Cardiovascular Medicine Book

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Fibric Acid

Aka: Fibric Acid, Gemfibrozil, Clofibrate, Fenofibrate, Tricor, Trilipix
  1. Efficacy
    1. Lipid effects
      1. Decreases Triglycerides (20-50%)
      2. Increases LDL Cholesterol (10-15%)
      3. Decreases VLDL Cholesterol
      4. Increases HDL Cholesterol (10-15%)
    2. Outcome effects
      1. No effect on all cause mortality
      2. NNT to prevent one coronary event: 46-125
  2. Adverse effects
    1. Gastrointestinal effects
      1. Gastrointestinal upset
      2. Abdominal Pain
      3. Higher rate of Gastrointestinal Disease
        1. Cholecystitis (increased risk by 2-3%)
        2. Appendicitis
    2. Miscellaneous
      1. Rash
      2. Renal dysfunction (rare)
      3. Myopathy (rare)
  3. Drug Interactions
    1. May potentiate effects of:
      1. Coumadin
      2. Oral Hypoglycemic Agents
  4. Contraindications
    1. Absolute
      1. Severe Hepatic or renal disease
      2. Preexisting Gallstones
    2. Relative
      1. Concurrent Statin due to Myopathy risk
        1. Exercise caution when using these together
        2. Tricor is commonly used with Statins (Gemfibrozil is higher risk)
      2. Concurrent Coumadin use
      3. Avoid as a single agent in Coronary Artery Disease
  5. Preparations
    1. Gemfibrozil (Lopid)
      1. Dose: 600 mg bid ($75/month)
    2. Fenofibrate (Tricor)
      1. Less likely to cause Rhabdomyolysis with Statin
    3. Fenofibrate (Trilipix)
      1. Rebranded version of Tricor in time for generic Fenofibrate release in 2011
    4. Clofibrate
      1. Increased mortality from malignant and GI disease
  6. References
    1. Last (2011) Am Fam Physician 84(5): 551-8
    2. Studer (2005) Arch Intern Med 165(7): 725-30
    3. Sharma (2009) Ann Intern Med 151(9):622-30

Clofibrate (C0009002)

Definition (MSH) A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Definition (CSP) fibric acid derivative used in the treatment of hyperlipoproteinemia and hypertriglyceridemia.
Definition (NCI) An aryloxyisobutyric acid derivate with antihyperlipidemic activity. Although the exact mechanism of action has not been fully characterized, clofibrate may enhance the conversion of very-low-density lipoprotein (VLDL) to low-density lipoprotein (LDL), decreasing the production of hepatic VLDL, inhibiting cholesterol production, and increasing fecal excretion of neutral sterols.
Definition (PDQ) An aryloxyisobutyric acid derivate with antihyperlipidemic activity. Although the exact mechanism of action has not been fully characterized, clofibrate may enhance the conversion of very-low-density lipoprotein (VLDL) to low-density lipoprotein (LDL), decreasing the production of hepatic VLDL, inhibiting cholesterol production, and increasing fecal excretion of neutral sterols. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42108&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42108&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C378" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D002994
SnomedCT 387439004, 77035009
English clofibrate, Chlorophenoxyisobutyrate, Ethyl, Ethyl Chlorophenoxyisobutyrate, Propanoic acid, 2-(4-chlorophenoxy)-2-methyl-, ethyl ester, 2-(4-Chlorophenoxy)-2-methylpropanoic acid ethyl ester, Ethyl 2-(4-Chlorophenoxy)-2-methylpropanoate, Ethyl p-Chlorophenoxyisobyturate, Clofibrate, CFB, clofibrate (medication), Clofibrate [Chemical/Ingredient], clofibrates, Clofibric Acid, Ethyl Ester, Clofibrate (product), Clofibrate (substance), CLOFIBRATE
Swedish Klofibrat
Czech klofibrát
Finnish Klofibraatti
Russian KLOFIBRAT, КЛОФИБРАТ
Italian Etil clorofenossi isobutirrato, Clofibrato
Croatian KLOFIBRAT
French Ester éthylique d'acide clofibrique, p-Chlorophénoxyisobutyrate d'éthyle, Clofibrate
Polish Klofibrat
Japanese クロフィブレート, クロフィブラート
Spanish clofibrato (producto), clofibrato (sustancia), clofibrato, Clofibrato
German Clofibrat
Portuguese Clofibrato
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Gemfibrozil (C0017245)

Definition (MSH) A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. These decreases occur primarily in the VLDL fraction and less frequently in the LDL fraction. Gemfibrozil increases HDL subfractions HDL2 and HDL3 as well as apolipoproteins A-I and A-II. Its mechanism of action has not been definitely established.
Definition (CSP) lipid regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol.
Definition (NCI) A fibric acid derivative with hypolipidemic effects. Gemfibrozil interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III results in subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).
Concepts Lipid (T119) , Pharmacologic Substance (T121)
MSH D015248
SnomedCT 35282000, 387189002
English Gemfibrozil, Gemfibrosil, Pentanoic acid, 5-(2,5-dimethylphenoxy)-2,2-dimethyl-, gemfibrozil, gemfibrozil (medication), gemfibrozil (Lopid), GEMFIBROZIL, Gemfibrozil [Chemical/Ingredient], gemfibrosil, Gemfibrozil product, Gemfibrozil (product), Gemfibrozil (substance)
Swedish Gemfibrozil
Czech gemfibrozil
Finnish Gemfibrotsiili
Russian GEMFIBROZIL, ГЕМФИБРОЗИЛ
Japanese ジェムフィブロジィル, ゲムフィブロジル, ゲンフィブロジル
Spanish genfibrocil (producto), gemfibrozilo (producto), genfibrocil, gemfibrozilo (sustancia), gemfibrozilo, gemfibrozil, genfibrocil (sustancia), Gemfibrozil, Gemfibrozilo
Italian Gemfibrosil, Gemfibrozil
French Gemfibrosil, Gemfibrozil
Polish Gemfibrozil
German Gemfibrozil
Portuguese Genfibrozila, Genfibrozil
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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