Уважаемые доктора, добрый день!
У меня вопрос может не очень по теме, но что -то интересно стало, хочется разобраться.
Я на статинах с января, до этого пила Тевастор, а тут купила Розарт, прочитала внимательно инструкцию http://www.rusmedserv.com/lekarstva/rozart-10mg-90sht.html , а там в побочке, в самом конце- "Прочие: часто - боль в спине, ринофарингит;" 
Можете объяснить механизм их возникновения при лечении, как Розарт к ним причастен? И почему в инструкциях в другим розувастатинам такого нет?
Спасибо!
В американской инструкции такого нет.Вот полная его инструкция.Напишите им на сайт вопрос.Можете в переводчик кинуть.
Rosuvastatin: Drug information
Rosuvastatin: Drug information
Copyright 1978-2014 Lexicomp, Inc. All rights reserved.
(For additional information see "Rosuvastatin: Patient drug information" and see "Rosuvastatin: Pediatric drug information" )
For abbreviations and symbols that may be used in Lexicomp ( show table )
Special Alerts
HMG-CoA Reductase Inhibitors and Risk of Increased Blood Glucose Concentrations and Diabetes January 2013
Health Canada has notified healthcare professionals of updates to the product monographs of HMG-CoA reductase inhibitors (aka, “statins”) marketed in Canada regarding the risk of increased blood glucose concentrations and a small increased risk of diabetes mellitus following administration of these agents. The risk appears to be greatest in patients already at risk for diabetes (eg, patients with increased blood glucose concentration, hypertriglyceridemia, obesity, hypertension). However, Health Canada continues to acknowledge that the benefits of statin therapy far outweigh the risk of dysglycemia. It is recommended that clinicians carefully monitor the use of statins in patients at high risk of developing diabetes mellitus.
For additional information, please refer to file://healthycanadians.gc.ca/recall-alert-rappel-avis/hc-sc/2013/16949a-eng.php.
Brand Names: U.S.
Crestor®
Brand Names: Canada
Apo-Rosuvastatin;
CO Rosuvastatin;
Crestor®;
Jamp-Rosuvastatin;
Mylan-Rosuvastatin;
PMS-Rosuvastatin;
RAN™-Rosuvastatin;
Sandoz-Rosuvastatin;
Teva-Rosuvastatin
Pharmacologic Category
Antilipemic Agent, HMG-CoA Reductase Inhibitor
Dosing: Adult Note: Doses should be individualized according to the baseline LDL-cholesterol levels, the recommended goal of therapy, and patient response; adjustments should be made at intervals of 4 weeks or more.
Hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia, slowing progression of atherosclerosis: Oral:
Initial dose:
General dosing: 10 mg once daily; 20 mg once daily may be used in patients with severe hyperlipidemia (LDL >190 mg/dL) and aggressive lipid targets
Conservative dosing: Patients requiring less aggressive treatment or predisposed to myopathy (including patients of Asian descent): 5 mg once daily
Titration: After 2 weeks, may be increased by 5-10 mg once daily; dosing range: 5-40 mg daily (maximum dose: 40 mg once daily)
Note: The 40 mg dose should be reserved for patients who have not achieved goal cholesterol levels on a dose of 20 mg daily, including patients switched from another HMG-CoA reductase inhibitor.
Homozygous familial hypercholesterolemia (FH): Oral: Initial: 20 mg once daily (maximum dose: 40 mg daily)
Dosage adjustment with concomitant medications: Oral:
U.S. labeling:
Cyclosporine: Rosuvastatin dose should not exceed 5 mg once daily
Gemfibrozil: Avoid concurrent use; if unable to avoid concurrent use, initiate rosuvastatin at 5 mg once daily; dose should not exceed 10 mg once daily
Atazanavir/ritonavir or lopinavir/ritonavir: Initiate rosuvastatin at 5 mg once daily; dose should not exceed 10 mg once daily
Canadian labeling:
Cyclosporine: Concomitant use is contraindicated
Gemfibrozil: Rosuvastatin dose should not exceed 20 mg daily
Dosage adjustment for hematuria and/or persistent, unexplained proteinuria while on 40 mg daily: Reduce dose and evaluate causes.
