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At least 19 recordsLinked to original sources
PubMed1991

The safety of dimetridazole alone and in conjunction with oxytetracycline in Hereford crossbred steers.

Dimetridazole was given intraruminally alone, and in conjunction with oxytetracycline to healthy, 10-11 month-old Hereford cross-bred steers (n = 6). Intraruminal treatment with dimetridazole was given through a fistula at 75 mg kg-1 daily for 5 d, while the oxytetracycline was injected intramuscularly at 10 mg kg-1 on Days 1 and 3 of the dimetridazole treatment. The animals were observed at various intervals throughout the trial period for adverse reactions, including effects on ruminal activity and motility, changes in live-mass, venous acid-base balance, haematology and ruminal and serum ammonia concentrations. Dimetridazole, either when used alone or in conjunction with oxytetracycline, had a marked effect on ruminal function. Within 6 h of dosing, the ruminal pH fell to below 5, but then returned to pretreatment values over the next 24-48 h. This was followed by the eradication of the ruminal protozoal population in all animals tested and an increase in the methylene blue reduction time to more than 6 min. Ruminal motility remained unaffected throughout this period. During the week of treatment, the mean live-mass of the animals dropped by 20 +/- 9.9 kg in the dimetridazole treated group and by 13.3 +/- 2.8 kg in the animals treated with both dimetridazole and oxytetracycline. A mild to severe watery diarrhoea, which continued for 1 to 2 d, occurred in 4 animals after the first dimetridazole treatment. A compensated metabolic acidosis and an increase in haematocrit were observed. An initial transient rapid rise in rumen ammonia concentrations did not result in a concurrent rise in serum ammonia concentrations.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1996

Pharmacokinetics and anti-trichomonal efficacy of a dimetridazole tablet and water-soluble powder in homing pigeons (Columba livia).

The anti-trichomonal efficacy and pharmacokinetics of dimetridazole were investigated in the homing pigeon (Columba livia). Dimetridazole was formulated for drinking water medication and as a prolonged-release tablet. To suppress a Trichomonas gallinae infection successfully, medicated drinking water containing dimetridazole (400 mg/L) had to be administered for at least 3 days. A two-day treatment with a dimetridazole tablet (20 mg/tablet) in fasted, as well as in fed, pigeons was shown to be ineffective. After intravenous administration of 20 mg dimetridazole, the drug plasma concentration-time profile fitted a one-compartment open model with a mean half-life of 3.9 h. The absolute bioavailability of the tablet in fasted pigeons was 83.8%. The bioavailability of the tablet administered with food was reduced by 20%. Dimetridazole was rapidly metabolised to (1-methyl-5-nitroimidazol-2-yl) methanol.

Animals↗
PubMed1987

Chemical and biological properties of acetyl derivatives of the hydroxylamino reduction products of metronidazole and dimetridazole.

Metronidazole and related 5-nitroimidazoles undergo reduction of their nitro group apparently to produce such reactive species as 5-hydroxylaminoimidazoles. To define the role of these species we have sought ways to prepare them by the catalytic reduction of metronidazole, dimetridazole and flunidazole. Although their respective 5-hydroxylaminoimidazoles were too unstable to be isolated directly, their O,N-diacetyl derivatives were isolable. Of these, the diacetyl derivative of the hydroxylamine derived from dimetridazole, O,N-diacetyl-1,2-dimethyl-5-hydroxylaminoimidazole (DiacDMH), was used for further study. DiacDMH was converted to its monoacetyl derivative, N-acetyl-1,2-dimethyl-5-hydroxylaminoimidazole (AcDMH), by enzymatic deacylation. Both DiacDMH and AcDMH were examined for bactericidal activity against such strains as Bacteroides fragilis, Clostridium perfringens, and Escherichia coli strain SR58, which are known to be sensitive to dimetridazole, as well as a variety of other bacteria. No bactericidal activity was detected, even in the presence of deacetylating enzymes. As the 5-hydroxylaminoimidazole itself could not be shown to form in these bacterial incubations, it remains uncertain whether or not the hydroxylamino functionality of a 5-nitroimidazole has bactericidal activity.

