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At least 19 recordsLinked to original sources
PubMed1989

Evaluation of albendazole, pyrantel, bephenium, pyrantel-praziquantel and pyrantel-bephenium for single-dose mass treatment of necatoriasis.

An effective drug for single-dose mass treatment of necatoriasis was sought by testing three drugs and two drug combinations in Ethiopian immigrants to Israel found to have light infections. The drugs tested sequentially in single-doses were pyrantel pamoate (20 mg kg-1, 81 subjects); bephenium hydroxynaphthoate (2.5-5 g, 65 subjects); combined pyrantel and bephenium (25 subjects); combined pyrantel (20 mg kg-1) and praziquantel (40 mg kg-1) (16 subjects); and albendazole (400 mg, 77 subjects). Follow-up under conditions without likelihood of reinfection was by one stool examination. Cure rates with albendazole, pyrantel-bephenium and pyrantel-praziquantel were 84, 80 and 81% respectively; these rates were significantly higher than the 49% found for bephenium and the 51% for pyrantel (P less than 0.05). Egg reductions in those not cured were pyrantel (22%), bephenium (6%), pyrantel-bephenium (34%), pyrantel-praziquantel (3%) and albendazole (6%). Albendazole was the most promising single drug treatment; unexpected was the high effectiveness of pyrantel-praziquantel in combination.

Adolescent↗
PubMed2006

Clinical field efficacy and safety of pyrantel pamoate paste (19.13% w/w pyrantel base) against Anoplocephala spp. in naturally infected horses.

Clinical field trials were conducted at five geographical locations in the USA (Oklahoma, Wisconsin, Tennessee, Virginia and Idaho) to evaluate the efficacy and safety of pyrantel pamoate paste (19.13%, w/w, pyrantel base) administered at the recommended dosage of 13.2 mg pyrantel base/kg (6.0 mg pyrantel base/lb) body weight (b.w.) against tapeworm infections of Anoplocephala spp. in naturally infected horses. Horses at each study site were allocated by restricted randomization based on the cestode status (positive or negative) of pre-treatment fecal egg counts to complete sets of four animals each or incomplete sets of fewer than four animals. Within sets comprising of two to four horses, one animal was randomly allocated to receive placebo vehicle paste and the remaining horse(s) received pyrantel pamoate paste administered orally at a minimum dosage of 13.2 mg pyrantel base/kg b.w. on Test Day (TD) 0. Single animal sets received pyrantel pamoate paste. Fecal samples of horses were collected and examined for equine tapeworm (Anoplocephala spp.) eggs a minimum of four times (once or thrice between TD -28 and -14, twice between TD -14 and -7, and once on TD 0) prior to treatment on TD 0. Fecal samples of horses that were positive for cestode infection pre-treatment were examined for cestode eggs on TD 7, 8, 9, 14, 15 and 16. Cestode-negative pre-treatment horses were not sampled again after treatment. A total of 241 horses (141 mares, 16 stallions and 84 geldings; 6 months-30 yrs of age; 173-646 kg; 13 recognized breeds and various crossbreds) were evaluated. The prevalence of Anoplocephala spp. determined by pre-treatment fecal examination ranged from 38.3% in Idaho to 68.1% in Tennessee with an overall prevalence of 52.3%. Ninety cestode-positive and 88 cestode-negative horses were treated with pyrantel pamoate paste, 36 cestode-positive and 27 cestode-negative horses were treated with placebo vehicle paste. Overall, 178 horses were treated with pyrantel pamoate paste, and 63 horses were treated with placebo paste. Of the 178 horses treated with pyrantel pamoate paste, no drug related, adverse clinical or neurological health events were observed. No doses of pyrantel pamoate paste were refused or lost during dosing. At each post-treatment time sampling interval, significantly fewer cestode eggs (P < 0.0115) were passed by cestode-positive horses treated with pyrantel pamoate paste compared to cestode-positive horses that received placebo paste. Efficacy of the pyrantel pamoate paste treatment ranged from 92 to 96% from TD 7 to TD 16 with an overall efficacy of 95%. The results of these trials demonstrated that pyrantel pamoate paste (19.13%, w/w, pyrantel base) administered orally at a dosage of 13.2 mg pyrantel base/kg b.w. is highly efficacious (95%) against Anoplocephala spp. and safe for use in horses with no adverse clinical or neurological health events observed under field use conditions.

