Clinical and pharmacological group: & nbsp

Vitamins and vitamin-like remedies

Hepatoprotectors

Included in the formulation
  • Essley Forte®
    capsules inwards 
    NIZHFARM, JSC     Russia
  • АТХ:

    A.11.A.B   Multivitamins in other combinations

    Pharmacodynamics:

    The effect of the drug due to the properties of its constituent thiamine, riboflavin, pyridoxine, alpha-tocopheryl acetate, cyanocobalamin, vitamin E, nicotinamide, phospholipids.

    "Essential" phospholipids - complex substances which are esters of phosphatidic diglycerides and unsaturated fatty acids (mainly oleic and linoleic). They are an important structural element of cell membranes and membranes of organelles of hepatocytes. Phospholipids regulate the permeability of membranes, the activity of membrane-bound enzymes, ensuring normal processes of oxidative phosphorylation.

    The drug normalizes the biosynthesis of phospholipids and total lipid metabolism in hepatocyte lesions of various etiologies.

    Restores membrane hepatocyte regeneration by structural and due to competitive inhibition of oxidative processes: incorporating into biomembranes, unsaturated fatty acids are able to assume toxigenic exposure instead of membrane lipids.

    Promotes the regeneration of liver cells, stabilizes the physico-chemical properties of bile.

    Thiamine (vitamin B1) as a coenzyme participates in carbohydrate metabolism.

    Riboflavin (vitamin B2) - the most important catalyst in the processes of cellular respiration.

    Pyridoxine (vitamin B6) as a coenzyme takes part in the metabolism of amino acids and proteins.

    Cyanocobalamin (vitamin B12) together with folic acid is involved in the synthesis of nucleotides.

    Nicotinamide (vitamin PP) is involved in the processes of tissue respiration, fat and carbohydrate metabolism.

    Tocopherol (vitamin E) has antioxidant properties, provides protection of unsaturated fatty acids in membranes from lipid peroxidation.

    Pharmacokinetics:

    Essential phospholipids are well absorbed in the gastrointestinal tract, including in the form of biologically active products of their hydrolysis by digestive enzymes, which are transported through the intestinal wall into the lymphatic channel. In the liver, a partial resynthesis of phosphatidylcholine from the products of hydrolysis occurs. Essential phospholipids are excreted from the body mainly during defecation, a small part with urine.

    Nicotinamide: Absorption is fast and complete, 60-70% of the dose taken internally. Low fat foods increase bioavailability. Biotransformation in the liver.Half-life 45 min. Elimination by the kidneys (in the form of a metabolite, to a lesser extent - unchanged).

    Pyridoxine: metabolized in the liver with the formation of pharmacologically active metabolites (pyridoxalphosphate and pyridoxamino phosphate). Distribution is predominantly in the muscles, liver and CNS. Penetrates through the placenta and into the mother's milk. It is excreted by the kidneys (with intravenous injection with bile - 2%).

    Riboflavin: absorption rapid (in the duodenum). Relationship with plasma proteins 60%. Biotransformation in the liver. Half-life 66-84 min. Elimination of the kidneys in the form of metabolites, in high doses - in unchanged form.

    Thiamine: aAbsorption full (in the duodenum), alcohol hampers the absorption of vitamin B1. The connection with plasma proteins is low. Biotransformation (phosphorylation) in the liver; active metabolite - thiamine pyrophosphate (cocarboxylase). Elimination by the kidneys (metabolites and unchanged) and with feces.

    Vitamin E (tocopherol): when taken orally, the absorption is 50%; in the process of absorption forms a complex with lipoproteins (intracellular carriers of tocopherol). Absorption requires the presence of bile acids. Associated with alpha1- and beta-lipoproteins, in part - with serum albumin. If there is a violation of protein metabolism, transport is difficult. Maximum concentration is achieved after 4 hours. It is deposited in the adrenal glands, pituitary gland, testes, adipose and muscle tissue, erythrocytes, liver. More than 90% is excreted with bile, 6% - with kidneys. The period of semi-elimination of the drug is about 20 hours.

