Use of antibiotics for inducing remission in Crohn's disease

ON THE USE OF ANTIBIOTICS IN CROHN’S DISEASE.

Van Kruiningen HJ, Department of Pathobiology, University of Connecticut, Storrs 06269-3089, USA. J Clin Gastroenterol, 1995 Jun, 20:4, 310-6

It is difficult to understand how a disease process characterized by ulcerations, fissures, abscesses, fistulas, lymphangitis, and granulomas has not attracted greater use of antibiotics, particularly as the sites are constantly contaminated by intestinal bacteria. I have had a favorable experience with broad-spectrum antibiotics in the treatment of a variety of forms of ileocolitis in animals and now advocate that Crohn’s disease be treated at length with these drugs. Microbiologic culture of serosa, mesenteric lymph nodes, and fistulas has demonstrated that bacterial species are present in a significant proportion of cases, and serology has shown that patients have elevated antibody levels to many of these same microorganisms. Now immunocytochemistry provides documentation of Escherichia coli and streptococcal antigen within the lesions of a majority of patients. That these bacteria may be secondary invaders should not decrease our need to address them. Several chronic granulomatous diseases that were once thought to be intractable now yield to long-term antibiotic treatment, including Whipple’s disease, malakoplakia, and granulomatous colitis of Boxer dogs. Many of the perianal lesions of Crohn’s disease respond to short-term metronidazole, and the medium-term (3-6 months) use of broad-spectrum antibiotics, most recently ciprofloxacin, has shown promising results. In view of the increasing evidence of bacterial participation in this disease, it is now important that physicians test some of our newer broad-spectrum antibiotics, in a controlled format, and over an extended time.
 

COMBINATION CIPROFLOXACIN AND METRONIDAZOLE FOR ACTIVE CROHN’S DISEASE.
Greenbloom SL; Steinhart AH; Greenberg GR; Division of Gastroenterology, Mount Sinai Hospital, Toronto, Ontario. Can J Gastroenterol, 1998 Jan, 12:1, 53-6

Recent experimental evidence underscores the contribution of intestinal bacteria to the inflammatory process of Crohn’s disease. This open study examined the efficacy and safety of combination ciprofloxacin and metronidazole for patients with active Crohn’s disease of the ileum and/or colon. Seventy-two patients with active Crohn’s disease of the ileum (n = 27), ileocolon (n = 22) or colon (n = 23) were treated with ciprofloxacin 500 mg bid and metronidazole 250 mg tid for a mean of 10 weeks. Clinical remission was defined as a Harvey-Bradshaw index of three points or less; an index reduction of at least three points indicated a clinical response. Clinical remission was observed in 49 patients (68%), and 55 patients (76%) showed a clinical response. A clinical response was noted in 29 of 43 patients (67%) who were not taking concurrent prednisone treatment and in 26 of 29 patients (90%) receiving prednisone (mean dose of 15 mg/day). A clinical response also occurred in a greater proportion of patients with colonic disease, with or without ileal involvement (84%), compared with patients with ileal disease alone (64%), and in patients without resection (86%) compared with those with previous resection (61%). Five patients discontinued antibiotics because of adverse events. After a mean follow-up of nine months, clinical remission was maintained in 26 patients off treatment and in 12 patients who continued antibiotic therapy. Ciprofloxacin in combination with metronidazole is well tolerated and appears to play a beneficial role in achieving clinical remission for patients with active Crohn’s disease, particularly when there is involvement of the colon.
 

