Benign prostatic hyperplasia (BPH) is a common disease among older men. Finasteride and tamsulosin hydrochloride drugs are used in BPH treatment. This study aimed to evaluate the side effects of both finasteride and/or tamsulosin hydrochloride administration on sex hormones, prostate markers and neurotransmitters in male rats. The study was carried out on a total of sixty male rats were divided equally into four groups. Group I was the control group. Groups II and III were rats administered with finasteride and tamsulosin hydrochloride, respectively. Group IV included rats administered with both finasteride and tamsulosin hydrochloride. Results showed that serum testosterone, DHT levels and sperm count were lower than normal in all rats administered with finasteride or/and tamsulosin hydrochloride. Serum PSA level and acid phosphatatse activity showed insignificant decrease in group II and increase in group III. Prolactin levels showed insignificant increase in all groups. Neurotransmitters as dopamine and acetylcholine esterase activity showed significant decrease in all treated rats. In conclusion, tamsulosin hydrochloride has higher harmful side effects than finasteride in rats, represented in disturbances in prostatic biomarkers and testis functions and neurotransmitters. Combination therapy of both finasteride and tamsulosin hydrochloride can be considered safer than only tamsulosin hydrochloride administration.