Actimarin

Actimarin Uses, Dosage, Side Effects, Food Interaction and all others data.

Silymarin possess hepatoprotective and antioxidant activity. The hepatoprotective effect is due to stimulation of synthesis of structural and functional proteins and phospholipids, as well as acceleration of the regeneration of hepatocytes.

Antioxidant effect is determined by interaction of bioflavones with free radicals in the liver and its detoxication. In such manner the process of peroxidation of the lipids is interupted and further liver destruction is prevented.

Clinically, these effects are manifested by improvement of the signs and symptoms and normalization of the liver variables (serum level of transaminases, gamma-globulins, and bilirubin).

Ursodeoxycholic Acid is a naturally occurring bile acid used to treat different hepatobilliary disorders. The activity of Ursodeoxycholic Acid is achieved through a decrease in secretion of cholesterol in bile. Ursodeoxycholic Acid 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. Ursodeoxycholic Acid also promotes the formation of liquid cholesterol crystal complexes which enhance removal of the cholesterol from the gallbladder into the intestine to be expelled. Ursodeoxycholic Acid improves cholestatic liver diseases by-

Protecting cholangiocytes against cytotoxicity of hydrophobic bile acidsStimulating hepatobilliary secretionProtecting hepatocytes against bile acid-induced apoptosisUrsodeoxycholic Acid 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 Ursodeoxycholic Acid 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 Ursodeoxycholic Acid appear in the circulation and very small amounts are excreted into urine. The biologic half life of Ursodeoxycholic Acid 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.

Actimarin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Actimarin
Generic	Silymarin + Ursodeoxycholic Acid
Weight	70mg
Type	Tablet
Therapeutic Class
Manufacturer	Albert David Limited
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

For the treatment of jaundice, chronic inflammatory liver conditions, i.e. hepatitis, alcoholic liver damage and hepatic cirrhosis. It has anti-oxidant property.

Ursodeoxycholic Acid 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.

Actimarin is also used to associated treatment for these conditions: Primary Biliary Cholangitis, Gallstone formation

How Actimarin 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

Actimarin dosage

70 mg or 140 mg or 500 mg capsule should be taken 3 times daily as per the instruction of a physician. The medication should be continued until the relief of the symptoms according to the advice of a physician.

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

A mild laxative effect has occasionally been observed.

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

Ursodeoxycholic Acid 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.

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

No experience is available about the use of Silymarin 70 mg or 140 mg during pregnancy and lactation. Therefore, if needed Silymarin 70 mg or 140 mg should be taken with caution according to the physician’s advice.

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

No adequate data of investigations are available about the use of this drug in children. Therefore, it should be used in children under 12 years of age with caution under the direct supervision of a physician.

Non-functioning gall-bladder calcified and pigmented gallstones, inflammatory bowel disease.