Atorvastatin 10Mg, 20Mg, 40Mg & 80Mg Film-Coated Tablets

Total Page:16

File Type:pdf, Size:1020Kb

Atorvastatin 10Mg, 20Mg, 40Mg & 80Mg Film-Coated Tablets Atorvastatin 10mg, 20mg, 40mg & 80mg film-coated tablets (Pharmacare®) Atorvastatin (as Atorvastatin calcium) New Zealand Consumer Medicine Information What is in this leaflet What is cholesterol? vessels can lead to several types of blood vessel disease, heart attack, Everyone has cholesterol in their angina and stroke. This leaflet answers some of the blood. It is a type of blood fat more common questions about needed by the body for many things, There is another type of blood fat Atorvastatin. such as building the cell lining, called triglyceride, which is a source It does not contain all of the available making bile acids (which help to of energy. However, high levels of information. It does not take the digest food) and some hormones. triglyceride can be associated with a place of talking to your doctor or However, too much cholesterol can low level of 'good' cholesterol and pharmacist. be a problem. may increase your risk of heart disease. All medicines have risks and Cholesterol is present in many foods benefits. Your doctor has weighed and is also made in your body by the In some patients, Atorvastatin is used the risks of you taking Atorvastatin liver. If your body makes too much to treat high cholesterol and high against the benefits he/she expects it cholesterol or you have too much triglycerides together. will have for you. cholesterol in your diet, then your In most people, there are no level becomes too high. If you have any concerns about symptoms of abnormal cholesterol or taking this medicine, ask your High cholesterol is more likely to triglyceride levels. Your doctor can doctor or pharmacist. occur with certain diseases or if you measure your levels with a simple have a family history of high blood test. Keep this leaflet with your cholesterol. medicine. How Atorvastatin works There are different types of You may need to read it again. cholesterol. LDL, or low-density Atorvastatin belongs to a group of lipoprotein, is the 'bad' cholesterol medicines called HMG- CoA that can block your blood vessels. reductase inhibitors. It works by HDL, or high density lipoprotein, reducing the amount of cholesterol What cholesterol is the 'good' cholesterol made by the liver. ATORVASTATIN that is thought to remove the bad Atorvastatin reduces the 'bad' is used for cholesterol from the blood vessels. cholesterol and can raise the 'good' When you have high levels of 'bad' cholesterol. Atorvastatin also helps Atorvastatin is used to lower high cholesterol in your blood, it may to protect you from a heart attack or cholesterol levels. begin to 'stick' to the inside of your stroke. Atorvastatin is also used to help blood vessels instead of being carried Ask your doctor if you have any reduce the risk of having a heart to the parts of the body where it is questions about why Atorvastatin attack or stroke in people who have needed. Over time, this can form has been prescribed for you. high blood pressure and coronary hard areas, also called plaque, on the Your doctor may have prescribed it heart disease (CHD) or who are at walls of your blood vessels, making for another reason. risk of CHD. Examples of risk it more difficult for the blood to flow. Atorvastatin is not addictive. factors for CHD include diabetes, a Sometimes, the plaque can detach history of stroke, or small blood from the vessel wall and float in the This medicine is available only with vessel disease. bloodstream; it can then reach a a doctor's prescription. smaller vessel and completely block it. This blocking of your blood ATORVASTATIN 10mg, 20mg, 40mg, 80mg film-coated tablets (Pharmacare®) 1 Before you take Before you start to take it Tell your doctor or pharmacist if you are taking any of the ATORVASTATIN Your doctor will ask you to have following: your liver function tested before you • digoxin, a medicine used to treat When you must not take it start to take Atorvastatin. some heart problems Do not take Atorvastatin if you Tell your doctor if you have • diltiazem, a medicine used to have an allergy to: allergies to any other medicines, foods, preservatives or dyes. treat angina • any medicine containing • other medicines to treat high atorvastatin Tell your doctor if you have or have had any of the following cholesterol or triglycerides • any of the ingredients listed at the medical conditions: including other brands that end of this leaflet. contain the medicine atorvastatin • liver problems Some of the symptoms of an allergic • antacids, medicines used to treat • kidney problems reaction may include: reflux or ulcers • muscle pain, tenderness or • shortness of breath • the antibiotics erythromycin, weakness from other medicines • clarithromycin, rifampicin or wheezing or difficulty breathing used to treat high cholesterol or dfusidic aci • swelling of the face, lips, tongue triglycerides • phenytoin, a medicine used to or other parts of the body • a type of stroke called a treat epilepsy (seizures) • rash, itching or hives on the skin. haemorrhagic stroke or a type of • oral contraceptives for birth Do not take Atorvastatin if you stroke called a lacunar stroke control have active liver disease. If you have had one of these • cyclosporin, a medicine used to Do not take this medicine if you strokes before, this medicine may suppress the immune system are pregnant or intend to become increase the risk of you having a pregnant. haemorrhagic stroke • some medicines used to treat some fungal infections, such as If you are a woman of child- • breathing problems. itraconazole or ketoconazole bearing age and are taking this Tell your doctor if you drink • medicine, use a proven method of alcohol regularly. protease inhibitors for the birth control to avoid pregnancy. treatment of HIV infection and/or If you have not told your doctor Hepatitis C, such as efavirenz, The medicine may affect your about any of the above, tell fosamprenavir, ritonavir and developing baby if you take it during him/her before you start taking boceprevir pregnancy. Atorvastatin. • spironolactone, a medicine used Do not breast-feed if you are to treat high blood pressure and taking this medicine. Taking other medicines certain types of swelling The active ingredient in Atorvastatin Tell your doctor or pharmacist if • vitamin B3 may pass into breast milk and affect you are taking any other your baby. medicines, including: • colchicine, a medicine used to treat a disease with painful, • all prescription medicines Do not take Atorvastatin if you swollen joints caused by uric acid are taking the antibiotic fusidic • all medicines, vitamins, herbal crystals. acid which is used to treat supplements or natural therapies Your doctor and pharmacist have infections. you buy without a prescription more information on medicines to be from a pharmacy, supermarket, Do not take this medicine after the careful with or to avoid while taking naturopath or health food shop. expiry date printed on the pack or Atorvastatin. if the packaging is torn or shows Some medicines may be affected by signs of tampering. Atorvastatin or may affect how well If it has expired or is damaged, return it works. You may need different it to your pharmacist for disposal. amounts of your medicines, or you may need to take different If you are not sure whether to start medicines. Your doctor will advise taking Atorvastatin, talk to your you. doctor. ATORVASTATIN 10mg, 20mg, 40mg, 80mg film-coated tablets (Pharmacare®) 2 Atorvastatin helps to lower your How to take levels of cholesterol, but it does not While you are taking ATORVASTATIN cure your condition. It is ATORVASTATIN important to keep taking your medicine even if you feel well. If Follow all directions given to you you stop taking Atorvastatin, your Things you must do by your doctor and pharmacist cholesterol levels may rise again. carefully. Keep all of your doctor's appointments so that your progress These directions may differ from the If you forget to take it can be checked. information contained in this leaflet. If it is less than 12 hours before Your doctor will ask you to have Your doctor will discuss with you the your next dose, skip the dose you your liver function tested from time need to be on a diet while you are missed and take your next dose to time while you are taking taking Atorvastatin. when you are meant to. Otherwise, Atorvastatin to make sure the Follow your agreed diet plan take it as soon as you remember, medicine is working and to prevent carefully. and then go back to taking your unwanted side effects. If you do not understand the tablet as you would normally. Your cholesterol and triglyceride instructions, ask your doctor or Do not take a double dose to make levels also need to be checked pharmacist for help. up for the dose that you missed. regularly while you are taking this This may increase the chance of you medicine. How much to take getting an unwanted side effect. If you become pregnant while you Your doctor will tell you how many If you are not sure what to do, talk are taking Atorvastatin, stop tablets you need to take each day. to your doctor or pharmacist. taking it and contact your doctor This may depend on your condition immediately. If you have trouble remembering and whether or not you are taking to take your tablets, ask your If you are about to be started on any other medicines. pharmacist for some hints. any new medicine, remind your The usual dose of Atorvastatin is doctor and pharmacist that you between 10-80 mg taken once a day. If you take too much are taking Atorvastatin.
