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At least 19 recordsLinked to original sources
PubMed1987

Treatment of fish parasites. 2. Effects of praziquantel, niclosamide, levamisole-HCl, and metrifonate on monogenea (Gyrodactylus aculeati, Diplozoon paradoxum).

In research for successful treatment of fish parasitized by monogeneans, four substances (Praziquantel, Niclosamide, Levamisole-HCl, and Metrifonate) were tested in vivo against Gyrodactylus aculeati parasitizing the skin of sticklebacks (Gasterosteus aculeatus). Fish were incubated in water containing different solutions of the drugs. Praziquantel, Niclosamide and Levamisole-HCl were effective against Gyrodactylus aculeati. Praziquantel caused irreversible lesions in the parasite tegument (beginning with 1 microgram/ml and 90 min exposure). Niclosamide was effective in a narrow concentration range of 0.075-0.1 microgram/ml (90 min). Levamisole-HCl was effective in a concentration range of 20-50 micrograms/ml for 120 min. Like Praziquantel, Niclosamide and Levamisole-HCl led to damage of the parasite tegument. The opisthaptor region and the openings of the cephalic glands were most severely affected. Furthermore, the effects of Niclosamide, Levamisole-HCl and Metrifonate on Diplozoon paradoxum parasitizing the gills of chubs (Squalius cephalus) and breams (Abramis brama) were investigated. Levamisole-HCl (10 micrograms/ml) and Niclosamide (0.2 microgram/ml) were effective against Diplozoon paradoxum after an exposure of 90 min and 45 min in vitro. The parasites were severely affected along the midbody. Metrifonate caused a lysis of the tegument and a strong secretion of slime. It is suggested that chemotherapy against Gyrodactylus sp. may be accomplished with 10 mg Praziquantel/l for 3 h during storage in smaller tanks. Niclosamide (0.1 mg/l for 90 min), or Levamisole-HCl (50 mg/l for 120 min) may be used alternatively. Concentrations of Niclosamide and Levamisole-HCl have to be calculated with accuracy, since fish only tolerate a very narrow range of these drugs (Niclosamide: 0.1 mg/l for 120 min; Levamisole-HCl: 50 mg/l for 120 min).

Animals↗
PubMed2000

The effects of clofazimine, niclosamide & amphotericin B, on electron transport of Leishmania donovani promastigotes.

BACKGROUND & OBJECTIVES: The study was undertaken to explore the locus of interaction of clofazimine and niclosamide which showed substantial growth inhibition property in Leishmania donovani promastigotes. METHODS: The uptake of final electron acceptor oxygen and 2,6-dichlorophenolindophenol (DCPIP) reduction in the electron transport chain were measured by constant volume Warburg respirometer and monitoring absorbance at 600 nm, respectively. Irreversibility of O2 uptake inhibition by clofazimine and niclosamide was determined by dilution of cell suspension followed by centrifugation. RESULTS: Clofazimine and niclosamide showed their minimum inhibitory concentration (MIC) at 33 and 150 micrograms/ml, respectively. Oxygen uptake inhibition by clofazimine and niclosamide was not reversed by removal of the drug by centrifugation. Rotenone, a potent inhibitor of mammalian electron transport chain showed no inhibition on the electron transport chain of L. donovani promastigotes. Cyanide at 1 mM concentration showed partial inhibition in L. donovani promastigotes. Oxygen uptake and DCPIP reduction by L. donovani promastigotes were highly sensitive to sulphhydryl group inhibitors. Strong inhibition of oxygen uptake (80-100%) by L. donovani promastigotes was achieved by clofazimine, niclosamide and amphotericin B. Amphotericin B failed to inhibit DCPIP reduction by L. donovani promastigotes, whereas DCPIP reduction was inhibited by clofazimine and niclosamide, respectively. INTERPRETATION & CONCLUSION: DCPIP reduction was mediated by transplasma membrane electron transport as evidenced by its inhibition with membrane impermeable quinone 1,2-naphthoquinone-4-sulphonic acid (NQSA). Transplasma membrane electron transport requires b-cytochromes and sulphhydryl groups for its function and was inhibited by clofazimine and niclosamide.

Amphotericin B↗
PubMed1987

Laboratory selection for increased tolerance to niclosamide in Bulinus truncatus (Gastropoda: Planorbidae) from Iran.