AN ANTIBIOTIC REGIMEN FOR THE TREATMENT OF ACTIVE CROHN’S DISEASE: A RANDOMIZED, CONTROLLED CLINICAL TRIAL OF METRONIDAZOLE PLUS CIPROFLOXACIN.
Prantera C; Zannoni F; Scribano ML; Berto E; Andreoli A; Kohn A; Luzi C; Division of Gastroenterology, Ospedale Nuovo Regina Margherita, Rome, Italy.  Am J Gastroenterol, 1996 Feb, 91:2, 328-32

OBJECTIVES: Bacteria in the gut lumen may play a role in the etiology and/or the symptoms of Crohn’s disease (CD). Although various antibacterial drugs have been employed in clinical practice, few controlled trials have been conducted, and those had conflicting results. The aim of this study was to investigate the efficacy and the safety of a combination of metronidazole and ciprofloxacin, compared with methylprednisolone, in treating 41 consecutive patients with active CD. METHODS: Eligible patients, 13 men and 28 women, mean age 38 yr, were randomly allocated to receive, for 12 wk, ciprofloxacin 500 mg twice daily plus metronidazole 250 mg four times daily or methylprednisolone 0.7-l mg/kg/day, with variable tapering to 40 mg, followed by tapering of 4 mg weekly.  RESULTS: Ten of the 22 antibiotic patients (45.5%) and 12 of the 19 steroid patients (63%) obtained clinical remission (Crohn’s Disease Activity Index < or = 150) at the end of the 12-wk study (p = NS). Five patients on antibiotics (22.7%) and five patients on steroids (26.3%) were considered treatment failures because of deterioration or persistent symptoms. Six patients receiving antibiotics (27.3%) and two on steroids (10.6%) were withdrawn from the trial because of side effects. One patient on antibiotics was not compliant. CONCLUSIONS: metronidazole and ciprofloxacin could be an alternative to steroids in treating the acute phase of CD.
 

ORNIDAZOLE IN THE TREATMENT OF ACTIVE CROHN’S DISEASE: SHORT-TERM RESULTS.
Triantafillidis JK; Nicolakis D; Emmanoullidis A; Antoniou A; Papatheodorou K; Cheracakis P; Department of Gastroenterology, Saint Pantelelmon General State Hospital, Nicea, Piraeus, Greece. Ital J Gastroenterol, 28(1):10-4 1996 Jan

The object of this work was to test the efficacy of ornidazole in patients with active Crohn’s disease. Twenty-five patients with active Crohn’s disease (Crohn’s disease activity index greater than 150 points) participated in this open study. The analysis of results was based on changes in the severity of the Crohn’s disease activity index measured at entry and at the end of the first, second, and third and fourth week. Analysis of variance, correlation analysis, multiple regression analyses and chi-square test were used for statistical evaluation of results. The results showed that the Crohn’s disease activity index fell gradually from week 0 to week 4 (p < 0.001), while the number of patients going into remission increased gradually from week 0 to week 4 (18/25 patients, 75%).  Sex, location of disease, age at onset, first attack or recurrence and duration of disease were not statistically related to response to treatment. Presence and severity of abdominal pain both decreased and bowel movements were also reduced. General well-being improved significantly, the loss of weight stopped and an increase in body weight was noted at the end of the fourth week.  Side effects were minimal. It is concluded that ornidazole is an effective and safe drug for the treatment of active Crohn’s disease.
 

METRONIDAZOLE. A THERAPEUTIC REVIEW AND UPDATE.
Freeman CD; Klutman NE; Lamp KC  Department of Medicine, University of Missouri-Kansas City School of Medicine, USA. cfreeman@cctr.umkc.edu  Drugs, 1997 Nov, 54:5, 679-708

