Description
Essentiale N ampoules for IV by Sanofi labs (plaquex therapy)
5 x 5 ml ampoules for IV with 250 mg of essential phospholipids (phosphatidylcholine) per vial – the same ingredients are used in the so called ‘plaquex’ therapy.
ATTENTION: due to the war in Ukraine, this product became extremely hard to get. If the product shows ‘back order’, the waiting time could be several weeks – please keep this in mind when ordering.
Essentiale N has the same composition as the long gone original Lipostabil by Natterman, the product that eventually became the most widely used targeted fat burner worldwide up to this day.
1 ampoule of 5 ml contains: essential phospholipids – EPL® – substance (phospholipids from soybeans (93% (3-sn-phosphatidyl) choline)), which contain: α-tocopherol, ethanol 96%) – 250 mg;
Other ingredients: deoxycholic acid, sodium chloride, sodium hydroxide, riboflavin (dye), water for injection, benzyl alcohol.
Indications:
- Fatty degeneration of the liver of various etiologies (including liver in diabetes);
- atherosclerosis
- Acute and chronic hepatitis;
- Cirrhosis of the liver;
- Necrosis and degeneration of liver cells of various origins;
- Liver coma and precoma;
- Toxic damage of hepatic parenchyma;
- Morning sickness during pregnancy;
- Liver damage in alcoholism;
- Psoriasis;
Pharmacological properties
The phospholipids contained in the composition of the drug “Essentiale N”, regulate the metabolism of lipoproteins, carry neutral fat and cholesterol to oxidation. This occurs by increasing the ability of HDL to cholesterol contact. Is a normalizing effect on the metabolism of lipids and proteins, detoxification function of the liver, the recovery of the cellular structure of the liver and phospholipid-dependent enzyme systems, which prevents the formation of scar tissue in the liver.
Communicating with the high-density lipoproteins, phosphatidylcholine enters the liver cells. The half-life of the choline component is 66 hours, and the excretion of unsaturated fatty acids occurs in 32 hours.
The principle of “Essentiale N”
Due to the fact that the composition of the “Essentiale N” includes phospholipids from soybeans, it normalizes the metabolism of lipids, proteins and detoxification function of the liver, promotes the restoration and preservation of its cells, the structure of the organ and enzyme systems. The drug inhibits the formation of connective tissue and is good for the cardiovascular system, prevents the process fatty liver.
Atherosclerosis
Essentiale has a whole battery of different functions in cell membranes that influence many different parameters involved in atherosclerosis.For a quick read, here is a summary of actions that reduce Atherosclerosis.
Summary
– LDL and VLDL reduction
– HDL increase
– Triglyceride reduction
– Reduces Lipid Peroxidation
– Increases Enzyme activity such as LCAT
– Reduces Platelet Aggregation
– Improves RBC deformability
– Anti-Inflammatory
– Increases anti-oxidants (Glutathione)
– Activates Immune Cells
– Reduces Endocytosis
– Reduces Mast Cell formation
– Cell Membrane Repair
Lipid Metabolism
It reduces LDL Cholesterol and Triglyceride levels while it increases HDL Cholesterol levels. It is becoming very evident that elevated LDL cholesterol is NOT the cause of heart disease. In fact studies involving statins show that lowering LDL cholesterol has no influence on the rate of heart attacks. Fast CT exams show Calcium deposits in coronary blood vessels and the rate of increase of the Calcium score over time is more predictive for future heart attacks that LDL levels that show no correlation whatsoever. But it is hypothesized that the body uses Cholesterol as “Bandaid” to patch up damaged endothelial cells, but it is not the primary cause of the damage and the plaque. Since plaque deposits contain some cholesterol, removing it will reduce the size of the plaque.
Essentiale activates the enzyme LCAT Lecithin Acyl Cholesterol Transferase) which esterifies cholesterol, including deposits in plaque, enabling HDL to take it up and remove it from vascular walls and eliminate it through the liver.1
Effects on Total Cholesterol
In a documentation of 15 clinical trials with a duration of PC treatment between 1 and 12 months, total cholesterol was lowered 8.8% to 28.2 %. The initial values, route of administration, PC dosage and duration of the treatment determine the amount of the reduction.
