ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03778.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03779.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03780.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03781.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

The authors studied the effect of chronic amantadine ingestion on its own disposition and that of acetaminophen in five healthy young adults. The half‐life of amantadine after 42 days ingestion was 15.1 ± 2.3 hours and was not different from 14.8 ± 4.4 hours after an acute ingestion (mean ± SD). However, chronic amantadine ingestion was associated with an increased apparent volume of distribution for acetaminophen, 1.1 ± 0.1 L/kg compared with 0.9 ±0.1 L/kg, when the two drugs were concurrently ingested after a 2‐week washout period. This difference in kinetic distribution was not reflected in terminal acetaminophen half‐life, 149 ± 54 versus 151 ± 55 minutes for chronic and acute amantadine ingestion, respectively. Plasma acetaminophen clearance with chronic amantadine ingestion (5.8 ± 2.6 mL/min/kg) was not different from that determined after acute coingestion of both drugs (4.3 ± 1.1 mL/min/kg). Thus, no change in recommended dose is necessary when these two drugs

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03782.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

Albendazole pharmacokinetics were studied in eight patients who were receiving albendazole in doses of 15 mg/kg per day for 8 days as treatment of brain cysticercosis. Albendazole was not detected in plasma, but its main metabolite albendazole sulphoxide could be measured. Maximum plasma levels for albendazole sulphoxide ranged from 0.45 to 2.96 pg/mL. The half‐life of albendazole sulphoxide was between 10 and 15 hours. A double peak was found in three patients. Mean residence time values were from 14 to 20 hours. Plasma levels of albendazole sulphoxide at the steady state showed great intraindividual variability. The results suggest that albendazole can be administered twice daily rather than three times as is currently don

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03783.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

To evaluate the effect of food on bioavailability, clarithromycin and 14‐hydroxy clarithromycin (active metabolite) pharmacokinetics were assessed in 26 healthy adult volunteers after ingestion of a single oral 500‐mg dose of clarithromycin in a fasting state (2 hours before breakfast after an overnight fast) and a nonfasting state (0.5 hours after the start of breakfast). Clarithromycin and 14‐hydroxy metabolite plasma concentrations were measured using a high‐performance liquid chromatographic technique. Food intake immediately before dosing increased the extent of absorption from the 500‐mg tablet formulation by approximately 25%. The mean increase in metabolite area under the plasma concentration‐time curve was approximately 9%. These results suggest that clarithromycin can be taken without regard to timing in relati

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03784.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

A new synthesis is proposed for cordiachromene A (CCA), a bioactive component of the ascidianAplidium antillenseGravier, using a method producing a racemic mixture. The anti‐inflammatory activities of a natural extract and a chemically synthetic form of CCA were assessed in vivo by carrageenan‐induced rat‐paw edema. The activity of synthetic CCA was confirmed by a test on kaolin‐induced granuloma in the rat. Strong activities were measured for both CCA, but comparison of results of the first test suggests that only the natural optically active isomer has an anti‐inflammatory effect. CCA is similar to indomethacin in its effect on carrageenan‐induced rat‐paw edema and ten times as active as p

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03785.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

The pharmacokinetics of flurbiprofen (Ansaid Tablets, Upjohn Company of Canada, Don Mills, Ontario) were evaluated in both younger (40 to 60 years) and elderly (65 to 83 years) rheumatoid arthritic patients after both a 100‐mg single‐dose administration and at steady state during a 100‐mg twice‐a‐day dosage regimen. Both flurbiprofen plasma concentration‐time profiles and the urinary excretion of flurbiprofen and its major metabolites were evaluated. The results indicate that the pharmacokinetics of flurbiprofen are linear in both age groups based on only minor changes between single‐dose and steady‐state parameter determinations and the agreement between calculated and predicted accumulation values in plasma concentrations. Only minor differences in the pharmacokinetic parameters were observed between the younger and elderly patients. Only free flurbiprofen clearance was found to have a significant but variable correlation to patient age. The effect of flurbiprofen on the urinary excretion of two prostaglandins were also evaluated throughout this study. In both age groups, the maximum decrease in urinary excretion was observed after the first dose, and this effect was maintained throughout the remainder of the study. Percent decreases from baseline in urinary excretion during drug administration were similar for both age groups. Similar side‐effect profiles were observed b

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03786.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY

摘要:

Topically applied antifibrinolytic drugs may be of value in the control of bleeding in active ulcerative colitis. Any impairment of systemic fibrinolysis in this condition, however, is potentially harmful. Since pharmacokinetic data after the rectal administration of tranexamic acid are non‐existent, plasma concentration and recovery in the urine were recorded after a single dose of 2 g tranexamic acid given rectally to five patients with ulcerative colitis and to five healthy volunteers. The median area under the curve was, for the volunteers, 7.64 mg/L × hr (range: 4.43–11.56) and, for the patients, 13.84 mg/L × hr (range: 9.32–50.22) (P<.05). The median 24‐hour recovery in the urine was 0.8% (0.3–1.1) and 2.7% (1.1–4.0), respectively (P<.05). The median peak plasma concentration was, for the volunteers, 0.40 mg/L (range: 0.20–0.69) 6 hours after administration and, for the patients, 1.10 mg/L (range: 0.53–2.90) 5 hours after administration (P<.05). The plasma concentrations and recovery in the urine that were observed in the patients and volunteers were low compaired with those seen after oral intake of the same dose. The plasma concentrations did not reach levels that were considered liable to impair syst

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1992.tb03787.x

出版商:Blackwell Publishing Ltd    

年代:1992

数据来源: WILEY