Pentoxifylline-Solofarm Politvist solution for injection 2%, 5ml ampoules plastic, 10pcs

Composition

1 ml of the drug contains:  

Active ingredient:

pentoxifylline – 20 mg.  

auxiliary substances:  

sodium chloride – 6 mg,  

sodium dihydrophosphate dihydrate – 1 mg,  

1 M sodium hydroxide solution – up to pH 6.0-8.0,  

water for injection – up to 1 ml.

Pharmacological action

Pentoxifylline is a derivative of xanthine. microcirculation and rheological properties of blood. The mechanism of action is associated with the inhibition of phosphodiesterase and an increase in the content of cyclic 3,5-adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (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 systolic and minute blood volume without a significant change in heart rate.

Dilating the coronary arteries, increases oxygen delivery to the myocardium (slight antianginal effect), lung vessels – blood oxygenation. When administered intravenously, it leads to increased collateral circulation, an increase in the volume of blood flowing through the unit section.

Reduces blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (due to the effect on pathologically altered deformability of red blood cells). microcirculation in areas of impaired blood circulation. With occlusive lesions of the peripheral arteries (intermittent lameness), it leads to an elongation of the walking distance, elimination of nocturnal cramps of the calf muscles and pain at rest.  

pHarmacokinetics

The drug is rapidly metabolized in the liver after use. In the process of metabolism, two main metabolites are formed: 1-(5-hydroxyhexyl)-3,7-dimethylxanthine (metabolite I) and 1-(3-carboxypropyl)-3,7-dimethylxanthine (metabolite V), which have similar activity to pentoxifylline.

1.5-2 hours after the infusion, the concentration of metabolites I and V in the blood plasma, respectively, is 5 and 8 times higher than the concentration of the starting substance. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood is significantly reduced (up to 10% of the initial one). The half-life is from 30 minutes to 1.5 hours.  

It is excreted mainly by the kidneys (94%) in the form of metabolites (mainly metabolite V), by the intestine (4%), up to 90% of the dose is excreted in the first 4 hours. 2% of the drug is excreted unchanged. Pentoxifylline and its metabolites do not bind to plasma proteins. It is excreted in breast milk.

In severe renal dysfunction, the excretion of metabolites is slowed down. With impaired liver function, there is an elongation of the half-life and an increase in bioavailability.

Indications

– Peripheral circulatory disorders against the background of atherosclerotic, diabetic and inflammatory processes (including intermittent lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis);

– trophic tissue disorders due to arterial and venous microcirculation disorders (varicose ulcers, gangrene, frostbite);

– angioeuropathy (paresthesia, acrocyanosis, Raynaud’s disease); – acute and chronic ischemic cerebral circulatory disorders (including cerebral atherosclerosis);

– conditions after hemorrhagic or ischemic stroke;

– circulatory disorders in the vessels of the eye (acute and chronic insufficiency of blood supply to the retina and vascular membranes of the eye); – violations of the function of the middle ear of vascular genesis, accompanied by hearing loss.

Contraindications

– Hypersensitivity to pentoxifylline or other xanthine derivatives, as well as to any auxiliary substance of the drug;

– severe coronary or cerebral atherosclerosis; 

– a recent myocardial infarction;

– hemodynamically significant cardiac arrhythmias;

– uncontrolled arterial hypotension;

– massive bleeding (risk of increased bleeding);

– extensive hemorrhages in the retina of the eye (risk of increased bleeding);

– hemorrhages in the brain;

– peptic ulcer of the stomach and duodenum; 

– violation of the parameters of the blood coagulation system;

– age up to 18 years (efficacy and safety have not been established).  

With caution:  

Patients with labile blood pressure, a tendency to hypotension, chronic heart failure, hemorrhagic diathesis, a tendency to bleeding (including with peptic ulcer of the stomach and duodenum), in the condition after recent surgical interventions, with severe hepatic and / or renal (creatinine clearance less than 10 ml / min) insufficiency. The patient should be prescribed Pentoxifylline with caution in conjunction with direct and indirect anticoagulants due to the increased effect of the latter. Pregnancy and lactation: Pentoxifylline is contraindicated during pregnancy, because the experience of using the drug in pregnant women is limited. If it is necessary to prescribe pentoxifylline during lactation, breastfeeding should be discontinued due to the fact that pentoxifylline penetrates into breast milk.

Side effects

The frequency of possible side effects listed below is determined as follows: very often (1/10); often (1/100 to 1/10); infrequently (1/1000 to 1/100); rarely (1/10000 to 1/1000); very rarely (; 1/10000);

frequency unknown (cannot be estimated from available data).  

Disorders of the blood and lymphatic system:  

Very rare: thrombocytopenia, thrombocytopenic purpura, aplastic anemia, pancytopenia.  

Rare: bleeding (incl. nosebleeds, gastrointestinal bleeding, bleeding from the urinary tract, etc. ).  

Disorders of the immune system: Infrequent: hypersensitivity reactions.  

Very rare: severe anaphylactic or anaphylactoid reactions occurring within a few minutes after use of pentoxifylline, Quincke’s edema, bronchospasm, anaphylactic shock.  

Mental disorders:  

Infrequently: increased excitability, insomnia.  

Disorders of the nervous system:  

Infrequently: dizziness, tremor, headache.  