Administration, Oral↗
PubMed1981

Relative efficacies of pyrantel tartrate and pyrantel citrate against Oesophagostomum sp in swine.

The relative efficacies of pyrantel tartrate and of pyrantel citrate against Oesophagostomum sp in swine were evaluated in a controlled-critical study and the efficacy of pyrantel citrate in a field trial. In the controlled-critical study, pigs naturally infected with Oesophagostomum dentatum were either not treated or were treated with pyrantel citrate or pyrantel tartrate at a dosage of 510 mg of free pyrantel base/kg of feed. Six days later, the pigs were necropsied, adult O dentatum was recovered and counted, and fecal samples were examined for helminth eggs. The efficacies of pyrantel citrate and pyrantel tartrate were each 100% based on fecal egg counts and numbers of adults at necropsy. The field trial was conducted in a similar manner except that pyrantel citrate only was tested against a control group on the basis of fecal egg counts made both at the beginning and at the termination of the trial. In this study pyrantel citrate was found to reduce Oesophagostomum sp egg counts by 89.4%.

Animals↗
PubMed1996

The kinetic disposition of pyrantel citrate and pamoate and their efficacy against pyrantel-resistant Oesophagostomum dentatum in pigs.

The pharmacokinetic disposition of pyrantel after intravenous (i.v.) and oral (p.o.) administration as the citrate and p.o. administration as the pamoate salt was determined in pigs. Following i.v. administration pyrantel was quickly cleared from the bloodstream, exhibiting a terminal half-life of 1.75 +/- 0.19 h and a residence time (MRT) of 2.54 +/- 0.27 h. After p.o. administration as the citrate salt, the absorption time (MAT) of pyrantel was 2.38 +/- 0.25 h and although significant quantities of pyrantel were absorbed (mean bioavailability of 41%) the rapid clearance resulted in a MRT of only 4.92 +/- 0.36 h. By comparison, the significantly extended MAT of the less soluble pamoate salt resulted in reduced circulating concentrations and a significantly lower mean bioavailability of 16%. The poor efficacy of pyrantel citrate against nematodes inhabiting the large intestine of pigs is therefore suggested to result from insufficient quantities of drug passaging to the site of infection. When tested against pyrantel-resistant adult Oesophagostomum dentatum the mean efficacy of pyrantel citrate was only 23%, whereas the efficacy of the lesser absorbed pyrantel pamoate was 75%. These results indicate that for maximum activity pyrantel should be administered to pigs as the pamoate salt.

Administration, Oral↗
PubMed2000

The disposition of pyrantel in the gastrointestinal tract and effect of digesta flow rate on the kinetic behaviour of pyrantel in the pig.

Pigs consuming a diet with slow digesta transit time were orally administered with molar equivalent doses of pyrantel as the citrate and pamoate salt. At appropriate intervals pigs were killed and the quantitative-time distribution of pyrantel throughout the gut contents was determined. Compared with the citrate, there appeared to be greater quantities of the less soluble pamoate salt in the small and large intestine. An additional group of pigs fed on diets with "slow" or "fast" digesta transit time were orally treated with molar equivalent amounts of pyrantel as the citrate and pamoate salt and the respective kinetic disposition of pyrantel in peripheral plasma and quantitative excretion in faeces was determined. The diet type had little effect on pyrantel availability after administration of the less soluble pamoate salt. However, the maximum concentration of pyrantel in plasma was lower and there appeared to be greater quantities of pyrantel retained in the gut and excreted in faeces when the citrate salt was orally administered to pigs fed the "fast" compared to the "slow" diet. Since it is the quantity of pyrantel contained in the gut lumen which is believed to affect efficacy against gastrointestinal parasites, greater efficacy with this anthelmintic should be obtained when pigs are consuming a high fibre diet.

