Critical appraisal of the role of pitavastatin in treating dyslipidemias and achieving lipid goals.
Pitavastatin is a potent HMG-CoA reductase inhibitor and efficient hepatocyte low-density lipoprotein cholesterol (LDL-C) receptor inducer, producing robust reduction of the serum LDL-C levels, even at a low dose. Pitavastatin and its lactone form are minimally metabolized by CYP enzymes, and are therefore associated with minimal drug-drug interactions (DDIs). Pitavastatin 2 to 4 mg has potent LDL-C-reducing activity, equivalent to that of atorvastatin 10 to 20 mg; several clinical trials have revealed consistently superior high-density lipoprotein cholesterol (HDL-C) elevating activity of pitavastatin than that of atorvastatin. Pitavastatin-induced HDL-C elevation has been shown to be sustained, even incremental, in long-term clinical trials. Pitavastatin was as well-tolerated as atorvastatin or simvastatin in double-blind randomized clinical trials. Two-year long-term safety and effectiveness of pitavastain has been confirmed in a large-scale, prospective post-marketing surveillance. The safety and efficacy profile of pitavastatin is favorable for the treatment of dyslipidemia, especially in metabolic syndrome patients. In addition to control of LDL-C, adequate control of triglyceride (TG) and HDL-C, hypertension and hyperglycemia is also necessary in metabolic syndrome patients. Pitavastatin produces adequate control of LDL-C and TG, along with potent and incremental HDL-C elevation, with a low frequency of DDIs.
Saito
Yasushi
Y
Chiba University, Chiba, Japan. ysaito@office.chiba-u.jp
D000818:Animals; D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D004347:Drug Interactions; D050171:Dyslipidemias / Q000097:blood / Q000188:drug therapy*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D008055:Lipids / Q000097:blood*; D008958:Models, Molecular; D015394:Molecular Structure; D011804:Quinolines / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013329:Structure-Activity Relationship; D016896:Treatment Outcome; D014280:Triglycerides / Q000097:blood
D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008055:Lipids; D011804:Quinolines; D014280:Triglycerides; C108475:pitavastatin