Very rare: paresthesia, convulsions, intracranial hemorrhage, aseptic meningitis. Visual organ disorders:  

Infrequently: visual impairment, conjunctivitis.  

Very rare: hemorrhage into the retina of the eye, detachment of the retina of the eye.  

Disorders of the heart:  

Infrequently: cardiac arrhythmia, tachycardia.  

Rare: angina pectoris, shortness of breath.  

Vascular disorders:  

Often: hyperemia of the skin of the face.

Rare: decreased blood pressure, peripheral edema.  

Very rarely: increased blood pressure.  

Gastrointestinal disorders: Often: nausea, vomiting, bloating, feeling of heaviness in the stomach, diarrhea.  

Disorders of the liver and biliary tract:  

Very rarely: intrahepatic cholestasis, increased activity of “hepatic” transaminases.  

Disorders of the skin and subcutaneous tissues:  

Infrequently: itching, erythema, urticaria.  

Very rare: toxic epidermal necrolysis, Stevens-Johnson syndrome, increased sweating.  

General disorders and disorders at the injection site:  

Infrequently: an increase in body temperature.

Interaction

Pentoxifylline can enhance the effect of drugs affecting the blood clotting system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephallosporins – cefamandole, cefoperazone, cefotetan), valproic acid.  

With the simultaneous use of pentoxifylline with ketorolac, the risk of bleeding and / or prolongation of prothrombin time increases. Joint use of these drugs is undesirable. Increases the effectiveness of antihypertensive drugs, insulin, hypoglycemic agents for oral use.

cImetidine increases the concentration of pentoxifylline in blood plasma (risk of side effects). Co-use with other xanthines can lead to excessive nervous excitement.  

In some patients, with the simultaneous use of pentoxifylline and theophylline, there is an increase in the concentration of theophylline in the blood. In the future, this may lead to an increase or intensification of side effects associated with theophylline.  

In some patients, with the simultaneous use of pentoxifylline and ciprofloxacin, there is an increase in the concentration of pentoxifylline in blood plasma. In the future, this may lead to an increase or increase in side effects associated with the use of this combination.

How to take, course of use and dosage

Intravenously and intraarterially.  

During the infusion, the patient should be in the “lying down” position. The drug is administered intravenously drip slowly at a dose of 100 mg in 250-500 ml of 0.9% sodium chloride solution or Ringer’s solution (duration of use – 90-180 minutes).100 mg of pentoxifylline should be administered intravenously for at least 60 minutes.  

The daily dose for intravenous use can be increased to a maximum of 300 mg / day. Intra-arterial – first at a dose of 100 mg in 20-50 ml of 0.9% sodium chloride solution, and in the following days – 200-300 mg in 30-50 ml of 0.9% sodium chloride solution (the rate of use is -10 mg / min).  

With severe atherosclerosis of the cerebral vessels, the drug should not be injected into the carotid artery. Patients with chronic renal failure (creatinine clearance less than 30 ml / min) are prescribed 50-70% of the usual dose. Elderly patients may need to reduce the dose (increase bioavailability and decrease the rate of elimination).

Dose reduction, taking into account individual tolerability, is necessary in patients with severe hepatic impairment. The administered dose should be reduced in patients with low and unstable blood pressure.

Procedure for working with a polymer ampoule: 

1. Take the ampoule and shake it, holding it by the neck.

2. Squeeze the ampoule by hand, while the drug should not be released, and rotate and separate the valve with rotating movements.

3. Immediately connect the syringe to the ampoule through the resulting hole.

4. Turn the ampoule over and slowly fill the syringe with its contents.

5. Put the needle on the syringe.

Overdose

Symptoms: weakness, dizziness, marked decrease in blood pressure, tachycardia, drowsiness, loss of consciousness, tonic-clonic convulsions, increased nervous excitability, hyperthermia, areflexia, signs of gastrointestinal bleeding (vomiting like “coffee grounds”).

Treatment: symptomatic, aimed at maintaining respiratory function and blood pressure.

Special instructions

Treatment should be carried out under the control of blood pressure. In patients with chronic heart failure, circulatory compensation should be achieved.

In patients with diabetes mellitus taking hypoglycemic agents, the use of high doses of pentoxifylline may cause severe hypoglycemia (it may be necessary to adjust the doses of hypoglycemic agents and conduct glycemic control).

When administered simultaneously with anticoagulants, monitoring of blood clotting parameters is necessary. In patients who have recently undergone surgery, regular monitoring of hemoglobin and hematocrit is necessary.

The administered dose should be reduced in patients with low and unstable blood pressure, as well as in patients with severe atherosclerosis of the coronary and/or cerebral arteries, since in the latter case, an additional decrease in blood pressure can lead to a deterioration in blood supply to the heart and/or brain.

Elderly patients may need to reduce the dose (increase bioavailability and decrease the rate of elimination). Smoking may reduce the therapeutic effectiveness of the drug.

Compatibility of the pentoxifylline solution with other infusion solutions should be checked on a case-by-case basis. During therapy, monitoring of the sodium content in the blood plasma is required, especially in patients who follow a diet with a restriction of table salt (the total sodium content in a 5 ml ampoule is 11.8 mg).

Influence on the ability to drive vehicles and mechanisms: 

Taking into account possible side effects (for example, dizziness), caution should be exercised when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Active ingredient

Pentoxifylline

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection