Ursidesox
Ursidesox Uses, Dosage, Side Effects, Food Interaction and all others data.
Ursidesox is a naturally occurring bile acid used to treat different hepatobilliary disorders. The activity of Ursidesox is achieved through a decrease in secretion of cholesterol in bile. Ursidesox achieves this through a few mechanisms: it reduces cholesterol absorption, suppresses liver cholesterol synthesis and it does not inhibit bile acid synthesis.
Therefore, alters bile composition from supersaturated to unsaturated. Ursidesox also promotes the formation of liquid cholesterol crystal complexes which enhance removal of the cholesterol from the gallbladder into the intestine to be expelled. Ursidesox improves cholestatic liver diseases by-
Protecting cholangiocytes against cytotoxicity of hydrophobic bile acidsStimulating hepatobilliary secretionProtecting hepatocytes against bile acid-induced apoptosisUrsidesox is completely absorbed in the upper intestine. Time to peak serum concentration varies from 30 to 150 minutes. The rate of absorption ranges from 60-80%. After absorption Ursidesox enters the portal vein and undergoes extraction from portal blood by liver where it is conjugated with amino acid & that may be either glycine or taurine and then secreted into the hepatic bile ducts. Small quantities of Ursidesox appear in the circulation and very small amounts are excreted into urine. The biologic half life of Ursidesox ranges from 3.5-5.8 days.
Ursodiol (commonly known as ursodeoxycholic acid) is a product of metabolism of bacteria in the intestine. It is considered a secondary bile acid. The other type of bile acid, primary bile acids, are produced hepatically and subsequently stored in the gallbladder. When primary bile acids are secreted into the large intestine, they can be broken down into secondary bile acids by bacteria present in the intestine. Both types of bile acids assist in the metabolism of dietary fat. Ursodeoxycholic acid regulates cholesterol levels by slowing the rate at which the intestine is able to absorb cholesterol and also acts to break down micelles, which contain cholesterol. Because of this property, ursodeoxycholic acid is used to treat gall stones non-surgically.
| Trade Name | Ursidesox |
| Generic | Ursodeoxycholic Acid |
| Ursodeoxycholic Acid Other Names | Acide ursodesoxycholique, Acido ursodeossicolico, Acido ursodeoxicolico, Acidum ursodeoxycholicum, UDCA, Ursodeoxycholate, Ursodeoxycholic acid, Ursodiol |
| Type | |
| Formula | C24H40O4 |
| Weight | Average: 392.572 Monoisotopic: 392.292659768 |
| Groups | Approved, Investigational |
| Therapeutic Class | Anti-gallstones drugs: Bile Acids |
| Manufacturer | |
| Available Country | Argentina |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Ursidesox is used for the treatment of Cholestasis (Jaundice), Viral Hepatitis, Alcoholic Fatty Liver, Primary Billiary Cirrhosis (PBC), Primary Sclerosing Cholangitis (PSC), Dissolution of Gallstones and Non-Alcoholic Steato Hepatitis (NASH).
Ursodeoxycholic acid is used to reduce the cholesterol saturation of bile and to promote the dissolution of gallstones. The cholesterol saturation of bile is reduced by Ursodeoxycholic acid, allowing gradual solubilization of cholesterol gallstones. Cholesterol of secretion into bile is reduced and bile acid secretion rate is increased during Ursodeoxycholic acid treatment without a reduction in phospholipids.
Ursidesox is also used to associated treatment for these conditions: Primary Biliary Cholangitis, Gallstone formation
How Ursidesox works
Ursodeoxycholic acid reduces elevated liver enzyme levels by facilitating bile flow through the liver and protecting liver cells. The main mechanism if anticholelithic. Although the exact process of ursodiol's anticholelithic action is not completely understood, it is thought that the drug is concentrated in bile and decreases biliary cholesterol by suppressing hepatic synthesis and secretion of cholesterol and by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution.
Dosage
Ursidesox dosage
Dissolution of Gall stones: 8-12 mg/kg/day either as single night time dose or in divided doses
PBC: 10-15 mg/kg/day in 2-4 divided doses
Acute Viral Hepatitis: 600 mg/day
Alcoholic Fatty Liver: 300 mg/day
PSC: 25-30 mg/kg/day
NASH: 13-15 mg/kg/day
Side Effects
Commonly reported side effects are nausea, vomiting, diarrhoea, gallstone opacilication, pruritus.
Toxicity
Neither accidental nor intentional overdosing with ursodeoxycholic acid has been reported. Doses of ursodeoxycholic acid in the range of 16-20 mg/kg/day have been tolerated for 6-37 months without symptoms by 7 patients. The LD50 for ursodeoxycholic acid in rats is over 5000 mg/kg given over 7-10 days and over 7500 mg/kg for mice. The most likely manifestation of severe overdose with ursodeoxycholic acid would probably be diarrhea, which should be treated symptomatically.
