Brand Name :
lopid
Synonyms :
gemfibrozil
Class :
Fibric acid agents
Dosage Forms & Strengths
Tablet
600mg
600mg orally every 12 hours
Administer 30 mins before morning and night meals
Safety and efficacy not established
Refer adult dosing
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of OATP1/1B3 substrates
may diminish the absorption of fibric acid derivatives
may enhance the serum concentration of OATP1/1B3 substrates
may increase the nephrotoxic effect of fibric acid derivatives
may enhance the serum concentration of OATP1/1B3 substrates
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the anticoagulant effect of fibric acid derivatives
may enhance the anticoagulant effect of fibric acid derivatives
may enhance the anticoagulant effect of fibric acid derivatives
may enhance the anticoagulant effect of fibric acid derivatives
may enhance the anticoagulant effect of fibric acid derivatives
when both drugs are combined, there may be an increased risk of adverse effects
may increase the toxicity of each other
may increase the toxicity of each other
may enhance the myopathic (rhabdomyolysis) effect
may enhance the serum concentration of OATP1/1B3 substrates
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
it increases the toxicity of fibric derivatives
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
may enhance the serum concentration of CYP2C8 inhibitors
May enhance the serum concentration of montelukast
May enhance the serum concentration of zafirlukast
may increase the hypoglycemic effect of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
fibric acid derivatives increase the effect of hypoglycemia of sulfonylureas
it increases the effect of loperamide via decreasing metabolism
fibric acid derivatives increase the effect of anticoagulation of vitamin K antagonists
fibric acid derivatives increase the effect of anticoagulation of vitamin K antagonists
fibric acid derivatives increase the effect of anticoagulation of vitamin K antagonists
fibric acid derivatives increase the effect of anticoagulation of vitamin K antagonists
fibric acid derivatives increase the effect of anticoagulation of vitamin K antagonists
Mechanism of action
It is a lipid-lowering agent used to treat hyperlipidaemia and primary dysbetalipoproteinemia. The mechanism of action of gemfibrozil is the inhibition of the synthesis of very low-density lipoproteins (VLDL) in the liver, leading to an increase in the elimination of VLDL and decreased plasma levels of triglycerides.
Spectrum
The spectrum of activity of gemfibrozil is mainly limited to decreasing triglycerides and increasing high-density lipoprotein (HDL) levels, and a lesser extent decreasing low-density lipoprotein (LDL) levels. It is ineffective in lowering cholesterol levels in patients with homozygous familial hypercholesterolemia.
Frequency defined:
>10%
Dyspepsia
1-10%
Atrial fibrillation
Fatigue
Eczema
Vertigo
Headache
Abdominal pain
Diarrhea
Rash
constipation
<1%
Rhabdomyolysis
Cholelithiasis
Hypokalemia
Myopathy
Taste disturbance
Flatulence
Myalgia
Acute appendicitis
Angioedema
Eosinophilia
Synovitis
Xerostomia
Rash
Contraindications
Caution
Pregnancy consideration: It should be used with caution in pregnant women, as its safety in these populations has not been established
Lactation: Excretion of the drug in human breast milk is unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology
It has multiple mechanisms of action to decrease lipid levels in the blood. It inhibits peripheral lipolysis, decreases the hepatic uptake of free fatty acids, which may, in turn, inhibit the secretion of very low-density lipoprotein (VLDL), and may also increase high-density lipoprotein (HDL) cholesterol, although the mechanism for this increase is not fully understood.
Pharmacodynamics
The main pharmacodynamic effect of gemfibrozil is to decrease levels of triglycerides and very low-density lipoprotein (VLDL) in the blood, improving the lipid profile. This is achieved by inhibiting the synthesis of VLDL in the liver, decreasing the hepatic uptake of free fatty acids, and increasing the elimination of VLDL.
In addition, gemfibrozil may increase high-density lipoprotein (HDL) levels, although the exact mechanism for this increase still needs to be fully understood.
Pharmacokinetics
Absorption: It is well absorbed from the gastrointestinal tract, with a peak serum time of 1-2 hours after oral administration.
Distribution: It is highly protein bound (99%) and distributes into tissues, including the liver and fat.
Metabolism: It undergoes extensive enterohepatic circulation, which is metabolized in the liver and reabsorbed in the small intestine.
Excretion/Elimination: The half-life of gemfibrozil is approximately 1.5 hours. It is excreted primarily in the urine (70%) and to a lesser extent in the feces (6%)
Administration
It is administered orally in the form of a tablet. The recommended adult dose is 600 mg twice daily, taken with meals.
It is important to note that gemfibrozil should not be crushed, chewed, or broken before swallowing, as this may lead to an increased risk of adverse events.
In addition, gemfibrozil should be used with a diet low in saturated fat and cholesterol and a program of regular exercise to optimize lipid-lowering efficacy.
The dose of gemfibrozil may need to be adjusted based on individual patient factors, such as age, liver or kidney function, and other medical conditions or medications.
Patient information leaflet
Generic Name: gemfibrozil
Pronounced: [ jem-FYE-broe-zil ]
Why do we use gemfibrozil?
It is used in the treatment of hyperlipidemia and primary dysbetalipoproteinemia