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Atorvastatin and Micronized Fenofibrate Alone and In Emerging Treatment and Technologies ORIGINAL ARTICLE Atorvastatin and Micronized Fenofibrate Alone and in Combination in Type 2 Diabetes With Combined Hyperlipidemia 1 3 VASILIOS G. ATHYROS, MD DIMOKRITOS S. DEMITRIADIS, MD ombined hyperlipidemia (CHL), a 2 ATHANASIOS A. PAPAGEORGIOU, MD ATHANASIOS G. KONTOPOULOS, MD, FACC, highly atherogenic lipid disorder 1 3 VALASIA V. ATHYROU, BSC FESC C characterized by increased LDL cho- lesterol, elevated triglycerides (TGs), and low HDL cholesterol, is not rare in pa- tients with type 2 diabetes (1). Moreover, metabolic abnormalities, such as predom- OBJECTIVE — This study evaluated the effect of a atorvastatin-fenofibrate combination on inance of small dense LDL particles (2) lipid profile, in comparison to each drug alone, in patients with type 2 diabetes and combined hyperlipidemia (CHL). and increased glycation of LDL (3), raise the atherogenic risk in these patients. Gly- RESEARCH DESIGN AND METHODS — A total of 120 consecutive patients, who cemic control appears to improve but not were free of coronary artery disease (CAD) at entry, were studied for a period of 24 weeks. These normalize these abnormalities (4). Statins patients were randomly assigned to atorvastatin (20 mg/day, n ϭ 40), micronized fenofibrate or fibrates can be used in this setting. St- (200 mg/day, n ϭ 40), or a combination of both (atorvastatin 20 mg/day plus fenofibrate 200 atins have been shown to reduce athero- mg/day, n ϭ 40). The effect of treatment on LDL cholesterol, triglycerides (TGs), HDL choles- sclerosis-related morbidity and mortality terol, apolipoprotein A-I and B, lipoprotein(a), and plasma fibrinogen (PF) was recorded. More- in patients with diabetes (5,6). On the over, the percentage of patients that reached the American Diabetes Association treatment goals and the estimated CAD risk status were calculated. other hand, fibrates are drugs that can de- crease TG concentrations and elevate RESULTS — No patient was withdrawn from the study because of side effects. The atorva- HDL cholesterol, thus reducing cardio- statin-fenofibrate combination reduced total cholesterol by 37%, LDL cholesterol by 46%, TGs vascular morbidity and mortality (7,8). by 50%, and PF by 20%, whereas it increased HDL cholesterol by 22% (P Ͻ 0.0001 for all). Recent studies (9,10) showed that statin These changes were significantly better than those of both monotherapies. Of the patients on or fibrate monotherapies can improve the drug combination, 97.5% reached the LDL cholesterol treatment goal of Ͻ100 mg/dl, 100% lipid profile in patients with type 2 diabe- reached the desirable TG levels of Ͻ200 mg/dl, and 60% reached the optimal HDL cholesterol Ͼ tes and CHL; however, these affect differ- levels of 45 mg/dl. These rates were significantly higher than those of both monotherapies. ent aspects of lipoprotein (LP) Combined treatment reduced the 10-year probability for myocardial infarction from 21.6 to 4.2%. metabolism. Hence, it is difficult to mod- ify the lipid profile of patients with type 2 CONCLUSIONS — The atorvastatin-fenofibrate combination has a highly beneficial effect diabetes and CHL using monotherapy on all lipid parameters and PF in patients with type 2 diabetes and CHL. It improved patients’ with either a statin or a fibrate, according CAD risk status significantly more than each drug alone. to the recent suggestions of the American Diabetes Association (ADA) (11). Diabetes Care 25:1198–1202, 2002 An effective therapeutic approach of CHL in nondiabetic patients is a statin- fibrate combination (12–19). This regi- men has not been widely adopted because of the concern about side effects, mainly ●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●●● myopathy, reported with the lovastatin- gemfibrozil combination (20). This has From the 1Lipid Out-patient Clinic, Aristotelian University, Hippocration Hospital, Thessaloniki, Greece; the 2Second Propedeutic Department of Internal Medicine, Aristotelian University, Hippocration Hospital not been confirmed by studies using other Thessaloniki, Greece; and the 3Division of Cardiology, Aristotelian University, Hippocration Hospital, Thes- statin-fibrate combinations (12–19). The saloniki, Greece. recently reported problems with cerivas- Address correspondence and reprint requests to Vasilios G. Athyros, MD, 15 Marmara St., Thessaloniki, tatin, when combined with gemfibrozil, 551 32, Greece. E-mail: [email protected]. Received for publication 10 November 2001 and accepted in revised form 2 March 2002. seem to be related mainly to the toxicity of Abbreviations: ADA, American Diabetes Association; apo, apolipoprotein; BIP, Bezafibrate Infarction cerivastatin, because most deaths due to Prevention; CAD, coronary artery disease; CARDS, Collaborative Atorvastatin Diabetes Study; CHL, com- myopathy-rhabdomyolysis reported in bined hyperlipidemia; CK, creatine kinase; Lp, lipoprotein; FIELD, Fenofibrate Intervention and Event the U.S. were associated with