ursodeoxycholic acid

Action and Spectrum

Actions and Spectrum

Ursodeoxycholic acid acts by reducing the production of cholesterol in the liver thereby enhancing the bile acid secretion. This further helps in the improvement of liver conditions and prevents the formation of gallstones.UDCA is also known to possess anti-inflammatory and cytoprotective properties.

Drug Interaction

Adverse Reaction

Frequency not defined

Pain in the abdomen

Pasty stools

Rashes

Diarrhea

Indigestion

Headache

Constipation

Sleep disturbances

Dry skin

Bronchitis

Dyspepsia

Flatulence

Loss of hair

Pain in chest

Black Box Warning

Black Box Warning

In case of liver disease, use with caution

Contraindication / Caution

Contraindication/Caution:

Contraindication

Frequent recurrence of biliary colic

Non-functioning gall bladder

Inflammatory diseases

Radio-opaque stones

Unsuccessful portoenterostomy

Caution

Liver disease

Hepatic encephalopathy

Liver bleeding disorder

Pregnancy / Lactation

Pregnancy/Lactation

Pregnancy consideration: 

Not recommended for use in pregnancy. Benefits should outweigh the risks before prescribing to pregnant women.

Lactation: 

Data about the excretion of ursodeoxycholic acid into breast milk is not known.

Pregnancy category: 

• Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
• Category B: There was a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.
• Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology

Ursodeoxycholic acid is a bile acid that occurs naturally. It is used in the treatment of certain diseases of gall bladder and liver.

Pharmacodynamics

UDCA is a hydrophilic bile acid with choleretic, cytoprotectant, and immunomodulating effects. Ursodeoxycholic acid enhances the flow of bile acids and promotes bile acid secretion.

Pharmacokinetics

Absorption

Ursodeoxycholic acid is absorbed incompletely following oral administration.

Distribution

Small amounts of ursodeoxycholic acid are distributed in the small intestine and gall bladder.

70% of unconjugated UDCA is bound to plasma proteins.

Metabolism

Ursodeoxycholic acid undergoes hepatic metabolism via conjugation with taurine or glycine. Taurine or glycine conjugates are absorbed in the small intestine through active or passive mechanisms.

Unabsorbed UDCA undergoes 7-dehydroxylation in the colon to lithocholic acid by intestinal bacteria. Some quantity of ursodeoxycholic acid epimerizes to chenodeoxycholic acid through 7-oxo intermediate.

Elimination and excretion

UDCA is primarily excreted in feces. Elimination through the renal route is a minor pathway.

Half-life:

3.5 to 5.8 days

Adminstartion

Administration

Take ursodeoxycholic acid tablets or capsules orally with meals.

The suspension should not be used for more than four months when once opened.

Shake the suspension well before use.

Patient Information Leaflet

Patient information leaflet

Generic Name: ursodeoxycholic acid

Why do we use ursodeoxycholic acid?

Ursodeoxycholic acid is a natural bile acid. It is indicated in treating problems of gall bladder and liver. UDCA is indicated in treating primary biliary cholangitis, cystic fibrosis in children of age 6-18 years, TPN-induced cholestasis in children, and dissolution of gall bladder.