controlled clinical trial of the efficacy of two different dosing schedules of metronidazole for chemoprophylaxis following third molar surgery

Design

Single-blind, single-center, prospective, randomized trial

N= 57

Objective

To compare the incidence of post-surgical complications with varying dosage schedules of metronidazole

Study Groups

Twice daily (n= 30)

Three times daily (n= 27)

Inclusion Criteria

Age 18 to 32 years; surgical excision of both mandibular third molars under general anesthesia

Exclusion Criteria

Any other surgical removals of maxillary third molars; adverse medical history; acute infection; receiving concurrent antibiotics

Methods

Patients were randomized to receive metronidazole 400 mg PO two or three times daily for 5 days postoperative. Patients were given a prescription of acetaminophen-codeine compound for analgesia but could use others for pain control. Patients and the operative procedures by four different clinicians were blinded, but not the investigators.

Duration

Follow-up: 7 days

Outcome Measures

Postoperative complications; reported side effects

Baseline Characteristics

There are no statistical differences in baseline characteristics (specifics not provided) or surgeon performing the procedure.

Results

Endpoint

Three times daily (n= 27)

Twice daily (n= 30)

Postoperative complications

Swelling

Wound erythema

Wound breakdown

Wound discharge

 

23

14

5

2

 

21

16

3

3

Side effect

Nausea

Vomiting

Abdominal discomfort

Diarrhea

Constipation

Drowsiness

Headache

Dizziness

Change in urine color

 

15*

6

2

1

3

9

7

6

8

 

8

7

3

3

6

11

10

8

7

*p < 0.05 versus three times daily group

Three patients admitted to not being compliant with prescribed metronidazole. Compliance variation was not analyzed between groups.

Study Author Conclusions

It would appear that a 12-hourly dose interval of metronidazole is no different from an 8-hourly dose interval in the prevention of local wound infection following minor oral surgery.

InpharmD Researcher Critique

This is an older study and may not reflect current clinical practices. The setting is specific to the removal of molars and does not apply to all clinical scenarios. Patients had confessed not to be fully compliant with metronidazole therapy. Therefore, the true comparative efficacy and safety between dosing intervals of metronidazole remain uncertain.

 

References:

Lloyd CJ, Earl PD. Metronidazole: two or three times daily--a comparative controlled clinical trial of the efficacy of two different dosing schedules of metronidazole for chemoprophylaxis following third molar surgery. Br J Oral Maxillofac Surg. 1994;32(3):165-167. doi:10.1016/0266-4356(94)90102-3

Twelve-hourly dosage schedule for oral and intravenous metronidazole

Design

Prospective, non-randomized study

N= 48

Objective

To examine the adequacy of metronidazole given every 12 hours by assaying the trough and peak serum concentrations in patients receiving the drug either orally or intravenously (IV)

Study Groups

Metronidazole PO (n= 25)

Metronidazole IV (n= 23)

Inclusion Criteria

Undergoing surgery

Exclusion Criteria

N/A

Methods

Patients received a prophylactic or treatment regimen of either metronidazole 400 mg PO every 12 hours or 500 mg IV every 12 hours. Two blood samples were drawn, the first was taken immediately before a dose (trough) and the second was taken 1.5 hours after the dose (peak). All patients received beta-lactam antibiotics with metronidazole but were inactivated in the assay procedure using 0.03 mL of broad-spectrum beta-lactamase.  

Duration

1.5 hours after dose

Outcome Measures

Mean trough and peak concentrations

Baseline Characteristics

Not provided

Results

Endpoint

Metronidazole PO (n= 25)

Metronidazole IV (n= 23)

Trough, mg/L

5.5

6.7

Peak, mg/L

17.4

23.6

Adverse Events

N/A

Study Author Conclusions

The trough concentrations are well in excess of the minimum inhibitory capacity (MICs) for the majority of obligate anaerobes and thus the 12-hourly regimen achieves and maintains therapeutic serum concentrations of metronidazole. The reduction from 8-hourly regimens of this agent to 12-hourly represents a substantial saving in the drug budget.

InpharmD Researcher Critique

Antimicrobial Resistance patterns are often based on geographic regions. While the trough and peak levels were acceptable for the author's particular institution, it is unknown whether these results reflect the current clinical landscape. The MIC goal levels for coverage of anaerobic microbial were not discussed.
References:

Earl P, Sisson PR, Ingham HR. Twelve-hourly dosage schedule for oral and intravenous metronidazole. J Antimicrob Chemother. 1989;23(4):619-621. doi:10.1093/jac/23.4.619