The nitroimidazole antibiotic metronidazole has a limited spectrum of activity that encompasses various protozoans and most Gram-negative and Gram-positive anaerobic bacteria. Metronidazole has activity against protozoans like Entamoeba histolytica, Giardia lamblia and Trichomonas vaginalis, for which the drug was first approved as an effective treatment. Anaerobic bacteria which are typically sensitive are primarily Gram-negative anaerobes belonging to the Bacteroides and Fusobacterium spp. Gram-positive anaerobes such as peptostreptococci and Clostridia spp. are likely to test sensitive to metronidazole, but resistant isolates are probably encountered with greater frequency than with the Gram-negative anaerobes. Gardnerella vaginalis is a pleomorphic Gram-variable bacterial bacillus that is also susceptible to metronidazole. Helicobacter pylori has been strongly associated with gastritis and duodenal ulcers. Classic regimens for eradicating this pathogen have included metronidazole, usually with acid suppression medication plus bismuth and amoxicillin. The activity of metronidazole against anaerobic bowel flora has been used for prophylaxis and treatment of patients with Crohn’s disease who might develop an infectious complication. Treatment of Clostridium difficile-induced pseudomembraneous colitis has usually been with oral metronidazole or vancomycin, but the lower cost and similar efficacy of metronidazole, coupled with the increased concern about imprudent use of vancomycin leading to increased resistance in enterococci, have made metronidazole the preferred agent here. Metronidazole has played an important role in anaerobic-related infections. Advantages to using metronidazole are the%age of sensitive Gram-negative anaerobes, its availability as oral and intravenous dosage forms, its rapid bacterial killing, its good tissue penetration, its considerably lower chance of inducing C. difficile colitis, and expense.  Metronidazole has notable effectiveness in treating anaerobic brain abscesses. Metronidazole is a cost-effective agent due to its low acquisition cost, its pharmacokinetics and pharmacodynamics, an acceptable adverse effect profile, and its undiminished antimicrobial activity. While its role as part of a therapeutic regimen for treating mixed aerobic/anaerobic infections has been reduced by newer, more expensive combination therapies, these new combinations have not been shown to have any therapeutic advantage over metronidazole.  Although the use of metronidazole on a global scale has been curtailed by newer agents for various infections, metronidazole still has a role for these and other therapeutic uses. Many clinicians still consider metronidazole to be the ‘gold standard’ antibiotic against which all other antibiotics with anaerobic activity should be compared.
 

CONTROLLED TRIAL OF METRONIDAZOLE TREATMENT FOR PREVENTION OF CROHN’S RECURRENCE AFTER ILEAL RESECTION [SEE COMMENTS]
Rutgeerts P; Hiele M; Geboes K; Peeters M; Penninckx F; Aerts R; Kerremans R, Department of Medicine, University Hospital Gasthuisberg, University of Leuven, Belgium. Gastroenterology, 1995 Jun, 108:6, 1617-21

BACKGROUND/AIMS: New lesions recur within weeks to months after ileal resection and ileocolonic anastomosis for Crohn’s ileitis. A double-blind controlled trial was performed using metronidazole to prevent recurrence after ileal resection. METHODS: Sixty patients who underwent curative ileal resection and primary anastomosis were included within 1 week after surgery. Thirty patients received metronidazole (20 mg/kg body wt) daily for 3 months, and 30 patients received placebo. Treatment was then discontinued. Nine patients dropped out during treatment, 7 in the metronidazole group and 2 in the placebo arm. RESULTS: At 12 weeks, 21 of 28 patients (75%) in the placebo group had recurrent lesions in the neoterminal ileum as compared with 12 of 23 patients (52%) in the metronidazole group (P = 0.09). The incidence of severe endoscopic recurrence was significantly reduced by metronidazole (3 of 23; 13%) as compared with placebo (12 of 28; 43%; P = 0.02). Patients in the metronidazole arm had more frequent side effects. Metronidazole therapy statistically reduced the clinical recurrence rates at 1 year (4% vs. 25%). Reductions at 2 years (26% vs. 43%) and 3 years (30% vs. 50%) were not significant. CONCLUSIONS: Metronidazole therapy for 3 months decreases the severity of early recurrence of Crohn’s disease in the neoterminal ileum after resection and seems to delay symptomatic recurrence.
 

