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Historically, the use of Iodinated Contrast Media (ICM) for diagnostic purposes, particularly radiography and
computed tomography (CT), is well-known. Many of the ICM are included in the World Health Organization (WHO)’s List
of Essential Medicines. Depending on the chemotype and the presence of ionizable functional group(s), the ICM are categorized in the ionic/nonionic monomers/dimers. The lipophilicity, aqueous solubility, viscosity and osmolality are major characteristics dictating their use for one procedure versus the other. Over last several decades, substantial advancement occurred in the design and development of novel ICM, solely to reduce their propensity to cause adverse effects. Given the nature of their acute usage, some of the agents with appreciable toxicity are still used. Understanding their chemistry aspects is
crucial to appreciate, acknowledge and justify the usage of these extremely important torch-bearers of diagnostic agent’s
class. The present review article presents an in-depth overview of the synthetic methods, therapeutic indications, potential
adverse effects along with the commercial and environmental aspects of ICM. The safety and tolerability of these agents is a
field that has gained significant importance, which is given due importance in the discussion.