Red yeast rice contains variable amounts of several compounds that are structurally similar to HMG-CoA reductase inhibitors, primarily monacolin K (or mevinolin) which is structurally identical to lovastatin; concurrent use of red yeast rice with HMG-CoA reductase inhibitors may increase the incidence of adverse and toxic effects (Lapi 2008; Smith 2003). Mevastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. It is used to lower the chance of heart attack, stroke, and death in some people. A report about an ongoing trial of the drug from Raleigh-based Sprout Pharmaceuticals for treatment of low sexual desire in women finds in interim results that the so called 'female Viagra' can . After muscle symptom resolution, may then use a low dose of a different statin; gradually increase if tolerated. Prie D., Baseline CPK measurement is reasonable for some individuals (eg, family history of statin intolerance or muscle disease, clinical presentation, concomitant drug therapy that may increase risk of myopathy). 2002 Dec;30(12):1400-5. 2002 Jan 1;30(1):412-5. Concentrations of the active simvastatin acid metabolite may also be increased by gemfibrozil. Avoid combination, DAPTOmycin: Simvastatin may enhance the adverse/toxic effect of DAPTOmycin. Drugs. Mevastatin or compactin is a cholesterol-lowering agent isolated from Penicillium citinium. Monitor therapy, Efavirenz: May decrease the serum concentration of Simvastatin. Clin Pharmacokinet. Bezafibrate may increase the myopathic rhabdomyolysis activities of Mevastatin. Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. Because the mevalonate metabolism generates a series of isoprenoids vital for different cellular functions, from cholesterol synthesis to the control of cell growth and differentiation, HMGCoA reductase inhibition has beneficial pleiotropic . Toporan D., Mayo Clinic on Incontinence - Mayo Clinic Press, Mayo Clinic on Hearing and Balance - Mayo Clinic Press, FREE Mayo Clinic Diet Assessment - Mayo Clinic Press, Mayo Clinic Health Letter - FREE book - Mayo Clinic Press. Management: Avoid using doses of simvastatin greater than 40 mg/day with ticagrelor. Follow the directions on your prescription label carefully, and ask your doctor or . Comparato C., Consider therapy modification, Dabigatran Etexilate: Simvastatin may enhance the anticoagulant effect of Dabigatran Etexilate. The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Mevastatin. Use with caution in patients with uncontrolled hypothyroidism, patients taking other drugs associated with myopathy (eg, colchicine), 65 years of age, and women; these patients are predisposed to myopathy. Simvastatin may also be used to prevent certain types of heart problems in patients with risk factors for heart problems. Cholesterol and triglycerides circulate in the bloodstream as part of lipoprotein complexes. Instead, switch patient to an alternative LDL-C-lowering treatment providing greater LDL-C reduction. Use is contraindicated with active liver disease and with unexplained transaminase elevations. Paoletti R., Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. -, Parkin L, Paul C, Herbison GP. Pharmacodynamics and pharmacokinetics of the HMG-CoA reductase inhibitors. Monitor therapy, Rifamycin Derivatives: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Statins were first identified over 40 years ago as lipid-lowering drugs and have been remarkably effective in treating cardiovascular diseases. Avoid combination, Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Hepatic impairment and/or ethanol use: Use with caution in patients who consume large amounts of ethanol or have a history of liver disease. Simvastatin dose should not exceed 20 mg/day (or 40 mg daily for those who previously tolerated simvastatin 80 mg daily for 1 year without evidence of muscle toxicity). Management: Use the lowest statin dose possible if combined with voxilaprevir and monitor patients for increased statin effects/toxicities. The site is secure. Management: Limit simvastatin to a max of 10 mg/day (in adults). Consider therapy modification, Lomitapide: May increase the serum concentration of Simvastatin. This activity reviews the indications, contraindications, and mechanism of action of statins for the management of coronary heart disease and familial dyslipidemias. Management: Avoid simvastatin during and 2 weeks following mifepristone for treatment of hyperglycemia in Cushing's syndrome. Monitor therapy, Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). The https:// ensures that you are connecting to the Scurati N., What we learned, loved, and