Generic Name and Formulations:
Obeticholic acid 5mg, 10mg; tabs.
Indications for OCALIVA:
Treatment of primary biliary cholangitis in combination with ursodeoxycholic acid (UDCA) in adults with inadequate response to UDCA, or as monotherapy in adults unable to tolerate UDCA.
Initially 5mg once daily. Increase to 10mg once daily if inadequate reduction in ALP and/or total bilirubin after 3 months and tolerated the drug; max 10mg once daily. Moderate or severe hepatic impairment: initially 5mg once weekly; increase to 5mg twice weekly (≥3 days apart) then to 10mg twice weekly (≥3 days apart) if inadequate reduction in ALP and/or total bilirubin after 3 months and tolerated the drug. Intolerable pruritus: consider adding an antihistamine or bile acid binding resin; or reducing dose to 5mg every other day (if intolerant to 5mg daily) or 5mg once daily (if intolerant to 10mg daily); or temporarily interrupt for up to 2 weeks then restart at lower dose. Increase dose to 10mg once daily as tolerated for optimal response.
Complete biliary obstruction.
Discontinue if intolerable pruritus persists or complete biliary obstruction develops. Monitor for elevations in liver biochemical tests and liver-related adverse effects. Monitor for changes in serum lipid levels. If unresponsive after 1 year of treatment at max tolerable dose (10mg once daily) and experienced HDL-C reduction, reevaluate. Pregnancy. Nursing mothers.
Separate dosing by ≥4hrs or at greatest possible interval with bile acid binding resins (eg, cholestyramine, colestipol, colesevelam). Concomitant warfarin: monitor INR and adjust dose as needed. Concomitant CYP1A2 substrates with narrow therapeutic index (eg, theophylline, tizanidine); monitor.
Farnesoid X receptor (FXR) agonist.
Pruritus, fatigue, abdominal pain/discomfort, rash, oropharyngeal pain, dizziness, constipation, arthralgia, thyroid function abnormality, eczema; liver-related effects, HDL-C reduction.