Inositol Niacinate

Uses

Inositol Niacinate has a fairly broad range of therapeutic applications. The most well researched conditions include the hyperlipidemias, Raynaud's disease and intermittent claudication. Promising applications, which bear further investigation, include its use for stasis ulcers, dysmenorrhea, dermatitis herpetiformis, alcoholism, diabetes, cancer prevention and hypertension.

How Inositol Niacinate works

Inositol nicotinate and other niacins directly and noncompetitively inhibit microsomal enzyme diacylglycerol acyltransferase 2 (DGAT2) responsible for esterification of fatty acids to form triglycerides, resulting in decreased triglyceride synthesis and hepatic atherogenic lipoprotein secretion. Inhibitied triglyceride synthesis results in accelerated intracellular hepatic apo B degradation and the decreased secretion of VLDL and LDL particles . Niacin also inhibits hepatic expression of beta-chain adenosine triphosphate synthase which inhibits the removal or uptake of HDL–apo A-I. It is also suggested that niacin increases vascular endothelial cell redox state, resulting in the inhibition of oxidative stress and vascular inflammatory genes or key cytokines involved in atherosclerosis. It acts as a ligand on G-protein coupled receptor 109A (HCAR2/HM74A) and 109B (HCAR3/HM74) which mediates the anti-lipolytic and lipid-lowering effects of nicotinic acid. Niacin-mediated signalling of GPR109A expressed on adipocytes and G(i)-mediated decrease in cAMP levels result in decreased lipolysis, fatty acid mobilization, and triglyceride synthesis. The action of inositol nicotinate on GPR109A expressed on skin and macrophages to cause increased prostaglandin D2/E2 activity is thought to be less significant compared to other niacin molecules as it involves sustained release that leads to less flushing .

Dosage

Inositol Niacinate dosage

Recommended dosage for lipid-lowering and improving conditions related to peripheral vascular insufficiency ranges from 1500 mg to 4000 mg daily, in divided dosages of two to three times daily.

Side Effects

The most common side effects are headache, rash, paraesthesia, dizziness, nausea and vomiting, flushing, excessive fluid retention in the body tissues, postural hypotension, fainting

Toxicity

NOAEL is 4000mg. Inositol nicotinate can cause muscle pain, headache, redness of face, nausea, vomiting, edema and rash.

Precaution

Cautions should be exercised in patients with angina not well controlled by medical treatment and decreased blood supply through the vessels of the brain (cerebrovascular insufficiency).

Food Interaction

Volume of Distribution

Mean Vd following intravenous administration of 50mg/kg of inositol nicotinate in rats is 1051±250 mL/kg .

Elimination Route

Gastrointestinal absorption of inositol hexanicotinate varies widely, with an average of 70% of an orally ingested dose absorbed from stomach and upper small intestines into the bloodstream as intact form. The maximum serum levels of nicotinic acid is reached approximately 6-10 hours after oral ingestion. At low concentrations, the absorption of nicotinic acid and nicotinamide is mediated by sodium ion-dependent facilitated diffusion. At higher concentrations, passive diffusion predominates with doses of 3 to 4 g of niacin being almost completely absorbed .

Half Life

Mean elimination half life in healthy human adults is approximately one hour .

Clearance

Mean clearance rate following intravenous administration of 50mg/kg of inositol nicotinate in rats is 65.4±19 mL/min/kg .

Elimination Route

Unabsorbed inositol nicotinate is detected in feces.

Pregnancy & Breastfeeding use

Pregnancy: There is no information available about the safety of this medicine during pregnancy, therefore it is not recommended for use during pregnancy, unless considered essential by your doctor. Seek medical advice from your doctor.

Lactation: There is no information available regarding the safety of this medicine during breastfeeding

Contraindication

Inositol nicotinate is contraindicated to children, early stage of stroke & people who have recently had a heart attack. It should not be used if anyone is allergic to one or any of its ingredients

Acute Overdose

Both acute and chronic toxicities have been reported from the use of highdose 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

Storage Condition

Should be stored in cool and dry place

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