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At least 19 recordsLinked to original sources

Blood kinetics of sulfamonomethoxine and oxytetracycline following intrauterine spray injection in dairy cows.

Intrauterine administration was performed in six Friesan cows with a disposable spray preparation containing 3 g of sulfamonomethoxine and 3 g of oxytetracycline, in order to investigate their serum kinetics. Sulfamonomethoxine levels were determined by a reversed-phase HPLC method, whilst oxytetracycline quantities were detected by a microbiological method. The sulphonamide had a peak 1.17 h after the administration, the tetracycline reached its highest concentration after 8 h. The bioavailability of both drugs was low and detectable drug amounts were no longer recovered after 24 h.

Animals↗

Comparison of the inhibitory effect of sulfamonomethoxine and other sulfonamides on capsule formation of Bordetella bronchiseptica.

The inhibitory effect of sulfamonomethoxine and other sulfonamides on the capsule formation of sulfonamide-resistant Bordetella bronchiseptica was investigated. All the sulfonamides having MeO(-OCH3) groups inhibited the capsule formation of B. bronchiseptica. Strong inhibition was obtained with sulfamonomethoxine. Inhibition was not seen with sulfonamides having no MeO groups.

Bacterial Capsules↗

Medication of feedlot calves infected with Eimeria spp. by a combination of sulfamonomethoxine and ormetoprim.

Feedlot calves naturally infected with Eimeria spp. were medicated by a combination of sulfamonomethoxine and ormetoprim (Ektecin). Calves, less than one year old and positive for coccidiosis, were administered with Ektecin (5, 10 and 20 ml/100 kg of body weight/day) and Daimeton (100% sulfamonomethoxine: 5 g/100 kg of body weight/day) for five days. No diarrhea were found on and after 3 days of medication in all the groups, and no oocysts were detected on and after day 5, 2, 1 or 3 from calves of the respective medicated groups. In samples from a group of calves administered with lowest dose of Ektecin, eimerian oocysts of 4 species were detected on day 0, and additionally 3 species (totally 7 species) were found on day 3 of medication.

Animals↗

A combination of sulfamonomethoxine and pyrimethamine versus other drugs for the treatment of malaria.

Sixty-eight cases of vivax and 30 cases of falciparum malaria patients were treated with a combination of sulfamonomethoxine-pyrimethamine (MP tablet with 500 mg of sulfamonomethoxine and 25 mg of pyrimethamine) and the results were compared with those with chloroquine, Fansidar and quinine. Vivax malaria: Fever and parasites were cleared by the 4th day of treatment in 94 and 92% of the patients, respectively. Chloroquine was the most effective drug and Fansidar and MP tablets shared the next position. Falciparum malaria: Fever and asexual parasites were cleared by the 4th day of treatment in 67 and 78% of the patients, respectively. MP tablets were effective in chloroquine-resistant falciparum malaria contracted in Kalimantan (Indonesia) and Oceanian countries (Vanuatu etc.). Fever and parasite clearance times were shorter with chloroquine or with Fansidar than with MP tablets. Defective preschizonts used to appear following administration of MP tablets both in vivax and falciparum malarias. They were the premonitory laboratory indications that the asexual parasites will be soon eradicated.

Adolescent↗

[Treatment of experimental glanders with combinations of sulfazine or sulfamonomethoxine with trimethoprim].

Combinations of sulfazine or sulfamonomethoxine with trimethoprim were found to be efficient in the prophylaxis and treatment of experimental glanders simulated by various strains and doses of the causative agent, the treatment being started and terminated at various periods. The efficacy indices and treatment schemes were elaborated. By the efficacy indices the sulfazine combination with trimethoprim was shown to be 2-3 times more efficient than the sulfamonomethoxine combination with trimethoprim.

Animals↗

Determining sulfamonomethoxine and its acetyl/hydroxyl metabolites in chicken plasma under organic solvent-free conditions.

A quantitative technique is described for a sample preparation followed by high performance liquid chromatography method for the simultaneous determination of sulfamonomethoxine and its metabolites, N4-acetyl SMM and 2,6-dihydroxy SMM, in chicken plasma. The average recoveries, analytical total time, and limits of quantitation were >/=80% (relative standard deviations (SD) </=6%), <30 min sample-1 (12 samples in 2 h), and </=0.09 microg ml(-1), respectively. The procedure, performed under 100% aqueous conditions, uses no organic solvents and toxic reagents at all and is, therefore, harmless to the environment and humans.

Animals↗

Antithyroid effects of propylthiouracil and sulfamonomethoxine in rats and monkeys.

