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What Is Ursodeoxycholic Acid Used For?
2022-02-25
Ursodeoxycholic acid is a cholelithiant commonly used in the gastroenterology department, and also a cholelithiasis dissolving agent, so it can be used in the treatment of gallstones under normal circumstances, on the premise that the gallbladder has normal contraction function.
When it is only used for lytic treatment, the treatment course is as long as 6 to 24 months, and the oral dose is 10 ml per kg body weight per day.In addition, the drug can treat cholestatic liver diseases, such as primary cholestatic cirrhosis.At the same time can also treat bile reflux gastritis, each time 250 mg, once a day, before going to bed oral.
This product is white powder; No smell, bitter taste. It is soluble in ethanol but insoluble in chloroform. It is soluble in acetic acid and soluble in sodium hydroxide test solution. Melting point The melting point of this product is 200 ~ 204℃. The specific curl was taken, weighed accurately, dissolved with anhydric ethanol and diluted quantitatively to make a solution containing 40mg per 1ml. The specific curl is from +59.0 to +62.0.
This medicine can promote the secretion of endogenous bile acid and reduce the reabsorption. Antagonize the cytotoxic effect of hydrophobic bile acid and protect liver cell membrane. Dissolution of cholesterol calculus; Ursodeoxycholic acid capsules should not be taken at the same time with drugs such as caleenine (cholestylamine), Caletipol (cholestylamine), aluminum hydroxide and/or aluminum hydroxide magnesium trisilicate, as these drugs can bind to ursodeoxycholic acid in the intestine, thereby impeding absorption and affecting efficacy.
Ursodeoxycholic acid capsules should be taken two hours before or two hours after taking the drug if the above drug must be taken.Ursodeoxycholic acid capsule can increase the absorption of cyclosporin in the intestinal tract. Patients taking cyclosporin should do the monitoring of cyclosporin serum concentration, and adjust the dose of cyclosporin if necessary. In some cases, ursodeoxycholic acid capsule will reduce the absorption of ciprofloxacin.
1. Pharmacodynamics
ursodeoxycholic acid (UDCA) is the 7-isomer of goosenodeoxycholic acid (primary bile acid in normal bile), which has the following functional characteristics :
(1) increase the secretion of bile acid, lead to the change of bile acid composition, and increase its content in bile, which is beneficial to the bile effect.
(2) Can inhibit the synthesis of liver cholesterol, significantly reduce the amount of cholesterol and cholesterol ester in bile and cholesterol saturation index, thus conducive to the gradual dissolution of cholesterol in stones. UDCA also promotes the formation of crystalline complexes of liquid cholesterol, which accelerate the excretion and clearance of cholesterol from the gallbladder to the intestine.
(3) Relax THE sphincter of Oddi to strengthen the gallbladder.
(4) Reduce liver fat, increase the activity of liver catalase, promote the accumulation of liver glycogen, and improve the liver's ability of anti-toxin and detoxification; It can also reduce the concentration of triacylglycerol in liver and blood.
(5) Inhibit the secretion of digestive enzymes and digestive fluids.
(6) the results also show that UDCA in chronic liver disease have immunomodulatory effect, can significantly reduce liver cell type Ⅰ expression of human leucocyte histocompatibility antigens (HLA), reduce the number of the activation of T cells.
Compared with this drug, goose-deoxycholic acid (CDCA) is basically the same in terms of stone dissolution mechanism and efficacy, but the AMOUNT of CDCA is large, the tolerance is slightly poor, the incidence of diarrhea is high, and it has certain toxicity to the liver. Foreign data suggest that this medicine also has the following characteristics :
(1) caused by the dissolution of stone effect faster than CDCA.
(2) Unlike CDCA, patient weight is not a predictor of treatment success.
(3) There is evidence that the dissolution rate of this drug for larger stones is higher than that of CDCA.
(4) The efficacy of this drug is dose-dependent. Therefore, CDCA has been rarely used, and this drug is recommended as the first choice for the treatment of cholesterol gallstones.
2. Pharmacokinetics
This drug is weakly acidic, which is absorbed rapidly through passive diffusion after oral administration, and two peaks of blood drug concentration occur at 1 hour and 3 hours respectively.Because only a small amount of drugs enter the systemic circulation, blood drug concentration is very low.The most effective site of absorption is the ileum, which has a moderately alkaline environment. After absorption, it binds to glycine or taurine in the liver and is discharged from the bile into the small intestine to participate in the enterohepatic circulation.
Lithocholic acid (LCA) was converted by bacteria into the same hydrolyzed part of UDCA in the small intestine, while the other was converted by bacteria into Lithocholic acid (LCA), which thus decreased its potential hepatic toxicity. The therapeutic effect of this drug was related to the concentration of the drug in bile, but not plasma concentration. The half-life is 3.5-5.8 days, mainly excreted with feces, with a small amount of renal excretion. It is not clear whether UDCA is excreted in human breast milk, as only a small amount of UDCA appears in serum after oral administration, and therefore very small amounts, even if UDCA can be secreted into milk.
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