Ursolic300 mg

Ursolic is a naturally occurring bile acid used for the following established indications:

• Dissolution of gallstones: Ursolic is indicated for the dissolution of small to medium-sized radiolucent (non-calcified, cholesterol-rich) gallstones in patients for whom surgery (cholecystectomy) is not an option or is being deferred.
• Prevention of gallstones during rapid weight loss: Ursolic is used to prevent gallstone formation in patients undergoing rapid weight loss, such as after bariatric surgery or very-low-calorie diet programs.
• Primary biliary cholangitis (PBC), previously called primary biliary cirrhosis: Ursolic is indicated to slow disease progression and improve liver biochemistry and survival without liver transplantation in patients with PBC.

Ursolic is also used, under specialist guidance, in certain other cholestatic liver conditions (e.g., intrahepatic cholestasis), though such use should be individualized by the treating physician.

Ursolic is not a substitute for cholecystectomy when surgery is clinically indicated.

Ursodeoxycholic Acid is available as oral tablets and capsules, commonly in strengths of 150 mg, 200 mg, 250 mg, and 300 mg. Each tablet/capsule contains Ursodeoxycholic Acid as the active ingredient along with standard pharmaceutical excipients such as binders, fillers, and coating agents. Exact strengths and formulations vary by manufacturer; refer to the specific product label for details.

Ursolic (also known as ursodiol) is a hydrophilic bile acid that occurs naturally in small quantities in human bile. As a medicine, Ursolic is used to dissolve certain types of gallstones and to treat chronic cholestatic liver diseases such as primary biliary cholangitis. Ursolic works by altering the composition of bile, reducing cholesterol saturation, and exerting cytoprotective and choleretic effects on liver cells.

Bile acid preparation / Hepatobiliary and gallstone-dissolving agent

Ursodeoxycholic Acid is a naturally occurring, hydrophilic bile acid that alters bile composition and exerts hepatoprotective effects through several mechanisms:

• Reduces hepatic cholesterol synthesis and secretion into bile, and decreases intestinal absorption of cholesterol, thereby lowering the cholesterol saturation index of bile.
• Promotes the formation of a liquid crystalline phase that gradually dissolves cholesterol from the surface of gallstones.
• Displaces more hydrophobic, cytotoxic endogenous bile acids in the bile acid pool, reducing bile-acid-induced injury to hepatocyte and bile duct cell membranes.
• Has immunomodulatory and anti-apoptotic effects on liver cells, which contribute to its benefit in cholestatic liver diseases such as primary biliary cholangitis.
• Stimulates biliary secretion (choleretic effect).

Onset of gallstone dissolution with Ursodeoxycholic Acid is gradual, typically requiring months of continuous therapy, with response monitored by periodic ultrasound.

Ursolic tablets/capsules should be swallowed whole with a full glass of water. Taking Ursolic with food may help reduce stomach upset and improve absorption. Doses are usually divided through the day as directed by the physician (see "Dosage and Administration"). If a dose of Ursolic is missed, it should be taken as soon as remembered unless it is close to the next scheduled dose, in which case the missed dose should be skipped — do not double the dose.

The following interactions with Ursolic are clinically significant:

• Bile acid-binding resins (cholestyramine, colestipol) and aluminum-containing antacids can bind Ursolic in the gut and reduce its absorption, decreasing its effectiveness. If concurrent use is necessary, doses should be spaced at least 2 hours apart from Ursolic.
• Estrogens and estrogen-containing oral contraceptives may increase cholesterol secretion into bile and could counteract the gallstone-dissolving effect of Ursolic.
• Clofibrate and other lipid-lowering agents of the fibrate class may similarly increase biliary cholesterol secretion and reduce the effectiveness of Ursolic for gallstone dissolution.

Inform the physician of all medications, including over-the-counter antacids and supplements, before starting Ursolic.

Ursolic is generally well tolerated. Reported side effects include:

• Common: Diarrhea (the most frequently reported effect), abdominal pain, dyspepsia (indigestion), nausea, and headache.
• Less common: Constipation, dizziness, fatigue, hair thinning, skin rash, itching (pruritus), and metallic or unusual taste.
• Rare: Calcification of gallstones, and paradoxical worsening of liver function tests in some patients with primary biliary cholangitis, which requires periodic monitoring (see Precautions and Warnings).

Patients should seek medical attention if they notice worsening abdominal pain, jaundice (yellowing of skin/eyes), dark urine, or signs of an allergic reaction while taking Ursolic.

Data on the use of Ursolic during pregnancy are limited. Ursolic should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus, and only under direct physician supervision; it is generally not recommended for routine use during pregnancy given the limited safety data, although inadvertent exposure in reported cases has not shown clear fetal harm.

