lasalocid and salinomycin

Topics: Animals; Chickens; Chromatography, Liquid; Coccidiosis; Eggs; Food Analysis; Humans; Lactones; Lasalocid; Liquid-Liquid Extraction; Monensin; Nigericin; Piperidines; Poultry; Pyrans; Quinazolinones; Robenidine; Tandem Mass Spectrometry; United States; United States Food and Drug Administration

An analytical method was developed and validated for the determination of three polyether ionophores (monensin, lasalocid, and salinomycin) in 60 samples of Brazilian Minas Frescal cheese by UHPLC-MS/MS. Linearity ranged from 1 to 8 μg kg

Topics: Brazil; Cheese; Chromatography, High Pressure Liquid; Food Contamination; Ionophores; Lasalocid; Monensin; Pyrans; Tandem Mass Spectrometry

Topics: Antineoplastic Agents; Betulinic Acid; Cell Line, Tumor; Cell Proliferation; Cell Survival; Ethers; Humans; Ionophores; Lasalocid; Molecular Structure; Monensin; Pentacyclic Triterpenes; Polymerization; Pyrans

Ionophore antimicrobials are heavily used in the livestock industries, both for preventing animal infection by coccidia protozoa and for increasing feed efficiency. Ionophores are excreted mostly unmetabolized and are released into the environment when manure is land-applied to fertilize croplands. Here, an analytical method was optimized to study the occurrences of five ionophore residues (monensin, lasalocid, maduramycin, salinomycin, and narasin) in dairy manure after solid-liquid separation and further treatment of the liquid manure by a membrane-based treatment system. Ionophore residues from the separated solid manure (dewatered manure) and suspended solids of manure slurry samples were extracted using ultrasonication with methanol, followed by sample clean-up using solid phase extraction (SPE) and subsequent analysis via liquid chromatography-tandem mass spectrometry (LC-MS/MS). The use of an ethyl acetate and methanol (1:1 v:v) mixture as an SPE eluent resulted in higher recoveries and lower method quantitation limits (MQL), when compared to using methanol. Overall recoveries from separated solid manure ranged from 73 to 134%. Liquid manure fractions were diluted with Nanopure™ water and cleaned up using SPE, where recoveries ranged from 51 to 100%. The developed extraction and LC-MS/MS methods were applied to analyze dairy manure samples subjected to an advanced manure treatment process involving a membrane-based filtration step (reverse osmosis). Monensin and lasalocid were detected at higher concentrations in the suspended solid fractions (4.40-420 ng/g for lasalocid and 85-1950 ng/g for monensin) compared to the liquid fractions (

Topics: Animals; Anti-Infective Agents; Cattle; Chromatography, Liquid; Coccidia; Coccidiosis; Ionophores; Lactones; Lasalocid; Manure; Methanol; Monensin; Pyrans; Solid Phase Extraction; Tandem Mass Spectrometry

A confirmatory multi-residue method was developed for the determination in milk of 19 coccidiostats (amprolium, arprinocid, clazuril, clopidol, decoquinate, diclazuril, ethopabate, halofuginone, lasalocid, maduramicin, monensin, narasin, nicarbazin, nequinate, robenidine, salinomycin, semduramicin, toltrazuril sulfone and toltrazuril sulfoxide). Sample preparation utilising extraction with organic solvent and clean up by SPE and freezing was found reliable and time-efficient. Optimised chromatography and MS conditions with positive and negative ESI achieved sufficient sensitivity and selectivity. Validation experiments has proven method usefulness for routine analysis of coccidiostats in milk samples. An on-farm study conducted on dairy cows fed with experimentally contaminated feed with salinomycin and lasalocid showed negligible transfer to milk. No residues of lasalocid were found in collected samples. Salinomycin was found only in 5 of 168 samples analysed, while the concentrations of salinomycin in those samples (0.119-0.179 µg kg

Topics: Animal Feed; Animals; Cattle; Coccidiostats; Drug Residues; Food Contamination; Lasalocid; Milk; Pyrans

Topics: Animals; Anti-Bacterial Agents; Biofilms; Cattle; Female; Gram-Positive Bacteria; Ionophores; Lasalocid; Mastitis, Bovine; Microbial Sensitivity Tests; Monensin; Pyrans; Staphylococcal Infections; Staphylococcus; Streptococcal Infections; Streptococcus

Chemotherapeutic treatment of human and animal trypanosomiasis is unsatisfactory because only a few drugs are available. As these drugs have poor efficacy and cause adverse reactions, more effective and tolerable medications are needed. As the polyether ionophore antibiotic lasalocid acid is used as medicated feed additive in cattle, the compound was tested for its trypanocidal and cytotoxic activity against bloodstream forms of Trypanosoma brucei and human myeloid HL-60 cells. The concentrations required of lasalocid acid to reduce the growth rate of trypanosomes by 50% and to kill the parasites were 1.75 and 10 μM, respectively. The ionophore displayed also cytotoxic activity against HL-60 cells but the human cells were about 10 to 14 times less sensitive indicating moderate selectivity. As the trypanocidal mechanism of action of polyether ionophore antibiotics is due to a sodium influx-induced cell swelling, the effect of lasalocid acid on cell volume change in bloodstream-form trypanosomes was investigated. Interestingly, lasalocid acid induced a much faster cell swelling in trypanosomes than the more trypanocidal related ionophore salinomycin. These results support further investigations of lasalocid acid and derivatives thereof as potential agents against African trypanosomiasis.

