Pharmacokinetics of Tamsulosin Hydrochloride in Patients with Renal Impairment: Effects of α1‐Acid Glycoprotein
Kenkichi KoisoHideyuki AkazaKoji KikuchiKazumasa AoyagiShoji OhbaMitsuhiro MiyazakiMitsue ItoToshiyuki SueyoshiHiroshi MatsushimaHidetaka KamimuraTakashi WatanabeSaburo Higuchi
21
Citation
29
Reference
10
Related Paper
Citation Trend
Abstract:
The pharmacokinetics of tamsulosin hydrochloride in patients with renal impairment were compared with those in healthy volunteers, and the factors that influenced plasma levels of tamsulosin were elucidated. A single oral dose of 0.2 mg of tamsulosin was given and blood and urine samples were obtained for 36 hours after administration. Unbound plasma concentration of tamsulosin was measured by a combination of equilibrium dialysis and liquid chromatography tandem mass spectrometry methods to examine the effect of protein binding on the pharmacokinetics of tamsulosin. Mean values for maximum concentration (C max ) and area under the concentration—time curve (AUC) of total drug (C max,t and AUC 1 in patients with renal impairment were 73% and 211% greater, respectively, than those in healthy volunteers. Mean C max and AUC of unbound drug (C max,u and AUC u ), however, were almost the same in the two groups. A high correlation was found between α 1 ‐acid glycoprotein (α 1 ‐AGP) concentration and AUC t , but no correlation was found between α 1 ‐AGP concentration and AUC u,0–36 or between creatinine clearance (Cl CR ) and AUC u,0–36 . These results show that in patients with renal impairment, the pharmacokinetics of tamsulosin are affected by the change in protein binding that is associated with alteration of plasma α 1 ‐AGP concentration, but are not largely affected by the decrease in the renal excretion. Although total tamsulosin levels increased as plasma protein binding increased, unbound tamsulosin levels (which are directly associated with the pharmacologic effects) remained unchanged in these patients.Keywords:
Tamsulosin
Several pharmacokinetics relative datas such as absorption, distribution, elimination and bioavailability have been set up in this study on pharmacokinetics of Norfloxacin in carp following different forms administration. Following single muscular injection and oral administration, the serum concentration the data of Norfloxacin in carp were best described by a two-compartment open model for dose of 10 mg Norfloxacin /kg body weight. Following single mixed in diet oral administration, the serum concentration-time data for Norfloxacin were best described as a one-compartment open model. The main pharmacokinetics parameters by muscular injection administration: AUC 24.9481 μg·h·mL-1, Cmaxl6.8992 μg·mL- 1, t1/2α 0. 1279 h, t1/2β 3.4032 h. The main pharmacokinetics prameters by orally administration: AUC 150.6029 μg·h·mL-l, Cmax5.7998 μg·mL-l, t1/2α3.407lh, t1/2β77. 1239h. The chief pharmacokinetics parameters by mixed in diet oral administered: AUC 6.8183 μg·h·mL- l, Cmax1 .7217μg·mL- l, t1/2ka 0.22643h,t1/2ke 2.0213h. The results showed that the main parameters following different forms administration were significantly different (P 0.01).
Cite
Citations (1)
The pharmacokinetics of nalbuphine were studied in 10 healthy volunteers on two separate occasions following administration by either the intravenous (20 mg) or oral (60 mg) route. After administration, serum concentrations of nalbuphine were measured for 12 h using a high pressure liquid chromatography assay, and pharmacokinetic parameters were derived using a three compartment model. After i.v. administration, elimination half‐life was 222 (111‐460) min (mean and range) and total body clearance was 1.5 (0.8‐2.3) 1 min‐1. Cmax after oral administration was 21.4 (6.0‐36.2) ng ml‐1 and tmax was 46.6 (15.3‐ 89.0) min. Bioavailability of the oral preparation was 11.8 (6.1‐20.1)%.
