PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “Bephenium Compounds”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

214 records · Page 12Linked to original sources
PubMed1993

[Field studies on different control schemes for hookworm infection].

Three different control schemes including selective chemotherapy, a combination of selective chemotherapy and management of fecal disposal and mass treatment with mebendazole-medicated salt were implemented for the control of hookworm infection in Luwo Town and Taiping Village, Wuming County, Guangxi Zhuang Autonomous Region during 1971-1990. Through ten years of selective chemotherapy, the results showed that the hookworm infection rate dropped from 42.6% to 3.9% and the infection intensity from 425.6 eggs per gram faeces to 1.6 eggs per gram faeces. After seven years of selective chemotherapy combined with management of fecal, the hookworm infection rate dropped from 58.7% to 10.9% and the infection intensity from 111.5 eggs per gram faeces to 8.5 eggs per gram faeces. However, 3 years after the termination of the combined treatment, the hookworm infection rate increased to 14.5%. As for the implementation of the third scheme, mebendazole-medicated salt was given at 100 mg daily for 30 consecutive days or at 50 mg daily for 30 consecutive days. Stool examination was made one year after the treatment, the results showed that the infection rate of the inhabitants dropped from 36% and 36% to 2% and 1.3%, respectively, and the infection intensity dropped from 110.3 and 246 eggs per gram faeces to 1.3 and 0.24 eggs per gram faeces. After three years, the infection rate of inhabitants remained under 2% and the infection intensity under 1 egg per gram faeces. It was concluded that mass treatment with mebendazole-medicated salt might be the most practical scheme for the control of hookworm infection.

Ancylostomiasis↗
PubMed2006

Pharmacology of N-, L-, and B-subtypes of nematode nAChR resolved at the single-channel level in Ascaris suum.

Pharmacological experiments on Ascaris suum have demonstrated the presence of three (N-, L-, and B-) subtypes of cholinergic receptor mediating contraction of body wall muscle in parasitic nematodes. In the present study, these ionotropic acetylcholine (ACh) receptors (nAChRs) were activated by levamisole and bephenium under patch-clamp conditions and competitively antagonized by paraherquamide and 2-desoxoparaherquamide. A number of recordings exhibited three separate current amplitude levels, indicating the presence of small, intermediate, and large conductance subtypes of receptor. The mean conductance of the small conductance subtype, G25, was 22 +/- 1 pS; the intermediate conductance channel, G35, was 33 +/- 1 pS; and the large conductance channel, G45, was 45 +/- 1 pS. The small channel was not antagonized significantly by paraherquamide and was identified as the N-subtype. The intermediate channel was preferentially activated by levamisole rather than bephenium and antagonized by paraherquamide: the intermediate channel was identified as the L-subtype. The large conductance channel was preferentially activated by bephenium, antagonized more by 2-desoxoparaherquamde than by paraherquamide and was identified as the B-subtype. These observations reveal that the three channel subtypes have different selectivity for cholinergic anthelmintics. The different selectivity of these compounds should be considered when dealing with drug resistant infections.

Animals↗
PubMed1977

Comparative studies on the evaluation of the effect of new anthelminthics on various intestinal helminthiasis in Iran. Effects of anthelminthics on intestinal helminthiasis.

The effect of pyrantel pamoate, levamisole, mebendazole, thiabendazole and bephenium hydroxynaphthoate on various intestinal helminths were evaluated among the inhabitants of four villages in the Dezful area southwest of Iran. A total number of 328 persons, all infected simultaneously with Ascaris and hookworm (Ancylostoma duodenale) and 49.2% with Trichostrongylus spp., were randomly divided into six groups. One group was kept as the control and the other five were each treated with one compound. Follow-up examinations showed that all of the drugs used were highly effective on Ascaris, and the differences in the cure rate were not statistically significant except for bephenium hydroxynaphthoate which showed a lower cure rate. For hookworm, cure rates of 100, 90, and 85% were observed with levamisole, pyrantel pamoate and bephenium hydroxynaphthoate, respectively. Cure rates observed with mebendazole and thiabendazole were 35 and 51%, respectively. For Trichostrongylus, the highest cure rate was achieved with levamisole, followed by thiabendazole and mebendazole. While the percentage of people showing side-effects was rather low for all drugs, thiabendazole and bephenium hydroxynaphthoate produced a higher, and levamisole a lower, percentage of side effects.

Adolescent↗
PubMed2005

Contractile activity and motility responses of the dog heartworm Dirofilaria immitis to classical anthelmintics and other compounds.

A variety of compounds including classical anthelmintics and avermectin analogs were screened for their effects on movements of adult heartworms (HW) (Dirofilaria immitis). Contractile activity was measured by tension recording of spontaneous movements of intact HW coil preparations (6 min compound exposure) and motility was evaluated by observation of spontaneous, free movements in culture (3 and 7 days compound exposure). Results for female HW indicated that some compounds caused spastic paralysis of contractile activity and inhibition of motility in culture (bephenium, DL-tetramisole, and pyrantel); some caused only spastic paralysis of contractile activity (methyridine and disophenol); and some caused only inhibition of motility in culture (chlorpromazine, dithiazanine, 1-ethoxycarbonylmethyl-1-methylpyrrolidinium, and 4-methyltropolone). Effects on motility in culture appeared to be lethal. The following compounds lacked effects: amprolium, 2-amino-2-thiazoline, bithionol, bitoscanate, bitriben, hexachlorophene, ivermectin, and 10 H-phenothiazine. A group of avermectin analogs was screened for effects only on motility in culture of both adult female and male HW. Several of the analogs affected motility, but the effects appeared to be non-lethal. Microfilaria release into the culture media was suppressed by two of the analogs (an aglycone and avermectin B2). The HW maintenance system used in the present study facilitated screening of compounds for effects on this parasite.

