DOCSLIB.ORG

“A Review on Rosuvastatin”

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
“A Review on Rosuvastatin” REVIEW PAPER INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL ANALYSIS (2017, VOl. 01(02) WWW.IJPPA.COM ISSN: 2394-1618 Page numbers:96-105 ISSN:XXXXX “A REVIEW ON ROSUVASTATIN” AISWARYA S*, GOWRISANKAR N L, FARSENA A AND SREE LAKSHMI P S *Department of Pharmaceutics, Prime College of Pharmacy, Erattayal, Palakkad-678551, Kerala, India ABSTRACT Rosuvastatin is a new generation HMG-CoA reductase inhibitor which exhibits some unique pharmacologic and pharmacokinetic properties. It has low extra hepatic tissue penetration, low potential for CYP3A4 interactions and substantial LDL-C lowering capacity and therefore has distinct advantages. Present review provides an account of pharmacology of rosuvastatin, highlighting its efficacy and safety and a brief comparison with other statins. Keywords: Rosuvastatin, Cardiovascular risk, Statins, Low density lipoprotein cholesterol. *Address of the corresponding author: Aiswarya S, M.Pharm, Department of Pharmaceutics, Prime college of Pharmacy, Erattayal, Mobile: 8547053123, E-mail address: [email protected] INTRODUCTION and the incidence of cardiovascular Cholesterol is a waxy, fat like substance disease. The associated morbidity and that is found in all cells of the body. Our mortality is positively correlated to low body needs some cholesterol to make density lipoprotein cholesterol (LDL) and hormones, vitamin D, and substances that inversely related to high density help you process nourishment. Our body lipoprotein cholesterol (HDL). [1, 2] makes all the cholesterols it needs. Ischemic heart diseases are the leading Cholesterols go through our circulatory cause of mortality worldwide and system in little bundles called lipoprotein. constitute a major health burden. These bundles are made of fat within and According to world health organization proteins on the outside. Two sorts of statistics it accounts for 12.8% of death, lipoproteins convey cholesterol all with strokes and other cerebrovascular through your body. Low thickness disease accounting for 10.8 %. In United lipoproteins (LDL) and high thickness Kingdom, data from the Health survey for lipoproteins (HDL). Having sound levels England suggest that while mortality may of both sorts of lipoproteins is important. decline, cardiovascular disease morbidity Epidemiological studies have established continues to rise. Epidemiology studies a strong correlation between cholesterol have established a strong correlation REVIEW PAPER INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL ANALYSIS (2017, VOl. 01(02) WWW.IJPPA.COM ISSN: 2394-1618 Page numbers:96-105 ISSN:XXXXX between cholesterol and the incidence of ischemic heart disease patients, cardiovascular disease. The associated irrespective of the cholesterol morbidity and mortality is positively concentration. In addition to the correlated to low density lipoprotein beneficial cholesterol lowering effects, cholesterol and inversely related to high statins improve endothelial function, density lipoprotein cholesterol.[3, 4] enhance stability of atherosclerotic Statins are 3-hydroxy-3-methylglutaryl plaques, and inhibit inflammatory as well coenzyme A (HMG Co A) reductase as thrombogenic responses in arterial inhibitors that are effective in the walls. Furthermore extensive post reduction of total and LDL cholesterol. [5] marketing surveillance has shown that A number of large randomized control long term statin therapy is generally well trials have demonstrated unequivocally tolerated. [11] that lowering LDL-C particularly with The reduction in cardiovascular events statins reduces the risk of cardiovascular from statins therapy is proportional to deaths and events. [6] HMG CoA inhibitors the LDL-C reduction; larger reductions in have been shown to prevent initial LDL-C are associated with greater cardiovascular events and subsequent reduction in cardiovascular events, so cardiovascular events in ischemic heart more potent statins results in greater disease patients, irrespective of the cardiovascular risk reduction. [12] cholesterol concentration. [7,8] In addition In this review, we outline the to the beneficial cholesterol lowering pharmacology of rosuvastatin, highlights effects, statins improve endothelial its effects on cholesterol level, sides function, enhance stability of effects and contraindications. atherosclerotic plaques, and inhibit inflammatory as well as thrombogenic