| GEMFIL
Gemfibrozil
Description:
Gemfibrozil is a fibric acid derivative that
is used in the treatment of hyperlipidemias. It has also been
shown to be useful in prophylaxis of both fatal and non-fatal
coronary heart disease.
Composition:
Each capsule contains Gemfibrozil
USP 300 mg.
Pharmacology:
Gemfibrozil decreases serum triglyceride and
very low density lipoprotein (VLDL) cholesterol, and increases
HDL cholesterol. Modest decrease in total and LDL cholesterol
may be observed, except in Type IV hyperlipoproteinemia, patients
who often experience a rise in LDL and type IIb patients who
experience a rise in LDL levels but usually show significant
increase in HDL cholesterol. Gemfibrozil inhibits peripheral
lipolysis and decreases the hepatic extraction of free fatty
acids thus reducing hepatic triglyceride production. Gemfibrozil
also inhibits synthesis and increases clearance of VLDL carrier
apolipoprotein B, decreasing in VLDL production. The drug may
in addition to elevating HDL cholesterol reduce incorporation
of long-chain fatty acids into newly formed triglycerides, accelerate
turnover and removal of cholesterol from the liver and increase
excretion of cholesterol in the feces.
Pharmacokinetics:
Oral absorption
100%
Presystemic metabolism
none
Plasma half-life
Mean 1.5 h
Plasma protein binding
95%
Indications:
-
Patients with type IIa, IIb, III, IV, or
V hyperlipidemia unresponsive to diet.
-
Primary prevention of coronary heart disease
in men between 40 and 55 years of age with hyperlipidemias
who have not responded to diet and other appropriate measures.
Contraindications:
High Risk Group:
Neonates: The drug should not be given to neonates.
Lactating mother: Mothers taking the drug should
not breast feed.
Children: The drug should not be given to children.
Pregnant women: Gemfibrozil is contraindicated
during pregnancy.
The elderly: Patients aged 60 years or over with
lipid levels that are consistent with an increased risk of coronary
heart disease should be treated by diet modification for at
least 3 months. If this therapy is not effective, treatment
with Gemfibrozil can be considered. Dosage and incidence of
adverse effects is similar in young and elderly patients.
Dosage and administration:
The usual dose, by mouth is 1.2 g daily in 2
divided doses given 30 minutes before the morning and evening
meals. The dosage range may vary between 0.9 and 1.5 gm daily.
Side-effects:
Gastro-intestinal disturbances, rash, dermatitis,
pruritus, urticaria, impotence, headache, dizziness, blurred
vision, cholestatic jaundice, angioedema, laryngeal edema, atrial
fibrillation, pancreatitis, myasthenia, myopathy, rhabdomylysis,
painful extremities, myalgia accompanied by increases in creatine
kinase.
Drug Interaction:
Potentially hazardous interaction: Gemfibrozil
can potentate the action of anticoagulants, the dosage of which
may need to be reduced. Antithrombin III levels are also elevated
by the drug. Unlike other fibrates, there is no evidence that
gemfibrozil potentiates the action of hypoglycemic agents. Combined
administration of gemfibrozil and an HMG CoA-reductase inhibitor
appears to increase the chances of developing a myositic syndrome.
Other significant interaction: The bioavailability
of gemfibrozil may be reduced when it is given simultaneously
with resin-granule drugs, such as Colestipol. Administration
of the drugs 2 h or more apart is recommended.
Potentially Useful Interactions: Study showed
that combination of gemfibrozil and a statin (Provastatin, simvastatin,
fluvastatin, lovastatin or atronvastatin) compared with either
agent alone, results in improved long term control of lipid
abnormalities in mixed lipid disorders. The low incidence of
toxicity permits the use of combination therapy in patients
at high risk of atherosclerosis complications.
Storage:
Storage in a cool and dry place. Keep out of
the reach of children.
Packing:
Each box contains 3x10's capsules in strip pack.
|