Recommended publications
  • 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]
  • Atorvastatin Slows the Progression of Cardiac Remodeling in Mice with Pressure Overload and Inhibits Epidermal Growth Factor Receptor Activation
    335 Hypertens Res Vol.31 (2008) No.2 p.335-344 Original Article Atorvastatin Slows the Progression of Cardiac Remodeling in Mice with Pressure Overload and Inhibits Epidermal Growth Factor Receptor Activation Yulin LIAO1), Hui ZHAO2), Akiko OGAI1), Hisakazu KATO2), Masanori ASAKURA1), Jiyoong KIM1), Hiroshi ASANUMA1), Tetsuo MINAMINO2), Seiji TAKASHIMA2), and Masafumi KITAKAZE1) The aim of this study was to investigate whether atorvastatin inhibits epidermal growth factor receptor (EGFR) activation in cardiomyocytes in vitro and slows the progression of cardiac remodeling induced by pressure overload in mice. Either atorvastatin (5 mg/kg/day) or vehicle was orally administered to male C57BL/6J mice with transverse aortic constriction (TAC). Physiological parameters were obtained by echocardiography or left ventricular (LV) catheterization, and morphological and molecular parameters of the heart were also examined. Furthermore, cultured neonatal rat cardiomyocytes were studied to clarify the underlying mechanisms. Four weeks after TAC, atorvastatin reduced the heart/body weight and lung/body weight ratios (8.69±0.38 to 6.45±0.31 mg/g (p<0.001) and 10.89±0.68 to 6.61±0.39 mg/g (p<0.01) in TAC mice with and without atorvastatin, respectively). Decrease of LV end-diastolic pressure and the time con- stant of relaxation, increased fractional shortening, downregulation of a disintegrin and metalloproteinase (ADAM)12, ADAM17 and heparin-binding epidermal growth factor genes, and reduction of the activity of EGFR and extracellular signal–regulated kinase (ERK) were observed in the atorvastatin group. Phenyleph- rine-induced protein synthesis, phosphorylation of EGFR, and activation of ERK in neonatal rat cardiomyo- cytes were all inhibited by atorvastatin.
    [Show full text]
  • Effects of Generic Substitution on Refill Adherence to Statin Therapy: a Nationwide Population-Based Study Henrik Trusell1 and Karolina Andersson Sundell1,2*
    Trusell and Andersson Sundell BMC Health Services Research 2014, 14:626 http://www.biomedcentral.com/1472-6963/14/626 RESEARCH ARTICLE Open Access Effects of generic substitution on refill adherence to statin therapy: a nationwide population-based study Henrik Trusell1 and Karolina Andersson Sundell1,2* Abstract Background: Several countries have introduced generic substitution, but few studies have assessed its effect on refill adherence. This study aimed to analyse whether generic substitution influences refill adherence to statin treatment. Methods: Between 1 July 2006 and 30 June 2007, new users of simvastatin (n = 108,806) and atorvastatin (n = 7,464) were identified in the Swedish Prescribed Drug Register . The present study included atorvastatin users as an unexposed control group because atorvastatin was patent-protected and thus not substitutable. We assessed refill adherence using continuous measure of medication acquisition (CMA). To control for potential confounders, we used analysis of covariance (ANCOVA). Differences in CMA associated with generic substitution and generic substitution at first-time statin purchase were analysed. Results: Nine of ten simvastatin users were exposed to generic substitution during the study period, and their adherence rate was higher than that of patients without substitution [84.6% (95% CI 83.5-85.6) versus 59.9% (95% CI 58.4-61.4), p < 0.001]. CMA was higher with increasing age (60–69 years 16.7%, p < 0.0001 and 70–79 years 17.8%, p < 0.0001, compared to 18–39 years) and secondary prevention (12.8%, p < 0.0001). CMA was lower among patients who were exposed to generic substitution upon initial purchase, compared to those who were exposed to a generic substitution subsequently [80.4% (95% CI 79.4-90.9) versus 89.8% (88.7-90.9), p < 0.001].
    [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]
  • Pharmaceutical Appendix to the Harmonized Tariff Schedule
    Harmonized Tariff Schedule of the United States Basic Revision 3 (2021) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States Basic Revision 3 (2021) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known.