DRUG CLASS AND MECHANISM responses in arterial walls. [9] Rosuvastatin is an oral drug for lowering Furthermore extensive post marketing blood cholesterol levels. surveillance has shown that long term It belongs to a class of drug called HMG- statin therapy is generally well tolerated. CoA reductase inhibitors, more commonly [10] referred to as statins. Other drugs in this The reduction in cardiovascular events class include; from unequivocally that lowering LDL-C *Simvastatin (Zocor) particularly with statins reduces the risk *Lovastatin (Mevacor) of cardiovascular deaths and events. *Pravastatin (Pravachol) HMG CoA inhibitors have been shown to *Atrovastatin (Lipitor) prevent initial cardiovascular events and *Fluvastatin (Lescol) subsequent cardiovascular events in REVIEW PAPER INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL ANALYSIS (2017, VOl. 01(02) WWW.IJPPA.COM ISSN: 2394-1618 Page numbers:96-105 ISSN:XXXXX These drugs reduce cholesterol levels by PHARMACOKINETICS inhibiting HMG-CoA reductase, an enzyme The oral bioavailability of rosuvastatin is that produces cholesterol in the lever. 20 %, which is comparable to Rosuvastatin and other statins lower atorvastatin, pravastatin and fluvastatin, blood total cholesterol as well as blood and qualitatively higher than simvastatin LDL cholesterol levels. LDL cholesterol is and lovastatin. After a single oral dose the the bad type of cholesterol that increases peak plasma concentration is reached at 5 the risk of coronary artery disease and hours. This is longer than other HMG-CoA heart attacks. Lowering LDL cholesterol inhibitors which achieve maximum levels shows the progression of coronary plasma concentrations in less than 3 artery disease and may even reverse it. hours. In compiled data from Statins also increase HDL cholesterol, the pharmacokinetic trials, the peak plasma good type of cholesterols, and reduce concentration and area under the triglycerides. concentration time curve show a largely linear relationship as the dose of PHARMACOLOGY rosuvastatin increases from 5 to 80 mg. Rosuvastatin is a fully synthetic HMG-CoA Food intake decreases the rate of reductase inhibitor. Other HMG-CoA absorption of rosuvastatin by 20 % but reductase inhibitors are either natural, not the extent of absorption. This does mevinic acid derived (lovastatin, not reduce the cholesterol lowering simvastatin, pravastatin ) or synthetic, potency; therefore rosuvastatin can be heptenoic acid derived (atorvastatin, taken with or without food, and in the fluvastatin). Rosuvastatin belongs to a morning or evening. [13-18] new generation of methane • Approximately 90 % of rosuvastatin is sulphonamide •pyrimidine and N- protein bound mainly to albumin; other methane sulfonyl pyrrole-substituted 3, statins have approximately 95 % protein 5-dihydroxy-heptenoates. Although the binding except pravastatin which has a characteristic statin pharmacophore lower protein binding of 50 %. The mean remains similar to other statins, the volume of distribution is 134 litres in addition of a stable polar methane- steady state. Rosuvastatin is less sulphonamide group provides low lipophilic than other statins such as lipophilicity and enhanced ionic atorvastatin and simvastatin but more interaction with HMG-CoA reductase lipophilic than pravastatin. Penetration of enzyme thus improving its binding statins into extra-hepatic tissues occurs affinity to this enzyme. by passive diffusion and is dependent on their lipophilicity. This has implications on their muscle safety as increased REVIEW PAPER INTERNATIONAL JOURNAL OF PHARMACY AND PHARMACEUTICAL ANALYSIS (2017, VOl. 01(02) WWW.IJPPA.COM ISSN: 2394-1618 Page numbers:96-105 ISSN:XXXXX rhabdomyolysis was reported in patients rosuvastatin is responsible for on lipophilic agents like cerivastatin and approximately 90 % of plasma HMG-CoA lovastatin. [19, 20] inhibitor activity. Rosuvastatin is less Human hepatocyte studies indicate that likely to cause metabolic drug to drug rosuvastatin is a poor substrate for interactions since it has limited metabolism by cytochrome P450 and metabolism by CYP isoenzymes. Other hence 90 % of the drug is excreted HMG-CoA reductase inhibitors such as unchanged. CYP2C9 is the main atorvastatin and simvastatin are isoenzyme involved in metabolism with metabolised via CYP3A4. Their plasma minimal effect from CYP2C19. concentrations are increased by Rosuvastatin is metabolised to an N- inhibitors of CYP3A4 such as itraconazole, desmethyl metabolite which is less potent protease inhibitors and macrolide than the parent drug in inhibiting HMG- antibiotics. CoA reductase activity. The parent drug Table 1. Compares the pharmacokinetics of different statins Parameter Rosuva Atorva Simva Prava Fluva Pitava Lova statin statin statin statin statin statin statin Tmax (h) 3 2–3 1.3–2.4 0.9–1.6 0.4–2.1 0.6–0.8 2–4 Bioavailability 20 12 5 18 24 80 5 Lipophilicity No Yes Yes No Yes Yes Yes Protein 88 80–90 94–98 43–55 .98 96 95 binding Minimal Sulfation CYP2C9 Minimal Biliary Metabolism CYP2C19 CYP3A4 CYP3A4 CYP2C9 CYP2C8 CYP3A4 & urine Biliary CYP2C9 excretion excretion Active Active Metabolites Active Active
