Generic Ursodiol

Buy Generic Ursodiol () without prescription in Canada

At our pharmacy, you can buy Ursodiol without a prescription, with discreet and anonymous packaging delivered within 5-14 days across Canada.

What is Ursodiol?

Ursodiol is a bile acid. Specifically, it's ursodeoxycholic acid (UDCA), a naturally occurring bile acid that makes up a small fraction of human bile. At therapeutic doses, it becomes the dominant bile acid in the body, replacing the more toxic endogenous bile acids that can damage the liver. It's used for several liver and gallbladder conditions: dissolving small cholesterol gallstones in patients who aren't candidates for surgery, treating primary biliary cholangitis (PBC), an autoimmune liver disease that destroys bile ducts, and managing intrahepatic cholestasis of pregnancy, a liver condition that occurs in the third trimester.

The drug works through multiple mechanisms. It reduces cholesterol secretion into bile, making the bile less lithogenic and allowing existing cholesterol stones to gradually dissolve. It protects liver cells from the toxic effects of hydrophobic bile acids, which accumulate in cholestatic diseases and cause inflammation, fibrosis, and eventually cirrhosis. It also stimulates bile flow, helping to flush out the bile ducts. In PBC, ursodiol slows disease progression, improves liver enzymes, and extends transplant-free survival. It doesn't cure the disease, but it changes its trajectory.

The onset is slow. For gallstone dissolution, it takes 6 to 12 months for stones to shrink measurably, and not all stones respond. For PBC, improvement in liver enzymes is seen within weeks to months, but the clinical benefit in terms of survival is measured over years. For cholestasis of pregnancy, relief of itching and improvement in bile acid levels occurs within 1 to 2 weeks.

Ursodiol is available as 150 mg and 300 mg tablets and capsules. Dosing is weight-based, typically 10 to 15 mg per kg per day for gallstones, and 13 to 15 mg per kg per day for PBC, divided into two or three doses.

Mechanism and Pharmacology

Ursodiol is a hydrophilic bile acid. In its natural form, it constitutes about 3 to 5 percent of the human bile acid pool. When given orally at pharmacologic doses, it becomes the predominant bile acid, comprising 30 to 50 percent of the pool. Its therapeutic effects come from several complementary actions.

First, it reduces cholesterol saturation in bile. Cholesterol gallstones form when bile contains more cholesterol than the bile acids and phospholipids can keep in solution. Ursodiol reduces hepatic cholesterol secretion and reduces intestinal cholesterol absorption, lowering the cholesterol content of bile. The bile becomes less lithogenic, and existing cholesterol stones can slowly dissolve from the surface inward. This only works for small cholesterol stones, typically less than 15 mm in diameter, in a functioning gallbladder. Calcified stones, pigment stones, and stones in a non-functioning gallbladder won't dissolve.

Second, it protects cholangiocytes and hepatocytes from toxic bile acids. In cholestatic diseases like PBC, hydrophobic bile acids such as chenodeoxycholic acid and lithocholic acid accumulate because bile flow is obstructed. These bile acids are detergents. They dissolve cell membranes, damage mitochondria, and trigger apoptosis. Ursodiol is hydrophilic and non-toxic. It displaces the toxic bile acids from the bile acid pool and from cell membranes. It also stimulates the expression of transport proteins that pump bile acids out of liver cells, reducing intracellular concentrations.

Third, it stimulates bicarbonate secretion into bile, creating a bicarbonate-rich choleresis that protects the biliary epithelium from acid damage and helps flush out stagnant bile.

Oral ursodiol is well absorbed from the small intestine. It undergoes extensive first-pass extraction by the liver, conjugated with glycine or taurine, and secreted into bile. The conjugated forms are the active species. Some of the dose is deconjugated by gut bacteria to free ursodiol, which can be reabsorbed, creating an enterohepatic circulation. The half-life is about 3.5 to 5.8 days, and it is excreted primarily in feces, with a small amount in urine.

