Chemistry:Essentiale

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Essentiale
Clinical data
Trade namesEssentiale
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Essentiale (polyenylphosphatidylcholine or PPC, with or without synergistic vitamins) is a preparation of essential phospholipids. Essentiale normalizes the metabolism of lipids and proteins, improves the detoxification function of the liver, restores the cellular structure of the liver and retards the producing of conjunctive tissue. Essentiale medications are indicated for the treatment of fatty degeneration of the liver, hepatitis (including toxic hepatitis, liver damage caused by medicines or alcohol abuse), cirrhosis of the liver, and disturbances in liver function associated with different illnesses.

Pharmaceutical action

Phospholipids are essential structural components of all cellular membranes. Essential phospholipids (EPL substance -- an active ingredient in Essentiale medications) is a complex of substances of natural origin (ethers of cholinephosphoric acid (phosphatidylcholine) and unsaturated fatty acids (linoleic, linolenic, olein). Essentiale medications possess membranotropic properties, exert metabolic and hepatoprotective action, and regulate lipid and carbohydrate metabolism. Essential phospholipids increase the functional status of the liver.

Intervening in the disturbance of the liver's metabolism, Essential phospholipids enter the cell membrane and combine with the endogenous phospholipids. Essential phospholipids improve the patient's clinical status and the liver's lab indices.

Combination of Essentiale with cordiamin (nikethamide) and vitamin E (50 mg/kg for 35 days) considerably activates the mono-oxygenase, glucoro- and glutathione transferase systems of the liver, resulting in the free-radical processes becoming less intense.[1]

The spectrum of Essential phospholipids' activity in chronic degenerative liver diseases is illustrated by the following properties:

  • recovery and maintaining the consistency of the hepatocytes;
  • activation of the phospholipid-depending ferments;
  • improvement in the lipids' metabolism caused by accelerated synthesis of lipoproteins in the liver;
  • activation of RNA synthesis and as a result the normalization of protein metabolism;
  • increased synthesis of glycogen in the liver;
  • improvement in the detoxification function of the liver;
  • the conversion of neutral fats and cholesterol into easily metabolized forms;
  • decreased fatty infiltration of the hepatocytes.

Common use

Essentiale is used to treat the following diseases:

  • Hepatitis (acute and chronic), toxic hepatitis, medicinal and alcoholic hepatitis, poisonings;
  • Hepatic steatosis of different aetiology (in 53.6% of patients, the effect of a six-month treatment with Essentiale forte was very good, showing improvement of all investigated parameters);[2]
  • Diabetes (the data suggests that Essentiale protects and improves liver function in diabetic subjects with non alcoholic fatty liver[3] and chronic infections);
  • Disturbance in liver function in somatic diseases;
  • Hepatic cirrhosis;
  • Necrosis of the liver cells, liver failure, liver coma;
  • Pre- and Post- surgical treatment, especially in hepatobiliary area;
  • Hyperlipoproteinemia, hypercholesterolemia, hypertriglyceridemia;
  • Diseases of the cardiovascular system: coronary heart disease, stable stenocardia,[4] post-infarction condition, disturbance of the cerebral and peripheral circulation, Hypertension, thrombembolia prophylaxis, atherosclerosis, diabetic angiopathy, thrombembolia prophylaxis and fat embolism (solution for injection);
  • Digestive system diseases (chronic pancreatitis, gastric and duodenum ulcer);
  • Toxicosis of pregnancy (edema, proteinuria and blood pressure disorders);
  • Radiation sickness (radiation syndrome);
  • Psoriasis, atopic dermatitis, eczema;
  • Pyelonephritis;[5]
  • Prophylaxis of micromegaly.

Availability

Essentiale medications are manufactured under 4 trade names:

ESSENTIALE - solution for intravenous injections in vials 5 ml. Essentiale contains essential phospholipids (EPL substance) 250 mg, Pyridoxine chidrochloride 2,5 mg (Vitamin B6), Cyanocobolamine 0,1 mg (Vitamin B12), Sodium Pantothenate 1.5 mg, Nicotinamide 25 mg.

ESSENTIALE FORTE N - Capsules N30 or N100. One capsule contains essential phospholipids (EPL substance) 300 mg.

ESSENTIALE N - solution for intravenous injection in vials 5 ml. Essentiale N contains essential phospholipids (EPL substance) 250 mg.

ESSENTIALE FORTE - capsules N50. Essentiale forte contains essential phospholipids (EPL substance) 300 mg, Thiamine mono nitrate (Vitamin B1) 6 mg, Riboflavine (Vitamiin B2) 6 mg, Pyridoxine chidrochloride 6 mg (Vitamin B6), Cyanocobolamine 0.06 mg (Vitamin B12), Nicotinamide 30 mg, Tocopherole acetate 6 mg (Vitamin E).

Contradiction and cautions

Do not use Essentiale in hypersensitivity or allergy to any ingredients of the preparation. The application of Essentiale in newborn children is not safe. During pregnancy women are recommended to consult their health care provider prior to taking Essentiale.

Side effects

In very rare cases it can cause: abdominal pain, nausea, diarrhea and allergic reaction (skin rash).

Recommendation for storage

Capsules should be stored at temperature not more than 20 °C. Vials should be stored at 2° - 8 °C

Independent research

According to research conducted by Bronx Veterans Affairs Medical Center and the Mount Sinai School of Medicine in 2003, phospholipids treatment did not affect progression of liver diseases in those who continued to drink heavily.[6]

References

  1. IV Zverinskiĭ; VE Karpovich; MI Bushma; LF Legon'kova; NG Mel'nichenko; LI Nechiporenko; VS Nikitin (Jan–Feb 1998). "The action of Essentiale and its combination with cordiamine and vitamin E.". Eksp Klin Farmakol. (61(1):33-6): 212–214. 
  2. The effect of polyene phosphatidylcholine (Essentiale forte) in the treatment of liver steatosis and ultrasound findings--preliminary study.. Interní klińika, Institutu postgraduálního vzdélávání ve zdravotnictví, Praha. Jun 1994. 
  3. S Poongothai; K Karkuzhali; G Siva Prakash; T Sangeetha; G Saravanan; R Deepa; Sharadha Gopalakrishnan; V Mohan (2005). "EFFECT OF ESSENTIALE IN DIABETIC SUBJECTS WITH NON - ALCOHOLIC FATTY LIVER". Int J Diab Dev Ctries 25. 
  4. The effect of laser therapy and its combination with essentiale on the course of stable stenocardia. Lik Sprava (0) 0: 72-4. 
  5. AA Ovchinnikov; VE Tsvettsikh; BA Berdichevskiĭ; VN Lykov; VR Suktanbaev; AV Murychev (Jul–Aug 1996). "Essential phospholipids in the treatment of chronic pyelonephritis.". Urol Nefrol (Mosk).. 
  6. II. Veterans Affairs Cooperative Study of polyenylphosphatidylcholine in alcoholic liver disease..