Ankle capsular ligamentous apparatus damage is one of the most common problems. Ankle injuries account for one-fifth of all lower extremity sports injuries. More than 81 % of acute ankle injuries are treated conservatively, with the rate of unsatisfactory results after this treatment ranging from 2 to 36.9 %. Objective: to evaluate the efficacy and safety of the combined use of aceclofenac (Airtal) and tolperisone (Mydocalm Long) in patients with acute ankle ligament injuries. Material and methods. Sixty patients aged 18 to 65 years with acute ankle ligament injury of grade II according to Kannus and Renstrom, with pain intensity in the joint on a visual analogue scale (VAS) ≥ 50 mm, who had no contraindications for the use of these drugs, participated in the study. Patients in the main group (n = 30) received aceclofenac 100 mg in powder form 2 times daily and tolperisone 450 mg in tablets once daily for 14 days. Patients in the comparison group (n = 30) received only aceclofenac 100 mg in powder form 2 times daily for 14 days. The efficacy of therapy was assessed by pain dynamics according to VAS and functional abilities according to the Foot and Ankle Ability Measure (FAAM) questionnaire, which included the Activities of Daily Living (ADL) subscale and the Sports subscale. To assess safety, laboratory tests were performed at visits 1 and 4, and adverse events (AEs) were assessed at visits 2, 3, and 4. Results and discussion. Combined use of aceclofenac and tolperisone in patients with acute ankle ligament injuries resulted in more clinically significant pain reduction and improvement in functional indicators than aceclofenac monotherapy. In the combination therapy group, after completion of treatment on day 15, the severity of pain decreased by 94.8%, the increase in the score on the ADL scale was 62.9 % and on the Sports scale – 70.4 %. In the monotherapy group, pain intensity decreased by 85.1 %, the increase in the score on the ADL scale reached 40.7% and onthe Sports scale – 43.4 %. Throughout the study period, the medications were well tolerated, and no AEs were recorded. Conclusion. The combined use of aceclofenac and tolperisone in patients with acute ankle ligament damage leads to a reduction in pain intensity in a short time, significantly improves indicators of functional activity, promotes a faster return to sports activities, and at the same time has a favourable safety profile.