Dosing: Pediatric
(For additional information see "Rosuvastatin: Pediatric drug information" )
Note: Doses should be individualized according to the baseline LDL-cholesterol levels, the recommended goal of therapy, and patient response; adjustments should be made at intervals of 4 weeks or more.
Heterozygous familial hypercholesterolemia (HeFH):
U.S. labeling: Children 10-17 years (females >1 year postmenarche): Oral: 5-20 mg once daily; maximum: 20 mg daily
Dosage adjustment for rosuvastatin with concomitant cyclosporine, atazanavir/ritonavir or lopinavir/ritonavir: Refer to adult dosing.
Canadian labeling: Oral: 5-10 mg once daily; maximum: 10 mg daily
Dosing: Geriatric Refer to adult dosing.
Dosing: Renal Impairment
Mild-to-moderate impairment: No dosage adjustment required.
Cl cr <30 mL/minute/1.73 m 2 : Initial: 5 mg once daily; do not exceed 10 mg once daily
Dosing: Hepatic Impairment
U.S. labeling: Active hepatic disease, including unexplained persistent transaminase elevations: Use is contraindicated.
Canadian labeling:
Active hepatic disease or unexplained persistent transaminase >3 x ULN: Use is contraindicated.
Mild-to-moderate impairment: No dosage adjustment required.
Severe impairment: Initial: 5 mg daily; do not exceed 20 mg once daily.
Dosage Forms: U.S. Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral:
Crestor®: 5 mg, 10 mg, 20 mg, 40 mg
Generic Equivalent Available: U.S. No
Administration May be administered with or without food. May be taken at any time of the day.
Use
Treatment of dyslipidemias:
Used with dietary therapy for hyperlipidemias to reduce elevations in total cholesterol (TC), LDL-C, apolipoprotein B, nonHDL-C, and triglycerides (TG) in patients with primary hypercholesterolemia (elevations of 1 or more components are present in Fredrickson type IIa, IIb, and IV hyperlipidemias); increase HDL-C; treatment of primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia); treatment of homozygous familial hypercholesterolemia (FH); to slow progression of atherosclerosis as an adjunct to diet to lower TC and LDL-C
Heterozygous familial hypercholesterolemia (HeFH): In adolescent patients (10-17 years of age, females >1 year postmenarche) with HeFH having LDL-C >190 mg/dL or LDL >160 mg/dL with positive family history of premature cardiovascular disease (CVD), or ≥2 other CVD risk factors.
Primary prevention of cardiovascular disease: To reduce the risk of stroke, myocardial infarction, or arterial revascularization procedures in patients without clinically evident coronary heart disease or lipid abnormalities but with all of the following: 1) an increased risk of cardiovascular disease based on age ≥50 years old in men and ≥60 years old in women, 2) hsCRP ≥2 mg/L, and 3) the presence of at least one additional cardiovascular disease risk factor such as hypertension, low HDL-C, smoking, or a family history of premature coronary heart disease.
Secondary prevention of cardiovascular disease: To slow progression of atherosclerosis
Medication Safety Issues
Sound-alike/look-alike issues:
Rosuvastatin may be confused with atorvaSTATin, nystatin, pitavastatin
Adverse Reactions Significant
>10%: Neuromuscular & skeletal: Myalgia (3% to 13%)
2% to 10%:
Central nervous system: Headache (6%), dizziness (4%)
Gastrointestinal: Nausea (3%), abdominal pain (2%), constipation (2%)
Hepatic: ALT increased (2%; >3 times ULN)
Neuromuscular & skeletal: Arthralgia (4% to 10%), CPK increased (3%; >10 x ULN: Children 3%), weakness (3%)
<2% (Limited to important or life-threatening): Alkaline phosphatase increased, amnesia (reversible), AST increased, bilirubin increased, blood glucose increased, cataracts, cognitive impairment (reversible), confusion (reversible), depression, diabetes mellitus (new onset), GGT increased, glycosylated hemoglobin (Hb A 1c ) increased, gynecomastia, hematuria (microscopic), hepatic failure, hepatitis, hyperglycemia, hypersensitivity reactions (including angioedema, pruritus, rash, urticaria), insomnia, jaundice, memory disturbance (reversible), memory impairment (reversible), myoglobinuria, myositis, myopathy, nightmares, pancreatitis, proteinuria (dose related), renal failure, rhabdomyolysis, thyroid function test abnormalities
