MINISTRY OF PUBLIC HEALTH OF THE REPUBLIC OF BELARUS
Stamp:
Agreed by
the Ministry of Public Health of the Republic of Belarus
Order of the Ministry of Public Health of the Republic of Belarus
from 27.01.2011 No 63
committee on drugs No 1 from 10.01.2011
INSTRUCTION
(core data sheet for specialists)
for medical application of
Gepsile-Rn®
Reg. No.: R
Description of the drug
Trade name: Gepsile-Rn®
International nonproprietary name: Silymarin
General description
Gepsile-Rn® (Silymarin), 35 mg. Biconvex round-shaped coated tablets of brown color; some
inclusions on the surface are admissible.
Ingredients
Each tablet contains
active pharmaceutical ingredient: dry extract of milk thistle seeds equal to 35 g of silymarin;
auxiliary components: microcrystalline cellulose, lactose, sodium starch glycollate,
magnesium stearate, povidone; film coat: partially hydrolised polyvinyl alcohol, macrogol
350, talc, iron oxide yellow, iron oxide red, iron oxide black, titanium dioxide.
Dosage form
Coated tablets
ATC class: A05B A03
Pharmacotherapeutic class:
Drugs, used for the treatment for liver and bile passages disorders. Hepatotrophic agents.
Silymarin.
Pharmacological properties
Pharmacodynamics
Hepatoprotector. It’s a phytogenic drug, made from the plant Silybum marianum (Cardui
mariae fructus).
The effectiveness of this drug is provided by silymarin, which is a mixture of different
flavonoids, the most active of which is silibinin. It stimulates cell metabolism. It activates the
protein and phospholipids synthesis in hepatocytes, inhibits the destruction of cell membranes,
which prevents from the loss of the cell components and inhibits the toxins penetration into
hepatocytes.
Pharmacokinetics
Absorption and distribution
After an intake silymarin is slowly absorbed from the gastrointestinal tract (GIT). Period of
half-absorption is 2.2 hour. It isn’t cumulated in the organism.
Distribution: the drug weakly binds with plasma proteins. After a single dosing the
concentration in plasma reaches its maximum in 30 minutes.
Metabolism and excretion
It’s biotransformed in the liver by means of conjugation. More than 80% of the drug is
excreted together with bile in the form of gluconorides and sulphates. As a result of splitting
by the gut microflora, up to 40% of silymarin excreted together with bile is reabsorbed, and it
leads to the creation of the enterohepatic circulation.
Stamp:
Agreed by
the Ministry of Public Health of the Republic of Belarus
Order of the Ministry of Public Health of the Republic of Belarus
The maximum amount of excretion together with bile occurs in two hours.
Half-life is 6 hours. It’s not accumulated in the organism.
Indications and usage
- chronic liver intoxication by toxic factors, such as toxic plant protecting agents, heavy
metals and so on;
- drug-induced liver disorders (caused by some psychotropic agents, oral contraceptives,
paracetamol, some antibiotics, anesthetics);
- chronic hepatitis, liver cirrhosis of different origin, and moreover, in case of a viral
one, the drug should be prescribed as a part of a complex treatment;
- liver damage caused by alcoholism;
- as a preventive means while long-term drugs and alcohol intake, chronic intoxications
(including work-related).
Dosage and administration
Oral administration.
Adults and children over 12 years old are prescribed 4 tablets 3 times a day as the treatment
for serious liver disorders.
If the case isn’t so serious and as a means of supportive therapy, 1-2 tablets 3 times a day are
prescribed.
As a preventive measure 2-3 tablets a day are prescribed.
The tablets should be taken before meal without chewing them with a sufficient amount of
water.
Adverse reactions
The drug is well tolerated, but in rare cases adverse reactions are possible, which disappear by
themselves or after the drug withdrawal. Sometimes, when large doses are used, a slight
laxative action occurs. Very seldom an acute condition of existing vestibular diseases occurs.
The following allergic reactions in some cases are possible: skin itch, rash.
In such cases the dosing should be reduced or the drug should be withdrawn.
Contraindications
Hypersensitivity to the components of the drug.
Children under 12 years old.
Overdosage
Overdosage cases have not been reported to date.
In case of an overdosage by accident, it’s necessary to provoke vomiting, carry out gastric
lavage with the use of active carbon, and a symptomatic treatment.
Precautions
The manifestation of oestrogen-like action of silymarin can occur while use of the drug.
So the patients with hormonal disorders (endometriosis, hysteromyoma, mammary gland,
ovaries, uterus, and prostate gland carcinoma) should be prescribed the drug with some
precaution. In this case you should consult the doctor.
Administration during pregnancy and lactation
The drug can be used during pregnancy and lactation on condition that the expected positive
effect is greater than the risk of its administration.
Special instructions
During pregnancy and breast feeding the drug should be used only under doctor’s supervision.
Effects on ability to drive and use machines
The drug doesn’t influence the ability to drive and use machines.
Drug interactions
While simultaneous use of silymarin with oral contraceptives and drugs, which are used for
hormonal replacement therapy, the decrease of their effect can occur.
Silymarin inhibits P450 cytochrome system and can increase the effects of such drugs as
diazepam, alprazolam, ketoconazole, lovastatin, vinblastine.
Storage conditions
It should be stored at the temperature of 15Cº- 25°C in a dark dry place.
Keep away from children!
Shelf life is 2 years. Don’t use after the expiration date.
Conditions of sales by pharmacies
Available without prescription.
Package Description
One blister contains 10 tablets; each pack contains 3 or 5 blisters.
Information about the manufacturer:
ООО (LLC) «Rubikon» Belarus, 210002, Vitebsk, M. Gor’kogo str, 62 B,
tel/fax: +375(212) 34-06-29
The translation of this document from Russian into English is made by Alina Sasnouskaya,
translator.
Настоящий документ переведен с русского языка на английский язык мною,
переводчиком САСНОВСКОЙ АЛИНОЙ ВИКТОРОВНОЙ, достоверность перевода
подтверждаю.