Background: Use of medications containing the 5-aminosalicylic acid (5-ASA) moiety may cause a rare but potentially lethal side effect involving inflammation of the heart (myocarditis) or pericardium (pericarditis) or both (myopericarditis). Early recognition of 5-ASA as the cause is important to prevent progression of the inflammation. Objective: To provide clinicians with information to assist in recognizing the signs and symptoms of 5-ASA-induced cardiac inflammation and the characteristics of the suspected therapy, and in determining the appropriate approach to treatment. Data Sources, Study Selection, and Data Extraction: The Embase database was searched, for the period 1974 to July 17, 2015, for published descriptions of cases of cardiac inflammation caused by 5-ASA-containing medications. The search terms included the names of specific agents, as well as terms for different types of cardiac inflammation. Articles in any language were retained for inclusion in this narrative review. Findings: There is no symptom, sign, laboratory test, or constellation of symptoms and signs that is pathognomonic for 5-ASA-induced myocardial-pericardial toxicity. Similarly, there is no single laboratory, electrocardiographic, or echocardiographic finding or combination of findings that implicates 5-ASA as the cause of nonspecific symptoms. However, most patients present with chest pain, shortness of breath, and fever within the first 28 days after initiating 5-ASA. Physical examination, electrocardiography, and diagnostic imaging will yield findings consistent with myocarditis, with or without accompanying pericarditis. Prompt discontinuation of the 5-ASA will result in resolution of symptoms within days, without the need for any adjunctive therapies. Rechallenge with any 5-ASA-containing compound carries a high risk for recurrence of the inflammation. Conclusions: Any patient presenting with chest pain, shortness of breath, or fever within 28 days after initiating a 5-ASA-containing drug should be considered as exhibiting drug-induced inflammation. The 5-ASA-containing drug should be stopped immediately until other causes can be proven (or excluded); if no other cause is discovered, the 5-ASA should not be restarted.