Dosing and uses of Actigall, Urso Forte (ursodiol)
Adult dosage forms and strengths
capsules
- 300mg
tablets
- 250mg
- 500mg
Gallstone Dissolution
8-10 mg/kg/d PO divided q8-12hr PO; not to exceed 300 mg/dose
Maintenance: 250 mg PO HS x6 months
Primary Biliary Cirrhosis
13-15 mg/kg/d PO divided PO with food
Cystic Fibrosis Liver Disease (Orphan)
Indicated for treatment of cystic fibrosis liver disease
Orphan indication sponsor
- Asklepion Pharmaceuticals, LLC; 5200 Maryland Way; Brentwood, TN 37027
Pediatric dosage forms and strengths
capsules
- 300mg
tablets
- 250mg
- 500mg
Biliary Atresia (Off-Label)
10-15 mg/kg PO qDay
Actigall, Urso Forte (ursodiol) adverse (side) effects
>10%
Headache
Dizziness
Diarrhea
Dyspepsia
Nausea/vomiting
Back pain
Upper respiratory tract infection
1-10%
Alopecia
Rash
Hyperglycemia
Flatulence
Peptic ulcer
Urinary tract infection
Leukopenia
Thrombocytopenia
Cholecystitis
>1%
Fatigue
Abdominal pain
Thrombocytopenia
Pruritus
Angioedema
Peripheral edema
Biliary pain
Postmarketing Reports
Hepatobiliary disorders: Jaundice (or aggravation of pre-existing jaundice)
Abnormal laboratory tests: Increased ALT, AST, alkaline phosphatase, bilirubin, gamma-Gt
Warnings
Contraindications
Hypersensitivity
Gallstone complication requiring surgery
Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
Calcified gallstones, bile acid allergy, chronic hepatic disease
Billiary gastrointestinal fistula
Patients requiring cholecystectomy
Cautions
Only use in radiolucent, non calcified, high cholesterol content gallstone
Chronic liver disease
Liver function tests (gamma-GT, alkaline phosphatase, AST, ALT) and bilirubin levels should be monitored q3months x3 months after start of therapy, and q6months thereafter
Gallbladder stone dissolution may take several months
50% of cases have stone recurrence in 5 yr
Pregnancy and lactation
Pregnancy category: B
Lactation: unknown if excreted in breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Actigall, Urso Forte (ursodiol)
Mechanism of action
Naturally-occurring bile acid; reduces cholesterol secretion from the liver; reduces the fractional reabsorption of cholesterol by the intestines.
Absorption
Bioavailability: 90%
Onset: Initial response for gallstone dissolution is 3-6 months
Distribution
Protein Bound: 70%
Metabolism
Taken up rapidly by the liver, conjugated with glycine or taurine, and excreted in the bile
Nonabsorbed ursodiol passes into the colon where it is 7-dehydroxylated to lithocholic acid (an intermediary compound, sometimes formed, is called chenodiol); chenodiol is then dehydroxylated to lithocholic acid
Metabolites: Glyco-ursodeoxycholic acid, tauro-ursodeoxycholic acid, 7-keto-lithocholic acid (inactive); lithocholic acid (inactive) is formed from the 7-hydroxylation of ursodiol and chenodiol; a small portion is metabolized to sulfated lithocholic acid conjugates which are excreted in bile & eliminated in feces
Elimination
Excretion: Mainly in feces
