Pharmacodynamics and pharmacokinetics
Pharmacodynamics
The membranes and organelles of liver cells are always affected in pathologies of the organ, which can lead to changes in the activity of membrane-associated enzymes and receptor systems, disruption of the metabolic function of hepatocytes and a decrease in the intensity of organ regeneration.
The EPL substance contained in the Essentiale N preparation is similar in its chemical structure to endogenous phospholipids, but is much superior to the latter due to its high PUFA content.
Being embedded primarily in the structures of cell membranes, these high-energy molecules contribute to the restoration of damaged liver tissue.
The cis-double bonds of PUFAs prevent the hydrocarbon chains in the phospholipids of the cell membranes from being parallel, as a result of which the phospholipid structure of the hepatocyte membranes becomes looser. This results in an increase in their elasticity and fluidity, as well as an increase in the rate of entry of substances into the cell and their removal from it.
Membrane-bound enzymes form functional blocks that can enhance their activity and ensure the physiological course of basic metabolic processes.
Phospholipids, by regulating lipoprotein metabolism, influence impaired metabolism , promoting the biotransformation of cholesterol and neutral fats into forms suitable for transportation and their transfer to sites of oxidation. This is achieved primarily by increasing the ability of HDL to bind to cholesterol.
When phospholipids are eliminated through the biliary tract, a decrease in the lithogenicity index and stabilization of bile .
Pharmacokinetics
When taken orally, about 90% of the dose is absorbed in the small intestine. The main part of the EPL substance, under the influence of phospholipase-A, is cleaved to 1-acyl-lysophosphatidylcholine, half of which is immediately reacylated into polyunsaturated phosphatidylcholine (PPC) during absorption in the small intestine.
PPC enters the bloodstream through the lymphatic tract and then, mainly from high-density lipid substances, is transported to the liver.
It takes 6 to 24 hours for the concentration of phosphatidylcholine in the blood The half-life of saturated fatty acids is 32 hours, for the choline component - 66 hours.
During studies of the pharmacokinetics of the drug, it was found that less than 5% of each of the administered 14C and 3H isotopes is excreted in the intestinal contents.
Essential solution for injection 250mg/5ml 5ml amp 5 pcs
Pharmacological group:
Hepatoprotective agent.
ATX code: A05C. Pharmacodynamics:
Essential phospholipids are the main elements of the structure of the cell membrane and cellular organelles. In liver diseases, there is always damage to the membranes of liver cells and their organelles, which leads to disruptions in the activity of associated enzymes and receptor systems, deterioration in the functional activity of liver cells and a decrease in the ability to regenerate.
The phospholipids included in the preparation Essentiale® N correspond in their chemical structure to endogenous phospholipids, but are superior to endogenous phospholipids in activity due to their higher content of polyunsaturated (essential) fatty acids. The integration of these high-energy molecules into damaged areas of hepatocyte cell membranes restores the integrity of liver cells and promotes their regeneration. The cis-double bonds of their polyunsaturated fatty acids prevent the parallel arrangement of hydrocarbon chains in the phospholipids of cell membranes; the phospholipid structure of the cell membranes of hepatocytes is “loosened,” which increases their fluidity and elasticity and improves metabolism.
The resulting functional blocks increase the activity of enzymes fixed on the membranes and contribute to the normal, physiological pathway of the most important metabolic processes.
Phospholipids included in the drug Essentiale® N regulate the metabolism of lipoproteins, transferring neutral fats and cholesterol to sites of oxidation, mainly by increasing the ability of high-density lipoproteins to bind to cholesterol.
Thus, there is a normalizing effect on the metabolism of lipids and proteins; on the detoxification function of the liver; to restore and preserve the cellular structure of the liver and phospholipid-dependent enzyme systems; which ultimately prevents the formation of connective tissue in the liver.
With the excretion of phospholipids into the bile, the lithogenic index decreases and the bile is stabilized.
