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At least 19 recordsLinked to original sources
PubMed1985

Efficacy of morantel against nematode populations in calves exposed on a pasture stocked for two years with morantel sustained-release bolus-treated calves.

Two groups of 10 parasite-free calves were maintained either for 2 weeks on a pasture grazed by nonmedicated cattle (pasture A) or for 3 weeks on a pasture grazed by morantel sustained-release bolus-treated cattle (pasture B) for the preceding 2 years. After a 4-week holding period to allow for maturation of acquired gastrointestinal nematodes, 5 calves from each group were administered a therapeutic dose (10 mg/kg of body weight) of morantel tartrate. All calves were necropsied 1 week later, and the abomasal and small intestinal nematodes were isolated, identified, and enumerated. A comparison of efficacies between nonmedicated and morantel tartrate-treated calves of each pasture demonstrated that morantel was equally effective against the gastrointestinal nematode infections, regardless of infection source (ie, pasture A vs pasture B). The overall nematode reductions due to morantel tartrate treatment of calves that grazed pastures A and B were 98% and 96%, respectively. It was concluded that the sensitivity of gastrointestinal nematodes to morantel tartrate was not diminished in calves maintained on pasture B, which had been stocked with morantel sustained-release bolus-treated calves for the preceding 2 grazing seasons.

Animals↗
PubMedDate not supplied

Determination of depletion and statistical distribution of morantel-related residues in bovine milk following administration of morantel tartrate to dairy cows.

Residue depletion studies were conducted in dairy cattle to monitor morantel-related residues in milk following oral administration of morantel tartrate (Rumate. Eleven lactating cows of various ages, periods of lactation, and known milk production were orally dosed with the bolus formulation of morantel tartrate with an actual dose range of 8.4-9.8 mg/kg body weight. Representative samples of milk were collected at 10-14 h intervals post-dose, and subsamples were assayed for the major and minor hydrolysis products of morantel-related residues, MAPA and CP-20,107. Residues assayed as precursors of MAPA peaked at the second milking (24 h post-dose) and were below 25 ppb (range: less than 12-24 ppb). Precursors of CP-20,107, which confirm the identity of morantel, also peaked at 24 h post-dose (range: 2.1-3.3 ppb) and declined rapidly thereafter. A statistical model was used to project the level of residues at the upper limit of 99% of the total target animal (i.e., dairy cattle) population with 95% confidence. The calculated peak levels from this model were 50 and 5.0 ppb for morantel-related residues convertible to MAPA and CP-20,107, respectively.

Animals↗
PubMed1985

Effect of the morantel sustained-release bolus, used during one grazing season, on the sensitivity of Ostertagia and Cooperia to morantel tartrate in calves.

Infective 3rd-stage larvae of Ostertagia and Cooperia, obtained from the feces of nonmedicated and morantel sustained-release bolus (MSRB)-treated calves, were orally administered to 2 groups of parasite-free calves. After a 42-day maturation period, a therapeutic dose of morantel tartrate was administered to half of the calves from each group. All calves were necropsied 7 days after treatment. After comparing the nematode counts for the nonmedicated and morantel-treated calves of each group, morantel tartrate was demonstrated to be equally effective against the nonmedicated-derived and MSRB-derived nematode populations. The sensitivity of Ostertagia spp and Cooperia spp to morantel tartrate, therefore, was not diminished after use of the MSRB for a single grazing season.

Animals↗
PubMed1996

Activation and cooperative multi-ion block of single nicotinic-acetylcholine channel currents of Ascaris muscle by the tetrahydropyrimidine anthelmintic, morantel.

