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At least 19 recordsLinked to original sources
PubMed2006

Chiral separation of rac-Ornidazole and detection of the impurity of (R)-Ornidazole in (S)-Ornidazole injection and raw material.

(S)-Ornidazole is a subject of research as an antifertility agent in male animals at present. However, there seems to be no relative report on chiral separation for rac-Ornidazole, which has been used as an effective medicine for more than 30 years. In this article, the chiral separation of rac-Ornidazole on a Chiralcel OB-H column based on normal-phase high-performance liquid chromatography (NP-HPLC) is investigated and the methodology for detection of impurity of (R)-Ornidazole in (S)-Ornidazole injection and raw material is established. The novel mobile phase is utilized by mixing n-hexane, methanol and isopropyl alcohol (95:4:1, v/v/v) instead of the typical mobile phase of n-hexane and isopropyl alcohol, although the methanol, which offers a good resolution factor for the enantiomeric separation in this system, is not recommended on the Chiralcel OB-H column according to the instruction supplied by Daicel Chemical Ind., LTD (Japan).

2-Propanol↗
PubMed2002

The effect of (R,S)-ornidazole on the fertility of male mice and the excretion and metabolism of 36Cl-(R,S)-ornidazole and 36Cl-(R,S)-alpha-chlorohydrin in male mice and rats.

(R,S)-Ornidazole, an effective antifertility agent for male rats at 400 mg/kg/day, was ineffective at this dose in male mice and at 1000 mg/kg/day caused neural effects. The compound was not excreted unchanged and more polar metabolites and Cl- were detected in 0-8 h urine following a single injection (400 mg/kg). In 8-24 h urine even these metabolites and most Cl ion were absent, indicating rapid metabolism of ornidazole. There was no organ specific accumulation of 36Cl-(R,S)-ornidazole in murine tissues. After injection of 36Cl-(R,S)-alpha-chlorohydrin, another antifertility agent in the rat but not the mouse, there was also no tissue-specific accumulation of radioactivity in the reproductive tract of either species. Urinary excretion rates of alpha-chlorohydrin were twice as rapid in mice as in rats. In mice, alpha-chlorohydrin was the major urinary metabolite, but in the rat metabolites included Cl-, 3-chlorolactate (BCLA) at 5 and 10 h and BCLA only at 24 h. BCLA was the major metabolite detected in most tissues at 10 and 24 h. In the rat cauda (but not caput) epididymidis the glycolytic inhibitor 3-chlorolactaldehyde was present at 5 h (but not 10 h), indicative of early metabolism. These results demonstrate a greater metabolism and excretion of putative antifertility agents in the mouse than the rat, lowering the amount of effective inhibitor circulating in the animal, which may explain why (R,S)-alpha-chlorohydrin and (R,S)-ornidazole are ineffective in this species at the dosages and injection times used, despite their spermatozoa being sensitive to inhibition by (R,S)-alpha-chlorohydrin in vitro.

Amebicides↗
PubMed1997

Toxicity of ornidazole and its analogues to rat spermatozoa as reflected in motility parameters.

Ornidazole, a 5-nitro-imidazole derivative, has contraceptive properties in rats. As some ornidazole passes through the body unmetabolized after administration, the aim of this study was to investigate if ornidazole itself has a direct effect on sperm motility and whether these effects are limited or potentiated by the epididymal epithelium or structural changes to the molecule. Cauda epididymal spermatozoa or cauda epididymal tubules were incubated with ornidazole or ornidazole analogues, and motility parameters were subsequently measured by means of a computer-assisted sperm analysis (CASA) system. Incubation of spermatozoa in 2.5 mmol/L ornidazole for 4 h reduced their motility significantly, whereas incubation of epididymal tubules for 8 h in 10 mmol/L ornidazole was required to alter the velocity parameters of the enclosed spermatozoa upon release, suggesting that extratubular non-metabolized ornidazole can participate in inhibiting the motility in vivo. The in vitro toxicity of ornidazole derivatives depends on the halogen present and on the position of the nitro-group. The putatively inactive (R)- and the active (S)-ornidazole exhibited equivalent depression of sperm motility by direct incubation. This observation, and the differences between the in vitro and the in vivo efficacies of various ornidazole analogues, indicates distinct mechanisms of motility inhibition in the two experimental systems.

