This paper proposes the closed-form analytical design of proportional-integral (PI) controller parameters for the optimal control of an open-loop unstable first order process subject to operational constraints. The main idea of the design process is not only to minimize the control performance index, but also to cope with the constraints in the process variable, controller output, and its rate of change. To derive an analytical design formula, the constrained optimal control problem in the time domain was transformed to an unconstrained optimization in a parameter space associated with closed-loop dynamics. By taking advantage of the proposed analytical approach, a convenient shortcut algorithm was also provided for finding the optimal PI parameters quickly, based on the graphical analysis for the optimal solution of the corresponding optimization problem in the parameter space. The resulting optimal PI controller guarantees the globally optimal closed-loop response and handles the operational constraints precisely.