Nalbuphine
Half-life
Cite
Citations (41)
Etretinate
Isotretinoin
Active metabolite
Cite
Citations (117)
Abstract The pharmacokinetics of α‐dihydroergocriptine methane sulphonate in rats were investigated using an HPLC method for the detection of unchanged α‐dihydroergocriptine (DHEK) in plasma, organs (kidneys, heart, lungs, spleen, liver, and brain), and urine. The plasma profile of DHEK obtained after intravenous administration at a dose of 5 mg kg −1 (as base) of DHEK methane sulphonate showed a three compartment pharmacokinetic model with an elimination half‐life of 6.78 h. The kinetics of DHEK after a single oral administration at a dose of 20 mg kg −1 (as base) showed two peaks: the second peak, at about 6 h, was probably due to an enterohepatic cycle. The disposition of DHEK consisted of an absorption half‐life of 0.02 h, a distribution half‐life of 2.15 h and an elimination half‐life of 5.83 h. The pharmacokinetics of DHEK, after repeated oral administrations at the same dose, were similar to those after a single oral administration. The absolute bioavailability was 4.14% after a single oral administration and 3.95% after repeated oral administrations. The analysis of the organs showed that DHEK was rapidly absorbed and distributed in all tissues, mostly in lungs, kidneys, and liver, but it is interesting to observe that it also reached the brain. After repeated oral administrations plasma and tissue concentrations were similar to those obtained after a single administration; therefore it is possible to exclude the onset of autoinduction or accumulation phenomena of DHEK in rats' organs. Urinary excretion of the unchanged drug was low (0.38% of the administered dose in the intravenous route and 0.04% in the oral route), being in agreement with a low oral bioavailability and a rapid and extensive metabolism (first‐pass effect).
Enterohepatic circulation
Half-life
Cite
Citations (2)
Oral dose
Cite
Citations (0)
Objective To determine the pharmacokinetic parameters of 2 epimers of glycyrrhizic acid (GL) after oral administration of α-GL and β-GL in rats.Methods α-GL and β-GL solvent were administered orally at a dose of 25 mg·kg-1.The concentration in the plasma was measured by HPLC method.Experimental data and the pharmacokinetic parameters were processed with the computer program DAS 2.0 and SPSS.Results The main pharmacokinetic parameters were:AUC0-36=(57.04±14.64)μg·mL-1·h;Cmax= (4.68±2.56)μg·mL-1 t1/2=(5.56±1.65)h,tmax=(10.0±4.0)h after oral administration of α-GL;AUC0-36=(36.55±13.18)μg·mL-1·h;Cmax=(4.24±1.69)μg·mL-1,t1/2=(7.88±2.40)h,tmax=(9.0±1.1)h respectively after oral administration of β-GL.Conclusion The main pharmacokinetic parameters of GA after the oral administration of α-GL and β-GL are different.
Epimer
Oral dose
Cite
Citations (0)
Abstract Pharmacokinetic studies are reported after single oral administration of 3 mg/kg of stereochemically pure (S)‐ketoprofen [(S)‐KP] and (R)‐ketoprofen [(R)‐KP] to three male Cynomolgus monkeys and after repeated administration for 6 months of 3, 15 and 75 mg/kg/day of (S)‐KP to both male and female monkeys. A high‐performance liquid chromatographic (HPLC) analysis was performed without derivatization of the samples, using a chiral column. The pharmacokinetic parameters for (S)‐KP after administration of (S)‐KP and for (R)‐KP after administration of (R)‐KP were, respectively, elimination half‐life 2.32 ± 0.36 and 1.64 ± 0.40 h; oral clearance 3.50 ± 0.66 and 7.50 ± 3.20 ml/min/kg; apparent volume of distribution 0.74 ± 0.24 and 1.16 ± 0.76 liter/kg; mean residence time 1.79 ± 0.77 and 1.41 ± 0.65 h; area under the concentration/time curve 14.16 ± 2.93 and 7.31 ± 2.98 μg·h/ml. Forty‐nine percent unidirectional bioinversion of (R)‐KP to (S)‐KP was observed in this species and the pharmacokinetic parameters for the (S)‐KP resulting from this inversion were also calculated. In the study of 6‐month repeated administration of (S)‐KP, linear pharmacokinetic behavior and no evidence of drug accumulation were observed at the three dose levels. © 1994 Wiley‐Liss, Inc.
Ketoprofen
Half-life
Cite
Citations (21)
Route of administration
Cite
Citations (12)
To study the pharmacokinetics of rhein in 12 healthy volunteers after oral administration of rhubarb extract.The blood sample were obtained at 0,0.083,0.5,1,1.5,2,3,4,5,7,10 h after a single dose oral administration of rhubarb (50 mg x kg(-1)). The plasma rhein concentration was determined by HPLC. The pharmacokinetics of rhein were analysed by 3P97 program.The absorption of rhein was very fastafter oral administration of rhubarb extract in the healthy volunteers. The main pharmacokinetic parameters of rhein were C(max) (3.20 +/- 1.08) microg x mL(-1); t(max) (1.03 +/- 0.41) h; t(1/2alpha) (0.21 +/- 0.02) h; t(1/2beta) (2.68 +/- 1.09) h; MRT(5.31 +/- 1.78) h; AUC(0-infinity) (1 573.08 +/- 366.48) microg x mL(-1) min(-1), respectively.Rhein could be absorbed rapidly and its pharmacokinetics was consistent with two-compartment model.
Cite
Citations (8)