Animals↗
PubMed2005

Ornidazole for prophylaxis of postoperative Crohn's disease recurrence: a randomized, double-blind, placebo-controlled trial.

BACKGROUND & AIMS: Crohn's disease almost inevitably recurs after ileocolonic resection, and effective prophylactic therapy has not been identified. We investigated the efficacy and safety of ornidazole, a nitroimidazole antibiotic, for the prevention of clinical recurrence of Crohn's disease after curative ileocolonic resection in a placebo-controlled double-blind clinical trial. METHODS: Eighty patients were randomized to ornidazole 1 g/day or placebo started within 1 week of resection and continued for 1 year. The primary end point was the proportion of patients with clinical recurrence at 1 year. Secondary end points were endoscopic recurrence at 3 months and 12 months after resection. RESULTS: Two patients in the ornidazole group withdrew consent and were not dosed. Ornidazole significantly reduced the clinical recurrence rate at 1 year from 15 of 40 (37.5%) patients in the placebo group to 3 of 38 (7.9%) patients in the ornidazole group (Fisher exact test, 8.03; P = .0046; odds ratio, 0.14; 95% confidence interval, 0.037-0.546). Ornidazole reduced endoscopic recurrence at 12 months from 26 of 33 (79%) in the placebo group to 15 of 28 (53.6%) in the ornidazole group (chi2 , 4.37; P = .037; odds ratio, 0.31; 95% confidence interval, 0.10-0.94). Endoscopic recurrence at 3 and 12 months predicted clinical recurrence. Significantly more patients in the ornidazole group dropped out from the study because of side effects (P = .041). CONCLUSIONS: Ornidazole 1 g/day is effective for the prevention of recurrence of Crohn's disease after ileocolonic resection.

Adult↗
PubMed2002

Giardiasis treatment in Turkish children with a single dose of ornidazole.

This study was designed to compare the treatment efficacy of single dose of ornidazole with 5 d treatments of ornidazole and metronidazole in children with giardiasis. 175 children, between 2 and 15 y old, whose stool samples were found to be positive for Giardia lamblia cysts and/or trophozoites by either saline-Lugol, formalin-ethyl acetate or trichrome staining, were enrolled in the study. Of these children, 105 were treated with a single dose of ornidazole: 35 with 30 mg/kg, 35 with 25 mg/kg and 35 with 20 mg/kg; 35 were treated with 25 mg/kg per day of ornidazole for 5 d in 2 doses and 35 children were treated with 20 mg/kg per day metronidazole for 7 d in 3 doses. All cases were examined on the 7th, 10th and 14th days after treatment by the same methods; clinical symptoms were also evaluated. Giardia lamblia was eradicated in 34 of 35 (97%), 34 of 35 (97%) and 33 of 35 (94%) patients treated with 30, 25 and 20 mg/kg single doses of ornidazole, respectively. Eradication was achieved in all 35 patients treated with 25 mg/kg per day ornidazole for 5 d and in 31 of 35 (89%) patients treated with metronidazole. There was no statistically significant difference among doses of ornidazole (p > 0.05); however, all ornidazole treatment regimens were significantly more effective than metronidazole treatment (p < 0.05). No important side-effects were detected in any patients and clinical symptoms disappeared in all. Single-dose ornidazole treatment could be considered as a proper and effective alternative method for the treatment of giardiasis in children.

Adolescent↗
PubMedDate not supplied

Studies on the development of colon targeted oral drug delivery systems for ornidazole in the treatment of amoebiasis.