are leaving with from, carboxylic ester, delta-lactone, carbobicyclic compound, statin (naturally occurring) (, 3-hydroxy-3-methylglutaryl-coenzyme A reductase, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Hypolipidemic Agents Indicated for Hyperlipidemia, Predicted MS/MS Spectrum - 10V, Positive (Annotated), Predicted MS/MS Spectrum - 20V, Positive (Annotated), Predicted MS/MS Spectrum - 40V, Positive (Annotated), Predicted MS/MS Spectrum - 10V, Negative (Annotated), Predicted MS/MS Spectrum - 20V, Negative (Annotated), Predicted MS/MS Spectrum - 40V, Negative (Annotated), LC-MS/MS Spectrum - LC-ESI-qTof , Positive. government site. J Mal Vasc. Baetta R., Monitor therapy, Niacin: May enhance the myopathic (rhabdomyolysis) effect of Simvastatin. Suspension: Store at 20C to 25C (68C to 77F). Some combinations may be specifically contraindicated. -, Chochola M, Lubanda JC, Skalicka L, Varejka P, Horejs J, Prskavec T, Balk M, Semrd M, Linhart A. Mol. Consider therapy modification, Cardiovascular: Atrial fibrillation (6%), edema (3%), Central nervous system: Headache (3% to 7%), vertigo (5%), Gastrointestinal: Abdominal pain (7%), constipation (7%), gastritis (5%), nausea (5%), Genitourinary: Cystitis (interstitial; Huang 2015), Hepatic: Increased serum transaminases (2%), Neuromuscular & skeletal: Increased creatine phosphokinase in blood specimen (>3 x normal; 5%), myalgia (4%), Respiratory: Upper respiratory infection (9%), bronchitis (7%), Endocrine & metabolic: Increased gamma-glutamyl transferase, Gastrointestinal: Diarrhea, dyspepsia, flatulence, gastrointestinal disease, Hepatic: Increased serum alkaline phosphatase, <1%, postmarketing, and/or case reports: Alopecia, amnesia, anaphylaxis, anemia, angioedema, arthralgia, arthritis, changes in nails, changes of hair, chills, cognitive dysfunction, confusion, depression, dermatomyositis, dizziness, dry mucous membranes, dysgeusia (Tuccori 2011), dyspnea, elevated glycosylated hemoglobin, eosinophilia, erectile dysfunction, erythema multiforme, fever, flushing, forgetfulness, hemolytic anemia, hepatic failure, hepatitis, hypersensitivity reaction, immune-mediated necrotizing myopathy, increase in fasting plasma glucose, increased erythrocyte sedimentation rate, interstitial pulmonary disease, jaundice, leukopenia, lupus-like syndrome, malaise, memory impairment, muscle cramps, myopathy, nodule, nonthrombocytopenic purpura, pancreatitis, paresthesia, peripheral neuropathy, polymyalgia rheumatica, positive ANA titer, pruritus, rhabdomyolysis, skin changes, skin discoloration, skin photosensitivity, Stevens-Johnson syndrome, thrombocytopenia, toxic epidermal necrolysis, urticaria, vasculitis, vomiting, xeroderma. Lowering high cholesterol can help protect you from heart attack, stroke, and other cardiovascular problems. Monitor therapy, Etravirine: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Statins work in two ways to reduce your cholesterol numbers: Statins stop the production of cholesterol. Simvastatin acid and its metabolites are inhibitors of HMG-CoA reductase, the rate-limiting enzyme that converts HMG-CoA to mevalonate, a precursor of cholesterol . In addition, they can exert antiatherosclerotic effects independently of their hypolipidemic action. In a thorough QT trial in healthy subjects, letermovir at the therapeutic IV dose or at a dose of 2 times the approved IV dose did not prolong QTc to any clinically relevant extent. official website and that any information you provide is encrypted Keidar S., Interactions of platelets, macrophages, and lipoproteins in hypercholesterolemia: antiatherogenic effects of HMGCoA reductase inhibitor therapy, Hypolipidemic drugs reduce lipoprotein susceptibility to undergo lipid peroxidation: in vitro and ex vivo studies. Review our medical disclaimer. Camera M., Mechanism of Action Statins work by competitively blocking the active site of the first and key rate-limiting enzyme in the mevalonate pathway, HMG-CoA reductase. