Abstract
Shenxiong glucose injection (SGI), a traditional Chinese medicine (TCM) preparation, has been widely used for the treatment of various cardiovascular and cerebrovascular diseases for many years. We assessed the potential influences of SGI on the activities of six CYP enzymes (CYP1A2, CYP2C11, CYP2C19, CYP2D4, CYP2E1, and CYP3A2) and on the pharmacokinetics of warfarin in rats. We compared plasma pharmacokinetics of six probe drugs (caffeine/CYP1A2, tolbutamide/CYP2C11, omeprazole/CYP2C19, metoprolol/CYP2D4, chlorzoxazone/CYP2E1, and midazolam/CYP3A2) and of warfarin between control and SGI-pretreated groups, to estimate the effect on the relative activities of the six isozymes and warfarin metabolism. There were no significant differences in the pharmacokinetic parameters of caffeine, omeprazole, metoprolol, chlorzoxazone, and midazolam between the SGI-pretreated and control groups. However, many pharmacokinetic parameters of tolbutamide in SGI-pretreated rats were affected significantly (p < 0.05), and indicated tolbutamide metabolism in the former group was markedly slower. Moreover, SGI reduced the clearance of warfarin. These results suggested SGI showed no effects on the enzyme activities of rat CYP1A2, CYP2C19, CYP2D4, CYP2E1, and CYP3A2, but inhibited the enzyme activity of CYP2C11, and improved the blood concentration of warfarin. This suggests that the dose of warfarin may need be adjusted when co-administrated with SGI.
Highlights
Shenxiong glucose injection (SGI) is a preparation containing the water extracts of Salvia miltiorrhizaBunge and ligustrazine hydrochloride
This indicates that SGI had no influence on CYP1A2 activity in vivo
Pretreatment with SGI caused significant increases in area under the curve (AUC)(0–t), AUC(0–∞), MRT(0–t), MRT(0–∞), and CL of tolbutamide, compared with those observed in the blank control group (BCG)
Summary
Shenxiong glucose injection (SGI) is a preparation containing the water extracts of Salvia miltiorrhiza. Bunge, called red sage or Danshen in Chinese, is one of the most versatile Chinese herbal drugs, and has been used for hundreds of years. It has been suggested that some Salvia miltiorrhiza Bunge products may be associated with a number of clinically important herb–drug interactions that can cause adverse outcomes, as well as in interactions with other herbs [11,12,13]. Ligustrazine (2,3,5,6-tetramethylpyrazine) is the main active ingredient of Szechwan lovage rhizome, and has been extensively used to treat cardiovascular and cerebrovascular diseases [17]. To date, no systematic study has reported on the impact of SGI on cytochromes P450 enzyme activities
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