Creating an effective learning environment is not an easy task in today’s world and is even more complex in nursing education. Innovative teaching learning approaches such as role-playing and simulation games were utilized primarily to determine its effectiveness in teaching and learning pharmacological concepts. This study considered the experimental method of research that utilized the pretest-posttest true-control group design. Findings of the study revealed that innovative teaching learning approach was very effective in teaching pharmacological concepts such as general principles and basic concepts in pharmacology; hematologic, hormones, steroids, and thyroid hormones; and immunologic, musculoskeletal, anti-arthritis, and topical medications. In addition, lecture-discussion method of instruction was effective in teaching pharmacological concepts. However, the innovative teaching-learning approach was found to be more effective particularly in allergy, anti-infective, antineoplastic, and respiratory medications; cardiovascular, renal-diuretics, central nervous system, and gastrointestinal medications; and hematologic hormones, steroids and thyroid hormones. Hence, innovative teaching and learning pharmacological concepts is effective in acquisition, retention and provides a key to the structure of one’s personality and general behavior. It is therefore recommended that role playing and simulation games be utilized as teaching approaches to make learning fun and to enhance students retention and communication skills.