Monacolin K
Red yeast rice/Drug Interactions:
AlcoholAlcohol: According to secondary sources, risk of hepatotoxicity may increase with concomitant use of red yeast rice and alcohol, due to HMG-CoA reductase inhibitor properties of red yeast rice.AntibioticsAntibiotics: According to secondary sources, taking cyclosporine, ranitidine (Zantac?), and certain antibiotics with red yeast rice extract (RYRE) may increase the risk of muscle breakdown or kidney damage.Anticoagulants and antiplateletsAnticoagulants and antiplatelets: According to a review of HMG-CoA reductase inhibitor products, red yeast rice (RYR) may increase the risk of bleeding (59). Antidiabetic agentsAntidiabetic agents: In animal and human research, red yeast rice decreased glucose (62; 61; 60). However, another animal study noted increased glucose with red yeast rice use (22). In human clinical trials, red yeast rice combination products revealed increased insulin sensitivity in insulin-resistant individuals (107; 108). AntifungalsAntifungals: According to a review of HMG-CoA reductase inhibitor products, RYR may interact with azoles (59). AntihypertensivesAntihypertensives: In animal research, the aqueous extract of Monascus purpureus M9011 had antihypertensive and metabolic effects when used in fructose-induced hypertensive rats (64; 65). In human clinical trials, Xuezhikang combined with either valsartan or nifedipine had antihypertensive effects (53; 66). Other human trials and reviews reported a lack of significance with respect to improvements in blood pressure profiles with RYR supplementation (31; 73). Anti-inflammatory agentsAnti-inflammatory agents: In animal and clinical trials, red yeast rice products decreased inflammation (109; 110; 71). AntineoplasticsAntineoplastics: In a large multicenter clinical trial, a significant reduction in deaths caused by cancer was reported in patients using RYR (36). In vitro, ankaflavin, from red yeast rice, was toxic to human cancer cell lines (19), and monacolin K, the major monacolin of red yeast rice, inhibited the proliferation of Caco-2 cells in a dose-dependent manner (18). In an animal study, oral administration of monascorubrin, from red yeast rice, inhibited skin tumor production in induced animals (20). Antiobesity agentsAntiobesity agents: In vitro, RYRE suppressed adipogenesis (25). In human combination studies, red yeast rice combined with alternative treatments resulted in net weight loss (119). AntiretroviralsAntiretrovirals: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with protease inhibitors (59). Cardiac glycosidesCardiac glycosides: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with cardiac glycosides (59). Cardiovascular agentsCardiovascular agents: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with cardiac glycosides (59). CyclosporineCyclosporine: According to a review of HMG-CoA reductase inhibitor products and because red yeast rice works similarly to those drugs, the risk of myopathy, myalgia, and rhabdomyolysis may increase, because cyclosporine may increase blood levels of red yeast rice (59). Cytochrome P450-modifying agentsCytochrome P450-modifying agents: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with CYP 450-metabolized agents (59). Cytochrome P450-3A inhibiting drugs include theophylline, ketoconazole, itraconazole, fluconazole, nefazodone, and protease inhibitors. However, in laboratory research, dyes such as Monascus were not substrates for CYP2A6, although Monascus was able to inhibit UGT1A6 and UGT2B7 (121). Dermatologic agentsDermatologic agents: According to a systematic review, mild cases of pruritus and rash were reported (31; 32). DigoxinDigoxin: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with digoxin (59). Drugs that cause rhabdomyolysisDrugs that cause rhabdomyolysis: According to a review of HMG-CoA reductase inhibitor products may increase the risk of rhabdomyolysis (59). Fibric acid derivativesFibric acid derivatives: According to a review of HMG-CoA reductase inhibitor products, the risk of myopathy may increase, based on an increased risk in individuals using combination drug therapy of fibrates and HMG-CoA reductase inhibitor products (59). Gastrointestinal agentsGastrointestinal agents: In human clinical trials, red yeast rice caused gastrointestinal concerns, such as nausea, heartburn, inflammatory bowel disease, or gas (34; 36; 31; 44; 45; 35; 46; 47; 43; 48; 39; 49; 50; 51; 52; 53). HepatotoxinsHepatotoxins: In human research, red yeast rice increased aspartate aminotransferase (AST) and alanine aminotransferase (ALT) (7; 33; 34; 31; 35; 36; 39). Similarly, a