Pentoxifylline-Eskom - instructions for use, dose, side effects, contraindications

Excipients: sodium chlRead 6.0 mg, sodium dihydrogen phosphate dihydrate ("sodium phosphate monobasic 2-hydro ") - 1 mg, 0.1 M sodium hydrateroxide - to pH 5.5-7.5, water for injection - up to 1 ml.

Description:

clear, colorless or slightly yellowish liquid, odorless.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline is a purine derivative improves microcirculation and blood rheology. The mechanism associated with inhibition of zy fosfodiestera- and increased content of 3,5 cyclic adenosine monophosphate (cAMP) in platelets and adenozingrifosfata (ATP) in erythrocytes with simultaneous saturation of the energy potential which in turn leads to vasodilation, reducing the total peripheral vascular resistance (TPR), ascending the stroke volume (CRM) and cardiac output (IOC) without significant change in heart rate (HR).

Expanding the coronary arteries, increases oxygen delivery to the myocardium (anti-anginal effect), lung vessels - improves oxygenation of the blood.

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm).

Intravenous injection, along with the above action, leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section. Increases concentration of ATP in the brain, a positive effect on bioelectric activity of the central nervous system (CNS).

Reduces the viscosity of blood, causes disaggregation of platelets, increases the elasticity of erythrocytes (due to the impact on pathologically altered erythrocyte deformability). Improves microcirculation in areas of impaired blood flow. In the occlusive lesion of peripheral arteries ("intermittent" lameness) leads to an elongation of the distance of walking, elimination of night cramps of gastrocnemius muscles and pain at rest.

Pharmacokinetics:

The drug is rapidly metabolized in the liver. In the process of metabolism, several active metabolites are formed, the main of which are: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V). The concentration of metabolites I and V in the plasma, respectively, is 5 and 8 times higher than pentoxifylline. It is excreted by the kidneys - 94% in the form of metabolites (mainly metabolite V), intestine - 4 %, for the first 4 hours, up to 90% of the dose is output. Unchanged, 2% of the drug is excreted Pentoxifylline and its metabolites do not bind to blood plasma proteins. Excreted in breast milk.

With severe renal dysfunction, excretion of metabolites is slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

- violations of peripheral circulation against the background of atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis);

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

- angioneuropathy (paresthesia, acrocyanosis, Raynaud's disease);

- acute and chronic disorders of cerebral circulation of the ischemic type (including cerebral atherosclerosis);

- condition after hemorrhagic or ischemic insult;

- disorders of blood circulation in the vessels of the eye (acute and chronic failure

blood supply to the mesh and vascular membranes of the eye);

- disturbances in the function of the middle ear of vascular genesis, accompanied by deafness.

Contraindications:

- increased sensitivity to pentoxifylline and other xanthine derivatives;

- acute myocardial infarction;

- severe cardiac rhythm disturbances;

- pronounced atherosclerosis of the coronary or cerebral arteries;

- uncontrolled arterial hypotension;

- porphyria;

- massive bleeding;

- acute hemorrhagic stroke;

- hemorrhage in the retina of the eye;

- pregnancy, lactation;

- age to 18 years (efficacy and safety not established).

Carefully:

Patients with labile arterial pressure, a tendency to arterial hypotension, chronic heart failure, a penchant for hemorrhages, a condition after recent surgery, liver and / or kidney failure.

Pregnancy and lactation:

The drug is contraindicated for use during pregnancy. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

The drug can be administered intravenously, intraarterially (the patient should be in the "lying" position), intramuscularly.

Intravenously drip slowly in a dose of 100 mg in 250-500 ml of 0.9% isotonic sodium chloride solution (NaCl) or in a 5% solution of dextrose (duration of administration - 90-180 min).

Intraarterially - first in a dose of 100 mg in 20-50 ml of a 0.9% solution NaCl, and on subsequent days - 200-300 mg in 30-50 ml of the solvent (injection rate: 100 mg (5 ml of 2% solution of pentoxifylline) for 10 mg / min).

Intramuscularly deep - 100-200 mg 2-3 times a day.

Patients with chronic renal failure (glomerular filtration less than 10 ml / min) are prescribed 50-70% of the usual dose.

Side effects:

From the central nervous system: headache, dizziness, anxiety, sleep disturbances, convulsions.

From the skin: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, swelling, increased brittleness of the nails.

From the gastrointestinal tract: nausea, vomiting, a feeling of heaviness in the stomach, decline appetite, exacerbation of cholecystitis, cholestatic hepatitis, bleeding from the mucous membranes of the stomach, intestines

From the sense organs: visual impairment, scotoma

From the cardiovascular system: tachycardia, arrhythmia, cardialgia, rarely - the progression of symptoms of angina, lowering blood pressure (BP).

On the part of the system of hemostasis and hemopoiesis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia, epistaxis.

Allergic reactions: rarely - itching, skin hyperemia, urticaria, angioedema, anaphylactic shock.

Laboratory indicators: increased activity of "liver" transaminases (ALT, ACT, LDH) and alkaline phosphatase.

Overdose:

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

Treatment: symptomatic, aimed at maintaining the function of breathing and blood pressure.

Interaction:

Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefaperazone, cefotetan, valproic acid).

Increases the effectiveness of antihypertensive drugs, insulin and oral hypoglycemic drugs.

Cimetidine increases the concentration of pentoxifylline in the plasma (risk of side effects).

Co-administration with other xanthines can lead to excessive nervous excitement.

Special instructions:

Treatment should be carried out under the control of blood pressure. In patients with diabetes mellitus, who take hypoglycemic drugs,administration in large doses can cause severe hypoglycemia (dose adjustment is required). At appointment simultaneously with anticoagulants it is necessary to watch carefully indicators of a coagulating system of a blood. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary. The administered dose should be reduced in patients with low and unstable blood pressure. In elderly people, a dose reduction may be required (increased bioavailability and reduced rate of excretion). Smoking can reduce the therapeutic effectiveness of the drug The compatibility of a solution of pentoxifylline with an infusion solution should be checked in each case

Effect on the ability to drive transp. cf. and fur:

Form release / dosage:

Concentrate for the preparation of solution for injection 20 mg / ml.

5 ml of the drug into neutral glass ampoules.

For 10 ampoules together with instructions for medical use and scarifier ampullum in a cardboard bundle with cardboard partitions, or 5 or 10 ampoules in a contiguous cell pack of a polyvinyl chloride film.

When using ampoules with a notch or a fracture ring, the scarifier is not inserted.

For 1 or 2 contour pack together with instructions for medical use in a cardboard box.

Packaging:(1) - ampoules (10) - contour plastic packaging (pallets)
(1) - ampoule (10) / complete with a knife ampoule or scarifier, if necessary for ampoules of this type / - packs cardboard
(1) - ampoules (5) - packings contour plastic (pallets)

Storage conditions:

In protected from light location at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005602/09

Date of registration:13.07.2009

The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia

Manufacturer: & nbsp

ESKOM NPK, OAO Russia

Information update date: & nbsp24.08.2015

Illustrated instructions

Instructions

Pentoxifylline-Eskom (Pentoxifylline-Eskom)