Animals↗
PubMed1988

Mutagenicity of products generated by the reaction between several antiparasitic drugs and nitrite.

Drugs containing secondary aliphatic amines, heterocyclic nitrogen, or secondary aliphatic amido groups (chloroquine, dehydroemetine, mebendazole, and piperazine) and pyrimidine derivatives such as pyrantel pamoate were reacted in vitro with sodium nitrite at pH 3.7 and became mutagenic for Salmonella typhimurium strain TA1535. The products derived from the nitrosation of chloroquine and dehydroemetine required metabolic activation by mammalian hepatic S9 to be mutagenic. The N-nitroso derivatives of mebendazole, piperazine, and pyrantel pamoate were mutagenic with and without S9, although more activity was noted in the presence of S9 with the nitrosated compounds formed from mebendazole and piperazine. Under identical conditions, no mutagenic products were detected from quaternary ammonium salts such as bephenium hydroxynaphthoate or drugs containing tertiary heterocyclic amino groups, such as iodochlorhydroxyquin.

Amebicides↗
PubMed1989

Mutagenicity of urine from mice exposed orally to nitrite and various aminated antiparasitic drugs.

Mutagenic N-nitroso compound formation from the in vitro reaction of amebicides and anthelmintic drugs, which are pyrimidine derivatives or contain secondary aliphatic amines or heterocyclic nitrogens, has been previously described (Arriaga Alba et al.: Environmental and Molecular Mutagenesis 12:65-73, 1988). Under similar conditions, antiparasitic drugs containing halogenated derivatives of tertiary amines or quaternary ammonium salts do not form mutagenic nitrosated compounds. In the present study the mutagenic activity of mouse urine was determined after oral administration of sodium nitrite and the two above-mentioned groups of drugs (pyrantel pamoate, chloroquine, piperazine and dehydroemetine/iodochlorhydroxyquin and bephenium hydroxynaphthoate, respectively). Results show that the simultaneous administration of piperazine or chloroquine with sodium nitrite produced urinary mutagens that appeared conjugated as glucuronides, whereas pyrantel pamoate and dehydroemetine in the presence of nitrite caused only slightly mutagenic urine. No mutagenic activity was detected in the urine of mice to which halogenated derivatives of tertiary amines (iodochlorhydroxyquin) or quaternary ammonium salts (bephenium hydroxynaphthoate) were administered together with nitrite.

Amebicides↗
PubMed2002

Paraherquamide and 2-deoxy-paraherquamide distinguish cholinergic receptor subtypes in Ascaris muscle.

Paraherquamide is a novel natural anthelmintic product with a mode of action that is incompletely characterized. Nicotine and cholinergic-anthelmintic agonists of different chemical classes were used to produce contraction in Ascaris muscle strips. Paraherquamide and a semisynthetic derivative, 2-deoxy-paraherquamide, antagonized these responses. Analysis of the actions of the antagonists was made using the simple competitive model and nonlinear regression to estimate the pK(B) values of the antagonists. The analysis was tested using Clark plots. The pK(B) values for paraherquamide were: nicotine, 5.86 +/- 0.14; levamisole, 6.61 +/- 0.19; pyrantel, 6.50 +/- 0.11; and bephenium, 6.75 +/- 0.15. The pK(B) of nicotine was significantly different from the pK(B) values for levamisole, pyrantel, and bephenium, showing that paraherquamide can distinguish a subtype of cholinergic receptors sensitive to nicotine and a subtype of cholinergic receptors sensitive to levamisole, pyrantel, and bephenium. The pK(B) values for 2-deoxy-paraherquamide were: levamisole, 5.31 +/- 0.13; pyrantel, 5.63 +/- 0.10; and bephenium, 6.07 +/- 0.13. The Clark plots of the antagonism illustrated the degree of fit to the competitive model for 2-deoxy-paraherquamide. 2-Deoxy-paraherquamide selectively antagonized the effects of bephenium; the pK(B) values of levamisole and pyrantel were significantly different from the pK(B) of bephenium. Paraherquamide and 2-deoxy-paraherquamide are selective competitive cholinergic antagonists that distinguish subtypes of cholinergic receptor in Ascaris muscle corresponding to nicotine-, levamisole-, and bephenium-sensitive receptors.

Algorithms↗
PubMed1976

[Worm-diseases].

Intestinal parasites are common among labourers from foreign countries and in immigrants. Some worm-infections like ascaridiasis or enterobiasis occur in children quite often even in the cold climates. In cases of ascaridiasis only a heavy infection causes clinical symptoms. The diagnosis is made through the detection of eggs in the stools, as all the other worm-infections are diagnosed from the stool-test. Piperazine-derivatives are highly effective against ascaris; another useful drug is Pyrantel-Pamoate. Toxocara canis, which affects normally only dogs, can occur occasionally in humans. Its larvae migrate in the body and cause granulomas. The main clinical symptom of threadworms (enterobiasis) is itching around the anus. This parasite can be eradicated through Pyrvinium-Pamoate. The first symptom a patient notices in cases of taeniasis are proglottides--parts of the worms--which are passed with the stools. The drug of choice against all kinds of tapeworms is Niclosamide. Hookworms are rampant in tropical countries. Heavy infections can cause severe anemias, especially in children. Bephenium-Naphthoate and Bitoscanate are effective drugs against this parasite. The whipworm (Trichuris trichura) is very common in the warm countries. It can be treated by Tiabendazole and nowadays also with Mebendazole, which is virtually atoxic. Infections with Strongyloides stercoralis are difficult to eradicate, as there are different ways of reinfection. In case an infection with strongyloides is accompanied by other serious diseases cachexia and even fatal outcome has been seen.

Ascariasis↗