Nicorandil

Nicorandil

Clinical data
Pregnancy category	AU: B3
Routes of administration	Oral
ATC code	C01DX16 (WHO)
Legal status
Legal status	UK: POM (Prescription only)
Pharmacokinetic data
Bioavailability	75 to 80%
Protein binding	25%
Metabolism	Hepatic
Elimination half-life	1 hour
Excretion	Renal (21%)
Identifiers
IUPAC name 2-(pyridine-3-carbonylamino)ethyl nitrate
CAS Number	65141-46-0
PubChem CID	47528
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C8H9N3O4
Molar mass	211.175 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

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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.

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