Acetylation↗
PubMed1977

The effect of the nitroimidazole drug dimetridazole on microaerophilic campylobacters.

Dimetridazole, a nitroimidazole drug reported to act only on obligately anaerobic micro-organisms, is widely used for the prevention and treatment of swine dysentery. Forty-four strains of the microaerophilic bacterium Campylobacter coli isolated from either healthy or diseased pigs, and a strain of Campylobacter fetus, were all sensitive to dimetridazole. The sensitivities (minimal inhibitory concentration less than 10 microng per ml) were similar to those of anaerobic bacteria. Dimetridazole inhibited growth of campylobacters in a shaken culture in air, but did not inhibit uptake of oxygen. Inhibition of growth appeared to result from an inhibition of nucleic-acid synthesis and does not seem to depend upon interference with electron transport in the catabolism of pyruvate.

Animals↗
PubMed1988

The use of metronidazole, tinidazole and dimetridazole in eliminating trichomonads from laboratory mice.

Metronidazole, tinidazole and dimetridazole were administered in the drinking water for 5 days to mice experimentally infected with Tritrichomonas muris and Tetratrichomonas microta. Mice were successfully infected with T. muris and T. microta recovered from infected gerbils. The trichomonas infection was successfully eliminated in mice given a 1% sucrose solution containing 2.5 mg/ml metronidazole or tinidazole. Mice receiving 1.0 mg/ml metronidazole, 1.0 mg/ml tinidazole and 1.2, 5.0 and 10.0 mg/ml dimetridazole failed to eliminate the trichomonas organism. A reduction in water intake was only noted with mice receiving 10 mg/ml dimetridazole. In mice receiving only 1% sucrose the infection was not eliminated.

Animals↗
PubMed1979

Effect of intestinal flagellate Spironucleus (Hexamita) muris and of dimetridazole on intestinal microflora in thymus-defficient (nude) mice.

Two groups of the intestinal microflora, the lactobacilli and the coliforms, were examined in thymus-deficient (nude) mice during the development of an experimental infection with the intestinal flagellate Spironucleus (Hexamita) muris and during the treatment with dimetridazole. The observed significant decrease in the number of lactobacilli under infection was probably due to the fact that the protozoan parasite fed on the microbes. Dimetridazole (0.3% in drinking water) did not influence the quantity of the lactobacilli but, owing to its selective killing of anaerobes and the lack of their antagonistic activity, a 100- to 1000-fold rise in the number of coliform microbes was observed. No of the drugs tested (dimetridazole, ornidazole, metronidazole, tinidazole, carbimazole BP and chlormethoxy-acridilamino-diethylamino-propanol-dihydrochliorde) was fully successful in the treatment of experimental spironucleosis in mice (Kunstýr, 1978) and it is suggested that recent reports on the therapeutic success of tinidazole in human giardiasis be treated with caution.

Animals↗
PubMed1991

Chromatographic and spectroscopic characterization of sulphur-bound dimetridazole and ranidazole derivatives.

The 5-nitroimidazoles, dimetridazole and ronidazole, two important veterinary drugs, were reacted under reductive conditions with the sulfhydryl-containing substrates cysteine and glutathione to yield 5-amino-4-S-substituted imidazoles. After purification by reversed-phase liquid chromatography (RP-LC), the four adducts were characterized by RP-LC with photodiode array detection using conditions where their parent drugs were not eluted from the column. Structural identification was conducted by spectroscopic techniques, mainly 1-dimensional and 2-dimensional NMR. While the dimetridazole adducts were found to be monosubstituted at the C-4 position, the two ronidazole products contained two units of the sulfhydryl substrate, located at the C-4 and C-6 positions.

Chromatography, Liquid↗
PubMed1978

Effect of dimetridazole on transmission of Histomonas meleagridis by Heterakis gallinarum.