The aim of the present study is to develop colon-targeted drug delivery systems for ornidazole using guar gum as a carrier. The core formulation containing ornidazole was directly compressed. Compression-coated tablets of ornidazole containing various proportions of guar gum in the coat were prepared. All the formulations were evaluated for hardness and drug content uniformity and were subjected to in vitro drug release studies. The amount of ornidazole released from tablets at different time intervals was estimated by the HPLC method. The compression-coated formulations released less than 8% of ornidazole in the physiological environment of stomach and small intestine. The compression-coated tablets with 85%, 75%, and 65% of guar gum coat released about 21%, 38%, and 73% of ornidazole, respectively, in simulated colonic fluids indicating the susceptibility of the guar gum formulations to the rat caecal contents. The results of the study show that compression-coated ornidazole tablets with either 65% (OLV-65) or 75% (OLV-75) of guar gum coat are most likely to provide targeting of ornidazole for local action in the colon owing to its minimal release of the drug in the first 5 hr. The ornidazole compression-coated tablets showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/75% relative humidity for 6 months.

Administration, Oral↗
PubMed2006

Treatment of rheumatoid arthritis with ornidazole: a randomized, double-blind, placebo-controlled study.

The aim of our study was to evaluate the clinical efficacy, safety, and tolerability of ornidazole in patients with rheumatoid arthritis (RA). This was 3 months, randomized, double-blind,placebo-controlled study. A total of 160 patients with active RA were randomly assigned to receive 1,000 mg ornidazole (n = 53), 500 mg ornidazole (n = 55), or placebo (n = 52). A significantly greater percentage of patients treated with 1,000 mg ornidazole met the American College of Rheumatology 20% improvement criteria (achieved an ACR20 response) at 3 months compared with patients who received placebo (62.0 vs. 32.4%; P < 0.001). Greater percentages of patients treated with 1,000 mg ornidazole also achieved ACR50 responses (38.3 vs. 10.9%; P < 0.001) and ACR70 responses (19.6 vs. 1.2%; P < 0.001) compared with patients who received placebo. Ornidazole treatment was also associated with significant reductions in pain and duration of morning stiffness, significant improvement in the quality of life and both the physician's and patient's global assessments, and significant reductions in disease activity as assessed by objective laboratory measures (erythrocyte sedimentation rate and C-reactive protein level). Ornidazole was well tolerated. There were no dose-limiting toxic effects. In this 3-month-trial ornidazole was safe, well tolerated, and associated with improvement in the inflammatory symptoms of RA.

Adult↗
PubMed1998

Treatment of bacterial vaginosis with oral or vaginal ornidazole, secnidazole and metronidazole.

OBJECTIVE: To evaluate the clinical efficacy and tolerance of oral or vaginal ornidazole, secnidazole and metronidazole or their combinations for treatment of bacterial vaginosis. METHOD: In an open, randomized, prospective study, 152 patients with bacterial vaginosis according to Amsel's criteria were included into the study. The patients were divided into eight groups: (1) oral ornidazole 2 x 500 mg/day for 5 days; (2) vaginal ornidazole 500 mg/day for 5 days; (3) oral and vaginal ornidazole for 5 days; (4) oral secnidazole 2 g in a single dose; (5) oral secnidazole 2 g in a single dose and vaginal ornidazole 500 mg/day for 5 days; (6) oral secnidazole 2 g in a single dose and vaginal metronidazole 2 x 500 mg/day for 7 days; (7) oral ornidazole 2 x 500 mg/day for 5 days and vaginal metronidazole 2 x 500 mg/day for 7 days; and (8) vaginal metronidazole 2 x 500 mg/day for 7 days. None of the partners received any treatment. RESULT: We found a 100% cure rate in both oral and vaginal ornidazole and oral secnidazole-vaginal metronidazole groups. CONCLUSION: Vaginal treatments including ornidazole and metronidazole are not as effective as both oral and vaginal drug combinations.

Administration, Intravaginal↗
PubMed1994

Induction of reversible infertility in male rats by oral ornidazole and its effects on sperm motility and epididymal secretions.