Adverse reactions reported with other HMG-CoA reductase inhibitors (not necessarily reported with rosuvastatin therapy) include a hypersensitivity syndrome (symptoms may include anaphylaxis, angioedema, arthralgia, erythema multiforme, eosinophilia, hemolytic anemia, immune-mediated necrotizing myopathy (IMNM), interstitial lung disease, lupus syndrome, photosensitivity, polymyalgia rheumatica, positive ANA, purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, vasculitis)
Contraindications Hypersensitivity to rosuvastatin or any component of the formulation; active liver disease; unexplained persistent elevations of serum transaminases (>3 times ULN); pregnancy; breast-feeding
Canadian labeling: Additional contraindications (not in U.S. labeling): Concomitant administration of cyclosporine; use of 40 mg dose in Asian patients, patients with predisposing risk factors for myopathy/rhabdomyolysis (eg, hereditary muscle disorders, history of myotoxicity with other HMG-CoA reductase inhibitors, concomitant use with fibrates or niacin, severe hepatic impairment, severe renal impairment [Cl cr <30 mL/minute/1.73 m 2 ], hypothyroidism, alcohol abuse)
Warnings/Precautions
Concerns related to adverse effects:
• Diabetes mellitus: Small increases in Hb A 1c (mean: ~0.1%) and fasting blood glucose have been reported with rosuvastatin; however, the benefits of statin therapy far outweigh the risk of dysglycemia.
• Hematuria/proteinuria: Hematuria (microscopic) and proteinuria have been observed; more commonly reported in patients receiving rosuvastatin 40 mg daily. Typically, transient and not associated with a decrease in renal function. Consider dosage reduction if unexplained hematuria and proteinuria persists.
• Hepatotoxicity: Postmarketing reports of fatal and nonfatal hepatic failure are rare. If serious hepatotoxicity with clinical symptoms and/or hyperbilirubinemia or jaundice occurs during treatment, interrupt therapy. If an alternate etiology is not identified, do not restart rosuvastatin. Liver enzyme tests should be obtained at baseline and as clinically indicated; routine periodic monitoring of liver enzymes is not necessary.
• Immune-mediated necrotizing myopathy (IMNM): IMNM, an autoimmune-mediated myopathy, has been reported (rarely) with HMG-CoA reductase inhibitor therapy. IMNM presents as proximal muscle weakness with elevated CPK levels, which persists despite discontinuation of HMG-CoA reductase inhibitor therapy; additionally, muscle biopsy may show necrotizing myopathy with limited inflammation. Immunosuppressive therapy (eg, corticosteroids, azathioprine) may be used for treatment.
• Myopathy/rhabdomyolysis: Patients receiving HMG-CoA reductase inhibitors have developed rhabdomyolysis with acute renal failure and/or myopathy; patients should be monitored closely. This risk is dose-related and is increased with concurrent use of other lipid-lowering medications (fibric acid derivatives or niacin doses ≥1 g/day), other interacting drugs, other drugs associated with myopathy (eg, colchicine), age ≥65 years, female gender, uncontrolled hypothyroidism, and renal dysfunction. The manufacturer recommends temporary discontinuation for elective major surgery, acute medical or surgical conditions, or in any patient experiencing an acute or serious condition predisposing to renal failure (eg, sepsis, hypotension, trauma, uncontrolled seizures). However, based upon current evidence, HMG-CoA reductase inhibitor therapy should be continued in the perioperative period unless risk outweighs cardioprotective benefit. Use caution in patients with renal impairment, inadequately treated hypothyroidism, and those taking other drugs associated with myopathy (eg, colchicine); these patients are predisposed to myopathy. Patients should be instructed to report unexplained muscle pain, tenderness, weakness, or brown urine.
Disease-related concerns:
• Hepatic impairment and/or ethanol use: Use with caution in patients who consume large amounts of ethanol or have a history of liver disease. Use is contraindicated with active liver disease or unexplained transaminase elevations.
• Renal impairment: Dosage adjustment required in patients with a Cl cr <30 mL/minute/1.73 m 2 and not receiving hemodialysis (contraindicated in the Canadian labeling).
