Pantothenic Acid And Pantethine

Contents
Introduction
Properties
Therapeutic Usage
Lipid Profile Dysfunction
Adrenal Function Enhancement
Therapeutic Dosage

The term "Pantos" means "everywhere" in Greek. It is from this term that the name Pantothenic Acid or more commonly known as Vitamin B5 is derived.

Pantothenic acid is a form of vitamin manufactured by plants. Mammals do not manufacture this vitamin intrinsically. But, fortunately, we can obtain substantial amounts of this acid in our diet. If our bodies do not have enough of this acid, we can develop a rare form of disease call Pantothenic acid deficiency.

The recommended daily dosage has yet to be established. However, some scientists have given an estimation with regards to the safe and adequate daily dietary intake as follows:-

What type of food should we eat to obtain adequate levels of pantothenic acid? Doctors say that Brewer's yeast, torula (nutritional) yeast and calf liver are excellent sources of pantothenic acid. In addition, we can also eat peanuts, split peas, pecan nuts, oatmeal, mushrooms, soybeans, buckwheat, sunflower seeds, red chilli peppers, avocados, lentils, cashew nuts and other whole grains and nuts.

PROPERTIES

When pantothenic acid enters our bodies, it forms a substance call pantethine. Pantethine is a more stable disulfide form (or a double bond) of pantothenic acid. It is also a more active metabolic substrate that is converted into an enzyme called "Co-Enzyme A" (CoA). CoA plays a critical role in the metabolism and breakdown of the three essential micronutrients namely proteins, carbohydrates and fats.

CoA is also a cofactor in more than 70 enzymatic pathways which includes the following:-

1 Fatty acid oxidation
2 Carbohydrate metabolism
3 Pyruvate degradation
4 Amino acid catabolism
5 Heme synthesis
6 Acetylcholine synthesis
7 Phase II detoxification acetylationsin

CoA is also responsible for the initial steps of cholesterol synthesis, all down-stream metabolites of cholesterol including steroids, Vitamin D and bile acids.

As such, we can see that CoA is a very important enzyme. It also helps to breakdown the carbon skeleton of most amino acids, which are metabolized to pyruvate and enter the TCA cycle.

CoA directs acetyl groups to form all polyisoprenoid compounds, which include ubiquinone (CoQ10), squalene and cholesterol. Our bodies also need CoA for the transportation of long chain fatty acids into the mitochondria where fats are converted into energy.

In a nutshell, CoA is the basis for the production of hemoglobin, bile, sex and adrenal steroids, cholesterol, and a few brain chemicals and neurotransmitters.

We can consume pantothenic acid through dietary means. However, it must be noted that the more active form of pantethine, or its reduced-SH form pantetheine that contains the SH molecule necessary for enzyme activity cannot be obtained by consuming whole foods.

When we compare pantethine with pantothenic acid, pantethine by far more active when it comes to the production of CoA. This hypothesis has been proven true by many clinical trials. Although taking pantothenic acid as a form of supplement will ultimately lead to the creation of CoA, researchers have pointed out that pantethine creates twice as much CoA than pantothenic acid. This is because structure of pantethine is closer to the CoA production pathway.

Pantothenic acid also has its own benefits. It enhances adrenal functions and inflammatory response modulation. Both pantothenic acid as well as pantethine should be considered as one synergistical unit and not as mutually exclusive nutrients.

THERAPEUTIC USAGE

Many people have been using pantethine as a supplement to treat cardiovascular disease, autoimmune disorders, colitis and Crohn's disease and rheumatoid arthritis. Sometimes, it is also used as an "anti-stress" nutrient.

Pantethine is also well known for its effectiveness in reducing total cholesterol, LDL cholesterol, and triglyceride level, while at the same time raising the good HDL cholesterol.

Pantothenic acid, on the other hand is ideal for enhancing adrenal functions and reducing reliance on steroids. It also reduces elevated uric acid levels frequently associated with gout and reduces inflammatory response. Sometimes, it can be used as substitute for non-steroidal anti-inflammatory drugs.


LIPID PROFILE DYSFUNCTION

About 40 percent of Americans suffer from abnormal lipid dysfunction. As such, the recent focus has been on the use of pantethine as a therapeutic agent in the treatment of this illness. Taking pantethine orally is  effective for reducing and normalizing a variety of risk factors in patients with hypercholesterolemia, arteriosclerosis and diabetes.

