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Gemfibromax

Gemfibromax - General Information

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. Gemfibromax increases HDL subfractions HDL2 and HDL3 as well as apolipoproteins A-I and A-II. Its mechanism of action has not been definitely established. [PubChem]

 

Pharmacology of Gemfibromax

Gemfibromax, 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).

 

Gemfibromax for patients

Gemfibrozil is used to lower high triglyceride and cholesterol levels. Notify your physician if you are pregnant or nursing. Gemfibrozil should be taken 30 minutes before the morning and evening meals. This medication may cause dizziness or blurred vision; use caution while driving or operating hazardous machinery. Gemfibrozil may cause an increase in blood sugar. If you have diabetes mellitus, carefully monitor blood sugar levels. Notify your physician if you develop severe stomach pain, muscle pain or weakness, or unexplained fever.

 

Gemfibromax Interactions

)

 
 Clinical Laboratory
 

increased creatine

positive antinuclear

 

phosphokinase

antibody

 

increased bilirubin

 
 

increased liver

 
 

transaminases (AST

 
 

(SGOT), ALT (SGPT)

 
 

increased alkaline

 
 

phophatase

 
 Hematopoietic

anemia

   
 

bone marrow hypoplasia

 
 

eosinophilia

 
 Immunologic

angioedema

anaphylaxis

 

laryngeal edema

Lupus-like syndrome

 

urticaria

vasculitis

 Integumentary

exfoliative dermatitis

alopecia

 

rash

 
 

dermatitis

 
 

pruritus

 

 

Gemfibromax 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.

 

Additional information about Gemfibromax

Gemfibromax Indication: 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.
Mechanism Of Action: Gemfibromax 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. Gemfibromax also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL.
Drug Interactions: Anisindione Gemfibromax increases the anticoagulant effect
Dicumarol Gemfibromax increases the anticoagulant effect
Acenocoumarol Gemfibromax increases the anticoagulant effect
Warfarin Gemfibromax increases the anticoagulant effect
Atorvastatin Increased risk of myopathy/rhabdomyolysis
Cerivastatin Increased risk of myopathy/rhabdomyolysis
Fluvastatin Increased risk of myopathy/rhabdomyolysis
Lovastatin Increased risk of myopathy/rhabdomyolysis
Pioglitazone Increases the effect and toxicity of rosiglitazone/pioglitazone
Rosiglitazone Increases the effect and toxicity of rosiglitazone/pioglitazone
Pravastatin Increased risk of myopathy/rhabdomyolysis
Simvastatin Increased risk of myopathy/rhabdomyolysis
Repaglinide Increases the effect and toxicity of repaglinide
Rosuvastatin Rosuvastatin possibly increases the effect of the fibrate
Ursodeoxycholic acid The fibric acid derivative decreases the effect of ursodiol
Food Interactions: Take 30 minutes before meals.
Generic Name: Gemfibrozil
Synonyms: Not Available
Drug Category: Antilipemic Agents; Fribic Acid Derivatives
Drug Type: Small Molecule; Approved

Other Brand Names containing Gemfibrozil: Apo-Gemfibrozil; Bolutol; Cholespid; Decrelip; Fibratol; Fibrocit; Gemfibril; Gemfibromax; Gemlipid; Gen-Fibro; Genlip; Gevilon; Hipolixan; Jezil; Lipozid; Lipur; Lopid; Novo-Gemfibrozil; Nu-Gemfibrozil;
Absorption: Well absorbed from gastrointestinal tract (within 1-2 hours).
Toxicity (Overdose): Oral, mouse: LD50 = 3162 mg/kg. Symptoms of overdose include abdominal cramps, diarrhea, joint and muscle pain, nausea, and vomiting.
Protein Binding: 95%
Biotransformation: Hepatic. Gemfibrozil mainly undergoes oxidation of a ring methyl group to successively form a hydroxymethyl and a carboxyl metabolite.
Half Life: 1.5 hours
Dosage Forms of Gemfibromax: Tablet Oral
Capsule Oral
Chemical IUPAC Name: 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid
Chemical Formula: C15H22O3
Gemfibrozil on Wikipedia: https://en.wikipedia.org/wiki/Gemfibrozil
Organisms Affected: Humans and other mammals