    [Show full text]
  • Frequently Asked Questions (Faqs) About LIPITOR and Cholesterol
    Frequently Asked Questions (FAQs) About LIPITOR and Cholesterol Below are some FAQs that you may still have after visiting LIPITOR.com. Q: What are LIPITOR tablets? A: LIPITOR is a prescription medicine that lowers the LDL-C (“bad” cholesterol) and triglycerides in your blood. It can raise your HDL-C (“good” cholesterol) as well. LIPITOR is for adults and children over aged 10 years whose cholesterol does not come down enough with exercise and a low-fat diet alone. LIPITOR can lower the risk for heart attack, stroke, certain types of heart surgery, and chest pain in patients who have heart disease or risk factors for heart disease, such as: Age, smoking, high blood pressure, low HDL-C, heart disease in the family. LIPITOR can lower the risk for heart attack or stroke in patients with diabetes and risk factors such as: Eye problems, kidney problems, smoking, or high blood pressure. LIPITOR starts to work in about 2 weeks. Q: What are the possible side effects of LIPITOR? A: LIPITOR can cause serious side effects, which only a small number of people have experienced. Your doctor can monitor you for them. These side effects usually go away if your dose is lowered or LIPITOR is stopped. These serious side effects include: Muscle problems. LIPITOR can cause serious muscle problems that can lead to kidney problems, including kidney failure. You have a higher chance for muscle problems if you are taking certain other medicines with LIPITOR. Liver problems. Your doctor should do blood tests to check your liver before you start taking LIPITOR and if you have symptoms of liver problems while you take LIPITOR.
    [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]
  • LIPITOR® (Atorvastatin Calcium) Tablets for Oral Administration Hypothyroidism, and Renal Impairment
    HIGHLIGHTS OF PRESCRIBING INFORMATION ----------------------WARNINGS AND PRECAUTIONS-----------------------­ These highlights do not include all the information needed to use Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): Risks increase LIPITOR safely and effectively. See full prescribing information for when higher doses are used concomitantly with cyclosporine, fibrates, and LIPITOR. strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, HIV protease inhibitors). Predisposing factors include advanced age (> 65), uncontrolled LIPITOR® (atorvastatin calcium) Tablets for oral administration hypothyroidism, and renal impairment. Rare cases of rhabdomyolysis with Initial U.S. Approval: 1996 acute renal failure secondary to myoglobinuria have been reported. In cases of myopathy or rhabdomyolysis, therapy should be temporarily withheld or discontinued (5.1). ----------------------------INDICATIONS AND USAGE--------------------------- LIPITOR is an inhibitor of HMG-CoA reductase (statin) indicated as an Liver enzyme abnormalities and monitoring: Persistent elevations in hepatic adjunct therapy to diet to: transaminases can occur. Monitor liver enzymes before and during treatment • Reduce the risk of MI, stroke, revascularization procedures, and angina (5.2). in patients without CHD, but with multiple risk factors (1.1). • Reduce the risk of MI and stroke in patients with type 2 diabetes without A higher incidence of hemorrhagic stroke was seen in patients without CHD CHD, but with multiple risk factors (1.1). but with stroke
    [Show full text]
  • Effects of Atorvastatin and Niacin, Alone and in Combination, On
    etabolic f M S o y l n a d n r o r Jhuma et al., J Metabolic Synd 2013, 3:1 m u o e J Journal of Metabolic Syndrome DOI: 10.4172/2167-0943.1000136 ISSN: 2167-0943 Research Article Open Access Effects of Atorvastatin and Niacin, Alone and in Combination, On Lowering Serum LDL-Cholesterol and Lipoprotein (a) in Hyperlipidemia Patients Jhuma KA1*, Giasuddin ASM2, Haq AMM3, Huque MM3 and Mahmood N4 1Department of Biochemistry, Medical College for Women & Hospital, Plot-4, Road-9, Sector-1, Uttara Model Town, Dhaka-1230, Bangladesh 2Department of Medical Laboratory Science, State College of Health Sciences & Adjunct Professor, State University of Bangladesh, Dhanmondi, Dhaka-1209, Bangladesh 3Department of Medicine, Medical College for Women & Hospital, Plot-4, Road-9, Sector-1, Uttara Model Town, Dhaka-1230, Bangladesh 4Department of Medicine, (Nephrology Unit), Medical College for Women & Hospital, Plot-4, Road-9, Sector-1, Uttara Model Town, Dhaka-1230, Bangladesh Abstract Background & objectives: Effects of statins on serum lipids in hyperlipidemia are not well defined. We compared the effects of atorvastatin and niacin, alone and combination, on lowering serum LDL-C and Lp (a) and increasing HDL-C in hyperlipidemia patients. Patients and methods: A total of 150 adult patients (Group-A) with hyperlipidemia and 100 normal adults controls (Group-B) were included in the study. The fasting blood samples were taken and serum (I°) were stored frozen until analysed for TG, TC, LDL-C, HDL-C, and Lp (a). The 50 patients (Group A1) were prescribed Atorvastatin (10 mg once daily for 3 months), 50 patients (Group A2) were prescribed Niacin (50 mg twice daily for 3 months) and 50 patients (Group A3) were prescribed combination of the two drugs with same doses for 3 months.
