Actigall (ursodiol)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Ursodiol, a naturally occurring bile acid, is used for its cholelitholytic or anticholestatic action.
Ursodiol, the 7beta-hydroxyepimer of chenodeoxycholic acid (chenodiol), is a naturally occurring, hydrophilic bile acid found in small quantities in normal human bile (normally about 5% of total bile acids) and in the bile of certain animals.
The exact mechanism of action(s) of ursodiol in the dissolution of gallstones has not been fully elucidated, but it has been suggested that the drug suppresses hepatic synthesis and secretion of cholesterol and inhibits intestinal absorption of cholesterol.
Despite aqueous insolubility of cholesterol, in the presence of dihydroxy bile acids cholesterol can be solubilized in aqueous media through the dispersion of cholesterol as liquid crystals or in micelles.
Increases the concentration at which saturation of cholesterol occurs.
Ursodiol may affect the nucleation of cholesterol from bile by altering nucleation factors.
Appears to have small inhibitory effect on synthesis and secretion of endogenous bile acids into bile; does not appear to affect secretion of phospholipids into bile.
Sites of therapeutic action include the liver, bile, and gut lumen.
In patients with gallstones, combined actions of ursodiol change the bile from cholesterol-precipitating to cholesterol-solubilizing, which results in dissolution of cholesterol stones.
Has hepatoprotective effects, which are thought to be principally related to displacement of more hydrophobic and toxic bile acids (e.g., lithocholic acid) that accumulate in the setting of cholestasis. May also protect injured bile duct epithelial cells (cholangiocytes) against toxic effects of bile acids, inhibit apoptosis of hepatocytes, and stimulate bile secretion by hepatocytes and cholangiocytes.
Reduction in serum bilirubin in patients with PBC may be related to improved biliary transport.
Immunomodulatory effects, including reduction in expression of class I antigens on hepatocytes, also may play a role in beneficial effects in patients with PBC.
USES: Ursodiol is used to dissolve certain types of gallstones, to prevent gallstones from forming in obese patients who are losing weight rapidly, and to treat a certain type of liver disease (primary biliary cholangitis). Ursodiol is a bile acid.
Generic name: ursodiol
Pronunciation: (UR-soe-DYE-ol)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Actigall
Indications
The following indications are listed for Actigall:
- Biliary Calculus
- Cholelithiasis Prevention
Also known as: Cholelithiasis, Cholelithiasis Prophylaxis.
Dosing
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Hypersensitivity or intolerance to ursodiol, bile acids, or any component of the formulation.
Complete biliary obstruction.
Do not use for dissolution of calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones.
Do not use in patients with compelling reasons for cholecystectomy, including unremitting cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-gastrointestinal fistula.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Capsules (gallstone dissolution): Abdominal pain, diarrhea, viral infection, headache, dyspepsia, upper respiratory tract infection, nausea, sinusitis, constipation, vomiting, pharyngitis, arthralgia, flatulence, back pain, cough, bronchitis, urinary tract infection, arthritis, myalgia, allergy, cholecystitis, rhinitis, fatigue.
Capsules (prevention of gallstone formation): Constipation, diarrhea, headache, nausea, dizziness, vomiting, upper respiratory tract infection, back pain, viral infection, fatigue, influenza-like symptoms, abdominal pain, musculoskeletal pain, dysmenorrhea, alopecia, sinusitis, flatulence.
Tablets (PBC): Abdominal discomfort, abdominal pain, alopecia, diarrhea, nausea, pruritus, rash.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy have not been established in pediatric patients.
Available data on use of ursodiol in pregnant women have not identified a drug-associated risk of major birth defects, spontaneous abortion, or other adverse maternal or fetal outcomes; most of the reported exposures occurred in the second and third trimesters of pregnancy. Reproduction studies in animals have revealed no adverse embryofetal developmental effects.
The manufacturer of ursodiol capsules states that although fetal harm seems unlikely, the possibility cannot be ruled out and therefore the drug is not recommended for use during pregnancy.
Ursodiol is naturally present in human milk. There are no reports of adverse effects of the drug on breast-fed infants, but the reports are extremely limited. It is not known whether ursodiol affects milk production. The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for ursodiol and any potential adverse effects on the breast-fed infant from the drug or from the underlying maternal condition.
Select dosage with caution.
No substantial differences in safety and efficacy for gallstone dissolution have been observed in geriatric patients relative to younger adults, but increased sensitivity and small differences in efficacy cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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