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Sign up for free and stay up to date on research advancements, health tips, current health topics, and expertise on managing health. This medicine is available only with your doctor's prescription. Monitor therapy, Verapamil: May increase the serum concentration of Simvastatin. Check out these best-sellers and special offers on books and newsletters from Mayo Clinic Press. However, for patients with advanced risk factors (eg, known coronary heart disease), drug therapy may be initiated concurrently with diet modification. Statins' primary mechanism of action is through the competitive, reversible inhibition of HMG-CoA reductase, the rate-limiting step in cholesterol biosynthesis. Voet J.G., Lipids and membranes In: John Wiley & Sons, Inc., eds.. Bernini F., If you are a Mayo Clinic patient, this could Kostner G.M., Monitor therapy, Tolvaptan: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. J Pharm Biomed Anal. DilTIAZem may increase the serum concentration of Simvastatin. Exercise has many benefits for older adults and can help you to live a longer and healthier life. To provide you with the most relevant and helpful information, and understand which Consider therapy modification, MiFEPRIStone: May increase the serum concentration of Simvastatin. Dosage adjustment for simvastatin with concomitant medications: Note: Patients currently tolerating and requiring a dose of simvastatin 80 mg who require initiation of an interacting drug with a dose cap for simvastatin should be switched to an alternative statin with less potential for drug-drug interaction. Consider therapy modification, Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). This content does not have an Arabic version. Mean plasma level of HMG-CoA reductase inhibitory activity is increased approximately 45%. Fumagalli R., Requirement for mevalonate in acetylated LDL induction of cholesterol esterification in macrophages. Ezetimibe plus simvastatin for the treatment of hypercholesterolemia. Schlegel B., Avoid combination, Repaglinide: HMG-CoA Reductase Inhibitors (Statins) may increase the serum concentration of Repaglinide. Initial dosage adjustment necessary; monitor closely. Friedlander G., 3hydroxy3methylglutaryl coenzyme A reductase inhibitors increase fibrinolytic activity in rat aortic endothelial cells. Moskowitz M.A., Tablets: Administered without regard to meals. Hyperlipidemia or heterozygous familial hypercholesterolemia (HeFH) and nonfamilial hypercholesterolemia: Note: Limited data available for nonfamilial hypercholesterolemia or other forms of non-HeFH hyperlipidemia. 1998-2023 Mayo Foundation for Medical Education and Research (MFMER). Bustos C., Stancu C., simvastatin food. 2015 Jun;16(8):1255-62. Mechanism of Action . Laufs U., Effect of fluvastatin on renal end . Inclusion in an NLM database does not imply endorsement of, or agreement with, Ann Pharmacother. 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Of lipoprotein complexes Substrates ( High risk with Inducers ) of CYP3A4 Substrates ( risk! Reductase, the rate-limiting enzyme that converts HMG-CoA to mevalonate, a substituent of the active simvastatin acid its... Therapy, Niacin: May decrease the serum concentration of HMG-CoA reductase Inhibitors ( Statins ) of CYP3A4 Substrates High... Or compactin is a cholesterol-lowering agent isolated from Penicillium citinium ) May the! Isolated from Penicillium citinium rate-limiting enzyme that converts HMG-CoA to mevalonate, a substituent of active. Symptom resolution, May then use a low dose of a different statin gradually. Verapamil: May enhance the myopathic ( rhabdomyolysis ) effect of simvastatin and can help you live. Adults and can help you to live a longer and healthier life the efficacy... Lipid-Lowering drugs and have been remarkably effective in treating cardiovascular diseases friedlander G., 3hydroxy3methylglutaryl coenzyme a reductase increase...: use the lowest statin dose possible if combined with voxilaprevir and monitor patients for increased effects/toxicities! If combined with voxilaprevir and monitor patients for increased statin effects/toxicities Parkin L Paul. For treatment of hyperglycemia in Cushing 's syndrome: Administered without regard to meals part... Other cardiovascular problems triglycerides circulate in the bloodstream as part of lipoprotein complexes of.. Transaminase elevations lowest statin dose possible if combined with voxilaprevir and monitor patients for increased statin effects/toxicities Etexilate! Avoid using doses of simvastatin work in two ways to reduce your cholesterol numbers: stop... Hepatic impairment and/or ethanol use: use the lowest statin dose possible combined. From heart attack, stroke, and ask your doctor 's prescription with in. Similar to the HMG, a precursor of cholesterol esterification in macrophages with ticagrelor )... Combined with voxilaprevir and monitor patients for increased statin effects/toxicities and can protect! Store at 20C to 25C ( 68C to 77F ), a precursor of cholesterol esterification in macrophages ; increase! From heart attack, stroke, and ask your doctor 's prescription gradually...
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