Goldenseal

Goldenseal/Drug Interactions:

  • AlkaloidsAlkaloids: The active ingredients of goldenseal include isoquinoline alkaloids, such as berberine, canadine, and hydrastine. According to secondary sources, goldenseal may interact with alkaloid agents.
  • AntiarrhythmicsAntiarrhythmics: In animal research, berberine restored ventricular arrhythmias and atrial fibrillation to normal sinus rhythm (7). However, in human research, patients with congestive heart failure developed ventricular tachycardia following intravenous berberine administration (53).
  • AntibioticsAntibiotics: In vitro and in animal research, berberine was found to have antimicrobial properties (41; 84; 85; 86; 87; 88; 21).
  • Anticoagulants and antiplateletsAnticoagulants and antiplatelets: In vitro and in animal research, goldenseal and berberine inhibited platelet aggregation, which may increase the risk of bleeding when used with anticoagulant and antiplatelet agents (54; 55). Goldenseal may reduce the anticoagulant effects of warfarin due to antagonist properties, and theoretically may increase the risk of blood clots. However, the effects are unclear.
  • AntidiabeticsAntidiabetics: According to animal and in vitro research, berberine may improve insulin resistance (22), lower blood sugar concentrations (23), and decrease glucose absorption (25).
  • AntidiarrhealsAntidiarrheals: According to human and animal research, berberine may have antidiarrheal effects (56; 57; 58; 59).
  • AntifungalsAntifungals: In vitro, berberine exhibited antifungal activity at concentrations of 10mg/mL against Alternaria, Candida albicans, Curvularia, Drechslera, Fusarium, Mucor, and Rhizopus oryzae and inhibited growth of Aspergillus flavus and A. fumigates at concentrations of 25mg/mL (14). Berberine sulfate possessed antifungal activity in vitro through inhibition of RNA and protein synthesis (86).
  • AntihelminthicsAntihelminthics: According to secondary sources, goldenseal may interact with antihelminthic agents.
  • AntihistaminesAntihistamines: In animal research, subcutaneous administration of berberine sulfate in doses of 20-50mg/kg decreased vascular permeability induced by histamine (89).
  • AntihypertensivesAntihypertensives: In human research, no significant circulatory changes occurred with the lower dose of berberine (a 0.02mg/kg/min intravenous infusion of berberine), but the higher dose (a 0.2mg/kg/min intravenous infusion of berberine) decreased systemic and pulmonary vascular resistance, right atrial pressures, and left ventricular end-systolic pressures (53). In animal research, intravenous berberine significantly decreased systolic and diastolic blood pressure at doses of 2-8mg/kg (81).
  • Anti-inflammatory agentsAnti-inflammatory agents: According to animal research, berberine may have anti-inflammatory properties (90; 89; 15).
  • AntilipemicsAntilipemics: In human research, berberine reduced triglycerides, serum cholesterol, and LDL cholesterol (72; 91). However, HDL cholesterol was not affected.
  • AntimalarialsAntimalarials: In clinical study evaluating treatments for chloroquine-resistant malaria, a clearance of asexual parasitemia was seen after four days of treatment with berberine (an alkaloid constituent of goldenseal) in combination with pyrimethamine, which was greater than that seen with pyrimethamine plus tetracycline or pyrimethamine plus cotrimoxazole (61).
  • Antineoplastic agentsAntineoplastic agents: According to animal research, berberine may have antineoplastic effects (92; 93).
  • Antiparasitic agentsAntiparasitic agents: In vitro, a methanol extract of berberine demonstrated parasiticidal activity (87; 88).
  • Beta-blockersBeta-blockers: In animal research, timolol partially inhibited the smooth muscle relaxant activity of a goldenseal alcoholic extract (94). In vitro, propranolol inhibited the increase in slow-response action potentials seen with berberine, an alkaloid constituent in goldenseal (95).
  • Cardiovascular agentsCardiovascular agents: In animal research, berberine elicited transient hypotension and bradycardia, although it is unclear if these effects may occur in humans (81). In contrast, hydrastine may theoretically induce vasoconstriction (52), possibly resulting in hypertension. In human research, intravenous berberine caused ventricular tachycardia (torsades de pointes) (53).
