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

Excipients: lactose monohydrate 32.00 mg, potato starch 22.42 mg, methylcellulose, water soluble 0.48 mg, povidone (low molecular weight povidone) 3.50 mg, stearic acid 1.60 mg, triethyl citrate - 1.50 mg, acryl-from 93-A (methacrylic acid copolymer, type C, talc, titanium dioxide, silicon dioxide, sodium bicarbonate, sodium lauryl sulfate) -13,50 mg.

Description:

The tablets covered with a cover of pink color, round, biconcave.

Pharmacotherapeutic group:Vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline microcirculation and rheological properties of blood, has a vasodilating effect, blocks phosphodiesterase and promotes the accumulation of cAMP in cells. Pentoxifylline inhibits the aggregation of platelets and erythrocytes increases their flexibility, reduces the level of fibrinogen in plasma and enhances fibrinolysis, thus reducing blood viscosity and improves its flow characteristics. Has a weak myotropic, vasodilating action. Pentoxifylline somewhat reduces the peripheral resistance and slightly dilates the coronary vessels.

Generally, pentoxifylline causes improvement in microcirculation and supply of tissues with oxygen in the brain and in the extremities, and to a lesser extent in the kidneys.

Pharmacokinetics:

After oral administration Pentoxifylline almost completely absorbed from the gastrointestinal tract. The drug undergoes a "first pass" through the liver with the formation of 2 major pharmacologically active metabolites: 1-5-hydroxyhexyl-3,7-dimethylxanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V).The concentration of metabolite I and V in the blood plasma, respectively, is 5 and 8 times higher than pentoxifylline. The time to reach the maximum concentration is 1 hour. Period of sexexcretion - 0,5 -1,5 hours. Pentoxifylline is 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. Excreted in breast milk. With severe renal dysfunction, excretion of metabolites is slowed down. If the liver function is abnormal, the half-life is prolonged and bio-availability is increased.

Indications:

violation of peripheral circulation due to atherosclerosis, diabetes (diabetic angiopathy);

chronic disorders of cerebral circulation of ischemic genesis;

- atherosclerotic and dyscirculatory encephalopathies; Angiopathy (paresthesia, Raynaud's disease);

- trophic tissue disorders due to violation of arterial or venous microcirculation (trophic ulcers, postthrombophlebitic syndrome, frostbite, gangrene);

- obliterating endarteritis;

- acute, subacute and chronic circulatory insufficiency in the retina or in the choroid of the eye;

- hearing loss of vascular genesis.

Contraindications:

Hypersensitivity to pentoxifylline, other methylxanthine derivatives or other ingredients of the finished dosage form, porphyria; acute myocardial infarction; massive bleeding; hemorrhage in the retina of the eye; acute hemorrhagic stroke; severe coronary or cerebral atherosclerosis; severe cardiac rhythm disturbances; pregnancy; the period of breastfeeding; age to 18 years (efficacy and safety not established).

Carefully:

Carefully: the drug is prescribed to patients with atherosclerosis of cerebral and / or coronary vessels, especially in cases of arterial hypotension and heart rhythm disorders, heart failure, hepatic insufficiency. Care should also be taken when administering Pentoxifylline to patients with peptic ulcer and duodenal ulcer, patients who have recently undergone surgical intervention (risk of bleeding).

Patients with labile arterial pressure and a tendency to arterial hypotension and patients with severe renal dysfunction increase the dose gradually and select individually.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Pentoxifylline taken inside after eating, swallowed whole and washed down with a small amount of water. Take 200 mg (2 tablets) 3 times a day. After reaching the therapeutic effect (usually 1-2 weeks), the dose is reduced to 100 mg (1 tablet) 3 times a day.

The maximum daily dose is 1200 mg. The course of treatment is 1-3 months.

In patients with chronic renal failure (creatinine clearance less than 10 ml / min.), The dose is halved.

The duration of treatment and the dosing regimen of Pentoxifylline are established by the attending physician individually, depending on the clinical picture of the disease and the therapeutic effect obtained.

Side effects:

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

From the skin and subcutaneous fat: 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 system: dry mouth, decreased appetite, intestinal atony, exacerbation of cholecystitis, cholestatic hepatitis.

From the sense organs: impaired vision, scotoma.

From the cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina, lowering of arterial pressure.

On the part of the organs of hematopoiesis and the system of hemostasis: Thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia; bleeding from the vessels of the skin, mucous membranes, stomach, intestines.

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

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

Overdose:

Symptoms: nausea, dizziness, tachycardia, decreased blood pressure, redness of the skin, loss of consciousness, fever (chills), agitation, areflexia, tonic-clonic seizures, vomiting "coffee grounds", arrhythmia.

If the above described violations occur, the patient should urgently consult a doctor. Treatment: symptomatic. When the first signs of an overdose (sweating, nausea, cyanosis) immediately stop taking the drug.Particular attention should be paid to maintaining blood pressure and respiratory function.

Seizures are removed by the introduction of diazepam.

Interaction:

Pentoxifylline enhances the action of heparin, fibrinolytic agents, theophylline, anti-hypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

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

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 of patients.

Special instructions:Patients with severe renal impairment when taking Pentoxifylline require particularly careful medical supervision. In the event that during the period of application of the drug in patients with hemorrhages in the retina of the eye, the drug is immediately canceled. Treatment should be carried out under the control of arterial pressure.In patients with diabetes mellitus, taking hypoglycemic agents, the appointment in large doses can cause 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. 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.

Effect on the ability to drive transp. cf. and fur:During drug treatment, one should refrain from managing motor vehicles and performing potentially dangerous activities related to the need for concentration and increased speed of psychomotor reactions, due to the possibility of dizziness.

Form release / dosage:

Tablets, covered with enteric coating, 100 mg each.

For 60 tablets in cans of light-protective glass or in cans of polyethylene.

For 10 tablets in a planar cell package.

The bank or 6 contour mesh packages together with the instruction for use are placed in a cardboard box.

Packaging:(10) - packings, cell planimetric (6) - packs cardboard
(60) - polyethylene cans (1) - packs cardboard
(60) - cans of light-protective glass (1) - packs cardboard

Storage conditions:

At a temperature of no higher than 30 ° 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-002529/08

Date of registration:04.04.2008

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp26.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)