Modification of propranolol's bioavailability by Eurycoma longifolia water-based extract

J Clin Pharm Ther. 2010 Dec;35(6):691-6. doi: 10.1111/j.1365-2710.2009.01147.x.

Abstract

What is known and background: Eurycoma longifolia (E. longifolia), a herb commonly consumed for its aphrodisiac properties, is widely used by Asian males. This may include hypertensive patients receiving propranolol which may cause sexual dysfunction as one of its side-effects. There is no published study of the potential pharmacokinetic interaction between propranolol and the herb.

Objective: To study propranolol's pharmacokinetics when E. longifolia is consumed, comparing volunteers given either propranolol or a placebo.

Methods: This is a placebo-controlled randomized single-blinded crossover study of the effect of a water-based extract of E. longifolia on the pharmacokinetics of a single dose of proporanolol (Inderal(®)) in 14 healthy non-smoker young males. Eighty milligram of propranonol was orally administered with (i) placebo (Lactose) or (ii) 200 mg of water-based extract of E. longifolia (0·0272 ± 0·0026%eurycomanone) following an overnight fasting. Blood samples were collected at 0, 0·5, 1, 1·5, 2, 3, 4, 6, 8 and 10 h for propranolol's plasma concentration determinations using a validated high-performance liquid chromatography (HPLC) method.

Results and discussion: When propranolol was administered with E. longifolia, its bioavailability (AUC0-∞) decreased by 29% while C(max) was reduced by 42% and T(max) was significantly prolonged by almost 86%. The terminal elimination half-life, however, was not significantly affected.

Conclusion: The bioavailability of propranolol is significantly decreased when consumed together with E. longifolia. The interaction is due to a reduction in absorption, rather than an increase in propranolol's metabolism. Although the pharmacodynamics of propranolol was not affected in healthy volunteers, caution is still advisable with co-administration of the drug and the herb.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aphrodisiacs / pharmacology*
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Eurycoma*
  • Half-Life
  • Herb-Drug Interactions*
  • Humans
  • Male
  • Phytotherapy
  • Plant Extracts / pharmacology*
  • Plant Roots / chemistry
  • Propranolol / blood
  • Propranolol / pharmacokinetics*
  • Propranolol / pharmacology
  • Quassins / pharmacology*
  • Sexual Dysfunction, Physiological / drug therapy
  • Single-Blind Method
  • Water
  • Young Adult

Substances

  • Aphrodisiacs
  • Plant Extracts
  • Quassins
  • eurycomanone
  • Water
  • Propranolol