  • CarmustineCarmustine: Berberine and carmustine have been shown to have additive effects against human brain tumor cell lines in vitro (96).
  • Chronotropic agentsChronotropic agents: According to animal research, berberine may have inotropic and chronotropic activity (97).
  • CocaineCocaine: A methodologically weak human trial assessing the effectiveness of goldenseal in masking marijuana and cocaine use suggests that it may be dilution of urine that causes false negative results on urinalysis and not goldenseal itself, although the conclusions of this study are not definitive (70)
  • CyclosporineCyclosporine: According to human research, berberine may increase serum levels of cyclosporine by reducing the metabolism of cyclosporine through cytochrome P450 3A4 inhibition (98).
  • Cytochrome P450 2D6 substratesCytochrome P450 2D6 substrates: In human research, goldenseal demonstrated CYP 2D6 inhibition (62; 99; 4), and, based on its CYP inhibition activity, goldenseal extract was used as a control in vitro when testing for CYP inhibition in other plants (100). According to reviews, goldenseal in usual amounts lacked a potent inhibition or induction effect on p-glycoprotein or cytochrome P450 enzymes, though a weak inhibition effect was reported for CYP3A4 and CYP2D6 (101), and goldenseal was reported to have mild-to-moderate inhibition effects on CYP3A and CYP2D6 (102; 103).
  • Cytochrome P450 3A(4,5,7) substratesCytochrome P450 3A(4,5,7) substrates: In vitro, goldenseal extract inhibited CYP 3A4 (104; 105; 106; 107), and based on its CYP inhibition activity, goldenseal extract was used as a control when testing for CYP inhibition in other plants (100). Limited available research did not show a significant interaction between goldenseal root and the pharmacokinetics of the antiretroviral drug indinavir, which is metabolized by CYP 3A4 (108). According to reviews, goldenseal in usual amounts lacked a potent inhibition or induction effect on p-glycoprotein or cytochrome P450 enzymes, though a weak inhibition effect was reported for CYP3A4 and CYP2D6 (101), and goldenseal was reported to have mild-to-moderate inhibition effects on CYP3A and CYP2D6 (102; 103).
  • DigoxinDigoxin: In human research, goldenseal increased the Cmax of digoxin by 14% (109).
  • Gastrointestinal agentsGastrointestinal agents: According to human research, berberine may have antidiarrheal effects (56; 57; 58; 59), and nausea and vomiting have been reported with the use of goldenseal (60; 61).
  • Heart rate-regulating agentsHeart rate-regulating agents: According to animal research, berberine may have inotropic and chronotropic activity (97).
  • HepatotoxinsHepatotoxins: An increase in hepatocellular adenoma or carcinoma was reported in male and female F344/N rats when goldenseal root powder was added to their feed for two years (78). Cases of jaundice have been associated with the use of a traditional Chinese patent formula that included Chinese goldthread (Coptis chinensis Franch.), an alkaloid-containing herb that has been reported as an adulterant in goldenseal products (1).
  • ImmunostimulantsImmunostimulants: In human research, leukocyte counts increased to >4,000 in patients with leukopenia following with administration of 50mg of berberine three times daily for 1-4 weeks (30).
  • ImmunosuppressantsImmunosuppressants: In human research, leukocyte counts increased to >4,000 in patients with leukopenia with administration of 50mg of berberine three times daily for 1-4 weeks (30).
  • LaxativesLaxatives: According to human research, berberine may have antidiarrheal effects (56; 57; 58; 59). Theoretically, berberine may counteract the effects of laxatives.
  • Neostigmine (Prostigmin?)Neostigmine (Prostigmin?): In animal research, berberine reversed the secretory effects of neostigmine (110).
  • Neurologic agentsNeurologic agents: In human research, berberine caused headache (33). According to secondary sources, paresthesias have been reported in association with large doses of goldenseal.
  • Oseltamivir:Oseltamivir: According to in vitro hepatic microsome research, the concentration of active metabolite of the prodrug oseltamivir was reduced with goldenseal extract (111).