Ornidazole (400 mg kg-1 day-1) given by oral gavage rendered male rats infertile by 6.6 +/- 0.7 days (mean +/- SEM, n = 9, range 3-10) after beginning the treatment and fertility returned within 5-10 days after treatment with ornidazole for 6-7 days. At 200 mg ornidazole kg-1 day-1, fertility was reduced but total infertility was not achieved. No differences were found in the percentage motility of spermatozoa recovered from any region of the epididymides of ornidazole-treated rats compared with controls. However, computer aided sperm analysis revealed significantly lower straight-line and average path velocities in ornidazole-treated animals (400 mg kg-1 day-1) for spermatozoa from the distal regions of the tract than for controls. Curvilinear velocity was significantly lower than that of controls in the distal corpus and cauda regions. The motility characteristics of spermatozoa from animals receiving 200 mg ornidazole kg-1 day-1 were lower than, but not significantly different from, motility in controls. There were no differences between the total protein, L-carnitine, glycerophosphocholine or total alpha-glucosidase content in epididymal homogenates from fertile control and infertile ornidazole-treated animals. Spermatozoa released from the cauda epididymidis of untreated rats into ornidazole solutions displayed no changes in the percentage motility up to 20 mmol l-1 and were only depressed at 50 mmol l-1. All velocities revealed a biphasic response with an initial increase in motility and then inhibition at higher concentrations, but a significant difference from velocities in the absence of orindazole was evident only for straight line velocity (VSL) at 50 mmol l-1.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1989

High haemodialysis clearance of ornidazole in the presence of a negligible renal clearance.

The pharmacokinetics of ornidazole was studied in 6 patients treated by haemodialysis and in 8 subjects with a creatinine clearance between 4 and 99 ml/min x 1.73 m2. Blood and urine collections were performed for 72 h after i.v. and oral administration of 1.0 g ornidazole. Total body clearance, half-life, volume of distribution and systemic availability were independent of renal function and did not differ from previously reported values in normal volunteers. The haemodialysis clearance of ornidazole was greater than 100% higher than the total body clearance. The renal clearance of ornidazole accounted for less than 7% of the total body clearance. The percentage of the dose of ornidazole recovered in urine as parent compound or as the biologically active metabolites [alpha-(chloromethyl)-2 hydroxymethyl-5 nitroimidazole-1 ethanol and 3-(2 methyl-5 nitroimidazole-1-yl)1,2 propanediol] decreased linearly with decreasing renal function. Although the sum of those three compounds recovered in urine accounted for less than 10% of the total dose of ornidazole administered, they yielded therapeutic concentrations (greater than 4 micrograms/ml) in urine over 24 h after dosing. Due to the peculiar pharmacokinetic behaviour of ornidazole, i.e. high haemodialysis clearance in the absence of significant renal clearance, no dosage adjustment is necessary while renal function declines, but an increased dose is mandatory while patients are on dialysis.

Administration, Oral↗
PubMed2006

Antimicrobial drug ornidazole inhibits hamster sperm capacitation, in vitro.

To be fertilization competent, spermatozoa undergo a series of changes in the female reproductive tract collectively referred to as capacitation. In an attempt to understand, if ornidazole, a known anti-fertility drug, adversely affects sperm functions by targeting capacitation, we designed experiments to study the influence of this drug on hyperactivation (HA), capacitation-associated protein tyrosine phosphorylation (pY) and the acrosome reaction (AR). Addition of ornidazole at 0 h, inhibited the onset of HA and total pY in a dose dependent manner. However, when ornidazole was added at 3.5h, severe effects were still seen on HA and pY of high molecular weight proteins but, pY of lower M(r) proteins (50-56 kDa) was affected only marginally. Further, lower doses of ornidazole (5 and 10 mM) had greater inhibitory effect when added at 0 h, while addition of ornidazole at 3.5 h required higher doses of ornidazole (25 mM) to cause significant inhibition of acrosome reaction. Collectively, through in vitro studies, we demonstrate that ornidazole affects the onset and progression of hamster sperm hyperactivation, capacitation associated protein tyrosine phosphorylation and acrosome reaction, and the severity depends on the dose (5, 10 or 25 mM) and the time of addition (0 or 3.5 h) of the drug to the spermatozoa.

Acrosome Reaction↗
PubMed2003

In vivo evaluation of guar gum-based colon-targeted drug delivery systems of ornidazole in healthy human volunteers.

