Lipoflavon

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT LIPOLAVON (LIPOFLAVON)

Composition:

Active substances: 1 vial or bottle contains: lecithin-standard (calculated as lecithin) – 550 mg, quercetin (calculated as dry substance) – 15 mg;

Excipient: lactose monohydrate.

Pharmaceutical form. Lyophilisate for emulsion for injection.

Main physicochemical characteristics: amorphous mass of light yellow or light yellow color with a lemon tint and characteristic odor, easily suspends in aqueous solutions forming an emulsion.

Pharmacotherapeutic group. Combined cardiac preparations.

ATC Code C01E X.

Pharmacological Properties

Pharmacodynamics

The medicinal product has antioxidant, anti-hypoxic, and anti-inflammatory effects. It exhibits antiarrhythmic and cardioprotective activity. The therapeutic effect is due to the combined action of the drug's components: inhibition of the 5-lipoxygenase pathway of arachidonic acid metabolism by quercetin, as well as the anti-hypoxic and antioxidant effects of lecithin liposomes. The drug restores the functional activity of vascular endothelium and promotes the synthesis and/or release of endothelium-derived relaxing factor (nitric oxide). It inhibits lipid peroxidation processes in blood and tissues, supports the activity of the body's antioxidant systems, prevents a decline in cellular energy metabolism, and demonstrates membrane- and endothelioprotective effects.

When used in combination with basic therapy:

• In the treatment of non-Q-wave acute myocardial infarction and unstable angina, it leads to a faster positive dynamics in creatine phosphokinase-MB fraction activity and serum C-reactive protein levels, prevents an increase in serum levels of the pro-inflammatory cytokine IL-8, and promotes myocardial electrical stability;
• In the treatment of stable angina, it reduces the severity of angina attacks, decreases platelet aggregation, improves blood rheological parameters (reduces erythrocyte viscosity and aggregation), and enhances microcirculation;
• During polychemotherapy of breast cancer with anthracyclines, it promotes a favorable dynamics in cardiac-specific troponin levels, regression of extrasystolic arrhythmia, and stabilization of vagosympathetic balance.
  No drug accumulation occurs.

Pharmacokinetics

After intravenous administration as a liposomal emulsion, the drug circulates in the blood for up to 2 hours. Maximum accumulation of the drug is observed in the liver and spleen (up to 20%). The drug is excreted in urine and feces.

Clinical characteristics.

Indications.

In complex therapy:

• acute myocardial infarction without Q wave,
• unstable and stable angina pectoris (CHD),
• myocarditis,
• for prevention of toxic myocardial damage during cycles of polychemotherapy for breast cancer.

Contraindications.

Individual hypersensitivity to any components of the medicinal product or to drugs with P-vitamin activity; history of allergic reactions to vaccines or proteins.

Interaction with other medicinal products and other types of interactions.

LIPOTHAVON must not be used concomitantly with cardiac glycosides, and other drugs must not be mixed with LIPOTHAVON in the same syringe. LIPOTHAVON should be administered as part of combined therapy with cardiovascular and anticancer drugs. The interval between administration of LIPOTHAVON and other drugs must be at least 30 minutes.

When using quercetin:

• concomitant use with ascorbic acid preparations results in summation of effects;
• with nonsteroidal anti-inflammatory agents, the anti-inflammatory effect of the latter is enhanced, while their ulcerogenic effect is reduced;
• with digoxin, the maximum serum concentration and overall area under the "concentration–time" curve of digoxin are increased;
• with cyclosporine, bioavailability and blood concentration of cyclosporine are increased;
• with paclitaxel – effect on the metabolism of the latter;
• with verapamil – bioavailability of the latter is increased;
• with tamoxifen – bioavailability is increased, metabolism and elimination of the latter are reduced.

Special precautions for use.

The drug should be administered as soon as possible after the onset of ischemia symptoms to achieve the best therapeutic effect. LIPOLAVON should be administered slowly with monitoring of arterial pressure. If a sharp drop in systemic arterial pressure (more than 40 mm Hg) occurs, the infusion rate should be reduced or administration discontinued. The drug must be administered only in a previously warmed to 37–39 °C 0.9% sodium chloride solution for injection or infusion, after thorough mixing. Administration of the drug is contraindicated if layering of the resuspended emulsion occurs.

The drug contains lactose; therefore, it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding.

Due to limited available data, LIPOLAVON is not recommended for use during pregnancy or breastfeeding.

Ability to affect reaction rate when driving or operating machinery.

Patients should refrain from driving or operating machinery if a decrease in arterial pressure occurs during treatment.

Method of Administration and Dosage

Administer intravenously. Before use, allow the vial (bottle) containing the medicinal product to stand at room temperature for 30 minutes. Prepare the LIPOFLAVON emulsion for intravenous bolus administration immediately before use by adding 10–20 mL of 0.9% sodium chloride solution for injection or infusion, previously warmed to 37–39°C, to the vial (bottle). Shake the vial (bottle) vigorously for 2 minutes to form a liposomal emulsion.

In acute myocardial infarction without Q wave: administer the emulsion formed by adding 0.9% sodium chloride solution for injection or infusion to 2 vials (bottles) of the drug as a slow intravenous bolus over 5 minutes. Repeat subsequent doses according to the same regimen every 12 hours during the first 2 days, then reduce the dose of LIPOFLAVON from day 3 onward (once daily, 2 vials (bottles)) for an additional 3–5 days.

In the treatment of myocarditis, unstable and stable angina pectoris (ischemic heart disease): administer the emulsion formed by adding 0.9% sodium chloride solution for injection or infusion to 2 vials (bottles) as a slow intravenous bolus once daily for 7–10 days.

For prevention of cardiotoxic damage during anthracycline-containing polychemotherapy cycles: administer LIPOFLAVON at the same dose—2 vials (bottles) per day—prior to cytostatic administration, followed by continued administration at the same dose for 3 days after cytostatic administration. The physician determines the further duration of treatment.

Children.

Due to limited available data, LIPOFLAVON is not recommended for use in children.

Overdose.

Symptoms of individual intolerance may occur, requiring discontinuation of the drug and initiation of symptomatic therapy.

Side effects.

Immune system side effects: allergic reactions.

Nervous system side effects: headache, dizziness, limb tremor, tingling sensation in limbs.

Cardiac side effects: tachycardia, palpitations.

Vascular side effects: decreased blood pressure.

Respiratory system, thoracic organs, mediastinum side effects: sensation of breathlessness, dyspnea, shortness of breath.

Gastrointestinal side effects: nausea, vomiting, diarrhea.

Skin and subcutaneous tissue side effects: rash, urticaria, pruritus.

General disorders and administration site reactions: weakness, back and chest pain, hyperthermia; changes, hyperemia at the injection site.

Shelf life. 1 year.

Storage conditions.

Store in the freezer compartment at a temperature from minus 20 °C to minus 10 °C. Keep out of reach of children.

Incompatibility. Concomitant use of LIPOFLAVON with cardiac glycosides is contraindicated. Do not mix with other medicinal products in the same syringe.

Packaging. 1 vial or bottle per carton.

Prescription category. Prescription only.

Manufacturer.

LLC "BIOLIK PHARMA".

Manufacturer's location and address of business activity.

Legal entity location:

70 Pomyrky, Kharkiv, Kharkiv region, 61070, Ukraine.

Address of business activity:

Pomyrky-70, building n/a, Kharkiv, Kharkiv region, 61070, Ukraine.