Dosing & Uses
Radiolucent Gallstone Dissolution
For dissolution of gallstones; effective only in the treatment of cholesterol-rich, radiolucent gallstones (not radiopaque stones) in well-opacifying gallbladders
Monotherapy: 250 mg PO q12hr for 2 weeks initially, then increase by 250 mg/day at weekly intervals, up to 13-16 mg/kg/day divided q12hr PO
Combination therapy (off-label): 5-7.5 mg/kg/day PO qHS in combination with ursodeoxycholic acid, with or without adjuvant lithotripsy
Xanthomatosis (Orphan)
Indicated for treatment of cerebrotendinous xanthomatosis
Orphan indication sponsor
- Dr. Falk Pharma GmbH; Leinenweberstrasse 5, 9041; Freiburg, Germany
- Sigma-Tau Pharmaceuticals, Inc; 9841 Washingtonian Blvd, Suite 500; Gaithersburg, MD 20878
- Manchester Pharmaceuticals, Inc; 8236 Benson Ct; Fort Collins, CO 80525
Administration
Indicated in patients whom selective surgery would be undertaken except for the presence of increased surgical risk because of systemic disease or age
Successful dissolution is more likely if the stones are floatable or small
Safety of use beyond 24 months is not established
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (0)
Monitor Closely (7)
- aluminum hydroxide
aluminum hydroxide decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- calcium carbonate
calcium carbonate decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- crofelemer
crofelemer increases levels of chenodiol by Other (see comment). Use Caution/Monitor. Comment: Crofelemer has the potential to inhibit transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.
- eluxadoline
eluxadoline increases levels of chenodiol by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.
- sodium bicarbonate
sodium bicarbonate decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- sodium citrate/citric acid
sodium citrate/citric acid decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2 hours.
- warfarin
chenodiol increases effects of warfarin by unspecified interaction mechanism. Use Caution/Monitor.
Minor (3)
- cholestyramine
cholestyramine decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- colesevelam
colesevelam decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
- colestipol
colestipol decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.
Adverse Effects
>10%
Diarrhea (30-40%)
Biliary pain (10-15%)
Increased aminotransferase (>30%)
Frequency Not Defined
Abdominal cramps
Nausea
Vomiting
Abdominal pain
Constipation
Heartburn
Flatulence
Increased LFT's
Increased LDL and total cholesterol
Warnings
Black Box Warnings
Not an appropriate treatment for many patients with gallstones because of potential hepatotoxicity, poor response rate in some patient subgroups, and increased rate of cholecystectomy in other subgroups
Reserve for carefully selected patients
Treatment must include systematic monitoring for liver function alterations
Contraindications
Gallstone complication requiring surgery
Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
Pregnancy
Cautions
Orphan drug status, for use in surgical high-risk patients with radiolucent stones
Breastfeeding
Concomitant use with clofibrate
Hepatotoxicity
Dose related diarrhea occurs
50% of cases have stone recurrence in 5 yr
Pregnancy & Lactation
Pregnancy Category: X
Lactation: unknown whether cevimeline is distributed into breast milk, avoid using in nursing women
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Chenodiol itself is a primary acid excreted into the bile, constitutes 1/3 of total biliary bile acid; drug action on gallstone dissolution relies on negative feedback effect on the rate-limiting enzyme for synthesis of cholesterol and bile
Pharmacokinetics
Onset: initial response for gallstone dissolution: 3-6 month
Bioavailability: 81-100%
Excretion: Mainly in feces (80%)
Metabolism: After absorption, chenodiol is conjugated with glycine or taurine in the liver and rapidly located in the bile; conjugated chenodiol is then reabsorbed in terminal ileum and jejunum, completing the enterohepatic cycle; lithocholic acid (inactive) is formed in the intestine by bacterial dehydroxylation of unabsorbed chenodiol (active); conjugated, sulfated and excreted in the bile; hepatotoxic in animals
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Chenodal oral - | 250 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
chenodiol oral
CHENODIOL - ORAL
(KEE-noe-DYE-ol)
COMMON BRAND NAME(S): Chenodal
USES: Chenodiol is used to dissolve certain types of gallstones (non-calcified). Chenodiol is a bile acid. Chenodiol may be tried before surgery in patients that are at high risk of complications from gallstone surgery. If the gallstones do not dissolve, emergency surgery may still be needed.
HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually twice a day (once in the morning and once at night).Dosage is based on your medical condition, weight, and response to treatment.Aluminum-containing antacids and certain drugs to lower your cholesterol (bile acid-binding resins such as cholestyramine or colestipol) can decrease how much of this medication your body absorbs. If you are taking any of these medications, separate them from chenodiol by at least 4 hours.To reduce your risk of side effects such as diarrhea, your doctor will direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully. Tell your doctor if you have severe diarrhea. Your doctor may need to lower your dose or stop the medication.Do not increase your dose or take this medication more often without your doctor's approval. Your condition will not improve any faster, and the risk of serious side effects may be increased.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. Do not stop taking this medication without talking with your doctor.It may take up to 24 months before the gall stones are completely dissolved. Your doctor will order tests (gall bladder sonograms or x-rays) to check your progress. Keep all medical appointments. Tell your doctor if your condition lasts or gets worse (stomach/abdominal pain, nausea, or vomiting).
SIDE EFFECTS: Diarrhea, nausea, or heartburn may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This drug may cause serious (possibly fatal) liver disease. Your doctor will order blood tests to check for liver problems. It is very important to keep all lab appointments. Get medical help right away if you have any symptoms of liver damage, including: nausea/vomiting that doesn't stop, yellowing eyes/skin, dark urine, unusual tiredness, severe stomach/abdominal pain.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking chenodiol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems (such as hepatitis, cirrhosis), a certain red blood cell problem (hemolysis), regular use/abuse of alcohol.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).This medication must not be used during pregnancy. It may harm an unborn baby. Estrogen-containing birth control may increase your risk of gall stones. Discuss the use of reliable forms of birth control with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown whether this drug passes into breast milk and the effect on a nursing infant is unknown. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: estrogens (such as estradiol, estrogen pills/patch/cream, birth control pills/patch/ring), "blood thinners" (such as warfarin).
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver function, cholesterol tests) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.Maintaining a normal weight and a diet high in fiber (such as bran) and low in cholesterol/carbohydrates may help prevent gall stones. Ask your doctor, pharmacist, or nutritionist for more information.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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