Survivors of Bulinus truncatus from one exposure to niclosamide (Bayluscide) were used to establish the next generation in a five generation long laboratory selection for increased tolerance to niclosamide. In a comparison of the tolerance to the molluscicide between two original and two selected strains about 150 snails of each strain, divided into four size-groups, were exposed to aliquots of the same niclosamide solution on the same day and during the same time of the day. It was shown that five generations of relatively mild selection (30-50% survival) resulted in a significant increased tolerance to niclosamide in snails with only one exposure before start of the selection procedure. A comparison with published data indicated that the unselected strains did not change their tolerance to niclosamide during seven years of laboratory breeding. The strain exposed to niclosamide once in each of 16 generations showed an avoidance reaction to the chemical by crawling out of the water.

Animals↗
PubMed1994

Evaluation of a twice-a-week application of 1% niclosamide lotion in preventing Schistosoma haematobium reinfection.

A randomized double-blind trial was conducted to assess the efficacy of a twice-a-week application of 1% niclosamide lotion for prevention of Schistosoma haematobium reinfection. Six hundred farmers in Fayoum, Egypt, 18-40 years of age, were treated to cure their S. haematobium infection, then randomly assigned to self-apply niclosamide or placebo lotion to their limbs, neck, and torso. Subjects were exposed to schistosomal-infested water during routine irrigation activities from April to October 1992. Three hundred fifty subjects met the inclusion criteria and completed the trial, 169 (48.3%) in the niclosamide group and 181 (51.7%) in the placebo group. The subjects assigned to the niclosamide-treated group were comparable with those in the placebo group in age (27.2 versus 27.8 years), total water contact (101.9 versus 109.0 hr), lotion application compliance (93.5% versus 90.6%), and avoidance of whole body water contact (94.7% versus 96.7%). The reinfection rate with S. haematobium was 30.8% in the niclosamide-treated group and 28.2% in the placebo group. Niclosamide lotion applied to the limbs and trunk twice a week failed to prevent S. haematobium reinfection.

Administration, Topical↗
PubMed1988

Sperm shape abnormality and urine mutagenicity in mice treated with niclosamide.

Niclosamide, a widely used anthelmintic drug in underdeveloped countries, is known to be mutagenic in the Salmonella typhimurium microsomal test system. The urine obtained from mice treated with niclosamide is mutagenic in the TA98 and TA1538 strains. Its effects on mouse-sperm morphology were evaluated in CD1 and (BALB/cJ x DBA/2J) F1 mice after 5 daily oral niclosamide doses of either 60, 80, 100 or 120 mg/kg. A statistically significant increase in abnormal sperm morphology was detected in both CD1 and (BALB/cJ x DBA/2J) F1 mice. No drug-related effects on testis weight nor on sperm count were observed in either genotype. Urine samples obtained from niclosamide-treated F1 mice were assayed with the Salmonella typhimurium strain TA1538 both in the absence and presence of beta-glucuronidase. In the absence of glucuronidase, urine mutagenicity increased with increasing dose and the highest doses were toxic. In the presence of glucuronidase, urine mutagenicity and toxicity also increased. Only at the highest dose (120 mg/kg), however, was there a positive correlation between the urine mutagenic activity and an increase in the number of abnormal sperm. The results of this study suggest that the increase in abnormal sperm depends on the systemic presence of non-conjugated niclosamide metabolites.

Animals↗
PubMed1977

The metabolism of niclosamide and related compounds by Moniezia expansa, Ascaris lumbricoides var suum, and mouse- and sheep-liver enzymes.

1. Niclosamide and related nitro compounds were reduced to the corresponding amines by Moniezia expansa, Ascaris lumbricoides var suum and by enzymes prepared from these species and by mouse and sheep liver homogenates. The reduction of niclosamide by the helminths required as cofactors NADH2 and glutathione, but was inhibited 50% by 2 X 10(-7) M allopurinol. 2. Unlike benzanilide, niclosamide was not hydrolysed by either the helminths, or the mammalian liver preparations. Rates of hydrolysis of compounds related to niclosamide indicate that niclosamide was not hydrolysed because substituents in both benzene rings ortho to the amide bond sterically hinder the hydrolase. 3. Hydrolysis of benzanilide and related compounds was inhibited by anthelmintic organophosphates.

Allopurinol↗
PubMed1991

Mutagenic activity of 2-chloro-4-nitroaniline and 5-chlorosalicylic acid in Salmonella typhimurium: two possible metabolites of niclosamide.

