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Loperamide is an antidiarrheal agent available as an inexpensive over-the-counter (OTC) medication. In general, it is considered to be safe, but lately, loperamide drug abuse has been reported due to its opioid properties. When used in high doses, several harmful effects including cardiotoxicity, central nervous system (CNS) and respiratory depression have been reported. This prompted the FDA to release a warning in 2016 regarding the arrhythmogenic potential of loperamide. We present a case of a 32-year-old male with a history of polysubstance abuse who presented to the emergency department (ED) requesting “detoxification” from loperamide. The patient complained of opiate withdrawal symptoms including chills, nausea, vomiting, constipation, and abdominal cramps thought to be secondary to the abuse of loperamide. He was found to have right bundle branch block (RBBB) and bradycardia with a heart rate (HR) of 51 beats per min (bpm). He also reported an unexplained syncopal episode, one day prior to visiting the ED. In the current case report, we discuss loperamide abuse, its harmful effects, and management.