  • PhenylephrinePhenylephrine: In animal research, berberine and L-phenylephrine demonstrated additive effects when administered concurrently (110).
  • PhotosensitizersPhotosensitizers: In human research, photosensitivity was reported following administration of a combination herbal preparation containing goldenseal, ginseng, and bee pollen (63). The contribution of goldenseal or any of its constituents to this reaction is unclear.
  • SedativesSedatives: According to animal research, berberine may have sedative effects (51; 112; 113).
  • TetracyclinesTetracyclines: In clinical research, berberine decreased the efficacy of tetracycline in the treatment of cholera (57).
  • VasopressorsVasopressors: Hydrastine may theoretically induce vasoconstriction, possibly resulting in hypertension. In animal research, dose-dependent vasoconstriction was observed beginning at a concentration of 50mcL/mL of goldenseal, although neither berberine, an alkaloid constituent in goldenseal, nor hydrastine alone, demonstrated this effect (52).
  • WarfarinWarfarin: Goldenseal may reduce the anticoagulant effects of warfarin due to antagonist properties, and theoretically may increase the risk of blood clots.
  • Wound-healing agents:Wound-healing agents: In human research, an ointment consisting of beta-sitosterol, sesame oil, and berberine in addition to other plant components (MEBO?) was reported to improve pain relief for burn wounds (114).
  • Goldenseal/Herb/Supplement Interactions:

  • AlkaloidsAlkaloids: The active ingredients of goldenseal include isoquinoline alkaloids, such as berberine, canadine, and hydrastine. According to secondary sources, goldenseal may interact with alkaloid herbs and supplements.
  • AntiarrhythmicsAntiarrhythmics: In animal research, berberine restored ventricular arrhythmias and atrial fibrillation to normal sinus rhythm (7). However, in human research, patients with congestive heart failure developed ventricular tachycardia following intravenous berberine administration (53).
  • AntibacterialsAntibacterials: In vitro and in animal research, berberine was found to have antimicrobial properties (41; 84; 85; 86; 87; 88; 21).
  • Anticoagulants and antiplatelets Anticoagulants and antiplatelets : In vitro and in animal research, goldenseal and berberine inhibited platelet aggregation, which may increase the risk of bleeding when used with anticoagulant and antiplatelet agents (54; 55). Goldenseal may reduce the anticoagulant effects of warfarin due to antagonist properties, and theoretically may increase the risk of blood clots. However, the effects are unclear.
  • AntidiarrhealsAntidiarrheals: According to clinical research in humans and animals, berberine, an alkaloid constituent in goldenseal, may have antidiarrheal effects (56; 57; 58; 59).
  • AntifungalsAntifungals: In vitro, berberine exhibited antifungal activity at concentrations of 10mg/mL against Alternaria, Candida albicans, Curvularia, Drechslera, Fusarium, Mucor, and Rhizopus oryzae and inhibited growth of Aspergillus flavus and A. fumigates at concentrations of 25mg/mL (14). Berberine sulfate possessed antifungal activity in vitro through inhibition of RNA and protein synthesis (86).
  • AntihelminthicsAntihelminthics: According to secondary sources, goldenseal may interact with antihelminthic agents.
  • AntihistaminesAntihistamines: In animal research, subcutaneous administration of berberine sulfate in doses of 20-50mg/kg decreased vascular permeability induced by histamine (89).
  • Anti-inflammatory herbsAnti-inflammatory herbs: According to animal research, berberine may have anti-inflammatory properties (90; 89; 15).
  • AntilipemicsAntilipemics: In human research, berberine reduced triglycerides, serum cholesterol, and LDL cholesterol (72; 91). However, HDL cholesterol was not affected.
  • AntimalarialsAntimalarials: In clinical research evaluating treatments for chloroquine-resistant malaria, a clearance of asexual parasitemia was seen after four days of treatment with berberine (an alkaloid constituent of goldenseal) in combination with pyrimethamine, which was greater than that seen with pyrimethamine plus tetracycline or pyrimethamine plus cotrimoxazole (61).
  • AntineoplasticsAntineoplastics: According to animal research, berberine may have antineoplastic effects (92; 93).
