Samarin

Samarin

silymarin

Manufacturer:

Berlin Pharm

Distributor:

Berlin Pharm
Full Prescribing Info
Contents
Silymarin.
Description
Samarin 70: Each tablet contains Silymarin 70 mg.
Samarin 140: Each tablet contains Silymarin 140 mg.
Action
Pharmacodynamics: Mechanism of Action: Silymarin, a flavonoid extract of milk thistle, is extracted from the seeds and fruit of Silybum marianum and in reality is a mixture of three structure components: silibinin, silydianine and silychristine. Silymarin has been shown to have hepatoprotective actions against chemical, infectious and environmental toxins. It has antioxidant, antihepatitis and anticirrhotic effects.
Flavonoids including Silymarin are good antioxidants due to their phenolic structure. They also act as plasma membrane stabilizer.
Silymarin is an antioxidant free-radical scavenger. It was postulated that free-radical scavenger and antioxidant activity of silymarin may be the mechanism of hepatotoxicity protection.
Silymarin is thought to protect the liver by altering the liver cell's outer membrane thus inhibiting the entrance of various toxins and blocking toxin-binding sites.
Silymarin influences the cell membranes, prohibiting the inflow of cell toxins like amanitin and phalloidin as well as loss of cell constituents (transaminases, potassium) from the cell body. This "stabilization" of cell membranes is supported by the antiperoxidative properties of silymarin, which is related to its radical scavenger. Thus, the pathophysiological cycle of lipid peroxidation responsible for damaging membranes is interrupted.
Silymarin increase intracellular concentrations of glutathione which is used by many detoxification systems in liver cells.
Silymarin inhibits lipid peroxidation of hepatocyte, microsomal, and erythrocyte membranes as well as increasing hepatocyte protein synthesis via stimulation of ribosomal RNA and increased regenerative capacity of liver cells. Furthermore, silymarin leads to increased formation of ribosomal RNA by stimulating the activity of RNA - polymerase I in the nucleus.
Silymarin is thought to exert an antiinflammatory response via inhibition of leukotriene production. This anti-inflammatory effect may be beneficial in treating liver cirrhosis or fibrosis.
Silymarin is used for the treatment of numerous liver disorders characterized by degenerative necrosis and functional impairment. Silymarin has been documented in clinical trials in terms of improvement of liver function.
Pharmacokinetics: Silymarin is not soluble in water, absorption after oral administration is rather poor. In human, the proportion absorbed from the intestine, as measured from renal and biliary elimination, was between 20%-40% of a single dose of 140 mg Samarin. Absorption is rapid with maximum biliary excretion reached in human subjects between 2 and 4 hours. After repeated therapeutic doses of Samarin (140 mg 3 times a day), the levels of silibinin found in human bile are the same as after a single dose. This finding shows that silibinin has no tendency to accumulate.
Peak plasma concentrations are achieved in 4 to 6 hours.
Silymarin is mainly excreted in the bile (>80% of the amount absorbed) and, to a lesser degree, in the urine. Its elimination half-life ranges from 6 to 8 hours. Silymarin and other components of silymarin are rapidly conjugated with sulfate and glucuronic acid in the liver. The conjugate pass into the plasma and into the bile, where they are found in amounts corresponding to 80% of the total dose administered. The metabolites detected in the bile are glucuronides and sulfates.
Indications/Uses
Acute and chronic hepatitis; Liver cirrhosis; Non-alcoholic fatty liver disease (NAFLD) / Non-alcoholic steatohepatitis (NASH); Infective hepatitis; Alcoholic liver disease.
Dosage/Direction for Use
Recommended Doses: Hepatoprotection: 420 mg/day divided into 3 doses for 6 to 8 weeks then a maintenance dose of 280 mg/day.
Mode of Administration: Oral.
Overdosage
Silymarin overdose information is limited. Treatment is symptomatic and supportive. Acute toxicity has not been reported after silymarin overdose. Gastrointestinal decontamination is generally not indicated except after very large ingestions or exposures where more toxic co-ingestants are involved.
Contraindications
Known hypersensitivity to silymarin or any of its components.
Special Precautions
Silymarin may inhibit cytochrome P450 2C9 and CYP450 3A4; but no effect on pharmacokinetics of indinavir in human studies. Silymarin may decrease blood glucose in patients with cirrhosis and diabetes.
Use In Pregnancy & Lactation
Pregnancy: Silymarin has been used to treat mothers with intrahepatic cholestasis of pregnancy for up to 3 weeks.
Lactation: Scientific evidence for the safe use during lactation is not available.
Adverse Reactions
Silymarin is usually well tolerated. Nausea, headache, diarrhea, dyspepsia, flatulence, abdominal bloating, fullness or pain, and anorexia have been reported. Allergic reactions to silymarin may occur.
Drug Interactions
Metronidazole: The concomitant administration of silymarin and metronidazole significantly accelerated the total body clearance of metronidazole and significantly reduced metronidazole exposure. If concomitant use is necessary, the dose of metronidazole may need to be increased.
Storage
Store below 30°C.
MIMS Class
Cholagogues, Cholelitholytics & Hepatic Protectors
ATC Classification
A05BA03 - silymarin ; Belongs to the class of drugs used in liver therapy.
Presentation/Packing
Form
Samarin FC tab 140 mg
Packing/Price
10 × 10's;25 × 10's
Form
Samarin FC tab 70 mg
Packing/Price
10 × 10's;25 × 10's
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