Is Ursodeoxycholic Acid Tablet Good for Liver Disease?

Posted On April 11, 2023

Introduction 

Have a liver problem? Here, I will review the Ursodeoxycholic acid tablet medicine, which is a promising agent in liver disease.

Ursodeoxycholic acid mainly works on the liver and has a classical role in Cholestasis and related conditions such as gallstones. It is also called Hepatoprotective medicine. 

The global prevalence of Cholestasis and Cholelithiasis have risen in recent years. It can also be seen commonly in pregnancy, affecting 0.3 to 5.6% of pregnancies worldwide. 

Ursodeoxycholic acid was known as a liver tonic earlier, but now this medicine is used in various liver diseases. 

Even, Ursodeoxycholic acid is considered a gold-standard medicine in Primary Biliary Cholangitis, which causes Intra-hepatic Cholestasis. 

In this article, I will discuss everything about Ursodeoxycholic acid tablet medicine, such as its uses, dosage, pharmacokinetics, mechanisms, side effects, and contraindications. 

Let’s get started 

What is Ursodeoxycholic acid?

Ursodeoxycholic acid (UDCA) belongs to a class of gallstone-dissolving agents. It is also known as “Ursodiol”. 

It is a derivative of chenodeoxycholic acid. This chenodeoxycholic acid is a natural bile acid that is present in the human body. 

Whenever we have a deficiency of this bile acid, we need to take it from outside.

Since chenodeoxycholic acid is not well tolerated in the human body. That’s why the researcher has made this classical Ursodiol medicine from bile acid of Bear. 

If we spilt Ursodeoxycholic acid, it would be “Ursus” and “deoxycholic acid.”

“Ursus” is a Latin word meaning Bear. While “Deoxycholic acid” is a bile salt. 

It means Ursodeoxycholic acid is natural bile salt that extracts from the bile of Bear. 

In 1955, a Japanese scientist made this gallstone-dissolving medicine. It was launched for therapeutic use in the US market in 1987. 

Initially, it was designated an orphan drug, but now it is frequently used in many liver diseases. 

What is Ursodeoxycholic acid used for? Who should take this medicine?

Ursodiol is a liver protective medicine. Your doctor may prescribe this medicine if you have liver-related diseases such as cholestasis, gallstones, etc. 

Let’s discuss the proper clinical use of Ursodiol in detail – 

Ursodeoxycholic acid tablet for Primary Biliary Cholangitis (PBC)

In PBC, Cholangitis means inflammation of the bile duct. It is an autoimmune disease that causes inflammation or destruction in your liver’s small bile ducts (or internal bile ducts). 

This inflammation causes intrahepatic bile duct obstruction that impairs bile flow into your bile duct. 

Due to this, many bile contents get a deposit or build up in your liver. 

Gradually, it starts damaging your liver cells and causes fibrosis. Eventually, it leads to cirrhosis if untreated. This is also called Primary Biliary Cirrhosis. 

This medical condition causes Intrahepatic Cholestatic Liver Disease (or Cholestasis Jaundice). 

The Ursodeoxycholic acid tablet is an FDA-approved medicine for treating Primary Biliary Cholangitis (PBC). It is also considered a first-line treatment for PBC. 

This medicine acts as a bile salt, dissolving a bunch of cholesterol and increasing bile flow in your liver cells.  

Over time, it reduces scarring and improves liver functioning. Overall, this medicine helps prevent or delay liver damage.

Ursodeoxycholic acid tablet for Gallstones

Gallstones are a common problem for most people. There is an imbalance of cholesterol and bile salt in your bile. 

↑ Cholesterol: ↓Bile salt → Cholesterol Stones Formation

Suppose your cholesterol level increases, and there is a bile salt deficiency. In that case, it causes crystallization and formation of cholesterol stones in your bile.

This excess cholesterol may deposit in your gall bladder and leads to cholesterol gallstones. Clinically, it is called Cholelithiasis. 

As we know, Ursodiol is a gallstone-dissolving drug. This medicine helps to dissolve cholesterol gallstones and reduces the cholesterol concentration in your bile. It also decreases cholesterol absorption from your intestine. 

Obviously, it should be used for gallstone problems who do not want cholecystectomy-like surgery. Still, ursodeoxycholic acid is not FDA approved drug for gallstones. 

According to a research study, this medicine can be used if there are small size of gallstones (less than 5 mm diameter), or it would be best if they are floating.

It is generally avoided if the gallstone size is more than 15 mm in diameter. 

Ursodeoxycholic acid tablet for Primary Sclerosing Cholangitis (PSC)

Primary Sclerosing Cholangitis (PSC) is also a type of chronic cholestatic liver disease. 