A COMPARATIVE STUDY OF METRONIDAZOLE AND SULFASALAZINE FOR ACTIVE CROHN’S DISEASE: THE COOPERATIVE CROHN’S DISEASE STUDY IN SWEDEN. II. RESULT.
Ursing B; Alm T; Bárány F; Bergelin I; Ganrot-Norlin K; Hoevels J; Huitfeldt B; Järnerot G; Krause U; Krook A; Lindström; B; Nordle O; Rosén A;  Gastroenterology, 1982 Sep, 83:3, 550-62

Seventy-eight patients with active Crohn’s disease participated in a randomized, double-blind,
cross-over trial. The study comprised two 4-mo period. The purpose was to test the efficacy of
metronidazole in comparison with that of sulfasalazine. As the main evaluation criteria the Crohn’s
Disease Activity Index and plasma levels of orosomucoid were chosen. In the first period no
difference in efficacy as measured by Crohn’s Disease Activity Index was found between the
treatment groups. The reduction of the plasma orosomucoid level was significantly more pronounced in the metronidazole group. The hemoglobin concentration increased more in this group than in the
sulfasalazine group, possibly due to a toxic effect of sulfasalazine. The erythrocyte sedimentation rate decreased similarly with both drugs. In 15 patients who had active disease throughout the first
period, Crohn’s Disease Activity Index decreased significantly in the second period for those who
switched to metronidazole, but not for those who switched to sulfasalazine. After crossover, no
apparent further change in Crohn’s Disease Activity Index occurred in either of the treatment groups
among patients who had responded favorably in the first period. The plasma concentration of
orosomucoid increased significantly among the patients in the sulfasalazine group but not in the
metronidazole group. It is therefore concluded that metronidazole is slightly more effective than
sulfasalazine in the treatment of crohn’s disease. It is worthwhile switching the drug regimen from
sulfasalazine, when it fails, to metronidazole, but not from metronidazole to sulfasalazine.
 

THE COURSE OF CROHN DISEASE AND SIDE EFFECT PROFILE WITH LONG-TERM TREATMENT USING METRONIDAZOLE
Gugler R; Jensen JC; Schulte H; Vogel R, Medizinische Universitätsklinik, Bonn. Z Gastroenterol, 1989 Nov, 27:11, 676-82

In a prospective study 21 patients with Crohn’s disease not responding to standard treatment (salazosulfapyridine and/or corticosteroids) received metronidazole in a dose of 12 to 20 mg per kg body weight over 6 and 12 months respectively. The objectives were documentation of side effects and pharmacokinetic behaviour of metronidazole in relation to the course of the disease. In 3 months intervals and 3 months after the end of treatment activity indices were determined, the side effects of metronidazole were recorded and the drug plasma concentration was measured. Compliance of drug intake was excellent (94%). Best-Index decreased to a minimum after 6 months, orosomucoid after 3 months. Side effects from metronidazole (black tongue, dark urine, paraesthesia, metallic taste, epigastric pain, skin reactions, nausea) were reported by over 80% of the patients at any time of the study. Nearly 50% of patients developed paraesthesia, which was still present 3 months after the end of treatment. A mean dose of 15.4 mg per kg corresponded to a mean plasma concentration of 10.9 micrograms/ml of metronidazole. Plasma concentrations were not related to treatment success nor to the incidence of side effects. Treatment of Crohn’s disease with metronidazole for longer than 3 months is not recommended both because of lack of additional therapeutic gain and because of the increasing risk of side effects.
 

In animal experiments investigating induction of chronic intestinal disease by inoculating them with isolates from Crohn's patients, "the addition of an antibiotic (ampicillin) prevented the appearance of these Crohn’s-like changes in 12 out of 12 rabbits" (Donnelly BJ, Delaney PV, Healy TM. Gut 1977 May;18(5):360-3), pointing to an infectious agent rather than a toxic chemical content in the isolate from Crohn's patient's intestines.
 

