Methylnicotinate
Methylnicotinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Methylnicotinate 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 .
Following topical administration, methyl nicotinate acts as a peripheral vasodilator to enhance local blood flow at the site of application. It induced vasodilation of the peripheral blood capillaries which are located in the dermal papillae of upper dermis layers adjacent to the epidermis–dermis junction . During tissue penetration at the dermis, methyl nicotinate is hydrolyzed to nicotinic acid . In human volunteers, topical administration of methyl nicotinate caused vasodilation-induced generalized cutaneous erythema .
| Trade Name | Methylnicotinate |
| Generic | Methyl nicotinate |
| Methyl nicotinate Other Names | 3-(Carbomethoxy)pyridine, Heat spray, Methyl nicotinate, Methyl-nicotinate, Methylnicotinate |
| Type | |
| Formula | C7H7NO2 |
| Weight | Average: 137.136 Monoisotopic: 137.047678473 |
| Protein binding | No pharmacokinetic data available. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Methylnicotinate is a methyl ester of niacin used to treat muscle and joint pain.
Indicated for the temporary relief of aches and pains in muscles, tendons, and joints.
Methylnicotinate is also used to associated treatment for these conditions: Generalized joint pain, Localized muscle pain, Soreness, Muscle
How Methylnicotinate works
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 .
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 .
Food Interaction
No interactions found.Volume of Distribution
According to the animal studies, nicotinic acid is mainly concentrated in the liver, kidneys, and adipose tissue .
Elimination Route
The presence of methyl group facilitates the penetration of methyl nicotinate through the skin with good lipophilicity, allowing rapid absorption following topical administration . In vitro, about 80-90% of the polar compounds methyl nicotinate rapidly penetrated the skin . It was demonstrated in excised skin of hairless mice that methyl nicotinate can effectively bypass the stratum corneum layer of the skin . In humans, nicotinic acid and nicotinamide were shown to be rapidly absorbed from the stomach and intestine via a sodium carrier-mediated mechanism at low concentrations .
Half Life
In vitro, the half-life of methyl nicotinate in the dermis was 3 to 10 minutes .
Clearance
No pharmacokinetic data available.
Elimination Route
Following epicutaneous administration of small radiolabelled dose of methyl nicotinate in human volunteers, approximately 15% of the dose was recovered in the urine within 108 hours after treatment . The excretion of nicotinic acid mainly takes place in the kidneys .
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