Load more

Recommended publications
  • Roszet (Rosuvastatin/Ezetimibe) – New Drug Approval
    Roszet (rosuvastatin/ezetimibe) – New drug approval • On March 23, 2021, the FDA approved Althera Pharmaceuticals’ Roszet (rosuvastatin/ezetimibe), in adults: as an adjunct to diet in patients with primary non-familial hyperlipidemia to reduce low- density lipoprotein cholesterol (LDL-C) and alone or as an adjunct to other LDL-C-lowering therapies in patients with homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C. • Roszet is a combination tablet containing rosuvastatin, an HMG CoA-reductase inhibitor (statin), and ezetimibe, a dietary cholesterol absorption inhibitor. Both components are available generically. • The approval of Roszet was based on previous efficacy data with rosuvastatin and ezetimibe. • Roszet is contraindicated in patients with: — Acute liver failure or decompensated cirrhosis — Hypersensitivity to rosuvastatin, ezetimibe, or any excipients in Roszet. Hypersensitivity reactions including anaphylaxis, angioedema, and erythema multiforme have been reported. • Warnings and precautions for Roszet include myopathy and rhabdomyolysis, immune-mediated necrotizing myopathy, hepatic dysfunction, proteinuria and hematuria, and HbA1c and glucose levels. • The most common adverse reactions (> 2% and greater than statin alone) with ezetimibe co- administered with a statin are nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, diarrhea, back pain, influenza, pain in extremity, and fatigue. • The recommended dosage range of Roszet is 5 mg/10 mg to 40 mg/10 mg once daily. — The recommended dose of Roszet depends on a patient’s indication for usage, LDL-C, and individual risk for cardiovascular events. — The starting dosage for patients switching to Roszet from co-administration of a statin and ezetimibe is based on an equivalent dose of rosuvastatin and 10 mg of ezetimibe.
    [Show full text]
  • Effects of Pitavastatin, Atorvastatin, and Rosuvastatin on the Risk Of
    biomedicines Article Effects of Pitavastatin, Atorvastatin, and Rosuvastatin on the Risk of New-Onset Diabetes Mellitus: A Single-Center Cohort Study Wei-Ting Liu 1, Chin Lin 2,3,4, Min-Chien Tsai 5, Cheng-Chung Cheng 6, Sy-Jou Chen 7,8, Jun-Ting Liou 6 , Wei-Shiang Lin 6, Shu-Meng Cheng 6, Chin-Sheng Lin 6,* and Tien-Ping Tsao 6,9,* 1 Department of Internal Medicine, Tri-Service General Hospital, National Defense Medical Center, Taipei 11490, Taiwan; [email protected] 2 School of Public Health, National Defense Medical Center, Taipei 11490, Taiwan; [email protected] 3 School of Medicine, National Defense Medical Center, Taipei 11490, Taiwan 4 Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 11490, Taiwan, 5 Department of Physiology and Biophysics, Graduate Institute of Physiology, National Defense Medical Center, Taipei 11490, Taiwan; [email protected] 6 Division of Cardiology, Department of Internal Medicine, Tri-Service General Hospital, National Defense Medical Center, Taipei 11490, Taiwan; [email protected] (C.-C.C.); [email protected] (J.-T.L.); [email protected] (W.-S.L.); [email protected] (S.-M.C.) 7 Department of Emergency Medicine, Tri-Service General Hospital, National Defense Medical Center, Taipei 11490, Taiwan; [email protected] 8 Graduate Institute of Injury Prevention and Control, College of Public Health and Nutrition, Taipei Medical University, Taipei 11031, Taiwan 9 Division of Cardiology, Cheng Hsin General Hospital, Taipei 11220, Taiwan * Correspondence: [email protected] (C.-S.L.); [email protected] (T.-P.T.); Tel.: +886-2-6601-2656 (C.-S.L.); +886-2-2826-4400 (T.-P.T.) Received: 25 October 2020; Accepted: 11 November 2020; Published: 13 November 2020 Abstract: Statins constitute the mainstay treatment for atherosclerotic cardiovascular disease, which is associated with the risk of new-onset diabetes mellitus (NODM).
