Pharmacokinetics and Cardiovascular Effects of Ma‐Huang (Ephedra sinica) in Normotensive Adults

Abstract

The purpose of this study was to evaluate heart rate and blood pressure responses to a commercially available source of ma‐haung, a natural source of the sympathomimetic substance, ephedrine, and to evaluate the pharmacokinetic properties of the product in normotensive, healthy adults. On day 1, twelve study participants were monitored with an ambulatory blood pressure device between hours 7 and 20. On day 2, they ingested four capsules of powdered ma‐huang at hours 8 and 17 while again wearing the monitor between hours 7 and 20. Serial plasma samples were obtained and concentrations of ephedrine were analyzed by high‐performance liquid chromatography. Pharmacokinetic parameters of ephedrine were determined from plasma concentration‐time profiles. The ephedrine alkaloid content of each capsule was also determined by high‐performance liquid chromatography. Six participants experienced a statistically significant increase in heart rate, but the effects on blood pressure were variable. The half‐life, volume of distribution, clearance, and maximum concentration in plasma of ephedrine in the ma‐huang product were similar to values previously reported for a 20‐mg, immediate‐release ephedrine tablet. Values for the absorption rate were considerably lower and time to reach maximum concentration was longer for the capsules, compared with the standard tablet. Variability in alkaloid content of ephedrine was low and yielded a mean dose of ephedrine at 19.4 mg; pseudoephedrine at 4.9 mg; and methylephedrine at 1.2 mg for a four‐capsule dose. In summary, ma‐haung had variable effects on blood pressure and increased heart rate in healthy, normotensive adults. Pharmacokinetic parameters for ephedrine were in agreement with those previously reported; however, the absorption rate was much slower after ingestion of ma‐huang.