1. We have investigated activation and block, by the tetrahydropyrimidine anthelmintic, morantel, of nicotinic-acetylcholine receptor (AChR) currents in membrane vesicles isolated from somatic muscle cells of the nematode parasite Ascaris suum. Standard single-channel recording techniques were employed. Morantel in the pipette (6 nM to 600 microM), activated single nicotinic AChR currents. 2. Kinetic properties of the main-conductance state of morantel-activated currents were investigated in detail throughout the concentration range, 0.6 microM to 600 microM. Open-time distributions were best fitted by a single exponential. Mean open-times were slightly voltage-dependent, increasing from 0.9 ms at +75 mV to 1.74 ms at -75 mV in the presence of 0.6 microM morantel. At low concentrations, closed-time distributions were best fitted by the sum of two or three exponential components. 3. As the concentration of morantel was increased (100-600 microM), fast-flickering open channel-block was observed at positive potentials, even though morantel, a cation, was only present at the extracellular surface of the membrane. The block rate was dependent on morantel concentration and both block rate and duration of block increased as the potential became less positive. A simple channel-block mechanism did not explain properties of this block. 4. At negative potentials, as the morantel concentration increased, a complex block was observed. With increases in morantel concentration two additional gap components appeared in closed-time distributions: one was short with a duration (approximately 13 ms) independent of morantel concentration; the other was long with a duration that increased with morantel concentration (up to many minutes). In combination, these two components produced a marked reduction in probability of channel opening (Po) with increasing morantel concentration. The relationship between the degrees of block and morantel concentration had a Hill coefficient of 1.6, suggesting the involvement of at least two blocking molecules. The data were analysed by use of a simple sequential double block kinetic model.

Acetylcholine↗
PubMed1993

Pharmacodynamics, pharmacokinetics and faecal persistence of morantel in cattle and goats.

Morantel could not be detected (< 0.05 microgram/ml) in the plasma of cattle or goats following the oral administration of morantel tartrate at a dose rate of 10 mg/kg bodyweight. No morantel was detected in the milk of lactating goats except in one animal where a concentration of 0.092 microgram/ml was detected at 8 h after drug administration. Morantel was highly effective against Cooperia oncophora infections in calves treated 6, 9 or 18 days after infection; however, was highly effective against Ostertagia ostertagi only when treated 18 days after infection. Morantel did not affect the fecundity of adult O. ostertagi surviving treatment 18 days after infection which had similar average numbers of eggs in their uteri (range 13.4 +/- 0.73-16.8 +/- 0.98) as did parasites from control animals (range 12.0 +/- 0.70-13.6 +/- 0.66). Morantel could be detected at a concentration of 96 +/- 4.5 micrograms/g (dry weight) in the faeces of a calf 24 h after treatment with 10 mg/kg bodyweight of morantel tartrate. The concentration of morantel in replicate samples of this faeces exposed to natural atmosphere, but not to soil or soil organisms, declined slowly over the following 322 days. At day 322 after the start of the experiment 8.8 micrograms/g of morantel could be measured in the remaining faecal material. Throughout the faecal degradation study the concentration of morantel in the crusts of the replicate sample pats was lower than the concentration in the core samples.

Animals↗
PubMed1992

Morantel tartrate release from a long-acting intraruminal device in cattle: pharmacokinetics and gastrointestinal distribution.

The pharmacokinetics and gastrointestinal distribution of morantel tartrate release from a sustained release trilaminate bolus in cattle were investigated over a 98-day period post-treatment. Six Holstein calves (125-150 kg) had permanent indwelling fistulae surgically inserted into the rumen, abomasum and terminal ileum. Samples of jugular blood, feces and ruminal, abomasal and ileal fluids were taken on days -3, 1, 4, 7, 10, 14 and weekly up to 98 days post-bolus administration. Morantel tartrate concentrations were measured by HPLC after extraction and clean-up. Morantel was not detected in plasma at any time after bolus administration. High concentrations of morantel tartrate were found in ruminal, abomasal and ileal fluids and feces over 98 days post-treatment. The morantel peak concentration (Cmax) was achieved at Day 1 post-administration in each of these compartments. The steady-state morantel concentration (Css) was achieved at approximately 10 days post-treatment and maintained for 91-98 days post-treatment in these gastrointestinal compartments. The morantel Cmax, Css, area under the zero (AUC) and first moment (AUMC) of the concentration-time curve were significantly higher (P less than 0.01) in feces than in other compartments. The in vivo drug release profile of this device has been determined. Steady-state concentrations for from 91 to 98 days have been confirmed.

Abomasum↗
PubMed1986

Resistance of Trichostrongylus colubriformis to levamisole and morantel: differences in relation to selection history.

