The supplement-drug interaction of quercetin with tamsulosin on vasorelaxation

M.F. Vrolijk, G.R. Haenen, A. Opperhuizen, E.H. Jansen, P.M. Schiffers, A. Bast

Research output: Contribution to journalArticleAcademicpeer-review

3 Citations (Scopus)

Abstract

The food supplement quercetin is used as self-medication for prostate disorders and is known to induce vasorelaxation. The drug tamsulosin is used in the treatment of benign prostatic hyperplasia. A major side effect of tamsulosin is orthostatic hypotension, mediated by vasorelaxation resulting from alpha1-adrenoceptor blockade. The overlapping profile prompted us to investigate the pharmacodynamic interaction of quercetin with tamsulosin. Since quercetin is extensively metabolized in the intestines and the liver, the metabolites quercetin-3-glucuronide and 4'O-methyl-quercetin were also examined. Vasorelaxation induced by the compounds was tested in rat mesenteric arteries (average diameter: 360+/-mum) constricted by the alpha1-adrenoceptor agonist phenylephrine. Tamsulosin (0.1nM) decreased phenylephrine sensitivity 17-fold (n=10). Quercetin (5, 10 and 20microM) also caused a decrease (2-, 4- and 6-fold respectively) of phenylephrine sensitivity, while 10microM of quercetin-3-glucuronide and 4'O-methyl-quercetin decreased this sensitivity (1.5- and 2-fold) only slightly (n=6). The combination of tamsulosin with quercetin or quercetin metabolites proved to be far more potent than the compounds in isolation. The combination of quercetin, quercetin-3-glucuronide or 4'O-methyl-quercetin with tamsulosin decreased the phenylephrine sensitivity approximately 200-, 35- and 150-fold (n=6). The strong pharmacodynamic interaction between the food supplement quercetin and tamsulosin underlines the potential of the impact of supplement-drug interactions that warrant more research.
Original languageEnglish
Pages (from-to)132-137
Number of pages6
JournalEuropean Journal of Pharmacology
Volume746
DOIs
Publication statusPublished - 5 Jan 2015

Keywords

  • Quercetin
  • Tamsulosin
  • Vasorelaxation
  • Orthostatic hypotension
  • Supplement-drug interaction
  • Pharmacodynamics
  • URINARY-TRACT SYMPTOMS
  • FLAVONOID QUERCETIN
  • ALPHA(1)-ADRENERGIC RECEPTORS
  • ELDERLY-PEOPLE
  • IN-VITRO
  • NUTRITIONAL-STATUS
  • HYDROGEN-PEROXIDE
  • BLOOD-PRESSURE
  • ARTERIES
  • RATS

Cite this

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title = "The supplement-drug interaction of quercetin with tamsulosin on vasorelaxation",
abstract = "The food supplement quercetin is used as self-medication for prostate disorders and is known to induce vasorelaxation. The drug tamsulosin is used in the treatment of benign prostatic hyperplasia. A major side effect of tamsulosin is orthostatic hypotension, mediated by vasorelaxation resulting from alpha1-adrenoceptor blockade. The overlapping profile prompted us to investigate the pharmacodynamic interaction of quercetin with tamsulosin. Since quercetin is extensively metabolized in the intestines and the liver, the metabolites quercetin-3-glucuronide and 4'O-methyl-quercetin were also examined. Vasorelaxation induced by the compounds was tested in rat mesenteric arteries (average diameter: 360+/-mum) constricted by the alpha1-adrenoceptor agonist phenylephrine. Tamsulosin (0.1nM) decreased phenylephrine sensitivity 17-fold (n=10). Quercetin (5, 10 and 20microM) also caused a decrease (2-, 4- and 6-fold respectively) of phenylephrine sensitivity, while 10microM of quercetin-3-glucuronide and 4'O-methyl-quercetin decreased this sensitivity (1.5- and 2-fold) only slightly (n=6). The combination of tamsulosin with quercetin or quercetin metabolites proved to be far more potent than the compounds in isolation. The combination of quercetin, quercetin-3-glucuronide or 4'O-methyl-quercetin with tamsulosin decreased the phenylephrine sensitivity approximately 200-, 35- and 150-fold (n=6). The strong pharmacodynamic interaction between the food supplement quercetin and tamsulosin underlines the potential of the impact of supplement-drug interactions that warrant more research.",
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author = "M.F. Vrolijk and G.R. Haenen and A. Opperhuizen and E.H. Jansen and P.M. Schiffers and A. Bast",
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language = "English",
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The supplement-drug interaction of quercetin with tamsulosin on vasorelaxation. / Vrolijk, M.F.; Haenen, G.R.; Opperhuizen, A.; Jansen, E.H.; Schiffers, P.M.; Bast, A.

