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Nicorandil

What is Nicorandil?

Nicorandil is a niacinamide derivative. It is a nitrate and ATP-sensitive K+ channel agonist that acts as a vasodilator and antianginal medication. It is available in India, the United Kingdom, Japan, most of Europe, the Philippines, Taiwan, Australia and South Korea. It was patented in 1976 and approved for medical use in 1983. It hasn’t been authorised as a drug by the FDA yet. It’s usually used for those with angina who are still experiencing symptoms despite getting effective anti-anginal therapy and is generally administered through the oral route.

Nicorandil is marketed under the brand names Ikorel (in the United Kingdom, Australia and most of Europe), Angedil (in Romania, Poland), Dancor (in Switzerland), Nikoran, PCA (in India), Aprior (in the Philippines), Nitorubin (in Japan), and Sigmart (in Japan, South Korea, Taiwan and China). Nicorandil is not available in the United States.

Macsen Laboratories is the leading manufacturer and supplier of Nicorandil with GMP and ISO certification.
PRODUCT SPECIFICATIONS
Name of Product Nicorandil
IUPAC Name 2-(pyridine-3-carbonylamino)ethyl nitrate
Pharmacopoeial Name Nicorandil
Synonyms 2-Nicotinamidoethyl nitrate, Nicorandilum, Ikorel, Dancor, Sigmart, Adancor, 2-(nicotinamido)ethyl nitrate, Nicorandilo
CAS No 65141-46-0
Molecular Formula C8H9N3O4
Molecular Weight 211.17 g/mol
Pubchem CID 47528
Pubchem SID 462770288
WHO-GMP Available soon
WC Available soon
DMF Available soon

Chemical Properties

SR. No Criteria Limit/Specification
1 Appearance (Color) White to Beige
2 Appearance (Form) Powder
3 Solubility (Turbidity) Clear
4 Storage Temperature Room Temperature
5 Concentration
DMSO
≥ 10.0 mg/ml
6 Purity (HPLC) ≥ 97.5 %
7 Identity Confirmed
8 Water Content ≤ 2.0 mol
9 Elemental Composition Pass

Uses

Nicorandil is primarily used to treat and prevent Angina pectoris. Angina is chest pain that results from episodes of transient myocardial ischemia which can be caused by diseases such as atherosclerosis, coronary artery disease and aortic stenosis. Vasospasm of the coronary arteries is a common cause of angina. It is also used to reduce the risk of acute coronary syndromes.

Mechanism of Action

  • Vasodilation – Nicorandil promotes vasodilation by activating ATP-sensitive potassium (K-ATP) channels in the smooth muscle cells of blood vessel walls. Activation of these channels leads to reduced calcium influx, which lowers the smooth muscle contraction. This relaxation of blood vessels lowers both preload and afterload, thereby decreasing the heart’s workload and alleviating anginal symptoms.
  • Cytoprotective Effect – Nicorandil exerts cytoprotective effects by opening mitochondrial K-ATP channels in cardiac myocytes. This mechanism helps protect heart tissue during hypoxic conditions, such as myocardial ischemia, by preserving cellular integrity and function. It contributes to the overall cardioprotective profile of the drug.
  • Nitric Oxide (NO) Mediation – Nicorandil also functions as a nitric oxide donor. It activates guanylate cyclase in vascular smooth muscle, which increases intracellular cyclic GMP (cGMP) levels. Elevated cGMP induces smooth muscle relaxation and further enhances vasodilation, particularly in the venous system.

Side effects

The side effects associated with Nicorandil are as follows:

  • Flushing (sense of warmth in the face, ears, neck, and trunk)
  • Weakness
  • Vomiting
  • Palpitations
  • Perianal, ileal, and peristomal ulceration
  • Severe migraine
  • Toothache
  • Nasal Congestion

FAQs

Q. Is Nicorandil a beta blocker?

Nicorandil is a potassium channel activator having arterial vasodilator properties. Furthermore, due to the presence of a nitrate group in its chemical composition, nicorandil also exhibits venodilating characteristics.

Q. What does Nicorandil do?

Nicorandil, being a vasodilator drug, works by widening the blood vessels. This increases the supply of blood and oxygen to the heart, thus helping to reduce angina attacks. It can also reduce the risk of further heart conditions.

Q. Is Nicorandil a blood thinner?

Nicorandil is not a blood thinner but is a vasodilatory drug used to treat angina.

Q. Which drug class does Nicorandil belong to?

Nicorandil belongs to the class of potassium channel activators, also described as a nitrate derivative. It works by dilating the blood vessels and increasing the supply of blood and oxygen to the heart.

Q. How quickly does Nicorandil work?

Generally, Nicorandil takes 30 to 60 minutes to show its action after its oral administration. However, its action also depends upon the dose and individual response.

Q. What drugs interact with Nicorandil?

Nicorandil interacts with several classes of medications, like phosphodiesterase 5 inhibitors, NSAIDs, and corticosteroids, potentially enhancing their adverse reactions.

Q. Is Nicorandil available in the USA?

Nicorandil is not approved by the U.S. Food and Drug Administration (FDA) and is therefore unavailable for prescription or over-the-counter (OTC) use in the United States.

Q. What is the popular brand name of Nicorandil?

The most widely recognized brand name for nicorandil is Ikorel. It is also sold under various brand names depending on the country and manufacturer, like Nicoril, Angedil, and Aprenor.

Q. Does Nicorandil cause weight gain?

Nicorandil is generally not associated with weight gain, though some reports indicate potential weight loss due to side effects.

Resources on Nicorandil

Nicorandil | Mechanism of action, Uses & Side effects

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