Administration, Oral↗
PubMed2005

Target animal safety and tolerance study of pyrantel pamoate paste (19.13% w/w pyrantel base) administered orally to horses.

Pyrantel pamoate paste (19.13% w/w pyrantel base) for the treatment of tapeworm, Anoplocephala spp was evaluated for target animal safety and tolerance in horses treated orally at 0, 1, 3, 5, and 10 times the clinical dose of 13.2 mg pyrantel base/kg body weight administered daily for six consecutive days. Parameters evaluated included clinical signs, food and water consumption, body weights, physical examinations, clinical pathology (hematology, coagulation, serum chemistry, urinalyses, and fecal examinations), complete necropsy, organ weights, and histopathology. No adverse events or test article-related effects were observed in any treatment group during daily clinical observations of the test animals. Statistically significant changes (P < .05) lacked a dose- and/or time-dependent trend and were considered incidental. Administration of pyrantel pamoate paste did not produce any macroscopic or microscopic tissue effects in any dose group of either sex. The no-observed-effect-level (NOEL) for pyrantel pamoate paste, when administered orally to horses once daily for 6 consecutive days, was determined to be 132 mg/kg/day. Pyrantel pamoate paste (19.13% w/w pyrantel base) can be safely administered orally to horses at 13.2 mg of pyrantel base/kg for the treatment of Anoplocephala infestations.

Administration, Oral↗
PubMed2006

Pyrantel pamoate resistance in horses receiving daily administration of pyrantel tartrate.

CASE DESCRIPTIONS: 16 horses treated daily with pyrantel tartrate (2.64 mg/kg [1.2 mg/lb], PO) as part of a prophylactic anthelmintic program. CLINICAL FINDINGS: Fecal worm egg counts (FWECs) were obtained on all 16 horses. Mean FWEC was 478 eggs/g (epg; range, 0 to 4,075 epg). Three of the 16 horses were responsible for 85% of the total fecal egg output for the herd on the day of sampling. Six horses had FWECs < 200 epg. Three horses that had arrived within 4 months of the sampling date had FWECs < 100 epg. TREATMENT AND OUTCOME: An FWEC reduction test was initiated the day after FWECs were obtained; all horses with FWECs > 100 epg (9 horses) were treated with pyrantel pamoate (6.6 mg/kg [3 mg/lb], PO), and 14 days later, the FWEC was repeated. During the 14-day period, all horses received pyrantel tartrate (2.64 mg/kg, PO) daily. Fecal worm egg count reduction was calculated for each horse. Mean FWEC reduction for the group was 28.5% (range, increase of 21% in FWECs 14 days after treatment to a decrease of 100% in FWEC 14 days after treatment). CLINICAL RELEVANCE: Farms should be monitored for cyathostomes resistant to pyrantel pamoate prior to use of pyrantel tartrate. Fecal worm egg counts should be monitored routinely in horses before and after treatment to ensure efficacy of cyathostome control measures.

Administration, Oral↗
PubMed1994

Comparison of daily and monthly pyrantel treatment in yearling thoroughbreds and the protective effect of strategic medication of mares on their foals.

Studies on a Thoroughbred breeding farm in Ohio were done to: (1) compare the effects of daily administration of pyrantel tartrate feed pellets with monthly administration of a pyrantel pamoate paste to yearling horses (21 January-3 September); (2) assess the effects of daily pyrantel tartrate given strategically in spring/summer to foaling mares (1 April-16 August) and given for a prolonged period to barren mares (21 January-3 September); (3) determine if strategic medication of foaling mares with daily pyrantel tartrate protected their foals until weaning. There were no differences in cyathostome egg counts, pasture larval counts, body condition scores, or body weights of yearlings treated with daily pyrantel tartrate or monthly pyrantel pamoate. Both treatments failed to maintain fecal egg counts of yearlings below 100 eggs per gram (epg), and mean counts exceeded 400 epg (pyrantel pamoate) and 700 epg (pyrantel tartrate) in August and September, resulting in a sharp, but moderate increase in pasture infectivity in October. By contrast, prolonged or strategic use of daily pyrantel tartrate in mature horses were each highly effective in reducing pasture contamination and infectivity with cyathostome eggs and larvae respectively. Strategic medication of foaling mares provided protection of their foals until weaning and first treatment of foals was delayed until after weaning when mean strongyle counts exceeded 100 epg. Treatment of weanlings with pyrantel pamoate had little effect on egg counts. A comparative anthelmintic study with ivermectin, oxibendazole, and pyrantel pamoate confirmed earlier studies showing reduced efficacy of anthelmintics in young horses.

