Nicorandil

Nicorandil is an active substance that is used to treat angina pectoris. It belongs to the group of vasodilators. It has vasodilating and blood pressure-lowering properties. Nicorandil is an organic nitrate and a combination of nicotinamide (vitamin B3) and ethyl nitrate. It lowers the preload and afterload of the heart, relieves it and increases blood flow in the coronary vessels.

Nicorandil is a potassium channel opener and nitric oxide donor (NO donor) in arteries and veins. It binds to the sulfonylurea receptors (SUR2) in the muscle cells of the blood vessels. This leads to increased ATPase activity and consequently to a reduced ATP concentration in the cell. This causes the ATP-dependent potassium channels to open and a potassium outflow occurs. The result is hyperpolarization of the muscle cells in the vessels and muscle relaxation with subsequent vasodilation. The hyperpolarization also causes voltage-dependent calcium channels to close, which leads to prolonged vasodilation. Nicorandil also releases nitric oxide, which activates guanylate cyclase. This subsequently leads to dephosphorylation of myosin, resulting in relaxation of the muscle cells.

Nicorandil is broken down via the liver and excreted via the kidneys. The bioavailability of Nicorandil, i.e. the percentage of the active substance available in the blood, is 75%. The half-life, the time the body needs to excrete half of the active substance, is one hour. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood), is reached after 30-60 minutes and is approx. 300 ng/ml.

Always take Nicorandil exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose is 10 mg - 20 mg twice a day .

The maximum daily dose is 40 mg.

The following side effects may occur:

Very common:

• Headache

Common:

• Skin abscess
• Dizziness
• Cardiac arrhythmia
• Reddening of the skin
• Nausea and vomiting
• Feeling of weakness

Occasionally:

• Conjunctivitis (inflammation of the conjunctiva)
• Eye damage
• Corneal damage
• Drop in blood pressure

Rarely:

• Skin rash
• Itching
• Muscle pain

Very rare:

• High potassium levels in the blood (hyperkalemia)
• Liver problems
• Swelling due to an allergic reaction
• Stomach pain

Frequency unknown:

• Double vision

Interactions may occur if the following medicines are taken at the same time:

• Medications for impotence such as sildenafil, tadalafil or vardenafil
• Medication for pulmonary hypertension such as riociguat
• Medication for high blood pressure
• Drugs that dilate the blood vessels
• Drugs that increase blood potassium levels
• Dapoxetine
• Medication for the treatment of inflammation (corticosteroids, NSAIDs)
• Medication for depression
• Acetylsalicylic acid (aspirin)

Nicorandil must NOT be taken in the following cases:

• if you are allergic to Nicorandil
• in the case of low blood pressure (hypotension)
• in cardiogenic shock
• in case of left heart failure
• in case of cardiac decompensation
• when taking medication for erectile dysfunction such as sildenafil, tadalafil or vardenafil
• when taking medication for the treatment of pulmonary hypertension such as riociguat
• with reduced blood volume
• for fluid accumulation in the lungs (pulmonary oedema)

Nicorandil should only be used from the age of 18 .

Nicorandil should NOT be taken during pregnancy and breastfeeding.