Pharmacokinetics:
By binding mainly to high-density lipoproteins, phosphatidylcholine enters, in particular, liver cells.
The half-life of the choline component is 66 hours, and that of the unsaturated fatty acids is 32 hours.
Essentiale ampoules, instructions for use
According to the instructions for use of Essentiale N, the standard dose of the drug for patients over 12 years of age is 5-10, in severe cases - up to 20 ml/day. (10 ml of solution can be administered once).
To dilute the drug, it is recommended to use the patient’s blood in a 1:1 ratio. The drug is infused intravenously for up to 10 days.
They try to supplement (support) parenteral therapy with the administration of Essentiale capsules as early as possible.
The course of treatment usually lasts from 3 months to six months.
How to take the drug for psoriasis?
For psoriasis, treatment begins with the use of Essentiale Forte N at a dose of 1.8 g/day. (6 capsules). Treatment lasts 2 weeks, after which the patient is prescribed PUVA therapy and Essentiale N injections (10 doses of 5 ml intravenously).
Application of Essentiale in hair ampoules
Essentiale for hair is used in cases where it is necessary to strengthen weakened root bags.
The basis of the drug is fat-soluble substances, so a hair mask with Essentiale should be prepared with sour cream, kefir or egg yolks.
For short hair, a third of the volume of 1 ampoule of solution is usually enough, for long hair - half. The medicine is taken with a syringe and mixed with 1 chicken egg yolk and 1-2 teaspoons of sour cream/kefir.
Apply the mixture to clean, damp hair. The duration of exposure is 60 minutes. After this time, the composition is washed off with warm water. It is recommended to dry your hair without a hairdryer. The first 5 masks are done once a week, then to maintain the effect it is enough to repeat them once a month.
Dimexide to the mask .
Indications for use
Essentiale is a plant-based drug. Its effectiveness for the treatment and prevention of various liver pathologies has been proven in practice. Essentiale, the instructions for use indicate this, improves the antitoxic function of the organ, restores cell membranes and prevents the appearance of connective tissue in tissues.
The medicine is prescribed for the complex treatment of various liver diseases, in particular:
- Cirrhosis.
- Hepatitis A
It allows you to restore the exchange of bile and cholesterol, as well as eliminate the consequences of poor nutrition and bad habits. When taking the drug, associated positive effects are observed:
- The risks of developing atherosclerosis and blood clots are reduced.
- The level of harmful cholesterol in the blood decreases.
- The condition of the skin improves.
- Digestive function is normalized.
The indication for the drug is severe toxicosis during pregnancy. As an adjuvant therapy, it is used in the treatment of radiation syndrome and psoriasis. Injections are prescribed to patients before operations on the abdominal organs and during the recovery period after them. This allows you to minimize the risk of complications.
special instructions
If Essentiale N is infused via a dropper, in cases where the patient’s blood cannot be used for some reason, electrolyte-free solutions should be used, namely: 5% xylitol solution, 5 or 10% glucose solution in the ratio 1:1.
Only a clear solution is considered suitable for use.
Do not mix the drug in the same syringe with other drugs.
Essentiale IV should be administered very slowly. The solution is intended exclusively for intravenous infusion; injections into the muscle may cause local irritation.
The solution contains 0.6% alcohol (by volume).
Essentiale N
Essentiale N is a hepatoprotector containing essential phospholipids as an active substance, which, in turn, are the basis of cell membranes and organelles. Liver diseases are almost always accompanied by damage to these structures of liver cells, which entails a whole train of unpleasant consequences, such as disruption of the activity of enzymes and receptor blocks, deterioration of the “technical and tactical” characteristics of liver cells and a decrease in their ability to recover. The phospholipids that make up Essentiale H are almost identical to the body's own phospholipids, with a small but significant exception: they are much richer in polyunsaturated fatty acids, which makes them more active. By integrating into defective areas of the cell membranes of liver cells, phospholipids promote their regeneration, increase the fluidity and elasticity of cell membranes, and stimulate metabolism. Thus, the normalization of all important metabolic processes occurs.