In this liver disease, you may have internal and external bile duct inflammation. This causes fibrosis in your liver, and bile ducts become narrow and get a block. 

Due to this blockage, bile gets deposited and builds up in your liver cells. Eventually, it causes liver damage or liver cirrhosis. 

Still, there needs to be a satisfactory medicine for PSC. 

According to a research study in 2006, Ursodeoxycholic acid is the only option for treating Primary Sclerosing Cholangitis. 

Although Ursodiol has no obvious benefits in PSC patients, it has been seen that this medicine has the potential to improve the parameters of the liver function test like – serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), alanine aminotransferase (ALT), bilirubin, and GGT (Gamma-glutamyltransferase).

Therefore, Ursodiol can be used as an off-label in PSC if the benefits outweigh the risks. 

Ursodeoxycholic acid tablets for Non-Alcoholic Fatty Liver Disease (NAFLD)

A recent study published in the Journal of expert review of Gastroenterology and Hepatology, 2022 concluded that Ursodeoxycholic acid is an effective medicine in non-alcoholic steatohepatitis (NASH). 

It significantly reduces the ALT level, GGT level and other laboratory parameters of the liver. 

Ursodiol has some crucial clinical properties like anti-inflammatory, antioxidant, and anti-fibrotic. This may reduce the liver damage that occurs in non-alcoholic steatohepatitis. 

Ursodiol can be an effective medicine for NAFLD if combined with other drugs (like statins, vitamin E, etc.)

Ursodeoxycholic acid tablet for Post Bariatric Surgery

Bariatric surgery is a weight loss surgery where some part or entire stomach is removed and directly connected to your small intestine. 

After this surgery, you may have rapid weight loss that causes cholesterol gallstone formation due to changes in bile acid circulation. 

As per a study, Ursodeoxycholic acid tablet has a prophylactic role preventing cholesterol gallstones formation after bariatric surgery.

Therefore, this medicine can be recommended for Post-Bariatric Surgery. 

How does Ursodeoxycholic acid work in your body? 

Ursodeoxycholic acid is not a typical drug like systemic medicine. Typical medicines go to your bloodstream and do work, but Ursodiol is not like that. 

You might be thinking about how it works precisely and travels in the human body. 

Ursodiol has a unique mechanism, and it works in enterohepatic circulation. 

Here, I will reveal this mysterious drug and tell you the exact pharmacokinetics and mechanism of action of ursodeoxycholic acid. 

Before this, we need to understand something about bile – 

The main function of the liver is to bile synthesis so that the small intestine can absorb fatty meals easily. 

The bile has five main components: bile acid, conjugated bilirubin (bile pigment), free cholesterol, phospholipids and IgA antibody.

Among these, bile acid is an essential component that helps digestion and absorption of free cholesterol. 

Cholic acid and chenodeoxycholic acid are primary natural bile acids in our bile. Intestinal bacteria convert it into secondary bile acid (deoxycholic acid and lithocholic acid) in our small intestine. Eventually, it is eliminated through faeces. 

Generally, cholesterol remains to dissolve in bile with the help of bile acids (cholic acid and chenodeoxycholic acid). 

Suppose you have a liver problem, and your liver cells cannot produce sufficient bile acid. In that case, you will have bile acid deficiency that causes an increased amount of free cholesterol.

This increased free cholesterol may get deposited in your gallbladder, leading to gallstones. 

Here, you don’t need to worry.

The researcher has made a classical drug that mimics the natural bile acid (chenodeoxycholic acid). 

The name of this mysterious medicine is Ursodeoxycholic acid (or Ursodiol). This drug displaces endogenous bile acid. 

Ursodiol is an enterohepatic medicine that does not enter your main bloodstream. 

When you take a Ursodeoxycholic acid tablet, it gets absorbed from your small intestine. It reaches your portal hepatic circulation by the portal vein. After which, this medicine enters your liver.

Once Ursodiol reaches liver cells, it starts doing First-Pass Metabolism (FPM). Around 60 % of Ursodiol gets metabolized through liver cells.

In FPM, Ursodiol gets conjugate with glycine and taurine. After conjugation, this conjugated ursodeoxycholic acid gets mixed with natural bile juice. 

In this bile composition, ursodeoxycholic acid work as a bile acid. This conjugated ursodeoxycholic acid enters the bile and starts travelling in the bile duct and gall bladder. 

Eventually, this bile reaches the small intestine.

Here, conjugated Ursodiol comes out in the lumen of the small intestine. Then, conjugated Ursodiol gets metabolized with intestinal bacteria and converted into lithocholic acid. 

This lithocholic acid does not accumulate with bile acid and gets excreted via faeces. 

Although, Intestinal bacteria cannot metabolize the entire amount of Ursodiol. So, some amount of conjugated Ursodiol goes back to the liver by the hepatic portal vein. This pathway is called Enterohepatic Circulation.