In the past, taking niacin or Vitamin B3 would give the same effect. However, today we know that niacin can lead to inflammations in the liver and possibly raise blood sugar levels in diabetic patients. Furthermore, high doses of niacin required for therapeutic effect often lead to an intolerable flush. But, so far, pantothenic acid and pantethine do not have any of such negative side effects.

While the exact mechanism of pantethine in normalizing parameters associated with dyslipidemia is not clear, clinical studies have proven that when pantethine is added to cultured cells, it causes an 80% inhibition in cholesterol synthesis, most likely inhibiting the activity of HMG-CoA reductase.

Pantethine can also boost the production of enzymes that helps to break down blood fats. It helps to enhance Vitamin E's action and prevents cholesterol from building up in the blood. Pantethine also increases the amount of omega-3 fatty acids, which in turn stabilizes the cellular membrane. Furthermore, it also enhances the production of Coenzyme Q10, leading to stronger cardiac contraction force and increasing the efficiency of energy generation.

Over the years, numerous studies have validated the use of pantethine in management of abnormal lipid profile.

    · In a study, 30 patients with dyslipidemia were examined. They were all given 900 mg of pantethine daily. Six patients in the subgroup of type IIa dyslipidemia reported a decrease in total cholesterol level by 26%, triglycerides by 28%, "bad" LDL-cholesterol by 38%, very low-density lipoprotein (VLDL) cholesterol by 28%, and Apo-B by 16%. At the same time, their "good" HDL-cholesterol was increased by 34%. Another nine patients with type IIb dyslipidemia experienced a decrease of 25% for total cholesterol, 49% for triglycerides, 33% for LDL-cholesterol, 44% for VLDL-cholesterol, and 11% for Apo-B. At the same time, there was a significant increase in their HDL-cholesterol by 43%. Another 15 individuals with type IV dyslipidemia reported that their total cholesterol decreased by 13%, triglycerides by 68%, VLDL-cholesterol by 53%, and Apo-B by 18%. At the same time, their HDL cholesterol was increased by 25%.

     · In another study, a double-blind placebo-controlled study was conducted on 29 patients with high cholesterol and triglycerides for a period of 8 weeks. They were given pentethine at 300 mg 3 times daily. After eight weeks, the subjects reported a 30% reduction in blood triglycerides, a 13.5% reduction in LDL ("bad") cholesterol, and a 10% rise in HDL ("good") cholesterol.

    · Bertolini et al treated seven children and 65 adults who suffered from hypercholesterolemia or other diseases associated with hypertriglyceridemia (types IIa and IIb of Fredrickson's classification).  Pentethine at 900 mg for children and 1,200 mg for adults were given daily for a period of 3 years. The children reported a 20% reduction of total cholesterol and a 27% decrease in LDL-cholesterol. The adults with type IIa hyperlipoproteinemia reported a 25% decrease in total cholesterol, a 39% decrease in LDL-cholesterol, a 34% decrease in Apo-B, and a slight increase in HDL-cholesterol. In the adult patients with type IIb hyperlipoproteinemia, total cholesterol was reduced by 19.8%, LDL-cholesterol by 37%, triglycerides by 31%, and Apo-B by 6%. In this subgroup, a 23% increase of HDL-cholesterol and a 15% increase in apolipoprotein A-I were also observed.

    · Donati et al also tested the effectiveness and tolerability of pantethine in 31 patients with dyslipidemia undergoing chronic hemodialysis. These patients were given 600 to 1,200 mg of pantethine daily for a period of 9 months. The results revealed a significant improvement in total blood cholesterol for patients with basal hypercholesterolemia, and a highly significant reduction of serum triglycerides for the entire group. However, their HDL-cholesterol or total Apo-A did not increase.

    · In another separate study, 600 mg/day of pantethine was given to 37 hypercholesterolemic and/or hypertriglyceridemic patients for a three-month period. Out of all 37 patients, 21 of them were diabetic. After pantethine was given to these patients, their total cholesterol, triglycerides, low density lipoprotein (LDL) cholesterol and apolipoprotein B (Apo-B) was decreased. At the same time, there was an increase in high density lipoprotein (HDL) cholesterol and apolipoprotein A (Apo-A) in all the groups.  When pantethine was not given to these patients, a reversal in the improvement of these parameters was observed. 

