Monograph
Inositol Hexaniacinate
(Reprinted by permission of Alternative Medicine Review, 1998;3(3). Copyright c Thorne Research, Inc. All rights reserved.)
Inositol hexaniacinate (IHN) is the hexanicotinic acid ester of meso-inositol. This compound consists of six molecules of nicotinic acid (niacin) with an inositol molecule in the center. Pharmacokinetic studies indicate the molecule is, at least in part, absorbed intact, and hydrolyzed in the body with release of free niacin and inositol. It appears to be metabolized slowly, not reaching maximum serum levels until approximately 10 hours after ingestion.19
Mechanisms of Action: The mechanisms of action of inositol hexaniacinate are believed to be the same as those for niacin. These include a decrease in free fatty acid mobilization; a decrease in VLDL synthesis in the liver, resulting in a decrease in LDLs, total cholesterol, and triglycerides; inhibition of cholesterol synthesis in the liver; an increase in HDL levels by decreasing its catabolism; and fibrinolysis.
Clinical Indications:
Hyperlipidemia: Studies report significant lipid-lowering effects of IHN at doses of 400 mg 3-4 times daily. Welsh and Eade found IHN more effective than niacin in its hypocholesterolemic, antihypertensive, and lipotropic effects.20-21
Raynaud’s Disease: A review of the literature reveals numerous positive studies on the use of IHN in Raynaud’s Disease. The typical dosage is 1 g q.i.d. for several months. The mechanism of action appears to be more than just a transient vasodilation, involving lipid-lowering and fibrinolysis. This explains the need for long-term administration.22-23
Intermittent Claudication: The use of niacin esters for the treatment of intermittent claudication secondary to atherosclerosis has been examined extensively. Significant improvement has been reported by several investigators at dosages of 2 g twice daily, typically for at least 3 months. While arterial dilation may be a factor, it has been postulated that reduction in fibrinogen, improvement in blood viscosity, and resultant improvement in oxygen transport are involved in the therapeutic effects.24-26
Other Peripheral Vascular Diseases: IHN appears to have application in the treatment of other conditions resulting from peripheral vascular insufficiency, including threatened amputation from gangrene, restless legs syndrome, stasis dermatitis, atherosclerosis-related migraines, and hypertension.27
Dermatological Conditions: IHN has been used for the treatment of various dermatological conditions with mixed results. Included were lesions of scleroderma, acne, dermatitis herpetiformis, exfoliative glossitis, and psoriasis. IHN appeared to help four out of five patients with dermatitis herpetiformis. The one patient with sclerodermal skin lesions was reported to have improved significantly on 1200 mg IHN daily. The results with other skin conditions have been less promising. It appears the dermatological problems most benefited by IHN are those related to vascular insufficiency.28
Dosage: Recommended dosage for lipid-lowering and improving conditions related to peripheral vascular insufficiency ranges from 1500 mg to 4 g daily, in divided dosages of two to three times daily.
Deficiency: Although the inositol hexaniacinate complex is not an essential nutrient, niacin is vital to cellular metabolism, principally through its role in the coenzymes, nicotine-adenine dinucleotide (NAD) and nicotine-adenine dinucleotide phosphate (NADP), in oxidation-reduction reactions. There are certain population fractions that may be deficient, requiring niacin supplementation to prevent pellagra. These groups include alcoholics and the elderly.
Toxicity: Numerous toxic reactions, both acute and chronic, have been reported from the use of high-dose niacin. Reactions to niacin range from acute symptoms of flushing, pruritis, and GI complaints to chronic symptoms of hepatotoxicity, hyperuricemia, and impaired glucose tolerance. On the other hand, no adverse effects have been reported from the use of inositol hexaniacinate in dosages as high as four grams daily. Despite the lack of reported adverse reactions, use of IHN in patients with known liver disease probably should be avoided. In addition, if high doses (2 grams or greater daily) are being administered, liver enzymes should be monitored every 2-3 months for at least the first six months.29 Although no adverse reactions between inositol hexaniacinate and other nutrients or drugs have been reported, due to its fibrinolytic effect it should be used with caution in conjunction with other blood thinners.
Raising HDL
Most natural medicines that have been shown to decrease cholesterol also help in increasing HDL, while simultaneously lowering LDL.
There are many natural medicines that increase HDL, such as garlic, reishi mushroom, hawthorne berry (Crataegus oxycanthus), nopal (Opuntia cactus), Panax ginseng, garlic, ascorbic acid, and niacin.30-33
The excretion of cholesterol from the body itself is in the form of bile acids and bile salts that are produced from the liver. This pathway can be supported with the use of Panax ginseng, globe artichoke, curcumin, and dandelion root.
Cholesterol in the bile is excreted into stool matter. Normally 25 % is reabsorbed into the small intestine. Natural fiber, such as psyllium husks, oatmeal, and nopal, has shown to be effective in further helping the body to excrete cholesterol.
Minor Hypertension
Hypertension of any sort can be well treated with herbal medicine. For minor hypertension, herbal combinations, such as the following, work very well with no side effects.
Formula for Minor Hypertension
- Hawthorne Berry
- Motherwort
- Valerian
Hawthorne berry (Cratagaus oxycanthus): Hawthorne berry helps not only with hypertension but also hypotension due to its adaptogenic effects. It tones the heart. Hawthorne berry is a rich source of bioflavonoids, which are also important in preventing lipid peroxidation of LDL.34
Motherwort (Leonurus cardiaca): Motherwort is also a tonic for the heart and effective in minor to moderate hypertension. It also can be used as a beverage, eaten fresh in salads, or made into salad dressings.
