scholarly journals Biliary excretion of amphetamine and methamphetamine in the rat

1972 ◽  
Vol 129 (1) ◽  
pp. 25-29 ◽  
Author(s):  
J. Caldwell ◽  
L. G. Dring ◽  
R. T. Williams

1.14C-labelled amphetamine and methamphetamine were injected into rats cannulated at the bile duct under thiopentone anaesthesia and the output of their metabolites in urine and bile was determined. 2. With amphetamine, 69% of the14C was excreted in the urine and 16% in the bile in 24h. The main metabolite in bile was the glucuronide of 4-hydroxyamphetamine. The output of unchanged amphetamine was much greater in cannulated rats than in intact rats. 3. With methamphetamine, 54% of the14C appeared in the urine and 18% in the bile. The main metabolite in the bile was the glucuronide of 4-hydroxynorephedrine. The output of amphetamine, a metabolite of methamphetamine, was much greater in cannulated rats than in intact rats. 4. Evidence has been obtained for the enterohepatic circulation of certain amphetamine and methamphetamine metabolites in the rat. 5. Thiopentone anaesthesia appeared to inhibit the ring hydroxylation of amphetamine administered as such or formed as a metabolite of methamphetamine.

1987 ◽  
Vol 253 (6) ◽  
pp. G787-G792
Author(s):  
A. D. Bedrick ◽  
M. A. Wells ◽  
D. L. Ford ◽  
O. Koldovsky

Tritium-labeled prostaglandin F2 alpha was administered via orogastric tube to bile duct-cannulated suckling and weanling rats to determine if maturational differences were present in the biliary excretion of prostaglandin F2 alpha and metabolites. Animals were killed 2 h after radioactivity administration. Characterization of radioactivity present in bile revealed age-related differences in biliary prostaglandin F2 alpha excretion. Suckling rats had a greater proportion of radioactivity migrating in chromatographic regions of greater polarity than prostaglandin F2 alpha. Compared with the weanling, a significantly greater amount of radioactivity cochromatographed with intact, unmetabolized prostaglandin F2 alpha (33.08 +/- 1.99 vs. 21.38 +/- 1.46). These results indicate that orogastrically administered prostaglandin F2 alpha can be absorbed from the gastrointestinal tract, transported to the liver, and subsequently excreted into bile and detected in an unmetabolized form in suckling and weanling rats. The enterohepatic circulation of milk-derived prostaglandin present in bile may contribute to the overall content of intestinal prostaglandins.


1973 ◽  
Vol 136 (4) ◽  
pp. 967-978 ◽  
Author(s):  
Robin D. Hughes ◽  
Peter Millburn ◽  
R. Tecwyn Williams

1. The excretion in the bile and urine of intraperitoneally injected14C-labelled monoquaternary ammonium or pyridinium cations was measured in bile-duct-cannulated rats (ten compounds) and in guinea pigs and rabbits (six compounds). 2. Seven of these, namely N-methylpyridinium, tetraethylammonium, trimethylphenylammonium, diethylmethylphenylammonium, methylphenyldipropylammonium, dibenzyldimethylammonium and tribenzylmethylammonium, were excreted largely unchanged in the bile and urine. 3. 3-Hydroxyphenyltrimethylammonium, 3-bromo-N-methylpyridinium and cetyltrimethylammonium were metabolized to an appreciable extent in the rat. 4. In intact rats intraperitoneally injected trimethylphenylammonium (mol.wt. 136) was excreted mainly in the urine, dibenzyldimethylammonium (mol.wt. 226) was excreted in roughly equal amounts in the urine and faeces, and tribenzylmethylammonium (mol.wt. 302) was excreted mainly in the faeces. The faecal excretion of these compounds corresponded to their biliary excretion in bile-duct-cannulated rats. About 3–4% of tribenzyl[14C]methylammonium was eliminated as14CO2. 5. In rats the extent of biliary excretion of four cations with molecular weights in the range 94–164 was less than 10% of the dose, whereas that of five cations with molecular weights 173–302 was greater than 10%. These results and other data from the literature suggested that the molecular weight needed for the biliary excretion of such cations to an extent of 10% or more of the dose was about 200±50. Studies with six cations in guinea pigs and rabbits suggest that this value applies also to these species. 6. The results suggest that the threshold molecular weight for the appreciable (>10%) biliary excretion of monoquaternary cations is different from that for anions (Millburn et al., 1967a; Hirom et al., 1972b). With rats, guinea pigs and rabbits, no significant species difference was noted, whereas with anions there is a marked species difference.