Metabolism regulation occurs, among other things, through the transfer of cholesterol and neutral fats to sites of their oxidation. This occurs due to the ability of phospholipids to bind high-density lipoproteins to cholesterol. As a result, the metabolism of proteins and lipids is streamlined, the liver’s ability to cleanse the body of toxic products is restored, the energy consumption of this organ is reduced, the physicochemical properties of bile are stabilized, and hepatocytes and liver enzyme systems are not only preserved, but also regenerated.
Essentiale N is used intravenously, and the administration should be slow. According to general recommendations, the daily dose of the drug is 5-10 ml or 1-2 ampoules. In especially severe cases, it can be doubled. You can administer two ampoules at a time, but mixing the drug in the same syringe with other medications is not recommended. Before administration, it is advisable to perform the following therapeutic trick: mix the patient’s blood with the contents of the syringe in a ratio of 50 to 50. Injection administration of Essentiale N is optimally supplemented by taking a capsulated form, which is called Essentiale Forte, and the faster this is done, the better. Before injection, it is necessary to examine the contents of the ampoule in daylight. Attention: the drug can only be used if it is transparent (taking into account its special storage conditions, if not observed, irreversible changes may occur).
Analogues of Essentiale N
Level 4 ATC code matches:
Essential phospholipids
Galstena
Fosphonziale
Essentiale Forte N
Livolin Forte
Essliver Forte
Eslidin
Analogues of the drug are the drugs Antraliv , Livolife Forte , Fosfontiale , Essentiale Forte N , Esslial , Livenciale , Essliver , Rezalut Pro .
Analogs are cheaper than Essentiale: Rezalut pro , Fosfonziale , Essliver . The price of Essentiale analogues is from 345 rubles. (the most inexpensive substitute is Fosphonciale capsules).
What is the difference between Essentiale N and Essentiale Forte N?
Essentiale N and Essentiale Forte N are different forms of the same medicine. Essentiale Forte N is available in the form of capsules, each of which contains 300 mg of EPL substance.
It is impossible to unequivocally answer the question of which is better - Essentiale or Essentiale Forte. The choice in favor of one or another dosage form is made taking into account the indications for use (for example, in case of toxicosis in pregnant women, preference is given to taking capsules, since the solution contains alcohol).
In this case, capsules are often used as an adjunct to parenteral therapy.
Ovesol or Essentiale - which is better?
The basis of Ovesol are extracts of mint, oats, immortelle, and turmeric. Its main difference from Essentiale is that it is not a drug, but a dietary supplement.
The active substances contained in the tablets are very beneficial for the liver, as they help cleanse the liver of toxic substances and toxins, eliminate bile stagnation and the formation of stones.
Ovesol is contraindicated in patients under 18 years of age, while Essentiale can be used in adolescents over 12 years of age.
Treatment with Ovesol is carried out three times a year in courses lasting 3 weeks. Continuous use of Essentiale capsules is possible for 3-6 months.
Which is better - Essentiale or Phosphogliv?
The active ingredients of the drug Phosphogliv (available in the form of capsules and lyophilisate for the preparation of d/i solution) are phospholipids and glycyrrhizic acid (glycyrate). Their content in capsules is 65 and 35 mg, respectively, in lyophilisate - 500 and 200 mg.
Glycyrate is a steroidal saponite derived from licorice (licorice) root extract. Its molecule contains a fragment whose structure is similar to the structure of hormones produced by the adrenal cortex .
In this regard, long-term (more than 6 weeks in a row) use of glycirate, as well as use of the drug in a dose exceeding the therapeutic dose, provokes the development of serious adverse reactions.
With long-term use of glycyrrhizic acid, patients experience symptoms of intoxication : high blood pressure, headache , edema , hypokalemia , lethargy , cardiac arrest .
Side effects are similar to those caused by corticosteroid drugs and are due to the fact that glycyrate interferes with the breakdown of endogenous hormones of the adrenal cortex .