Administration, Oral↗
PubMed1993

Effects of pyrantel pamoate on adult and preadult Toxocara canis worms: an electron microscope and autoradiography study.

Adult as well as preadult Toxocara canis isolated from the intestine of a beagle were incubated for 2, 4, and 14 h in medium containing either different concentrations of pyrantel pamoate (23.6, 236, and 2360 micrograms/ml medium) or tritiated pyrantel pamoate (2.36 micrograms/ml medium). These incubations were performed to study the effects of pyrantel pamoate on the morphology of the parasitic nematodes and to obtain information concerning the mode of uptake, the distribution, and the total amount of pyrantel pamoate ingested by T. canis. The results of the ultrastructure studies indicate that the intestine, hypodermis, and muscle cells are the organs that are predominantly affected by the drug. Additionally, it turned out that the duration of the treatment, i.e., the incubation time, was more important in determining the efficacy of pyrantel pamoate against T. canis than was the concentration itself. Autoradiography studies revealed that the adult worms ingest the drug orally, whereas preadults absorb pyrantel pamoate mainly through the whole body surface. Finally, measurements of the total amount of pyrantel pamoate taken up by T. canis indicated that adult worms can limit or even reduce the ingestion of pyrantel for more than 4 h, but then ingest large amounts of the drug. Preadult worms, however, absorb the drug more or less continuously during the first 14 h through the cuticula, albeit in lower concentrations than the adults. The different experiments elucidate differences in the uptake of pyrantel pamoate as well as in the total amount of drug ingested or absorbed by adult or preadult worms, leading to the assumption that repeated treatment with lower concentrations will be more effective than high concentrations given only once.

Aging↗
PubMed1994

The action of pyrantel as an agonist and an open channel blocker at acetylcholine receptors in isolated Ascaris suum muscle vesicles.

The anthelmintic pyrantel is believed to act as an agonist at acetylcholine receptors on somatic muscle from the parasite Ascaris suum. This study aimed to confirm this mode of action of pyrantel. Single-channel recordings from muscle vesicles formed from the extrasynaptic region of the bag of somatic muscle cells of Ascaris suum were made using the patch-clamp technique. Pyrantel (0.03-100 microM) activated cation-selective channels with at least 2 conductance levels: main conductance 41 +/- 2.04 pS (mean +/- S.E., n = 28), smaller conductance 22.4 +/- 0.34 pS (mean +/- S.E., n = 8). The current/voltage plots showed a linear relationship. Detailed kinetic analysis revealed that activation of the receptor by pyrantel resulted in at least 2 distinct open and burst states and at least 3 distinct closed states. The mean open time of the channel, with 0.1 microM pyrantel, was 1.53 +/- 0.22 ms (mean +/- S.E., n = 7) at -75 mV. We have previously shown that acetylcholine activated channels with similar properties to the pyrantel-activated channels (Pennington, A.J. and R.J. Martin, 1990, J. Exp. Biol. 154, 201) confirming that pyrantel is an acetylcholine agonist. With high concentrations (100 microM) of pyrantel a sequence of rapid openings and closings of the channel was observed, indicating the presence of an open channel block. Previous experiments have shown that the anthelmintic levamisole, which also acts as an acetylcholine agonist on this preparation, induced channel block at hyperpolarised potentials with high concentrations (Robertson, S.J. and R.J. Martin, 1993, Br. J. Pharmacol. 108, 170). A comparison is made of the actions of the 3 agonists pyrantel, levamisole and acetylcholine at the nicotinic receptor in Ascaris muscle, and implications for the therapeutic use of the compounds are discussed.

