Metabolism of 14 C-iodochlorohydroxyquinoline (chinoform) in mice.

In order to know the organ distribution of Chinoform, I4C.Chinoform was injected into the tail vein of the mice, and radioactivity was measured in the chloroform soluble fractions in some organs and tissues containing non.conjugated Chinoform. The results obtained are as follows. 1. Uptake of Chinoform by the visceral organs was found to be in the following ascending order: fat tissue, kidney, spleen, liver, small intestine, (blood), muscle and eye, and marked uptake by the fat tissue and kidney was observed. 2. The presence of radioactive Chinoform in the chloroform soluble fraction of the central nervous system was recognized and it was almost in the same degree of specific radioactivity as that of blood. 3. A higher uptake in the chloroform soluble fraction of the sciatic nerve than that of central nervous system was recognized, and the value of the former was about 3 to 8 times as high as that of the latter. 4. The presence of Chinoform in the chroloform soluble fraction of the bile, although it increased after incu bation of the bile with j9-glucuro. nidase was observed. High radiogctivity of chinoform in the total fraction of the bile suggests a possible presence of “liver-intestine-circulation” of the drug. ∗PMID: 4263521 [PubMed indexed for MEDLINE] Copyright c ©OKAYAMA UNIVERSITY MEDICAL SCHOOL Acta Med. Okayama 25, 199-204 (971) METABOLISM OF 14C.IODOCHLOROHYDROXYQUINOLINE (CHINOFORM) IN MICE Masana OGATA*, Shosuke WATANABE**, Jun TATEISHI**, Shigetoshi KURODA **, Katsumaro TOMOKUNI*, and Saburo OTSUKI** Department of Public Health*, and N euro-Psychiatry**, Okayama University Medical School, Okayama, jaban Received for publication, May 2, 1971 5-Chloro.7.iodo-8-hydroxyquinoline (Chinoform) is a well.known intestinal antiseptic in the world.wide use. BERGGREN, L. et ai. (l) drew attention by reporting that optic atrophy has followed long. term medica. tion with Chinoform. It is often stated that Chinoform is not absorbed in the gastrointestinal tract. But urinary excretion of the glucuronic and sulfuric acid conjugates of Chinoform given orally to rabbit (2) and man (3~5) has been reported. In Japan, so.called subacute myelo.optico.neuropathy with abdominal symptoms (SMON) was first reported by T AKASAKI (6) in 1961 in Mie Prefecture, central part of Japan. Since then, the number of patients of SMON has been found increasing in many places throughout Japan, and the number of patients reported during 1967 to 1968 reached 4, 280 (7). The clinical symptoms of SMON show signs of lateral corticospinal tracts and of posterior column disturbances (8) ensuing from abdominal symptoms, and 89.5 per cent of patients show sensory disturbances and 60.8 per cent motor disturbances and 23.5 per cent are accompanied by visual disturbances (7). Recently, it is suspected that long term administration of Chinoform may be one of the causal factors of this syndrome (9). In the present study the distribution in the visceral and nervous tissues and bile-excretion of Chinoform in mice were investigated. The results are briefly described here. MATERIALS AND METHODS Materials: ddN-Strain female mice weighing about 20 grams were used. Animals were kept in a stock on ad libitum diet. The day before the experiment, animals were administered ad libitum 1 per cent iodine solution, orally as thyroid blocking agent.