Topics: Animals; Cattle; Cell Line, Tumor; Cell Size; HL-60 Cells; Humans; Ionophores; Lasalocid; Pyrans; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosomiasis, African

Hydrolytic and photolytic degradation were investigated for the ionophore antibiotics lasalocid, monensin, salinomycin, and narasin. The hydrolysis study was carried out by dissolving the ionophores in solutions of pH 4, 7, and 9, followed by incubation at three temperatures of 6, 22, and 28 °C for maximum 34 days. Using LC-MS/MS for chemical analysis, lasalocid was not found to hydrolyse in any of the tested environments. Monensin, salinomycin, and narasin were all stable in neutral or alkaline solution but hydrolysed in the solution with a pH of 4. Half-lives at 25 °C were calculated to be 13, 0.6, and 0.7 days for monensin, salinomycin, and narasin, respectively. Absorbance spectra from each compound indicated that only lasalocid is degraded by photolysis (half-life below 1 h) due to an absorbance maximum around 303 nm, and monensin, salinomycin, and narasin are resistant to direct photolysis because they absorb light of environmentally irrelevant wavelengths.

Topics: Anti-Bacterial Agents; Half-Life; Hydrogen-Ion Concentration; Ionophores; Lasalocid; Models, Chemical; Monensin; Photolysis; Pyrans; Temperature; Water Pollutants, Chemical

A published confirmatory method for the quantitative determination of four ionophoric coccidiostats (lasalocid, monensin, salinomycin and narasin) in eggs and broiler meat has been further developed. It is proposed for replacement of liquid chromatography methods previously used in analysis of ionophoric coccidiostats. The samples were extracted with acetonitrile and purified on a silica solid phase extraction column. Purified samples were analysed by liquid chromatography-mass spectrometry and the method, was validated according to the Commission Decision 2002/657/EC. The validation parameters selectivity, linearity, specificity, precision, recovery, decision limit (CCalpha) and detection capability (CCbeta) were determined. The recoveries of coccidiostats analysed ranged from 64-99% in eggs and 62-100% in broiler meat. CCalpha varied from 0.8-1.4 microg/kg in eggs and from 1.5-2.5 microg/kg in broiler meat. CCbeta varied from 0.9 microg/kg to 2.0 microg/kg in eggs and from 1.7-3.2 microg/kg in broiler meat.

Topics: Animals; Chickens; Chromatography, Liquid; Coccidiostats; Eggs; Food Contamination; Lasalocid; Mass Spectrometry; Meat; Monensin; Pyrans; Reproducibility of Results

A sensitive and selective liquid chromatographic tandem mass spectrometric method (LC/MS/MS) for the simultaneous detection of the ionophoric coccidiostats narasin, monensin, lasalocid and salinomycin in whole eggs has been developed. A very simple sample preparation consisting of an extraction with an organic solvent was carried out. Sample extracts were injected into the LC/MS/MS system on a C18 column and an isocratic elution was performed. Nigericin was used as internal standard. The precursor ions produced by electrospray positive ionisation were selected for collisional dissociation with argon into product ions. Validation of the methods was performed based on Commission Decision 2002/657/EC.1 CC(alpha) was found to be 1 microg/kg for all four compounds. Monitoring of Belgian egg samples in 2004 revealed that residues of salinomycin, lasalocid and monensin could be found.

Topics: Animals; Chromatography, High Pressure Liquid; Coccidiostats; Eggs; Food Contamination; Ionophores; Lasalocid; Monensin; Pyrans; Spectrometry, Mass, Electrospray Ionization

A survey of the presence of residues of anticoccidials was performed. Three hundred and twenty egg samples, purchased in eight different European countries, were analysed for the presence of nine different compounds: dimetridazole, diclazuril, halofuginone, robenidine, nicarbazin, narasin, salinomycin, lasalocid and monensin. Analyses were performed by LC-MS/MS. Of the samples analysed, 114 (35.6%) contained one or more of the nine anticoccidials in concentrations ranging from 0.1 to 63 microg kg-1. Salinomycin and lasalocid account for more than 60% of all positive samples. Almost 90% of all positive samples contained less than 2 microg kg-1. Results were put into perspective of the farming method and country of origin.

Topics: Animal Husbandry; Animals; Chromatography, Liquid; Coccidiostats; Drug Residues; Eggs; Europe; Food Analysis; Humans; Lasalocid; Mass Spectrometry; Pyrans

Eimeria parasites were isolated from Nanhai Guangdong province (southern China) and studied in chickens in wire cages to evaluate their drug resistance against commonly used ionophores: monensin (100 mg/kg of feed), lasolacid (90 mg/kg), salinomycin (60 mg/kg), maduramicin (5 mg/kg) and semduramicin (25 mg/kg). Chinese Yellow Broiler Chickens were infected with 40,000 crude sporulated Eimeria oocysts at 15 days of age and prophylactic medication commenced a day prior to infection. Drug resistance was assessed for each ionophore drug by calculating the anticoccidial index (ACI) and percentage optimum anticoccidial activity (POAA) based on relative weight gain, rate of oocyst production and lesion values. Results revealed that Nanhai Eimeria oocysts comprising of E. tenella, E. maxima and E. acervulina, were resistant to monensin, sensitive to both salinomycin and lasolacid and partially sensitive to maduramicin and semduramicin. By selection for early development of oocysts during passage through chickens, the prepatent time of E. tenella, E. maxima and E. acervulina were reduced by 49, 36 and 22 h, respectively. The precocious lines are less pathogenic than the parent strains from which they were selected and conferred a satisfactory protection for chickens against coccidiosis. These ionophore-tolerant precocious lines could have wider applications in the development of anticoccidial vaccines for sustainable control of coccidiosis.

