Fylental (Concentrate) Instructions for Use

Marketing Authorization Holder

Veltrade, LLC (Russia)

Manufactured By

Velpharm, LLC (Russia)

ATC Code

C04AD03 (Pentoxifylline)

Active Substance

Pentoxifylline (Rec.INN registered by WHO)

Dosage Form

Fylental

Concentrate for solution for infusion 20 mg/1 ml: amp. 5 ml or 20 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Concentrate for solution for infusion as a clear, colorless or slightly yellowish liquid.

Excipients: sodium chloride, sodium dihydrogen phosphate dihydrate (sodium phosphate monobasic dihydrate), 1M sodium hydroxide solution, water for injections – up to 1 ml.

5 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
20 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
20 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.

Clinical-Pharmacological Group

Drug improving microcirculation. Angioprotector

Pharmacotherapeutic Group

Peripheral vasodilators; purine derivatives

Pharmacological Action

A drug that improves microcirculation, an angioprotector, a dimethylxanthine derivative. Pentoxifylline reduces blood viscosity, causes platelet disaggregation, increases the elasticity of erythrocytes (by acting on pathologically altered erythrocyte deformability), improves microcirculation and increases the concentration of oxygen in tissues.

It increases the concentration of cAMP in platelets and ATP in erythrocytes with simultaneous saturation of the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in stroke volume and minute volume of blood without a significant change in heart rate.

By dilating the coronary arteries, it increases oxygen delivery to the myocardium; by dilating the pulmonary vessels, it improves blood oxygenation. It increases the tone of the respiratory muscles (intercostal muscles and diaphragm).

Intravenous administration, along with the above action, leads to enhanced collateral circulation, an increase in the volume of blood flowing per unit cross-section.

It increases the concentration of ATP in the brain and has a beneficial effect on the bioelectrical activity of the central nervous system. It improves microcirculation in areas of impaired blood supply.

In occlusive lesions of peripheral arteries (intermittent claudication), it leads to an increase in walking distance, elimination of night cramps of the calf muscles and pain at rest.

Pharmacokinetics

After oral administration, it is well absorbed from the gastrointestinal tract. There is insignificant metabolism during the “first pass” through the liver. It binds to erythrocyte membranes. It undergoes biotransformation first in erythrocytes, then in the liver. Some metabolites are active. The T_1/2 of the unchanged substance from plasma is 0.4-0.8 hours, of metabolites – 1-1.6 hours. After 24 hours, most of the dose is excreted in the urine as metabolites, a smaller part (about 4%) – through the intestines.

The elimination of pentoxifylline is reduced in elderly patients and in liver diseases.

Indications

Peripheral circulation disorders (including intermittent claudication) associated with chronic occlusive circulatory disorders in the arterial vessels of the lower extremities. Ischemic cerebrovascular accident, ischemic stroke and post-stroke conditions; cerebral atherosclerosis (dizziness, headache, memory impairment, sleep disorders), dyscirculatory encephalopathy, viral neuroinfection (prevention of possible microcirculation disorders). Coronary artery disease, condition after myocardial infarction. Diabetic angiopathy. Acute circulatory disorders in the retina and choroid, acute ischemic optic neuropathy. Otosclerosis, degenerative changes against the background of pathology of the vessels of the inner ear with gradual hearing loss. Chronic obstructive pulmonary disease, bronchial asthma. Impotence of vascular origin.

ICD codes

Dosage Regimen

Administer Fylental concentrate only after dilution in an appropriate infusion solution.

For intravenous infusion, dilute the required dose in 250-500 ml of 0.9% sodium chloride solution or 5% dextrose solution.

Initiate therapy with a slow intravenous infusion. Administer an initial dose of 100 mg (one 5 ml ampoule) in 250 ml of solution over 90 minutes.

For maintenance infusion, administer 300 mg (three 5 ml ampoules or one 15 ml volume) daily, divided into one or two infusions.

The maximum single dose should not exceed 200 mg. The maximum daily dose must not exceed 400 mg.

Adjust the infusion rate based on patient tolerance, aiming for a total daily dose of up to 600 mg in severe cases.

Monitor blood pressure and heart rate continuously during and immediately after the infusion.

Reduce the dosage in patients with severe renal impairment (creatinine clearance below 30 ml/min) or severe hepatic impairment.

For intramuscular administration, inject deeply into the muscle, up to 100 mg (one 5 ml ampoule) three times daily.

Transition to oral pentoxifylline formulations for long-term maintenance therapy when clinically appropriate.

Adverse Reactions

From the central nervous system headache, dizziness; anxiety, sleep disorders, convulsions.

Dermatological reactions facial skin hyperemia, “flushes” of blood to the skin of the face and upper chest, edema, increased nail brittleness.

From the digestive system dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis, increased activity of hepatic transaminases and alkaline phosphatase.

From the organ of vision visual impairment, scotoma.

From the cardiovascular system tachycardia, arrhythmia, cardialgia, progression of angina pectoris, decreased blood pressure.

From the hematopoietic system thrombocytopenia, leukopenia, pancytopenia.

From the blood coagulation system hypofibrinogenemia, bleeding from skin vessels, mucous membranes, stomach, intestines.

Allergic reactions itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

Contraindications

Acute myocardial infarction, porphyria, massive bleeding, hemorrhagic stroke, retinal hemorrhage, pregnancy, lactation period. For intravenous administration (additionally) – arrhythmias, severe atherosclerosis of coronary or cerebral arteries, uncontrolled arterial hypotension.

Hypersensitivity to pentoxifylline and other xanthine derivatives.

Use in Pregnancy and Lactation

Adequate and well-controlled clinical studies on the safety of pentoxifylline use during pregnancy have not been conducted.

Pentoxifylline and its metabolites are excreted in breast milk. If it is necessary to use during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

In severe liver function disorders, correction of the pentoxifylline dosage regimen is required.

Use in Renal Impairment

In renal function disorders, correction of the pentoxifylline dosage regimen is required.

Pediatric Use

Use with caution in children and adolescents under 18 years of age (efficacy and safety have not been studied).

Special Precautions

Use with caution in case of blood pressure lability (tendency to arterial hypotension), chronic heart failure, gastric and duodenal ulcer (for oral administration), after recent surgical interventions, in hepatic and/or renal failure, in children and adolescents under 18 years of age (efficacy and safety have not been studied).

In case of renal function disorders or severe liver function disorders, correction of the pentoxifylline dosage regimen is required.

During treatment, blood pressure levels should be monitored.

With simultaneous use with antihypertensive agents, insulin, oral hypoglycemic drugs, a reduction in the dose of pentoxifylline may be required.

With simultaneous use with anticoagulants, blood coagulation parameters should be carefully monitored.

Drug Interactions

Pentoxifylline may potentiate the effect of antihypertensive drugs.

Against the background of parenteral use of pentoxifylline in high doses, an increase in the hypoglycemic effect of insulin in patients with diabetes mellitus is possible.

With simultaneous use with ketorolac, an increased risk of bleeding and/or increased prothrombin time is possible; with meloxicam – an increased risk of bleeding; with sympatholytics, ganglion blockers and vasodilators – a decrease in blood pressure is possible; with heparin, fibrinolytic drugs – enhancement of the anticoagulant effect.

Cimetidine significantly increases the plasma concentration of pentoxifylline, in connection with this, with simultaneous use, the likelihood of side effects may increase.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.