Abstract

Epimedium sagittatum (Sieb. et Zucc.) Maxim is one of the herbs used to treat erectile dysfunction in Traditional Chinese Medicine. Sildenafil is a phosphodiesterase 5 inhibitor used to treat erectile dysfunction in Western Medicine. This study evaluates the herbal-drug interaction of Epimedium sagittatum extract on the pharmacokinetics of sildenafil in rats by ultra-performance liquid chromatography. The rat plasma was sampled from each anesthetized rat after pretreatment with 3-days Epimedium sagittatum extract (1/2 g/kg/day) and intravenous injection with sildenafil (10/30 mg/kg). The pharmacokinetic data demonstrate that the area under the concentration-time curve (AUC) of sildenafil (10 mg/kg) was significantly decreased in groups that received a high dose of Epimedium sagittatum extract. In conclusion, the study demonstrates that there was significant herb-drug interaction of Epimedium sagittatum extract on the pharmacokinetics of sildenafil at low and high daily doses, suggesting co-administration use of Epimedium sagittatum extract and sildenafil in clinical practice should be prevented due to possible herb-drug interactions.

Highlights

  • Erectile dysfunction is an age-related problem with a prevalence rate of 17.7% in men older than40, and it increases with age and number of comorbidities [1]

  • Since 1998, sildenafil, one of the phosphodiesterase-5 inhibitors, which acts by regulating the blood flow of penis via inhibition of cGMP specific phosphodiesterase 5 in the corpus cavernosum, was considered the treatment of choice for erectile dysfunction, with a response rate ranging from 68–69% [7]

  • D. (n = 6). * The relative standard deviation (RSD) was estimated from the observed concentrations as follows: RSD (%) = (standard deviation (SD)/Cobs) × 100. ** The accuracy was calculated by the nominal concentration (Cnom) and the mean value of the observed concentrations (Cobs) : accuracy (%) = (Cobs/Cnom) × 100

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Summary

Introduction

Erectile dysfunction is an age-related problem with a prevalence rate of 17.7% in men older than40, and it increases with age and number of comorbidities [1]. The inability to maintain erectile function results in anxiety, loss of self-esteem and relationship strains [2,3] It is not surprising erectile dysfunction affects interpersonal relationships between partners, resulting in diminished psychosocial functioning in men with erectile dysfunction. Since 1998, sildenafil, one of the phosphodiesterase-5 inhibitors, which acts by regulating the blood flow of penis via inhibition of cGMP specific phosphodiesterase 5 in the corpus cavernosum, was considered the treatment of choice for erectile dysfunction, with a response rate ranging from 68–69% [7]. There are some possible side effects mentioned in the literature, such as hot flushes, blue tinged vision, headache, and dizziness. It remains the treatment of choice for men with mild to moderate erectile dysfunction [11]

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