Pinacidil API Manufacturers & Suppliers

Pinacidil (CAS Number 60560-33-0) is a pharmaceutical compound classified chemically as a pyridine derivative and pharmacologically as a potassium channel opener. It is a cyanoguanidine drug that acts primarily through the activation of ATP-sensitive potassium (K_ATP) channels in arteriolar smooth muscle cells.

The mechanism of action involves the opening of these ATP-sensitive potassium channels, leading to hyperpolarization of the vascular smooth muscle cell membrane. This hyperpolarization decreases calcium influx through voltage-dependent calcium channels, resulting in relaxation of arteriolar smooth muscle. The consequent vasodilatation reduces peripheral vascular resistance, thereby lowering blood pressure.

Pinacidil’s pharmacological activity situates it within several drug categories including antihypertensive agents, cardiovascular agents, and vasodilators. It has been identified as a substrate for the cytochrome P450 enzyme system, particularly CYP3A4, indicating potential interactions with other drugs metabolized by this pathway.

Key absorption, distribution, metabolism, and excretion (ADME) characteristics include its metabolism via CYP3A4 isoenzymes, although comprehensive ADME parameters are not extensively characterized in publicly available literature. The renal and hepatic clearance pathways may be relevant to its pharmacokinetic profile, given its systemic vasodilatory effects.

Safety and toxicity data highlight that pinacidil has been withdrawn from the U.S. market by the FDA, which suggests concerns related to safety or tolerability. Common class-associated adverse effects for potassium channel openers include reflex tachycardia, fluid retention, and potential for hypotension, although specific clinical data for pinacidil should be referenced from regulatory communications.

While clinical indications were not explicitly provided, pinacidil was primarily utilized as an antihypertensive agent aimed at managing elevated blood pressure through vasodilation.

In terms of sourcing and quality considerations, procurement of pinacidil API requires strict adherence to Good Manufacturing Practice (GMP) standards, given its pharmacologically active nature and involvement with CYP3A4 metabolism. Analytical rigor in purity, assay, and residual solvent assessment is critical to ensure suitability for pharmaceutical formulation and compliance with regulatory expectations. Due to its discontinued status and specialized use, sourcing may be limited and should be verified with current supplier certifications and regulatory clearances.