Niclosamide is an anti-helminthic drug susceptible to being metabolized into a bacterial mutagen by the action of enzymes present in the S9 activation mixture. Additional results from genotoxic studies in rodents and humans suggest that the drug is absorbed from the gastrointestinal tract, and mutagenic metabolites are excreted both in the free form and as conjugated glucuronides. As in the case of other secondary amides, phase I metabolism of niclosamide may result in a hydrolytic cleavage of the amide bond, giving rise to 5-chlorosalicylic acid and 2-chloro-4-nitroaniline as the main metabolites. In this study, the mutagenicity of these compounds was tested using the Salmonella typhimurium assay. Bacterial mutagenicity tests with these 2 compounds reveal a non-mutagenic response with 5-chlorosalicylic acid and a mutagenic one with 2-chloro-4-nitroaniline. However, the mutagenic potency observed with this compound is lower than that of niclosamide. The role of nitroreduction in the activation of niclosamide and 2-chloro-4-nitroaniline was also investigated with the help of S. typhimurium strains TA98NR, YG1020, YG1021 and YG1024. The results show a pattern of response which is qualitatively similar for both compounds and this indicates that its mutagenicity depends on both nitroreduction and transacetylation.

Aniline Compounds↗
PubMedDate not supplied

Taeniasis unresponsive to a single dose of niclosamide: case report of persistent infection with Taenia saginata and a review of therapy.

A patient infected in Ethiopia with the beef tapeworm Taenia saginata was unsuccessfully treated with 2 g of niclosamide on four separate occasions over four months. clinical and parasitologic cures were effected by a regimen of 2 g of niclosamide given on three consecutive days. Niclosamide is the drug of choice for treatment of T. saginata and Taenia solium (pork tapeworm) infection; cure rates are approximately 90%. It is not absorbable and thus is nontoxic. Alternative treatments of taeniasis vary in the degree of safety; tin compounds and Aspidium extracts often are toxic. Paromomycin sulfate, which is also nonabsorbable, is effective, although adverse gastrointestinal effects are common with multiple-dose regimens. A relatively safe therapy is with mebendazole, a broad-spectrum anthelmintic agent, although efficacy has varied in different trials. A number of benzimidazoles, as well as nitazoxamide, have been effective against tapeworms. Praziquantel is the best alternative to niclosamide in terms of cost, efficacy, availability, and safety.

Adult↗
PubMed1993

Field trial of 1% niclosamide as a topical antipenetrant to Schistosoma mansoni cercariae.

A randomized, double-blind, placebo-controlled field trial of a topical antipenetrant lotion, 1% niclosamide, applied daily to the upper and lower limbs of farmers occupationally exposed to Schistosoma mansoni cercarial-infested water, was conducted in the Nile Delta to assess its safety and efficacy in preventing reinfection. Farmers aged 18-40 years were treated to cure their S. mansoni infections three months prior to the onset of the trial. Subjects were randomly assigned to receive niclosamide or placebo lotion that was self-applied daily for five months. A total of 186 subjects met the inclusion criteria and completed the trial. The exposure to schistosomal-infested water occurred during routine irrigation activities from June to November 1991. Stool specimens were evaluated monthly during and for two months following the lotion application period. The subjects applying the niclosamide lotion were comparable to those applying placebo lotion in age (mean 30 years for both), total water contact (184.5 hr versus 173.8 hr), reported lotion application compliance (88% versus 92%), and reported water contact involving skin exposure other than upper and lower limbs (23% versus 27%). The schistosomal reinfection rate was lower in the niclosamide group (53.3%) compared with the placebo lotion group (71.3%), (P < 0.02). Increased protection might be obtained with total body application for shorter, less intense, water contact exposures.

Administration, Topical↗
PubMed1976

Comparative effects of uredofos, niclosamide, and bunamidine hydrochloride against tapeworm infections in dogs.

A single dose of a new broad-spectrum anthelmintic, uredofos, was more effective than single doses of either bunamidine hydrochloride (HCI) or niclosamide in removing natural infections of Dipylidium coninum from pound dogs, as determined by necropsy examination for scolices. The efficacy of uredofos was equal to that of bunamidine HCI and exceeded that of niclosamide in removing Taenia spp from his host. All of 12 dogs harboring D caninum and all of 5 dogs harboring Taenia spp were completely cleared of tapeworm infection following treatment with uredofos at 50 mg/kg of body weight. Bunamidine HCl cleared 9 of 11 dogs (82%) of D caninum and 5 of 5 dogs of Taenia spp. Niclosamide had the least anticestodal activity of the 3 drugs; 2 or more scolices of D caninum were found at necropsy in each of 12 dogs treated with this drug. Four of 5 dogs were cleared of Taenia spp following niclosamide therapy. Untreated control dogs did not shed tapeworms of either species during a 3-day period of posttreatment fecal collections, but did have tapeworms at the time of necropsy.

