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Gemfibrozil
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| Systematic (IUPAC) name | |
| 5-(2,5-dimethylphenoxy)-2,2-dimethyl-pentanoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | C10 |
| PubChem | |
| DrugBank | |
| 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.
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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.
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
Nontherapeutic effects and toxicities
- GI distress
- Musculoskeletal pain
- Increased incidence of gallstones
- Hypokalemia
- Increased risk of cancer[1]
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.
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
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.
External links
- DrugBank Gemfibrozil
- NIH Gemfibrozil Drug Info}
- Lopid International Study
- Safety of Statins - Circulation. 2004;109:III-50 – III-57
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Wikipedia content modification information:
- This page was last modified on 11 June 2008, at 16:32.
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