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41 ROSUVASTATIN ACCEPTABILITY, EFFICACY, AND SAFETY IN HYPERCHOLESTEROLEMIC PATIENTS UNABLE TO TOLERATE OTHER STATINS.
  1. Q. Khalil,
  2. M. Winiarska,
  3. M. Agloria,
  4. J. Munjal,
  5. M. Haque,
  6. D. Aregawi,
  7. P. Wang,
  8. C. J. Glueck
  1. Cholesterol Center, Jewish Hospital, Cincinnati, OH

Abstract

Statins as a class are well tolerated. We assessed acceptability, efficacy, and safety of rosuvastatin in 57 euthyroid patients with primary high LDL cholesterol (LDLC) who, serially, could not tolerate most other statins or cholesterol-lowering drugs, primarily because of myocitis. Of the 57 patients, 44 could not tolerate atorvastatin, 27 simvastatin, 15 pravastatin, 7 fluvastatin, 2 lovastatin, 1 Vytorin, 10 WelChol, 5 Zetia, 2 TriCor, and 2 Niaspan. Rosuvastatin (5 mg/day)-diet was given to 24 patients (3 men, 21 women, 21 white, 3 black, 3 type 2 diabetics, mean ± SD age 61 ± 9 years, BMI 31.7 ± 4.2, LDLC 179 ± 32 mg/dL). On rosuvastatin 5 mg-diet for a median of 5 months, weight fell 3.0 ± 7.7 lb (p = .016), LDLC fell 76 ± 35 mg/dL (p < .0001) to 103 ± 31 mg/dL, with median percent change -47%. Adjusted for changes in body weight, decrements in LDLC remained significant, LS mean ± SE -75 ± 8 mg/dL, p < .0001. None of the 24 patients discontinued the 5 mg rosuvastatin, muscle symptoms were minor to absent, and there were no untoward changes in liver function tests ($ 3 times the laboratory upper normal limit), or in CPK ($ 10 times the laboratory upper normal limit). Rosuvastatin (10 mg/day) was given to 33 patients, 16 men, 17 women, 31 white, 1 black, 1 other, 9 smokers, 4 type 2 diabetics, mean ± SD age 59 ± 10 years, BMI 31.1 ± 5.2, and LDLC 178 ± 53 mg/dL. On therapy for a median of 11 months, body weight fell 3.1 ± 6.8 lb (p = .014), LDLC fell 80 ± 49 mg/dL (p < .0001) to 96 ± 38 mg/dL, median percent change -48%. Adjusted for body weight change, decrements in LDLC remained significant, LS mean ± SE -82 ± 11 mg/dL, p < .0001. None of the 33 patients discontinued the 10 mg rosuvastatin, muscle symptoms were minor to absent, and there were no untoward changes in liver function tests ($ 3 times the laboratory upper normal limit), or in CPK ($ 10 times the laboratory upper normal limit). Since rosuvastatin is not metabolized by the 3A4 isoenzyme of the cytochrome P450 enzyme system and is < 10% metabolized by the 2C9 isoenzyme, we speculate that its acceptability, efficacy, and safety in hypercholesterolemic patients unable to tolerate other statins are related to reduced interactions with other drugs known to inhibit CYP 450 enzymes. By contrast, atorvastatin, lovastatin, and simvastatin are metabolized through the 3A4 pathway and fluvastatin through 2C9, common pathways for many other drugs, facilitating drug-drug interactions, which may be expressed clinically as muscle symptoms, leading to discontinuance of the statin. Rosuvastatin's LDLC lowering potency often facilitates reaching LDLC goals by use of low doses, 5 or 10 mg/day.

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