Active substancePentoxifyllinePentoxifylline
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  • Dosage form: & nbspTOoncentrat for solution for infusion.
    Composition:

    1 ml of the preparation contains:

    Active substance: pentoxifylline - 20 mg.

    Excipients: sodium chloride - 6 mg, sodium dihydrogen phosphate dihydrate - 1 mg, 1 M sodium hydroxide solution - to pH 6.0-8.0, water for injection - up to 1 ml.

    Description:

    Transparent, colorless or with a yellowish tinge of 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 (a slight antianginal effect), the vessels of the lungs - improves oxygenation of the blood.

    With intravenous administration leads to an increase in collateral circulation, an increase in the volume of flowing blood through a unit of section.

    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 occlusive lesion of peripheral arteries (intermittent claudication), leads to an elongation of the walking distance, elimination of night cramps of calf muscles and pain at rest.

    Pharmacokinetics:

    The drug is rapidly metabolized in the liver after administration. 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 a similar pentoxifylline activity . 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).

    Half-life from 30 minutes to 1.5 hours. Excreted primarily by the kidneys (94%) in the form of metabolites (mainly metabolite V), intestine (4%), in the first 4 hours up to 90% of the dose is excreted. Unchanged, 2% of the drug is withdrawn. Pentoxifylline and its metabolites do not bind to blood plasma proteins.

    Excreted in breast milk.

    In severe violations of kidney function excretion of metabolites is slowed down.

    When a violation of liver function prolonged half-life and increased bioavailability.

    Indications:

    - Violations of peripheral blood circulation against the background of atherosclerotic, diabetic and inflammatory processes (incl.with intermittent claudication 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 stroke;

    - disorders of blood circulation in the vessels of the eye (acute and chronic insufficiency of the blood supply to the retina and choroid of the eye);

    - Dysfunction of the middle ear of vascular genesis, accompanied by deafness.
    Contraindications:

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

    - severe coronary or cerebral atherosclerosis;

    - recently suffered myocardial infarction;

    - hemodynamically significant violations of the rhythm of the heart;

    - uncontrolled arterial hypotension;

    - massive bleeding (risk of increased bleeding);

    - extensive hemorrhage in the mesh of the eye (risk of increased bleeding);

    - hemorrhages in the brain;

    - peptic ulcer of the stomach and duodenum;

    - violation of the coagulation system;

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

    Carefully:

    Patients with labile blood pressure, prone to hypotension, congestive heart failure, hemorrhagic diathesis, a tendency to bleeding (including gastric ulcer and duodenal ulcer), with condition after recent myocardial surgical interventions, in severe liver and / or renal (clearance of creatinine less than 10 ml / min) insufficiency.

    Patients with connective tissue diseases (including systemic lupus erythematosus).

    Pentoxifylline should be administered with caution in conjunction with direct and indirect anticoagulants due to the increased effect of the latter.

    Pregnancy and lactation:

    Pentoxifylline is contraindicated in pregnancy, because the experience of using the drug in pregnant women is limited.

    The appointment of pentoxifylline during lactation breast-feeding should bediscontinue due to the fact that pentoxifylline penetrates into breast milk.

    Dosing and Administration:

    Intravenous and intra-arterial.

    When carrying out the infusion, the patient should be in the "lying" position.

    The drug is administered intravenously drip slowly in a dose of 100 mg in 250-500 ml of 0.9% solution of sodium chloride or Ringer's solution (duration of administration is 90-180 minutes). 100 mg of pentoxifylline should be administered intravenously for at least 60 minutes. The daily dose for intravenous administration can be increased to a maximum of 300 mg / day.

    Intraarterially - First, in a dose of 100 mg in 20-50 ml of 0.9% solution of sodium chloride, and on subsequent days - 200-300 mg in 30-50 ml of 0.9% sodium chloride solution (injection rate of -10 mg / min) .

    At the expressed atherosclerosis of vessels of a brain the drug can not be injected into the carotid artery.