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Drug Resistance; Eimeria; Eimeria tenella; Ionophores; Lactones; Lasalocid; Monensin; Nigericin; Oocysts; Parasitic Sensitivity Tests; Poultry Diseases; Pyrans; Random Allocation; Treatment Outcome

Little is known about the effects of residual veterinary drugs on the allergic reaction, except for the antigenicity of antibiotics and synthetic antimicrobials. Therefore, 59 kinds of veterinary drugs were investigated for their effects on the IgE receptor-mediated beta-hexosaminidase release from RBL-2H3 cells as an index of immediate allergic reaction. We found that the antibiotics chlorotetracycline, doxycycline, monensin, the synthetic antimicrobial pyrimethamine and the steroid hormone testosterone inhibited beta-hexosaminidase release. Most of the veterinary drugs showed no action, though the ionophores lasalocid, salinomycin and the steroid hormone hexestrol promoted beta-hexosaminidase release from injured cells. Based on the residual levels of these drugs and the frequencies of detection in actual food samples, it seems unlikely that these drugs have any immediate allergic effect in practice.

Topics: Animals; Anti-Bacterial Agents; beta-N-Acetylhexosaminidases; Chlortetracycline; Doxycycline; Drug Residues; Hexestrol; Hypersensitivity, Immediate; Lasalocid; Leukemia, Experimental; Monensin; Pyrans; Pyrimethamine; Rats; Receptors, IgE; Testosterone; Tumor Cells, Cultured; Veterinary Drugs

A rapid and very effective analytical procedure for the simultaneous determination of four polyether antibiotics (PEs) lasalocid, monensin, salinomycin and narasin in poultry feeds was tested. PEs were extracted from samples using methanol and without and clean-up derivatized with 2,4-dinitrophenylhydrazine (DNP) in an acidic medium at 55 degrees C. The derivatization mixture was analyzed directly on an ODS column (150 x 4.6 mm, 5 microns) with methanol--1.5% aqueous acetic acid (90:10, v/v) as eluent and UV detection was carried out at 305/392 nm. The recoveries of the PEs from spiked samples were 85-100% with RSDs of 4-10% in a concentration range of 50-150 mg/kg.

Topics: Animal Feed; Animals; Chromatography, Liquid; Coccidiostats; Indicators and Reagents; Lasalocid; Monensin; Phenylhydrazines; Poultry; Pyrans; Reference Standards; Reproducibility of Results; Spectrophotometry, Ultraviolet; Veterinary Drugs

Seven anticoccidial drugs commonly used in poultry (diclazuri), monensin, salinomycin, halofuginone, nicarbazin, robenidine, amprolium, and lasalocid) were tested for residual activity after withdrawal. In each test, the products were given at the recommended level to cages of 10 broiler chickens. Oral inoculation with coccidia was given after withdrawal of medication. Birds pretreated with 1 ppm of diclazuril and inoculated with Eimeria tenella after drug withdrawal had normal weight gain and very low lesion scores. Residual activity depleted gradually over several days, as shown by higher lesion scores when medication was withdrawn for up to 3 days before inoculation. Similar results were observed when young birds were inoculated with a mixture of E. tenella, E. maxima and E. acervulina, and also when birds were given diclazuril to market weight (6 weeks of age) and inoculated with a mixture of six species of Eiméria (The above species plus E. brunetti, E. mitis, and E. necatrix) after withdrawal of medication for 2 days. In contrast, there was no evidence of residual anticoccidial activity with nicarbazin, halofuginone, lasalocid, amprolium, salinomycin or monensin. Overall, the residual activity was unique to diclazuril.

Topics: Amprolium; Animal Feed; Animals; Chickens; Coccidiosis; Coccidiostats; Eimeria tenella; Feces; Female; Lasalocid; Male; Monensin; Nicarbazin; Nitriles; Piperidines; Poultry Diseases; Pyrans; Quinazolines; Quinazolinones; Random Allocation; Triazines

Monensin, salinomycin and narasin were detectable in six, two and one, respectively, out of 161 eggs surveyed in Northern Ireland in 1994. In all cases, the concentrations detected were less than 2.5 ng/g. Lasalocid was detectable in 107 eggs at concentrations ranging from 0.3 to 129 ng/g. Cross-contamination of unmedicated feeds with monensin during feed manufacture (up to eight batches of unmedicated feed contaminated with monensin) was similar to that previously observed for lasalocid (up to nine batches contaminated). Therefore differences in the incidence in eggs could not be explained by differential carry-over during feed manufacture. In a feeding trial it was shown that the relative ability of monensin, salinomycin and lasalocid to accumulate in eggs was in the ratio 0.12:3.3:63 ng/g egg per mg/kg feed, respectively. This indicated that the potential for monensin and salinomycin to cause residues in eggs was very low, by comparison with lasalocid. In 1995, a granular formulation of the lasalocid premix was introduced into the United Kingdom that decreased the carry-over of this drug from medicated to unmedicated feed. Six months after the introduction of this formulation, the incidence of lasalocid residues in eggs (21%) was lower than that found (66.5%) in an earlier survey (1994) carried out, and published, by this laboratory.

