A Comprehensive Monograph on Cimetidine (DB00501)

Introduction: A Paradigm of Rational Drug Design

Cimetidine's Place in Medical History: The Pre- and Post-Cimetidine Eras of Ulcer Therapy

Prior to the mid-1970s, peptic ulcer disease was a formidable and often life-threatening condition. Management was largely palliative, relying on bland diets and rudimentary antacids, with severe cases frequently culminating in invasive and debilitating surgeries like vagotomy or partial gastrectomy.[1] The introduction of cimetidine, marketed under the brand name Tagamet, represented a watershed moment in gastroenterology and pharmacology. Developed by a team at Smith Kline & French (SKF) in the United Kingdom, the drug entered commercial use in 1976 and was approved in the United States in 1979, fundamentally transforming the treatment of acid-related disorders.[3] So profound was its impact that many clinicians and medical historians now delineate the history of ulcer therapy into two distinct epochs: the era before cimetidine and the era after.[4] This single molecule shifted the therapeutic paradigm from surgical intervention to effective medical management, alleviating suffering for millions and earning a place on the World Health Organization's list of essential medicines.[4]

The Scientific Journey: From Histamine Theory to the First H2-Receptor Antagonist

The development of cimetidine stands as a landmark achievement in the history of pharmaceutical science, not merely for its therapeutic success but for the methodology that produced it. It is one of the earliest and most celebrated examples of rational drug design, a process where a therapeutic agent is logically engineered based on a deep understanding of pathophysiology and molecular targets, rather than being discovered through serendipity or mass screening.[1]