The new drug niclofolan (bayer 9015, Bilevon), 5,5'-dichloro-2,2'-dihydroxy-3, 3'-dinitrobiphenyl, has been used in the treatment of Paragonimus westermani in dogs and cats and P. iloktsuenensis in rats. It was proved that administration of daily dose of 1.0 mg/kg body weight for 3 days or in 2 doses of 2.0 mg/kg body weight by alternate days were evidently effective for the infected dogs, cats and rats with the lung flukes, and toxic manifestations were not found.
parasitology-helminth-trematoda ; Paragonimus iloktsuenensis ; paragonimiasis ; Paragonimus westermani ; dog ; cat ; rat ; niclofolan-chemotherapy ; niclofolan

The infection of Metagonimus yokogawai has been known to be present nationwidely and endemic in some parts in Korea. In order to select a highly effective compound against Metagonimus infections, the therapeutic effects were observed in 156 cases who were treated with several anthelmintic i.e. bithionol, niclosamide, niclofolan and praziquantel. All of the above drugs showed highly effective to the treatment of metagonimiasis by a single or two medication days. The egg reduction rates were in the range of 80.2 to 100 per cent. However, relatively low cure rates(8.3 to 37.5 percent) were observed in the groups treated by two doses of 30 mg/kg of bithionol, a single day treatment with 100 mg/kg of niclosamide and two doses of 1.0 mg/kg of niclofolan. On the other hand, the high cure rates were observed at the following dose rates of each drugs, i.e. the cure rate of 66.7 percent was obtained at two doses of 100 mg/kg of niclosamide, 88.9 percent of cure rate was observed at two doses of 2.0 mg/kg of niclofolan and a single dose of 10 and 20 mg/kg of praziquantel were shown as 85.0 percent and 88.0 percent of cure rates respectively. But the complete radical cure was obtained in the group treated by two doses of 20 mg/kg of praziquantel in 10 metagonimiasis cases. From the above results praziquantel was shown as the most highly effective against metagonimiasis and it was well tolerated without any side effect. Therefore, praziquantel is a very promising drug for mass treatment against metagonimiasis.
parasitology-helminth-trematoda ; Metagonimus yokogawai-metagonimiasis ; bithionol ; niclosamide ; niclofolan ; praziquantel ; chemotherapy

The authors reported a case of niclofolan intoxication occurred during the trial of clonorchiasis treatment. The case, a 15 years old Korean schoolboy, took niclofolan(Bilevon) of total 473 mg(11 mg/kg) in 11 divided doses during 20 days. And the case suffered from neurologic symptoms such as severe headache, dizziness, nausea, vomiting, blurred vision, papilledema, retinal hemorrhage, an epsiode of seizure attack and elevated intracranial pressure, and hepatotoxic symptoms such as hepatomegaly, increased serum transaminases, and shoulder pain, excessive sweating and weight loss. Therapy was concentrated to the management of the elevated intracranial pressure. Hepatotoxic manifestations subsided within one month. The clinical signs related to elevated intracranial pressure persisted two months. Body weight regained after 2 months. And the symptoms of headache, dizziness and vomiting were complained intermittently until 4 months after onset. However, no subsequent clinical problems related with this episode has been noted until this record.
parasitology-helminth-trematoda ; Clonorchis sinensis ; clonorchiasis ; intoxication ; niclofolan ; jaundice ; weakness ; hepatomegaly ; headache ; intracranial pressure ; nausea ; vomiting ; blurred vision ; ocular pain ; papilledema ; retinal hemorrhage ; case report

ERCP was performed in 38 cases of clonorchiasis of the liver, which was confirmed by stool egg test withStoll's dilution method from Apr. 1979 to Oct. 1982. The resuls were as follows 1. The sex distribution ofclonorchiasis showed marked male predominance by 97.4% and age distrigution were higher in 5th and 6th decades. 2.Multiple small filling defects in the intrahepatic bile duct was the most characteristic finding in ERCP and widespread irregular stenosis, dilatation of terminal portion, disturbance of peripheral filling, fuziness andraggedness of intrahepatic duct were also noted. 3. The severity of clonorchiasis by ERCP were classifed asfollows; Grade I-7 cases (18.4%), GradeII-9 cases(23.7%) Grade III-12 cases (31.6%) and Grade IV-10 cases(26.3%)4. Chronic cholecystitis 10 cases(26.3%), Billary tree stone 7 cases (18.4%), malignancy of distal CBD 1 case(2.6%) were found with clonorchiasis by ERCP. 5. Three cases, treated with Niclofolan, showed marked improvementof pathology on follow-up ERCP.
Bile Ducts, Intrahepatic ; Cholangiopancreatography, Endoscopic Retrograde ; Cholecystitis ; Clonorchiasis ; Constriction, Pathologic ; Dilatation ; Follow-Up Studies ; Humans ; Liver ; Male ; Methods ; Niclofolan ; Ovum ; Pathology ; Sex Distribution ; Trees