Two field strains of Trichostrongylus colubriformis were tested by in vitro and in vivo methods for resistance to morantel, levamisole and thiabendazole and compared with an anthelmintic-naive laboratory-passaged strain (McM). One field strain (TAS) was isolated from a dairy goat herd which had experienced severe helminthiasis despite intensive anthelmintic usage. The other (BCK) was isolated from sheep which had been treated solely with levamisole over a 6-year period. The BCK strain had very high levels of both levamisole and morantel resistance. In contrast the TAS strain was resistant to morantel but highly susceptible to levamisole. This finding is contrary to the expectation that selection with morantel automatically confers resistance to levamisole, the converse of which was shown to apply in the BCK strain. Although the TAS strain was exposed to levamisole prior to isolation, examination of the drug's pharmacokinetics in goats indicated that it exerted little if any anthelmintic effect, and therefore selection pressure, on the parasite population. This study suggests that the mechanism of levamisole resistance covers a wide spectrum, and embraces that for morantel. It also suggests that in order to conserve the effectiveness of the levamisole/morantel group of broad spectrum anthelmintics, morantel should be used to the exclusion of levamisole until resistance is detected, at which time levamisole may be introduced to re-establish high levels of control.

Animals↗
PubMed1991

Further studies with a strain of Ostertagia ostertagi resistant to morantel tartrate.

Two experiments with a morantel resistant strain of Ostertagia ostertagi were carried out. In the first experiment five groups of five calves were infected with 60,000 larvae of this resistant strain. Calves of one group remained untreated, calves of the other groups were treated with morantel tartrate, oxfendazole, levamisole or ivermectin in the recommended doses. It was demonstrated that there was side resistance to levamisole, but not to oxfendazole or ivermectin. Compared with the untreated controls the reduction percentages of the worm burdens were 45.3 (morantel tartrate), 99.7 (oxfendazole), 83.5 (levamisole) and 100 (ivermectin). In the second experiment a comparison was made between the effect of levamisole against a morantel susceptible strain of O. ostertagi and the resistant strain. Two groups of five calves were infected with the susceptible strain and two groups with the resistant one. One group of each pair remained untreated, the other was treated with levamisole. The reduction percentages of the worm burdens were 99.6 (susceptible strain) and 63.6 (resistant strain). This result confirms the efficacy of levamisole to susceptible O. ostertagi and the side resistance of the morantel resistant strain.

Animals↗
PubMed1989

Reliability and reproducibility of the larval paralysis test as an in vitro method for the detection of anthelmintic resistance of nematodes against levamisole and morantel tartrate.

In order to study the reliability of the larval paralysis test as an in vitro assay for the detection of resistance of nematodes to levamisole and morantel tartrate, the influence of different parameters was evaluated using resistant and susceptible Ostertagia ostertagi strains. The operator, the sample (10% of the larvae present in the suspension), the incubation time (24, 48 or 72 h), the incubation temperature (20 or 25 degrees C) and the observation period of the larvae (5 or 15 s) had no statistically significant influence on the test results. Statistical differences were obtained only when L3 larvae of different ages (1 or 2 months) were used. Reversibility of the paralysis did not occur when concentrations of levamisole of less than or equal to 200 micrograms ml-1 or morantel tartrate of less than 2000 micrograms ml-1 were used. The reproducibility of the test was fairly good, with a mean standard deviation of 21.3% for the LC50 values. Morantel resistance in a strain of O. ostertagi was not confirmed as such by the larval paralysis test. The resistance factor was less than or equal to 1, in spite of an efficacy of morantel of 77.4% as shown in vivo.

Animals↗
PubMed1989

Evaluation of the morantel sustained release trilaminate in the control of parasitic gastroenteritis in first season grazing cattle.

