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Biomedical subjects

N A Mankodi

Publications and source records attributed to N A Mankodi.

10 recordsLinked to original sources

Phase 1 tolerability and antiamoebic activity studies with 1-methylsulphonyl-3-(1-methyl-5-nitro-2-imidazolyl)-2-imidazolidinone (Go.10213): a new antiprotozoal agent.

Go.10213, a new nitroimidazole, was studied in 12 male volunteers for tolerability and in 20 patients with intestinal amoebiasis for antiamoebic activity. Go.10213 was well-tolerated by volunteers up to a dose of 400 mg X 3. Patients also tolerated well the dose of 100-150 mg X 3 for 7 days. In two patients, there were mild and transient side-effects like headache, dizziness, fatigue, etc. No neurological side-effects were observed. There were no significant changes in blood pressure, pulse rate and ECG. The organ function tests did not show any adverse effects of Go.10213 on bone-marrow, kidney, liver, etc. Go.10213, at a dose of 150 mg X 3, showed potent antiamoebic activity in 10 patients with intestinal amoebiasis, as judged by the clinical relief, the eradication of the trophozoites and cysts of Entamoeba histolytica from stools and the healing of colonic ulcers. Go.10213, a novel nitroimidazole, may prove to be the most potent and safe agent against the protozoal infections, e.g. amoebiasis, giardiasis and trichomoniasis.

Adolescent↗

Phase 1 tolerability and searching dose studies with 4-isothiocyanato-4'-nitrodiphenylamine (C.9333-Go/CGP 4540), a new anthelmintic.

1 Phase 1 and 2 studies were carried out in thirteen volunteers and thirty patients with hookworm anaemia with a new anthelmintic, 4-isothiocyanato-4'-nitrodiphenylamine (C.9333-Go/CGP 4540). Single and multiple doses were administered by mouth under careful supervision by the staff of the clinical pharmacology unit. 2 4-Isothiocyanato-4'-nitrodiphenylamine (C.9333-Go/CGP 4540) was well tolerated in volunteers up to a single dose of 1750 mg and in patients up to 3000 mg in divided doses. Side effects were rare, transient and mild. One patient had moderate giddiness for 24 h after the compound. The laboratory investigations did not show any adverse effects on organ functions. Transient non-specific changes in the T-wave were occasionally observed in the e.c.g. 3 Multiple doses (125 mg, 250 mg or 1000 mg X 3) of the compound were highly effective in eradicating hookworm infection, as judged by almost 100% reduction in faecal egg counts and significant recovery of parasites from 24 h stool samples. The compound also showed activity against A. lumbricoides, T. trichiura and E. vermicularis. The compound appears to be promising and more studies, in a field situation, are desirable.

Adolescent↗

Clinical trials of a new anthelmintic, 4-isothiocyanato-4'-nitrodiphenylamine (C.9333-Go/CGP 4540), for the cure of hookworm infection.

A new compound, 4-isothiocyanato-4'-nitrodiphenylamine (C.9333-Go/CGP 4540), was tried in 39 hospitalized patients with hookworm infection, using several treatment schedules. At effective dose schedules (125 mg X 3 given 4-hourly; 250 mg X 3, 8-hourly; 1,000 mg X 3, 12-hourly), the egg reduction was 96% to 100%; the zero egg-counts were confirmed by coproculture for larvae. The compound was very well tolerated. Transient and mild side effects--giddiness, diarrhea and sweating--were observed in only three patients. No toxic effects were seen as judged by serial organ function tests, except a transient and mild asymptomatic elevation of transaminases in one patient.

Adult↗