Guanfacine (DB01018): A Comprehensive Pharmacological and Clinical Monograph

I. Drug Identification and Physicochemical Profile

1.1. Overview and Classification

Guanfacine is a centrally acting sympatholytic agent, pharmacologically classified as a highly selective alpha-2A (α2A​) adrenergic receptor agonist.[1] Originally developed and approved for the treatment of hypertension, its distinct neuropharmacological properties, particularly its effects on the prefrontal cortex, have led to its successful repurposing for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) in pediatric populations.[3] In the context of ADHD management, it is categorized as a non-stimulant medication, offering a distinct therapeutic alternative to traditional psychostimulants like methylphenidate and amphetamines.[5]

Under the Anatomical Therapeutic Chemical (ATC) classification system, guanfacine is assigned the code C02AC02. This places it in the therapeutic group for cardiovascular system drugs (C), specifically antihypertensives (C02), antiadrenergic agents with central action (C02A), and imidazoline receptor agonists (C02AC).[4] This classification reflects its initial development as an antihypertensive agent, though its modern clinical utility has expanded significantly into the realm of neuropsychiatry.

1.2. Nomenclature and Identifiers

The precise identification of a chemical entity is paramount in scientific and clinical discourse. Guanfacine is identified by a standardized set of names and codes to ensure unambiguous reference across global databases and scientific literature.