Nicotredole (Tryptamide) is an orally active anti-inflammatory and analgesic agent. Nicotredole exhibits evident antiinflammatory effects of potency comparable with Phenylbutazone. Nicotredole has only weak ulcerogenic activity[1][2][3].
Nicotredole inhibits prostaglandin synthetase activity in vitro[1].
Nicotredole produces antiinflammatory effects in carrageenin-induced rat paw oedema[1].Nicotredole reverses pyrogen-induced hyperthermia in rats, elicits analgesic effects in rats, prolongs the time of hexobarbital sleep in rats and inhibits locomotor activity in rats and mice[1].Nicotredole (i.p.) has LD50s of 1260 mg/kg and 1980 mg/kg for male rats and male mice, respectively[1].Nicotredole (p.o.) has LD50s of 8.5 g/kg and 9.3 g/kg for male rats and male mice, respectively[1].Nicotredole (25 mg/kg; p.o. or i.p.) undergoes fast absorption (t1/2=4.92-17.5 min) and elimination (t1/2=55.72-74.52 min), can reach Cmax (11-13 μg/cm3) after 30 min, and gives AUC values in the range of 21.40-27.30 (μg•h/cm3)[2].
[1]. Herman ZS, et, al. Basic pharmacological properties of a novel antiinflammatory drug tryptamide. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):729-36. [2]. Szumi?o H. Pharmacokinetics of tryptamide following oral and intraperitoneal administration in rats. Acta Pol Pharm. 1990;47(1-2):19-22. [3]. Kulig D, et, al. A comparison of anti-inflammatory, analgesic and ulcerogenic action of tryptamide, ibuprofen and piroxicam. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):769-72.