Cholic acid

Cholic Acid is part of the drug class:

• Bile acid preparations

Serious side effects have been reported with cholic acid. See the “Cholic Acid Precautions” section.

Common side effects of cholic acid inlcude:

• diarrhea
• feeling tired
• yellowing of the skin
• skin lesions
• nausea
• vomiting
• abdominal pain
• urinary tract infections

This is not a complete list of cholic acid side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• Bile Salt Efflux Pump inhibitors such as cyclosporine (Neoral, Gengraf, Sandimmune, Restasis)
• Bile acid resins such as cholestyramine (Questran, Prevalite), colesevelam (Welchol), and colestipol (Colestid)
• Aluminum-based antacids

This is not a complete list of cholic acid drug interactions. Ask your doctor or pharmacist for more information.

Tell your doctor if you are pregnant or plan to become pregnant.

There are no well-controlled studies that have been done in pregnant women or animals. Cholic acid should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

There is a pregnancy surveillance program that monitors pregnancy outcomes in women exposed to cholic acid during pregnancy and women who become pregnant during cholic acid treatment are encouraged to enroll. Contact your healthcare provider for more informaiton.

Take cholic acid exactly as prescribed.

Cholic acid comes in capsule form and is usually taken once or twice daily with food. Do not chew, divide, or break cholic acid capsules. Swallow capsules whole.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take 2 doses of cholic acid at the same time.

• Cholic acid is a primary bile acid synthesized from cholesterol in the liver.1 3 4 Endogenous primary bile acids (i.e., cholic acid, chenodeoxycholic acid) improve bile flow and provide physiologic feedback inhibition of bile acid synthesis.1 5

• Cholic acid and its conjugates are endogenous ligands of the nuclear farnesoid X receptor (FXR), which regulates enzymes and transporters involved in bile acid synthesis and enterohepatic circulation to maintain bile acid homeostasis under normal physiologic conditions.1 4 Activation of the FXR through binding of cholic acid results in upregulation of transcription of genes coding for hepatic conjugation enzymes, resulting in increased metabolic conjugation of bile acids and bile acid-dependent bile flow.5

• Activated FXR also results in downregulation of cholesterol 7α-hydroxylase encoded by the CYP7A1 gene, potentially resulting in reduction in de novo synthesis of primary bile acids; clinical importance of such downregulation is not fully known.5

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution of cholic acid is restricted.8 9 (See Restricted Distribution Program under Dosage and Administration.)

Take cholic acid exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

Swallow the capsule whole. Do not crush, break, or chew it. Take cholic acid with food.

If you cannot swallow the capsules, you may open it and mix the contents of the capsule with 1 to 2 tablespoons of infant formula or expressed breast milk, or soft foods (eg, mashed potatoes or apple puree). This mixture must be swallowed immediately.

If you are also taking cholestyramine, colesevelam, colestipol, or aluminum-containing antacids, take cholic acid at least 1 hour before or 4 to 6 hours after these medicines.

Dosing

The dose of cholic acid will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of cholic acid. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (capsules):
  • For bile acid synthesis disorders and peroxisomal disorders (including Zellweger spectrum disorders):
    • Adults and children 3 weeks of age and older—Dose is based on body weight and must be determined by your doctor. The dose is usually 10 to 15 milligrams (mg) per kilogram (kg) of body weight once a day, or divided in two doses.
    • Children younger than 3 weeks of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of cholic acid, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

• It is used to treat certain bile acid problems caused by single enzyme defects (SEDs).
• It is used to treat peroxisomal disorders like Zellweger spectrum disorders.

• If you have an allergy to cholic acid or any part of this medicine.
• If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
• If you are taking cyclosporine.

This is not a list of all drugs or health problems that interact with cholic acid.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Use cholic acid as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take this medicine with food.
• Swallow whole. Do not chew, break, or crush.
• If you cannot swallow the capsule whole, you may open the capsule and mix the contents with certain foods. For younger children, the contents may be mixed with infant formula or breast milk. For older children and adults, the contents may be mixed with soft food like mashed potatoes or apple sauce. Stir for 30 seconds and swallow right away. Do not store for future use.
• If you also take cholestyramine, colesevelam, colestipol, or an antacid that has aluminum, do not take it within 4 to 6 hours before or 1 hour after cholic acid.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

There are no dosage adjustments provided in the manufacturer’s labeling.