    Patients with chronic renal insufficiency (creatinine clearance less than 30 ml / min) is prescribed 50-70% of the usual dose.

    In elderly patients a dose reduction may be required (increased bioavailability and reduced elimination rate).

    Dose reduction, taking into account individual tolerability, is necessary in patients with severe impairment of liver function.

    The administered dose should be reduced in patients with low and unstable blood pressure.

    The procedure for working with a polymer ampoule:

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

    2. Press the ampoule with your hand, while the drug should not be isolated, and rotate and separate the valve with rotating movements.

    3. Through the formed hole, immediately connect the syringe with the ampoule.

    4. Turn the ampoule over and slowly put the contents into the syringe.

    5. Put the needle on the syringe.

    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 is unknown (can not be estimated from available data).

    Violations of the blood and lymphatic system:

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

    Rarely: bleeding (including nosebleeds, gastrointestinal bleeding, bleeding from the urinary tract, etc.).

    Immune system disorders:

    Infrequent: hypersensitivity reactions.

    Very rarely: heavy,occurring within a few minutes after the administration of pentoxifylline anaphylactic or anaphylactoid reactions, Quincke's edema, bronchospasm, anaphylactic shock.

    Disorders of the psyche:

    Infrequent: increased excitability, insomnia.

    Disturbances from the nervous system:

    Infrequent: dizziness, tremor, headache.

    Very rarely: paresthesia, convulsions, intracranial hemorrhage, aseptic meningitis.

    Disturbances on the part of the organ of sight:

    Infrequent: impaired vision, conjunctivitis.

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

    Heart Disease:

    Infrequent: a violation of the rhythm of the heart, tachycardia.

    Rarely: stenocardia, dyspnea.

    Vascular disorders:

    Often: hyperemia of the skin of the face.

    Rarely: lowering blood pressure, peripheral edema.

    Very rarely: increased blood pressure.

    Disorders from the gastrointestinal tract:

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

    Disturbances from the liver and bile ducts:

    Very rarely: intrahepatic cholestasis, increased activity of "liver" transaminases.

    Disturbances from the skin and subcutaneous tissues:

    Infrequent: itchy skin, erythema, urticaria.

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

    General disorders and disorders at the site of administration:

    Infrequent: increased body temperature.

    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 the function of breathing and blood pressure.

    Interaction:

    Pentoxifylline may enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandol, cefoperazone, cefotetana), valproic acid.

    With the simultaneous use of pentoxifylline with ketorolac, the risk of bleeding and / or prolongation of prothrombin time increases. The joint administration of these drugs is undesirable.

    Increases the effectiveness of antihypertensive drugs, insulin, 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.

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

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

    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, who take hypoglycemic drugs,administration of large doses of pentoxifylline may cause severe hypoglycemia (dosage of hypoglycemic agents and glycemic control may be required).

    When appointing concomitantly with anticoagulants, blood coagulation monitoring is necessary.

    Patients who have undergone recent surgery need regular monitoring of hemoglobin and hematocrit.

    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. in the latter case, an additional reduction in blood pressure can lead to a deterioration of the blood supply to the heart and / or brain.

    Older patients may need a dose reduction (increased bioavailability and reduced elimination rate).

    Smoking can reduce the therapeutic effectiveness of the drug.

    The compatibility of a solution of pentoxifylline with other infusion solutions should be checked in each case.

    During therapy, it is required to monitor the sodium content in the blood plasma, especially in patients,observing a diet with restriction of table salt (total sodium content in an ampoule of 5 ml - 11.8 mg).

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

    Considering possible side effects (for example, dizziness), care should be taken when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:Concentrate for solution for infusion, 20 mg / ml.
    Packaging:

    5 ml per ampoule of low-density polyethylene or polypropylene.

    For 10 ampoules together with instructions for use in a pack of cardboard.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-003809
    Date of registration:23.08.2016
    Expiration Date:23.08.2021
    The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspGROTEKS, LLCGROTEKS, LLC
    Information update date: & nbsp11.10.2016
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