Inflammatory reaction is the most common characteristic reactions of tissue or organ injury. Sepsis and ischemia/reperfusion injury in organs can cause the massive release of inflammatory factors, resulting in systemic inflammatory response syndrome or multiple organ dysfunction syndrome. Regulation of inflammatory factors is an important method to ameliorate organ and tissue injury. In the present study, we investigated the regulation of penehyclidine hydrochloride on inflammatory factors, as well as the safety and effectiveness of its protective effects on tissue and organ injury. Recent studies concerning the regulation of the inflammatory response by penehyclidine hydrochloride were summarized, especially the protective effects of penehyclidine hydrochloride on the lung, and the anti-inflammatory protective effect on other organs such as the heart, brain, kidneys and liver. It is necessary to further explore the mechanisms of penehyclidine hydrochloride in tissue and organ protection.