What medication is used for bile stasis?

October 11, 2025 •

4 min read

Cholestasis, a condition where bile flow from the liver is reduced or blocked, affects about 1 in every 2,500 newborn infants [1.10.1]. Answering the question 'What medication is used for bile stasis?' involves exploring treatments that improve bile flow and manage symptoms.

Quick Summary

Bile stasis, or cholestasis, is treated with medications aimed at improving bile flow and alleviating symptoms. Ursodeoxycholic acid (UDCA) is a primary therapy, while other drugs target complications like severe itching.

Key Points

Primary Treatment: Ursodeoxycholic acid (UDCA) is the first-line medication for many cholestatic conditions, especially Primary Biliary Cholangitis (PBC) [1.2.2, 1.2.3].
Mechanism of UDCA: UDCA works by replacing toxic bile acids, stimulating bile flow, and protecting liver cells from damage [1.3.2, 1.3.4].
Second-Line Therapy: Obeticholic acid (OCA) is a second-line option for PBC patients who don't respond well to UDCA, but it carries a risk of side effects like severe itching [1.2.3, 1.5.4].
Pruritus Management: Severe itching (pruritus) is managed with a stepwise approach, starting with cholestyramine, followed by rifampin, naltrexone, and sertraline [1.4.5, 1.6.1].
Symptom-Specific Drugs: Medications like cholestyramine work by binding bile acids in the gut to prevent their reabsorption, directly addressing a cause of itching [1.4.4, 1.4.5].
Diverse Causes: Bile stasis (cholestasis) can be caused by issues inside the liver (intrahepatic) like PBC or pregnancy, or outside the liver (extrahepatic) like gallstones or tumors [1.9.1, 1.9.2].
Monitoring is Key: Treatments with drugs like rifampin and obeticholic acid require careful monitoring of liver function due to potential hepatotoxicity [1.4.5, 1.5.4].

Understanding Bile Stasis (Cholestasis)

Bile stasis, medically known as cholestasis, is a condition characterized by a decrease or stoppage in the flow of bile from the liver [1.9.3]. Bile is a digestive fluid essential for fat digestion and the removal of waste products like bilirubin from the body [1.10.1]. When bile flow is impaired, these substances can build up in the blood, leading to various symptoms and potential liver damage [1.9.3, 1.9.5].

Cholestasis can be categorized as either intrahepatic (originating within the liver) or extrahepatic (originating outside the liver) [1.9.1, 1.9.2].

Causes of Intrahepatic Cholestasis include:

Primary biliary cholangitis (PBC) [1.2.3]
Intrahepatic cholestasis of pregnancy (ICP) [1.2.2]
Alcoholic liver disease [1.9.1]
Viral hepatitis [1.9.1]
Certain medications [1.9.5]
Genetic defects [1.9.5]

Causes of Extrahepatic Cholestasis include:

Gallstones in the common bile duct [1.9.1]
Bile duct tumors or cysts [1.9.1]
Pancreatitis or pancreatic tumors [1.9.1]
Narrowing of the bile duct (strictures) [1.9.1]

Common symptoms include intense itching (pruritus), jaundice (yellowing of the skin and eyes), dark urine, and light-colored stools [1.9.2]. Diagnosis involves a review of medical history, physical exams, and blood tests to check liver enzyme levels. Imaging tests like ultrasound or MRI may also be used [1.9.2].

Primary Medication: Ursodeoxycholic Acid (UDCA)

Ursodeoxycholic acid (UDCA), also known as ursodiol, is the cornerstone of treatment for many cholestatic liver diseases, particularly Primary Biliary Cholangitis (PBC) [1.2.2, 1.2.3]. It is the only drug approved by the U.S. Food and Drug Administration (FDA) for treating PBC and can significantly delay the progression to liver cirrhosis in early-stage patients [1.2.2].

UDCA is a hydrophilic (water-loving) bile acid that works through several mechanisms [1.3.2]:

Altering the Bile Acid Pool: It displaces more toxic, hydrophobic bile acids, reducing their damaging effects on liver cells (hepatocytes) and bile duct cells (cholangiocytes) [1.3.2].
Stimulating Bile Flow: UDCA promotes the secretion of bile from the liver, a process known as choleresis [1.3.2].
Cytoprotection: It protects liver cells from bile acid-induced damage and apoptosis (programmed cell death) by stabilizing cell membranes and preserving mitochondria [1.3.2, 1.3.4].
Immunomodulation: It can reduce the aberrant expression of certain antigens on liver cells that can trigger immune-mediated destruction [1.3.2].

The recommended dosage for PBC is typically 13–15 mg/kg/day [1.2.3]. UDCA is also used off-label for other conditions like intrahepatic cholestasis of pregnancy and primary sclerosing cholangitis (PSC), although its efficacy in PSC is debated [1.2.2].

Second-Line and Symptomatic Treatments

Not all patients respond adequately to UDCA. For these individuals, and for managing specific symptoms like pruritus, other medications are used.

Obeticholic Acid (OCA)

For PBC patients who have an inadequate response to or cannot tolerate UDCA, Obeticholic Acid (OCA) is a second-line option [1.2.3]. OCA is a farnesoid X receptor (FXR) agonist that works by inhibiting bile acid synthesis [1.2.3, 1.5.3]. Clinical trials have shown that OCA, often in combination with UDCA, can significantly improve biochemical markers [1.2.3, 1.5.1]. However, a common side effect is pruritus, which can be severe [1.2.3, 1.5.4]. The FDA has also noted a risk of serious liver injury in some patients, requiring careful monitoring [1.5.4].