The aim of the present study was to find the in vivo performance of guar gum-based colon-targeted tablets of ornidazole (dose 250 mg) in comparison with an immediate release tablet of ornidazole (250 mg) in human volunteers. Six healthy volunteers participated in the study, and a cross over design was followed. The plasma concentration of ornidazole was estimated by HPLC. The immediate release tablets of ornidazole produced peak plasma concentration (Cmax of 2171.33+/-278.15 ng/ml) at 2.91+/-0.14 h (Tmax) whereas colon-targeted tablets produced peak plasma concentration (Cmax of 1716.66+/-125.83 ng/ml) at 11.91+/-0.14 h. The delayed Tmax, decreased Cmax, and decreased ka of ornidazole from guar gum-based colon-targeted ornidazole tablets, in comparison with the immediate tablets, indicated that the drug was not released in stomach and small intestine, but targeted to colon. Slow absorption of ornidazole from the less absorptive colon might result in the availability of drug for local action in the colon.

Adult↗
PubMed1993

Concentrations in plasma and tissue penetration of ceftriaxone and ornidazole during liver transplantation.

Plasma and epiploic fat drug concentrations and fat penetration of ceftriaxone and ornidazole given for antimicrobial prophylaxis were studied in 11 patients scheduled for liver transplantation. Ceftriaxone (1 g) and ornidazole (500 mg) were infused during 30 min after the induction of anesthesia. Arterial blood and epiploic fat samples were collected at 30, 60, and 120 min and then every 90 min following the end of the infusion until closure of the peritoneum. Blood samples were immediately centrifuged, and plasma and fat were stored at -35 degrees C until analysis. Ceftriaxone and ornidazole concentrations were determined by high-performance liquid chromatography. Surgery lasted 440 +/- 84 min and required a mean of 9.5 units of packed erythrocytes and 13 units of fresh frozen plasma. Plasma ceftriaxone concentrations decreased from 89 +/- 34 to 41 +/- 16.5 micrograms/ml from the beginning of the operation until the time of closure of the peritoneum. Corresponding levels in epiploic fat decreased from 8.7 +/- 3.3 to 4.5 +/- 3.5 micrograms/g. Ornidazole concentrations ranged, respectively, between 8.7 +/- 2.5 and 4.9 +/- 1.7 micrograms/ml in plasma samples and 4.6 +/- 1.2 and 2.5 +/- 1.1. micrograms/g in fat samples. Rates of penetration into the omentum remained at about 9% for ceftriaxone and between 50 and 70% for ornidazole. Tissue ceftriaxone concentrations were, in all cases, greater than typical MICs for 90% for Escherichia coli and Klebsiella isolates tested (MIC90S). They were insufficient in 40% of patients after 60 min with regard to the MIC90S for Staphylococcus aureus. Tissue ornidazole concentrations were not superior to MIC90S for anaerobes after 30 min in 50% of patients. These results show that a single dose of 1 g of ceftriaxone provides adequate coverage against gram-negative bacteria and that 1 g instead of 500 mg ornidazole may provide a protective effect against anaerobes during liver transplantation. Prophylaxis against S. aureus and Streptococcus faecalis requires more specific antibiotics. Prophylaxis for patients with significant blood loss or initial severe renal or hepatic failure needs further evaluation.

Adipose Tissue↗
PubMed1988

The effect of ornidazole on fertility and epididymal sperm function in rats.

A comprehensive study of male fertility and sperm production and function was performed in 20 control and 20 rats treated with ornidazole, a compound with trichomonacidal activity. Rats were treated for 4 weeks at dosages of 0 (control) and 400 mg/kg/day of ornidazole during which fertility was assessed by weekly matings. Testicular sperm production and epididymal sperm function were assessed in one-half of the rats while the reversibility of effects after a 2-week recovery period was assessed in the remaining half. Male rats treated with ornidazole were infertile during the second week of treatment. After 4 weeks of treatment, testicular and epididymal weights, testicular spermatid counts, epididymal sperm reserves, sperm morphology, and sperm viability were similar in treated and control rats. A quantitative assessment of epididymal sperm motility using a dark-field photomicroscope with a stroboscopic light source revealed that ornidazole markedly inhibited sperm motility. Although the percentage of nonmotile sperm was not substantially increased in treated rats, the vigor of tail movement was markedly decreased which resulted in decreased sperm velocity. Restoration of fertility and normal sperm motility and velocity were observed in the group of recovery rats assessed 2 weeks after the cessation of ornidazole treatment. It is concluded that ornidazole, at a high dosage of 400 mg/kg/day, produces infertility in male rats by inhibiting epididymal sperm motility in terms of decreased sperm velocity. These effects are rapidly reversible after the cessation of treatment.

