Gelicon Capsule 300 mg

Gelicon Capsule 300 mg Uses, Dosage, Side Effects, Food Interaction and all others data.

Gelicon Capsule 300 mg is an anti-lipemic agent. Gelicon Capsule 300 mg decreases serum triglycerides in healthy individuals and patients with hyper-triglyceridemia. It decreases very low-density lipoprotein (VLDL)- triglyceride concentration and to a lesser extent, LDL triglyceride concentration. HDL-triglyceride is usually decreased slightly. Gelicon Capsule 300 mg usually increases the HDL-cholesterol fraction in healthy individuals and patients with hyperlipoproteinemia, an action that may be beneficial in slowing the progression of atherosclerosis and in reducing the risk of coronary heart disease.

Gelicon Capsule 300 mg also inhibits synthesis of VLDL carrier apolipoprotein B, leading to a decrease in VLDL production. How gemfibrozil raises HDL concentration is not known. Gelicon Capsule 300 mg inhibits lipolysis of fat in adipose tissue and decreases the hepatic uptake of plasma free fatty acids, thereby reducing hepatic triglyceride production.

Gelicon Capsule 300 mg alters lipid metabolism to treat patients with hyperlipidemia. The duration of action requires twice daily dosing as the mean residence time of gemfibrozil is up to 9.6h in patients with chronic renal failure. Gelicon Capsule 300 mg has a wide therapeutic index as trials with twice the standard dose were not associated with severe side effects. Patients taking gemfibrozil may be at an increased risk of developing cholelithiasis and cholecystitis, as seen in patients taking clofibrate.

Gelicon Capsule 300 mg
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Gelicon Capsule 300 mg
Availability	Prescription only
Generic	Gemfibrozil
Gemfibrozil Other Names	Gemfibrozil, Gemfibrozilo, Gemfibrozilum
Related Drugs	Zetia, Praluent, Repatha, atorvastatin, simvastatin, rosuvastatin, Lipitor, fenofibrate, ezetimibe, Crestor
Weight	300 mg
Type	Capsule
Formula	C₁₅H₂₂O₃
Weight	Average: 250.3334 Monoisotopic: 250.15689457
Protein binding	Gemfibrozil is 99% protein bound. It is 98.6% bound to serum albumin, 0.8% bound to erythrocytes, and 0.8% unbound. There is negligible binding to alpha-1-acid glycoprotein.
Groups	Approved
Therapeutic Class	Dyslipidaemic Agents
Manufacturer	Eskayef Pharmaceuticals Ltd.
Available Country	Bangladesh
Last Updated:	October 19, 2023 at 6:27 am

Uses

Gelicon Capsule 300 mg is used as a hypolipidemic agent in conjunction with dietary modification. It is recommended in the treatment of type IIa, type IIb, type III, type IV and type V hyperlipoproteinemia.

Gelicon Capsule 300 mg is also used to associated treatment for these conditions: Coronary Heart Disease (CHD), Fredrickson classification type IV Hyperlipidemia, Fredrickson classification type V Hyperlipidemia

How Gelicon Capsule 300 mg works

Gelicon Capsule 300 mg activates peroxisome proliferator-activated receptor-α (PPARα), which alters lipid metabolism. This activation leads to increased HDL, apo AI, apo AII, lipoprotein lipase (LPL), inhibition of apo B synthesis, peripheral lipolysis, decreased removal of free fatty acids by the liver, and increased clearance of apoB.

Upregulated LPL reduces plasma triglyceride levels. Decreased hepatic removal of fatty acids decreases the production of triglycerides. The effects on apoB synthesis and clearance decrease VLDL production which also reduce plasma triglyceride levels.

Gelicon Capsule 300 mg's glucuronide metabolite is also an inhibitor of CYP2C8.

Dosage

Gelicon Capsule 300 mg dosage

The usual dose by mouth is 1.2 gm daily in 2 divided doses given 30 minutes before morning and evening meal. The dosage range may vary between 0.9-1.5 gm daily or as directed by the physician.

Side Effects

The most frequent adverse effect involves the G. I. Tract. Abdominal pain and epigastric pain or dyspepsia is common adverse G. I. effects. Other adverse reaction includes pruritus, rash, headache, dizziness, blurred vision, painful extremities and rarely myalgia.

