Nonlinear pharmacokinetics of hepatobiliary transport of rose bengal in rats after iv bolus administration with varying doses

1992 ◽  
Vol 13 (9) ◽  
pp. 647-662 ◽  
Author(s):  
Huan Kui Wang ◽  
Seiji Miyachi ◽  
Masayo Yamazaki ◽  
Yasufumi Sawada ◽  
Youn Bok Chung ◽  
...  
2012 ◽  
Vol 45 (1-2) ◽  
pp. 79-89 ◽  
Author(s):  
Karin G. Haug ◽  
Benjamin Weber ◽  
Guenther Hochhaus ◽  
Veronika Butterweck

1977 ◽  
Vol 232 (5) ◽  
pp. E445 ◽  
Author(s):  
J L Mahu ◽  
P Duvaldestin ◽  
D Dhumeaux ◽  
P Berthelot

The hepatobiliary transport of three structurally related phthaleins was compared in the rat, and found to differ to a large extent in three experimental conditions: 1) after a 72-h fast; 2) after a 4-day phenobarbital treatment; and 3) during infusion of bile salts: sodium dehydrocholate or taurocholate. In the fasting group, bile flow and bile salt excretion (on a whole liver basis) decreased by 49 and 41%, respectively; bromsulphthalein sodium (BSP) and dibromsulphthalein sodium (DBSP) transport maximum (Tm) were reduced by 59 and 50%; however, rose bengal (RB) Tm remained normal. Phenobarbital pretreatment yielded a 44 and 29% increase in BSP and DBSP Tm, respectively, whereas RB Tm remained unchanged. Dehydrocholate infusion caused a 27 and 49% increase in BSP and DBSP Tm, whereas RB Tm increased by 12%. On the contrary, equimolar taurocholate infusion yielded a more important increase in RB Tm (56%) than in BSP and DBSP (31 and 22% respectively). It is suggested that RB does not share the same liver-to-bile excretory pathway as that of the former molecules. Our results emphasize the difficulties in predicting the biliary excretion of foreign compounds, even when their structure is closely similar.


2014 ◽  
Vol 74 (S 01) ◽  
Author(s):  
JJ Löytved-Hardegg ◽  
M Brunner ◽  
JJ Ries ◽  
S von Felten ◽  
C Heugel ◽  
...  
Keyword(s):  

1999 ◽  
Vol 81 (04) ◽  
pp. 605-612 ◽  
Author(s):  
Dmitry V. Sakharov ◽  
Marrie Barrett-Bergshoeff ◽  
Rob T. Hekkenberg ◽  
Dingeman C. Rijken

SummaryIn a number of cases, thrombolytic therapy fails to re-open occluded blood vessels, possibly due to the occurrence of thrombi resistant to lysis. We investigated in vitro how the lysis of hardly lysable model thrombi depends on the choice of the plasminogen activator (PA) and is accelerated by ultrasonic irradiation. Lysis of compacted crosslinked human plasma clots was measured after addition of nine different PAs to the surrounding plasma and the effect of 3 MHz ultrasound on the speed of lysis was assessed.Fibrin-specific PAs showed bell-shaped dose-response curves of varying width and height. PAs with improved fibrin-specificity (staphylokinase, the TNK variant of tissue-type PA [tPA], and the PA from the saliva of the Desmodus rotundus bat) induced rapid lysis in concentration ranges (80-, 260-, and 3,500-fold ranges, respectively) much wider than that for tPA (a 35-fold range). However, in terms of speed of lysis, these three PAs exceeded tPA only slightly. Reteplase and single-chain urokinase were comparable to tPA, whereas two-chain urokinase, anistreplase, and streptokinase were inferior to tPA. In the case of fibrin-specific PAs, ultrasonic treatment accelerated lysis about 1.5-fold. For streptokinase no acceleration was observed. The effect of ultrasound correlated with the presence of plasminogen in the outer plasma, suggesting that it was mediated by facilitating the transport of plasminogen to the surface of the clot.In conclusion, PAs with improved fibrin-specificity induce rapid lysis of plasminogen-poor compacted plasma clots in much wider concentration ranges than tPA. This offers a possibility of using single-or double-bolus administration regimens for such PAs. However, it is not likely that administration of these PAs will directly cause a dramatic increase in the rate of re-opening of the occluded arteries since they are only moderately superior to tPA in terms of maximal speed of lysis. Application of high-frequency ultrasound as an adjunct to thrombolytic therapy may increase the treatment efficiency, particularly in conjunction with fibrin-specific PAs.


1975 ◽  
Vol 14 (04) ◽  
pp. 330-338
Author(s):  
L. G. Colombetti ◽  
J. S. Arnold ◽  
W. E. Barnes

SummaryTc-99m pyridoxylidene glutamate has proven to be an excellent biliary scanning agent, far superior in many respect to the commonly used 1-131 rose bengal. The preparation of the compound as previously reported by Baker et al is too time consuming and requires the use of an autoclave which is not available in most nuclear medicine departments. In our facility, we have been preparing similar compounds using several aldehydes and monosodium glutamate to make labeled complexes having the same pharmacological characteristics. The mixture of monosodium glutamate, aldehyde, and Tc-99m pertechnetate is made slightly alkaline, purged with helium, and placed in a sealed vial. The vial, which is protected by a wire basket, is then heated in a laboratory oven at 130° C for a period of 15 to 20 minutes. During this time, the technetium is reduced to a lower valence state and bound to the complex formed. Chromatographic data show that these compounds are chemically similar to that previously reported. The compounds prepared concentrate in the gall bladder of the rabbit in less than 10 minutes. Kinetic studies have been performed on dogs with a scintillation camera and small digital computer to measure rates of blood clearance, liver and gall bladder uptake, and excretion into the intestine. The aldehyde — glutamate complex promises to be a useful scanning agent for the diagnosis of biliary and hepatocellular diseases.


1994 ◽  
Vol 71 (06) ◽  
pp. 768-772 ◽  
Author(s):  
Gerhard Dickneite ◽  
Jörg Czech

SummaryRats which were infected with the gramnegative pathogen Klebsiella pneumoniae develop disseminated intravascular coagulation (DIC), multi-organ failure (MOF) and finally die in a septic shock. We investigated the therapeutic effect of antibiotic (tobramycin) treatment combined with the infusion of the highly specific thrombin inhibitor rec. hirudin. Although administration of 2 mg/kg tobramycin alone leads to a decrease of the bacterial burden, DIC could not be prevented. Infusion of rec. hirudin (0.25 mg/kg x h) for 4 h (start of treatment 1 h post infection), in addition to a bolus administration of tobramycin, led to an amelioration of DIC parameters as fibrinogen, thrombin-antithrombin complex (TAT) and platelets. Serum transaminase levels (GOT, GPT) as a marker of MOF were significantly improved by rec. hirudin, the T50 value increased from 17 h in the tobramycin group to 42 h in the tobramycin + rec. hirudin giuup, muilality rates were 90% or 60%, respectively. Combination of heparin (10011/kg x h) and tobramycin was not effective on survival.


1976 ◽  
Vol 12 (2) ◽  
pp. 282
Author(s):  
YS Kim ◽  
BS Choi ◽  
HY Kang ◽  
CY Park
Keyword(s):  

Sign in / Sign up

Export Citation Format

Share Document