There are no dosage adjustments provided in the manufacturer’s labeling. Discontinue if hepatic function does not improve within 3 months of starting treatment, if complete biliary obstruction develops, or if there are persistent clinical or laboratory indicators of worsening hepatic function or cholestasis; continue to monitor hepatic function and consider restarting a lower dose when parameters return to baseline.

Aluminum Hydroxide: May decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 hour before or 4 to 6 hours after administration of any aluminum hydroxide-containing products to minimize the potential for a significant interaction. Consider therapy modification

Bile Acid Sequestrants: May decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 to 4 hours before or 4 to 6 hours after administration of any bile acid-binding products to minimize the potential for a significant interaction. Consider therapy modification

BSEP/ABCB11 Inhibitors (Clinically Relevant): May decrease the excretion of Cholic Acid. Avoid combination

Sevelamer: May decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 hour before or 4 to 6 hours after administration of any bile acid-binding products, such as sevelamer, to minimize the potential for a significant interaction. Consider therapy modification

Sucralfate: May decrease the absorption of Cholic Acid. Consider therapy modification

>10%:

Gastrointestinal: Cholestasis (≤14%, exacerbation)

Hepatic: increased serum bilirubin ( ≤14%), increased serum transaminases ( ≤14%)

1% to 10%:

Central nervous system: Malaise (≤1%), peripheral neuropathy (≤1%)

Dermatologic: Skin lesion (≤1%)

Gastrointestinal: Diarrhea (1% to 2%), abdominal pain (≤1%), intestinal polyps (≤1%), nausea (≤1%), reflux esophagitis (≤1%)

Genitourinary: Urinary tract infection (≤1%)

Hepatic: Hepatic disease (6%, exacerbation), jaundice (≤1%)

<1% (Limited to important or life-threatening): Cholelithiasis (3β-HSD deficienct patient)

Disease-related concerns:

• Hepatic impairment: Monitor liver function tests (eg, aspartate aminotransferase [AST], alanine aminotransferase [ALT], gamma glutamyltransferase [GGT], alkaline phosphatase [ALP], bilirubin and INR) monthly for the first 3 months. Discontinue if hepatic function does not improve within 3 months of starting treatment, if complete biliary obstruction develops, or if there are persistent clinical or laboratory indicators of worsening hepatic function or cholestasis; continue to monitor hepatic function and consider restarting a lower dose when parameters return to baseline. Concurrent elevations of GGT and ALT may indicate cholic acid overdose.

Other warnings/precautions:

• Experienced physician: Treatment should be initiated and monitored by an experienced hepatologist or pediatric gastroenterologist.

Applies to cholic acid: oral capsule

Along with its needed effects, cholic acid may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking cholic acid:

• Abdominal or stomach pain
• chills
• clay-colored stools
• dark urine
• diarrhea
• dizziness
• fever
• general feeling of tiredness or weakness
• headache
• itching or rash
• light-colored stools
• loss of appetite
• nausea
• stomach pain, continuing
• unpleasant breath odor
• unusual tiredness or weakness
• vomiting
• vomiting of blood
• yellow eyes or skin

• Bladder pain
• bloody or cloudy urine
• clay-colored stools
• dark urine
• difficult, burning, or painful urination
• frequent urge to urinate
• lower back or side pain
• unpleasant breath odor

Some side effects of cholic acid may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Burning, numbness, tingling, or painful sensations
• chest pain
• difficulty with swallowing
• general feeling of discomfort or illness
• heartburn
• pain or burning in the throat
• skin lesions
• sores, ulcers, or white spots on the lips or tongue or inside the mouth
• unsteadiness or awkwardness
• weakness in the arms, hands, legs, or feet

No data available

Safety and efficacy have not been established in patients younger than 3 weeks of age.

Consult WARNINGS section for additional precautions.