combination study of red yeast rice with niacin and aliphatic alcohols showed increased AST, ALT, and gamma-GT (103). However, in at least one human study, RYR decreased blood levels of ALT and AST (52). Case studies have reported acute hepatitis associated with the use of supplements containing RYRE, with prompt resolution upon supplement discontinuation (37; 38). HypoglycemicsHypoglycemics: In animal and human research, red yeast rice decreased glucose (62; 61; 60). However, another animal study noted increased glucose with red yeast rice use (22). In a human clinical trials, red yeast rice combination products revealed increased insulin sensitivity in insulin-resistant individuals (107; 108). HypotensivesHypotensives: In animal research, the aqueous extract of Monascus purpureus M9011 had antihypertensive and metabolic effects when used in fructose-induced hypertensive rats (64; 65). In human clinical trials, Xuezhikang combined with either valsartan or nifedipine had antihypertensive effects (53; 66). Other human trials and reviews reported a lack of significance with respect to improvements in blood pressure profiles with RYR supplementation (31; 73). ImmunosuppressantsImmunosuppressants: Certain compounds found in Monascus may result in immune system suppression (17). IronIron: In animal research, red yeast rice decreased hemoglobin (22). LevothyroxineLevothyroxine: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may decrease the efficacy of levothyroxine (59). MacrolidesMacrolides: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may interact with macrolide antibiotics (59). Neurologic agentsNeurologic agents: In humans, cases of dizziness were reported in individuals prone to dizziness (45; 35; 49). Protease inhibitorsProtease inhibitors: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with protease inhibitors (59). RanitidineRanitidine: According to secondary sources, taking ranitidine (Zantac?) with red yeast rice extract may increase the risk of muscle breakdown or kidney damage.StatinsStatins: According to a review of HMG-CoA reductase inhibitor products, risk of myopathy may increase, based on an increased risk in individuals using combination drug therapy of fibrates and HMG-CoA reductase inhibitor products (59). Thyroid hormonesThyroid hormones: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may decrease the efficacy of thyroid agents (59). Red yeast rice/Herb/Supplement Interactions:
AntibacterialsAntibacterials: According to secondary sources, taking certain antibacterials with red yeast rice extract may increase the risk of muscle breakdown or kidney damage.Anticoagulants and antiplateletsAnticoagulants and antiplatelets: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may increase the risk of bleeding (59). Antidiabetic agentsAntidiabetic agents: In animal and human research, red yeast rice decreased glucose (62; 61; 60). However, another animal study noted increased glucose with red yeast rice use (22). In human clinical trials, red yeast rice combination products revealed increased insulin sensitivity in insulin-resistant individuals (107; 108). AntifungalsAntifungals: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may interact with azoles (59). AntihypertensivesAntihypertensives: In animal research, the aqueous extract of Monascus purpureus M9011 had antihypertensive and metabolic effects when used in fructose-induced hypertensive rats (64; 65). In human clinical trials, Xuezhikang combined with either valsartan or nifedipine had antihypertensive effects (53; 66; 53). Other human trials and reviews reported a lack of significance with respect to improvements in blood pressure profiles with RYR supplementation (31; 73). Anti-inflammatory agentsAnti-inflammatory agents: In animal and clinical trials, red yeast rice products decreased inflammation (71; 109; 110). AntineoplasticsAntineoplastics: In a large multicenter clinical trial, a significant reduction in deaths caused by cancer was reported in patients using RYR (36). In animal and laboratory research, red yeast rice had anticancer effects (18; 19; 20). AntioxidantsAntioxidants: Early clinical and laboratory research suggested that red yeast rice has antioxidant activity (76; 122). AstaxanthinAstaxanthin: In an animal study, the combination of policosanol, red yeast rice extract, and astaxanthin had antiatherosclerotic effects (123). Cardiac glycosidesCardiac glycosides: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with cardiac glycosides (59). Cardiovascular agentsCardiovascular agents: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with cardiac