The administration of an antihistomonal drug, dimetridazole, at a dose of 0.08% in feed, controlled experimental infections with Histomonas meleagridis in chickens. The treated birds developed no lesions and the duration of infection with H. meleagridis was reduced. This drug regimen, however, did not always prevent incorporation of H. meleagridis into eggs of Heterakis gallinarium; heterakid eggs pooled from medicated chickens in which H. meleagridis had never been detected transmitted the protozoan to 1 of 10 turkeys fed the eggs. Thus, therapeutic treatment of chickens with dimetridazole may reduce, but not eliminate, transmission of H. meleagridis by eggs of H. gallinarum from medicated birds.

Animals↗
PubMed1997

Determination of dimetridazole in poultry tissues and eggs using liquid chromatography-thermospray mass spectrometry.

A method is presented for the determination of the nitroimidazole drug dimetridazole (DMZ) in poultry tissues and eggs by liquid chromatography (LC)-thermospray mass spectrometry (MS). Deuteriated DMZ was employed as an internal standard. Samples were extracted with dichloromethane (muscle) or toluene (liver, egg) and applied to silica gel cartridges. Dimetridazole was eluted with acetone and the eluate evaporated to dryness at 40 degrees C under nitrogen. The residue was redissolved in methanol-water (1 + 1, v/v) and washed with hexane before LC-MS analysis. Quantification was by the ratios of the positive [M + H]+ ions at m/z 142 and 145 for DMZ and the internal standard, respectively. Internal standard corrected recoveries were between 93 and 102% with RSDs between 1.2 and 7.7% for liver spiked at 5, 10 and 20 ng g-1 and muscle and eggs spiked at 5 ng g-1. Absolute recoveries were approximately 80%. The method is suitable for statutory residue testing and was used to measure DMZ residues in eggs from chickens fed a diet containing DMZ at 10 mg kg-1.

Animals↗
PubMedDate not supplied

Gas chromatographic determination of incurred dimetridazole residues in swine tissues.

A gas chromatographic method for determination of 2-hydroxymethyl-1-methyl-5-nitroimidazole (DMZOH), the hydroxy metabolite of dimetridazole, in swime muscle has been developed. The method uses cleanup steps similar to those of an earlier polarographic method. The present method is capable of quantitating levels as low as 2 ppb and detecting less than 1 ppb. Recoveries from 30 control tissues spiked at 1, 2, or 4 ppb averaged 80.4%. Performance of the method in incurred tissue was documented and limited data on the depletion of the metabolite in muscle were generated. The muscle of swine given 150 ppm dimetridazole in feed for 14 days contained less than 1 ppb DMZOH at 12 h withdrawal time.

Animals↗
PubMedDate not supplied

Dimetridazole residues in pork tissue. II. Application of liquid chromatographic method to monitor elimination of drug and its major metabolite.

A study was conducted to monitor the elimination of dimetridazole (DMZ) and its major metabolite 2-hydroxymethyl-1-methyl-5-nitroimidazole (HMMNI) in swine plasma and tissue, using a liquid chromatographic method with electrochemical detector sensitive to 0.5 ppb. The study consisted of 2 experiments. In the preliminary experiment, one young female piglet was fed medicated ration containing 125 ppm dimetridazole (DMZ) for 2 weeks, followed by a withdrawal period using regular ration for 5 days. Another, control, piglet was given regular diet throughout. Plasma concentrations of DMZ and its most important residue, HMMNI, were measured daily at 2 h after the morning feeding and, on days 8 and 15, several times during the day. The 2 h concentrations after 3 days loading ranged from 47 to 77 ppb for DMZ and 424 to 1081 ppb for HMMNI. A daily cycle in the plasma levels was seen for both substances. Upon withdrawal of medication, elimination of drug and metabolite was biexponential with a terminal half-life of 6.7 h. In the second experiment, 5 piglets were medicated as above and slaughtered 2, 6, 12, 25, and 49 h after withdrawal of the medication; the concentration of DMZ and HMMNI was measured in plasma, muscle, kidney, and liver. DMZ in the plasma amounted to 22 and 1.8 ppb at 2 and 6 h, while HMMNI declined from 535 ppb at 2 h to 0.75 ppb at 25 h. Most values for both substances found in muscle were close to those in the plasma; in kidney they amounted to 9-17% of the plasma levels.(ABSTRACT TRUNCATED AT 250 WORDS)

