Adzu Bulus, Masimirembwa Collen, Mustapha Kudirat Bola, Thelingwani Roslyn, Kirim Rukaiyatu Abdullahi, Gamaniel Karniyus Shingu
Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development (NIPRD), PMB 21, Abuja, Nigeria,
Eur J Drug Metab Pharmacokinet. 2015 Mar;40(1):115-8. doi: 10.1007/s13318-014-0173-1. Epub 2014 Jan 24.
NIPRISAN(®) is a phytomedicine developed from herbal products used in folkloric practice for the management of sickle cell disease (SCD). The effect of NIPRISAN(®) was tested on human cytochrome P4503A4 drug metabolising enzyme to generate clinically significant data for its safe and efficacious use. Inhibitory activity on CYP3A4 was measured with and without the addition of NIPRISAN(®), by testing different concentrations of the product at 37 °C in reactive mixtures with ketoconazole (2.5 μM) as the positive control. Results showed a low IC(50) value of 0.06 mg/ml, indicating that metabolic processes of NIPRISAN(®) are likely to inhibit CYP3A4. The result suggests possible herb-drug interaction may occur, with potential implication on common medications that are CYP3A4 substrates. It is, therefore, advocated that concomitant administration of NIPRISAN(®) along with medications that are CYP3A4 substrates should be done with caution so as not to compromise NIPRISAN(®')s established beneficial effect in the management of SCD.
尼普瑞散(NIPRISAN®)是一种植物药,由民间疗法中用于治疗镰状细胞病(SCD)的草药产品研发而来。对尼普瑞散(NIPRISAN®)的效果进行了人体细胞色素P4503A4药物代谢酶测试,以生成关于其安全有效使用的具有临床意义的数据。通过在37℃下,以酮康唑(2.5μM)作为阳性对照,在反应混合物中测试该产品的不同浓度,来测量添加和不添加尼普瑞散(NIPRISAN®)时对CYP3A4的抑制活性。结果显示IC50值低至0.06mg/ml,表明尼普瑞散(NIPRISAN®)的代谢过程可能会抑制CYP3A4。该结果表明可能会发生草药与药物的相互作用,对作为CYP3A4底物的常用药物具有潜在影响。因此,提倡在同时使用尼普瑞散(NIPRISAN®)和作为CYP3A4底物的药物时应谨慎行事,以免损害尼普瑞散(NIPRISAN®)在治疗SCD方面已确立的有益效果。