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Obeticholic Acid Dosage

Medically reviewed by Drugs.com. Last updated on Mar 4, 2020.

Applies to the following strengths: 5 mg; 10 mg

Usual Adult Dose for Biliary Cirrhosis

Initial dose: 5 mg orally once a day
Maintenance dose: 5 mg orally once a day; if adequate reduction in alkaline phosphatase (ALP) and/or total bilirubin is not achieved after 3 months, increase the dosage to 10 mg orally once a day
Maximum dose: 10 mg/day

Comments:
-This drug was approved via accelerated approval process due to ALP reductions; an improvement in survival or disease-related symptoms was not established.
-Patients and prescribers should note that continued approval may be contingent upon verification and clinical benefit in additional confirmatory trials.
-Healthcare providers should determine the Child-Pugh classification in any patient with suspected ascites prior to starting treatment.

Uses: For the treatment of primary biliary cholangitis:
-As monotherapy in adults unable to tolerate ursodeoxycholic acid (UDCA)
-In combination with UDCA in adults with an inadequate response to UDCA

Renal Dose Adjustments

No adjustment recommended.

Liver Dose Adjustments

Mild liver dysfunction (Child Pugh Class A): No adjustment recommended.
Moderate to severe liver dysfunction (Child Pugh Class B and C):
-Initial dose: 5 mg orally once a week
-Maintenance dose: 5 mg orally once a week; if adequate reduction in ALP and/or total bilirubin is not achieved after 3 months, increase the dosage to 5 mg 2 times a week (at least 3 days apart), and subsequently to 10 mg 2 times a week (at least 3 days apart) depending on response and tolerability
-Maximum dose: 10 mg/day

Liver Dysfunction During Treatment:
-Patients with laboratory/clinical evidence of liver dysfunction: Interrupt treatment and monitor the patient's liver function.
-Patients with liver function returning to baseline: The risks versus benefits of restarting treatment should be considered; if this drug is restarted, the initial dose should be determined by the patient's Child-Pugh classification.
-Patients with clinically significant liver-related adverse reactions: Providers should consider treatment discontinuation.

IF INTOLERANT PRURITUS OCCURS DURING TREATMENT:
Mild liver dysfunction (Child-Pugh Class A):
-Add an antihistamine or bile acid binding resin
-Reduce the dose to 5 mg orally every other day (patients intolerant to a daily dose of 5 mg) or 5 mg orally once a day (patients intolerant to a daily dose of 10 mg).
-Temporarily stop treatment for up to 2 weeks, then restart at a lower dose.
-Consider discontinuation in patients with continued persistent, intolerable pruritus.

Mild to moderate liver dysfunction (Child-Pugh Class B or C) OR decompensated cirrhotic patients:
-Reduce the dose to 5 mg orally once a week (patients intolerant to a dose of 5 mg 2 times a week) OR 10 mg orally once a week (patients intolerant to a dose of 10 mg 2 times a week).
-Temporarily stop treatment for up to 2 weeks, then restart at a lower dose, with gradual increases to achieve optimal response (up to 10 mg orally 2 times a week).
-Consider discontinuation in patients with continued persistent, intolerable pruritus.

Comments:
-Patients with reduced/interrupted doses should receive dose titrations based on biochemical response and tolerability; adjustments should be made based on Child-Pugh classification.
-Patients should be monitored for the occurrence of liver-related adverse reactions.
-The potential risks should be weighed against benefits in patients with a history of clinically significant liver-related adverse reactions.

Dose Adjustments

Patients should be regularly monitored for response, disease progression, tolerability, and Child-Pugh classification should be re-evaluated to determine proper dosages are used.

Patients with Intolerant Pruritus:
-Add an antihistamine or bile acid binding resin
-Reduce the dosage to 5 mg every other day (patients intolerant to a daily dose of 5 mg) or 5 mg orally once a day (patients intolerant to a daily dose of 10 mg)
-Temporarily stop treatment for up to 2 weeks, then restart at a lower dose
-Consider discontinuation in patients with continued persistent, intolerable pruritus

PATIENTS WITH A PRIOR DECOMPENSATION EVENT:
-Initial dose: 5 mg orally once a week
-Maintenance dose: 5 mg orally once a week; if adequate reduction in ALP and/or total bilirubin is not achieved after 3 months, increase the dosage to 5 mg 2 times a week (at least 3 days apart), and subsequently to 10 mg 2 times a week (at least 3 days apart) depending on response and tolerability
-Maximum dose: 10 mg/day

If Intolerant Pruritus Occurs During Treatment:
-Add an antihistamine or bile acid resin
-Temporarily stop treatment for up to 2 weeks, then restart at a lower dose
-Consider discontinuation in patients with continued persistent, intolerable pruritus

Comment: Prior decompensation events include new/worsening jaundice, spontaneous bacterial peritonitis, and/or variceal bleeding.

Precautions

US BOXED WARNINGS:
HEPATIC DECOMPENSATION AND FAILURE IN INCORRECTLY DOSED PRIMARY BILIARY CHOLANGITIS (PBC) PATIENTS WITH CHILD-PUGH CLASS B OR C DECOMPENSATED CIRRHOSIS:
-In postmarketing reports, hepatic decompensation and failure, in some cases fatal, have been reported in patients with PBC with decompensated cirrhosis or Child-Pugh Class B or C liver dysfunction when this drug was dosed more frequently than recommended.
-The recommended starting dose of this drug is 5 mg once weekly for patients with Child-Pugh Class B or C liver dysfunction or a prior decompensation event.

CONTRAINDICATIONS: Patients with complete biliary obstruction

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:
-This drug may be taken with or without food.
-Patients taking concomitant bile acid binding resins should allow at least 4 to 6 hours before or after taking the bile acid resin, or they should separate administration of this drug as great an interval as possible.

Storage requirements:
-The manufacturer product information should be consulted.

General:
-This drug is indicated for patients who have not achieved adequate biochemical response to an appropriate response to UDCA for at least 1 year or are intolerant of UDCA.
-Approval of this drug is based on a reduction in ALP levels; improvements in survival/disease-related symptoms has not been established.
-The dose should be increased to 10 mg/day to achieve optimal response.

Monitoring:
-HEPATIC: Periodic liver function tests
-METABOLIC: Periodic HDL levels

Patient advice:
-Instruct patients to immediately report any signs/symptoms of severe pruritus, hepatitis/jaundice, or hypersensitivity reactions.
-Patients should be advised to speak to a healthcare provider if they become pregnant, intend to become pregnant, or are breastfeeding.
-Patients should be advised to report all concurrent prescription and nonprescription medications or herbal products they are taking.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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