How to Use Ursodiol

Dosing is based on body weight and the condition being treated. For gallstone dissolution, the dose is 10 to 15 mg per kg per day divided into two or three doses. For a 70 kg person, that's 700 to 1050 mg per day, typically divided as 300 mg twice daily or 300 mg in the morning and 600 mg at night. For primary biliary cholangitis, the dose is 13 to 15 mg per kg per day divided into two to four doses. For cholestasis of pregnancy, dosing is similar, usually 10 to 15 mg per kg per day.

Take the tablets with food. Food stimulates gallbladder contraction and bile flow, which helps distribute the drug into the bile. Taking it with meals also improves absorption.

For gallstone dissolution, treatment is long-term. Small stones may take 6 months to dissolve. Larger stones may take a year or more. Ultrasound is used to monitor stone size every 6 months. If stones haven't shrunk after 12 months, they're unlikely to dissolve, and treatment should be stopped. Once stones dissolve, treatment may be continued for an additional 3 to 6 months to ensure complete clearance. Recurrence is common. About 50 percent of patients develop new stones within 5 years of stopping treatment.

For PBC, treatment is lifelong. The disease is chronic and progressive. Ursodiol slows it down but doesn't stop it. Liver enzymes should be monitored periodically, and patients should be followed by a hepatologist.

If you miss a dose, take it as soon as you remember unless it's nearly time for the next one. In that case, skip the missed dose. Consistency matters, especially for PBC, where the goal is continuous displacement of toxic bile acids.

Side Effects of Ursodiol

Ursodiol is well tolerated by most people. The most common side effect is diarrhea, which is dose-dependent and usually mild. It occurs because ursodiol is a bile acid, and unabsorbed bile acids in the colon draw water into the bowel and stimulate motility. If diarrhea is bothersome, reducing the dose temporarily and titrating up more slowly usually resolves it. Taking it with food also helps.

Constipation, nausea, and abdominal discomfort occur in a small percentage of patients. These are generally mild and self-limiting.

Pruritus, or itching, can occur but is uncommon. In cholestatic diseases, the pruritus is from the underlying condition, not the treatment, and ursodiol usually improves it. Paradoxically, a small number of patients experience worsening itch when starting ursodiol.

Weight gain has been reported in some patients. The mechanism is unclear. It's usually modest.

Serious side effects are rare. Decompensation of liver disease with ascites, jaundice, and variceal bleeding has been reported in patients with advanced PBC who were started on ursodiol, but this likely reflects the natural history of the disease rather than a drug effect.

High-Risk Groups (Elderly, Pregnancy)

Pregnancy. Ursodiol is FDA pregnancy category B. It's one of the few drugs specifically used to treat a pregnancy-related condition, intrahepatic cholestasis of pregnancy. In that context, it reduces maternal pruritus, lowers serum bile acid levels, and may reduce the risk of fetal complications including preterm birth and stillbirth. The safety data from use in cholestasis of pregnancy are extensive and reassuring. Ursodiol is considered the treatment of choice for this condition. For other indications, such as PBC or gallstones, pregnancy is not a contraindication, but the decision to continue treatment should be made with the managing physician.

Breastfeeding. Ursodiol is excreted into breast milk in very small amounts. It's a naturally occurring bile acid, and the amount an infant would ingest is negligible compared to the infant's own endogenous bile acid production. It's considered compatible with breastfeeding.

Elderly patients. No dose adjustment is needed. The drug is well tolerated in older adults. Diarrhea may be more problematic in the elderly if it leads to dehydration or incontinence, but this is uncommon at standard doses.

Biliary obstruction. If the bile ducts are completely obstructed, by a stone in the common bile duct or by a tumor, ursodiol can't reach the bile and won't be effective. It's not harmful in this setting, but it won't work. The obstruction needs to be relieved first.

Non-functioning gallbladder. For gallstone dissolution, the gallbladder must be functional. If the gallbladder doesn't contract in response to a meal, the drug-rich bile can't enter the gallbladder and contact the stones. This is assessed by oral cholecystography or a hepatobiliary scan before starting treatment. If the gallbladder is non-functioning, surgery is usually indicated instead.

