Environmental pollution is an emerging global issue. Heterogenous photocatalytic degradation, which belongs to the advanced oxidation processes, is a promising sustainable technique for the removal of harmful pollutants (e.g., pharmaceuticals) from natural resources (surface and underground waters), as well as wastewaters. In our study, we examined the efficiency of photocatalytic degradation (with TiO2 and ZnO as photocatalysts) of tolperisone hydrochloride (TLP) and the effect of TLP and its degradation intermediates on germination, photosynthetic capacity, and biomass production of wheat. According to the UFLC-DAD and LC–ESI–MS results, we found that the complete degradation of TLP can be reached after 60.83 min of UV irradiation using TiO2 as a photocatalyst. Furthermore, we determined that germination, biomass production, and chlorophyll b (Chl b) were not related to the percentage of TLP after irradiation. Chlorophyll a (Chl a) (r = -0.61, p ≤ 0.05), Chl a+b (r = -0.56, p ≤ 0.05), and carotenoid (car) (r = -0.57, p ≤ 0.05) were strongly inversely (negatively) correlated with TLP, while Chl a+b/car (r = 0.36, p ≤ 0.05) was moderately (positively) related.