It is not fully established whether Ursolic passes into breast milk in clinically significant amounts. Because bile acids are naturally present in breast milk and no adverse effects have been documented in nursing infants in available reports, use during breastfeeding may be considered by the physician when clearly needed, weighing benefits and risks. Consult a physician before using Ursolic during pregnancy or breastfeeding.

Before and during treatment with Ursolic:

• Ursolic is not effective for dissolving calcified, radiopaque, or pigment gallstones; ultrasound or other imaging should confirm stone type before starting therapy.
• Periodic liver function testing is recommended during long-term therapy with Ursolic, particularly in patients with primary biliary cholangitis, as a small number of patients may show worsening of liver enzymes despite treatment.
• For gallstone dissolution, periodic ultrasound monitoring (e.g., every 6 months) is used to assess response; if gallstones do not appear to be dissolving after a reasonable treatment period, or if the patient becomes a surgical candidate, the physician may reassess the treatment plan.
• Gallstones can recur after Ursolic is discontinued; long-term follow-up may be advised.
• Rare cases of intestinal bezoar (enterolith) formation have been reported, mainly in patients with conditions causing intestinal stasis or stricture; report new or worsening abdominal/obstructive symptoms to the physician promptly.
• Use with caution in patients with chronic liver disease other than the labeled indications, and only under specialist supervision.
• See Contraindications, Drug Interactions, and Pregnancy and Lactation sections for additional safety information.

There is limited clinical experience with overdose of Ursolic. Based on its pharmacology, an overdose of Ursolic may be expected to cause watery diarrhea, which would generally resolve once the drug is stopped or eliminated. There is no specific antidote. In case of a suspected overdose of Ursolic, seek immediate medical attention or contact a poison control center; management is supportive and symptomatic, guided by the treating physician.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Hepatic impairment: Ursolic is used specifically to treat certain cholestatic and gallstone conditions of the liver and biliary tract, but is not indicated for all types of liver disease; use should be guided by a specialist, with periodic liver function monitoring (see Precautions and Warnings).

Renal impairment: No specific dose adjustment is established; Ursolic should be used with caution and physician oversight in patients with significant renal impairment.

Elderly: No overall differences in safety or efficacy of Ursolic have been consistently reported in elderly patients compared with younger adults, but dosing should be individualized, and comorbidities and concomitant medications should be considered.

Pediatric use: See "Pediatric Uses" section.

Pregnancy and breastfeeding: See "Pregnancy and Lactation" section.

Duration of treatment with Ursolic depends on the indication:

• Gallstone dissolution: Treatment with Ursolic is typically continued for several months up to about 2 years, with ultrasound monitoring (often every 6 months) to confirm dissolution. Even after gallstones dissolve, gallstones may recur after stopping Ursolic, and the physician may advise continued follow-up or a period of continued low-dose therapy.
• Gallstone prevention during rapid weight loss: Ursolic is usually continued for the duration of the weight-loss period (e.g., through the period of rapid weight loss following bariatric surgery), as directed by the physician.
• Primary biliary cholangitis: Ursolic is generally a long-term, often lifelong therapy, with periodic monitoring of liver function and clinical status.

Do not stop Ursolic without consulting the prescribing physician, as premature discontinuation may reduce treatment benefit or allow disease/gallstone recurrence.

Bile acids and derivatives; Gallstone-dissolving agent (cholelitholytic); Hepatoprotective agent

Ursodeoxycholic Acid works mainly by reducing the cholesterol saturation of bile — it decreases cholesterol secretion into bile and reduces intestinal cholesterol absorption, which promotes gradual dissolution of cholesterol-based gallstones. In cholestatic liver disease, Ursodeoxycholic Acid replaces more toxic, hydrophobic bile acids in the bile acid pool, protects liver and bile duct cells from bile-acid-induced injury, and has additional cytoprotective, anti-inflammatory, and immunomodulatory effects that help preserve liver function.

Category B (historical FDA pregnancy letter classification reported for ursodiol-containing products; current labeling uses narrative risk information rather than letter categories — consult the physician; see Pregnancy and Lactation).

Ursolic is not FDA-approved for general pediatric use for the labeled adult indications (gallstone dissolution/prevention). However, Ursolic has been used off-label, under specialist (pediatric hepatology/gastroenterology) guidance, in some pediatric cholestatic liver conditions, with dosing individualized by body weight and closely monitored. Use of Ursolic in children should only occur under the direct supervision of a pediatric specialist, with attention to liver function monitoring.