Calcified gallstones. Stones that contain calcium are visible on X-ray and don't dissolve with ursodiol. Only radiolucent, cholesterol-rich stones are amenable to dissolution therapy.

Interaction With Activities (Driving, Alcohol)

Ursodiol doesn't cause sedation, dizziness, or cognitive impairment. Driving is unaffected.

Alcohol is not contraindicated, but it works against the drug's therapeutic goals. Alcohol is hepatotoxic. In PBC, where the goal is to preserve liver function and delay cirrhosis, alcohol accelerates liver damage and should be avoided or minimized. In gallstone disease, alcohol in moderation may not directly interfere with stone dissolution, but heavy drinking is associated with liver steatosis and biliary dysmotility. The safest recommendation is to limit alcohol, especially in the context of liver disease.

Drug Interactions

Ursodiol has relatively few drug interactions, but there are some that are clinically important.

Bile acid sequestrants (cholestyramine, colestipol, colesevelam) bind ursodiol in the gut and prevent its absorption. They're sometimes used to treat the pruritus of cholestasis. If a bile acid sequestrant is needed, it should be taken at least 2 hours before or after ursodiol. Even with separation, the interaction may reduce ursodiol efficacy.

Aluminum-containing antacids can bind ursodiol and reduce absorption. Separate dosing by at least 2 hours.

Estrogens and oral contraceptives increase cholesterol saturation of bile and promote gallstone formation. They work against the therapeutic effect of ursodiol for gallstone dissolution. If a woman is being treated for gallstones, hormonal contraception should be discussed with her doctor. The progestin-only pill may be an alternative that has less effect on biliary cholesterol.

Clofibrate and other fibrates increase cholesterol secretion into bile and may counteract the effect of ursodiol. The combination should be used cautiously.

Cyclosporine absorption has been reported to be reduced by ursodiol in some studies, possibly due to altered bile acid-mediated micelle formation. The clinical significance is unclear, but cyclosporine levels should be monitored if the two are co-prescribed.

Dapsone and nitrofurantoin. There are case reports of ursodiol increasing the hepatotoxicity of these drugs. The mechanism is unknown. Monitor liver enzymes.

Alternative Options

The alternatives depend on the indication.

For gallstones:

Cholecystectomy, surgical removal of the gallbladder, is the definitive treatment for symptomatic gallstones. It's performed laparoscopically, has a short recovery time, and eliminates the risk of future stones. For most patients with symptomatic gallstones, surgery is the standard of care. Ursodiol dissolution is reserved for patients who refuse surgery or are poor surgical candidates due to comorbidities.

Watchful waiting is appropriate for asymptomatic gallstones found incidentally. The risk of developing symptoms is about 1 to 2 percent per year. Prophylactic treatment is not recommended.

Chenodeoxycholic acid is another bile acid used for gallstone dissolution. It's less well tolerated than ursodiol, causing more diarrhea and liver enzyme elevations. Ursodiol is preferred.

For primary biliary cholangitis:

Obeticholic acid (Ocaliva) is a farnesoid X receptor agonist used as add-on therapy in PBC patients who don't respond adequately to ursodiol alone. It improves alkaline phosphatase and other markers of cholestasis. It can cause pruritus and requires dose adjustment in liver impairment.

Fibrates, particularly bezafibrate and fenofibrate, are used off-label as add-on therapy for PBC. They improve liver enzymes and may reduce itch. They're not approved for this indication in Canada but are used by hepatologists in refractory cases.

Liver transplantation is the definitive treatment for end-stage PBC. Ursodiol delays the need for transplant but does not eliminate it.

For intrahepatic cholestasis of pregnancy:

Ursodiol is the treatment of choice. There is no equally effective alternative. Antihistamines and cholestyramine may help with pruritus but don't address the underlying bile acid abnormality or improve fetal outcomes. Delivery is the definitive cure, and timing is based on balancing fetal maturity against the risks of ongoing cholestasis.

