Rifampicin (DB01045): A Comprehensive Pharmacological and Clinical Monograph

Section 1: Introduction and Historical Context

1.1. Overview

Rifampicin, also known internationally as rifampin, is a semisynthetic antibiotic belonging to the ansamycin class.[1] It stands as a cornerstone in the modern therapeutic armamentarium against several critical bacterial infections, most notably tuberculosis (TB). For over half a century, it has been a first-line agent in multi-drug regimens designed to combat

Mycobacterium tuberculosis, the causative agent of TB, and remains indispensable for treating other mycobacterial diseases such as leprosy (Hansen's disease) and infections caused by Mycobacterium avium complex.[1] Its broad-spectrum activity extends to various Gram-positive and select Gram-negative bacteria, underpinning its use in niche indications like the eradication of meningococcal carriage and the management of severe staphylococcal infections.[2]

The profound efficacy of rifampicin is rooted in its unique mechanism of action: the highly specific inhibition of bacterial DNA-dependent RNA polymerase, which effectively halts transcription and protein synthesis, leading to a bactericidal effect.[2] This monograph provides a comprehensive examination of rifampicin, exploring its journey from a soil microbe to a life-saving medication. It will detail its chemical and physical properties, its complex pharmacology, its wide-ranging clinical applications, and its challenging safety profile. The central theme that emerges is that of a "double-edged sword": a profoundly effective antibiotic whose clinical utility is perpetually balanced by the rapid emergence of microbial resistance when used improperly and a formidable profile of drug-drug interactions that complicates its administration in an era of polypharmacy.[1]

1.2. Discovery and Development