URSODEOXYCHOLIC ACID: USE, THERAPEUTIC EFFECT, CONTRAINDICATIONS - MEDICINE - 2025

The ursodeoxycholic acid is a bile acid type hydrophilic possessing therapeutic properties in the case of cholestatic liver diseases. It is also known by the name of ursodiol and by its abbreviation UDCA (due to its acronym in English ursodeoxycholic acid).

The pharmaceutical industry introduced ursodeoxycholic acid in capsules. Each capsule contains inside a lyophilisate of 300 mg of ursodeoxycholic acid, this being the active principle of the drug.

Chemical structure of ursodeoxycholic acid, a drug used in the treatment of liver diseases. Source: Wikipedia.org/Pixabay.com. Design: Msc. Marielsa gil

It contains some excipients such as powdered cellulose, magnesium stearate, sodium carboxymethyl starch and colloidal silica. In addition, the capsule shell consists of gelatin, quinoline yellow, indigo carmine and titanium dioxide.

Its main function is to dissolve lithiasic stones, as well as to protect cells from oxidative stress, since most liver diseases present with an increase in lipid peroxidation, being a possible determining pathophysiological factor.

It is useful in treating non-alcoholic fatty liver disease and liver cirrhosis. Páez et al. Demonstrated that this drug is capable of reducing the value of transaminase (ALT) when used for a reasonable period of time.

Ursodeoxycholic acid has been shown to have anti-inflammatory as well as anti-apoptotic and immunomodulatory effects.

Like all medications, it must be administered following the instructions of the treating physician. It is also contraindicated under certain conditions and can cause gastrointestinal disorders as an adverse effect in a small group of individuals.

Use

It is used in the treatment of liver diseases, mainly in patients with gallstones. However, before prescribing this drug to dissolve stones, the doctor should perform an oral cholecystography study on the patient.

This study is carried out in order to determine if cholesterol gallstones are radiolucent or radio lucid and if the gallbladder is still functional, since only in these cases is it useful to use this drug.

It cannot be used if the study reveals a non-functioning gallbladder or if the cholesterol stones have any of the following characteristics: they are calcified, they are radio-opaque or if there is the presence of bile pigment stones.

It is also used in primary biliary cirrhosis and non-alcoholic fatty liver disease.

Finally, it is useful to prevent the formation of cholesterol stones in people who are subjected to strict weight loss diets.

Therapeutic effect

This drug is a hydrophilic substance that has the ability to lyse or dissolve cholesterol gallstones, and it also inhibits the absorption and synthesis of cholesterol at the intestinal and liver levels respectively. This allows the accumulated cholesterol to be eliminated by the intestine, preventing new stones from forming.

On the other hand, it modulates the immune response. That is, it has an anti-inflammatory effect. Also, it prevents cells from hasty death, which is why it has an antiapoptotic effect.

In addition, it generates the recovery of liver tissue, expressed by the decrease of certain biochemical parameters, such as transaminases, alkaline phosphatase, bilirubin, among others.

One of its mechanisms of action consists of the replacement of hydrophobic bile salts with toxic effects by hydrophilic ones.

The therapeutic effects of this drug are not immediate, long-term treatment is needed to observe satisfactory results. The duration of treatment can vary from one patient to another, although it usually ranges from 6 months to 2 years.

Pharmacokinetics

The drug is administered orally, being rapidly absorbed by the body. Upon reaching the liver, it is conjugated with the amino acid glycine, concentrated in the bile, and then directed to the intestine, where only 20% enters the enterohepatic circulation.

The drug is excreted in the feces. The drug has a shelf life of approximately 4 to 6 days.

Contraindications

It is contraindicated in:

-In patients allergic to this substance.

-During lactation (although very low concentrations of the drug have been found in breast milk, but the effect on the newborn is unknown).

