What is Actigall (ursodiol)?

Actigall (ursodiol) is a naturally-occurring bile acid made by the liver in humans and is secreted in small quantities into bile and is used to dissolve and prevent cholesterol gallstones and to treat primary biliary cirrhosis, a disease of the liver.

Actigall blocks the enzyme in the liver that produces cholesterol and thereby decreases production of cholesterol by the liver and the amount of cholesterol in bile. It also reduces the absorption of cholesterol from the intestine. By decreasing the concentration of cholesterol in bile, Actigall prevents the formation and promotes the dissolution of cholesterol-containing gallstones. The mechanism by which it acts in primary biliary cirrhosis is not clear. 

Common side effects of Actigall include:

Serious side effects of Actigall include serious allergic reactions and reduced concentration of white blood cells.

Drug interactions of Actigall include aluminum containing antacids, which reduce the absorption of Actigall and therefore reduce its action, such as:

The following drugs may counteract the effects of Actigall by increasing cholesterol secretion by the liver and the risk for gallstone formation:

There are no adequate studies of Actigall in pregnant women. It is unknown if Actigall is secreted in breast milk. Consult your doctor before breastfeeding.

What are the important side effects of Actigall (ursodiol)?

The most common side effects are:

Serious allergic reactions and reduced concentration of white blood cells also have occurred.

Actigall (ursodiol) side effects list for healthcare professionals

The nature and frequency of adverse experiences were similar across all groups.

The following tables provide comprehensive listings of the adverse experiences reported that occurred with a 5% incidence level:

GALLSTONE DISSOLUTION

  Ursodiol 8 -10 mg/kg/day
(N = 155)
Placebo
(N= 159)
N % N %
Body as a Whole
  Allergy 8 (5.2) 7 (4.4)
  Chest Pain 5 (3.2) 10 (6.3)
  Fatigue 7 (4.5) 8 (5.0)
  Infection Viral 30 (19.4) 41 (25.8)
Digestive System
  Abdominal Pain 67 (43.2) 70 (44.0)
  Cholecystitis 8 (5.2) 7 (4.4)
  Constipation 15 (9.7) 14 (8.8)
  Diarrhea 42 (27.1) 34 (21.4)
  Dyspepsia 26 (16.8) 18 (11.3)
  Flatulence 12 (7.7) 12 (7.5)
  Gastrointestinal Disorder 6 (3.9) 8 (5.0)
  Nausea 22 (14.2) 27 (17.0)
  Vomiting 15 (9.7) 11 (6.9)
Musculoskeletal System
  Arthralgia 12 (7.7) 24 (15.1)
  Arthritis 9 (5.8) 4 (2.5)
  Back Pain 11 (7.1) 18 (11.3)
  Myalgia 9 (5.8) 9 (5.7)
Nervous System
  Headache 28 (18.1) 34 (21.4)
  Insomnia 3 (1.9) 8 (5.0)
Respiratory System
  Bronchitis 10 (6.5) 6 (3.8)
  Coughing 11 (7.1) 7 (4.4)
  Pharyngitis 13 (8.4) 5 (3.1)
  Rhinitis 8 (5.2) 11 (6.9)
  Sinusitis 17 (11.0) 18 (11.3)
  Upper Respiratory Tract Infection 24 (15.5) 21 (13.2)
Urogenital System
  Urinary Tract Infection 10 (6.5) 7 (4.4)
GALLSTONE PREVENTION
  Actigall 600 mg
(N = 322)
Placebo
(N = 325)
N (%) N (%)
Body as a Whole
  Fatigue 25 (7.8) 33 (10.2)
  Infection Viral 29 (9.0) 29 (8.9)
  Influenza-like Symptoms 21 (6.5) 19 (5.8)
Digestive System
  Abdominal Pain 20 (6.2) 39 (12.0)
  Constipation 85 (26.4) 72 (22.2)
  Diarrhea 81 (25.2) 68 (20.9)
  Flatulence 15 (4.7) 24 (7.4)
  Nausea 56 (17.4) 43 (13.2)
  Vomiting 44 (13.7) 44 (13.5)
Musculoskeletal System
  Back Pain 38 (11.8) 21 (6.5)
  Musculoskeletal Pain 19 (5.9) 15 (4.6)
Nervous System
  Dizziness 53 (16.5) 42 (12.9)
  Headache 80 (24.8) 78 (24.0)
Respiratory System
  Pharyngitis 10 (3.1) 19 (5.8)
  Sinusitis 17 (5.3) 18 (5.5)
Upper Respiratory
  Tract Infection 40 (12.4) 35 (10.8)
Skin and Appendages
  Alopecia 17 (5.3) 8 (2.5)
Urogenital System
  Dysmenorrhea 18 (5.6) 19 (5.8)

What drugs interact with Actigall (ursodiol)?

Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Actigall by reducing its absorption. Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with Actigall in the same manner as the bile acid sequestering agents. Estrogens, oral contraceptives, and clofibrate (and perhaps other lipid-lowering drugs) increase hepatic cholesterol secretion, and encourage cholesterol gallstone formation and hence may counteract the effectiveness of Actigall.

Summary

Actigall (ursodiol) is a naturally-occurring bile acid made by the liver in humans and is secreted in small quantities into bile and is used to dissolve and prevent cholesterol gallstones and to treat primary biliary cirrhosis, a disease of the liver. Common side effects of Actigall include rash, itching, nausea, vomiting, stomach pain, back pain, constipation, diarrhea, and hair loss. Serious side effects of Actigall include serious allergic reactions and reduced concentration of white blood cells. Drug interactions of Actigall include aluminum containing antacids, cholestyramine and colestipol; estrogens; oral contraceptives; clofibrate; and potentially other cholesterol reducing drugs. There are no adequate studies of Actigall in pregnant women. It is unknown if Actigall is secreted in breast milk. Consult your doctor before breastfeeding.

Treatment & Diagnosis

Medications & Supplements

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Medically Reviewed on 4/15/2020
References
FDA Prescribing Information
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