Actigall - General Information
Actigall is an epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.
Pharmacology of Actigall
Ursodiol (also known as ursodeoxycholic acid) is one of the secondary bile acids, which are metabolic byproducts of intestinal bacteria. Primary bile acids are produced by the liver and stored in the gall bladder. When secreted into the colon, primary bile acids can be metabolized into secondary bile acids by intestinal bacteria. Primary and secondary bile acids help the body digest fats. Actigall helps regulate cholesterol by reducing the rate at which the intestine absorbs cholesterol molecules while breaking up micelles containing cholesterol. Because of this property, ursodeoxycholic acid is used to treat gall stones non-surgically.
Actigall for patients
Bile acid sequestering agents such as cholestyramine and colestipol may interfere with the action of Ursodiol by reducing its absorption. Aluminum-based antacids have been shown to adsorb bile acids in vitro and may be expected to interfere with Ursodiol 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 Ursodiol.
- Ursodiol will not dissolve calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones. Hence, patients with such stones are not candidates for Ursodiol therapy.
- Patients with compelling reasons for cholecystectomy including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-gastrointestinal fistula are not candidates for Ursodiol therapy.
- Allergy to bile acids.
Additional information about Actigall
Actigall Indication: Used to treat gall stones non-surgically.
Mechanism Of Action: Actigall reduces elevated liver enzyme levels by facilitating bile flow through the liver and protecting liver cells.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ursodeoxycholic acid
Synonyms: (3alpha,5beta,7beta)-3,7-dihydroxycholan-24-oic acid; 3,7-Dihydroxycholan-24-oic acid; 3-alpha,7-beta-Dihydroxy-5-beta-cholanoic acid; 3-alpha,7-beta-Dihydroxycholanic acid; 3-alpha,7-beta-Dioxycholanic acid; 3alpha,7beta-Dihydroxy-5beta-cholan-24-oic acid; 5beta-Cholan-24-oic acid-3alpha,7beta-diol; 7-beta-Hydroxylithocholic acid; 7beta-Hydroxylithocholic acid; Acide ursodesoxycholique [inn-french]; Acido ursodeossicolico [italian]; Acido ursodeoxicolico [inn-spanish]; Acidum ursodeoxycholicum [inn-latin]; Chenodeoxycholic acid; Iso-ursodeoxycholic acid; UDCS; Ursodesoxycholic acid; Ursodiol
Drug Category: Cholagogues and Choleretics
Drug Type: Small Molecule; Approved; Investigational
Absorption: Not Available
Toxicity (Overdose): Neither accidental nor intentional overdosing with ursodeoxycholic acid has been reported. Doses of ursodeoxycholic acid in the range of 16-20 mg/kg/day have been tolerated for 6-37 months without symptoms by 7 patients. The LD50 for ursodeoxycholic acid in rats is over 5000 mg/kg given over 7-10 days and over 7500 mg/kg for mice. The most likely manifestation of severe overdose with ursodeoxycholic acid would probably be diarrhea, which should be treated symptomatically.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Actigall: Tablet Oral
Chemical IUPAC Name: (4R)-4-[(3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
Chemical Formula: C24H40O4
Ursodeoxycholic acid on Wikipedia: https://en.wikipedia.org/wiki/Ursodiol
Organisms Affected: Humans and other mammals