Metabolism of hetrazan in the rat.
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A clinical trial was carried out with furapyrimidone in treating 51 patients with B. malayi, 159 with W. bancrofti and eight with D. perstans using different dosage schedules. Two hundred and fifty-seven cases of Malayan and bancroftian filariasis were treated with hetrazan for comparison. The results based on the microfilaricidal effects suggest that furapyrimidone possesses similar therapeutic effects of hetrazan on Malayan filariasis at eight-month follow-up, and higher incidences of microfilarial disappearance of W. bancrofti infection (81.3%) at six-month follow-up. The drug was also effective against D. perstans. The side effects consisted of fever and irritation of the digestive tract. Fever may be related to allergic reaction of foreign protein from the dead or dying parasites. The side reactions are similar to those of hetrazan and usually not serious. Comparing the efficacies and side effects of furapyrimidone with different dosage schedules the authors recommend regimens of 15 to 20 mg/kg/day for six days in treating Malayan filariasis and 20 mg/kg/day for seven days in treating bancroftian filariasis.
BACKGROUND: Loa Loa is a chronic parasitemic disease which is endemic in the tropical rain forests of Western Africa. Vector of this disease is a mangrove fly with the name Chrysops. Besides the eye worm and skin affections a systemic infection with microfilariae is common. PATIENT: A West African tourist from Bangibe showed up at the university eye clinic. His complaints were a red eye and a mobile subconjunctival tumor (Fig. 1) that showed vermiform movements. The worm was transparent and 4-5 cm in length. After topical anaesthesia and the attempt to paralyze the worm (1) with Pilocarpine 2% it vanished. Two days later the patient showed up in the morning for the planned blood test. No worm was visible at that time but at noontime the blood test was carried out and at that time the worm was visible in the nasal conjunctiva. This time the worm was removed without delay under topical anaesthesia. The worm was fixed with a forceps through the conjunctiva which was opened for 0.5 cm. The worm was grasped with a second forceps and drawn out under massive vermiform movement. Systemic therapy was recommended with Hetrazan (Diethylcarbamazine) using Corticosteroides and Antihistamine to minimize allergic side effects by the therapy due to the systemic microfilariae blood load. Eosinophilia was 8%. CONCLUSIONS: A subconjuctival Loa Loa worm can be removed under topical anaesthesia by fixing it with a forceps through the conjunctiva and opening it and grasping the worm with a second forceps. According to our experience the paralyzation with Pilocarpine cannot be realized. Careful systemic therapy avoiding reported allergic side effects with Hetrazan which is not available in Germany is necessary.
Cases of onchocerciasis were treated with three drugs, Antrypol, Pentostam and Hetrazan. Antrypol proved undoubtedly effective, producing disappearance of the microfilariae and onchocercal nodules, and improvement in cases of defective vision with anterior ocular manifestations, but little or no improvement in cases with well-defined posterior manifestations. The severe toxic effects of the drug, however, are sometimes fatal, and therefore preclude its use. Pentostam, although non-toxic, did not prove effective in the doses tried; it may be of some use in very large doses. Hetrazan was given to three cases only, in all of which it produced very rapid disappearance of the microfilariae, but this was accompanied by some allergic reactions and there was no other indication of improvement. Moreover, one month after treatment, microfilariae reappeared in one case. It seems that the more actively filaricidal a drug is, the more toxic it will be, and this is likely to be a serious limitation in the chemotherapy of onchocerciasis until some method of avoiding the allergic reactions can be devised.
Epidemiological survey of filariasis in Fujian Province, China showed that malayan filariasis, transmitted by Anopheles lesteri anthropophagus was mainly distributed in the northwest part and bancroftian filariasis with Culex quinquefasciatus as vector, in middle and south coastal regions. Both species of filariae showed typical nocturnal periodicity. Involvement of the extremities was not uncommon in malayan filariasis. In contrast, hydrocele was often present in bancroftian filariasis, in which limb impairment did not appear so frequently as in the former. Hetrazan treatment was administered to the microfilaremia cases identified during blood examination surveys, which were integrated with indoor residual spraying of insecticides in endemic areas of malayan filariasis when the vector mosquito was discovered and with mass treatment with hetrazan medicated salt in endemic areas of bancroftian filariasis. At the same time the habitation condition was improved. These factors facilitated the decrease in incidence. As a result malayan and bancroftian filariasis were proclaimed to have reached the criterion of basic elimination in 1985 and 1987 respectively. Surveillance was pursued thereafter and no signs of resurgence appeared.