Later on, a one-year follow up trial was again conducted in 24 patients with established dyslipidemia of Fredrickson's types IIa, IIb, and IV, alone or associated with diabetes mellitus. Blood lipid assays revealed consistent reductions in total cholesterol, LDL-cholesterol, and Apo-B, along with an increase of HDL-cholesterol and Apo-A in individuals with types IIa and IIb dyslipidemia. The results were equally favorable in patients with uncomplicated dyslipidemia and in those with associated diabetes mellitus. A marked reduction in triglycerides was also observed in the patients with Fredrickson's type IV dyslipidemia.

    · In another experiment conducted by Binaghi et al, he used 24 hypercholesterolemic perimenopausal women as his subjects. The women were supplemented with 900 mg/day of pantethine. After 16 weeks, they reported an efficacy rate of about 80% with significant reductions in total cholesterol, LDL-cholesterol, and LDL/HDL ratios.

Many other studies have proven the effectiveness of using pantethine to improve cholesterol and triglyceride levels in people with diabetes. The results were all encouraging. In one study, oral administration of pantethine given to 31 diabetic patients with hyperlipidemia led to a decrease in their cholesterol level from a mean value of 236 mg/dl to 217 mg/dl (10% reduction). Their HDL-cholesterol level was also increased from a mean value of 40 mg/dl to 43 mg/dl (5% increase).

ADRENAL FUNCTION ENHANCEMENT

Our adrenal glands need pantothenic acid to manufacturer anti-inflammatory hormones such as cortisol. Pantothenic acid is therefore a potent natural treatment for inflammatory related ailments such as arthritis, colitis, and allergies. As such, we can deduce that inflammatory and infectious processes lead to cardiovascular disease. The use of pantothenic acid has indeed been broadening.

Pantethine seems to exert an influence over some indicators of adrenal function. Several animal experiments have shown that a lack of pantothenic acid will affect adrenal cortex function, most likely due to the reduction of adrenal corticosteroids. When pantethine or CoA is injected into animals, there is a marked increase in steroidogenous effect.

During a study, it was reported that pantethine was given to 20 humans with a variety of clinical diseases to buffer the increase in 24-hour urinary 17-hydroxycorticosteroids and plasma 11-hydroxycorticosteroids stimulated by a loading dose of adrenocorticotropic hormone.

We all know that pantothenic acid is an important nutrient to maintain an optimum adrenal function. When the adrenal gland fails to function, our bodies will not be able to produce progesterone. This will result in estrogen dominance that can lead to cancer of the ovarian, breast and cervics.

People who are taking steroids such as prednisone for treating health conditions such as asthma and autoimmune disease should reduce their medication dosage. With the help of pantothenic acid, they can be slowly wean off their dependency on anti-inflammatory drugs.

Therapeutic Dosage

Disease	Dosage
Colitis and Crohn’s disease	900 mg daily of both pantethine and pantothenic acid to reduce inflammation.
Gout	Pantothenic acid (in the form of calcium   pantothenate) 200 mg four times a day
Autoimmune and Allergic Disorders	400 to 900 mg a day of both pantethine and pantothenic acid
Wound healing	900 mg of pantothenic acid daily
Stress and adrenal gland enhancement	400 to 900 mg a day of both pantethine and pantothenic acid
Cholesterol, triglycerides stabilization	400 to 1,200 mg daily of both pantethine and pantothenic acid

There are no significant side effects for high dose of pantothenic acid or pantethine, used by themselves or with other medications. Sometimes, minor digestive disturbances may occur.

However, more caution should be exercised for young children, pregnant or nursing women, or people with serious liver or kidney disease as the safe level dosage had yet to be established.

Pantothenic acid is often sold in the form of calcium pantothenate. Regular pantothenic acid cannot be used as a substitute for pantethine. They should be used together.

About The Author

Michael Lam, M.D., M.P.H., A.B.A.A.M. is a specialist in Preventive and Anti-Aging Medicine. He is currently the Director of Medical Education at the Academy of Anti-Aging Research, U.S.A. He received his Bachelor of Science degree from Oregon State University, and his Doctor of Medicine degree from  Loma Linda University School of Medicine, California. He also holds a Masters of Public Health degree and  is Board Certification in Anti-aging Medicine by the American Board of Anti-Aging Medicine. Dr. Lam pioneered the formulation of the three clinical phases of aging as well as the concept of diagnosis and treatment of sub-clinical age related degenerative diseases to deter the aging process. Dr. Lam has been published extensively in this field. He is the author of The Five Proven Secrets to Longevity (available on-line). He also serves as editor of the Journal of Anti-Aging Research.

