Active ingredient: Gemfibrozil - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antilipemic Agents
• Fribic Acid Derivatives

Dosage Forms

• Tablets
• Capsules

Brands / Synonyms

Apo-Gemfibrozil; Bolutol; Cholespid; Decrelip; Fibratol; Fibrocit; Gemfibril; Gemfibromax; Gemlipid; Gen-Fibro; Genlip; Gevilon; Hipolixan; Jezil; Lipozid; Lipur; Lopid; Novo-Gemfibrozil; Nu-Gemfibrozil

Indications

For treatment of adult patients with very high elevations of serum triglyceride levels (types IV and V hyperlipidemia) who are at risk of developing pancreatitis (inflammation of the pancreas) and who do not respond adequately to a strict diet.

Pharmacology

Gemfibrozil, a fibric acid antilipemic agent similar to clofibrate, is used to treat hyperlipoproteinemia and as a second-line therapy for type IIb hypercholesterolemia. It acts to reduce triglyceride levels, reduce VLDL levels, reduce LDL levels (moderately), and increase HDL levels (moderately).

Mechanism of Action

Gemfibrozil increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Gemfibrozil also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL.

Absorption

Well absorbed from gastrointestinal tract (within 1-2 hours).

Toxicity

Oral, mouse: LD₅₀ = 3162 mg/kg. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting.

Biotrnasformation / Drug Metabolism

Hepatic. Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and a carboxyl metabolite.

Contraindications

1. Combination therapy of LOPID with cerivastatin due to the increased risk of myopathy and rhabdomyolysis.

2. Hepatic or severe renal dysfunction, including primary biliary cirrhosis.

3. Preexisting gallbladder disease.

4. Hypersensitivity to gemfibrozil.

Drug Interactions

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Clinical Laboratory
	increased creatine	positive antinuclear
	phosphokinase	antibody
	increased bilirubin
	increased liver
	transaminases (AST
	(SGOT), ALT (SGPT)
	increased alkaline
	phophatase
Hematopoietic	anemia	thrombocytopenia
	leukopenia
	bone marrow hypoplasia
	eosinophilia
Immunologic	angioedema	anaphylaxis
	laryngeal edema	Lupus-like syndrome
	urticaria	vasculitis
Integumentary	exfoliative dermatitis	alopecia
	rash
	dermatitis
	pruritus