Acetylcholine↗
PubMed1992

Comparative neuromuscular blocking actions of levamisole and pyrantel-type anthelmintics on rat and gastrointestinal nematode somatic muscle.

The basis for the comparative toxicity to parasitic nematodes and their mammalian hosts of the anthelmintics levamisole, pyrantel, and several related analogs on somatic nicotinic cholinergic transmission was examined. Measurements of muscle contractility and membrane potential were made using the isolated hemidiaphragm preparation of the rat and isolated axial muscle segments from the gastrointestinal nematode Haemonchus contortus. Pyrantel caused a dose- and time-dependent reduction of nerve-evoked twitches in the rat diaphragm. These effects were exacerbated by increasing the frequency of phrenic nerve stimulation from 0.5 to 50 Hz. Levamisole was less potent and the onset of its effects slower than pyrantel. Neither drug significantly affected twitches evoked from d-tubocurarine-blocked preparations following direct stimulation of the diaphragm. Twitch depression was reversed by washing, but not by application of physostigmine. In H. contortus, both drugs stimulated a spastic contraction and sustained paralysis in the concentration range of 1-10 microM, mimicking the action of nicotine. Neither nicotinic nor muscarinic antagonists blocked these responses. Moreover, neither nicotinic antagonists nor muscarinic agonists or antagonists had any independent effect on contractility of the parasite muscle segments. The blocking actions of levamisole and pyrantel on H. contortus axial muscle were associated with membrane depolarization at the muscle. In the rat-isolated hemidiaphragm, pyrantel, but not levamisole, depolarized end-plate regions of muscle fibers. d-Tubocurarine blocked the depolarizing action of pyrantel but not levamisole on rat-isolated hemidiaphragm. In axial muscle fibers of H. contortus, d-tubocurarine did not block the depolarizing actions of pyrantel, levamisole, or nicotine. 3-Bromo and 3-amino derivatives of levamisole were equipotent with and mimicked the actions of the parent compound on H. contortus axial muscle contractility. In the rat preparation, the 3-bromo derivative was more potent than levamisole or 3-amino-levamisole. 3-Amino-levamisole, but not 3-bromo-levamisole, depolarized muscle end-plate membrane in the rat diaphragm. Results of the present study are consistent with the following conclusions: (a) both levamisole and pyrantel block contractility of nematode axial muscle by causing sustained depolarization of the muscle membrane; (b) both drugs block neuromuscular transmission at the mammalian neuromuscular junction but their mechanisms appear to differ; (c) levamisole and pyrantel are more potent blockers of neuromuscular transmission in H. contortus than in the rat. These results suggest that potentially important pharmacological differences exist between nematode and mammalian somatic nicotinic receptors.

Animals↗
PubMed1995

Controlled efficacy study of the bioequivalence of Strongid C and generic pyrantel tartrate in horses.

The bioequivalence of Strongid C and generic pyrantel tartrate was determined in a controlled study using 30 horses with naturally acquired endoparasitic infections. Three horses were randomly allocated to each of ten replicates based on quantitative nematode and ascarid egg counts and fecal larvae culture results. Horses within each replicate were randomly assigned to one of three treatment groups. Horses in Treatment Group 1 received only oats; horses in Treatment Group 2 received generic pyrantel tartrate pellets (2.65 mg pyrantel tartrate kg-1) mixed with oats; horses in Treatment Group 3 were fed Strongid C pellets (2.65 mg pyrantel tartrate kg-1) mixed with oats. Horses were treated daily for a 30 day continuous treatment period. At the termination of the study the horses were necropsied and endoparasites recovered, identified, and enumerated. In all instances, no significant difference (P > 0.05) in mean numbers of parasites recovered existed between horses treated with generic pyrantel tartrate and Strongid C. Numbers of gastrointestinal parasites recovered from horses treated with generic pyrantel tartrate or Strongid C were shown to be significantly different (P < 0.05) from numbers of gastrointestinal parasites recovered from non-treated controls for the large strongyles (Strongylus vulgaris, S. edentatus, and Triodontophorus spp.), small strongyles (Cyathostomum spp., Cylicocyclus spp., and Cylicostephanus spp.) and fourth-stage Parascaris equorum. Numbers of adult P. equorum recovered from horses treated with Strongid C were also significantly different (P < 0.05) from those from non-treated controls. Numbers of adult P. equorum recovered from horses treated with generic pyrantel tartrate were not significantly different (P = 0.0761) from those from non-treated controls. The determination of bioequivalence was based upon the 95% confidence interval of the difference between the mean number of parasites recovered from horses treated with generic pyrantel tartrate and the mean number of parasites recovered from horses treated with Strongid C. For all instances in which the numbers of parasites recovered from horses treated with either Strongid C or generic pyrantel tartrate were significantly different from the numbers of parasites recovered from non-treated controls, bioequivalence was demonstrated.