This is the reason that’s why Ursodeoxycholic acid is known as an enterohepatic drug. 

Let’s go through the Ursodeoxycholic acid mechanism of action in different organs – 

• In the Liver – Ursodiol has anti-inflammatory, anti-apoptotic, cytoprotectant and antioxidant properties that protect your liver from damage. It also increases the biosynthesis of bile acid in your liver cells. 
• In the Gallbladder – Ursodiol acts as a choleretic agent that stimulates the gallbladder to promote bile flow. It also helps the dissolving the cholesterol gallstones. 
• In the Intestine – Ursodiol reduces the cholesterol absorption from the intestine and clearly decreases the cholesterol content from your bile. 

What is the proper dosage of ursodeoxycholic acid? How long should ursodeoxycholic acid be taken? 

The proper dose of Ursodeoxycholic acid depends on body weight and type of medical condition. 

The usual starting dose of Ursodeoxycholic acid is 8 mg/kg/day. The maximum daily dose of Ursodeoxycholic acid can be 13 to 14 mg/kg/day. 

Taking long-term Ursodiol therapy with an overdose of 28-30 mg/kg/day can be lethal, which increases the risk of liver damage or death. You may need to do a liver transplantation.  

Ursodeoxycholic acid dosage for Gallstones

The recommended dose of Ursodeoxycholic acid for cholesterol gallstones is 8 to 10 mg/kg/day orally divided into three or four doses. 

Suppose your body weight is 75 kg; you should take Ursodeoxycholic acid 600 mg daily (75 x 8 mg = 600 mg). 

You may take this medicine 600 mg twice or thrice a day. 

Once you start this medicine, it starts dissolving stones at the rate of 1 mm in diameter in one month. 

According to a study, Ursodiol medicine can completely disappear small stones (less than 5 mm) if taken correctly.

The duration of Ursodiol therapy depends on the size of cholesterol gallstones. Still, you must take this medicine for 3 to 4 months. 

Ursodeoxycholic acid dosage for Primary Biliary Cholangitis (PBC)

Primary biliary cholangitis is a more vulnerable medical condition, where liver cells start damaging. So, you need to take Ursodiol 13.5 mg/kg/day. 

The optimum dose of ursodeoxycholic acid would be 900 mg/day for PBC, which can be taken in two-three frequencies. 

At this dose, it can be seen significant improvement in liver function tests. 

The duration of Ursodiol depends on the severity of PBC. You may need to take this medicine for 3 months to 24 months. 

Ursodeoxycholic acid dosage for Primary Sclerosing Cholangitis (PSC)

There is no official use of Ursodeoxycholic acid in PSC. But it can be used if there is no other option. You may need to take Ursodiol at a very high dose of 28-30 mg/kg/day in PSC, which can cause liver damage.  

Ursodeoxycholic acid dosage for Non-Alcoholic Fatty Liver Disease (NAFLD)

Ursodeoxycholic acid medicine does not have official use in fatty liver. But many research studies have shown the efficacy of Ursodiol in NAFLD. 

Your doctor can start this medicine with a minimum to moderate dose (8 to 10 mg/kg/day). 

When to take a Ursodeoxycholic acid tablet? 

Ursodiol absorption increases when you take this medicine with meals because bile acid helps enhance the absorption of Ursodeoxycholic acid medicine. 

Usually, bile acid is generally released in your intestine when you have food. 

It is always recommended to take Ursodiol just after your meal. 

Is Ursodeoxycholic acid safe in pregnancy? 

Intrahepatic cholestasis is very common in pregnancy, where a female has an itching problem. 

This itching is more vulnerable in advanced pregnancy because oestrogen and progesterone are at their peak during this time. 

These increased hormones go to the liver, which causes inflammation and blockage of the internal bile duct of the liver. Eventually, it leads to Intrahepatic Cholestasis. 

This Pregnancy-induced Intrahepatic Cholestasis increases levels of conjugated bilirubin and bile salts. 

These increased bile components get deposited in your skin and cause pruritus.

Currently, there is not any licenced drug for pregnancy-induced intrahepatic cholestasis. 

But ursodiol medicine can be used in pregnancy if clearly needed. 

Although it is not officially used in pregnancy, but it is believed to be safe medicine during pregnancy. 

Some studies suggested the effectiveness and safety of Ursodiol in pregnancy with mild gastrointestinal side effects. 

Who should not take Ursodeoxycholic acid?

Ursodeoxycholic acid (UDCA) is a prescription medicine. So, you are advised to take this medicine only under proper medical supervision.