    [Show full text]
  • Nustendi, INN-Bempedoic Acid, Ezetimibe
    Summary of risk management plan for Nustendi (Bempedoic acid/Ezetimibe) This is a summary of the risk management plan (RMP) for Nustendi. The RMP details important risks of Nustendi, how these risks can be minimized, and how more information will be obtained about Nustendi's risks and uncertainties (missing information). Nustendi's summary of product characteristics (SmPC) and its package leaflet give essential information to healthcare professionals and patients on how Nustendi should be used. This summary of the RMP for Nustendi should be read in the context of all this information, including the assessment report of the evaluation and its plain-language summary, all which is part of the European Public Assessment Report (EPAR). Important new concerns or changes to the current ones will be included in updates of Nustendi's RMP. I. The Medicine and What It Is Used For Nustendi is authorized for treatment of primary hypercholesterolemia in adults, as an adjunct to diet (see SmPC for the full indication). It contains bempedoic acid as the active substance and it is given by mouth. Further information about the evaluation of Nustendi’s benefits can be found in Nustendi’s EPAR, including in its plain-language summary, available on the EMA website, under the medicine’s webpage https://www.ema.europa.eu/en/medicines/human/EPAR/nustendi II. Risks Associated With the Medicine and Activities to Minimize or Further Characterize the Risks Important risks of Nustendi, together with measures to minimize such risks and the proposed studies for learning
    [Show full text]
  • SUMMARY of the PRODUCT CHARACTERISTICS 1. NAME of the MEDICINAL PRODUCT <Invented Name> 10 Mg/10 Mg Film-Coated Tablets
    SUMMARY OF THE PRODUCT CHARACTERISTICS 1. NAME OF THE MEDICINAL PRODUCT <Invented name> 10 mg/10 mg film-coated tablets <Invented name> 20 mg/10 mg film-coated tablets <Invented name> 40 mg/10 mg film-coated tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION <Invented name> 10 mg/10 mg: Each film-coated tablet contains 10 mg of rosuvastatin (as rosuvastatin calcium) and 10 mg of ezetimibe. <Invented name> 20 mg/10 mg: Each film-coated tablet contains 20 mg of rosuvastatin (as rosuvastatin calcium) and 10 mg of ezetimibe. <Invented name> 40 mg/10 mg: Each film-coated tablet contains 40 mg of rosuvastatin (as rosuvastatin calcium) and 10 mg of ezetimibe. Excipient with known effect: <Invented name> 10 mg/10 mg: Each film-coated tablet contains 111.2 mg of lactose (as lactose monohydrate). <Invented name> 20 mg/10 mg: Each film-coated tablet contains 168.6 mg of lactose (as lactose monohydrate). <Invented name> 40 mg/10 mg: Each film-coated tablet contains 286.0 mg of lactose (as lactose monohydrate). For the full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM Film-coated tablet (tablet) <Invented name> 10 mg/10 mg: white to off-white oblong film-coated tablets. <Invented name> 20 mg/10 mg: yellow to light yellow oblong film-coated tablets. <Invented name> 40 mg/10 mg: pink oblong film-coated tablets. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Primary Hypercholesterolaemia/Homozygous Familial Hypercholesterolaemia (HoFH) <Invented name> is indicated for substitution therapy in adult patients who are adequately controlled with rosuvastatin and ezetimibe given concurrently at the same dose level as in the fixed combination, but as separate products, as adjunct to diet for treatment of primary hypercholesterolaemia (heterozygous familial and non-familial) or homozygous familial hypercholesterolaemia.