A novel intraruminal bolus developed for the sustained delivery of the anthelmintic morantel tartrate was evaluated in the seasonal control of parasitic gastroenteritis in first season grazing calves. The morantel sustained release trilaminate is a trilaminate sheet consisting of a central lamina of a morantel tartrate/ethylene vinyl acetate matrix coated on both sides with a thin impermeable layer of ethylene vinyl acetate. A symmetrical pattern of circular perforations punched through the device controls the release of morantel. Administration of the trilaminate to calves significantly reduced their faecal egg output compared with untreated controls and thus reduced pasture larval contamination. Clinical parasitic gastroenteritis was prevented in the treated calves and there were significant reductions in their worm burdens compared with the untreated control calves both during and at the end of the grazing season. The control of parasitic gastroenteritis resulted in a significantly greater (P less than 0.0001) weight gain, of 45 kg, by the treated calves.

Animals↗
PubMed1986

Production, parasitological and carcase evaluation studies in steers exposed to trichostrongyle infection and treated with a morantel bolus or fenbendazole in two consecutive grazing seasons.

Friesian steers were exposed to natural trichostrongyle infection and left untreated (controls) or treated with either a morantel sustained release bolus or fenbendazole at two week intervals (clean) in each of two consecutive grazing seasons. In the second grazing season the mean liveweight gains of the clean, morantel treated and control groups of cattle over 152 days were 105, 131 and 109 kg respectively (morantel treated greater than clean, control P less than 0.02). The cattle were slaughtered following an indoor fattening period. The dressed carcase weight, killing out percentage and related carcase measurements were superior in the treated groups. Eighty per cent of the clean and morantel treated cattle graded satisfactorily and qualified for subsidy payment whereas less than 30 per cent of the control cattle were successful. Rib joint analyses showed significantly lower total weight, eye muscle weight and area together with a higher bone content in control cattle.

Animal Feed↗
PubMedDate not supplied

Determination of morantel-related residues in bovine milk by electron capture gas chromatography.

A gas chromatographic assay was developed to determine major residues of morantel in bovine milk over a range that is suitable for monitoring residues of the drug. The method is based on hydrolysis of the N-methyl-tetrahydropyrimidine portion of morantel and its metabolites to N-methyl-1,3-propanediamine, and converting the diamine to an N,N-bis-(2-nitro-4-trifluoromethylphenyl) derivative. The addition of an internal standard, the N-desmethyl-N-ethyl homolog of pyrantel, to the milk sample circumvents any potential problem that could arise from variable reaction yields, and eliminates the true recovery as a factor affecting the accuracy and precision of the procedure. The concentrations of the derivatives are determined by pulsed electron capture gas chromatography over a linear dynamic range that is equivalent to 12.5-50 ppb morantel. The method was evaluated at the 0, 12.5, 25, and 50 ppb levels in fortified bovine milk, and in a withdrawal sample containing physiologically incurred morantel residues. Mean values of 14 +/- 1.7, 24 +/- 3.7, and 47 +/- 6.9 were found for the fortified samples, approximately 3 ppb for control milk, and 16 +/- 1.7 ppb for the withdrawal sample.

Animals↗
PubMed1986

Efficacy of repeated doses of levamisole, morantel, fenbendazole, and ivermectin against gastrointestinal nematodes in ewes.

Levamisole, morantel, fenbendazole, or ivermectin was administered at 2-week intervals from May 1 through Sept 14, 1985, to breeding ewes (20 ewes/drug) infected with various gastrointestinal nematodes. All ewes had fewer gastrointestinal nematode eggs per gram of feces (epg) after 2 treatments, compared with pretreatment epg counts. Ewes administered ivermectin continued to have a low mean epg (0 to 3) throughout the study. The mean epg counts of ewes treated with levamisole increased from 3 to 483 during the study. This increase was similar to that of ewes treated with morantel (7 to 485 epg). The mean epg count of fenbendazole-treated ewes increased from 4 to 192 during the study. By the end of the study, the mean epg counts when expressed as a percentage of the pretreatment epg counts were 4% (ivermectin), 249% (fenbendazole), 627% (levamisole), and 630% (morantel). With the exception of the ivermectin-treated ewes, the epg count increased almost linearly in the ewes after the 2nd anthelmintic treatment. These data indicate that the gastrointestinal nematodes (including Haemonchus contortus) may have developed more resistance to levamisole and morantel than to fenbendazole. On the basis of the epg counts, resistance to ivermectin did not develop during the 4.5-month treatment period. The percentage of ewes shedding eggs after 2, 4, and 6 anthelmintic treatments was lowest for ewes treated with ivermectin (20%) and was similar (40%) for ewes treated with 1 of the other 3 anthelmintics. At the conclusion of the study, most of the ewes (90%) were shedding at least a small number of eggs, regardless of the anthelmintic treatment.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1982

Electron capture gas-liquid chromatographic determination of morantel-related residues in bovine liver.

