WordNet
- medication (trade name Lopid) used to lower the levels of triglyceride in the blood (同)Lopid
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/20 10:58:42」(JST)
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Gemfibrozil
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| Systematic (IUPAC) name |
| 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid |
| Clinical data |
| Trade names |
Lopid |
| AHFS/Drugs.com |
monograph |
| MedlinePlus |
a686002 |
| Pregnancy cat. |
Category C |
| Legal status |
By Prescription |
| Routes |
Oral |
| Pharmacokinetic data |
| Bioavailability |
Close to 100% |
| Protein binding |
95% |
| Metabolism |
Hepatic (CYP3A4) |
| Half-life |
1.5 hours |
| Excretion |
Renal 94%
Feces 6% |
| Identifiers |
| CAS number |
25812-30-0 Y |
| ATC code |
C10AB04 |
| PubChem |
CID 3463 |
| IUPHAR ligand |
3439 |
| DrugBank |
DB01241 |
| ChemSpider |
3345 Y |
| UNII |
Q8X02027X3 Y |
| KEGG |
D00334 Y |
| ChEBI |
CHEBI:5296 Y |
| ChEMBL |
CHEMBL457 Y |
| Chemical data |
| Formula |
C15H22O3 |
| Mol. mass |
250.333 g/mol |
SMILES
- O=C(O)C(C)(C)CCCOc1cc(ccc1C)C
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InChI
-
InChI=1S/C15H22O3/c1-11-6-7-12(2)13(10-11)18-9-5-8-15(3,4)14(16)17/h6-7,10H,5,8-9H2,1-4H3,(H,16,17) Y
Key:HEMJJKBWTPKOJG-UHFFFAOYSA-N Y
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| Y (what is this?) (verify) |
Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro.[citation needed]
Contents
- 1 Actions
- 2 Therapeutic effects
- 3 Nontherapeutic effects and toxicities
- 4 Indications
- 5 Contraindications and precautions
- 6 Drug Interactions
- 7 References
- 8 External links
Actions[edit]
- Is an activator of Peroxisome proliferator-activated receptor-alpha (PPARα), a nuclear receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides.[citation needed]
- Preliminary data has shown that gemfibrozil inhibits production of proinflammatory cytokines in addition to its clinically useful lipid-lowering activity, increased survival in BALB/c mice that were already ill from infection by influenza virus A/Japan/305/57 (H2N2). Gemfibrozil was administered intraperitoneally once daily from days 4 to 10 after intranasal exposure to the virus. Survival increased from 26% in vehicle-treated mice (n = 50) to 52% in mice given gemfibrozil at 60 mg/kg/day (n = 46) (P = 0.0026). If this principle translates to patients, a drug already approved for human use, albeit by a different route for another purpose, might be adapted relatively fast for use against influenza, conceivably including human infection with a derivative of the avian H5N1 strain.[1]
Therapeutic effects[edit]
- Reduce triglyceride levels[citation needed]
- Reduce very low density lipoprotein (VLDL) levels
- Modest reduction of low density lipoprotein (LDL) levels
- Moderate increase in high density lipoprotein (HDL) levels
Nontherapeutic effects and toxicities[edit]
- GI distress
- Musculoskeletal pain
- Increased incidence of gallstone
- Hypokalemia (low blood potassium)
- Increased risk of cancer
Indications[edit]
- Hyperlipidemia (Type III): Gemfibrozil is the drug of choice for therapy.