Animal Feed↗
PubMedDate not supplied

Determination of dimetridazole and ipronidazole in feeds at cross-contamination levels.

A rapid method for the determination of dimetridazole and ipronidazole in feeds is described. The compounds are extracted from a borate buffer (pH 8.65) with benzene, partitioned into 1N HCl, and then partitioned back into benzene from a basic aqueous phase. The benzene extract is concentrated and injected onto a nonpolar (Apiezon L) gas chromatographic column for determination by 63Ni electron-capture detection. Recoveries from feeds of various composition, spiked at 0.2 ppm with both dimetridazole and ipronidazole, ranged from 70 to 115%; for the same feeds spiked at 1 ppm or more, the recoveries were greater than 80%. Carbadox, furazolidone, levamisole, oxytetracycline, chlortetracycline, sulfamethazine, sulfaquinoxaline, arsanilic acid, piperazine, penicillin, and commonly added vitamins and minerals do not interfere. A 2-dimensional thin layer chromatographic system is presented as a means of additional identification.

Animal Feed↗
PubMed1996

Residues of dimetridazole in eggs after treatment of laying hens.

Laying hens were dosed orally with dimetridazole (DMZ) (50 and 250 mg/kg) for 3 days or intramuscularly (50 mg/kg), also for 3 days, and the residues were determined by liquid chromatography in albumen and yolk. The sensitivity of the whole procedure was 2 ng/g. The drug was excreted preferentially into the yolk (about 57% of the total) and the elimination period lasted for 4-6 days after treatment.

Administration, Oral↗
PubMed1997

Evaluation of the genotoxic activity of metronidazole and dimetridazole in human lymphocytes by the comet assay.

The genotoxicity of metronidazole (MZ) and dimetridazole (DZ) has been evaluated in human lymphocytes using the comet assay. The test has been performed using 3 doses (58.4, 175.2 and 292.1 microM for MZ; and 70.9, 212.6 and 354.3 microM for DZ) under 3 experimental protocols: aerobiosis, anaerobiosis (90% N2, 10% CO2) and with the presence of the microsomal fraction S9 mix. The effects of 4 antioxidants (8-hydroxyquinoline (8HQ), vitamin C (VitC), catalase (CAT) and superoxide dismutase (SOD), have been investigated on DNA damage generated by fixed concentrations of MZ (292.1 microM) and DZ (354.4 microM). In aerobic conditions, MZ and DZ produced significant dose-response relationships. The dose-related effects of both drugs decreased or were abolished in anaerobic conditions or in presence of S9 mix. 8HQ, VitC, CAT and SOD induced dose-related protective responses against DNA damage due to MZ and DZ. These findings suggest that MZ and DZ induce DNA damage in human lymphocytes through the futile cycle. The one-electron reduction of the drugs leads to the production of nitro radical anions. In the presence of oxygen, these radicals are reoxidized and generate oxygen-activated species.

Animals↗
PubMed1998

Determination of dimetridazole, ronidazole and their common metabolite in poultry muscle and eggs by high performance liquid chromatography with UV detection and confirmatory analysis by atmospheric pressure chemical ionisation mass spectrometry.