    [Show full text]
  • Product Monograph Crestor
    PRODUCT MONOGRAPH Pr CRESTOR® rosuvastatin calcium Tablets, 5, 10, 20 and 40 mg LIPID METABOLISM REGULATOR AstraZeneca Canada Inc. Date of Revision: May 14, 2020 1004 Middlegate Road Mississauga, Ontario L4Y 1M4 www.astrazeneca.ca Control No: 235939 CRESTOR® is a registered trademark of the AstraZeneca group of companies. Licensed from Shionogi & Co. Ltd. Osaka, Japan. COPYRIGHT 2003 – 2020 ASTRAZENECA CANADA INC. Page 1 of 46 TABLE OF CONTENTS PART I: HEALTH PROFESSIONAL INFORMATION......................................................3 SUMMARY PRODUCT INFORMATION ..............................................................3 INDICATIONS AND CLINICAL USE....................................................................3 CONTRAINDICATIONS ........................................................................................4 WARNINGS AND PRECAUTIONS .......................................................................5 ADVERSE REACTIONS ...................................................................................... 10 DRUG INTERACTIONS....................................................................................... 16 DOSAGE AND ADMINISTRATION.................................................................... 22 OVERDOSAGE..................................................................................................... 25 ACTION AND CLINICAL PHARMACOLOGY................................................... 25 STORAGE AND STABILITY............................................................................... 27 DOSAGE
    [Show full text]
  • Bempedoic Acid) Tablets, for Oral Use Most Common (Incidence ≥ 2% and Greater Than Placebo) Adverse Reactions Initial U.S
    HIGHLIGHTS OF PRESCRIBING INFORMATION • Tendon Rupture: Tendon rupture has occurred. Discontinue NEXLETOL These highlights do not include all the information needed to use at the first sign of tendon rupture. Avoid NEXLETOL in patients who NEXLETOL™ safely and effectively. See full prescribing information have a history of tendon disorders or tendon rupture. (5.2) for NEXLETOL. --------------------------------ADVERSE REACTIONS----------------------------­ NEXLETOL (bempedoic acid) tablets, for oral use Most common (incidence ≥ 2% and greater than placebo) adverse reactions Initial U.S. Approval: 2020 are upper respiratory tract infection, muscle spasms, hyperuricemia, back pain, abdominal pain or discomfort, bronchitis, pain in extremity, anemia, ----------------------------INDICATIONS AND USAGE--------------------------­ and elevated liver enzymes. (6.1) NEXLETOL is an adenosine triphosphate-citrate lyase (ACL) inhibitor indicated as an adjunct to diet and maximally tolerated statin therapy for the To report SUSPECTED ADVERSE REACTIONS, contact Esperion at treatment of adults with heterozygous familial hypercholesterolemia or 833-377-7633 (833 ESPRMED) or FDA at 1-800-FDA-1088 or established atherosclerotic cardiovascular disease who require additional www.fda.gov/medwatch. lowering of LDL-C. (1) --------------------------------DRUG INTERACTIONS----------------------------­ Limitations of Use: The effect of NEXLETOL on cardiovascular morbidity • Simvastatin: Avoid concomitant use of NEXLETOL with simvastatin and mortality has not been
    [Show full text]
  • Rosuvastatin (Crestor)
    What is most important to remember? If you have questions: Strong Internal Medicine • Use this medicine as directed by your doctor Ask your doctor, nurse or pharmacist for more information about rosuvastatin • It is important to continue taking (Crestor®) this medicine even if you feel normal. Most people with high cholesterol or triglycerides do not feel sick • Do not start any new medicines, over-the-counter drugs or herbal remedies without talking to your doctor • Tell all doctors, dentists and pharmacists that you are using Strong Internal Medicine rosuvastatin (Crestor®) 601 Elmwood Avenue th • Contact your prescriber right away Ambulatory Care Facility, 5 Floor Rochester, NY 14642 if you have severe muscle pain or Phone: (585) 275 -7424 weakness Rosuvastatin Visit our website at: (Crestor®): • Follow the diet and lifestyle www.urmc.rochester.edu/medicine/ - genera medicine/patientcare/ Important Patient Information changes that you talked about l- with your doctor in addition to taking your prescribed medicine to get the greatest health benefits What does rosuvastatin (Crestor®) do? Who should know I am taking rosuvastatin (Crestor®)? What are some things that I need to be aware of when • It is used to lower the level of bad cholesterol (LDL), • Keep a list of all your medicines (prescription, natural taking rosuvastatin (Crestor®)? raise the level of good cholesterol (HDL), and lower products, supplements, vitamins, over-the-counter) and • Tell your doctor or pharmacist if you have a “statin” triglycerides (TG) in the body give