Valerian (Valerian officinalis): Many patients with hypertension will also be suffering due to stress. Valerian is an ideal herb for hypertension because it is a smooth muscles relaxant of the arterial walls. It too can be consumed safely as a beverage.35
Moderate to Severe Hypertension
Severe hypertension can be also very well treated with herbal medicine. Unlike the herbs mentioned in moderate hypertension, these herbs should not be taken as foods. High doses should not be taken.
Formula for Severe Hypertension:
- Snakeroot
- Jamaican dogwood
- False Hellebore
- Dose: 20 drops two times a day
Snakeroot (Rauwolfia serpentia): The root contains 155 reserpine-rescinnamine groups of alkaloids called reserpine.36 The genus name was named after a German botanist, Dr Rauwolfia. Serpentia refers to the long tapering snakelike roots of the plant. For thousands of years, Rauwolfia has been used in Ayurvedic medicine to treat a variety of disorders, ranging from hypertension and insomnia to insanity. In 1952, scientists isolated the compound alkaloid reserpine from the root for use Western medicine. Currently, there are several drugs with this alkaloid, including Reserpine, Novoreserpine, and Serpasil.37
Jamaican dogwood (Piscidia Erythena). This herb is a smooth muscle relaxant, similar to Valerian, that can be very useful in treating hypertension by relaxing the smooth muscle of the vascular system.
Case Study
Lipids and Thyroid Metabolism Disorder
A 54-year-old female presented with hyperinsulinemia, diabetes, and hyperlipidemia. Her chief purpose for coming to our office was to lower her cholesterol with natural medicines. Physical exam revealed obesity and a temperature of 97.1°F, indicating an underactive thyroid. TSH levels were normal, indicating Wilson’s Temperature Syndrome. A holistic therapy was prescribed to lower her lipids in order to restore healthy thyroid function first because the Wilson’s thryoid syndrome was the root cause of her high lipids and obesity.
Jambul and Devil’s Club Extract: 1 teaspoon, three times a day to balance blood sugar and insulin levels
Kelp: 5 g daily to help with thyroid function
Lifestyle: Regular exercise also to help with thyroid function
Inositol Hexaniacinate: 1 g t.i.d. to lower lipid values
Case Study
Improvement of Essential Hypertension after EDTA Intravenous Infusion Treatment
Compiled by James A. Jackson, MT (ASCP)CLS, PhD, BCLD1, Professor and Chair, Clinical Sciences Department, The Wichita State University, Wichita, Kansas; and Hugh D. Riordan, MD, The Center for the Improvement of Human Functioning International, Inc., Wichita, Kansas.
Reprinted by permission from the Journal of Orthomolecular Medicine 1995;7(1)
This white male patient was first seen at the Center in 1985 for treatment of angina and essential hypertension. He was 51 years of age with a long history of essential hypertension. He was told at about age 18 that he had “high blood pressure” with a systolic blood pressure of 180 mm/Hg. No treatment was prescribed at that time. The history also revealed that both his mother and father died at age 69 of myocardial infarction.
While in his twenties, he became a private pilot and passed three separate FAA flight physical examinations. On each examination a comment was made that “his blood pressure was a little high.” Later, on a physical examination with a different physician, his blood pressure was 170/100 mm/Hg and he was diagnosed with essential hypertension. His medication consisted of daily doses of 120 mg of Inderal(R) “diazide capsules” and 3 SLOKr tablets. He failed his next FAA flight physical because of his essential hypertension and the medication being taken. He continued on medication over a period of 15 years with fluctuations in his blood pressure.
When first seen at the Center, his blood pressure was 140/85 with medication; 180/100 without medication. He was given an initial intravenous infusion of EDTA, which consisted of 3.0 g EDTA 15.0 g ascorbic acid buffered in sodium ascorbate (Bronson Pharmaceuticals), 800 mg magnesium chloride, 40.0 mg procaine, and 1000 units of heparin delivered in 500 mL of sterile, deionized water. Pre- and post-chelation 24 hour urine samples were collected, and aluminum, cadmium, lead, mercury, manganese, chromium, copper, iron, zinc, calcium, and magnesium levels measured.
The lead level was of particular interest, as several published studies demonstrated a relationship of lead levels and hypertension.38-39 His pre-chelation urine lead level was 14.0 mg/24 hours. The post-chelation urine lead level was 91 mg/24 hours. The Center considers a 5-fold increase in urine lead excretion after chelation an indication of increased body load of lead. He was then started on a series of 30 EDTA intravenous infusions administered at approximately weekly intervals over a period of 7 months. Each treatment was transfused over a period of 3-5 hours.
Other post-chelation urine studies were performed over a period of time and showed urine lead level of 39, 40, and 50 mg/24 hours, respectively. Complete blood counts, urinalysis, and chemistry profile were done throughout the treatment and showed no adverse effects of the treatment.
The patient slowly decreased his medication during the EDTA treatment and stopped them completely at the last chelation (March 14, 1986). His blood pressure at the last chelation was 124/84 mm/Hg. He has not taken any blood pressure medication since the last chelation treatment. He also decided to take another flight physical to renew his private pilot license. He passed without any problems.