Experiments were performed to investigate the species difference in antithyroid effects of propylthiouracil (PTU) and sulfamonomethoxine (SMM). Sprague-Dawley rats were administered 30 mg/kg of PTU, or 30 or 270 mg/kg of SMM orally for 5 weeks, while squirrel monkeys received 30 mg/kg of PTU or 270 mg/kg of SMM. In rats receiving 30 mg/kg of PTU, a decrease of both serum 3,5,3'-triiodothyronine and thyroxine concentrations and of 131I incorporation into the thyroid hormone precursors was observed, together with elevation of serum thyroid-stimulating hormone concentration, an increase in thyroid weight, and hyperplasia of the follicular epithelium of the thyroid gland. Similar changes were seen in rats receiving 270 mg/kg of SMM; however, the antithyroid effects of SMM were less severe than those of PTU. No change was produced in monkey thyroids by 5-week treatments with 30 mg/kg of PTU or with 270 mg/kg of SMM. The molar concentration of PTU required for the in vitro inhibition of thyroid peroxidase was markedly lower in rats than in monkeys. SMM showed a similar species difference in the inhibition of thyroid peroxidase in vitro, but the enzyme inhibition of SMM was weaker than that of PTU. These findings suggest that rats were more sensitive to the antithyroid effects of PTU and SMM than monkeys, and that inhibition of thyroid peroxidase may play an important role in species difference in the antithyroid effects of the two drugs.

Animals↗

High-performance liquid chromatographic method for the rapid and simultaneous determination of sulfamonomethoxine, miloxacin and oxolinic acid in serum and muscle of cultured fish.

A rapid method for the simultaneous determination of sulfamonomethoxine (SMM), miloxacin (MLX) and oxolinic acid (OA) in serum and muscle of cultured fish by high-performance liquid chromatography has been developed. A Hisep shielded hydrophobic phase column (15 cm x 4.6 mm I.D.) and a mobile phase of 0.05 M citric acid-0.2 M disodium hydrogenphosphate buffer, pH 2.5 in 10 mM tetra-n-butyl ammonium bromide-acetonitrile (85:15) with ultraviolet detection at 265 nm were used. The recoveries of SMM, MLX and OA from serum and muscle samples were 72-101%. The detection limits of the three drugs were 0.05-0.1 microgram/ml or g of sample.

4-Quinolones↗

Application of shielded column liquid chromatography for determination of sulfamonomethoxine, sulfadimethoxine, and their N4-acetyl metabolites in milk.

A hazardous-chemical free method for simultaneous determination of sulfamonomethoxine (SMM), sulfadimethoxine (SDM), and their N4-acetyl metabolites in raw milk using shielded column liquid chromatography is developed. The target analytes are extracted by mixing with ethanol-acetic acid (97:3, v/v) followed by centrifugation. The procedure uses a Hisep shielded hydrophobic phase (SHP) column, isocratic elution with 0.1% acetic acid solution (pH 3.1, in water)-ethanol (75:25, v/v), and a photo-diode array detector. Average recoveries from samples spiked at 25-500 ng/ml for each drug were >81% with relative standard deviations within 5%. The limits of quantitation were <25 ng/ml.

Animals↗

Inhibitory effect of sulfamonomethoxine on capsule formation of Bordetella bronchiseptica.

Bordetella bronchiseptica phase I organism possesses a capsule and has the ability to agglutinate with K antiserum, although phase III organism lacks both. The present study examines the effect of sulfamonomethoxine (SMMX) on capsule formation of B. bronchiseptica. I also investigated whether or not the organisms possessed a capsule by bacterial agglutination with K antiserum. Three SMMX-resistant strains of B. bronchiseptica phase I organisms showed loss of agglutinability with K antiserum by culturing them at a higher concentration of 1.56 micrograms/ml of SMMX. These results indicated that capsule formation of SMMX-resistant B. bronchiseptica is inhibited by SMMX.

Agglutination Tests↗

Role of deacetylation in the nonlinear pharmacokinetics of sulfamonomethoxine in pigs.

The role of deacetylation in the pharmacokinetics of sulfamonomethoxine (SMM) in pigs was studied using 6 Goettingen minipigs and a pig from a commercial breed. The rapid decrease of plasma concentration of the parent compound followed by the rapid increase of plasma concentration of the deacetylated metabolite, SMM, was observed after an i.v. injection of N4-acetylsulfamonomethoxine (AcSMM; 10 mg/kg). The concentration of the metabolite, SMM, was greater than that of AcSMM and after reaching peak, both compounds decreased in parallel on a semilogarithmic graph. On the other hand, the acetylated compound of SMM (AcSMM) appeared in the plasma and reached peak after an i.v. injection of SMM. After reaching the peak, both SMM and AcSMM decreased in parallel. The slopes of the terminal phases of SMM and AcSMM after both injections showed no significant difference. After the i.v. injection of a high dose of SMM (100 mg/kg), a nonlinear pharmacokinetics profile with capacity limited elimination type of SMM was observed. The concentration of plasma AcSMM increased rapidly and the parallel decrease of SMM and AcSMM was observed in both nonlinear and linear phases, while the renal excretion of AcSMM was saturated in the nonlinear phase. The results suggest that the deacetylation in pigs is so strong that it largely affected the pharmacokinetics of SMM in both high and low doses. In spite of the saturation in renal excretion of the main metabolite, AcSMM, after the high dose, the profile of the parallel decrease remained unchanged, which may be due to the rapid conversion of the excess AcSMM to SMM. The converted SMM was added to the existing plasma SMM. As a result, the nonlinear pharmacokinetics of SMM may have occurred after a high dose of SMM in pigs.