Topics: Animal Feed; Animals; Chickens; Coccidiostats; Drug Residues; Eggs; Food Contamination; Humans; Incidence; Ionophores; Lasalocid; Monensin; Northern Ireland; Pyrans

This study examined the effects of feeding monensin, lasalocid or salinomycin (at 1x and 2x therapeutic levels for 20 d) on the duration of xylazine+ketamine sleep time and the hepatic cytochrome P-450 content in broiler chickens of different age groups (3- and 6-w-old). The 3-w-old birds fed 120 ppm salinomycin had a reduced xylazine+ketamine sleep time as compared to control (no drug). The 6-w birds had a sleep time similar to the controls. Associated with ionophore feeding was a trend toward P-450 induction when compared to controls. Increased P-450 content was statistically significant in the 3-w birds fed 90 ppm lasalocid and in the 6-w birds fed 200 ppm monensin. Ionophore administration above recommended levels gave conflicting results for duration of xylazine+ketamine sleep time and hepatic cytochrome P-450 levels. The isozymes of cytochrome P-450 responsible for xylazine and ketamine metabolism may be different from those induced by the ionophores. There was no significant age-related difference in ionophore effects on cytochrome P-450 content.

Topics: Analysis of Variance; Anesthetics, Dissociative; Animals; Chickens; Cytochrome P-450 Enzyme System; Ionophores; Ketamine; Lasalocid; Liver; Male; Monensin; Pyrans; Sleep; Xylazine

Fluorescein diacetate (FDA) and propidium iodide (PI) were used as indicators of membrane integrity after Eimeria tenella sporozoites were treated with polyether ionophores. Flow cytometry was used to quantitate the structural and functional effects based on red or green fluorescence and shape index of the sporozoites. Two field isolates (FS119 and FS139) were essentially resistant to polyether ionophores administered under practical conditions, whereas a laboratory strain was considered sensitive. The shape of sporozoites changed after treatment with ionophores, and this could be detected by flow cytometry. Green-fluorescing cells declined in number as the membranes were compromised by ionophore treatment. Red-fluorescing cells increased as the compromised membranes allowed entry of PI to bind with the nucleic acids. These effects were generally slower to develop in ionophore-tolerant field isolates compared with the sensitive laboratory strain. The effect of lasalocid on FDA and PI uptake, change in shape of the sporozoites, and lysis of sporozoites was more rapid than that of monensin or salinomycin. The 2 field isolates responded at different rates to salinomycin and monensin. Flow cytometry was a sensitive and accurate instrument for analysis of the effects of ionophores on sensitive and resistant lines of coccidia.

Topics: Animals; Cell Membrane Permeability; Coccidiostats; Eimeria tenella; Flow Cytometry; Fluoresceins; Fluorescent Dyes; Ionophores; Lasalocid; Monensin; Propidium; Pyrans

The growth of Enterococcus faecium strains CCM 4231 and EF 26, and Staphylococcus gallinarum SG 31 was inhibited by salinomycin and lasalocid at concentrations of 25 and 50 mg/L. Staphylococcus gallinarum was more sensitive to the additives used than were enterococci. Maximum inhibition (90%) was measured after the growth with the SG 31 strain in the presence of both ionophores. Growth of organisms was more inhibited by salinomycin at 25 mg/L (67.5%) than at 50 mg/L (63%). The inhibitory effect in enterococcal strains reached after the addition of salinomycin and lasalocid (on average) 63 and 58%, respectively. The CCM 4231 strain was more inhibited by salinomycin as well as by lasalocid than was the EF 26 strain.

Topics: Enterococcus faecium; Ionophores; Lasalocid; Pyrans; Staphylococcus

The anticryptosporidial activities of three ionophorous antibiotics were assessed in dexamethasone-immunosuppressed rats infected with Cryptosporidium parvum. When administered prophylactically, lasalocid prevented infection in a dose-dependent manner, whereas monensin and salinomycin were ineffective. Therapeutically, lasalocid eliminated established overt infections of the intestine, although infection persisted in the common bile duct and intestinal infection recurred after lasalocid treatment was stopped. These findings suggest that lasalocid is a potentially useful anticryptosporidial agent but that long-term continuous administration may be necessary in the immunocompromised host.

Topics: Animals; Cryptosporidiosis; Cryptosporidium parvum; Female; Immunocompromised Host; Ionophores; Lasalocid; Monensin; Pyrans; Rats; Rats, Sprague-Dawley

Streptococcosis is a major disease of several fish species in Australia, Japan and South Africa. The minimum inhibitory concentration of some ionophores (lasalocid, monensin, narasin and salinomycin) was determined in vitro for an Enterococcus-like species pathogenic for rainbow trout (Oncorhynchus mykiss) in Australia. Forty isolates of the fish pathogen were tested, together with control strains of Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212 and Streptococcus bovis ATCC 9809. The minimum inhibitory concentrations (MIC) of erythromycin, the drug of choice for controlling streptococcosis, ranged between 0.1 and 0.8 microgram/ml whereas the MIC values for the ionophores ranged between 0.2 and 1.5 micrograms/ml. Of the ionophores tested, narasin was the most inhibitory (0.2-0.4 microgram/ml), while monensin was the least inhibitory (0.4-1.5 micrograms/ml). Salinomycin was marginally more inhibitory (0.4-0.8 microgram/ml) than lasalocid (0.8 microgram/ml).

