API Nicorandil

Nicorandil More Info

Nicorandil is a unique anti-anginal medication that combines the properties of a nitrate vasodilator and a potassium channel opener. It is primarily used for the treatment of chronic stable angina pectoris, particularly in patients who are intolerant to or have contraindications for β-blockers or calcium channel blockers.

Product Overview

Chemical Identity:

IUPAC Name: N-[2-(nitrooxy)ethyl]-3-pyridinecarboxamide

Molecular Formula: C₈H₉N₃O₄

Molecular Weight: 211.17 g/mol

CAS Number: 65141-46-0

Physical Form: White to off-white crystalline solid

Pharmacological Class:

Dual-Action Mechanism: Functions as a potassium channel activator and a nitrate donor. This dual action leads to both arterial and venous dilation, reducing both afterload and preload, and improving coronary blood flow without causing a steal phenomenon.

Metabolism: Primarily metabolized via denitration into the nicotinamide pathway; less than 20% excreted unchanged in urine.

Formulation and Packaging

Dosage Forms:

Tablets: Typically available in 5 mg, 10 mg, and 20 mg strengths. The recommended starting dose is usually 10 mg taken twice daily, with a maximum of 30 mg per day if needed.

API: Also supplied as a pure compound for research purposes, with purity specifications often exceeding 99% (e.g., 99.44% purity).

Packaging:

Common packaging includes 1 mg, 5 mg, 10 mg, 100 mg, 250 mg, 500 mg, and 1 g quantities for the API form.

Storage and Stability

Recommended Storage Conditions: Store in a tightly sealed container, protected from light, and at a temperature of -20°C for optimal stability. The product typically has a shelf life of up to 3 years under these conditions.

Solubility: Nicorandil is poorly soluble in water but soluble in organic solvents such as ethanol, methanol, DMF, DMSO, and ether.

Safety and Handling

Contraindications: Not recommended for use in patients with cardiogenic shock, severe hypotension, or left ventricular failure with low filling pressures.

Potential Interactions: Caution is advised when co-administering with PDE-5 inhibitors (e.g., Sildenafil), as the combination may lead to severe hypotension.

Regulatory Status: Approved and marketed in many countries, including the UK, Japan, and several European nations, under various trade names such as Ikorel, Angedil, and Dancor. However, it is not approved by the US FDA.