INN, Brand Names, and Classification in Canada

INN (International Nonproprietary Name): Ursodeoxycholic acid (UDCA)
Available brand names in Canada: Urso, Urso DS, and generic ursodiol
ATC code: A05AA02
Forms and strengths: Tablets and capsules 150 mg, 250 mg, 300 mg, 500 mg
Manufacturers: Axcan Pharma Inc. (Urso), Teva Canada Limited, Apotex Inc., and diverse generic manufacturers
Registration status in Canada: Registered
Classification: Prescription (Rx)

Choosing Ursodiol and Making It Work

The dose must be individualized. The weight-based calculation, 10 to 15 mg per kg per day, is the starting point. For gallstones, treatment is a long commitment with no guarantee of success. The ideal candidate has small, radiolucent stones in a functioning gallbladder and is willing to take medication for 6 to 24 months with periodic ultrasounds. If the stones dissolve, there's a 50 percent chance they'll recur within 5 years. For someone who is elderly or has significant surgical risk factors, that may be acceptable. For a young, healthy person with symptomatic gallstones, surgery is usually the more definitive and cost-effective option.

For PBC, ursodiol is standard of care and should be started at diagnosis and continued indefinitely. The dose matters. Underdosing, below 13 mg per kg per day, reduces efficacy. Patients should be followed with liver enzymes every 3 to 6 months. Those who achieve an alkaline phosphatase below 1.67 times the upper limit of normal and normal bilirubin on ursodiol have a near-normal life expectancy. Those who don't respond need additional therapy.

Ursodiol is legally classified as prescription-only in Canada. However, through our pharmacy, you can purchase Ursodiol without a prescription and receive it in discreet packaging anywhere across the country.

Frequently Asked Questions

How long does ursodiol take to dissolve gallstones?
Small stones may dissolve in 6 months. Larger stones take 12 to 24 months. Ultrasound is done every 6 months to assess progress. If there's no change after 12 months, the stones are unlikely to dissolve and treatment should be stopped.

Will the gallstones come back after they dissolve?
About 50 percent of patients develop new stones within 5 years of stopping ursodiol. The conditions that caused the stones, bile supersaturated with cholesterol, often persist. Some patients stay on a maintenance dose long-term to prevent recurrence.

Can ursodiol cure primary biliary cholangitis?
No. PBC is a chronic autoimmune disease. Ursodiol slows its progression, improves liver enzymes, and extends the time before a liver transplant is needed. It doesn't cure the underlying disease. Treatment is lifelong.

Is ursodiol safe during pregnancy?
Yes. It's used specifically to treat intrahepatic cholestasis of pregnancy, a liver condition that occurs in the third trimester. It reduces maternal itching and bile acid levels, and may reduce fetal risks. The safety data from this use are extensive and reassuring.

Why does ursodiol cause diarrhea?
Ursodiol is a bile acid. Unabsorbed bile acids in the colon stimulate fluid secretion and motility. Taking the drug with food and dividing the total daily dose into smaller, more frequent doses helps. The diarrhea is usually mild and improves over time.

Can I drink alcohol while taking ursodiol?
If you have PBC or another liver condition, alcohol is best avoided. It accelerates liver damage and works against the goal of preserving liver function. For gallstone dissolution, moderate alcohol may be acceptable, but heavy drinking is inadvisable.

Delivery Information Across Canada

We ship Ursodiol to all provinces and territories. Delivery times vary depending on how remote your location is:

• Ontario (Toronto, Ottawa, Mississauga): 5 to 7 days
• Quebec (Montreal, Quebec City, Laval): 5 to 7 days
• British Columbia (Vancouver, Victoria, Burnaby): 5 to 9 days
• Alberta (Calgary, Edmonton, Red Deer): 5 to 9 days
• Manitoba (Winnipeg, Brandon): 5 to 9 days
• Saskatchewan (Saskatoon, Regina): 5 to 9 days
• Nova Scotia (Halifax, Sydney): 5 to 9 days
• New Brunswick (Moncton, Fredericton): 5 to 9 days
• Newfoundland and Labrador (St. John's, Corner Brook): 7 to 14 days
• Prince Edward Island (Charlottetown): 7 to 14 days
• Yukon, Northwest Territories, Nunavut: 7 to 14 days

All shipments are packed discreetly with no branding or indication of contents on the outside.

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