Nicorandil
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| Nicorandil
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| Systematic (IUPAC) name | |
| 2-(pyridine-3-carbonylamino)ethyl nitrate | |
| Identifiers | |
| CAS number | |
| ATC code | C01 |
| PubChem | |
| Chemical data | |
| Formula | C8H9N3O4 |
| Mol. mass | 211.175 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 75 to 80% |
| Protein binding | 25% |
| Metabolism | Hepatic |
| Half life | 1 hour |
| Excretion | Renal (21%) |
| Therapeutic considerations | |
| Pregnancy cat. |
B3(AU) |
| Legal status | |
| Routes | Oral |
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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1] Phone:617-632-7753
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Overview
Nicorandil is a drug used to treat angina. It is marketed under the trade names Ikorel (in the United Kingdom, Australia and most of Europe), Zynicor (in India) and Sigmart (in Japan, South Korea and Taiwan). Nicorandil is not available in the United States.
Mechanism of action
Nicorandil acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It does this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of GMP leading to both arterial and venous vasodilatation. As it is selective for vascular potassium channels, it has no significant action on cardiac contractility and conduction.
Although it can dilate the coronary vessels of a healthy individual, its effects on the coronary vessels of someone with ischaemic heart disease will be little as they will already be completely dilated. Instead, it dilates the venous system, reducing preload and the work of the heart.
Side effects
Common side effects include flushing, palpitation, weakness, headache, mouth ulcers, nausea and vomiting. More recently peri-anal, ileal and peri-stomal ulceration has been reported as a side effect. Anal ulceration is now included in the British National Formulary as a recognised side effect.
References
- Kukovetz WR et al (1992). Molecular mechanism of action of nicorandil. Journal of Cardiovascular Pharmacology 20 Suppl.3:S1–S7.
- Tripathi, K.D. Essentials of Medical Pharmacology, chapter 37, page 499.
Vasodilators used in cardiac diseases (C01D) | |
|---|---|
| Nitrates | Glyceryl trinitrate • Isosorbide dinitrate • Isosorbide mononitrate • Molsidomine • Pentaerythritol tetranitrate |
| Quinolone vasodilators | Flosequinan |
| Others | Itramin tosilate • Prenylamine • Oxyfedrine • Benziodarone • Carbocromen • Hexobendine • Etafenone • Heptaminol • Imolamine • Dilazep • Trapidil • Molsidomine • Efloxate • Cinepazet • Cloridarol • Nicorandil • Linsidomine • Nesiritide • Gapicomine |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