Topics: Animals; Anti-Bacterial Agents; Enterococcus; Erythromycin; Fish Diseases; Gram-Positive Bacterial Infections; Ionophores; Lasalocid; Microbial Sensitivity Tests; Monensin; Oncorhynchus mykiss; Pyrans

Forty-six broiler houses were examined for the presence of oocysts of Eimeria in the litter before and after withdrawal of lasalocid or salinomycin from the feed. A decrease in number of small oocysts (Eimeria acervulina or Eimeria mitis) was observed following withdrawal of medication. Numbers of medium-sized oocysts (probably Eimeria tenella) remained the same, but an increase in large oocysts (Eimeria maxima) was recorded. No lesions attributable to Eimeria tenella were found in the ceca of birds after withdrawal of the drug. More small- and medium-sized oocysts were found at sites with new litter than at sites where the litter had been employed for previous flocks. No difference in the number of oocysts was found, whether birds were reared on oak shavings or a mixture of pine shavings and rice hulls. The number of oocysts was positively correlated with the moisture content of the litter, but there was no correlation between oocysts present and the final BW or feed conversion of the birds. Moisture levels were highest (after withdrawal of drug) for new litter or oak shavings. There was no correlation between moisture content of the litter and BW or feed conversion.

Topics: Animals; Cecum; Chickens; Coccidiosis; Coccidiostats; Eimeria; Feces; Lasalocid; Poultry Diseases; Pyrans

Topics: Animals; Chemical Phenomena; Chemistry; Chickens; Chromatography, Thin Layer; Ionophores; Lasalocid; Monensin; Pyrans

Two experiments were conducted to determine the effects of salinomycin and lasalocid on metabolism and growth of growing steers. In Exp. 1, 80 Angus steers (228 kg) were assigned to the following treatments: 1) control, 2) 50 mg salinomycin.hd-1.d-1, 3) 100 mg salinomycin.hd-1.d-1 and 4) 250 mg lasalocid.hd-1.d-1. Steers were fed corn silage once daily with allotments based on the amount of silage that each pen of five steers would consume in a 24-h period. In addition, .81 kg/hd of a corn-soybean meal supplement was fed daily during the 112-d study. Daily gains were similar across treatments, but feed intake was lower (P less than .05) for steers fed ionophores. Molar proportions of ruminal acetate were lower (P less than .05) in steers fed ionophores at 28 and 90 d. Ruminal propionate was lower (P less than .05) in control steers at 28 d, but values were similar across treatments on d 90. Plasma copper (Cu) was lower (P less than .05) in control steers on both sampling days. In Exp. 2, 16 Hereford steers were allotted to two blocks of eight animals each and assigned to one of three treatments: 1) control (n = 6), 2) 11 mg salinomycin/kg diet (n = 6) and 3) 33 mg lasalocid/kg diet (n = 4). Following a 28-d adjustment period, apparent absorption and retention of macrominerals and nitrogen (N) were determined during a 5-d collection period. Apparent absorption and retention of N did not differ among treatments when data were analyzed using N intake as a covariate.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Analysis of Variance; Animals; Anti-Bacterial Agents; Blood Urea Nitrogen; Calcium; Cattle; Copper; Eating; Fatty Acids, Volatile; Fermentation; Ionophores; Lasalocid; Male; Minerals; Nitrogen; Potassium; Pyrans; Random Allocation; Rumen; Silage; Weight Gain; Zea mays

The activities of five anticoccidials were compared against Eimeria species in/of chickens, in controlled in vivo and in vitro laboratory studies. Two more recent and potent market entries (maduramicin and halofuginone) were compared with three older polyether antibiotic anticoccidials (monensin, lasalocid and salinomycin). Halofuginone, lasalocid, maduramicin, monensin and salinomycin were evaluated at 3, 125, 5, 120 and 66 ppm, respectively, of active drug in the diets. At these levels, all five drugs demonstrated significant activity against Eimeria tenella, E. maxima, E. necatrix, E. brunetti and E. acervulina (in vivo). Monensin was least effective against E. tenella, and one of the lesser efficacious drugs against E. necatrix, maduramicin, was least effective against E. maxima. In studies of single Eimeria species infections, comparable weight gains were noted for the drugs. In the mixed Eimeria species infections, however, birds treated with maduramicin had significantly higher weight gains than did birds medicated with monensin. Unlike in vivo potencies, titration in vitro indicated that monensin was most potent (active at 10(-6) mcg ml-1), and maduramicin and lasalocid least potent (inactive at less than or equal to 10(-3) mcg ml-1).

Topics: Animals; Anti-Bacterial Agents; Body Weight; Chickens; Coccidiosis; Coccidiostats; Eimeria; Female; Ionophores; Lactones; Lasalocid; Male; Monensin; Piperidines; Poultry Diseases; Pyrans; Quinazolines; Quinazolinones

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Eimeria; Ionophores; Lasalocid; Monensin; Poultry Diseases; Pyrans

Chemoprophylaxis of Cryptosporidium baileyi infections was attempted by feeding 4 groups of chicks diets containing 3 mg of halofuginone/kg of feed, 60 mg of salinomycin/kg, 75 mg of lasalocid/kg, or 110 mg of monensin/kg. Rations were fed 5 days before oral or intratracheal inoculation with oocysts and were continued for 20 days. None of the drugs prevented C baileyi infections. Clinical signs of respiratory tract disease and gross lesions of airsacculitis were observed in intratracheally inoculated birds in all treatment groups and nonmedicated controls. Orally inoculated birds did not develop clinical signs of infection. Pathogenic bacteria were not isolated from the respiratory tract systems of any chicks. Halofuginone delayed the establishment of infections of the bursa of Fabricius and cloaca, but not of the trachea.

