Pain syndrome accompanies absolute majority of diseases, therefore problems of adequate anesthesia remain acute not only for urgent conditions but also for everyday medical practice. Modern approaches of anesthetic therapy should consider not only pathogenic mechanisms of evolving pain syndrome by a certain patient but also necessity to administer drug combinations. It allows potentiating an analgesic effect, to decrease effective dosages of individual drugs and minimize adverse effects. The administration of non-steroidal anti-inflammatory drugs together with B vitamins and tolperisone is justified in a marked pain syndrome with a spastic component and/or spasms of skeletal muscles, muscle contractures, myofascial pain syndromes, as well in rehabilitation therapy after orthopedic and traumatology surgeries. The article considers pathogenic details of such combined therapy, discloses mechanism of synergic action of the proposed drug combination.