In order to find a highly efficient compound against Clonorchis infection, the anthelmintic activity of disophenol, Tremerad (SYD-230), dithiazanine iodide, dehydroemetine-late-release tablets(RO 1-9334/20), niridazole (Ambilhar), hexachlorophene (G-11), Hetol(1, 4-bis-trichloromethylbenzol) and Bilevon (niclofolan) was tested against Clonorchis sinensis experimentally infected rabbits. All drugs showed a progressive increase in efficacy as the dose rate. They were highly efficient against Clonorchis infection if sufficiently high, potentially toxic doses were given. The efficacy was evaluated by the number of detected worms with vital condition at autopsy after the treatment with above drugs. The high efficacy was observed at the following dose rates of each drugs, i.e. disophenol at a single dose of 30 mg/kg, Tremerad at the daily dose of 200 mg/kg for 10 consecutive days, dithiazanine iodide at the daily dose of 50 mg/kg for 6 consecutive days, dehydroemetine at the daily dose of 10 mg/kg for 10 consecutive days, hexachlorophene at the daily dose of 20 mg/kg for 10 to 15 consecutive days, Hetol at the daily doses from 50 to 100 mg/kg for 5 to 10 consecutive days, and Bilevon at a single dose of 8 mg/kg. Moderate effectiveness was shown in niridazole at the dose of 25 mg/kg for 10 days medication. The use of these anthelmintics for the clinical treatment of Clonorchis sinensis infection is discussed.
parasitology-helminth-trematoda ; chemotherapy-Clonorchis sinensis ; clonorchiasis-rabbit ; disophenol ; Tremerad (SYD-230) ; dithiazanine iodide ; dehydroemetine-late-release tablets(RO 1-9334/20) ; niridazole (Ambilhar) ; hexachlorophene (G-11) ; Hetol(1, 4-bis-trichloromethylbenxol) ; Bilevon (niclofolan)

The present study was undertaken to evaluate in vitro activities of following drugs against adult worms of Clororchis sinensis: i.e., stibnal, chloroquine diphosphate, Hetol (1,4-bis-trichloromethylbenzol), dehydroemetine 'Roche' (Ro 1-9334), niridazole (Ambilhar), bisbendazole, gentian violet, dithiazanine iodide, hexachlorophene, bithionol, niclofolan (Bilevon, Bayer 9015) and praziquantel (Embay 8440, Biltricide). After isolation from bile ducts of experimentally infected rabbits (3 months infection), the parasites were rinsed in sterilized Tyrode's solution and incubated for 24 hours at 37 C in TC 199 medium with Earle's balanced salt solution containing 0, 0.01, 0.1, 1.0, 10 and 100 microgram/ml concentrations of each above drugs. The activities of each concentrations with each drugs were evaluated by the motility of the worms in culture tubes observing at 15, 30, 60 minutes and 2, 4, 6, 12, 18 and 24 hours by stereomicroscope. In the results, no effect was found at the adult worms of C. sinensis in all concentrations with stibnal, chloroquine diphosphate, Hetol, dehydroemetine, niridazole and bisbendazole. However, moderate activities were observed in the concentrations of 1.0 and 0.1 microgram/ml of gentian violet, dithiazanine iodide, hexachlorophene and bithionol. The highest activities were observed in all concentrations of niclofolan and praziquantel.
parasitology-helminth-trematoda ; Clonorchis sinensis ; chemotherapy ; in vitro ; stibnal ; chloroquine diphosphate ; Hetol(1,4-bis-trichloromethylbenzol) ; dehydroemetine ; 'Roche'(Ro 1-9334) ; niridazole(Ambilhar) ; bisbendazole ; gentian violet ; dithiazanine iodide ; hexachlorophene ; bithionol ; niclofolan ; praziquantel