A method was developed for the determination of the nitroimidazole compounds dimetridazole (DMZ) and ronidazole (RNZ) and their common metabolite, 2-hydroxymethyl-1-methyl-5-nitroimidazole (2-OH-M). Extracts obtained from a clean-up process using strong cation exchange (SCX) solid phase extraction (SPE) can be analysed either by high performance liquid chromatography with UV detection (HPLC-UV) or by high performance liquid chromatography with atmospheric pressure chemical ionisation mass spectrometry (HPLC-APCI-MS) as a confirmatory method. Up to 20 samples can be extracted in approximately 4 h. The HPLC-UV analysis had a limit of detection of 0.5 microgram kg-1. Validation in chicken muscle fortified at a concentration of 5 micrograms kg-1 gave recoveries of 75% DMZ, 77% RNZ and 81% 2-OH-M with RSDs of 16.4, 11.3 and 14.0%, respectively (n = 17). Validation in egg fortified at the same concentration gave recoveries of 77% DMZ, 80% RNZ and 80% 2-OH-M, with RSDs of 14.9, 22.0 and 18.2%, respectively (n = 18). The limit of detection of the HPLC-APCI-MS method was 0.1 microgram kg-1 for DMZ and RNZ and 0.5 microgram kg-1 for 2-OH-M. This method gave mean recoveries in fortified egg samples of 65% DMZ, 87% RNZ and 75% 2-OH-M with RSDs of 22, 11 and 14%, respectively (n = 10). The ratios of the peak areas of the molecular ion and a fragment ion were monitored as added confirmation of the presence of the analyte. Both the HPLC-UV screening procedure and the HPLC-APCI-MS confirmatory method have subsequently been used for the analysis of several hundred samples as part of UK surveillance programmes.

Animals↗
PubMedDate not supplied

The identification and assay of 2-methyl-5-nitroimidazole in pigs treated with dimetridazole.

An unidentified metabolite of dimetridazole (DMZ), found in pig plasma, muscle and kidney, was shown by chromatography and spectroscopy to be 2-methyl-5-nitroimidazole (2-MNI), resulting from N-demethylation of DMZ. This route of degradation competes with the oxidation pathway previously described. The concentration of 2-MNI in the plasma of pig fed medicated diet (DMZ 0.0125%) ranged from 29 to 83 ppb, 2 hours after the morning meal, similar to DMZ, but lower than that of the major metabolite, 2-hydroxymethyl-1-methyl-5-nitroimidazole (HMMNI). Its elimination profile in plasma was biphasic, similar to those of HMMNI and DMZ. Early and terminal half lives were 2.6 and 9.1 h respectively. None of the metabolites could be detected in any of the tissues studied 49 hours after withdrawal.

Animals↗
PubMedDate not supplied

Tissue concentration of dimetridazole in laying hens.

After laying hens had been dosed orally with dimetridazole (DMZ) for 3 days (50 and 250 mg/kg body weight (b.w.)) or intramuscularly, also for 3 days (50 mg/kg b.w.), the residues were determined in serum, liver, breast and thigh muscle by liquid chromatography. The limit of determination was 0.01 micrograms/g. The maximum concentration of DMZ was found at 1 h following application. After oral doses (50 and 250 mg/kg b.w.) no residues were found in muscle (breast and thigh) at 48 and 72 h, respectively. After intramuscular injection, residues in thigh muscle were below 0.01 micrograms/g at 72 h but breast muscle (injection site) still had concentrations above this level. Bioavailability (F > 80%) and some pharmacokinetic parameters were determined. The elimination half-lives from serum were 2.56h and 2.69h, after both oral doses, respectively, and 2.88 h after intramuscular application.

Administration, Oral↗
PubMed1979

Sensitivity in vitro to dimetridazole of treponemes associated with swine dysentery.

The minimum inhibitory concentration (MIC) of dimetridazole (DMZ) against Treponema hyodysenteriae (55 isolates) obtained over the period 1974-77 from individual pigs with swine dysentery from 41 herds where DMZ had been in use was determined. The MIC was less than or equal to 5.0 microgram per ml for 54 of the isolates and differences in the distribution of MICs between the annual sampling periods were not significant (P less than 0.05). There was no decrease in sensitivity of T hyodysenteriae to DMZ during the survey.

Animals↗