Acetylation↗

Possible active tubular secretion of sulfamonomethoxine and its metabolites in pigs.

The effect of probenecid on the plasma kinetics of sulfamonomethoxine (SMM) was examined in conscious pigs. A linear kinetic dose of SMM (10 mg/kg) was injected with or without probenecid. Probenecid (25 mg/kg, i.v.) was injected immediately before SMM injection and against at 1, 2, 3, 4 and 6 h later. The AUCs of SMM and of the acetylated compound of SMM (AcSMM) in probenecid injected animals were significantly larger when compared with those of non-injected animals (p less than 0.05). Next, possible active secretion from the renal tubule of SMM and its metabolites was examined using probenecid and pyrazinoate. Ten commercial pigs with ureter cannulae were used under anesthesia. The plasma concentration of SMM and AcSMM was maintained at a steady state by a priming dose of SMM (5 mg/kg, i.v.) followed by sustaining infusion (4 micrograms/kg/min). Renal clearance of AcSMM was suppressed by bolus injection of probenecid (25 mg/kg), but that of SMM was not. The renal excretion of a water soluble metabolite was suppressed by probenecid. No marked changes in renal excretory kinetics were found by pyrazinoate injection (12.5 mg/kg, i.v.). Consequently, the saturation in the active tubular secretion of AcSMM may play an important role in the nonlinear pharmacokinetics of SMM in pigs.

Acetylation↗

[Effect of sulfamonomethoxine and ormetoprim on leucocytozoon infection in chickens].

The preventive effect of sulfamonomethoxine (Smm) and ormetoprim (Omp) medicated in combination against leucocytozoon infection in chickens was tested in field trials. In trial 1, medication was given continuously throughout the experimental period. In trial 2, medication was given for seven days and no medication was given for the next seven days; then this schedule for the medication was repeated throughout the experimental period. In trial 1, almost complete prevention was obtained when Smm and Omp were added to the feed at the level of 12 ppm and 14 ppm, respectively, or at the level of 15 ppm and 5 ppm, respectively. Only a partial effect was obtained, however, when these drugs were used at the level of 9 ppm and 3 ppm, respectively. In trial 2, a nearly complete effect was obtained when Smm and Omp were added to the feed at the level of 18 ppm and 6 ppm respectively, but we found no effect when these drugs were used at the level of 15 ppm and 5 ppm, respectively. There were no significant differences among the groups as to the weight gain.

Animals↗

Plasma concentrations, plasma protein binding and residues of sulfamonomethoxine in pigs, horses and cattle.

The protein binding, the plasma half-life and the residue depletion of sulfamonomethoxine (SMM) after intramuscular administration were investigated in pigs, horses and cattle. Protein binding was weakly concentration-dependent. The bound fraction in plasma in the therapeutic range amounted to approximately 45, 40 and 50% for pigs, horses and cattle respectively, and the plasma half-lives were approximately 5.1, 5.7 and 3.1 hours respectively. SMM levels were less than 1 mug/g in muscle tissue after 36, 20 and 12 hours in pigs, horses and cattle respectively. In the kidney SMM levels were not less than 1 mug/g until 48, 60 (extrapolated) and 36 (extrapolated) hours respectively. In pigs and horses SMM residues in the injection site were extremely variable. In cattle, SMM disappearance from the injection site was more regular. SMM concentrations in pig, horse and cattle liver remained more or less constant in the latter part of the period investigated.

Animals↗

[Human pharmacokinetic characteristics of sulfamonomethoxine depending on the drug form].

Comparative study of sulfamonomethoxin pharmacokinetics in the man given the drug per os or parenterally in the form of methylglucaminate showed that the latter favours higher blood concentrations of the drug 12 hours following injection. Sulfamonomethoxinmeglumin is absorbed more rapidly and has a greater bioavailability. The drug is mainly excreted with urine, more than a half being excreted in an acetylated form. It is recommended that the initial and maintenance doses be not less than 1000 and 500 mg for both dosage forms respectively. The interval between sulfanilamide administrations should not exceed 24 hours.

Adult↗

[Several indices of the functional state of the adrenals of white rats during a prescribed course of sulfadimezine and sulfamonomethoxine combined with UV-irradiation].

Chronic treatment with sulfadimesin or sulfamonomethoxin combined with UV irradiation leads to potentiation of adrenocortical function. As the observation period increases, the weight ratios of the adrenals grow which is accompanied by the decreased content of ascorbic acid in them and by the reduced weight ratios of the goiter and spleen. Combined chronic use of sulfanilamides and UV irradiation results in an increase of the total acetylating capacity of the body, especially in the day time.

Acetylation↗