Topics: Animals; Chickens; Coccidiostats; Cryptosporidiosis; Lasalocid; Monensin; Piperidines; Poultry Diseases; Pyrans; Quinazolines; Quinazolinones

A simultaneous determination of three polyether antibiotics, salinomycin, monensin and lasalocid, was established by silica gel and RP-18 high-performance thin-layer chromatography (HPTLC) using 18,19-dihydrosalinomycin and 18,19-dihydro-20-ketosalinomycin as internal standards. Fluorescent derivatives of the polyethers were prepared by reaction of their sodium salts with 1-bromoacetylpyrene and Kryptofix 222 in acetonitrile. A silica gel HPTLC plate with carbon tetrachloride-ethyl acetate-acetonitrile (50:5:10) as a solvent system and a RP-18 HPTLC plate with dichloromethane-ethyl acetate-acetone-acetonitrile (15:2:1:55) gave satisfactory separations of the five pyrenacyl esters of salinomycin, monensin, lasalocid, 18,19-dihydrosalinomycin and 18,19-dihydro-20-ketosalinomycin. Under these conditions the internal standard 18,19-dihydrosalinomycin was found to be suitable for the simultaneous determination of salinomycin and monensin, and 18,19-dihydro-20-ketosalinomycin for lasalocid. A linear relationship was obtained between the fluorescence intensity and the amount of each antibiotic in the range 2-14 ng. The detection limit of the three antibiotics was 100 pg.

Topics: Chromatography, Thin Layer; Densitometry; Lasalocid; Monensin; Pyrans; Solvents; Spectrometry, Fluorescence

Prophylactic levels of three ionophorous antibiotics, monensin, salinomycin, and lasalocid, were administered to groups of chickens and turkeys. All three ionophores markedly inhibited invasion of cecal tissues by sporozoites of ionophore-sensitive (IS) Eimeria tenella. Monensin and salinomycin also reduced invasion in turkeys by sporozoites of E. adenoeides, but lasalocid only minimally inhibited invasion. Invasion of ceca of monensin-medicated chickens was significantly greater by sporozoites of ionophore-resistant (IR) E. tenella than of the IS isolate. Concomitant experiments showed significant differences in [14C]monensin accumulation among IS and IR isolates of E. tenella. The decreased uptake of monensin by the IR isolates appeared to be accompanied by a decrease in responsiveness to the activity of monensin as well as to two other ionophores, salinomycin and narasin in cell culture. The amount of monensin, salinomycin or narasin required to inhibit development of E. tenella by 50% was 20 to 40 times higher for the IR isolates than for the IS ones. Collectively, the data suggest that differences in ionophore accumulation by IS and IR isolates of E. tenella might reflect differences in membrane chemistry and that these differences are responsible for the expressions of resistance that were observed in these studies. This expression of resistance appears to be common to all ionophores tested.

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Drug Resistance; Ionophores; Lasalocid; Monensin; Poultry Diseases; Pyrans; Turkeys

Rabbits spontaneously infected with coccidia of the genus Eimeria were treated with salinomycin, lasalocid and monensin. The drugs were applied in pellets in the doses of 50 ppm. The weight gain in rabbits treated with salinomycin and monensin was higher than in those treated with lasalocid and by 22.6% higher than in control animals. The weight gain in animals treated with lasalocid was almost the same as in the control group. The oocyst production was suppressed most significantly by salinomycin.

Topics: Animals; Coccidiosis; Coccidiostats; Lasalocid; Monensin; Pyrans; Rabbits

Four isolates of Eimeria tenella obtained from the field were partially resistant to monensin. This resistance was not lost after 10 passages in unmedicated chickens, indicating that it was stable. One of the four isolates was examined and found to be resistant also to narasin, salinomycin and lasalocid.

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Drug Resistance, Microbial; Eimeria; Ionophores; Lasalocid; Monensin; Poultry Diseases; Pyrans

Salinomycin-Na and lasalocid-Na, two ionophorous antibiotics known for their anticoccidial activity, exhibit in vivo blood schizontocidal action on the Plasmodium berghei Keyberg 173 RC/M line that has a high level of resistance to chloroquine and mepacrine. Salinomycin was found to have a greater effect than lasalocid on asexual stages of this line. Trophozoites and schizonts were no longer found after a single dose of 20 mg/kg or five doses of 1.25 mg/kg of salinomycin whereas a single dose of 40 mg/kg or five doses of 20 mg/kg of lasalocid showed no marked effect on parasitaemia within 96 h of starting treatment in rats. Some toxicological data show that lasalocid, however, is better tolerated in domestic animals than salinomycin. Early morphological changes in asexual blood stages were membrane-coiling in the cytoplasm followed by vacuolization and disruption of the cell membrane or pellicle after treatment with both compounds. In particular mature schizonts were totally destroyed showing enormously large vacuoles. Toxicological data and blood schizontocidal activity indicate the narrow safety margin in P. berghei infected rats, and place salinomycin in the 'markedly toxic' group of antimalarial compounds.