A gas-liquid chromatographic assay has been developed to determine major residues of morantel in bovine liver, a target tissue, at levels of 0.2-0.8 ppm. The method is based on hydrolysis of the N-methyltetrahydropyrimidine portion of morantel and its metabolites to N-methyl-1,3-propanediamine, and conversion of the diamine to an N,N'-bis-(2-nitro-4-trifluoromethylphenyl) derivative. The addition of an internal standard, N-ethyl-1,3-propanediamine, to the tissue sample circumvents any potential problem that could arise from variable reaction yields, and eliminates the true recovery as a factor affecting the accuracy and precision of the procedure. The concentrations of the derivatives are determined by pulsed electron capture gas-liquid chromatography over a linear dynamic range equivalent to 0.2-0.8 ppm morantel. The method has been evaluated at 0, 0.2, 0.4, and 0.8 ppm levels in fortified bovine liver, and in a withdrawal sample containing physiologically incurred morantel residues. Mean values of 0.22 +/- 0.015, 0.40 +/- 0.033, and 0.79 +/- ppm were found for fortified samples, 0.02 ppm for control liver, and 0.56 +/- 0.050 ppm for the withdrawal sample.

Animals↗
PubMed1973

Some pharmacological effects of the nematocide, morantel.

1. In isolated nerve-muscle preparations as well as in nerve-muscle preparations in intact anaesthetized animals, morantel exhibited neuromuscular blocking properties similar to those of depolarizing blockers. The drug also caused spastic paralysis of 3 day-old chicks and contracture of the isolated toad rectus abdominis muscle.2. Morantel caused contraction of the guinea-pig and rabbit isolated small intestine. This effect was antagonized by atropine and hexamethonium.3. Morantel caused an increase in the blood pressure of the anaesthetized rat and cat and contraction of the nictitating membrane of the anaesthetized cat. These effects were antagonized by hexamethonium.4. It was concluded that morantel (like the related compound pyrantel) has acetylcholine-like action and that its structure is consistent with such action.

Animals↗
PubMed1987

[The transition of morantel in cow's milk following administration in the retard form, "Paratect Bolus" (Pfizer)].

The transition of Morantel into bovine milk was studied with three lactating cows. The active compound was administered as Paratect Bolus which continuously releases the anthelmintic agent. No residues of Morantel could be detected throughout the 92-day experiment (limit of detection: 0.5 micrograms Morantel tartrate/kg milk), nor could the compound be found in the blood serum at day 35 of the experiment. The same day an amount of 825 micrograms/kg was observed in faeces.

Animals↗
PubMed1983

Therapeutic and prophylactic efficacy of morantel when administered directly into the rumen of cattle on a continuous basis.

The efficacy of morantel tartrate when administered on a continuous basis directly into the rumen/reticulum of cattle, either by a cannula or from a specially designed device, was evaluated against gastrointestinal parasites under laboratory conditions. In two experiments the continuous infusion of morantel at rates between 0.26 and 1.04 mg/kg body weight per day using a peristaltic pump was highly efficacious in both preventing the establishment of infections and removing established infections of the following species: Ostertagia ostertagi, Haemonchus contortus, Cooperia oncophora and Trichostrongylus colubriformis. The same dose rates also prevented establishment of Dictyocaulus viviparus infection but were ineffective against established infections of this parasite. In another two experiments the continuous release of morantel tartrate for at least 60 days (at rates between 0.65 and 1.11 mg/kg body weight per day) from a specially designed intraruminal sustained release bolus (secured at each end by a polyethylene impregnated semi-permeable membrane) was highly efficacious in both preventing the establishment of infections and removing established infections of the following species: O. ostertagi, T. axei, T. colubriformis and C. oncophora.

Animals↗