    [Show full text]
  • Atorvastatin Calcium)
    PRODUCT INFORMATION LIPITOR® (atorvastatin calcium) NAME OF THE MEDICINE LIPITOR atorvastatin (as calcium) 10 mg, 20 mg, 40 mg and 80 mg tablets. LIPITOR contains the active ingredient atorvastatin calcium. The structural formula of atorvastatin calcium is shown below: CH3 CH3 CH OH OH O O CH CH CH C NHC 2 - N CH2 CH2 CH2 O •Ca 2+ •3H2 O F 2 Chemical name: [R-(R*,R*)]-2-(4-fluorophenyl)-ß,-dihydroxy-5-(1-methylethyl)- 3-phenyl-4-[(phenylamino) carbonyl] -1H-pyrrole -1-heptanoic acid, calcium salt (2:1) Molecular formula: (C33H34FN2O5)2Ca.3H2O Molecular weight: 1209.42 CAS registry number: 134523-03-8. DESCRIPTION Atorvastatin calcium is a white to off-white crystalline powder that is practically insoluble in aqueous solutions of pH 4 and below. Atorvastatin calcium is very slightly soluble in distilled water, pH 7.4 phosphate buffer, and acetonitrile, slightly soluble in ethanol and freely soluble in methanol. LIPITOR tablets contain atorvastatin calcium equivalent to 10, 20, 40 and 80 mg atorvastatin. The tablets also contain the following inactive ingredients: calcium carbonate, microcrystalline cellulose, lactose, croscarmellose sodium, polysorbate 80, hydroxypropylcellulose, magnesium stearate, Opadry White YS-1-7040 and Simethicone Emulsion. Version: pfplipit10613 Supersedes: pfplipit10512 Page 1 of 20 PHARMACOLOGY Mechanism of Action Atorvastatin is a synthetic lipid-lowering agent. Atorvastatin is an inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methyl-glutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol. Triglycerides (TG) and cholesterol in the liver are incorporated into very low density lipoprotein (VLDL) and released into the plasma for delivery to peripheral tissues.
    [Show full text]
  • Efficacy and Safety of Triplet Therapy With
    Interactive! Click on any of Efficacy and Safety of Triplet Therapy With Bempedoic Acid, Ezetimibe, TAP TO RETURN these bubbles to TO KIOSK MENU jump to each and Atorvastatin in Patients With Hypercholesterolemia section Diane E. MacDougall, MS1; John Rubino, MD2; Lulu Ren Sterling, PhD1; Jeffrey C. Hanselman, MS1; Stephen J. Nicholls, MD, PhD3 Results & Methods 1Esperion Therapeutics Inc., Ann Arbor, MI; 2PMG Research of Raleigh, Raleigh, NC; Results 3Monash Cardiovascular Research Centre, Monash University, Melbourne, VIC, Australia Conclusions INTRODUCTION METHODS • Patients with hypercholesterolemia often fail to achieve sufficient cholesterol lowering, despite the use of guideline- recommended lipid-lowering therapies1-3 STUDY DESIGN AND TREATMENT • Bempedoic acid is an oral, first-in-class ATP-citrate lyase inhibitor in development for treating hypercholesterolemia4,5 • Phase 2, randomized, double-blind, placebo-controlled study – The active form of bempedoic acid (bempedoyl-CoA) inhibits ATP-citrate lyase, an enzyme upstream of • The study consisted of 2 phases (Figure 1): HMG-CoA reductase (the target of statins) in the cholesterol biosynthesis pathway – A 6-week screening/washout period during which patients – Bempedoic acid is a prodrug that is activated in the liver by very long-chain acyl-CoA synthetase 1 (ACSVL1) discontinued lipid-lowering drugs and nutritional supplements – A double-blind treatment period in which patients were – ACSVL1 expression is limited to the liver; therefore, bempedoic acid is not converted to bempedoyl-CoA in randomized 2:1 to treatment with triplet therapy (bempedoic acid skeletal muscle 180 mg + ezetimibe 10 mg + atorvastatin 20 mg) or placebo once • In phase 3 clinical trials, bempedoic acid significantly lowered low-density lipoprotein cholesterol (LDL-C) when daily for 6 weeks administered alone or as an add-on to background lipid-lowering therapy6-9 OBJECTIVE FIGURE 1.
    [Show full text]