The advantages of Essentiale N include a higher concentration of phospholipids in it, as well as the fact that the drug contains only one substance as an active substance, which is why treatment with the drug is extremely rarely accompanied by unwanted reactions.
Which is better - Essentiale or Fosfontiale?
Fosphonziale capsules contain 200 mg of lipoid C100 (equivalent to 188 mg of phosphatidylcholine) and 70 mg of silymar (dry extract of milk thistle).
According to many doctors, the drugs are interchangeable, since the higher concentration of phospholipids in Essential is compensated by the fact that in Phosphonciale their effect is enhanced by the activity of milk thistle flavonoids.
For the consumer, the advantage of Fosfontiale is often its lower cost. The advantage of Essentiale is the presence of an injection form.
What is better - Essentiale or Gepabene?
The hepatoprotective effect of the drug Gepabene is due to the properties of extracts of milk thistle fruits and the herb fumitory.
Milk thistle contains the bioflavonoid silymarin , which has a hepatoprotective effect against toxic liver damage , and also exhibits membrane stabilizing properties and promotes the restoration of hepatocytes.
The fumarin alkaloid contained in the herb fumarin stimulates the secretion of bile and reduces the tone of the sphincter of Oddi .
Thus, the use of Gepabene is advisable for chronic liver diseases , especially if they are accompanied by bile .
Essentiale or Essliver - which is better?
Essliver and Essliver Forte are solutions and capsules that contain phospholipids as an active substance (as in Essential). At the same time, Essliver Forte vitamins to enhance the effect of the latter : nicotinamide , riboflavin , thiamine monohydrate , a- tocopherol acetate , cyanocobalamin , pyridoxine hydrochloride .
The concentration of phospholipids in one capsule is 300 mg (while phosphatidylcholine accounts for only 29%, while in Essential N its concentration is 93%). The phospholipid content in Essliver is 50 mg/ml.
Analysis of the accumulation of free radical oxidation (peroxidation) products showed that Essliver Forte capsules (when compared with the similar dosage form Essentiale) contain significantly more of them (which indicates a lower quality of the drug).
The accumulation of peroxidation products (in particular, malondialdehyde) in the body leads to the formation of intermolecular cross-links with proteins.
As a result, the load on the liver increases (which in turn may not have the best effect on the treatment of fatty hepatosis ) and the likelihood of developing hypersensitivity reactions, and the rate and pathways of metabolism of essential phospholipids in the body are disrupted.
The content of sufficiently high doses of vitamins with long-term use of the drug can also cause the development of hypersensitivity reactions. Considering all of the above, pharmacologists do not recommend using Essliver Forte for more than 2 weeks in a row.
Release form and composition of Essentiale Forte
The active ingredient of the drug is phospholipids from soybeans. It is known that a deficiency of such compounds in the human body leads to disruption of fat metabolism and provokes malfunction of the liver. Hepatoprotective drugs can eliminate the problem. These include the drug Essentiale Forte.
It can be purchased at pharmacies in two forms. This:
- Capsules 300 mg are brown in color with oily contents. They contain 76% choline. Their hard shell is created on the basis of gelatin, titanium dioxide and various dyes. The auxiliary components in the medicine are soybean oil, hard fat, alpha-tocopherol and some other ingredients.
- Transparent solution for injection in ampoules of 50 ml. It contains 93% choline. Auxiliary components are used for production: distilled water, benzyl alcohol, deoxycholic acid and other ingredients.
You can buy Essentiale in cardboard boxes. The packages contain 30, 90 or 100 capsules in blisters or 5 injection ampoules. The drug may differ in labeling. The presence of the designation “forte” in the name indicates an increased amount of phospholipids, and the letter “H” emphasizes that the product contains additional vitamins for the liver.
For children
Since one of the components of Essentiale N is benzyl alcohol, the solution cannot be used in newborns and premature infants.
