Objective: To evaluate the efficacy and safety of OxyContin (R) tablets (controlled-release oxycodone hydrochloride: 5, 10, 20, and 40 mg) in relieving moderate to severe postherpetic neuralgia (PHN) pain. Method: A multicenter, open-label, prospective, self-controlled clinical observation. Results: Pain was relieved in 17.3% of patients within 30 min and in 94.1% patients within 1 h after drug administration. OxyContin (R) tablets showed good clinical efficacy in relieving both moderate and severe PHN pain. Response rate reached 98.4% at the end of the 8th week of treatment. After the 1st week of treatment, stable pain relief was achieved, and pain scores on a Visual Analogue Scale decreased dramatically in most patients. During treatment with controlled-release OxyContin (R) tablets, the use of concomitant medications was significantly decreased. Some patients developed adverse drug reactions (ADRs) in the 1st week, which decreased significantly during the following weeks of treatment. Nausea (18.1%) was the most commonly reported ADR, followed by constipation (10.1%) and dizziness (10.1%). A number of ADRs disappeared during treatment. Conclusion: Controlled-release OxyContin (R) tablets demonstrated fast onset of PHN pain control, superior efficacy in relieving both moderate and severe PHN pain, and a good safety profile. Copyright (c) 2008 S. Karger AG, Basel.