Drug reference

Obeticholic acid

Bile Acid · Liver disorders, primary biliary cholangitis treatment

Bile AcidLiver disorders, primary biliary cholangitis treatmentATC A05AA04

CDSCO approvedSchedule HATC A05AA04

EXCRETION

—

not curated

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

Data available - not known to be harmful. Manufacturer advises to monitor patient parameters more frequently in pregnancy.

FDA category + note

Top interactions

GrazoprevirSevereDatabaseDDInter
TizanidineSevereDatabaseDDInter

Mechanism

Obeticholic acid is a selective farnesoid X receptor agonist which decreases circulating bile acid. It is a nontoxic bile acid believed to reduce liver injury by decreasing hepatic concentrations of more toxic endogenous bile acids. It also acts as a ligand for the nuclear farnesoid X receptor, modulating hepatic inflammation, fibrosis, gluconeogenesis, lipid synthesis, and insulin sensitivity.

Indications

Primary biliary cholangitis in combination with ursodeoxycholic acid when response to ursodeoxycholic acid has been inadequatePrimary biliary cholangitis as monotherapy in patients intolerant of ursodeoxycholic acidPrimary biliary cholangitis (in combination with ursodiol in adults with inadequate response, or as monotherapy in adults unable to tolerate ursodiol)

Dosing

Adult: Initially 5 mg once daily for 6 months, then increased to 10 mg once daily if necessary and if tolerated. Administered by mouth.
Hepatic adjustment: Follow dose reduction and monitoring advice to reduce the risk of serious liver injury in patients with pre-existing moderate or severe hepatic impairment. Adjust dose as the degree of impairment improves during treatment.
Max dose: 10 mg once daily

Pharmacokinetics

Metabolism

Conjugated with glycine or taurine in the liver and secreted into bile. Can be deconjugated by enteric microbiota to obeticholic acid for reabsorption or excretion.

Contraindications

Complete biliary obstruction

Side effects

Common

ArthralgiaConstipationDizzinessFatigueFeverGastrointestinal discomfortOropharyngeal painPalpitationsPeripheral oedemaSkin reactionsSevere pruritus (up to 25% of patients, especially at 10 mg dose)PruritusAbdominal pain and discomfortRashThyroid function abnormalityEczema

Serious

Hepatic failure
Serious liver injury and deaths in patients with pre-existing moderate or severe hepatic impairment
Hepatic decompensation
Liver failure (in incorrectly dosed patients, black box warning)