Generic Actigall (Ursodeoxycholic acid)

Introduction

Actigall is a prescription medication that contains the bile acid ursodeoxycholic acid (UDCA). It is supplied as 300 mg oral tablets and belongs to the class of bile acid therapeutics. The drug is approved primarily for the treatment of primary biliary cholangitis (PBC) and for the dissolution of radiolucent cholesterol gallstones in patients who are not suitable candidates for surgery. In addition, limited clinical evidence supports its use in certain forms of cholestatic liver disease, although those applications remain off-label.

What is Actigall?

Actigall is a brand of ursodeoxycholic acid, a naturally occurring secondary bile acid that has been chemically synthesized for therapeutic use. The medication is marketed by ActiPharma (formerly Shire) in the United States and is approved by the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the indications listed above.

• Classification: Bile acid; hepatoprotective agent.
• Development history: Ursodeoxycholic acid was first isolated from bear bile and later synthesized in the s. Clinical trials in the s demonstrated its ability to improve cholestasis, leading to FDA approval of the brand Actigall in 1997.
• Related brand names: The same active compound is marketed under several other trademarks, including Urso, Ursodiol, Ursocol, and Zytegra.

How Actigall Works

Ursodeoxycholic acid is a hydrophilic bile acid that replaces more toxic, hydrophobic bile acids within the enterohepatic circulation. Its therapeutic actions are threefold:

1. Cholagogue effect - UDCA stimulates bile flow by up-regulating the expression of bile salt export pump (BSEP) and multidrug-resistance protein 3 (MDR3), reducing intra-hepatic cholestasis.
2. Cytoprotective effect - The molecule protects cholangiocytes and hepatocytes from detergent-induced injury by stabilising cell membranes and decreasing oxidative stress.
3. Litholytic effect - UDCA reduces cholesterol saturation of bile, promoting the gradual dissolution of cholesterol-rich gallstones.

Pharmacokinetically, UDCA is absorbed primarily in the distal ileum (≈ 40 % oral bioavailability), reaches peak plasma concentrations within 2-3 hours, and is extensively conjugated with glycine or taurine before biliary excretion. The elimination half-life is about 3-5 hours, and steady-state concentrations are attained after 5-7 days of twice-daily dosing.

Conditions Treated with Actigall

• Primary biliary cholangitis (PBC):
  • Actigall improves biochemistry (alkaline phosphatase, bilirubin) and delays disease progression when administered at 13-15 mg/kg/day in two divided doses.
• Dissolution of cholesterol gallstones:
  • A regimen of 8-10 mg/kg/day for up to 2 years can reduce stone size or achieve complete dissolution in patients with functional gallbladders who cannot undergo cholecystectomy.

The drug’s efficacy in these conditions is supported by multiple randomized controlled trials and is reflected in the FDA-approved labeling.

Off-Label and Investigational Uses of Actigall

• Intra-hepatic cholestasis of pregnancy (ICP): Small pilot studies suggest that UDCA may lower maternal serum bile acids and improve fetal outcomes, but the FDA has not approved this indication.
• Primary sclerosing cholangitis (PSC): Observational data indicate modest biochemical improvement; however, no large-scale trial has demonstrated a clear clinical benefit.
• Non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH): Early-phase trials have explored UDCA as part of combination therapy, yet results remain inconclusive.

All off-label applications should be pursued only under direct supervision of a qualified healthcare professional because safety and efficacy are not formally established by regulatory agencies.

Is Actigall the Right Medication for You?

Actigall is most appropriate for adults who have:

• A confirmed diagnosis of primary biliary cholangitis with elevated cholestatic liver enzymes.
• Radiolucent cholesterol gallstones and a functional gallbladder, when surgery is contraindicated or declined.

The medication is not recommended for:

• Patients with complete biliary obstruction or severe hepatic failure (e.g., decompensated cirrhosis).
• Individuals with known hypersensitivity to ursodeoxycholic acid or any tablet excipients.
• Pregnant or breastfeeding women unless the benefits outweigh potential risks and the prescriber deems it necessary.

Clinical judgment, liver function tests, and imaging studies guide the decision to initiate therapy.

Risks, Side Effects, and Interactions

Common

• Diarrhea
• Nausea or vomiting
• Abdominal discomfort (cramping, dyspepsia)
• Fatigue
• Mild headache

These events are generally transient and improve with continued therapy or dose adjustment.

Rare

• Skin rash or pruritus
• Elevated serum amylase (possible pancreatic irritation)
• Dizziness or vertigo

Patients experiencing these symptoms should contact a clinician for evaluation.

Serious

• Hepatotoxicity: Although rare, severe liver injury may present with jaundice, markedly elevated transaminases, and coagulation abnormalities.
• Severe hypersensitivity reactions: Including Stevens-Johnson syndrome or anaphylaxis, requiring immediate emergency care.
• Pancreatitis: Persistent abdominal pain with elevated lipase/amylase warrants urgent assessment.

