Ocaliva and Alcohol/Food Interactions

MONITOR: Coadministration with obeticholic acid may increase the plasma concentrations of drugs that are substrates of the CYP450 1A2 isoenzyme. The mechanism is decreased clearance due to inhibition of CYP450 1A2 activity by obeticholic acid and its glycine and taurine conjugates. When a single 200 mg dose of caffeine (a probe CYP450 1A2 substrate) was administered with obeticholic acid 10 mg once daily, caffeine peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 6% and 42%, respectively.

MANAGEMENT: Caution is advised when obeticholic acid is prescribed with drugs that undergo metabolism by CYP450 1A2, particularly those with a narrow therapeutic range such as theophylline or tizanidine. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever obeticholic acid is added to or withdrawn from therapy.

obeticholic acid - lipids disorder

Patients with primary biliary cholangitis generally exhibit hyperlipidemia characterized by a significant elevation in total cholesterol primarily due to increased levels of high-density lipoprotein-cholesterol (HDL-C). Exercise care when using obeticholic acid in patients with lipids disorder. It is recommended to monitor patients for changes in serum lipid levels during treatment with obeticholic acid. For patients who do not respond to treatment after 1 year at the highest recommended dosage that can be tolerated (maximum of 10 mg once daily), and who experience a reduction in HDL-C, weigh the potential risks against the benefits of continuing treatment.