glycosides (59). Coenzyme Q10Coenzyme Q10: In an animal trial, acute use of red yeast rice depleted tissue CoQ10 levels (124). In a case study of an elderly male, Chinese red rice depleted muscle coenzyme Q10 and maintained muscle damage after discontinuation of statin treatment (54). In clinical research, three months of statin treatment lowered plasma and platelet levels of CoQ10 in the absence of CoQ10 supplementation (125). Serum CoQ10 decreased by up to 30% with use of statins, including lovastatin (126; 127; 128; 129). Further understanding of the clinical implications of this reduction is needed, especially with prolonged use of statins (126). Cytochrome P450-modifying agentsCytochrome P450-modifying agents: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with CYP 450-metabolized agents (59). However, in laboratory research, dyes such as Monascus were not substrates for CYP2A6, although Monascus was able to inhibit UGT1A6 and UGT2B7 (121). Gastrointestinal agentsGastrointestinal agents: In human clinical trials, red yeast rice caused gastrointestinal concerns, such as nausea, heartburn, inflammatory bowel disease, or gas (34; 36; 31; 44; 45; 35; 46; 47; 43; 48; 39; 49; 50; 51; 52; 81; 53). GrapefruitGrapefruit: According to a review of HMG-CoA reductase inhibitor products, grapefruit juice may elevate the bioavailability of red yeast rice (130). In clinical research, grapefruit juice in combination with lovastatin greatly increased serum concentrations of lovastatin and lovastatin acid, its active metabolite (130). HepatotoxinsHepatotoxins: In human clinical trials, red yeast rice increased AST and ALT (7; 33; 34; 31; 35; 36; 39). In human combination trials, red yeast rice combined products with niacin and aliphatic alcohols increased AST, ALT, and gamma-GT (103). However, in at least one human study, RYR decreased blood levels of ALT and AST (52). Case studies have reported acute hepatitis associated with the use of supplements containing RYRE, with prompt resolution upon supplement discontinuation (37; 38). HypoglycemicsHypoglycemics: In human and animal research, red yeast rice decreased glucose (62; 61; 60). However, another animal study noted increased glucose with RYR rice use (22). In human clinical trials, red yeast rice combined products revealed increased insulin sensitivity in insulin-resistant individuals (107; 108). HypotensivesHypotensives: In animal research, the aqueous extract of Monascus purpureus M9011 had antihypertensive and metabolic effects when used in fructose-induced hypertensive rats (64; 65). In human clinical trials, Xuezhikang combined with either valsartan or nifedipine had antihypertensive effects (53; 66). Other human trials and reviews reported a lack of significance with respect to improvements in blood pressure profiles with RYR supplementation (31; 73). ImmunostimulantsImmunostimulants: Certain compounds found in Monascus may result in immune system suppression (17). A clinical trial revealed one case of influenza while on a RYR supplement (44). ImmunosuppressantsImmunosuppressants: Certain compounds found in Monascus may result in immune system suppression (17). A clinical trial revealed one case of influenza while on a RYR supplement (44). IronIron: In animal research, red yeast rice decreased hemoglobin (22). Milk thistleMilk thistle: According to secondary sources, RYR may interact with red yeast rice. The clinical significance is unknown.Neurologic agentsNeurologic agents: In humans, cases of dizziness were reported in individuals prone to dizziness (45; 35; 49). NiacinNiacin: According to a review of HMG-CoA reductase inhibitor products, the combination of niacin and red yeast may be synergistic and may increase risk of myopathy, myalgia, and rhabdomyolysis (59). In clinical research, a dietary supplement made of Monascus purpureus, octacosanols, and niacin decreased TC, LDL-C, and TG (102). Octacosanol, policosanolOctacosanol, policosanol: In clinical research, a dietary supplement made of Monascus purpureus, octacosanols, and niacin decreased TC, LDL-C, and TG (102). In animal research, the combination of policosanol, red yeast rice extract, and astaxanthin had antiatherosclerotic effects (123). St. John's wortSt. John's wort: According to a review of HMG-CoA reductase inhibitor products, use of St. John's wort may reduce red yeast levels via hepatic enzymes (cytochrome P450 3A4) (59). Tannin-containing agentsTannin-containing agents: In laboratory research, certain water extracts of red yeast rice contained a high percentage of condensed tannins (122). Thyroid agentsThyroid agents: According to a review of HMG-CoA reductase inhibitor products, RYR may decrease the efficacy of thyroid agents (59). Vitamin AVitamin A: In human research, RYR increased levels of serum vitamin A (131). ZincZinc: In vitro, antibacterial activity of Monascus purpureus was affected by zinc (132).Red yeast rice/Food Interactions:
