What is Ocaliva?
Ocaliva is a prescription medicine used to treat primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults who have not responded well enough to UDCA, or alone in adults who cannot tolerate UDCA.
It is not known if taking Ocaliva will improve your chance of survival or improve your symptoms of PBC.
It is not known if Ocaliva is safe and effective in children.
OCALIVA is a farnesoid X receptor (FXR) agonist. Chemically, obeticholic acid is 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid. It is a white to off-white powder. It is soluble in methanol, acetone and ethyl acetate. Its solubility in water is pH dependent. It is slightly soluble at low pH and very soluble at high pH. Its chemical formula is C26H44O4, the molecular weight is 420.63 g/mol, and the chemical structure is:
OCALIVA tablets are supplied in 5 mg and 10 mg strengths for oral administration. Each tablet contains obeticholic acid as the active ingredient and the following inactive ingredients: microcrystalline cellulose, sodium starch glycolate, and magnesium stearate. The film coating is Opadry II (Yellow) containing polyvinyl alcohol-part hydrolyzed, titanium dioxide, macrogol (polyethylene glycol 3350), talc, and iron oxide yellow.
Mechanism of Action
Obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine. FXR is a key regulator of bile acid, inflammatory, fibrotic, and metabolic pathways. FXR activation decreases the intracellular hepatocyte concentrations of bile acids by suppressing de novo synthesis from cholesterol as well as by increased transport of bile acids out of the hepatocytes. These mechanisms limit the overall size of the circulating bile acid pool while promoting choleresis, thus reducing hepatic exposure to bile acids.
What is the most important information I should know about Ocaliva?
If you have primary biliary cholangitis (PBC) with advanced cirrhosis, you may need a lower dose of Ocaliva.
- Before you start Ocaliva, and during your treatment with Ocaliva, your healthcare provider will do tests to check your liver. These tests will help your healthcare provider decide how much Ocaliva you should take and how often you should take it.
- If you have worsening liver problems, your dose of Ocaliva may be changed, stopped for a period of time, or stopped completely by your healthcare provider.
Ocaliva can cause serious side effects including:
Worsening of liver problems, liver failure, in some cases leading to death, have happened in people with PBC with advanced liver cirrhosis when Ocaliva was taken more often than recommended.
- Tell your healthcare provider right away if you have any of the following symptoms of worsening liver problems during treatment with Ocaliva:
- swelling of your stomach-area from a build-up of fluid
- yellowing of your skin or the whites of your eyes
- black, tarry, or bloody stools
- coughing up or vomiting blood, or your vomit looks like “coffee grounds”
- mental changes such as confusion, sleepier than usual or harder to wake up, slurred speech, mood swings, or changes in personality
- Tell your healthcare provider right away if you have any of the following symptoms during treatment with Ocaliva and they are severe or do not go away:
Who should not take Ocaliva?
Do not take Ocaliva if you:
- have a complete blockage of the bile ducts in your liver or gall bladder.
What should I tell my healthcare provider before taking Ocaliva?
Before taking Ocaliva, tell your healthcare provider about all of your medical conditions, including if you:
- are pregnant or plan to become pregnant. It is not known if Ocaliva will harm your unborn baby.
- are breastfeeding or plan to breastfeed. It is not known if Ocaliva passes into your breast milk. Talk with your healthcare provider about the best way to feed your baby if you take Ocaliva.
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Ocaliva can affect the way certain medicines work. Certain other medicines may affect the way Ocaliva works.
How should I take Ocaliva?
- Take Ocaliva exactly as your healthcare provider tells you to.
- Do not take more Ocaliva than your healthcare provider tells you to.
- Take Ocaliva with or without food.
- If you take a bile acid binding resin, take Ocaliva at least 4 hours before or 4 hours after you take your bile acid binding resin. If this is not possible, space the time between taking Ocaliva and your bile acid binding resin as far apart as possible.
- If you take too much Ocaliva, call your healthcare provider or get emergency medical help right away.
What are the possible side effects of Ocaliva?
Ocaliva can cause serious side effects, including:
- See “What is the most important information I should know about Ocaliva?”
- Severe itching (pruritus). Itching is a common side effect of Ocaliva and can sometimes become severe (intense itching or itching over much of your body). Severe itching can cause discomfort, problems sleeping, and problems doing daily activities and usually needs to be treated. Tell your healthcare provider if you get severe itching or if your itching gets worse.
- Lower HDL-C (“good” cholesterol). Ocaliva can lower high levels of HDL-C. Your healthcare provider will check your cholesterol levels during your treatment with Ocaliva.
The most common side effects of Ocaliva include:
- stomach pain and discomfort
- joint pain
- mouth and throat pain
- swelling in your hands, ankles, or feet
- fast or irregular heartbeat
- changes in how your thyroid gland works
- dryness, irritation, redness, crusting or drainage of the skin (eczema)
These are not all the possible side effects of Ocaliva. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
General information about the safe and effective use of Ocaliva
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use Ocaliva for a condition for which it was not prescribed. Do not give Ocaliva to other people, even if they have the same symptoms that you have. It may harm them. You can ask your pharmacist or healthcare provider for information about Ocaliva that is written for health professionals.
How should I store Ocaliva?
- Store Ocaliva at room temperature between 68°F to 77°F (20°C to 25°C).
Keep Ocaliva and all medicines out of the reach of children.
What are the ingredients in Ocaliva?
Active ingredient: obeticholic acid
Inactive ingredients: microcrystalline cellulose, sodium starch glycolate, magnesium stearate
Film coating: Opadry II (Yellow) containing polyvinyl alcohol-part hydrolyzed, titanium dioxide, macrogol (polyethylene glycol 3350), talc, iron oxide yellow
PRINCIPAL DISPLAY PANEL – 5 MG TABLET BOTTLE LABEL
- NDC 69516-005-30
(obeticholic acid) tablets
- 5 mg
- 30 tablets
PRINCIPAL DISPLAY PANEL – 10 MG TABLET BOTTLE LABEL
- NDC 69516-010-30
(obeticholic acid) tablets
- 10 mg
- 30 tablets
SRC: NLM .