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

sodium chloride - 6 mg, sodium dihydrogen phosphate dihydrate (sodium phosphate monohydratesubstituted 2-hydroxy) -1 mg, sodium hydroksid 1 M solution to pH 6.0-8.0, water for injections-up to 1 ml.

Description:

Transparent, colorless or slightly yellowish liquid.

Pharmacotherapeutic group:vasodilator

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline is a derivative of xanthine.Improves microcirculation and rheological properties of blood. The mechanism of action is associated with 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 a 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.

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

Increases the tone of the respiratory musculature (intercostal muscles and diaphragm). With intravenous administration leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section. It leads to an increase in the content of ATP in the brain, favorably affects the bioelectric activity of the central nervous system. 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 circulation.

In the occlusal lesion of peripheral arteries ("intermittent" lameness), leads to lengthening the distance of walking, eliminating night cramps calf muscles and pain at rest.

Pharmacokinetics:

The drug is rapidly metabolized in the liver. When ingested, the "first pass through the liver to form two major pharmacologically active metabolites: 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 blood plasma, respectively, 5 and 8 times higher than pentoxifylline.

Half-life from 30 min. up to 1.5 hours, is excreted by the kidneys - 94% in the form of metabolites (mainly metabolite V), intestine - 4%, in the first 4 hours, up to 90 % dose. 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 the peripheral circulation caused by atherosclerosis, diabetes mellitus (diabetic angiopathy),chronic cerebrovascular disorders of ischemic origin, atherosclerotic and discirculatory encephalopathy, angiopathy (paresthesia, Raynaud's disease), trophic tissue disorders (postthrombotic syndrome, varicose veins, trophic ulcers of the lower leg, gangrene, frostbite); obliterating endarteritis; acute circulatory disorders in the retina and choroid of the eye; otosclerosis, degenerative changes on the background of the pathology of the vessels of the inner ear with a gradual decrease in hearing.

Contraindications:

- hypersensitivity to pentoxifylline, other xanthine derivatives or other components included in the formulation;

- severe coronary or cerebral atherosclerosis;

- acute myocardial infarction;

- severe cardiac rhythm disturbances;

- uncontrolled arterial hypotension;

- massive bleeding;

- hemorrhage in the retina of the eye;

- hemorrhage in the brain;

- acute hemorrhagic stroke;

- 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, hepatic and / or renal failure.

Pregnancy and lactation:

Dosing and Administration:

Intravenously, intraarterially. When carrying out infusions, the patient should be in a prone position.

Intravenously drip slowly in a dose of 100 mg in 250-500 ml in a 0.9% solution of sodium chloride or in a 5% solution of dextrose (glucose) (duration of administration - 90-180 minutes); intraarterially - first in a dose of 100 mg in 20-50 ml of 0.9% solution of sodium chloride, and in the following days - 200-300 mg in 30-50 ml of 0.9% sodium chloride solution (rate of administration: 10 mg / min .).

When expressed atherosclerosis of the cerebral vessels can not be introduced into the carotid artery. Patients with chronic renal insufficiency (creatinine clearance less than 10 ml / min.) Are prescribed 50 - 70% of the usual dose.

Side effects:

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

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

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 digestive tract: nausea, vomiting, a feeling of heaviness in the stomach, a decrease in appetite, atony of the intestine, exacerbation of cholecystitis, cholestatic hepatitis, bleeding from the mucous membranes of the stomach, intestines.

From the sense organs: impaired vision, scotoma.

From the hemostasis and hematopoiesis system: Thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; nasal bleeding.

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

Laboratory indicators: increased activity of "liver" transaminases:

alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH) and alkaline phosphatase.

Other: Aseptic meningitis (rarely).

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: rinse the stomach, take Activated carbon, further - 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 - cefamandole, cefoperazone, cefotetana), valproic acid.

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

Cimetidine increases the concentration of pentoxifylline in the blood 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 arterial pressure. Patients with chronic heart failure should be compensated for blood circulation.

In patients with diabetes mellitus taking hypoglycemic agents, the administration of large doses of pentoxifylline can cause severe hypoglycemia (dose adjustment is required).

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

Form release / dosage:

Concentrate for the preparation of a solution for intravenous and intra-arterial administration20 mg / ml.

5 ml into neutral glass ampoules. 10 ampoules are placed in a box of cardboard. In each box, insert the instruction on application and scarifier ampoule ceramic or scarifier ampoule abrasive. A box is pasted with a label-parcel post.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film. 2 contour mesh packages together with instructions for use and a scarifier ampoule ceramic or scarifier ampoule abrasive put in a pack of cardboard. When packing ampoules with a dot or a ring of fracture, the scarifier is not inserted.

Packaging:(5) - ampoule (10) - the box

Storage conditions:

In the dark place at temperature from 2 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N000788 / 01

Date of registration:25.03.2009

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp24.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)