    [Show full text]
  • Efficacy of Combination Therapy of Rosuvastatin and Ezetimibe Vs
    Original Article DOI: 10.7860/JCDR/2017/30458.11004 Efficacy of Combination Therapy Internal Medicine Section of Rosuvastatin and Ezetimibe vs Rosuvastatin Monotherapy on Lipid Profile of Patients with Coronary Artery Disease SANDEEP JOSHI1, RUBY SHARMA2, HARBIR KAUR RAO3, UDIT NARANG4, NITIN GUPTA5 ABSTRACT baseline investigations and lifestyle modifications, Group I Introduction: Dyslipidaemia is one of the most important was started on rosuvastatin 10 mg once daily, while Group modifiable risk factor for the development of Coronary II was started on rosuvastatin 10 mg+ezetimibe 10 mg daily. Artery Disease (CAD). Although, statins are established as The fasting serum lipid profile was repeated initially after first line lipid-lowering therapy, they may not be able to 12 weeks and then after 24 weeks. The two groups were achieve treatment goals in significant number of patients. observed for side effects which were noted. Combination therapy of statin with a non-statin drug like Results: The combination therapy of rosuvastatin and Ezetimibe is a therapeutic option. ezetimibe resulted in significantly higher change in all Aim: To compare the efficacy and safety of Rosuvastatin/ lipid parameters (LDL-C, TC, TG, HDL-C) as compared to Ezetimibe combination therapy vs Rosuvastatin alone on the treatment with rosuvastatin alone. There was no difference in lipid profile of patients with CAD in Northern India. the adverse effects seen after treatment in the two groups. Materials and Methods: This randomized prospective Conclusion: Our study showed that combination therapy study was conducted on 80 patients of CAD presenting of ezetimibe with rosuvastatin can be used as an effective to Department of Medicine, Government Medical College, and safe therapy in high risk patients of CAD, especially in Patiala, Punjab, India.
    [Show full text]
  • CP.PMN.237 Bempedoic Acid (Nexletol)
    Clinical Policy: Bempedoic Acid (Nexletol), Bempedoic Acid/Ezetimibe (Nexlizet) Reference Number: CP.PMN.237 Effective Date: 09.01.20 Last Review Date: 02.21 Revision Log Line of Business: Commercial, HIM, Medicaid See Important Reminder at the end of this policy for important regulatory and legal information. Description The following are adenosine triphosphate-citrate lyase (ACL) inhibitors requiring prior authorization: bempedoic acid (Nexletol™) and bempedoic acid/ezetimibe (Nexlizet™). Nexlizet contains ezetimibe, which is a cholesterol absorption inhibitor. FDA Approved Indication(s) Nexletol and Nexlizet are indicated for use as adjuncts to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or established atherosclerotic cardiovascular disease (ASCVD) who require additional lowering of low-density lipoprotein cholesterol (LDL-C). Limitation(s) of use: The effect of Nexletol and Nexlizet on cardiovascular morbidity and mortality has not been determined. Policy/Criteria Provider must submit documentation (such as office chart notes, lab results or other clinical information) supporting that member has met all approval criteria. It is the policy of health plans affiliated with Centene Corporation® that Nexletol and Nexlizet are medically necessary when the following criteria are met: I. Initial Approval Criteria A. Heterozygous Familial Hypercholesterolemia and Atherosclerotic Cardiovascular Disease (must meet all): 1. Diagnosis of one of the following (a or b): a. ASCVD as evidenced by a history of any one of the following conditions (i-vii): i. Acute coronary syndromes; ii. Clinically significant coronary heart disease (CHD) diagnosed by invasive or noninvasive testing (such as coronary angiography, stress test using treadmill, stress echocardiography, or nuclear imaging); iii.