Diabetics with hypercholesterolemia type 2b and 4 were treated with PC for 6 weeks (pink line) and observed for another 2 weeks against placebo (blue line). The treated group had a significant reduction of total cholesterol levels, but they started to climb again after stopping treatment. This shows the importance of maintenance therapy.
Effects on LDL Cholesterol
In clinical studies in 1160 patients the mean reduction of LDL cholesterol was 31%. The extent of the reduction was determined by the type of hyperlipoproteinemia, the PC dosage and the duration of treatment. To short a treatment (14 days), to low of a dosage ( less than 1.5 grams) did not have any effect on LDL cholesterol. 20,21,22,23,24,25
LDL levels during 42 days treatment (green) with 1.9 g of PC per day against Placebo (purple).
Effects on HDL Cholesterol
In various studies an increase of HDL Cholesterol was found between 10-45%. Very low initial HDL levels were raised significantly while close to normal initial levels were hardly influenced.26-33, The effect was more pronounced in non smokers than in smokers.
HDL levels during a 6 week treatment (pink line) with 2.7 g/day against placebo (blue line). Two weeks after stopping treatment, HDL levels begin to decline, showing the importance of maintenance therapy.
Effects on Triglyceride Levels
Elevated Triglyceride levels were treated and observed in 2734 patients. The extent of the reduction was dependent on the initial levels. Very high levels were reduced significantly while close to normal levels were hardly influenced. The mean reduction was a 25% drop. The table below shows the reduction of Triglyceride levels dependent on the method of application and duration of treatment. 22,26,34-36
A correlation was found to caloric intake. The more calories the patient eats, the less the extent of the drop in Triglyceride levels.
Lipid Peroxidation
An important factor in the development of atherosclerosis is lipid peroxidation. A close relationship was found between lipid peroxidation and increased platelet aggregation. In vivo and in vitro studies show a decrease in lipid peroxidation parameters when PC is applied. It’s surmised that increased Glutathione and SOD levels help reduce/prevent lipid peroxidation.
PC reduces LDL oxidation as well. In a study the time was measured until LDL was oxidized when mixed with various forms of PC or alpha tocopherol as well as an oxidizing agent. When LDL was incubated with unsaturated PC as in Plaquex, the lag time until it oxidized was much longer than with all other forms of PC or alpha Tocopherol.
Effects on Enzymes involved with lipid metabolism
The most important enzyme is LCAT. It’s synthesized in the liver. It catalyzes the esterification of free cholesterol, including cholesterol in plaques and in cell membranes, so it can be taken up by HDL and transported to the liver for elimination. PC with saturated fatty acid chains such as from egg yolk diminish the activity of LCAT while PC with unsaturated fatty acid chains activates LCAT. 2,3,5,4,5,6,7,8,9 Other enzymes activated by polyunsaturated PC are Lipoprotein Lipase and hepatic Triglyceride Lipase.10
Reduced Platelet Aggregation
There is a close relationship between high cholesterol levels in the membranes of platelets and an increased tendency to adhesion and aggregation of platelets.40 Deposits of platelets on vascular walls enhance the sensitivity of the wall towards substances released from platelets, increasing the wall permeability, leading to deposits of plasma constituents such as lipids in the injured wall. Plaquex, through the activation of LCAT, reduces the amount of cholesterol in the membranes of platelets, thereby reducing their tendency to adhesion and aggregation. During a 14 day trial with 500 mg PC/day given as infusions, the reactive platelet aggregation was reduced by 60%. A further study using 250mg/day over a period of 30 days in elderly patients with increased tendency to coagulation showed fibrinolytic acitivity to increase in the thrombo-elastogram. 1.5 g oral PC over 16 weeks increased serum 6-keto-PGF1, a stabilized metabolite of the antiaggregatory and vasodilatory prostaglandin PGI2 and a drop in Thromboxane levels. 49
Improved Deformability of Red Blood Cells