Precaution
It should be used cautiously in those with liver disease.
Interaction
Ursidesox should not be used with drugs, such as oestrogenic hormones, that increase bile cholesterol. Concomitant administration with bile-acid binding drugs including antacids, charcoal and cholestyramine should be avoided, since this may reduce the effectiveness of therapy with Ursodeoxycholic acid.
Food Interaction
- Take with food.
Elimination Route
Only small quantities of ursodiol appear in the systemic circulation and very small amounts are excreted into urine. Eighty percent of lithocholic acid formed in the small bowel is excreted in the feces, but the 20% that is absorbed is sulfated at the 3-hydroxyl group in the liver to relatively insoluble lithocholyl conjugates which are excreted into bile and lost in feces.
Pregnancy & Breastfeeding use
Pregnancy category B. No evidence of harm has been reported in pregnancy. It has been effectively used for the treatment of cholestasis of pregnancy during the last trimester without any side effects. Problems have not been documented in humans regarding breast feeding.
Contraindication
Non-functioning gall-bladder calcified and pigmented gallstones, inflammatory bowel disease.
Storage Condition
Store below 25° C. Protected from light and moisture. Keep the medicine out of the reach of children.
Innovators Monograph
You find simplified version here Ursidesox
FAQ
What is Ursidesox used for?
Ursidesox usued to prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones. It has a role as a human metabolite and a mouse metabolite.
How safe is Ursidesox?
Ursidesox appears to be a safe and effective alternative to surgery in selected patients with gallstones. Ursidesox use to safe if you are not allergic to it.
What are the common side effects Ursidesox ?
Common side effects of Ursidesox are include:
Stomach upset, nausea, diarrhea, dizziness, back pain, hair loss, or cough may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
What does Ursidesox do to my body?
Ursidesox works by reducing the amount of cholesterol released by your liver and by slowly dispersing the cholesterol.
How long should Ursidesox be taken?
For the first 3 months of treatment Ursidesox should be taken divided over the day. The use of Ursidesox capsules in PBC may be continued indefinitely.
Is Ursidesox safe during pregnancy?
Ursidesox is effective and safe in patients with intrahepatic cholestasis of pregnancy of early onset, attenuating pruritus and correcting some biochemical abnormalities in the mothers.
Is Ursidesox safe during breastfeeding?
Because of the low levels of Ursidesox in breastmilk, amounts ingested by the infant are small and are not expected to cause any adverse effects in breastfed infants.No special precautions are required.
Can I drink alcohol with Ursidesox?
Avoid alcoholic drinks when taking Ursidesox. Alcohol may change how the drug is released in your body. This may cause more side effects or cause the drug to become less effective
When is the best time to take Ursidesox?
Ursidesox is usually taken once daily at bedtime. Sometimes your doctor may suggest you take two doses each day, in which case, take your last dose of the day at bedtime. If you are taking Ursidesox for primary biliary cholangitis, it is likely that you will be asked to take 2-4 doses daily.
How long does it take for Ursidesox to work?
Ursidesox take for up to two years for the treatment of gallstones. Once the gallstones have dissolved, your doctor may continue your treatment for three to four months to ensure that they have completely cleared up.
Does Ursidesox cause weight gain?
People gain an average of 2.3kg during the first year of taking Ursidesox, although there's not usually any more weight gain after this.
Can Ursidesox cause kidney problems?
Ursidesox may reduces albuminuria and prevent progression of kidney damage.
When should I take Ursidesox?
It is best to take Ursidesox with meals, unless otherwise directed by your doctor. Take this medicine for the full time of treatment, even if you begin to feel better.
Is Ursidesox a steroid?
Ursidesox is a steroid bile acid approved for primary biliary cirrhosis.
Will Ursidesox affect my fertility ?
Ursidesox could help achieve conception in infertile women with primary biliary cirrhosis.
Will Ursidesox affect my contraception?
Ursidesox does not affect ethinylestradiol bioavailability in women taking oral contraceptives.
What are the indications of Ursidesox?
Ursidesox is indicated in the treatment of primary biliary cirrhosis (PBC) and for the dissolution of radiolucent gallstones in patients with a functioning gall bladder.
Where does Ursidesox come from?
Produced in humans and most other species from metabolism by intestinal bacteria.
Who should not take Ursidesox?
You should not use if you are allergic to it or have an obstruction in your liver or gallbladder.
What happens if I stop taking Ursidesox?
If you stop taking Ursidesox too soon, the gallstones may not dissolve as fast or may not dissolve at all. It is thought that body weight and the kind of diet the patient follows may affect how fast the stones dissolve and whether new stones will form.