Amidines↗
PubMed2000

Mepacrine therapy in niclosamide resistant taeniasis.

OBJECTIVE: To evaluate the efficacy of mepacrine (quinacrine) in patients with niclosamide resistant Taenia saginata infection. METHODS: Eighty six cases with niclosamide resistant Taenia saginata (unresponsive to 2-8 courses of niclosamide) were treated with quinacrine (1 g) administered orally or via a nasogastric tube, and followed at 2, 4, 8 and 12 weeks for recurrence of passage of proglottids and presence of Taenia eggs in the stool examinations. Pre and post-therapy egg counts were obtained and egg viability was tested by staining with methylene blue. RESULTS: Eighty-one (94.2%) patients responded promptly with passage of the worm within 4-72 hours. The egg counts showed a drastic fall in 79 cases and a fall in viability from a median of 100% to 0% was observed. Only one patient demonstrated a relapse at 4 weeks. Gastrointestinal side effects occurred in 9 cases but were controlled easily by symptomatic therapy. CONCLUSION: We conclude that quinacrine is a safe, inexpensive, effective and generally well tolerated drug for the treatment of niclosamide resistant Taenia saginata infestations.

Adolescent↗
PubMedDate not supplied

Studies on the comparative efficacy of mebendazole, flubendazole and niclosamide against human tapeworm infections.

The efficacy of Mebendazole and Niclosamide was studied in two groups of 24 and 38 cases, respectively of patients suffering from taeniasis. Mebendazole with dose schedule of 200 and 300 mg twice daily for 3 consecutive days showed a cure rate of 71.42% and 92.30%, whereas Niclosamide at the dose rate of 200mg per patient was 94.76% effective. Flubendazole showed a cure rate of 66.66% only. Mebendazole and Niclosamide possess high taeniacidal activity, ability to reduce the clinical symptoms of taeniasis without any side effects. Niclosamide with high activity and excellent tolerance, is a drug of choice for the treatment of taeniasis in single dose treatment while for hymenolepsiasis it needs extended course.

Antinematodal Agents↗
PubMed1996

The molluscicidal activity of two 2-benzamido-5-nitrothiazole bihalogenated derivatives and niclosamide. Influence of some environmental factors on their toxicity.

Two synthetic molluscicides, 3,4-dichloro-2-benzamido-5-nitrothiazole (3,4-dichloro-BNT) and 3,5-dichloro-BNT, were studied to determine their efficacy against the snail Lymnaea glabra. Results were compared with those of a reference molluscicide, niclosamide. Snail exposure to these chemicals markedly increased overall snail mortality during the experiment (96 h). The LC50 values slightly decreased and, at day 4, were lower for the two BNT derivatives than for niclosamide. The effect of several factors on compound toxicity was also studied using lethal concentrations near LC50. Acclimatization duration under controlled conditions had a variable influence upon overall snail mortality according to the compound. No significant variation in the overall mortality was detected in snail groups exposed to 3,4-dichloro-BNT. On the other hand, snail mortality greatly increased in the 3,5-dichloro-BNT-exposed groups when the duration increased from 24 h to 15 days; the same result was obtained in the niclosamide-exposed snails acclimatized for 8 days. Snail mortality increased in the presence of sand, whatever compound was used, and greatly decreased in the presence of marl; it was also higher with water of low calcium content. When the food supply was low, snail mortality greatly decreased in the niclosamide- and 3,4-dichloro-BNT-exposed groups, whereas it increased in the case of 3,5-dichloro-BNT. In the presence of running water, the number of dead snails with 3,4-dichloro-BNT was identical to that of controls, whereas it was greater with the other molluscicides. These experiments, carried out under controlled conditions, demonstrate that the use of a molluscicide in the field must take into account its chemical properties as well as the characteristics of the snail habitat to optimally eliminate snails.

Adaptation, Physiological↗
PubMed1991

Dermal absorption of niclosamide in rats and minipigs.