Drug-Drug and Drug-Food Interactions

• Cholestyramine, colestipol, or other bile-acid sequestrants: Significantly decrease UDCA absorption; separate administration by at least 4 hours.
• Warfarin: UDCA may potentiate anticoagulant effect; monitor INR more frequently.
• Cyclosporine: Potential for increased nephrotoxicity; assess renal function regularly.
• Antacids (aluminum, magnesium): May reduce bioavailability; take UDCA with water, preferably on an empty stomach.

Patients should disclose all concurrent medications, supplements, and herbal products.

Use: Dosing, Missed Dose, Overdose

Standard dosing:

• PBC: 13-15 mg/kg/day divided into two doses (e.g., 300 mg tablet taken twice daily).
• Gallstone dissolution: 8-10 mg/kg/day divided into two doses.

Doses are adjusted based on body weight and treatment response; physicians may order liver function tests after 3-6 months to confirm efficacy.

Missed dose: If a dose is forgotten, take it as soon as remembered provided the next scheduled dose is not less than 4 hours away. Do not double the dose to compensate for a missed tablet.

Overdose: Symptoms of acute overdose are uncommon but may include nausea, vomiting, and diarrhea. Management is supportive: encourage hydration, monitor liver enzymes, and seek medical attention if symptoms are severe or persist.

Practical precautions:

• Take tablets with a full glass of water; food may delay absorption but does not affect overall exposure.
• Avoid excessive alcohol consumption, as it may enhance hepatotoxic risk.
• Do not operate heavy machinery or drive if you experience dizziness or significant gastrointestinal upset.

FAQ

• What should I do if my Actigall tablets become discolored?

  • Check the expiration date and storage conditions first. Discoloration may indicate degradation; discard the product and obtain a new supply from a reputable source.

• Can I travel internationally with Actigall?

  • Yes, but keep the medication in its original packaging with a copy of the prescription (or a physician’s letter) to satisfy customs regulations in many countries.

• Does Actigall interact with citrus juices?

  • Unlike some antibiotics, UDCA is not significantly affected by grapefruit or other citrus juices, but taking the tablet with plain water is still recommended.

• Are there differences in inactive ingredients between regions?

  • Formulations may contain varying fillers such as lactose, magnesium stearate, or microcrystalline cellulose. Patients with specific excipient allergies should review the product label for their locale.

• How long does it take for gallstones to dissolve with Actigall?

  • Clinical studies report a median dissolution time of 12-24 months, depending on stone size, composition, and patient adherence.

• Is Actigall safe for patients with mild renal impairment?

  • UDCA is primarily eliminated via the bile; however, severe renal dysfunction can alter drug handling. Dose adjustments are usually unnecessary for mild impairment but should be discussed with a clinician.

• Can Actigall affect routine laboratory tests?

  • Yes, it may modestly raise alkaline phosphatase and bilirubin values, which can be misinterpreted as liver pathology if the clinician is unaware of therapy.

• What storage conditions are optimal for Actigall?

  • Store at 20-25 °C (68-77 °F) in a dry place, away from direct sunlight and moisture. Extreme temperatures can degrade the tablet’s potency.

• Does the medication have any impact on pregnancy testing?

  • There is no evidence that UDCA interferes with urine or serum hCG assays, but clinicians should be informed of all medications before testing.

• Is it possible to split a 300 mg tablet to adjust dosing?

  • The tablets are not scored; splitting may lead to uneven dosing. If a lower dose is required, a prescriber should prescribe an alternative strength or adjust the dosing interval.

Glossary

Ursodeoxycholic acid

A hydrophilic bile acid used therapeutically to improve cholestasis and dissolve cholesterol gallstones.

Primary biliary cholangitis (PBC)

An autoimmune disease characterized by progressive destruction of the small bile ducts, leading to cholestasis and, eventually, cirrhosis.

Cholestasis

A condition in which bile flow from the liver is impaired, causing accumulation of bile acids in the bloodstream.

Litholysis

The pharmacologic dissolution of solid gallstones into soluble components.

Buying Actigall from Our Online Pharmacy

Patients who encounter limited availability or high out-of-pocket costs through conventional pharmacies can obtain Actigall from our online pharmacy.

• Cost efficiency: We source the generic formulation at prices close to the manufacturer’s wholesale cost, resulting in a lower retail price for the consumer.
• Verified quality: Every batch is procured from licensed, GMP-certified suppliers and undergoes third-party testing to confirm potency and purity.
• Discreet delivery: Orders are packaged in unbranded, tamper-evident containers and shipped via secure carriers; standard express shipping arrives within 7 days, while regular airmail typically takes 2-3 weeks.
• Global access: As a pharmacy-broker service, we collaborate with overseas licensed pharmacies, allowing patients in regions without local availability to receive the medication legally and safely.

By choosing our online pharmacy, you gain a reliable, private, and affordable pathway to maintain your prescribed therapy when traditional channels fall short.

Disclaimer

The details presented about Actigall are intended for general educational purposes and do not substitute for professional medical advice. Treatment decisions, including any off-label applications, must be made under the supervision of a qualified health-care provider. Readers are presumed to be responsible adults capable of making informed health choices. Our online pharmacy supplies Actigall to individuals who may face limited access through standard pharmacies or insurance plans and who seek a cost-effective generic alternative. Always discuss with a clinician before initiating, altering, or stopping any medication.