• Primary biliary cholangitis (PBC) in patients either without cirrhosis or with compensated cirrhosis and no evidence of portal hypertension (to be used either in combination with ursodeoxycholic acid [UDCA] if experienced an inadequate response to UDCA or as monotherapy if unable to tolerate UDCA).

Contraindicated in:

• Complete biliary obstruction.
• Decompensated cirrhosis (Child-Pugh Class B or C hepatic impairment) or a prior episode of hepatic decompensation
• Compensated cirrhosis with evidence of portal hypertension.

Use Cautiously in:

• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Safety and effectiveness not established in children.

CV: palpitations, peripheral edema.

Derm: pruritus, eczema, rash.

EENT: oropharyngeal pain.

Endo: ↓high-density lipoprotein cholesterol, hypothyroidism.

GI: HEPATIC DECOMPENSATION/FAILURE, VARICEAL BLEEDING, abdominal pain, ascites (worsening), constipation, ↑ liver enzymes, jaundice.

MS: arthralgia.

Neuro: ENCEPHALOPATHY, fatigue, dizziness.

Misc: fever.

Drug-Drug:

• Bile acid resins, including cholestyramine, colesevelam, and colestipol may ↓ absorption; give obeticholic acid 4 hr before or after bile acid resins.
• May ↓ efficacy of warfarin.
• May ↑ levels and risk of toxicity of CYP1A2 substrates, including theophylline and tizanidine.
• Cyclosporine may exacerbate accumulation of conjugated bile salts; avoid concurrent use.

• Tablets: 5 mg; 10 mg;

• PO (Adults): 5 mg once daily for 3 mo; if adequate reduction in alkaline phosphatase and/or total bilirubin not achieved and tolerating medication, ↑ dose to 10 mg once daily.

Ocaliva

• Stimulates farnesoid X receptor (FXR) in the liver and intestine, resulting in decreased synthesis of bile acids from cholesterol and increased transport of bile acids out of the hepatocytes. Overall, the result is a reduction in intracellular hepatocyte concentrations of bile acids.

• Reduction in alkaline phosphatase and total bilirubin concentrations.

Therapeutic Classification: n/a

Pharmacologic Classification: farnesoid X receptor agonists

Absorption: Rapidly absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: >99%.

Metabolism/Excretion: Conjugated in the liver to glycine and tauro conjugates of obeticholic acid (both are active metabolites) that undergo enterohepatic recirculation and conversion by intestinal microbiota back to obeticholic acid that is reabsorbed or excreted in feces. Minimal excretion in urine.

Half-life: Unknown.

(plasma concentrations)

• Instruct patient to take medication as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
• Advise patient to notify health care professional if signs and symptoms of disease progression or worsening liver function (stomach-area swelling from build-up of fluid; yellowing of skin or whites of eyes; black, tarry, or bloody stools; coughing up or vomiting blood, or coffee grounds vomit; mental changes such as confusion, sleepier than usual or harder to wake up, slurred speech, mood swings, changes in personality), complete biliary obstruction, severe or persistent signs of impaired health (nausea, vomiting, abdominal pain, diarrhea, weight loss, fever and chills, worsening or new fatigue, weakness, loss of appetite, dehydration) occur.
• Inform patient of potential for itching. Advise patient to notify health care professional if severe itching causing discomfort, problems sleeping, or interference with daily activities occurs.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.
• Emphasize need for regular laboratory tests to monitor liver function.

oh-bet-i-KOE-lik AS-id

NDC Code^*

• 69516- Intercept Pharmaceuticals Inc
  • 69516-005- Ocaliva
    • 69516-005-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (69516-005-30)

• 69516- Intercept Pharmaceuticals Inc
  • 69516-010- Ocaliva
    • 69516-010-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (69516-010-30)