International generic name

Pentoxifylline

Drug form and composition

Solution for injection. One ampoule of 5 ml contains 100 mg Pentoxifylline (20 mg/ml).

Indications

Pentofyllin is indicated in diseases, causing disorders in the peripheral perfusion, and in diabetes, atherosclerotic and inflammatory disorders, including shank ulcers; gangrene; diabetic angiopathy; intermittent claudication; Raynaud’s disease. In acute disorders of the brain perfusion, including ischemic stroke and resultant conditions. Acute disorders of the retinal blood supply.

Dosage and administration

The solution is applied intravenously or intramuscularly. Intravenously the preparation could be applied as intravenous jet or as infusions. The intravenous jet is injected slowly in dose 100 mg per 5 minutes, as the patient is in a supine position. It is advisable Pentofyllin to be applied as an intravenous infusion. The infusion solution is prepared as follows: 100-600 mg (1-6 ampoules) Pentofyllin is diluted in 100-500 ml saline or other infusion solution. In patients with gangrene or shank ulcer and severe pain a continuous intravenous drop infusion (within 24 hours) in dose 0.6 mg per kg body weight is advisable. Maximal dose should not exceed 1200 mg per 24 hours. Intramuscularly Pentofyllin is used rarely in dose 100 mg, injected deep in the gluteus, 2-3 times daily. In patients with renal failure the dose should be reduced (about 50-70% of the therapeutically dose).

Contraindications

Hypersensitivity to the preparation; acute myocardial infarction; recent brain and ocular hemorrhages; liver function disorders; pregnancy and lactation.

Special warnings and precautions

In patients with unstable or low blood pressure the preparation dose should be individualized with close monitoring of the patient. In patients with diabetes, treated with oral antidiabetics or insulin, higher doses Pentofyllin may provoke a blood glucose reduction. In patients with renal failure a lower doses Pentofyllin should be used (in case the creatine clearance is lower than 10 ml/min the dose should be 50-70% of the therapeutically). As a risk of blood pressure reducing exists, the preparation should be used with care in drivers and machinery operating persons.

Drug interactions

Pentofylline potentiates the action of the hypotensive and anticoagulant medicines. It may enhance the effect of the oral antidiabetics and insulin. The antiulcer preparation cimetidin increases the plasma concentration of Pentofyllin and the risk of adverse reaction of the latter. Concomitant administration of adrenergic medicines (epinephrine, norepinephrine, etc.) or xanthines (novphyllin, teophyllin, etc.) may cause a hyper-stimulation of the central nervous system.

Adverse reactions

In predisposed patients or in high dosage Pentofyllin may cause a stomach discomfort, nausea, vomiting; headache, dizziness, insomnia (rarely); precordial pain , heart rhythm disorders, blood pressure reduction (rarely); skin rash, itching; thrombocytopenia; sense of hot waves, etc.

Pharmacological mechanisms

Pentofyllin belongs to the group of the peripheral vasodilators. It dilates selectively blood vessels of the limbs, brain and retina. The vasodilatative effect of the preparation is a result of inhibition of the enzyme phosphodiesterase and increasing of the concentration of cAMP in the smooth muscle cells of the blood vessel wall. Pentofyllin possesses some antiaggregant effect also. The latter action is due to the elevation of the cAMP in platelets and (indirectly) to the prostacyclin synthesis potentiation. Pentofyllin improves blood rheology by reducing the internal viscosity and mobility of the red blood cell membrane. It improves significantly the microcirculation in the organism.

Supplied

100 ampoules of 5 ml (100 mg).

Expiry

3 years.