There are some contraindications with UDCA. So, it would be best if you do not take Ursodiol in certain medical conditions – 

• A complete biliary obstruction, such as biliary atresia
• Obstructive cholestasis
• Pregnancy (can be used if clearly needed) due to lack of safety data of UDCA.

You should immediately stop Ursodiol if you have had hypersensitivity to this medicine and consult your doctor. 

What are the side effects of ursodeoxycholic acid tablets? 

Ursodeoxycholic acid medicine is a well-tolerated and safe medicine. Although, patient compliance is often poor because the dissolution of gallstones is a slow process. So, it does not give you results immediately. 

As far as the concern of its side effects, UDCA does not have any serious or life-threatening side effects. It has negligible or minimal side effects. 

Diarrhoea is most commonly seen in patients with this medicine.  

Abdominal cramps, nausea, vomiting, and pruritus are also reported with UDCA medicine. 

There are no specific long-term side effects of Ursodeoxycholic acid. Still, prolonged uses of UDCA at high doses (28-30 mg/kg/day) can cause liver damage. 

What is Ursodeoxycholic acid brand name in India? 

Ursodeoxycholic acid is very popular with the brand name Udiliv, UDCA, Udihep, Ursopil, etc.  

It is available mainly in two strengths –

• Ursodeoxycholic acid tablets IP150 mg

• Ursodeoxycholic acid tablets IP 300 mg

You may also get Ursodeoxycholic acid in syrup or suspension form like Udcament, Ursolent, Udimarin etc. 

Sometimes, you have been prescribed Ursodeoxycholic acid combination medicines like Ursodeoxycholic acid and Silymarin tablets. It comes in Udibon, Ulyses plus, Ursokem Plus, Urdohep SL tablet. 

What drugs interact with Ursodeoxycholic acid?

There is no significant interaction of Ursodeoxycholic acid with other medicines. Still, some medications may interfere with the absorption of Ursodeoxycholic acid. 

So, it would be best if you avoid Ursodiol together with certain medicines like – 

• Some medicines (Activated charcoal, aluminium-containing antacids, cholestyramine and colestipol) decrease the absorption of Ursodiol.
• Ursodiol increases the absorption of Ciclosporin (an antirheumatic drug)
• Ursodiol decreases the absorption of Ciprofloxacin antibiotic. 

You should take Ursodeoxycholic acid 2 hours before or 2 hours later with these medicines. 

Conclusion 

The Ursodeoxycholic acid tablet is a liver-protective medicine that works with a unique mechanism. 

As we know, its other name is Ursodiol, which is a well-tolerated, effective and safe medicine with negligible side effects. It is licenced to use for Primary Biliary Cholangitis and small gallstones (<5mm) problems.

Many scientific studies have revealed that Ursodeoxycholic acid has some off-label uses. Still, it is used in medical practice if the benefits outweigh the risks. 

Ursodiol is currently used in primary sclerosing cholangitis (PSC), non-alcoholic fatty liver (NAFLD), Post-bariatric surgery, and pregnancy-induced intrahepatic cholangitis under proper medical supervision. 

This was the information about Ursodeoxycholic acid. 

Have questions?

Please ask in below comment box. 

FAQ 

Q 1. Does Ursodeoxycholic acid dissolve gallstones?

Yes. Ursodeoxycholic acid is a gallstone-dissolving drug that works in selected patients with gallstones. 

Q 2. Is Ursodeoxycholic a steroid?

Although Ursodeoxycholic acid has a steroidal ring in its structure that acts as a steroid bile acid, but it is not a steroid medicine like prednisolone. 

Q 3. Can Ursodeoxycholic acid cause weight gain?

Yes. Ursodiol can slightly increase in weight. You may gain some weight if you’re on this medicine. 

Q 4. Where is Ursodeoxycholic acid site of absorption?

Ursodiol is well absorbed from the small intestine and enters your liver through the portal vein. 

Q 5. What is the half-life of Ursodeoxycholic?

Ursodeoxycholic acid stays in your body for a long time because of its longer half-life, approximately 3.5 to 5.8 days. 

Q 6. What would be Ursodeoxycholic acid dose in children? 

According to a research study, the starting recommended dose of ursodeoxycholic acid for infants and children is 5 mg/kg/day in two or three divided doses. 

References – 

1. KD Tripathi. Essentials of Medical Pharmacology, 6^th Jaypee Brothers Medical Publishers; 2013. Chapter 47, Drugs for emesis, reflux and digestive disorders; Gallstones dissolving drugs; Page 649 to 650.
2. Ted George O. Achufusi et al. Ursodeoxycholic Acid. Last updated Feb, 2023.
3. Ursodeoxycholic Acid, Wikipedia
4. SmPC of Ursodeoxycholic Acid (Urdox 300). EMC. Last updated 2018.

Read more posts…