Animal Husbandry↗
PubMed2006

Cyathostomes in horses in Canada resistant to pyrantel salts and effectively removed by moxidectin.

Clinical trials using fecal egg count reduction tests and coproculture were conducted with yearlings and mares on a farm in 1997. Fecal samples were taken from each horse to estimate the number of strongyle eggs/g feces with Cornell-Wisconsin centrifugal flotation and Cornell-McMaster dilution techniques. Eleven of 15 yearlings, which had been on a daily feeding of grain with pyrantel tartrate for 66 d were found with strongyle eggs in feces. This was the first time the in-feed medication had been used on the farm. Nine yearlings were randomised into three groups; continuation of daily pyrantel tartrate or one treatment with pyrantel pamoate or moxidectin. Two of three yearlings given pyrantel tartrate or pamoate had no reduction in the eggs/g feces. These six yearlings were then given moxidectin and in all yearlings the eggs/g feces was reduced to zero. The 66 d of pyrantel tartrate use was an inadequate time for development of resistant cyathostomes and a hypothesis was the resistance was due to extensive use on the farm over many years of pyrantel pamoate at twice the label dose for control of tapeworms. That hypothesis was tested with 12 mares with strongyle eggs in the feces randomised into two treatment groups: pyrantel pamoate at label dose or moxidectin. Five of six mares given pyrantel had <80% reduction in egg/g feces. These mares were then given moxidectin and in all mares the eggs/g feces was reduced to zero. Only cyathostomes were found on culture and apparently there was side resistance among the pyrantel salts.

Animals↗
PubMed1970

Aspects of the pharmacology of a new anthelmintic: pyrantel.

1. The pharmacological properties of an anthelmintic, pyrantel, and some of its analogues have been described and compared with piperazine in a variety of vertebrate and helminth preparations.2. Pyrantel and its analogues in common with nicotine and decamethonium cause spastic paralysis in chicks and contracture of the chick semispinalis and toad rectus abdominis muscles.3. In the soleus and anterior tibialis muscles of the cat, pyrantel in large amounts caused a short-lived neuromuscular block that was preceded by initial depolarization.4. In preparations from cat and rat, pyrantel showed properties common to both competitive and depolarizing neuromuscular blocking drugs.5. Pyrantel blocked the contracture evoked by transmural stimulation and caused a marked contracture of the worm. Piperazine caused a gradually developing reduction in the responses to transmural stimulation and no contracture.6. Pyrantel and its analogues caused a slowly developing contracture of strip preparations of Ascaris, being more than 100 times more active than acetylcholine in this respect. Piperazine caused a relaxation of Ascaris strip preparations and in common with (+)-tubocurarine blocked the responses to acetylcholine and pyrantel analogues on this preparation.7. Pyrantel caused depolarization and increased spike discharge frequency in single muscle cells of Ascaris, these changes being accompanied by increase in tension. Piperazine, on the other hand, caused hyperpolarization and reduction in spike discharge frequency and relaxation, and antagonized the effects of pyrantel.

Animals↗