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

Excipients: sugar milk (lactose), potato starch, stearic acid, polyvinylpyrrolidone (povidone), methacrylic acid-ethyl acrylate copolymer 1: 1 (collagen MAE-100 P), macrogol-4000 (polyethylene oxide-4000), talc, titanium dioxide pigment (titanium dioxide), azorubin (carmoazine).

Description:Tablets, covered with enteric coating, pink, biconvex.Two layers are visible on the cross-section.

Pharmacotherapeutic group:Vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline improves microcirculation and blood rheology, has a vasodilating effect, blocks the 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 slightly reduces the overall peripheral resistance and slightly dilates the coronary vessels.

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

Pharmacokinetics:

After oral administration Pentoxifylline almost completely absorbed from the gastrointestinal tract. The drug undergoes "first pass" through the liver with the formation of 2 main pharmacologically active metabolites 1-5 gidroksigeksil--3,7-dimethyl xanthine (metabolite I) and 1-3-carboxypropyl-3,7-dimethylxanthine (metabolite V).The concentration of metabolite I and V in the plasma, respectively, is 5 and 8 times higher than pentoxifylline. The time to reach the maximum concentration is 1 hour. The half-life is 0.5-1.5 hours. Pentoxifylline is excreted primarily by the kidneys - 94% in the form of matabolites (mainly metabolite V), intestine - 4%, for the first 4 hours. up to 90% of the dose is output. 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 caused by atherosclerosis, diabetes mellitus (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; hemorrhages in the retina of the eye; cerebral hemorrhage, 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:

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 is taken orally after a meal. The tablets are covered with a special shell, soluble in the intestines, so they are swallowed whole, washed down with a small amount of water. Take 0.2 g (2 tablets) 3 times a day. After reaching a therapeutic effect (usually 1-2 weeks), the dose is reduced to 0.1 g (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.

Duration of treatment and dosing regimen Pentoxifylline is 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 disorders; 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, cyanosis, tachycardia, marked decrease in blood pressure, redness of the skin, fever (chills), agitation, areflexia, tonic-clonic convulsions, vomiting "coffee grounds", arrhythmia loss of consciousness.

Treatment: symptomatic. Particular attention should be paid to maintaining blood pressure and respiratory function. Seizures are removed by the introduction of diazepam.Urgent measures in the event of severe anaphylactic reactions (shock):

- when there are primary signs (sweating, nausea, cyanosis) immediately stop taking the drug;

- in addition to other necessary measures provide a lower position

head and upper body and provide freedom for breathing;

- urgent medical measures: enter / in epinephrine (adrenalin). If necessary, the introduction of epinephrine can be repeated.

Interaction:

Pentoxifylline enhances the action of heparin, fibrinolytic drugs, theophylline, antihypertensive and hypoglycemic agents (both insulin and oral hypoglycemic agents).

Pentoxifylline may enhance the effect of drugs affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephalosporins - cefamandole, cefoperazone, cefotetan), 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 the patients have 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, who take hypoglycemic agents, high-dose appointments 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.

Form release / dosage:

Intestinal-coated tablets, 100 mg

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50, 60, 100 tablets in cans of polymeric.

Each jar or 1,2, 3, 4, 5, 6 contour squares with instruction for use is placed in a pack of cardboard for consumer containers.

Packaging:(10) - polymer cans (1) - packs cardboard
(10) - packings of cellular contour
(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings, cellular, outline (2) - packs, cardboard
(10) - packings, cellular, outline (3) - packs, cardboard
(10) - packings, cellular, outline (4) - packs, cardboard
(10) - packings, cellular planimetric (5) - packs cardboard
(10) - packings, cell planimetric (6) - packs cardboard
(100) - polymer cans (1) - packs of cardboard
(20) - polymer cans (1) - cardboard packs
(30) - polymer cans (1) - packs of cardboard
(40) - polymer cans (1) - packs cardboard
(50) - polymer cans (1) - cardboard packs
(60) - polymer cans (1) - packs cardboard
(60) - cans of dark glass (1) - packs of cardboard

Storage conditions:

List B. In a dry place, at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002479/10

Date of registration:26.03.2010

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)