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
• Asian population: Increased risk of rosuvastatin-associated myopathy in certain subgroups; dosage adjustment should be considered for patients of Asian descent. Use of rosuvastatin at a dose of 40 mg/day in Asian patients is contraindicated in the Canadian labeling.
• Elderly: Use with caution in elderly patients as they are predisposed to myopathy.
Other warnings/precautions:
• Appropriate use: Secondary causes of hyperlipidemia should be ruled out prior to therapy. Rosuvastatin has not been studied when the primary lipid abnormality is chylomicron elevation (Fredrickson types I and V).
Metabolism/Transport Effects Substrate of CYP2C9 (minor), CYP3A4 (minor), SLCO1B1; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions
(For additional information: Launch Lexi-Interact™ Drug Interactions Program )
Amiodarone: May decrease the metabolism of HMG-CoA Reductase Inhibitors. Management: Dose of HMG-CoA reductase inhibitor may need to be reduced (limit simvastatin adult maximum dose to 20 mg/day, limit lovastatin adult maximum dose to 40 mg/day). Risk D: Consider therapy modification
Antacids: May decrease the serum concentration of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Bezafibrate: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors. Bezafibrate may increase the serum concentration of HMG-CoA Reductase Inhibitors. More specifically, bezafibrate may increase the serum concentration of fluvastatin Management: Monitor patients closely for myopathy with concomitant use of bezafibrate and HMG-CoA reductase inhibitors. Concomitant use is contraindicated in patients predisposed to myopathy and alternative therapy should be considered. Risk D: Consider therapy modification
Boceprevir: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy
Colchicine: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors. Colchicine may increase the serum concentration of HMG-CoA Reductase Inhibitors. Risk D: Consider therapy modification
CycloSPORINE (Systemic): May increase the serum concentration of Rosuvastatin. Management: Limit rosuvastatin to 5 mg/day in patients who are also receiving cyclosporine. Canadian labeling contraindicates concomitant use of rosuvastatin with cyclosporine. Risk D: Consider therapy modification
DAPTOmycin: HMG-CoA Reductase Inhibitors may enhance the adverse/toxic effect of DAPTOmycin. Specifically, the risk of skeletal muscle toxicity may be increased. Management: Consider temporarily stopping HMG-CoA reductase inhibitor therapy prior to daptomycin. If used together, regular (i.e., at least weekly) monitoring of CPK concentrations is recommended. Risk D: Consider therapy modification
Dronedarone: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy
Eltrombopag: May increase the serum concentration of Rosuvastatin. Management: According to eltrombopag prescribing information, consideration should be given to a preventative 50% reduction in rosuvastatin adult dose when starting this combination. Risk D: Consider therapy modification
Fenofibrate: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Fenofibric Acid: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Fusidic Acid: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Specifically, the risk for muscle toxicities, including rhabdomyolysis may be significantly increased. Management: Avoid concurrent use of HMG-CoA reductase inhibitors (statins) with fusidic acid if possible. If treatment with fusidic acid is necessary, consider temporarily stopping the statin. With any concurrent use monitor patients closely for statin toxicity. Risk X: Avoid combination
Gemfibrozil: May enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Gemfibrozil may increase the serum concentration of Rosuvastatin. Management: If possible, avoid concomitant use of rosuvastatin with gemfibrozil. If concomitant can not be avoided, limit rosuvastatin to 10 mg/day (US recommendation) or 20 mg/day (Canadian recommendation). Monitor for signs/symptoms of rhabdomyolysis. Risk X: Avoid combination
Itraconazole: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy
Lanthanum: HMG-CoA Reductase Inhibitors may decrease the serum concentration of Lanthanum. Management: Administer HMG-CoA reductase inhibitors at least two hours before or after lanthanum. Risk D: Consider therapy modification
Niacin: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Management: This is of greatest concern with niacin doses of 1 g or greater daily. Avoid simvastatin 80 mg in combination with niacin 1 g or greater in Chinese patients. Canadian labeling contraindicates use of niacin with rosuvastatin 40 mg. Risk D: Consider therapy modification
Niacinamide: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk C: Monitor therapy
Pazopanib: HMG-CoA Reductase Inhibitors may enhance the hepatotoxic effect of Pazopanib. Specifically, the risk for increased serum transaminase concentrations may be increased. Management: Simvastatin is specifically implicated in this interaction. There is a lack of data regarding the risk with other statins, but caution appears warranted with any statins. Risk C: Monitor therapy
Protease Inhibitors: May increase the serum concentration of Rosuvastatin. Management: Start with the lowest possible rosuvastatin dose and monitor for signs/symptoms of toxicity. In adult patients receiving atazanavir/ritonavir or lopinavir/ritonavir, initiate rosuvastatin at a 5 mg/day and do not exceed a dose of 10 mg/day. Risk D: Consider therapy modification
Red Yeast Rice: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors. Risk X: Avoid combination
Telaprevir: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy
Trabectedin: HMG-CoA Reductase Inhibitors may enhance the myopathic (rhabdomyolysis) effect of Trabectedin. Risk C: Monitor therapy
Vitamin K Antagonists (eg, warfarin): HMG-CoA Reductase Inhibitors may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid excessive ethanol consumption (due to potential hepatic effects).
