URSO FORTE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for URSO FORTE (URSO FORTE).
Ursodeoxycholic acid (UDCA) is a hydrophilic bile acid that reduces the concentration of hydrophobic bile acids in bile, thereby decreasing hepatocyte injury. It also has immunomodulatory effects, including inhibition of apoptosis and stimulation of bile flow.
| Metabolism | UDCA undergoes extensive enterohepatic circulation. Conjugation with glycine or taurine in the liver, followed by secretion into bile. Intestinal bacteria deconjugate and dehydroxylate it, forming lithocholic acid, which is partially reabsorbed but largely excreted in feces. |
| Excretion | Biliary (primary); renal (<1% as unchanged drug). Ursodeoxycholic acid undergoes extensive hepatic conjugation and enterohepatic circulation; fecal elimination of metabolites and minor amounts of parent drug. |
| Half-life | Terminal elimination half-life of ursodeoxycholic acid is approximately 3.5–5.8 days (range due to enterohepatic cycling). Clinically, this long half-life supports once-daily dosing and reflects slow turnover in the bile acid pool. |
| Protein binding | Approximately 70–90% bound to serum proteins, primarily albumin. |
| Volume of Distribution | Apparent volume of distribution (Vd/F) is approximately 0.15–0.25 L/kg, indicating distribution primarily within extracellular fluid and bile; limited tissue penetration. |
| Bioavailability | Oral bioavailability is approximately 30–60% after a single dose due to first-pass hepatic extraction; chronic administration achieves steady-state concentrations with absorption efficiency of ~90% of conjugated bile acids. |
| Onset of Action | Oral: Improvement in liver function tests may be observed within 2–4 weeks; complete dissolution of gallstones typically requires 6–24 months of continuous therapy. |
| Duration of Action | Duration of action after oral dose: Bile acid pool enrichment and therapeutic effects persist for weeks after discontinuation. Chronic therapy is required for maintained effects; withdrawal may lead to recurrence of gallstones or worsening of cholestasis within months. |
| Action Class | Hepatoprotectives |
| Brand Substitutes | Fortibile 150 Tablet, Ursomax 150 Tablet, Ursocad 150 Tablet, Udigold 150 Tablet, Urdiogem 150 Tablet |
13-15 mg/kg/day orally in 2-4 divided doses for primary biliary cholangitis; for gallstone dissolution, 8-10 mg/kg/day in 2-3 divided doses.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Use with caution in severe renal impairment (eGFR <30 mL/min) due to limited data; monitor for accumulation. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B: Reduce dose by 50% and titrate based on response. Child-Pugh Class C: Contraindicated due to risk of toxicity. |
| Pediatric use | Not FDA-approved for pediatric use; limited data. Suggested dosing for primary biliary cholangitis or other cholestatic liver diseases: 10-20 mg/kg/day orally in 2-4 divided doses. Maximum 600 mg/day. |
| Geriatric use | No specific dose adjustment required; same as adult dosing. Monitor renal and hepatic function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for URSO FORTE (URSO FORTE).
| Breastfeeding | Ursodeoxycholic acid is excreted into breast milk in low amounts. The M/P ratio is unknown but estimated to be <0.1. It is considered compatible with breastfeeding; however, monitor infant for diarrhea or loose stools. |
| Teratogenic Risk | Ursodeoxycholic acid (URSO FORTE) is not teratogenic in animal studies. Based on human data, no increased risk of major congenital malformations has been observed after first trimester exposure. However, benefit should outweigh risk, especially in severe cholestasis. Second and third trimester use is generally considered safe for maternal liver disease. |
■ FDA Black Box Warning
None.
| Serious Effects |
Absolute: Hypersensitivity to UDCA or bile acids. Relative: Calcified gallstones, non-functioning gallbladder, biliary obstruction, chronic liver disease other than PBC (unless specifically indicated).
| Precautions | 1. Can worsen gallbladder disease (cholecystitis, choledocholithiasis) if gallstones become calcified or if bile duct obstruction is present. 2. Monitor liver function tests; discontinue if worsening occurs. 3. Use with caution in patients with pre-existing liver disease other than PBC. 4. Diarrhea is a common side effect. |
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| Fetal Monitoring | Monitor maternal liver function tests (ALT, AST, ALP, GGT, bilirubin) and bile acids monthly. Assess for pruritus. In pregnancy, fetal monitoring with nonstress test and biophysical profile is recommended for intrahepatic cholestasis of pregnancy. |
| Fertility Effects | Ursodeoxycholic acid does not impair fertility in animals or humans. It may improve fertility in women with cholestasis by reducing bile acid levels and improving liver function. |