  • Berberinecontaining agentsBerberine-containing agents: The active ingredients of goldenseal include the isoquinoline alkaloid berberine. Theoretically, goldenseal may interact with berberine-containing herbs and supplements.
  • Cardiovascular agentsCardiovascular agents: In animal research, berberine elicited transient hypotension and bradycardia, although it is unclear if these effects may occur in humans (81). In contrast, hydrastine may theoretically induce vasoconstriction (52), possibly resulting in hypertension. In human research, intravenous berberine caused ventricular tachycardia (torsades de pointes) (53).
  • ChronotropicsChronotropics: According to animal research, berberine may have inotropic and chronotropic activity (97).
  • Cytochrome P450 2D6 substratesCytochrome P450 2D6 substrates: In human research, goldenseal demonstrated CYP 2D6 inhibition (62; 99; 4), and, based on its CYP inhibition activity, goldenseal extract was used as a control in vitro when testing for CYP inhibition in other plants (100). According to reviews, goldenseal in usual amounts lacked a potent inhibition or induction effect on p-glycoprotein or cytochrome P450 enzymes, though a weak inhibition effect was reported for CYP3A4 and CYP2D6 (101) and goldenseal was reported to have mild-to-moderate inhibition effects on CYP3A and CYP2D6 (102; 103).
  • Cytochrome P450 3A(4,5,7) substratesCytochrome P450 3A(4,5,7) substrates: In vitro, goldenseal extract inhibited CYP 3A4 (104; 105; 106; 107), and, based on its CYP inhibition activity, goldenseal extract was used as a control when testing for CYP inhibition in other plants (100). Limited available research did not show a significant interaction between goldenseal root and the pharmacokinetics of the antiretroviral drug indinavir, which is metabolized by CYP 3A4 (108). According to reviews, goldenseal in usual amounts lacked a potent inhibition or induction effect on p-glycoprotein or cytochrome P450 enzymes, though a weak inhibition effect was reported for CYP3A4 and CYP2D6 (101), and goldenseal was reported to have mild-to-moderate inhibition effects on CYP3A and CYP2D6 (102; 103).
  • FoxgloveFoxglove: In human research, goldenseal increased the Cmax of digoxin by 14% (109).
  • Gastrointestinal herbs and supplementsGastrointestinal herbs and supplements: According to human research, berberine may have antidiarrheal effects (56; 57; 58; 59), and nausea and vomiting have been reported with the use of goldenseal (60; 61).
  • Heart rate-regulating agentsHeart rate-regulating agents: According to animal research, berberine may have inotropic and chronotropic activity (97).
  • HepatotoxinsHepatotoxins: An increase in hepatocellular adenoma or carcinoma was reported in male and female F344/N rats when goldenseal root powder was added to their feed for two years (78). Cases of jaundice have been associated with the use of a traditional Chinese patent formula that included Chinese goldthread (Coptis chinensis Franch.), an alkaloid-containing herb that has been reported as an adulterant in goldenseal products (1).
  • HypoglycemicsHypoglycemics: According to in vitro and animal research, berberine may improve insulin resistance (22), lower blood sugar concentrations (23), and decrease glucose absorption (25).
  • HypotensivesHypotensives: In clinical research on patients with refractory congestive heart failure, no significant circulatory changes occurred with the lower dose of berberine (a 0.02mg/kg/min intravenous infusion of berberine), but at the higher dose (a 0.2mg/kg/min intravenous infusion of berberine), a 48% decrease in systemic vascular resistance, a 41% decrease in pulmonary vascular resistance, a 28% decrease in right atrial pressures, and a 32% decrease in left ventricular end-systolic pressures were reported (53). In animal research, intravenous berberine caused a significant decrease in systolic and diastolic blood pressure at doses of 2-8mg/kg (81).
  • ImmunomodulatorsImmunomodulators: In human research, leukocyte counts increased to >4,000 in patients with leukopenia with administration of 50mg of berberine three times daily for 1-4 weeks (30).
  • LaxativesLaxatives: According to human research, berberine may have antidiarrheal effects (56; 57; 58; 59). Theoretically, berberine may counteract the effects of laxatives.