Food: Red yeast rice contains an estimated 2.4 mg lovastatin per 600 mg rice.
Pregnancy Risk Factor X ( show table )
Pregnancy Implications Cholesterol biosynthesis may be important in fetal development. Contraindicated in pregnancy. Administer to women of childbearing potential only when conception is highly unlikely and patients have been informed of potential hazards.
Lactation Excretion in breast milk unknown/contraindicated
Dietary Considerations May be taken with or without food. Red yeast rice contains an estimated 2.4 mg lovastatin per 600 mg rice.
Pricing: U.S. (Medi-Span®)
Tablets (Crestor Oral)
5 mg (90): $581.89
10 mg (90): $581.89
20 mg (90): $581.89
40 mg (30): $193.97
Monitoring Parameters Baseline CPK (recheck CPK in any patient with symptoms suggestive of myopathy; discontinue therapy if markedly elevated); baseline liver function tests (LFTs) and repeat when clinically indicated thereafter. Patients with elevated transaminase levels should have a second (confirmatory) test and frequent monitoring until values normalize; discontinue if increase in ALT/AST is persistently >3 times ULN (NCEP, 2002).
Lipid panel (total cholesterol, HDL, LDL, triglycerides):
ATP III recommendations (NCEP, 2002): Baseline; 6-8 weeks after initiation of drug therapy; if dose increased, then at 6-8 weeks until final dose determined. Once treatment goal achieved, follow up intervals may be reduced to every 4-6 months. Lipid panel should be assessed at least annually, and preferably at each clinic visit.
Manufacturer recommendation: Upon initiation or titration, lipid panel should be analyzed within 2-4 weeks.
International Brand Names
Crestor (AR, AT, AU, BB, BE, BF, BG, BJ, BM, BR, BS, BZ, CH, CI, CL, CN, CO, CR, CZ, DK, DO, EC, EE, ET, FI, FR, GB, GH, GM, GN, GR, GT, GY, HK, HN, ID, IE, IL, IT, JM, KE, KP, LR, MA, ML, MR, MU, MW, MX, NE, NG, NI, NL, NO, NZ, PA, PE, PH, PR, PT, RU, SC, SD, SE, SG, SL, SN, SR, SV, TH, TN, TT, TW, TZ, UG, UY, VE, ZA, ZM, ZW);
Fortius (IN);
Lipichek (PH);
Rolip (PK);
Rosucol (PH);
Rosuvaz (PH);
Rovartal (PY);
Rovista (PK);
Rustor (PH);
Softan (CL);
Stator (IL);
Visacor (NZ);
Zyrova (PH)
Mechanism of Action Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism
Pharmacodynamics/Kinetics
Onset of action: Within 1 week; maximal at 4 weeks
Distribution: V d : 134 L
Protein binding: 88%
Metabolism: Hepatic (10%), via CYP2C9 (1 active metabolite identified: N-desmethyl rosuvastatin, one-sixth to one-half the HMG-CoA reductase activity of the parent compound)
Bioavailability: 20% (high first-pass extraction by liver)
Asian patients have been noted to have increased bioavailability.
Half-life elimination: 19 hours
Time to peak, plasma: 3-5 hours
Excretion: Feces (90%), primarily as unchanged drug
Автор
Тема: Доказательная медицина и эффективность лекарственных средств (Прочитано 994673 раз)