mono- Lowering in Diabetes; PF, plasma fibrinogen; 4S, Scandinavian Simvastatin Survival Study; TC, total cho- lesterol; TG, triglyceride; VA-HIT, Veterans Affairs High-Density Lipoprotein Intervention Trial. therapy rather than with combination A table elsewhere in this issue shows conventional and Syste`me International (SI) units and conversion therapy. factors for many substances. The present open-label prospective 1198 DIABETES CARE, VOLUME 25, NUMBER 7, JULY 2002 Athyros and Associates Table 1—Demographic characteristics and baseline values of measured parameters of the Statistics patients with type 2 diabetes and combined hyperlipidemia in the three treatment groups Results are reported as the means Ϯ SD. ANOVA, with 95% CIs, was used to com- Atorvastatin Fenofibrate Combination pare values within and between the treat- group group group ment groups. Differences were considered to be significant at P Ͻ 0.05. Mean per- n 40 40 40 cent changes of the LP and apo values Sex (M/F) 23/17 22/18 23/17 were also calculated. For all forms of sta- Age (years) 57 (44–67) 58 (48–69) 58 (50–68) tistical analysis, SPSS version 8.0 (SPSS, Hypoglycemic treatment (oral/insulin) 16/24 18/22 17/23 Chicago, IL) was used. Ϯ Ϯ Ϯ HbA1c (%) 8.1 0.2 8.0 0.3 8.1 0.2 Duration of diabetes (years) 8.6 Ϯ 1.6 8.9 Ϯ 1.8 8.5 Ϯ 1.6 RESULTS — All 120 patients con- Data are n, median (range), or means Ϯ 1 SD. cluded the study: 68 men and 52 women, with an age range of 44–69 years (median 58). At baseline, there were no significant randomized parallel study was under- combination of both (atorvastatin 20 mg/ differences in the demographic character- taken to investigate the hypothesis that day plus micronized fenofibrate 200 mg/ istics of the three treatment groups (Table combination therapy with atorvastatin day, n ϭ 40). Lipid profile assessment as 1). and micronized fenofibrate will be more well as physical and laboratory investiga- effective than each drug alone in tackling tion for drug-induced adverse effects Adverse effects multiple lipid coronary artery disease were performed every month. Hypogly- No significant adverse events were re- (CAD) risk factors in patients with type 2 cemic or other concurrent treatments re- corded. There was a nonsignificant in- diabetes and CHL. mained unchanged throughout the study. crease in serum transaminase values in patients on combination treatment. These RESEARCH DESIGN AND remained under the threefold level of the METHODS — The study included Assessments upper normal limit. No patient presented 120 consecutive patients with type 2 dia- After an overnight fast, TC, TG, and uric myalgia or creatine kinase (CK) levels Ͼ betes and CHL, who were free of CAD at acid were assessed by an Olympus AU 10-fold from pretreatment values. CK baseline, with fairly adequate glycemic 560 autoanalyzer, using respective re- was increased with combination therapy control. The inclusion criteria were no agents (Olympus Diagnostica, Clare, Ire- at a higher level than with both mono- previous hypolipidemic treatment, HbA1c therapies, but it remained within the nor- Ͻ land). LDL cholesterol was calculated by 8.5%, and laboratory findings of CHL. the Friedewald formula (in mg/dl) [LDL mal range. No patient was withdrawn CHL was defined as total cholesterol (TC) cholesterol ϭ TC Ϫ (TG/5 ϩ HDL cho- from the study because of side effects. Ͼ220 mg/dl (5.7 mmol/l), LDL choles- Ͼ lesterol)]. Apo B and A-I values were as- terol 130 mg/dl (3.4 mmol/l), TG from sessed by the immunoprecipitin method Glycemic control and lipid 200 mg/dl (2.3 mmol/l) to 399 mg/dl (4.5 parameters with the Technicon RA-1000 autoana- mmol/l), HDL cholesterol Ͻ40 mg/dl HbA remained unchanged throughout lyzer (Technicon-Swords, Dublin, Ire- 1c (1.04 mmol/l), and apolipoprotein (apo) the study in all groups. Combined treat- land), using the apo B and apo A-I B Ͼ150 mg/dl. Patients were on the Na- ment had a beneficial effect on all lipid reagents, respectively (Incstar, Stillwater, tional Cholesterol Expert Panel step 2 hy- parameters. It reduced TC and LDL cho- polipidemic diet for 6 weeks, during MN). Lp(a) levels were measured using a lesterol significantly more than atorvasta- which time they received a placebo tablet monoclonal anti–Lp(a) antibody tech- tin, whereas it had a better effect on TG daily. After that, if they still met the inclu- nique and enzyme-linked immunoassay and HDL cholesterol than micronized fe- sion criteria, they continued participating (Terumo Medical, Elkron, MD). Plasma nofibrate (Table 2). Lp(a) levels were not in the study. Fertile women were ex- fibrinogen (PF) was assessed with the affected by all three regimens. cluded. In all patients, normal liver and Clauss method, using the fibrin titer test renal function was established. The study Fibrindex (Ortho Diagnostic, Raritan, PF and uric acid protocol received ethical approval, and NJ). Atorvastatin had a neutral effect on PF informed consent was obtained by all par- levels. Fenofibrate and drug combination ticipants before enrolment.
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