Nicorandil

Oral
Stable angina

May be taken with or without food.

Acute pulmonary oedema, severe hypotension, cardiogenic shock, cardiac decompensation, hypovolaemia, left ventricular failure with low filling pressure. Coadministration with phosphodiesterase 5 (PDE-5) inhibitors and soluble guanylate cyclase stimulators (e.g. riociguat).

Patient with heart failure (NYHA class III and IV), hypertrophic obstructive cardiomyopathy, aortic stenosis, low systolic blood pressure, diverticular disease, G6PD deficiency, glaucoma, hyperkalaemia. Renal and hepatic impairment. Elderly. Pregnancy and lactation.

Significant: Gastrointestinal ulceration which may lead to perforation, fistula, abscess formation, and haemorrhage; skin or mucosal ulceration (e.g. perianal, genital or parastomal ulceration), severe hypotension, dose-related headache (particularly during initial dosing). Rarely, severe hyperkalaemia, ocular effects (e.g. conjunctivitis, conjunctival and corneal ulcers).
Cardiac disorders: Chest pain, palpitation.
Gastrointestinal disorders: Nausea, vomiting, abdominal pain, rectal bleeding, dyspepsia.
General disorders and administration site conditions: Weakness, lethargy.
Infections and infestations: Skin abscess.
Investigations: Increased heart rate.
Musculoskeletal and connective tissue disorders: Myalgia, back pain.
Nervous system disorders: Dizziness, vertigo.
Respiratory, thoracic and mediastinal disorders: Dyspnoea, bronchitis, respiratory tract disease.
Skin and subcutaneous tissue disorders: Rash, angioedema.
Vascular disorders: Cutaneous vasodilation, flushing.

This drug may cause dizziness, if affected, do not drive or operate machinery.

Monitor blood pressure and heart rate.

Symptoms: Reflex tachycardia, peripheral vasodilation with a fall in blood pressure. Management: Supportive treatment. Monitor cardiac function. May consider substitution of fluid to increase circulating plasma volume. Consider administering vasopressors in life-threatening situations.

Increased risk of gastrointestinal ulceration and haemorrhage with NSAIDs and aspirin. Increased risk of gastrointestinal perforation with corticosteroids. Hypotensive effects may be increased with antihypertensive drugs, other vasodilators, and TCAs. May increase the risk of hyperkalaemia with other agents that elevate serum K levels. Enhanced orthostatic hypotensive effect with dapoxetine.
Potentially Fatal: Significantly enhanced hypotensive effects with PDE-5 inhibitors (e.g. sildenafil, vardenafil, tadalafil) and soluble guanylate cyclase stimulators (e.g. riociguat).

Hypotensive effect may be increased with alcohol.

Description:
Mechanism of Action: Nicorandil, a nitrate derivative of nicotinamide, is an antianginal agent with a dual mechanism of action. It acts as a vasodilator by activating the K channels which cause vascular membrane hyperpolarisation, thereby dilating the arterioles and large coronary arteries and decreasing cardiac afterload. Additionally, its nitrate component relaxes the venous vascular smooth muscle by increasing cyclic guanosine monophosphate (cGMP) resulting in reduced preload.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Absolute bioavailability: 75%. Time to peak plasma concentration: 30-60 minutes.
Distribution: Plasma protein binding: 25-41.5%.
Metabolism: Metabolised in the liver via denitration into N-(2-hydroxyethyl)-nicotinamide (major metabolite), nicotinuric acid, nicotinamide, N-methylnicotinamide and nicotinic acid.
Excretion: Via urine (approx 20% mainly as metabolites, approx 1% as unchanged drug). Elimination half-life: Approx 1 hour.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 47528, Nicorandil. https://pubchem.ncbi.nlm.nih.gov/compound/Nicorandil. Accessed Apr. 27, 2023.

Store below 25°C. Protect from moisture.

Thuốc chống đau thắt ngực

C01DX16 - nicorandil ; Belongs to the class of other vasodilators used in cardiac diseases.

Anon. Nicorandil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2023.

Buckingham R (ed). Nicorandil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2023.

Joint Formulary Committee. Nicorandil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2023.

Nicoril 10 mg Tablets (Rivopharm UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 04/04/2023.

Pharmacy Retailing (NZ) Ltd t/a Healthcare Logistics. Ikorel 10 mg and 20 mg Tablets data sheet 20 June 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 04/04/2023.