    [Show full text]
  • Rosuvastatin
    Rosuvastatin Rosuvastatin Systematic (IUPAC) name (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamido)-6-(propan- 2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid Clinical data Trade names Crestor AHFS/Drugs.com monograph MedlinePlus a603033 Pregnancy AU: D category US: X (Contraindicated) Legal status AU: Prescription Only (S4) UK: Prescription-only (POM) US: ℞-only Routes of oral administration Pharmacokinetic data Bioavailability 20%[1] Protein binding 88%[1] Metabolism Liver (CYP2C9(major) andCYP2C19-mediated; only minimally (~10%) metabolised)[1] Biological half-life 19 hours[1] Excretion Faeces (90%)[1] Identifiers CAS Registry 287714-41-4 Number ATC code C10AA07 PubChem CID: 446157 IUPHAR/BPS 2954 DrugBank DB01098 UNII 413KH5ZJ73 KEGG D01915 ChEBI CHEBI:38545 ChEMBL CHEMBL1496 PDB ligand ID FBI (PDBe, RCSB PDB) Chemical data Formula C22H28FN3O6S Molecular mass 481.539 SMILES[show] InChI[show] (what is this?) (verify) Rosuvastatin (marketed by AstraZenecaas Crestor) 10 mg tablets Rosuvastatin, marketed as Crestor, is a member of the drug class of statins, used in combination with exercise, diet, and weight-loss to treat high cholesterol and related conditions, and to prevent cardiovascular disease. It was developed by Shionogi. Crestor is the fourth- highest selling drug in the United States, accounting for approx. $5.2 billion in sales in 2013.[2] Contents [hide] 1Medical uses 2Side effects and contraindications 3Drug interactions 4Structure 5Mechanism of action 6Pharmacokinetics 7Indications and regulation
    [Show full text]
  • Bempedoic Acid
    Drug and Biologic Coverage Policy Effective Date ............................................. 7/15/2020 Next Review Date ......................................... 7/1/2021 Coverage Policy Number .................................. 2015 Bempedoic acid Table of Contents Related Coverage Resources Coverage Policy ................................................... 1 Genetic Testing of Heritable Disorders FDA Approved Indications ................................... 4 Recommended Dosing ........................................ 4 General Background ............................................ 4 Coding/Billing Information .................................... 7 References .......................................................... 7 INSTRUCTIONS FOR USE The following Coverage Policy applies to health benefit plans administered by Cigna Companies. Certain Cigna Companies and/or lines of business only provide utilization review services to clients and do not make coverage determinations. References to standard benefit plan language and coverage determinations do not apply to those clients. Coverage Policies are intended to provide guidance in interpreting certain standard benefit plans administered by Cigna Companies. Please note, the terms of a customer’s particular benefit plan document [Group Service Agreement, Evidence of Coverage, Certificate of Coverage, Summary Plan Description (SPD) or similar plan document] may differ significantly from the standard benefit plans upon which these Coverage Policies are based. For example, a customer’s benefit
    [Show full text]
  • Rosuvastatin (Crestor®) VHA Pharmacy Benefits Management Strategic Healthcare Group and the Medical Advisory Panel
    National PBM-MAP Drug Monograph Rosuvastatin (Crestor®) VHA Pharmacy Benefits Management Strategic Healthcare Group and The Medical Advisory Panel Executive Summary Efficacy In 6 randomized, head-to-head statin comparative clinical trials, 10 mg of rosuvastatin resulted in a reduction in LDL-C of between 43-49%. The approximate equivalent daily dose of simvastatin and atorvastatin to rosuvastatin 10 mg are 80 mg and 40 mg, respectively. With regard to HDL-C elevation and triglyceride lowering, rosuvastatin produced changes similar to that seen with the other statins, with few exceptions. There are currently no published clinical trials demonstrating a reduction in health outcomes with rosuvastatin. Safety In pre-marketing controlled clinical trials, over 10,000 patients have been exposed to rosuvastatin. The most common adverse events included myalgia, constipation, asthenia, abdominal pain and nausea and were similar to those seen with other statins. Clinically significant elevation in liver function tests (LFTs, >3X upper limit of normal) was reported in 0-0.4% of patients receiving doses up to 40 mg daily. Clinically significant elevation in creatine kinase (CK, >10X upper limit of normal) was reported in 0.2-0.4% of patients taking up to 40 mg daily. Symptomatic myopathy, with significant elevation in CK, was reported in 0.1% of patients taking up to 40 mg of rosuvastatin daily. In the rosuvastatin clinical trials program, one case of rhabdomyolysis was reported with the 10 mg dose and 7 cases with the 80 mg dose. Rhabdomyolysis was not observed in pre-marketing clinical trials of other available statins. In the Stellar trial, 2 patients on rosuvastatin 80 mg per day developed renal failure of unknown etiology with one requiring short-term hemodialysis.
    [Show full text]