Medications for Cholestatic Pruritus

Intense itching is one of the most debilitating symptoms of cholestasis. The management often follows a stepwise approach [1.4.5, 1.6.1].

Cholestyramine: This is a first-line therapy for cholestatic pruritus [1.2.3, 1.4.4]. It's a bile acid sequestrant, a resin that binds to bile acids in the intestine, preventing their reabsorption and increasing their fecal excretion [1.4.4, 1.4.5]. It must be taken 4 to 6 hours apart from other medications, like UDCA, as it can interfere with their absorption [1.2.3, 1.4.4].
Rifampin (Rifampicin): Recommended as a second-line agent, rifampin is an enzyme inducer that can alleviate pruritus [1.2.3, 1.6.1]. Its mechanism is thought to involve the pregnane X receptor (PXR), which helps enhance bile acid detoxification [1.4.5, 1.6.5]. Due to the risk of hepatotoxicity, close monitoring of liver function is essential [1.4.5, 1.6.3].
Naltrexone: This oral opioid receptor antagonist is a third-line option [1.2.3, 1.7.1]. The rationale is that cholestasis may increase the body's natural opioidergic tone, contributing to the sensation of itch [1.7.4]. Naltrexone can be effective but may precipitate an opioid withdrawal-like reaction in some patients [1.4.5, 1.7.3].
Sertraline: A selective serotonin reuptake inhibitor (SSRI), sertraline is considered a fourth-line therapy [1.4.5, 1.8.4]. It is thought to modify the central perception of itch [1.8.1, 1.8.4]. Studies have shown it can be an effective and well-tolerated treatment for pruritus due to chronic liver disease [1.8.1].

Medication Comparison Table


Medication	Primary Use in Bile Stasis	Mechanism of Action	Common Side Effects
Ursodeoxycholic Acid	Primary treatment for PBC; improves bile flow	Displaces toxic bile acids, stimulates bile secretion, protects liver cells [1.3.2]	Generally well-tolerated; may cause abdominal discomfort [1.2.2]
Obeticholic Acid	Second-line for PBC (inadequate UDCA response)	FXR agonist; inhibits bile acid synthesis [1.2.3, 1.5.4]	Pruritus, fatigue, potential for liver injury [1.2.3, 1.5.4]
Cholestyramine	First-line for pruritus (itching)	Binds bile acids in the intestine, preventing reabsorption [1.4.4, 1.4.5]	Unpleasant taste, constipation, bloating [1.4.4]
Rifampin	Second-line for pruritus	PXR agonist; enhances bile acid detoxification [1.4.5]	Nausea, risk of hepatotoxicity [1.4.5]
Naltrexone	Third-line for pruritus	Opioid receptor antagonist; modulates central itch perception [1.7.1, 1.7.4]	Opioid withdrawal-like symptoms, nausea [1.4.5, 1.7.5]
Sertraline	Fourth-line for pruritus	SSRI; modifies central perception of itch [1.8.1, 1.8.4]	Nausea, dizziness, insomnia [1.8.4, 1.8.5]

Conclusion

The management of bile stasis is multifaceted, focusing on treating the underlying cause, improving bile flow, and relieving symptoms. Ursodeoxycholic acid (UDCA) stands out as the primary medication for many chronic cholestatic conditions like PBC, working to protect the liver and slow disease progression. For patients with an insufficient response, obeticholic acid offers an alternative, though it requires careful monitoring. Symptomatic treatment, especially for the pervasive issue of pruritus, involves a tiered approach starting with cholestyramine and escalating to drugs like rifampin, naltrexone, and sertraline. The choice of medication depends on the specific type of cholestasis, the patient's response to initial therapy, and the severity of their symptoms.

Disclaimer: This article is for informational purposes only and does not constitute medical advice. Consult with a qualified healthcare professional for any health concerns or before making any decisions related to your health or treatment.

Authoritative Link: National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)

Frequently Asked Questions

The main medication used for many forms of bile stasis, particularly primary biliary cholangitis (PBC), is ursodeoxycholic acid (UDCA), also known as ursodiol [1.2.2, 1.2.3].

UDCA is a hydrophilic bile acid that helps by displacing more toxic bile acids, stimulating bile flow from the liver, and protecting liver cells from damage and apoptosis (cell death) [1.3.2, 1.3.4].

Yes, for patients with primary biliary cholangitis who do not respond adequately to UDCA, obeticholic acid (OCA) is a second-line treatment option. It works by inhibiting the synthesis of bile acids [1.2.3, 1.5.4].

The itching (pruritus) from cholestasis is often treated first with cholestyramine, a resin that binds bile acids in the intestine. If that is ineffective, other options include rifampin, naltrexone, and sertraline [1.2.3, 1.4.4, 1.6.1].

Cholestyramine is a bile acid sequestrant. It's a powder that binds to bile acids in your intestines, preventing them from being reabsorbed into the body. This helps reduce the itching associated with high levels of bile acids in the blood [1.4.4, 1.4.5].

Yes, intrahepatic cholestasis of pregnancy (ICP) is a condition that occurs in the second or third trimester. It impairs the release of bile from the liver and typically resolves after delivery [1.2.1, 1.10.2].

Intrahepatic cholestasis originates from problems within the liver, such as liver disease, genetic defects, or pregnancy [1.9.1]. Extrahepatic cholestasis is caused by a physical blockage of the bile ducts outside the liver, such as from a gallstone or tumor [1.9.1, 1.9.2].