    Indications:
    • Radiation sickness
    • Psoriasis (as part of complex therapy)
    • Fatty degeneration of the liver of various etiologies
    • Hepatitis
    • Cirrhosis of the liver
    • Toxic liver disease (including alcohol, narcotic, drug etiology)
    • NARlipid exchange liver

    I.B15-B19.B19   Viral hepatitis, unspecified

    XI.K70-K77.K70   Alcoholic liver disease

    XI.K70-K77.K71   Toxic liver disease

    XI.K70-K77.K72.9   Hepatic failure, unspecified

    XI.K70-K77.K74   Fibrosis and cirrhosis of the liver

    XI.K70-K77.K76.0   Fatty degeneration of the liver, not elsewhere classified

    XII.L40-L45.L40   Psoriasis

    XIX.T36-T50.T40   Poisoning and Drug psychodysleptics [hallucinogens]

    XIX.T36-T50.T50   Poisoning with diuretics and other unspecified drugs, medications and biological substances

    XIX.T51-T65.T51   Toxic effect of alcohol

    XXI.Z40-Z54.Z51.0   Radiotherapy course (supportive)

    XXI.Z40-Z54.Z51.1   Chemotherapy for neoplasm

    XXI.Z55-Z65.Z58.4   Impact of radiation contamination

    Contraindications:
    • Hypersensitivity
    • Cholestasis
    • Empyema of the gallbladder
    • Children under 16 years old
    Carefully:

    Pregnancy, feedlBreastfeeding.

    Pregnancy and lactation:

    Category FDA not determined. The use of the drug during pregnancy is possible only on the recommendation of a doctor if the expected benefit for the mother exceeds the potential risk to the fetus. If you need to take the drug during lactation, it is recommended that you decide whether to stop breastfeeding.

    Dosing and Administration:

    Orally 2 capsules 2-3 times a day during meals, swallowing whole with enough water. The course of treatment is 3 months. For psoriasis - 2 capsules 3 times a day, the course is 2 weeks.

    Side effects:
    • Discomfort in epigastrium
    • Allergic reactions
    • Gas formation
    • Heartburn
    • Nausea
    • Diarrhea
    • Staining of urine in a dark yellow color (due to the content of B vitamins).
    Overdose:

    Not described, treatment is symptomatic.

    Interaction:

    Nicotinamide: with alcohol - skin rashes and itching are possible. When combined with colestyramine, the absorption of nicotinamide, which is part of the combination multivitamins + phospholipids. It is recommended to observe the interval of 4-6 hours between the reception of these drugs.

    Pyridoxine: the physiological function of vitamins B1 and B6 is the potentiation of the actions of each other, manifested in a positive effect on the nervous, muscular and cardiovascular systems. With simultaneous use with hormonal contraceptives, an increase in the concentration of pyridoxine in the blood plasma is possible. With simultaneous use, potentiates the action of diuretics.

    When combined with levodopa, the effects of levodopa are reduced or completely inhibited. With simultaneous use with isonicotinhydrazide, penicillamine, cycloserine, a decrease in the effectiveness of pyridoxine is possible. With simultaneous use with phenytoin, phenobarbital, the concentrations in the blood plasma of phenytoin and phenobarbital may decrease.

    Riboflavin: when used simultaneously with m-holinoblokatorami, absorption and bioavailability of riboflavin increases (due to a decrease in intestinal motility).

    With simultaneous use with thyroid hormones, metabolism of riboflavin is accelerated.

    With simultaneous use decreases the activity of doxycycline, tetracycline, oxytetracycline, erythromycin and lincomycin.

    Riboflavin is not compatible with streptomycin.

    With simultaneous use, the side effects of chloramphenicol are reduced and prevented (violation of hemopoiesis, optic neuritis).

    With simultaneous application chlorpromazine, amitriptyline due to blockade of flavinokinase, the incorporation of riboflavin into flavinadenine mononucleotide and flavinadenine dinucleotide is disrupted and its excretion in the urine is increased.

    Thiamine: ethanol sharply reduces the absorption of thiamine (concentration in the blood can decrease by 30%). Long-term treatment with anticonvulsant drugs can lead to a thiamine deficiency. Thiamine completely disintegrates in solutions containing sulfites. Thiamine is unstable in alkaline and neutral solutions; the appointment with carbonates, citrates, barbiturates, copper preparations is not recommended.

    Tocopherol: when used simultaneously with tocopherol, the effects of warfarin and dicumarol may change.

    There are reports of a decrease in the effectiveness of simultaneous treatment with iron in children.

    With simultaneous application of tocopherol with cyclosporin, the absorption of cyclosporin increases.

    Special instructions:

    Impact on the ability to drive vehicles and manage mechanisms not found.

    Instructions
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