Aminogiycoside系抗生物質 : KW-1062に関する薬理学的研究 (第1報 一般薬理作用)

抄録

The pharmacological actions of KW-1062, a new aminoglycoside antibiotic, were investigated. Summary of pharmacological actions and minimal effective doses (MED) of KW-1062 was as follows : fall of blood pressure of the rabbit (10 mg/kg), inhibition of respiration of the rabbit (50 mg/kg), bradycardia of rabbit ECG (100 mg/kg), inhibiton of isolated guinea pig atrium (5×10^-5 g/ml), stimulation of permeability of rabbit skin vessels (10 dug) and inhibition of isolated rabbit and guinea pig intestine (10^-4 g/ml), of isolated guinea pig trachea (10^-4 g/ml), and of isloated nonpregnant and pregnant rat uteri (2×10^-5 and 2×10^-6 g/ml). No effect on rabbit ear vessels was observed in a concentration up to 2×10^-1 g/ml. The actions and MED were similar to those of gentamicin. In nerve-muscle preparation of rat diaphragm, contraction by indirect stimulation was inhibited at a concetration of 5×10^-4 g/ml. ED₅₀ in which moderate paralysis was elicited in mice was calculated as approximately 200 mg/kg (sc). No potentiating effects of KW-1062 on ether anesthesia and Pentobarbital sleep were observed. KW-1062 did ont protect the Pentetrazol convulsions. The increase in body weight, volume of urine, urinary excretion of sodium and potassium, and urinary findings in the rat applied KW-1062 in doses from 12. 5 to 100 mg/kg subcutaneously once a day for 7 days were similar to normal values and those of the control group, except that application of 100 mg/kg showed tendency of inhibition of body weight increase and decreased excretion of sodium.