For More Information

For the latest anti-aging related health issues, visit Dr. Lam at www.LamMD.com. Feel free to email Dr. Lam at dr@LamMD.com if you have any questions.


Reprint Information

This article may, in its unabridged, unaltered form and in its entirety only, be reprinted and republished without permission provided that it is for personal and non commercial education use only and further provided that credit be given to the author, with copyright notice and www.LamMD.com clearly displayed as source. Written permission from Dr. Lam is required for all other use.
 

©2002  Michael Lam, M.D. All Rights Reserved.

References

Angelico M, et al. Improvement in serum lipid profile in hyper-lipoproteinaemic patients after treatment with pantethine: a crossover, double-blind trial versus placebo. Curr Ther Res 1983; 33: 1091.

Arsenio L, Caronna S, Lateana M, et al. Hyperlipidemia, diabetes and atherosclerosis: efficacy of treatment with pantethine. Acta Biomed Ateneo Parmense 1984;55:25-42.

Arsenio L, Bodria P, Magnati G, et al. Effectiveness of long-term treatment with pantethine in patients with dyslipidemia. Clin Ther 1986;8:537-545.

Bertolini S, Donati C, Elicio N, et al. Lipoprotein changes induced by pantethine in hyperlipoproteinemic patients: adults and children. Int J Clin Pharmacol Ther Toxicol 1986; 24:630-637.

Binaghi P, Cellina G, Lo Cicero G, et al. Evaluation of the cholesterol-lowering effectiveness of pantethine in women in perimenopausal age. Minerva Med 1990;81:475-479.

Coronel F, Tornero F, Torrente J, et al. Treatment of hyperlipidemia in diabetic patients on dialysis with a physiological substance. Am J Nephrol 1991; 11: 32-36.

Dacol PG, et al. Pantethine in the treatment of hypercholesterolemia: a randomized double-blind trial versus tiadenol. Curr Ther Res 1984;36: 314-322.

Donati C, Barbi G, Cairo G, et al. Pantethine improves the lipid abnormalities of chronic hemodialysis patients: results of a multicenter clinical trial. Clin Nephrol 1986;25:70-74.

Donati C, Bertieri RS, and Barbi G. Pantethine, diabetes mellitus and atherosclerosis. Clinical study of 1045 patients. Clin Ther 1989; 128: 411-422.

Gaddi A, Descovich GC, Noseda G, et al. Controlled evaluation of pantethine, a natural hypolipidemic compound, in patients with different forms of hyperlipoproteinemia. Artherosclerosis 1984;50:73-83.

Hiramatsu K, Nozaki H, Arimori S. Influence of pantethine on platelet volume microviscosity, lipid composition and functions in diabetes mellitus with hyperlipidemia. Tokai J Exp Clin Med 1981;6:49-57.

Kosaka M, Kikui S, Fujiwara T, Kimoto T. Action of pantetheine on the adrenal cortex. Horumon To Rinsho 1966 Oct;14(10):843-847.

Maggi GC, Donati C, Criscuoli G. Pantethine: A physiological lipomodulating agent, in the treatment of hyperlipidemias. Cur Ther Res 1982;32:380-386.

Murai A, Miyahara T, Tanaka T, et al. The effects of pantethine on lipid and lipoprotein abnormalities in survivors of cerebral infarction. Artery 1985;12:234-243.

Noma A, Kita M, Okamiya T. Effect of pantethine on post-heparin plasma lipolytic activities and adipose tissue lipoprotein lipase in rats. Horm Metab Res 1984;16:233-236.

Ranganathan S, Jackson RL, Harmony JA. Effect of pantethine on the biosynthesis of cholesterol in human skin fibroblasts. Atherosclerosis 1982;44:261-273.

Rubba R, Postiglione A, DeSimone B, et al. Comparative evaluation of the lipid-lowering effects of fenofibrate and pantethine in type II hyperlipoproteinemia. Curr Ther Res Clin Exp 1985: 38: 719-727.

Tahiliani AG, Beinlich CJ. Pantothenic acid in health and disease. Vit Horm 1991;46:165-227.