In: European Journal of Pharmacology, Vol. 746, 05.01.2015, p. 132-137.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - The supplement-drug interaction of quercetin with tamsulosin on vasorelaxation

AU - Vrolijk, M.F.

AU - Haenen, G.R.

AU - Opperhuizen, A.

AU - Jansen, E.H.

AU - Schiffers, P.M.

AU - Bast, A.

PY - 2015/1/5

Y1 - 2015/1/5

N2 - The food supplement quercetin is used as self-medication for prostate disorders and is known to induce vasorelaxation. The drug tamsulosin is used in the treatment of benign prostatic hyperplasia. A major side effect of tamsulosin is orthostatic hypotension, mediated by vasorelaxation resulting from alpha1-adrenoceptor blockade. The overlapping profile prompted us to investigate the pharmacodynamic interaction of quercetin with tamsulosin. Since quercetin is extensively metabolized in the intestines and the liver, the metabolites quercetin-3-glucuronide and 4'O-methyl-quercetin were also examined. Vasorelaxation induced by the compounds was tested in rat mesenteric arteries (average diameter: 360+/-mum) constricted by the alpha1-adrenoceptor agonist phenylephrine. Tamsulosin (0.1nM) decreased phenylephrine sensitivity 17-fold (n=10). Quercetin (5, 10 and 20microM) also caused a decrease (2-, 4- and 6-fold respectively) of phenylephrine sensitivity, while 10microM of quercetin-3-glucuronide and 4'O-methyl-quercetin decreased this sensitivity (1.5- and 2-fold) only slightly (n=6). The combination of tamsulosin with quercetin or quercetin metabolites proved to be far more potent than the compounds in isolation. The combination of quercetin, quercetin-3-glucuronide or 4'O-methyl-quercetin with tamsulosin decreased the phenylephrine sensitivity approximately 200-, 35- and 150-fold (n=6). The strong pharmacodynamic interaction between the food supplement quercetin and tamsulosin underlines the potential of the impact of supplement-drug interactions that warrant more research.

AB - The food supplement quercetin is used as self-medication for prostate disorders and is known to induce vasorelaxation. The drug tamsulosin is used in the treatment of benign prostatic hyperplasia. A major side effect of tamsulosin is orthostatic hypotension, mediated by vasorelaxation resulting from alpha1-adrenoceptor blockade. The overlapping profile prompted us to investigate the pharmacodynamic interaction of quercetin with tamsulosin. Since quercetin is extensively metabolized in the intestines and the liver, the metabolites quercetin-3-glucuronide and 4'O-methyl-quercetin were also examined. Vasorelaxation induced by the compounds was tested in rat mesenteric arteries (average diameter: 360+/-mum) constricted by the alpha1-adrenoceptor agonist phenylephrine. Tamsulosin (0.1nM) decreased phenylephrine sensitivity 17-fold (n=10). Quercetin (5, 10 and 20microM) also caused a decrease (2-, 4- and 6-fold respectively) of phenylephrine sensitivity, while 10microM of quercetin-3-glucuronide and 4'O-methyl-quercetin decreased this sensitivity (1.5- and 2-fold) only slightly (n=6). The combination of tamsulosin with quercetin or quercetin metabolites proved to be far more potent than the compounds in isolation. The combination of quercetin, quercetin-3-glucuronide or 4'O-methyl-quercetin with tamsulosin decreased the phenylephrine sensitivity approximately 200-, 35- and 150-fold (n=6). The strong pharmacodynamic interaction between the food supplement quercetin and tamsulosin underlines the potential of the impact of supplement-drug interactions that warrant more research.

KW - Quercetin

KW - Tamsulosin

KW - Vasorelaxation

KW - Orthostatic hypotension

KW - Supplement-drug interaction

KW - Pharmacodynamics

KW - URINARY-TRACT SYMPTOMS

KW - FLAVONOID QUERCETIN

KW - ALPHA(1)-ADRENERGIC RECEPTORS

KW - ELDERLY-PEOPLE

KW - IN-VITRO

KW - NUTRITIONAL-STATUS

KW - HYDROGEN-PEROXIDE

KW - BLOOD-PRESSURE

KW - ARTERIES

KW - RATS

U2 - 10.1016/j.ejphar.2014.11.006

DO - 10.1016/j.ejphar.2014.11.006

M3 - Article

VL - 746

SP - 132

EP - 137

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

ER -