Animals↗
PubMed1986

Use of ornidazole in fractionated radiotherapy: dose tolerance, serum and tumour tissue concentration.

Sensitizing and neurotoxic effect of ornidazole, was tested in a double-blind randomized study in patients with carcinoma of the cervix and larynx. Ornidazole or placebo were given orally, two times weekly, for 3 weeks. Dose was 2.5 g/m2 for each administration. Total dose given was 15 g/m2. Radiation therapy was given 3 h after the drug administration. Ornidazole was well tolerated in the majority of the patients. No neurotoxic side effects, such as peripheral neuropathy or convulsion, were observed with a total dose of up to 30 g. Dizziness, somnolence and nausea were the prominent acute side effects, seen mostly (70%) in women. In the placebo group this rate was 17% (p less than 0.01). No important side effect was observed in men receiving ornidazole. Serum concentration of ornidazole reached the maximum level in 2-4 h after oral administration and ranged (23 patients) from 65.1 to 139.8 micrograms/ml. Mean half-life was 15.6 +/- 2.8 h. Peak concentration in tumour tissue was achieved 1-3 h after the administration, ranging from 13.0 to 78.0 micrograms/g. Tumour concentration of ornidazole ranged from 14 to 93% of the serum concentration at the time of irradiation.

Adult↗
PubMed1995

Disposition of ornidazole and its metabolites during pregnancy.

The disposition of ornidazole and its two major hydroxylated metabolites was studied in five pregnant women (gestational ages 25 5/7 to 38 4/7 weeks) with either chorioamnionitis or pyelonephritis treated with ceftriaxone 2 g, tobramycin 3 mg/kg body weight and ornidazole 1 g all administered once-daily. Two series of blood samples were obtained, the first on the first day of treatment and the second at steady-state on day 5. Local and systemic tolerability of ornidazole was excellent and patients showed complete remission without premature delivery. There was no evidence of ornidazole accumulation, and the pharmacokinetic parameters were very similar to those seen in healthy subjects. The dosage regimen of ornidazole therefore requires no adjustment during pregnancy. Trough concentrations of ornidazole measured at 24 h post dose were above the MIC of sensitive organisms. Children born to the trial patients showed normal initial development and their growth was normal.

Adult↗
PubMed1985

Pharmacokinetics of ornidazole in patients with renal insufficiency; influence of haemodialysis and peritoneal dialysis.

The pharmacokinetics of ornidazole (Tiberal) was studied after intravenous administration of a single 500 mg dose in eight patients with advanced chronic renal failure (ACRF) (creatinine clearance 2-16 ml/min), in seven patients treated by haemodialysis (residual renal creatinine clearance 0-5 ml/min) and in five patients treated by continuous ambulatory peritoneal dialysis (CAPD) (residual renal creatinine clearance 0-6 ml/min). In ACRF patients, the half-life of ornidazole was 10.8 +/- 1.4 h, the total plasma clearance 46.3 +/- 2.3 ml/min and the volume of distribution 0.73 +/- 0.06 l/kg. During haemodialysis, ornidazole was partly removed: the dialyser extraction ratio was 42 +/- 5% and the dialysis clearance 64 +/- 7 ml/min. During CAPD, peritoneal excretion was low: the dialysis clearance was 3.0 +/- 0.4 ml/min and in 48 h 6.0 +/- 1.1% of the administered dose was found in the peritoneal fluids. In these patients, the half-life of ornidazole was 11.8 +/- 0.8 h and total plasma clearance was 48.3 +/- 5.5 ml/min, values which were close to those determined in non dialysed patients. In patients with end-stage renal disease, the half-life of ornidazole is comparable to that of subjects with normal renal function. This is due to the predominantly extra-renal elimination of the drug. Therefore, there is no need to modify the usual dosage of ornidazole for these patients. Because of the large elimination of the drug during haemodialysis it is necessary to administer the drug after the dialysis session.

Adult↗