Statins

Statins Definition Statins, also known as HMG-CoA reductase inhibitors or CSE inhibitors for short, are the most important lipid-lowering drugs with a proven improvement in prognosis. Statins are effective LDL cholesterol-lowering agents. Among other things, they reduce the risk of heart attack and overall mortality and are recommended for all diseases associated with atherosclerosis. Definition Pharmacodynamics (Effect) concept only! not complete and not final!HMG-CoA reductase inhibitors Most important lipid-lowering agents with proven improvement in prognosis. Reduction of LDL by 30-40%, of HDL by 6-10%, of TG by 10-20%. Many endpoint studies, especially on pravastatin and simvastatin (40 mg each) other preparations not as well investigated, reduce the risk of further serious MI and stroke events in high-risk patients and reduce mortality after MI dose effect)Pronounced hepatic "first-pass" effectLDL decrease is dose-dependentMetabolization via cytochrome P450 (blockade of CYP3A4 by other drugs leads to a considerable increase in the concentration of the CSE inhibitor (atorvastatin, lovastin, simvastatin) with an increased risk of myotoxic ADRs. Fluvastatin is metabolized via CYP 2C9, paravastatin and rosuvastatin have no significant cytochrome P450 metabolism. (Atorvastatin 20 mg more effective for LDL-C reduction than pravastatin or simvastatin 40 mg; better risk reduction? other statins?)(Approval for treatment of hypercholesterolemia and also approval for primary and secondary prevention of cardiovascular events?)(head to head comparisons? - Comparability studies (patient population, dosage, etc.) - would go too farClassification by the Drug Commission of the German Medical Association as 'in principle' equivalent (differences exist, pleiotropic effects, presumably no arbitrary interchangeability, binding standards for comparability?)PROVE-IT study (40 mg pravastatin vs. 80 mg atorvastatin) in MI shows better risk reduction for 80 mg atorvastatin treat to target study comparing 80 mg atorvastatin with 10 mg atorvastatin after MI dose effect) is only concept for me personally key points, no final formulation and also not complete! Pharmacokinetics this was also only a concept, not definitive!Lovastatin isolated from fermentation of Aspergillus terreus; simvastatin and pravastatin closely related to lovastatin other active ingredients are produced fully synthetically. (Lovastatin and simvastatin lactones or cyclic esters, prodrug hydrolyzed to active ingredient) hydrophilic and lipophilic active ingredients; pravaastatin and rosuvastatin lipophilic. The following half-lives (HWZ) and LDL reductions result for the individual preparations: Simvastatin: half-life: 3 hours; max. possible LDL reduction dose-dependent: 40 to 45 % Lovastatin: HWL: 1.1 hours; max. possible LDL reduction dose-dependent: 40 to 45 % Pravastatin: HWL: 1.8 hours; max. possible LDL reduction dose-dependent: 30 to 40 % Fluvastatin: HWL: 3 hours; max. possible LDL reduction dose-dependent: 30 to 44 % Atorvastatin: HWL: 14 hours; max. possible LDL reduction dose-dependent: 50 to 55 % Rosuvastatin: HWL: 20 hours; max. possible LDL reduction dose-dependent: 56 to 60 % Pitavastatin: HWL: 5.7-8.9 hours; max. possible LDL reduction dose-dependent: 33 to 54 % Indication First-choice drug for hypercholesterolemia or hyperlipidemia with predominant hypercholesterolemia. Pregnancy/nursing period Dosage and method of use Undesirable effects Headache (frequent)Gastrointestinal complaints (frequent)Increase in transaminases (0.5-2%): Therapy stop at >3 times the normCK increase: still tolerable up to 4 times the norm. Muscle pain: reversible after discontinuation of the drug within 2-4 days (CK determination, exclude other causes).Rhabdomyolysis (very rare) at high CK risk of rhabdomyolysis, myoglobilinemia and acute renal failure. Interactions Contraindication Hypersensitivityliver diseasesmuscle diseasesPregnancy, lactation, caution in childrenRosuvastatin: Combination with Ciclosporin! Preparations Atorvastatin (Sortis®) 10 mg, 20 mg, 40 mg, 80 mgSimvastatin (Zocor®) 5 mg, 10 mg, 20 mg, 40 mgPravastatin (generics) 10 mg, 20 mg, 40 mgRosuvastatin (Crestor®) 5 mg, 10 mg, 20 mg, 40 mgLovastatin 10 mg, 20 mg, 40 mg, 80 mgFluvastatin (generics) 20 mg, 40 mg, 80 mgPitavastatin (Livazo®) 1 mg, 2 mg, 4 mgNote: All products are also available as generics. In addition, there are numerous combination products (ezetimibe) in different concentrations as generics.

Statins

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