Increased accumulation of cholesterol in RBC membranes impair the fluidity and functioning of the membrane and RBC deformability, making it hard for RBCs to pass through tight capillaries. An improved passage of red blood cells through microfilters and the normalisation of RBC aggregation was found in patients given 500mg by IV injection and taking 1.8 g orally/day for three months. Studies confirmed that an increase in LCAT activity lowered the cholesterol content in the membranes of red blood cells, thereby making the membranes more fluid and deformable. 28,40,50,51,52
Effects on Inflammatory Parameters
Studies showed a reduction of inflammatory parameters Interleukin 6 and 10, Tumor Necrosis Factor alpha as well as Nuclear Factor Kappa when animals of various species were given PC. 53, 54
Effects on Antioxidants
Essentiale increases the levels of Glutathione and Sodium Oxide Dismutase by increasing the enzymes in the cell membranes responsible for these antioxidants. It thereby combats lipid peroxidation and prevents alcohol induced liver fibrosis by inhibiting alcohol induced oxidative stress. 55-57
Activation of Immune Cells
Immune cells require unsaturated PC in their membranes in order to activate. It is surmised that the activation of immune cells could take down bacterial biofilms found in vascular plaque deposits.
Reduced Endocytosis and Mast Cell Formation
Essentiale inhibits endocytosis in smooth muscle cells thereby preventing the formation of atherosclerotic plaque. Bowyer et al (69) described a highly significant inhibition of endocytosis in the smooth muscle cells of pig aortas after in vitro incubation with PC. According to the authors, these results suggest that PC inhibits atherogenic processes by reducing the endocytosis of plasma constituents. It also reduces the accumulation of cholesterol in macrophages by 15-20%, thereby preventing the formation of foam cells.
Reduction of Atherosclerosis
The combination effects on lipids, LCAT, antioxidation, anti inflammation, inhibition of endocytosis, immune cell activation, reduced platelet aggregation and enhanced RBS deformability reduce atherosclerotic plaque deposits. In total 22 studies in 7 animal models were done and they showed prevention of atherosclerosis if given together with a high cholesterol diet and BSA injections or a regression of atherosclerotic changes if treated after atherosclerosis has developed. 63-67 BSA injections are Bovine Serum Albumin. It is an known method of inducing atherosclerosis in animals given a high cholesterol diet.
Semilunar valves, ascending & descending branches and aortic arch of a rat. (44). Above after 2 months on a cholesterol diet. Below after the same diet for 2 months but given PC after two months for two months.
Atherosclerosis was induced in animals with a 3 month atherogenic diet. The placebo group (pink line) developed atherosclerosis. The group given i.v. PC treatments showed marked regression of atherosclerosis (green line).
A number of studies were done with EKG diagnostics. Depending on the PC dosage and the duration of treatment, an improvement of EKG findings could be achieved in many cases. Among them they found a dose-related disappearance of S-T depressions and reversal of previously negative T-waves to positive. These favourable changes went along with symptomatic relief of sternocardiac symptoms. Exercise tolerance as tested on the bicycle ergometer improved. The phase until S-T depression occurred became longer, with the depressions themselves being less distinct.
Treatment of angina attacks
Other studies looked at the frequency of angina pectoris attacks and Nitroglycerine consumption. The investigations of Almazov et al. included 34 male patients suffering from ischaemic heart disease and angina pectoris of stages III-IV.
They received 500 mg/d of intravenous PC for a period of 14 days. 20 of the 34 patients reported an absence of anginal attacks already at the end of the first and beginning of the second week of treatment. The other 14 patients experienced a reduction of attacks from 8 to 10 per day to 1 to 3 attacks per day, with the severity decreasing as well. Daily nitro-consumption therefore, could be reduced to 2 to 5 doses from the initial 8-10 doses. It’s important though to realize that the fast decline of symptoms has to do with the improved flow capability of the RBCs and the reduced aggregation of platelets.
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