Dosing & Uses
Dosing & Strengths
Radiolucent Gallstone Dissolution
For dissolution of gallstones; effective only in the treatment of cholesterol-rich, radiolucent gallstones (not radiopaque stones) in well-opacifying gallbladders
Combinatin therapy (off-label): 5-7.5 mg/kg/day PO qHS in combination with ursodeoxycholic acid, with or without adjuvant lithotripsy
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
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
Serious - Use Alternative
Significant - Monitor Closely
Billiary pain (10-15%)
Increased aminotransferase (>30%)
Frequency Not Defined
Increased LDL and total cholesterol
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
Gallstone complication requiring surgery
Known hepatocyte or bile ductal abnormalities, inflammatory bowel disease
Orphan drug status, for use in surgical high-risk patients with radiolucent stones
Concomitant use with clofibrate
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
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.
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
Onset: initial response for gallstone dissolution: 3-6 month
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
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