1991 ◽  
Vol 3 (2) ◽  
pp. 98-100 ◽  
Author(s):  
F. Rulli ◽  
M. Muzi ◽  
E. Zanella ◽  
P. Cipriani ◽  
A. Magni ◽  
...  
Keyword(s):  

2020 ◽  
Vol 18 (5) ◽  
pp. 36-41
Author(s):  
V.P. Novikova ◽  
◽  
L.N. Belousova ◽  

Bile acid diarrhoea is a common cause of chronic diarrhoea associated with disturbance of the enterohepatic circulation: either excessive biosynthesis/secretion of bile acids or disordered absorption of bile acids in the ileum. At the same time bile acid diarrhoea is an insufficiently studied, frequently underestimated condition, and the questions remain concerning its diagnosis and management. The work discusses the main groups of causes of this pathology, modern diagnostic methods and the difficulties of a differential search. Also, the article offers information about the diet therapy of bile duct diarrhoea and the main groups of administered medications, in particular, modern enterosorbents.


PEDIATRICS ◽  
1973 ◽  
Vol 51 (6) ◽  
pp. 992-997
Author(s):  
Adolf Stiehl ◽  
M. Thaler ◽  
William H. Admirand

The effects of phenobarbital (PB) on bile salt metabolism in a patient with severe cholestasis due to congenital paucity of perilobular bile ducts were studied with 14C-cholate and 3H-chenodeoxycholate. During the control period (without PB) cholate was the predominant bile salt in the peripheral blood, whereas chenodeoxycholate was predominant in the total bile salt pool. This difference in the distribution of the two primary bile salts appeared to be caused by relatively greater impairment of excretion of cholate from the liver cell into the bile. PB administration caused a decrease in the total serum bile salt concentration (from 132 to 62µg/ml), in the total bile salt pool (from 412 to 304 mg) and in the biologic half-life (cholate from 106 to 34 hours; chenodeoxycholate from 77 to 42 hours). The proportion of the total bile salt pool present in the peripheral blood decreased from 16.8% to 11.7%. In addition, PB markedly increased the fecal bile salt excretion. These data suggest the PB improves pruritus in this type of intrahepatic cholestasis by reducing serum bile salt concentrations. This is accomplished by a shift in bile salts from the peripheral blood into the enterohepatic circulation and by enhancing fecal bile salt excretion.


1986 ◽  
Vol 79 (9) ◽  
pp. 522-527 ◽  
Author(s):  
Xu Guorong ◽  
C J C Kirk ◽  
A W Goode

Changes in biliary concentrations of bile acids, phospholipids and cholesterol and biliary pressures were measured in dogs. These parameters were studied during 7-day periods of partial biliary obstruction, of varying degrees, and after 24-hour and 48-hour periods of complete obstruction. The samples were obtained via an exteriorized but intact enterohepatic circulation allowing the introduction of varying degrees of obstruction and bile sampling. Biliary obstruction reduced the concentration of all biliary lipids especially when the obstruction produced pressures in excess of 75% of the maximum biliary secretion pressure. Only immediately after the release of a 48-hour period of complete obstruction did the risk of cholesterol supersaturation of bile occur. However, at that time there was a greatly reduced concentration of lipids in the bile and the amount of cholesterol that could potentially have precipitated was very small. It is suggested that this supersaturation would not play a significant role in the formation of gallstones.


1978 ◽  
Vol 13 (3) ◽  
pp. 255-263 ◽  
Author(s):  
FRANCIS A. BURGENER ◽  
HARRY W. FISCHER ◽  
THEODORE D. KENYON

1982 ◽  
Vol 242 (5) ◽  
pp. G522-G532 ◽  
Author(s):  
M. Gascon-Barre

The biliary excretion of [3H]-25-hydroxyvitamin D3 ([3H]25(OH)D3) was studied in vitamin D-depleted female rats over a 3-h period after intravenous or intraduodenal administration of intact [3H]25(OH)D3 and after the intraduodenal readministration of the [3H]25(OH)D3-derived biliary material. In each group four doses of 25(OH)D3 were administered (0.25, 2.5, 25, and 250 nmol/100 g). Over the dose range studied, the biliary excretion of [3H]25(OH)D3 could not be saturated, indicating that the biliary excretion of 25(OH)D3 is a reliable detoxification mechanism in circumstances of 25(OH)D3 intoxication. Analysis of plasma, liver, and bile suggests that the canalicular membrane seems to be rate limiting in the biliary excretion of 25(OH)D3. The intraduodenal administration of biliary excretion compounds derived from [3H]25(OH)D3 showed that they are efficiently reexcreted in newly secreted bile, confirming the existence of an enterohepatic circulation for 25(OH)D3. In this group of animals, however, the plasma analysis indicates that these compounds reach the systemic circulation in insignificant quantities, suggesting that the enterohepatic circulation probably plays a limited role in the body 25(OH)D3 economy.


Xenobiotica ◽  
1981 ◽  
Vol 11 (3) ◽  
pp. 189-196 ◽  
Author(s):  
D. Brewster ◽  
M. J. Humphrey ◽  
M. A. McLeavy

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