The administration of drugs containing benzyl alcohol to newborns/premature infants was accompanied by the development of gasping syndrome ( fatal asphyxia syndrome ) - a serious condition with respiratory depression, purpura , metabolic acidosis , encephalopathy , arterial hypotension , sudden suffocation, hemorrhages in various organs (brain, kidneys, adrenal glands, liver, heart) due to hypoxia.
“ Dyspnea syndrome ” in children is fatal (the cause of death is cardiovascular collapse ).
In pediatrics, the drug is used to treat children over 12 years of age weighing 43 (or more) kg.
Essentiale during pregnancy
What is Essentiale used during pregnancy?
During pregnancy, Essentiale capsules are used. The drug is most often prescribed when it is necessary to eliminate manifestations of early toxicosis or signs of gestosis .
The medicine is especially indispensable for gestosis . Late toxicosis can seriously harm the development of a child, but taking Essentiale promotes the normal absorption by the fetus of the microelements and valuable substances it needs and, thus, ensures proper development and normal weight gain.
Essentiale allows you to prevent liver problems in women who suffered from jaundice before pregnancy, and also helps to normalize metabolic processes in case of detected disorders of the placental circulation.
In some cases, taking capsules is continued in the postpartum period, especially if the course of labor was difficult.
With proper use of Essentiale, not only all liver functions are normalized, but also the functioning of the body as a whole. Moreover, the drug is completely safe for both the expectant mother and her child.
Use of the solution during pregnancy
Due to the limited data from clinical studies regarding the use of the drug during pregnancy, as well as due to the presence of benzyl alcohol in the solution, which can pass through the placental barrier, it is not recommended to prescribe Essentiale N to pregnant and lactating women.
Reviews about Essential N
Reviews from doctors, as well as everyday practice, confirm the high effectiveness of Essentiale. The drug compares favorably with other hepatoprotectors , and its safety (including during pregnancy) is confirmed by the results of various clinical studies (including double-blind studies).
It is very important that similar studies have not been conducted for most Essentiale generics.
The drug is an integral part of the treatment of liver diseases of metabolic and toxic origin, and it is suitable not only for humans, but also for dogs and cats.
The properties of the phospholipids contained in the medicine allow it to be used for hair as a strengthening agent. Reviews from women indicate that the effect of masks with Essentiale is noticeable after the first procedure.
Contraindications and side effects
Contraindications to Essentiale, the instructions focus on this, relate exclusively to the patient’s individual intolerance to the components in the composition of the drug. This medicine may cause serious allergic reactions. In addition, a direct contraindication for Essentiale Forte, as the instructions for use indicate this, is age under 12 years. This is due to the high content of phospholipids. A contraindication to taking the drug is the period of lactation.
You should not take Essentiale Forte; the instructions warn about this in case of exacerbation of pancreatitis. If you experience any pain in the abdomen, you must consult a doctor before starting to take the drug.
Essentiale Forte, the instructions for use warn about this, has side effects. It must be remembered that when taking the drug in patients prone to hypotension, blood pressure may decrease. An overdose of the drug can provoke arrhythmia or tachycardia.
Sometimes when taking Essentiale Forten, the instructions for use indicate this, allergic reactions to the vitamins included in the product occur. Symptoms of this are most often a skin rash or watery eyes. In the first days of use, disruptions in the functioning of the digestive system may occur:
- Nausea.
- Discomfort in the abdomen.
- Stool disorder.
Price Essentiale N, where to buy
The price of Essentiale ampoules (package No. 5) in Kharkov, Kyiv, Odessa and other cities of Ukraine is 176-205 UAH. The cost of 1 ampoule is 41-43 UAH.
In Russian pharmacies, liver medicine can be bought for 927-1160 rubles. (Essentiale injections in 5 ml ampoules, package No. 5).
The price of Essentiale IV in Belarus is from 156 thousand rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
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Pharmacy Dialogue
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Pharmacy24
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186 UAH.order - Essentiale N 5 ml N5 injection solution PAT "Galichfarm", Ukraine
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PaniPharmacy
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