The dermal absorption of niclosamide, a drug shown to prevent Schistosomiasis by blocking the dermal penetration of cercariae, has been examined in Sinclair minipigs and rats. Radioactivity in the urine and feces collected daily for 7 days after application of 14C-niclosamide accounted for less than 2 per cent and 10 per cent of the labelled compound applied to pig and rat skin, respectively. Approximately 20 per cent of the radioactivity from the dose solution was recovered on the skin excised from the area of application in both minipigs and rats. No radioactivity was detected in organs removed from the pig 7 days after application of radiolabelled drug while less than 6 per cent of the dose could be accounted for in the rat organs/carcass. Radioactivity in swine blood, removed 0.5, 1, 2, 4 and at 24 h intervals after dosing, was at or below three times background in all of the samples. Total recovery of the applied radioactivity was 78 per cent in pigs and 57 per cent in rats. These studies indicate that niclosamide is very poorly absorbed after dermal application. The results are consistent with earlier comparative studies showing that dermal penetration of xenobiotics in rats is generally higher than in swine.

Administration, Cutaneous↗
PubMed1980

Extractive alkylation of 5,2'-dichloro-4'-nitrosalicylanilide (niclosamide) for gas-liquid chromatographic analysis.

Niclosamide (5,2'-dichloro-4'-nitrosalicylanilide), formulated as the ethanolamine salt, is one of the most effective and widely used molluscicides for the control of snail vectors of schistosomiasis, a parasitic disease afflicting over 200 million people in more than 70 countries. This report details the development of a sensitive, specific analytical method for the evaluation of niclosamide formulations and assessment of the impact of residues on the environment. Efficient (greater than 85%) phase-transfer, N,O-dimethylation of niclosamide and the synthesized 5-deschloro analog internal standard, followed by gas-liquid chromatographic separation and electron-capture detection, permits the determination of as little as 10 ppb analyte in fortified, stagnant water. Tetrabutylammonium chloride was the phase-transfer agent, while methyl iodide was the methylating agent of choice among four investigated.

Animals↗
PubMedDate not supplied

The prolonged use of niclosamide as a molluscicide for the control of Schistosoma mansoni.

Applications of niclosamide at three-monthly intervals were undertaken for 14 years in foci of Biomphalaria glabrata in the water sources of Peri-Peri (Capim Branco, MG). All the residents of the area were submitted to an annual fecal examination (Kato/Katz) and those individuals eliminating Schistosoma mansoni eggs were treated with oxamniquine. A malacological survey was undertaken at three-monthly intervals by means of ten scoops with a perforated ladle each ten metres along the two banks of the ditches and streams of the region. Where snails were found, molluscicide was applied by means of dripping or aspersion using a 3 ppm aqueous suspension of niclosamide. Initially, a mean of 14.3% of snails in the region were found to be eliminating cercariae. Following the first four applications of molluscicide, this was reduced to 0.0% and maintained at about 1.5% throughout the program. Thus, there was a continued possibility of schistosomiasis transmission in the area and it was observed that the population of snails reestablished itself within three months of molluscicide application. The results obtained in this study do not encourage the continual use of niclosamide as the only method of control of schistosomiasis.

Animals↗
PubMed2000

Effect of niclosamide on the marketable fish Liza ramada (Risso, 1826) concerning accumulation in muscles and activities of three metabolic liver enzymes.

The accumulation in muscles and the effect of different concentrations of niclosamide (Bayluscide) on the metabolic enzymes; succinate dehydrogenase (SDH), pyruvate dehydrogenase (PDH) and lactate dehydrogenase (LDH) in the liver of the Thin-lip grey mullet after 1, 2 & 3 weeks were studied. The molluscicide residues were detected in the muscles. The residues increased with the increase of concentrations of niclosamide as well as the time of exposure. On the other hand, LDH showed significant increase. But, SDH and PDH showed significant decrease. No doubt, this disturbance in the three liver enzymes cause disturbance in the process of metabolism. The important point is what about man who consumes a fish with niclosamide accumulated in its muscles.

Animals↗
PubMed1991

Topical niclosamide as a protective agent against schistosome infection.

Niclosamide, as a semisolid pharmaceutical form suitable for external use, was used in 4 different concentrations (0.5%, 1%, 2% & 4%) to paint albino mice tails at different periods before exposure to infection with S. mansoni cercariae. Complete protection (100%) was achieved in all mice painted on the same day, the previous day and 3 days before exposure to cercariae irrespective to the niclosamide concentrations. Neither eggs nor worms were detected. Also, no pathological changes were found in livers, spleens or intestines of those mice. On the other hand, no protection against infection was achieved in mice painted with, 0.5% or 1%, 7 days before exposure to cercariae. Partial protection (25% and 40%) was gained in mice painted with 2% or 4% concentration of the drug respectively. It can be concluded that locally application of niclosamide as an ointment can completely prevent the infection with S. mansoni for three days. So, testing the promising drug for human trials to evaluate its efficacy specially for those at high risk is recommended.

Administration, Topical↗