Methyl nicotinate:Mechanism, Uses and Toxicity

Methyl nicotinate is a herbal, tobacco, and warm tasting compound. Methyl nicotinate has been detected, but not quantified in, several different foods, such as fruits, robusta coffees (Coffea canephora), papayas (Carica papaya), alcoholic beverages, and arabica coffees (Coffea arabica). This could make methyl nicotinate a potential biomarker for the consumption of these foods.

Mechanism of action

While the mechanism of action of methyl nicotinate and other topically-administered nicotinic acid esters is not clear, it is thought that methyl nicotinate promotes the release of prostaglandin D2 that is strictly locally-acting due to its short half-life. It was demonstrated in human subjects that the local cutaneous vascular response to methyl nicotinic was suppressed by inhibitors of prostaglandin biosynthesis, indicating that the effect of methyl nicotinate on vascular smooth muscles may be mediated by the release of local prostaglandins. Prostaglandins released from the skin and blood vessels induce cutaneous vasodilation.

Uses

Methyl nicotinate is the methyl ester of Niacin that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation. For veterinary purposes, methyl nicotinate is used to treat respiratory diseases, vascular disorders, rheumatoid arthritis, and muscle and joint pains.

Toxicity

The acute subcutaneous LD50 of structurally-related nicotinamide and nicotinic acid in rats were 1.68 and 5.0 g/kg bw, respectively. In humans, oral ingestion of 3-9 g of nicotinic acid per day resulted in "niacin hepatitis", gout, and impaired glucose intolerance within a short period of time.

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