Use of antibiotics against H. hepaticus in mice IBD
 
EVALUATION OF ANTIBIOTIC THERAPIES FOR ERADICATION OF H. HEPATICUS.
Foltz CJ; Fox JG; Yan L; Shames B Division of Comparative Medicine, Massachusetts Institute of
Technology, Cambridge 02139, USA. Antimicrob Agents Chemother, 1995 Jun, 39:6, 1292-4

The newly recognized murine pathogen Helicobacter hepaticus is known to colonize the ceca and
colons of several strains of mice from a variety of commercial suppliers. Additionally, the organism
persistently infects mice, causes a chronic hepatitis, and is linked to hepatic tumors in the A/JCr
inbred mouse strain. For this reason, eradication of the organism from infected mouse colonies is
desirable. Treatment modalities for eradication of H. hepaticus from the gastrointestinal system
consisted of oral administration of various antibiotic combinations previously evaluated for
eradication of experimental H. felis gastric infection in mice. A/JCr mice (8 to 10 weeks old)
naturally infected with H. hepaticus were divided into six treatment groups of 10 animals each.
Animals received monotherapy of amoxicillin, metronidazole, or tetracycline or triple therapy of amoxicillin-metronidazole-bismuth (AMB) or tetracycline-metronidazole-bismuth (TMB). All medications were administered by oral gavage three times daily for 2 weeks. One month after the final treatment, mice were euthanatized and livers, ceca, and colons were cultured for H. hepaticus. All untreated control animals had H. hepaticus isolated from the cecum and/or colon. H. hepaticus was not recovered from the livers, ceca, or colons of the AMB or TMB treatment groups. All animals receiving the various antibiotic monotherapies had H. hepaticus isolated from the cecum and colon. We conclude that at the doses and the route evaluated, AMB and TMB triple therapies are effective for eradication of H. hepaticus in 8- to 10-week old A/JCr mice.
 

THE GOOD NEWS IS THAT ONCE DIAGNOSED, H. HEPATICUS APPEARS TO BE
TREATABLE WITH THE SIMILAR 2 WEEK TREATMENT (in mice) APPROVED BY FDA
FOR H. PYLORI (or may be 3 months in chronic IBD):

From the Journal of American Medical Association( AMA ), June 18, 1997:

The FDA has also approved 3 combination regimens for treatment of H pylori infection: omeprazole plus clarithromycin(cure rate about 70%), ranitidine bismuth citrate plus clarithromycin (cure rate about  80%), and bismuth subsalicylate plus metronidazole plus tetracycline combined with an antisecretory drug (cure rate about 80%), each given for 2 weeks. However, most experts believe the best therapy may be a combination of ranitidine bismuth citrate or a proton pump inhibitor plus clarithromycin plus either amoxicillin or metronidazole given for 7 to 10 days (cure rate about 90%).

NOTE: Metronidazole is not the only antibiotic used successfully in both H pylori and Crohn's. According to Prof. Hermon-Taylor, St. George's Hospital Medical School, London, about 80% of more than 100 Crohn's patients he treated with a combination of rifabutin and clarithromycin had "a profound and lasting remission" of their illness. David Graham, MD, VA Medical Center and Baylor College of Medicine in Houston, and colleagues conducted a placebo-controlled trial looking at the efficacy of clarithromycin as a treatment for Crohn's disease. They randomly assigned 17 people with severe Crohn's disease to receive either conventional therapy plus a placebo or conventional therapy plus clarithromycin. They did not determine whether the patients harbored M. paratuberculosis. Forty percent of the patients in the antibiotic arm became well and stayed well for up to three years, said Graham, who is chief of gastroenterology at the Veterans Administration Medical Center in Houston. In contrast, one person in the placebo arm became well but did not remain well. (Graham, D.Y., M.T. Al-Assi, and M. Robinson.  Prolonged remission in Crohn's disease following therapy for Mycobacterium paratuberculosis infection. 1995. Gastroenterology, vol. 108, no. 4, A826 AGA Abstracts). To confirm their findings, Graham and colleagues are conducting a larger placebo-controlled study looking at the efficacy of clarithromycin plus ethambutol.
 
In conclusion, regardless if the presumed infective agent in Crohn's disease is Mycobacterium paratuberculosis or Helicobacter species, clinical studies have shown the following similarities with H pylori (and H hepaticus):

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