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Lopid

Lopid
Lopid - a drug used in the therapy of the heart and blood vessels The need to use Lopid depends on the diagnosis. Treatment with Lopid should be carried out according to the instructions and recommendations of the doctor.

Brand: Gemfibrozil

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: November 2023
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Lopid 300 mg
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Product description

Pharmacodynamics of the drug Lopid

Buy Lopid in Canada

Lopid®  is a hypolipidemic agent derived from fibric acid. The mechanism of action of the drug is based on the activation of lipoprotein lipase, as well as the ability to increase the catabolism of triglycerides (TG) into very low density lipoproteins (VLDL) and accelerate the transition of cholesterol from atherogenic VLDL to antiatherogenic high density lipoproteins (HDL), while reducing the production of VLDL.

Accelerates the circulation and removal of cholesterol from the liver, promotes the excretion of the latter with bile. Reduces the incorporation of long-chain fatty acids into newly synthesized triglycerides.

In patients with mixed hyperlipidemia, peripheral lipolysis inhibits. Reduces the extraction of free fatty acids in the liver, which leads to a decrease in the formation of triglycerides and reduces the level of triglycerides in the blood plasma (up to 30%), due to a decrease in the level of VLDL and IDL. Reduces (up to 25%) the level of LDL, while increasing the level of HDL, which has an antiatherogenic effect.

In patients with isolated type 4 hyperlipidemia, it reduces the level of triglycerides while increasing the level of HDL, especially HDL2 and HDL3 fractions. This action is associated with:

• activation of lipolysis and the formation of smaller particles of lipoproteins enriched in triglycerides, which leads to a decrease in the proportion of circulating small and relatively dense atherogenic particles of low density lipoproteins (LDL).

• with the formation of large composite HDL molecules, especially apo A-1 and apo A-2 types.

It potentiates fibrinolysis due to a direct inhibitory effect on the synthesis of plasminogen activator (PAI-1).

It has a beneficial effect on the inhibition of the thrombolytic cascade, which determines its positive effect on the outcomes of the disease in patients with CHD.

When taken for 5 years, it reduces the incidence of sudden death from non-fatal and fatal myocardial infarction.

The onset of the lipid-lowering action of Lopid® is noted after 2-5 days, Cmax - after 4 weeks, followed by a weakening of the effect. The duration of action after discontinuation of Lopid® is 6-8 weeks.

The combination of Lopid® with lovastatin, in patients with heterozygous familial hypercholesterolemia, does not lead to potentiation of the effect of lovastatin in reducing the level of LDL in blood plasma. However, this combination is associated with an increased risk of myopathy.  

Pharmacokinetics

After oral administration, Lopid® is  well absorbed from the gastrointestinal tract, the peak concentration (Cmax) is reached within 1-2 hours.

Bioavailability of gemfibrozil is 97%. Food intake does not have a clinically significant effect on its bioavailability.

Lopid® is  metabolized to 4 metabolites. The half-life (T½) is 1.5 hours with constant use, after repeated administration - 1.3 hours.  

In the blood plasma, it is not bound to proteins. Elimination of the drug is carried out by 70% through the kidneys and in the form of conjugates of gemfibrozil and its metabolites. Up to 2% of the drug is excreted unchanged. Since feces excreted to 6% Lopid®. In renal failure, drug accumulation is observed. In case of impaired liver function, the biotransformation of gemfibrozil decreases.

Indications for use Lopid

Lopid is prescribed along with a diet to lower blood cholesterol

• type IIb, IV and V hyperlipoproteinemia, not corrected by a special diet and physical activity, especially in the presence of other risk factors (development of pancreatitis);

• secondary hyperlipoproteinemia caused by diseases that are difficult to treat (diabetes mellitus, gout, hypothyroidism).

Method of administration and dosage the drug Lopid

The drug is well tolerated. Usually appoint 600 mg 2 times a day (morning and evening) or 900 mg 1 time (evening). The maximum daily dose is 1.5 g (patients with type V hypertriglyceridemia).

The drug should be taken 30 minutes before meals without chewing, washed down with water. The course of treatment is several months, if necessary, repeated courses are carried out.  

Treatment of elderly patients:

The use of Lopid® in elderly patients is associated with a number of difficulties in dosing the drug. This is due to the presence of multiple organ changes in patients of this group, as well as the presence of concomitant therapy. In this regard, we recommend starting the use of the drug, with maximum consideration of concomitant therapy, with low initial doses. In addition, it is necessary to take into account the high susceptibility of elderly patients to the development of side effects.

