Gemfibrozil

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Gemfibrozil
Systematic (IUPAC) name
5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid
Identifiers
CAS number	25812-30-0
ATC code	C10AB04
PubChem	3463
DrugBank	APRD00293
Chemical data
Formula	C15H22O3
Mol. mass	250.333 g/mol
Pharmacokinetic data
Bioavailability	Close to 100%
Protein binding	95%
Metabolism	Hepatic (CYP3A4)
Half life	1.5 hours
Excretion	Renal 94% Feces 6%
Therapeutic considerations
Pregnancy cat.	Category C
Legal status	By Prescription
Routes	Oral

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.

Contents 1 Actions 2 Therapeutic effects 3 Nontherapeutic effects and toxicities 4 Indications 5 Contraindications and Precautions 6 Drug Interactions 7 External links

[edit] Actions

• Increases activity of Peroxisome proliferator-activated receptor-alpha (PPARα), a receptor which is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increases synthesis of lipoprotein lipase therefore increasing clearance of triglycerides.

[edit] Therapeutic effects

• Reduce triglyceride levels
• Reduce Very low density lipoprotein (VLDL) levels
• Modest reduction of Low density lipoprotein (LDL) levels
• Moderate increase in High density lipoprotein (HDL) levels

[edit] Nontherapeutic effects and toxicities

• GI distress
• Musculoskeletal pain
• Increased incidence of gallstones
• Hypokalemia
• Increased risk of cancer[1]

[edit] Indications

• Hyperlipidemia (Type III): Gemfibrozil is the drug of choice for therapy.
• Hypertriglyceridemia (Type IV): Gemfibrozil, though not as effective as niacin, is better tolerated.

[edit] Contraindications and Precautions

• Gemfibrozil should not be given to these patients:
  • Hepatic dysfunction
  • Renal dysfunction

• Gemfibrozil should be used with caution in these higher risk categories:
  • Biliary tract disease
  • pregnant women
  • obese patients
  • Native Americans

[edit] Drug Interactions

• Anticoagulants: Gemfibrozil potentiates the action of coumadin and indanedione anticoagulants.
• Statin drugs: Concomidant administration of fibrates (including gemfibrozil) with statin drugs increases the risk of muscle cramping, myopathy, and rhabdomyolysis.

[edit] External links

• DrugBank Gemfibrozil
• NIH Gemfibrozil Drug Info}
• Lopid International Study
• Safety of Statins - Circulation. 2004;109:III-50 – III-57

v • d • e Lipid modifying agents (C10) Statins Atorvastatin • Cerivastatin‡ • Fluvastatin • Lovastatin • Mevastatin • Pitavastatin • Pravastatin • Rosuvastatin • Simvastatin Fibrates Clofibrate‡ • Bezafibrate • Aluminium clofibrate • Gemfibrozil • Fenofibrate • Simfibrate • Ronifibrate • Ciprofibrate • Etofibrate • Clofibride Bile acid sequestrants Colestyramine • Colestipol • Colextran • Colesevelam Niacin and derivatives Niceritrol • Niacin • Nicofuranose• Aluminium nicotinate• Nicotinyl alcohol • Acipimox CETP inhibitors Anacetrapib† • Torcetrapib§ Combinations Niacin/lovastatin • Niacin/simvastatin • Ezetimibe/simvastatin Other Dextrothyroxine • Probucol • Tiadenol • Benfluorex • Meglutol • Omega-3-triglycerides • Magnesium pyridoxal 5-phosphate glutamate • Policosanol • Ezetimibe • Laropiprant†, Lapaquistat§ †Undergoing clinical trials. ‡Withdrawn from market. §Development terminated.