The present invention relates to prodrugs of (S)- or (R)-ketamine, including isotopically labeled ketamine, compositions and uses thereof. Compounds having formula (Ia) or (Ib) as the prodrugs of (S)- or (R)-ketamine, including isotopically labeled ketamine, and pharmaceutical compositions comprising the compounds provided herein are used for treating or preventing a CNS disease. More particularly, the related diseases include depression and pain.本發明關於(S)-或(R)-K他命(包括同位素標記的K他命)的前藥及其組成物及用途。作為(S)-或(R)-K他命(包括同位素標記的K他命)的前藥之具有式(Ia)或(Ib)之化合物及包含本文中提供的化合物之醫藥組成物係有用於治療或預防CNS疾病。更具體地,相關疾病包括抑鬱和疼痛。