After rats being given ig FCE 22250 5, 10 and 25 mg.kg-1, the plasma peak times (Tmax) were 12-14 h, the max plasma concentrations (Cmax) were 3.0, 5.6 and 12 micrograms.ml-1 respectively, and the half-lives of elimination (T1/2) were 24-26 h. The apparent volumes of distribution of the three doses were about 1 L.kg-1, suggesting that FCE 22250 in blood and in tissue was balanced. Total body clearance rate of each of the three doses was 29 ml.kg-1.h-1. The ig absolute bioavailability ranged from 69-84%. Its distribution in rats was as follows: the highest in liver, next in lung and then in fat, kidney, intestine, spleen, lymphaticode, heart, muscle, testis, the lowest in brain. It was eliminated mainly via the bile with feces. The human serum protein binding rate of FCE 22250 was 96.2%. It was shown that the rate was not correlated with drug concentration in serum under our experimental conditions.
Download full-text PDF |
Source |
---|
Nihon Rinsho
December 1998
Department of Internal Medicine, National Minami-Okayama Hospital.
The development of new drugs with strong antituberculous activity and fewer side effects which are not cross-resistant to conventional antituberculosis drugs is urgently desired now. The chemotherapeutic agents under study which are considered a candidate for a new antituberculosis drug are listed below. 1) Rifamycin derivatives: rifabutin, rifapentin, KRM-1648, FCE-22250, 22807, CGP-7040, 27557, 29035, 29861, P-DEA, SPA-S-565, R-76-1.
View Article and Find Full Text PDFKekkaku
November 1994
Department of Infection and Inflammation, Kyoto University, Japan.
The number of cases with tuberculosis is again increasing in many countries, and recently several nosocomial outbreaks of multidrug-resistant tuberculosis have occurred in the United States. The number of patients with disseminated Mycobacterium avium complex (MAC) infections in AIDS population, and patients with MAC pulmonary disease unassociated with HIV seem to be also increasing. It takes at least 6 to 9 months for an initial treatment of active tuberculosis due to drug-sensitive strains with the standard regimen which includes isoniazid (INH) and rifampicin (RFP).
View Article and Find Full Text PDFZhongguo Yao Li Xue Bao
January 1991
Department of Pharmacology, School of Pharmacy, Shanghai Medical University, China.
After rats being given ig FCE 22250 5, 10 and 25 mg.kg-1, the plasma peak times (Tmax) were 12-14 h, the max plasma concentrations (Cmax) were 3.0, 5.
View Article and Find Full Text PDFJ Antimicrob Chemother
October 1988
Division of Sexually Transmitted Diseases, MRC Clinical Research Centre, Harrow, Middlesex.
Thirty-eight strains of Haemophilus ducreyi isolated in southern Africa were tested in vitro against 15 antimicrobial agents including those frequently used for the treatment of chancroid. In addition, newer compounds which possess characteristics consistent with their possible use as single-dose therapy for the disease were tested. All isolates were found to be resistant to penicillin as a result of beta-lactamase production.
View Article and Find Full Text PDFGenitourin Med
August 1988
Division of Sexually Transmitted Diseases, MRC Clinical Research Centre, Harrow, Middlesex.
The susceptibility of 119 strains of Neisseria gonorrhoeae isolated in Munich in 1986 to eight antibiotics was assessed. Although some degree of resistance to penicillin and tetracycline, as well as high minimum inhibitory concentrations (MIC) of spectinomycin, were observed, all the strains were sensitive to ciprofloxacin, enoxacin, fleroxacin, cefotaxime, and FCE 22250.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!