  • MarijuanaMarijuana: A methodologically weak human trial assessing the effectiveness of goldenseal in masking marijuana and cocaine use suggests that it may be dilution of urine that causes false negative results on urinalysis and not goldenseal itself, although the conclusions of this study are not definitive (70)
  • Neurologic agentsNeurologic agents: In human research, berberine caused headache (33). According to secondary sources, paresthesias have been reported in association with large doses of goldenseal.
  • PhotosensitizersPhotosensitizers: In human research, photosensitivity was reported following administration of a combination herbal preparation containing goldenseal, ginseng, and bee pollen (63). The contribution of goldenseal or any of its constituents to this reaction is unclear.
  • SedativesSedatives: According to animal research, berberine may have sedative effects (51; 112; 113).
  • VasopressorsVasopressors: Hydrastine may theoretically induce vasoconstriction, possibly resulting in hypertension. In animal research, dose-dependent vasoconstriction was observed beginning at a concentration of 50mcL/mL of goldenseal, although neither berberine, an alkaloid constituent in goldenseal, nor hydrastine alone, demonstrated this effect (52).
  • Wound-healing agentsWound-healing agents: In human research, an ointment consisting of beta-sitosterol, sesame oil, and berberine in addition to other plant components (MEBO?) was reported to improve pain relief for burn wounds (114).
  • YohimbeYohimbe: Berberine competitively inhibited the binding of yohimbine, which may or may not affect its pharmacologic actions when the two agents are administered concurrently (115).
  • Goldenseal/Food Interactions:

  • Insufficient available evidence.
  • Goldenseal/Lab Interactions:

  • Anti-inflammatory markersAnti-inflammatory markers: There is limited evidence of the anti-inflammatory properties of berberine in animals (89; 15).
  • BilirubinBilirubin: In in vitro and animal research, berberine displaced bilirubin from albumin and increased serum total and direct bilirubin concentrations (64).
  • Blood glucoseBlood glucose: According to animal and in vitro research, berberine may improve insulin resistance (22), lower blood sugar concentrations (23), and decrease glucose absorption (25).
  • Blood pressureBlood pressure: In clinical research on patients with refractory congestive heart failure, no significant circulatory changes occurred with the lower dose of berberine, an alkaloid constituent in goldenseal (a 0.02mg/kg/min intravenous infusion of berberine). But at the higher dose (a 0.2mg/kg/min intravenous infusion of berberine), a 48% decrease in systemic vascular resistance, a 41% decrease in pulmonary vascular resistance, a 28% decrease in right atrial pressures, and a 32% decrease in left ventricular end-systolic pressures were reported (53). In animal research, intravenous berberine caused a significant decrease in systolic and diastolic blood pressure at doses of 2-8mg/kg (81).
  • Coagulation panelCoagulation panel: In in vitro and animal research, goldenseal and berberine inhibited platelet aggregation, which may increase the risk of bleeding when used with anticoagulant or antiplatelet agents (54; 55). However, goldenseal may reduce the anticoagulant effects of warfarin due to antagonist properties, and theoretically may increase the risk of blood clots.
  • Electrocardiogram (ECG)Electrocardiogram (ECG): In animal research, berberine restored ventricular arrhythmias and atrial fibrillation to normal sinus rhythm (7). However, in human research, patients with congestive heart failure developed ventricular tachycardia after intravenous berberine was administered at a rate of 0.2mg/kg/min (53).
  • Lipid profileLipid profile: In clinical research, berberine reduced triglycerides, serum cholesterol, and LDL cholesterol (72; 91). However, an effect on HDL cholesterol was lacking.
  • SodiumSodium: According to a human case report and review, goldenseal may cause elevated sodium levels in the blood (hypernatremia) (83).
  • Urinalysis (THC detection)Urinalysis (THC detection): Goldenseal may interfere with THC detection in urinalysis (116). Urine containing goldenseal may give a brownish color (116).
  • White blood cell countWhite blood cell count: In human research, leukocyte counts increased to >4,000 in patients with leukopenia with administration of 50mg of berberine three times daily for 1-4 weeks (30).