Gemfibrozil helps reduce cholesterol and triglycerides (fatty acids) in the blood. High levels of these types of fat in the blood are associated with an increased risk of atherosclerosis (clogged arteries).
Gemfibrozil is used together with diet to treat very high cholesterol and triglyceride levels in people with pancreatitis.
Gemfibrozil is also used to lower the risk of stroke, heart attack, or other heart complications in certain people with high cholesterol and triglycerides who have not been helped by other treatment methods.
Gemfibrozil (Lopid, Gempid) 300 mg and 600 mg is used as a twice-daily oral medicine for the treatment of hypertriglyceridemia as an adjunct to dietary management.
Warnings
You should not take gemfibrozil if you have severe liver or kidney disease, gallbladder disease, or if you are also taking repaglinide, dasabuvir, or simvastatin.
Gemfibrozil Uses:
It is used in the treatment of hypertriglyceridemia in Fredrickson types IV and V hyperlipidemia for patients who are at greater risk for pancreatitis and who have not responded to dietary management.
It is also used to reduce the risk of coronary heart disease development in Fredrickson type IIb patients without a history and symptoms of existing CHD who have not responded to dietary and other interventions including pharmacologic treatment, and who have decreased HDL, increased LDL, and increased triglyceride levels.
Gemfibrozil (Lopid) Dose in the treatment of Hyperlipidemia/ hypertriglyceridemia:
It is given orally as 600 mg twice a day 30 minutes before breakfast and dinner.
Note:
Discontinue if lipid response is inadequate after 3 months of therapy.
Use in Children:
Not indicated.
Gemfibrozil Pregnancy Category: C
Studies on animal reproduction have revealed negative results.
It can also cross the placenta.
Triglyceride concentrations may rise during pregnancy and fetal growth.
If the increase is more than anticipated, it’s time to start supervised dietary intervention.
Gemfibrozil may be an option for women with high levels of triglycerides or who are at higher risk of developing pancreatitis.
Gemfibrozil use during breastfeeding:
It is unknown whether breast milk secretes it.
Breast milk contains lipids, which are an acceptable component. Infant neurological development is normalized by the fatty acids.
The mother’s diet and other factors affect the composition of breast milk.
Due to severe hypertriglyceridemia, the risk of pancreatitis is increased and gemfibrozil therapy can be considered.
Other agents are preferred when treatment is required for other indications.
The benefits of continuing therapy during pregnancy must be greater than the risks to both mother and baby’s health.
Gemfibrozil (Lopid) Dose in Kidney disease:
Manufacturer’s labeling:
Mild-to-moderate impairment:
According to the literature, there are no dose adjustments are required however caution is advised. Deterioration of renal function has been reported in patients with baseline serum creatinine >2 mg/dL
Severe impairment:
Its use is not recommended at all in severe renal impairment.
Alternate recommendations:
GFR >50 mL/minute: No dosage adjustment necessary.
GFR 10 to 50 mL/minute: Administer 75% of dose.
GFR <10 mL/minute: Administer 50% of dose.
Intermittent hemodialysis: Supplemental dose is not necessary.
Peritoneal dialysis: Administer 50% of the dose as a supplement for dialysis.
Dose in Liver disease:
Its use is contraindicated in severe liver impairment.
Common Side Effects of Gemfibrozil (Lopid):
Gastrointestinal:
Dyspepsia
Less Common Side Effects of Gemfibrozil (Lopid):
Cardiovascular:
Atrial fibrillation
Central nervous system:
Fatigue
Vertigo
Dermatologic:
Eczema
Skin rash
Gastrointestinal:
Abdominal pain
Nausea and vomiting
Contraindications to Gemfibrozil (Lopid):
A contraindication is absolute hypersensitivity to gemfibrozil and any component of the formulation.
Hepatic and severe renal dysfunction.
Primary biliary dysfunction.
Gallbladder disease that is already present
Concurrent use of dasabuvir or repaglinide, simvastatin, selexipag, and repaglinide.
Canadian labeling: Additional contraindications not in the US labeling
Renal dysfunction.
Concurrent use of cerivastatin.
Pregnancy.
Breastfeeding
There is not much evidence of cross-reactivity between fibrates and allergens.Cross-sensitivity is possible due to similarities in chemical structure and pharmacologic characteristics.
Warnings and precautions
Cholelithiasis
Cholelithiasis can be increased by using it.If gallstones are detected on gallbladder scans, the drug should be stopped.
Transaminases with elevated levels:
Transaminitis is possible and it is important to monitor liver enzymes regularly.
Hematologic effects
The initiation can cause anemia and a drop in the hematocrit. However, this usually resolves with long-term treatment.
However, anemia, leukopenia and thrombocytopenia are rare.During the first year of therapy, frequent monitoring is recommended.
Malignancy
Malignancy is more likely.
Myopathy/rhabdomyolysis:
Rare myositis and rhabdomyolysis have been linked to it.It is important to monitor patients closely.
Patients should be taught to report any unexplained pain, tenderness or weakness in their muscles.
Renal impairment
Patients with moderate-to-severe renal impairment should exercise caution.It is not recommended for patients with severe impairment.
Patients with serum creatinine levels above 2 mg/dL have shown worsening of RFTs.
Monitoring parameters:
Serum cholesterol.
LFTs periodically.
CBC periodically during the first year of use
How to administer Gemfibrozil?
Administer 30 minutes prior to breakfast and dinner.
Mechanism of action of Gemfibrozil (Lopid):
Gemfibrozil’s exact mechanism of action is not known. However, there are many theories about the VLDL effect. It can inhibit lipolysis and reduce subsequent hepatic fat acid uptake, as well as inhibiting hepatic secretion VLDL.
These actions together decrease serum VLDL levels, and increase HDL cholesterol levels.It is not known what causes HDL elevation.
The onset of action: It may require several days.
Absorption:
Well absorbed
Protein binding:
99%
Metabolism:
It has hepatic metabolism via oxidation to two inactive metabolites. It undergoes enterohepatic recycling.
Half-life elimination:
1.5 hours
Time to peak, serum:
1 to 2 hours
Excretion:
Urine (~70% primarily as conjugated drug).
via feces (6%)
International Brands of Gemfibrozil:
Lopid
APO-Gemfibrozil
DOM-Gemfibrozil
Gemfibrozil-600
MYLAN-Gemfibrozil
PHL-Gemfibrozil
PMS-Gemfibrozil
TEVA-Gemfibrozil
Antalip
Ausgem
Brezimed
Brozil
Cell
Clearol
Detrichol
Elmogan
Fetinor
Fibropid
F.B.-600
Gedum
Gem-S
Gemd
Gemfi
Gemfibril
Gemfil
Gemnpid
Gevilon
Goprozil
Gozid
Hidil
Hipolixan
Innogem
Ipolipid
Lesdown
Lifibron
Lipazil
Lipicap
Lipigem
Lipison
Lipistorol
Lipitrop
Lipizile
Lipofor
Lipolo
Lipres
Lipur
Loceride
Lopid
Lopid OD
Low-Lip
Lozil
Manobrozil
Mersikol
Minilip
Normolip
Polyxit
Qualipid
Reducel
Regulip
Ronox
Synbrozil
Tgil
Trialmin
Triglizil
Weijiangzhi
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