Topics: Animals; Anti-Bacterial Agents; Cell Membrane; Chloroquine; Cytoplasm; Drug Resistance, Microbial; Lasalocid; Lethal Dose 50; Malaria; Male; Microscopy, Electron; Plasmodium berghei; Pyrans; Quinacrine; Rats; Rats, Inbred Strains; Time Factors

Two, 7-week floor pen experiments were conducted consecutively with male broilers and then female broilers to determine the effects of feeding salinomycin (60 ppm), monensin (99 ppm), or lasalocid (125 ppm) at the following three levels of dietary protein: 1) that which meets National Research Council specifications (NRC, 1977), 2) that level deficient in sulfur amino acids (SAA), or 3) that deficient in protein. Group body weights, feed intake, and water consumption were noted at 28 and 49 days of age with feed efficiency and overall mortalities determined. Reducing SAA resulted in depressed (P less than .05) body weights at 7 weeks in both experiments, whereas deficient protein reduced (P less than .05) growth, feed efficiency, and water consumption. Generally, inclusion of coccidiostats in the diet did not significantly hinder growth or feed efficiency. Feeding of coccidiostats in combination with the low protein diet did not produce additional anorexigenic effects. Although a significant lasalocid SAA-sparing effect was not observed, diet X coccidiostat interactions (P less than .05) were apparent and attributable to an apparent "protein-sparing" effect upon body weight gain when salinomycin was fed in combination with the low protein diet. Lasalocid increased water consumption (P less than .05) relative to monensin in the female broilers.

Topics: Amino Acids, Sulfur; Animals; Body Weight; Chickens; Coccidiostats; Dietary Proteins; Drinking; Female; Food Additives; Lasalocid; Male; Monensin; Mortality; Pyrans; Sex Factors

Salinomycin, a new ionophore antibiotic, was tested and compared with lasalocid and monensin for preventing experimentally induced lactic acidosis. Five rumen-fistulated adult cattle were used in a 5 X 5 Latin square design, and the treatments were as follows: no treatment (control), 0.11 mg of salinomycin/kg of body weight (S1), 0.22 mg of salinomycin/kg (S2), 0.66 of lasalocid/kg, and 0.66 mg of monensin/kg. Acidosis was induced by intraruminal administration of a ground corn-corn starch mixture (50:50, 12.5 g/kg) once a day for up to 4 days. Antibiotics were administered along with grain-starch mixture. Rumen and blood samples were obtained before and at 6, 12, and 24 hours after each carbohydrate-antibiotic dosing to monitor acid-base status. Control and S1-treated cattle became ruminally acidotic within 54 hours, whereas cattle treated with S2, lasalocid, and monensin resisted acidosis for up to 78 hours after dosing. Cattle treated with S2, lasalocid, or monensin had higher rumen pH and lower L(+)- and D(-)-lactate concentrations than did control or S1-treated cattle. Rumen pH decrease to below 5.0 in S2-, lasalocid-, and monensin-treated cattle was not due to lactic acid, but to increased production of volatile fatty acids. Rumen propionate proportion increased initially in antibiotic-treated cattle, but after 48 hours, butyrate proportion increased significantly. Despite low rumen pH and high lactate concentration, lacticacidemia was not evident, and the systemic acid-base disturbance was mild in control cattle.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Acidosis; Animal Feed; Animals; Cattle; Cattle Diseases; Food Additives; Hydrogen-Ion Concentration; Lactates; Lasalocid; Monensin; Pyrans; Rumen

The rate of feather growth was measured in Hubbard X Hubbard broilers given monensin, salinomycin, or lasalocid for 8 weeks in floor pens. Chicks were given a nutritionally adequate diet. Feathers on male chicks were shorter at 10 days of age but grew faster than those on female chicks. Male chicks had longer feathers than female chicks after 31 days of age. Back feather scores were similar in male and female chicks at 52 days of age. Dietary ionophores had no effect on the rate of feather growth or the back feather coverage under the condition of this study.

Topics: Animals; Body Weight; Chickens; Coccidiostats; Feathers; Female; Food Additives; Lasalocid; Male; Monensin; Pyrans; Sex Factors

Topics: Animal Feed; Anti-Bacterial Agents; Chromatography, Thin Layer; Furans; Lasalocid; Monensin; Pyrans

In high concentrations, the ionophores salinomycin, monensin and X-537A cause cardiac arrhythmias in vivo. To determine if these arrhythmias result from a direct action of these ionophores on cardiac electrophysiology, we studied their effects on automaticity and transmembrane action potentials of isolated canine left ventricular Purkinje fibers. High concentrations of the ionophores suppressed automaticity and shortened action potential duration. These data suggest that high concentrations of the ionophores provoke cardiac arrhythmias in vivo by similar mechanisms despite their diverse cation transport selectivities.

Topics: Action Potentials; Animals; Arrhythmias, Cardiac; Cations; Dogs; Heart Rate; Ionophores; Lasalocid; Monensin; Nadolol; Propanolamines; Purkinje Fibers; Pyrans

The effect of three polyether antibiotics (monensin, salinomycin, lasalocid) on developmental stages of Eimeria tenella (Coccidia, Sporozoa) was studied in vivo and in vitro by means of light and electron microscopy. It was found that these three drugs act against free merozoites, which are destroyed by bursting of the cell border (i.e. pellicle), endoplasmic reticulum and internal organelles even after very short exposure times (20 min) in media containing 1 ppm, 10 ppm or 100 ppm of these drugs. Sporozoites, however, survived these drug concentrations during an exposure time of 30 min (this would be sufficient to penetrate host cells and start development). Intracellular stages, which were situated in a parasitophorous vacuole within an intact host cell, were not attacked, apparently because these drugs are almost incapable of penetrating host cells. On the other hand, parasites (such as differentiated schizonts, gamonts) located within degenerating host cells showed slight disintegration, which did not necessarily led to their death. From these results it becomes clear why these polyether antibiotics have to be fed daily. Doses of 70 ppm salinomycin, 125 ppm monensin and 125 ppm lasalocid were found to bring about an equivalent protective effect against an infection with 40,000 Eimeria tenella oocysts.

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Eimeria; Furans; Lasalocid; Male; Microscopy, Electron; Monensin; Pyrans; Vacuoles

Sporozoites of Eimeria tenella were treated with different anticoccidial drugs in vitro and their subsequent viability was tested by inoculating them into chicken embryos. Monensin, salinomycin, lasalocid, and arprinocid, at concentrations between 0.01 and 1.0 micrograms/ml, greatly reduced sporozoite viability as judged by mortality, hemorrhage and specific lesions in the embryo chorioallantois. Monensin was also effective in reducing the viability of sporozoites of E. mivati and E. tenella as judged by oocyst production occurring in embryos; activity of monensin was greater against E. tenella than against E. mivati. Monensin (0.1 mg) inoculated into embryos inhibited development of E. tenella. Oocysts which were produced in the presence of the drug sporulated normally and sporozoites obtained from them were fully infective. By initiating treatment of chickens with monensin at different times in relation to infection, it was shown that the drug exerts its anticoccidial effect on the primary invasive stage and on the gametogonous stage of E. tenella and E. necatrix. The effect of gametogony was tested by initiating infections with second generation merozoites of E. tenella. Significant reduction in oocyst production occurred in three of four strains of E. tenella tested. Medication with monensin initiated before merozoite inoculation was effective in inhibiting oocyst production, but medication starting 5 hr after merozoite inoculation was not. This differed from the effects of arprinocid and sulfaquinoxaline which were expressed both before and 5 hr after merozoite inoculation. The results show that the ionophorous anticoccidial drugs exert their anticoccidial action primarily against the invasive stages of Eimeria.

Topics: Adenine; Animals; Chick Embryo; Coccidiosis; Coccidiostats; Eimeria; Furans; Ionophores; Lasalocid; Monensin; Pyrans; Temperature

Free Eimeria tenella sporozoites were exposed to the anticoccidial ionophores monensin, lasalocid, narasin, or salinomycin for 4 hr at 40 C, whereupon the drugs were removed by dilution centrifugation and the parasites inoculated into cultures of chick kidney cells. Cultures were fixed and stained at 4 and 96 hr postinoculation to determine the effect of ionophore uptake by the extracellular sporozoites on invasion and development. Pretreatment with each of these antibiotics significantly reduced the number of intracellular sporozoites and dramatically inhibited asexual development. These effects were dose-dependent. Exposure of free (extracellular) sporozoites to monensin at 40 C caused a significant decline in the number of surviving organisms over time as compared to nontreated sporozoites. This response also appeared to be dose-dependent. Scanning and transmission electron microscopy revealed that the surface of the treated sporozoites was very irregular and the organisms often exhibited a gross swelling. These results indicated that free Eimeria tenella sporozoites may incorporate a potentially lethal concentration of the polyether ionophorous antibiotics and that a coccidiocidal activity may be expressed whether or not penetration of host's cells occurs.

Topics: Animals; Cells, Cultured; Chickens; Dose-Response Relationship, Drug; Eimeria; Furans; Ionophores; Kidney; Lasalocid; Monensin; Pyrans

Topics: Animals; Anti-Bacterial Agents; Chickens; Coccidiosis; Coccidiostats; Drug Combinations; Eimeria; Ionophores; Lasalocid; Male; Monensin; Poultry Diseases; Pyrans

Three polyether, ionophorous anticoccidial drugs were fed to broiler chickens in floor pens for 5 or 6 weeks, then withdrawn for 2 weeks or 1 week, respectively. With monensin and salinomycin there was evidence of increased feed consumption and compensatory growth during the first week, but not the second week, after drug withdrawal. There was no evidence of compensatory growth in birds fed lasalocid. Final weights were best in birds fed lasalocid and salinomycin in comparison with unmedicated controls and birds fed monensin. There was evidence of increased feed consumption and compensatory growth in some treatments in which birds weighed more than controls prior to drug withdrawal.

Topics: Animals; Antibodies; Body Weight; Chickens; Eating; Furans; Ionophores; Lasalocid; Monensin; Pyrans

Topics: Animals; Anti-Bacterial Agents; Coccidiosis; Eimeria; Female; Lasalocid; Male; Monensin; Pyrans; Rabbits; Species Specificity

Topics: Animals; Chickens; Coccidiosis; Coccidiostats; Furans; Ionophores; Lasalocid; Male; Monensin; Poultry Diseases; Pyrans

Topics: Animals; Anti-Bacterial Agents; Chickens; Coccidiosis; Coccidiostats; Furans; Lasalocid; Monensin; Poultry Diseases; Pyrans