GeneralGeneral: Food may enhance the bioavailability of lovastatin (monacolin K). Taking it with food may reduce the risk of heartburn, gas, and stomachache.FructoseFructose: In animal research, an aqueous extract of Monascus purpureus M9011 prevented and reversed fructose-induced hypertension (64). The clinical significance in humans in unknown. GrapefruitGrapefruit: In clinical research, grapefruit juice in combination with lovastatin greatly increased serum concentrations of lovastatin and lovastatin acid, its active metabolite (130; 130). Red yeast rice/Lab Interactions:
AlbuminAlbumin: In a human clinical trial, RYR was associated with an increase in serum albumin after one year of treatment (85). Beta-2-microglobulinBeta-2-microglobulin: Reduction in serum and urine beta-2-microglobulin levels has been reported in human trials (115). Blood urea nitrogen (BUN)Blood urea nitrogen (BUN): In animal research, decreased BUN has been noted with red yeast rice use (22). In a meta-analysis of human trials, a small proportion of studies reported an increase in BUN levels (35; 43). Carboxy-terminal propeptide of procollagen type I (PIP)Carboxy-terminal propeptide of procollagen type I (PIP): In a human clinical trial, RYR treatment resulted in significant decreases of serum PIP after 72 weeks (66). Circulating endothelial progenitor cells (CEPCs): Circulating endothelial progenitor cells (CEPCs): In human research, Xuezhikang increased the number of circulating and adherent cells, as well as the proliferation of circulating endothelial progenitor cells (CEPCs) (73). C-reactive protein (CRP) levelsC-reactive protein (CRP) levels: In clinical trials, use of red yeast or Xuezhikang decreased CRP (71; 109; 66; 50). Coenzyme Q10 (CoQ10)Coenzyme Q10 (CoQ10): In clinical research, three months of statin treatment lowered plasma and platelet levels of CoQ10 in the absence of CoQ10 supplementation (125). Serum CoQ10 decreased by up to 30% with use of statins, including lovastatin (126; 127; 128; 129). Creatine kinase (CK)Creatine kinase (CK): Elevation in CK levels may occur, according to a review of HMG-CoA reductase inhibitor products (59) and as has been demonstrated in human clinical trials and meta-analyses of red yeast products (84; 34; 31; 36; 44). CyclosporineCyclosporine: According to a review of HMG-CoA reductase inhibitor products, and because red yeast rice works similarly to those drugs, the risk of myopathy, myalgia, and rhabdomyolysis may increase, because cyclosporine may increase blood levels of red yeast rice (59). DigoxinDigoxin: According to a review of HMG-CoA reductase inhibitor products, red yeast may interact with digoxin (59). EndothelinEndothelin: In human research, RYR decreased blood endothelin levels (50)GlucoseGlucose: In animal and human clinical trials, red yeast rice decreased glucose (62; 61; 60). However, another animal study noted increased glucose with red yeast rice use (22). Hemoglobin levelsHemoglobin levels: In animal research, red yeast rice decreased hemoglobin (22). Immunological biochemistryImmunological biochemistry: Reduction in IgG levels and serum immune complex have been reported in human trials (115). Lactate levelsLactate levels: In animal research, red yeast rice decreased lactate levels (22). Nitric oxide (NO)Nitric oxide (NO): In human clinical research, RYR increased serum NO levels (50).Prothrombin time (PT)Prothrombin time (PT): Prolongation of PT may occur, according to a review of HMG-CoA reductase inhibitor products (59). Serum creatinineSerum creatinine: In a human clinical trial, Xuezhikang treatment resulted in elevated serum creatinine (47). Thyroid hormone levelsThyroid hormone levels: According to a review of HMG-CoA reductase inhibitor products, red yeast rice may affect thyroid hormone levels (59). Transaminases/liver enzyme levelsTransaminases/liver enzyme levels: In human clinical research, red yeast rice increased AST and ALT (7; 33; 34; 31; 35; 36; 46; 43; 39). In human combination trials, red yeast rice combined products with niacin and aliphatic alcohols increased AST, ALT, and gamma-GT (103). However, in at least one human study, RYR decreased blood levels of ALT and AST (52). Uric acidUric acid: In a clinical trial, RYR combined with nattokinase for 3-6 months decreased uric acid by up to 10.8% (114).