Toxicity

The oral TDLO of gemfibrozil in humans is 18gm/kg/3Y. The oral LD₅₀ in mice is 2218mg/kg and in rats is 1414mg/kg. The intraperitoneal LD₅₀ in rats is 445mg/kg.

Patients experiencing an overdose may present with abdominal cramps, adnormal liver function tests, diarrhea, increased CPK, joint and muscle pain, nausea, and vomiting. Patients should be treated with symptomatic and supportive measures.

Precaution

Causes of secondary hyperlipidaemia such as hypothyroidism and diabetes must be treated before initiating therapy. Renal impairment; blood disorders. Periodic monitoring of the serum lipids should be done; if no adequate response after 3 mth, treatment should be withdrawn. May increase risk of cholelithiasis.

Interaction

Concomitant anticoagulant dosage may need to be reduced and frequent determinations of prothrombin carried out to confirm that the desired prothrombin level has been re-established. There have been reports of severe myositis with marked elevation of creatinine kinase and myoglobinuria when Gelicon Capsule 300 mg and lovastatin were used concomitantly. In most subjects who have had an unsatisfactory lipid response to either drug alone, the possible benefit of combined therapy with lovastatin and Gelicon Capsule 300 mg does not outweigh the risks of severe myopathy, rhabdomyolysis and acute renal failure.

Food Interaction

Take before a meal. Take 30 minutes before meals.

Gelicon Capsule 300 mg Cholesterol interaction

[Major] There have been reports of severe decreases in HDL cholesterol (HDL-C) levels (as low as 2 mg

The decrease has been reported to occur within 2 weeks to years after initiation of therapy.

It is recommended that HDL-C levels be checked within the first few months after initiation therapy and if a severely depressed HDL-C level is detected, therapy with these agents should be withdrawn.

Monitor HDL-C level until it has returned to baseline, and therapy with these agents should not be re-initiated in these patients.

Gelicon Capsule 300 mg Drug Interaction

Major: rosuvastatin, rosuvastatinUnknown: aspirin, aspirin, duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, pregabalin, pregabalin, metoprolol, metoprolol, metoprolol, metoprolol, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Gelicon Capsule 300 mg Disease Interaction

Major: biliary cirrhosis, cholelithiasis, HDL cholesterol, rhabdomyolysis, liver disease, renal dysfunctionModerate: hematological changes

Volume of Distribution

The volume of distribution of gemfibrozil is estimated to be 0.8L/kg.

Elimination Route

Gelicon Capsule 300 mg is absorbed from the gastrointestinal tract.

In healthy volunteers, a 900mg oral dose of gemfibrozil has a C_max of 46±16µg/mL with a T_max of 2.2±1.1h. In patients with chronic renal failure, gemfibrozil has a C_max of 13.8±11.1µg/mL with a T_max of 2.3±1.0h. In patients with liver disease, gemfibrozil has a C_max of 23.0±10.3µg/mL with a T_max of 2.6±1.7h.

Half Life

Gelicon Capsule 300 mg has a plasma half-life of 1.5 hours. In patients with renal failure the half life is 2.4h and in patients with liver disease the half life is 2.1h.

Clearance

The clearance of gemfibrozil is estimated to be 6.0L/h.

Elimination Route

Approximately 70% of a dose of gemfibrozil is eliminated in the urine. The majority of a dose is eliminated as a glucuronide conjugate and 11 6% of a dose is eliminated in the feces.

In healthy volunteers, 0.02-0.15% of a dose was detected in the urine as unmetabolized gemfibrozil, with 7-14% detected as conjugated metabolites. In patients with renal failure, trace amounts of unmetabolized gemfibrozil is present in the urine, with 0.5-9.8% detected as conjugated metabolites. In patients with liver disease, 0.1-0.2% of a dose was detected in the urine as unmetabolized gemfibrozil, with 25-50% detected as conjugated metabolites.

Pregnancy & Breastfeeding use

Safe use in human pregnancy has not been established. It is not known whether gemfibrozil is secreted in human milk. Like most drugs, gemfibrozil should normally be avoided during pregnancy and lactation.