- Hypertriglyceridemia (Type IV): Gemfibrozil, though not as effective as niacin, is better tolerated.[citation needed]
Contraindications and precautions[edit]
- Gemfibrozil should not be given to these patients:[citation needed]
- Gemfibrozil should be used with caution in these higher risk categories:[citation needed]
- Biliary tract disease
- Renal dysfunction
- Pregnant women
- Obese patients
Drug Interactions[edit]
- Anticoagulants: Gemfibrozil potentiates the action of warfarin and indanedione anticoagulants.[citation needed]
- Statin drugs: Concomitant administration of fibrates (including gemfibrozil) with statin drugs increases the risk of muscle cramping, myopathy, and rhabdomyolysis.[citation needed]
References[edit]
- ^ Budd A, Alleva L, Alsharifi M, et al. Antimicrob Agents Chemother. 2007 Aug;51(8):2965-8. Epub 2007 Jun 11 PMID 17562808
External links[edit]
- DrugBank Gemfibrozil
- NIH Gemfibrozil Drug Info
- Lopid International Study
- Safety of Statins - Circulation. 2004;109:III-50 – III-57
- http://www.ihs.gov/nptc/documents/NPTC%20Lipid%20Review.pdf
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Lipid modifying agents (C10)
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|
| GI tract |
|
Cholesterol absorption inhibitors, NPC1L1
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|
|
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Bile acid sequestrants/resins (LDL)
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- Cholestyramine
- Colestipol
- Colestilan
- Colextran
- Colesevelam
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|
|
| Liver |
|
Statins (HMG-CoA reductase, LDL)
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- Simvastatin#
- Atorvastatin
- Fluvastatin
- Lovastatin
- Mevastatin
- Pitavastatin
- Pravastatin
- Rosuvastatin
- Cerivastatin‡
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|
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Niacin and derivatives (HDL and LDL)
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- Niceritrol
- Niacin
- Nicofuranose
- Aluminium nicotinate
- Nicotinyl alcohol
- Acipimox
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MTTP inhibitors (VLDL)
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- Dirlotapide
- Lomitapide
- Mitratapide
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| Blood vessels |
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Fibrates (PPAR)
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- Clofibrate‡
- Bezafibrate
- Aluminium clofibrate
- Gemfibrozil
- Fenofibrate
- Simfibrate
- Ronifibrate
- Ciprofibrate
- Etofibrate
- Clofibride
- Clinofibrate
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CETP inhibitors (HDL)
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- Anacetrapib†
- Dalcetrapib§
- Evacetrapib§
- Torcetrapib†
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| Combinations |
- Niacin/lovastatin
- Niacin/simvastatin
- Ezetimibe/simvastatin
- Ezetimibe/atorvastatin
- Niacin/laropiprant
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| Other |
- Dextrothyroxine‡
- Probucol
- Tiadenol
- Benfluorex
- Meglutol
- Omega-3-triglycerides
- Magnesium pyridoxal 5-phosphate glutamate
- Policosanol
- Lapaquistat§
- Mipomersen
- Alipogene tiparvovec
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|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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mt, k, c/g/r/p/y/i, f/h/s/l/o/e, a/u, n, m
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k, cgrp/y/i, f/h/s/l/o/e, au, n, m, epon
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m (A16/C10), i (k, c/g/r/p/y/i, f/h/s/o/e, a/u, n, m)
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UpToDate Contents
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English Journal
- Formulation of poorly water-soluble Gemfibrozil applying power ultrasound.
- Ambrus R, Naghipour Amirzadi N, Aigner Z, Szabó-Révész P.SourceDepartment of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, H-6725 Szeged, Hungary. arita@pharm.u-szeged.hu
- Ultrasonics sonochemistry.Ultrason Sonochem.2012 Mar;19(2):286-91. Epub 2011 Jul 22.
- The dissolution properties of a drug and its release from the dosage form have a basic impact on its bioavailability. Solubility problems are a major challenge for the pharmaceutical industry as concerns the development of new pharmaceutical products. Formulation problems may possibly be overcome by
- PMID 21835674
- DSC, X-ray and FTIR studies of a gemfibrozil/dimethyl-β-cyclodextrin inclusion complex produced by co-grinding.
- Aigner Z, Berkesi O, Farkas G, Szabó-Révész P.SourceDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, H-6720 Szeged, Eötvös u. 6, Hungary.
- Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2012 Jan 5;57(1):62-7. Epub 2011 Aug 30.
- The steps of formation of an inclusion complex produced by the co-grinding of gemfibrozil and dimethyl-β-cyclodextrin were investigated by differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD) and Fourier transform infrared (FTIR) spectroscopy with curve-fitting analysis. The
- PMID 21920691
Japanese Journal
- A Simple Method to Evaluate Reactivity of Acylglucuronides Optimized for Early Stage Drug Discovery
- Field Survey on the Removal of Endocrine Disrupting Chemicals and Pharmaceutical Residues in Oxidation Ponds and Constructed Wetlands in Tropical Areas
Related Links
- Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro. ...
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