The use of buprenorphine in the preparation of a medicament for a method of effectively treating pain in humans is achieved by administering buprenorphine in a manner indicative of first order pharmacokinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in a manner indicative of zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.