-During pregnancy. However, despite the fact that it is the only drug that has been effective in reducing the symptoms of intrahepatic cholestasia during pregnancy and that no cases of malformations of fetuses born to mothers treated with ursodeoxycholic acid have been reported, there are still doubts about its use in pregnant women.

-Patients with gastric or duodenal ulcer.

-In patients with positive cholecystography studies for: non-functioning gallbladder, calcified cholesterol stones or radiopaque cholesterol stones.

- Diseases that present with deficiency of the enterohepatic circulation.

- Inflamed gallbladder.

-Decrease in the contractile capacity of the gallbladder.

-Obstruction of the common bile duct or bile ducts (cystic ducts).

Precautions

The effect of this medicine can be interfered with or blocked if it is administered together with other drugs or drugs, therefore special care should be taken in patients who are being treated with:

-Oral contraceptives.

-Antiacid with aluminum.

-Medicines to lower the concentration of lipids in the blood.

-Neomycin (Antibiotic of the aminoglycoside family).

-Hepatotoxic drugs.

Most of them interfere with the absorption of the drug or its effectiveness.

Dose

It should be noted that the medications must be prescribed by your treating physician and the dose and duration of the treatment will be determined by the doctor according to the clinical and pathology that the patient presents. Self-medication is never advisable.

In the case of gallstones, the recommended daily dose for adults is 8-10 mg / kg / day. This concentration is distributed during the day (several doses), approximately 2 capsules, for 6 to 12 months.

For biliary cirrhosis it is 13-15 mg / kg / day, equally distributed in several doses. Approximately 3-4 capsules. Treatment usually lasts 9 to 24 months.

In the case of patients on weight loss programs (diets), a dose of 2 capsules a day of 300 mg is recommended (in two doses), for 6-8 months.

Adverse effects

Any medication can cause unwanted effects, however, these can occur with different degrees of frequency. For example, the use of ursodeoxycholic acid can cause gastrointestinal disorders in a ratio of 1-10 patients per 10,000 treated.

Gastrointestinal disorders include: abdominal pain, nausea, vomiting, indigestion, constipation, biliary pain, altered sense of taste, flatulence or dizziness, among others. In very sporadic cases, diarrhea may occur.

If any of these disorders occur, the prescribed dose should be reduced, but if the symptoms continue, the drug should be permanently discontinued.

recommendations

It is advised that all patients treated with this drug undergo monitoring studies in order to evaluate the evolution of the disease. The liver profile should be performed monthly for 3 months, mainly AST, ALT and g-glutamyltransferase (GGT).

Subsequently, the studies are removed every 3 months and, after 6 to 10 months of treatment, the doctor will indicate a cholecystography.

References

1. Herrera A, Nasiff A, Arus E, Cand C, León N. Fatty liver: diagnostic and therapeutic approach. Rev cubana med. 2007; 46 (1). Available at: scielo.sld
2. Rodríguez A, Coronado J Julián, Solano A, Otero W. Primary biliary cholangitis. Part 1. Update: generalities, epidemiology, factors involved, pathophysiology and clinical manifestations. gastroenterol. Peru. 2017; 37 (4): 357-364. Available at: scielo.org.
3. Morgan G, Villalón V, Danilla S, Villavicencio L, Kottmann C, Illanes S. Does the use of ursodeoxycholic acid improve the perinatal prognosis in pregnant women with intrahepatic cholestasis of pregnancy? Chil. Obstet. Ginecol. 2007; 72 (5): 292-297. Available at: scielo.conicyt.
4. Cerrillo M, Argüello A, Avilés C, Gil L, Amezcua A, González G. Cholestasis of pregnancy: Etiology, Clinic, Diagnosis and Treatment. Archives of Medicine, 2005; 5 (1): 1-15. Available at: redalyc.org
5. "Ursodeoxycholic acid." Wikipedia, The Free Encyclopedia. 24 Sep 2017, 18:20 UTC. 24 Jul 2019, 16:39