In 1950, P
54 was for the first time administered orally to 9 cases of lepra tuberosa and as the result of which an obvious degeneration of the lepra bacilli of the modules was observed. However, in approximately 4 months some started complaining of anorexia with occasional hearttap and the treatment was discontinued. In an effort to remedy these by-effects, 30 mg of P
54 was suspended in 1cc refined Chaulmoogra Oil, and 1cc of this was injected to 4 rabbits, each weighing approximately 3, 000 g, six times weekly for 4 weeks consecutively with the intention of observing changes in their weight, appetite and induration of the injected parts. The following was observed: appetite unchanged; one rabbit showed a weight decrease; no case of incuration indicating that absorption was good. Therefore, in April 1951 it was decided to adopt this injection for the treatment of lepra patients.
The formula of P
54 is as follows : C
2H
5SO
2_??_CH: N-NH-C_??_NH
2 S It is in the form of brilliant white crystal with melting point at 132°C. It does not melt easily in water, however, it is soluble in aceton, propylglycocol, chloroform, ether and alcohol. P
54L is liquidized at 25°C and when injected intramuscularly, it is painless and does not form induration even when administered eonsecutevely.
Dosage is : start with 0.5cc 3 times weekly, increasing gradually up to 3cc. Simultaneous administration of 2.5cc-5cc of Promin by intravenous injection every other day will be excellent, and the usual by-effect of Promin, i, e. anaemia and general weekness, do not occur.
Starting in April 1951, 59 patients (4 cases of lepra maculosa, 15 lepra nervosa and 40 lepra tuberosa) were treated with P
54L alone or together with Promin for 2 to 34 months. As for the lepra maculosa cases, generally speaking, in about one year resorption of macula was observed and in 2 years sense of the affected area was restored and an investigation of the histopathological tissues of skin proved it cured. However, the thickening of ulnar nerve was not completely resorbed.
In the cases of lepra nervosa, no remarkable results were obtained, except for the restoration of sense, increase of perspiration area, cure of malum perforans pedis, and restoration of motorial paralysis where hyarulonidase was given simultaneously.
In the cases of lepra tuberosa, in appsoximately six months, absorption of nodule became obvious, together with degeneration of leprosy bacteria and in about 2 years leprosy bacteria were negative. The Mitsuda-Skin-Test turns positive approximately 6 months before leprosy bacteria prove negative. Hair and eye-brows start growing; no infiltration in the histopathological tissues of skin is observed; vegetation of connective tissue was noticed and in some cases lepro bacteria were completely negative. In such cases no erythema nodosum leprosa was observed. Cure of ulcer was also seen and there were hardly any violent complaints of leprous ueuralgia. It results in considerably less erythema nodosum leprosa than where other antileprotics are used. It is believed that simultaneous administration of Metionin will prevent such growth to a considerable extent. As a toxic manifestation, 2 cases developed jaundice but whether or not such was caused by P
54L is not known. However, there was no case of albuminuria, anaemia or leucopenia.
Bacteriostatic action upon tubercle bacilli (Typus humanus H37RV) of P
54L is 30 times as strong as that of P
54 alone. Blood concentration is highest on the 2 nd day and it is proved that it remains in a human body for 5 days, and consequently it can be said that even a small dose is effective.
P
54L is one of the drugs to be used for the treatment of leprosy.
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