Active substancePentoxifyllinePentoxifylline
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  • Dosage form: & nbspconcentrate for solution for intravenous and intra-arterial administration
    Composition:

    active substance: pentoxifylline - 20 mg;

    Excipients: sodium chloride - 6 mg, sodium dihydrogen phosphate dihydrate (sodium phosphonic acid monosubstituted 2-aqueous) - 1 mg, 0.1 M sodium hydroxide solution to pH 6.0 - 8.0, water for injection up to 1 ml.

    Description:transparent colorless or light yellow liquid.
    Pharmacotherapeutic group:vasodilating agent.
    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 increased collateral circulation, 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 occlusive lesions of peripheral arteries ("intermittent" lameness), leads to an elongation of the walking distance,elimination of night cramps calf muscles and pain at rest.

    Pharmacokinetics:

    The drug is rapidly metabolized in the liver after administration. In the process of metabolism, there are two main metabolites: 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).

    The half-life is from 30 minutes to 1.5 hours. Excreted mainly 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 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 liver function is disrupted, the half-life is prolonged and bioavailability is increased.

    Indications:

    - disturbances of peripheral blood circulation against atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteriitis);

    - 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);

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

    Contraindications:

    - hypersensitivity to pentoxifylline or other xanthine derivatives, as well as other components of the drug;

    - severe coronary or cerebral atherosclerosis;

    - acute myocardial infarction;

    - severe cardiac rhythm disturbances;

    - uncontrolled arterial hypotension;

    - massive bleeding;

    - hemorrhage into the retina of the eye;

    - cerebral hemorrhage;

    - peptic ulcer of the stomach and duodenum;

    - violation of the coagulation system;

    - pregnancy;

    - the period of breastfeeding;

    - 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, with severe hepatic and / or renal (creatinine clearance 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.

    If it is necessary to administer Pentoxifylline during lactation, breastfeeding should be discontinued due to the fact that pentoxifylline penetrates into breast milk (according to the section "Pharmacokinetics").

    Dosing and Administration:

    Intravenous or 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 in a 0.9% solution of sodium chloride or in a 5% solution of dextrose (glucose) (duration of administration is 90-180 min). The daily dose for intravenous administration can be increased to a maximum of 300 mg / day.

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

    At the expressed atherosclerosis of vessels of a brain the preparation should not be entered into a carotid artery.

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

    The procedure for working with a polymer ampoule: "see the scheme on the package of the drug," namely:

    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 / 10,000 to <1/1000); very rarely (<1/10000); frequency is unknown (can not be estimated from available data).

    Violations from the blood and lymphatic system:

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

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

    Immune system disorders:

    Infrequent: hypersensitivity reactions.

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

    Disorders of the psyche:

    Infrequent: increased excitability, insomnia.

    Impaired nervous system:

    Infrequent: dizziness, tremor, headache.

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

    Disorders from the side of the organ of vision:

    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.

    Disorders from the liver and bile ducts:

    Rarely: intrahepatic cholestasis, increased activity of "hepatic" transaminase.

    Disturbances from the skin and subcutaneous tissues:

    Infrequent: itchy skin, erythema, urticaria.

    Very rarely: toxic epidermal necrolysis, Stephen-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 respiration and

    blood pressure.

    Interaction:

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

    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.

    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 may 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 concentration is necessary.

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

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

    Tobacco smoking can reduce the therapeutic effectiveness of the drug.

    The compatibility of Pentoxifylline with other infusion solutions should be checked in each case.

    During the therapy, it is required to monitor the sodium content in the blood plasma, especially in patients who observe a diet with restriction of table salt (total sodium content in an ampoule of 5 ml - 11.8 mg, in an ampoule of 10 ml - 23.6 mg.

    Effect on the ability to drive transp. cf. and fur:Not studied.
    Form release / dosage:

    Concentrate for the preparation of solution for intravenous and intra-arterial administration of 20 mg / ml.

    By 5 or 10 ml in polymeric ampoules made by technology "blow-fill-seal"

    "blow-fill-seal" on the production line Bottelpack.

    For 5 or 10 polymer ampoules, along with the instructions for medical use, put in a pack of cardboard.

    Packaging:ampoules polymeric (10) - packs cardboard
    ampoules polymeric (5) - packs cardboard
    Storage conditions:

    In the dark place at a temperature of no higher than 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:LP-002386
    Date of registration:27.02.2014
    The owner of the registration certificate:SLAVYANSKAYA APTEKA, LLC SLAVYANSKAYA APTEKA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.08.2015
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