Treatment of patients with renal or hepatic impairment:

in this category of patients there is a higher susceptibility to the development of side effects, and therefore treatment with Lopid® should be started taking into account the severity of organ changes and the presence of concomitant therapy. Patients in this category must always be treated with close supervision by medical personnel, due to the high risk of complications.

Overdose

There is currently no information on overdose of this drug.  

Interaction with other medicinal products

• When used simultaneously with antacids, absorption of Lopidis reduced® from the gastrointestinal tract.

• With the simultaneous use of Lopid® and indirect anticoagulants, the effects of indirect anticoagulants are enhanced.

• In an application Lopid® and oral hypoglycemic agents, sulfonylurea derivatives, there is increased activity of sulfonylurea derivatives, and as a consequence - the fall in blood glucose levels.

• With the simultaneous use of Lopid® with atorvastatin, lovastatin, simvastatin, cerivastatin, the risk of developing severe myopathy increases, especially when used simultaneously with lovastatin or cerivastatin.

• With the simultaneous use of Lopid® and carbamazepine (Tigretol), cases of an increase in the concentration of carbamazepine in the blood plasma have been described, which can lead to an increase in its side effects.

• If simultaneous reception and colestipol Lopid® Lopidabsorption® decreases.

• With the simultaneous use of Lopid® with cyclosporine, cases of decrease in absorption and concentration of cyclosporine in blood plasma have been described.

Special instructions

During treatment, systematic monitoring of blood lipids is required (if treatment is ineffective within 3 months, drug withdrawal is indicated). During and after treatment, a special hypocholesterol diet must be followed.

With long-term treatment, systematic monitoring of the peripheral blood picture and indicators of liver function is necessary (if the functional "liver" tests deviate from the norm, the treatment is suspended until they are normalized). If the next dose is missed, it is necessary to take it as soon as possible, but not double it if it is time for the next dose. If cholelithiasis is detected, treatment is stopped.

Diabetic Patients

In patients with type 2 diabetes who are taking sulfonylurea derivatives, Lopid®  may cause a decrease in blood sugar, which may require changing the single doses of Lopid®.

Patients receiving anticoagulant therapy

When Lopidadministered concurrently to® is patients receiving anticoagulant therapy, it is necessary to take into account the increased effects of indirect anticoagulants due to their increased plasma clearance.

The muscular system.

If muscle pain occurs during treatment with Lopid®, the presence of myositis should be excluded (including determination of CPK). If it is found, the drug is canceled.

Lopid® can cause muscle weakness. In patients suffering from muscle weakness, disorders of the spine, it is necessary to reduce the therapeutic dose of Lopid®. Lopidpatients with myasthenia gravis® is   contraindicated in.

Use of Lopid®  in renal-hepatic impairment

In patients with renal-hepatic impairment, the administration of Lopid®  may increase the incidence of side effects, as a result of which it may be necessary to change the single doses of Lopid®. If necessary, long-term treatment of such patients should regularly monitor the function of these organs.

Elderly patients

In elderly patients, patients of this category may have an increased tendency to a variety of negative reactions developing on the basis of multiple organ failure, which may lead to the need for dose adjustment of Lopid®.

Carcinogenicity

There is currently no conclusive evidence that Lopidcarcinogenic® is. At the same time, to date, there are no large independent multicenter controlled studies on the use of this drug.

Side Effects

generally Lopid®   is well tolerated, however the following adverse effects may occur in some patients:

nervous system: Lopid®  may cause sedation, drowsiness, fatigue, confusion, headache, dizziness, muscle weakness. These reactions usually result from the use of high doses or prolonged treatment Lopid® and are reversible.

Musculoskeletal system: myasthenia gravis, myalgia, arthralgia, rhabdomyolysis.

Gastrointestinal tract: dry mouth, constipation or diarrhea, decreased appetite, nausea, sometimes vomiting, heartburn, unmotivated abdominal pain, flatulence, hyperbilirubinemia, increased activity of hepatic transaminases and alkaline phosphatase, cholelithiasis.

Hematopoietic organs: leukopenia, anemia, bone marrow hypoplasia.

Urogenital system: decreased potency and / or libido.

Allergic reactions: skin rash, dermatitis.

Others: hypokalemia, alopecia, visual impairment, synovitis, decreased potency and libido.