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

composition of the shell: methacrylic acid and ethyl acrylate copolymer [1: 1] -10.20 mg, propylene glycol-2.50 mg, talc-1.64 mg, titanium dioxide E 171-0.64 mg, azorubin E 122 dye 0,02 mg.

Description:round biconvex tablets, covered with a shell, pink. On the cross-section are visible: the core of white or white with a creamy shade of color, a shell of pink color.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

The xanthine derivative. Pentoxifylline improves the rheological properties of blood, (fluidity) due to exposure. on pathologically altered erythrocyte deformability, inhibiting platelet aggregation and decreasing the increased blood viscosity. Pentoxifylline improves microcirculation in areas of impaired blood supply. The mechanism of its action is associated with the inhibition of phosphodiesterase and the accumulation of cAMP in the cells of the smooth muscles of the vessels and in the shaped elements of the blood.

Having a weak myotropic vasoraxis, pentoxifylline slightly reduces the overall peripheral resistance and slightly dilates the coronary vessels.

Treatment with pentoxifylline leads to an improvement in the symptoms of cerebral circulation disorders.

The success of treatment in the occlusal lesion of peripheral arteries (for example, intermittent claudication) is manifested in the elongation of the distance of walking, elimination, night cramps in the gastrocnemius muscles and the disappearance of pain at rest.

Pharmacokinetics:

After oral administration pentoxifylline quickly and almost completely absorbed.

After almost complete absorption pentoxifylline is metabolized. Bioavailability - 6- 32%. When oral intake is exposed to the "first pass" through the liver with 2 main 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 the plasma, respectively, is 5 and 8 times higher than that of pentoxifylline.

The intake of food increases the maximum concentration (C max) of pentoxifylline in the blood plasma by 28%; the maximum concentration of metabolite I is increased by 20%.

The time to reach the maximum concentrations (TCmax) for oral administration is 1 hour. The ptlumination period (T1 / 2) of pentoxifylline after oral administration is 0.4-0.8 hours, metabolites -1-1.6 hours.

Pentoxifylline is completely metabolized and excreted by the kidneys - 94% in the form of metabolites (mainly metabolite V), intestine - less than 4%, in the first 4 hours up to 90% of the dose is excreted. Penetrates into breast milk.

With severe impairment of renal function, excretion of metabolites is slowed down. When liver function is disrupted, the half-life is prolonged and bioavailability is increased.

Indications:

Peripheral circulatory disorders due to atherosclerosis (incl.

- "intermittent" lameness), diabetes mellitus (diabetic angiopathy); trophic disorders (including trophic ulcers of the lower leg, gangrene), frostbite, postthrombotic syndrome.

Symptomatic treatment of the consequences of cerebral circulation disorders of atherosclerotic origin (impaired concentration, dizziness, deterioration of memory), a condition after the transferred ischemic and hemorrhagic stroke.

Circulatory disturbances 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 and auxiliary components of the drug;

- acute myocardial infarction;

- massive bleeding;

- hemorrhagic stroke;

- extensive hemorrhage in the retina of the eye;

- hereditary lactose intolerance, impaired absorption of glucose-galactose, insufficiency of lactase;

- age to 18 years (effectiveness and safety not established)

Carefully:Arterial hypotension (risk of pronounced reduction in blood pressure), chronic heart failure, condition after recent surgery, severe hepatic insufficiency, severe chronic renal failure (creatinine clearance less than 30 ml / min). Stomach ulcer and duodenal ulcer, severe arrhythmias.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Dosage is set by the doctor in accordance with the individual characteristics of the patient. The tablets are swallowed whole, washed down with a small amount of water.

The usual dose is: one pentoxifylline tablet 3 times a day, followed by a slow increase in the dose to 200 mg 2-3 times a day. The maximum single dose is 400 mg, the daily dose is 1200 mg.

In patients with chronic renal failure (creatinine clearance less than 30 ml / min) daily dose of 100-200 mg.

Dose reduction (taking into account individual tolerance) is necessary in patients csevere hepatic insufficiency.

Treatment can be initiated in small doses in patients with low blood pressure, as well as in people at risk because of possible lowering of blood pressure (patients with severe ischemic heart disease or hemodynamically significant stenoses of cerebral vessels). In these cases, the dose can be increased only gradually.

Side effects:

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

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: nausea, vomiting, diarrhea, dryness of the oral mucosa, anorexia, intestinal atony, sensation of pressure and overfilling of the stomach, intrahepatic cholestasis.

From the sense organs: impaired vision, scotoma.

Co cardiovascular system: tachycardia, arrhythmia, cardialgia, progression of angina pectoris, lowering of arterial pressure.

On the part of the organs of hematopoiesis and the system of hemostasis: thrombocytopenia, leukopenia, pancytopenia, hypofibrinogenemia, bleeding (including 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.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: dizziness, urge to vomit, marked decrease in blood pressure, chills, skin flushing, signs of gastrointestinal bleeding (vomiting like "coffee grounds"), tachycardia, arrhythmia, loss of consciousness, areflexia, tonic-clonic convulsions.

Treatment: symptomatic therapy (including measures aimed at maintaining respiration and blood pressure), with convulsions - diazepam.

Interaction:

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

Strengthens the hypotensive effect of ACE inhibitors and nitrates.

Strengthens the hypoglycemic action - insulin and oral hypoglycemic drugs (risk of developing hypoglycemia). Strict monitoring of such patients is necessary.

Cimetidine increases the concentration of pentoxifylline in the plasma (risk of side effects).

Co-administration with other xanthines can lead to excessive nervous excitement of patients.

Increases the concentration of theophylline, which can lead to an increase in its side effect.

Special instructions:

Treatment should be carried out under the control of arterial pressure.

In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit is necessary.

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

In elderly people, a dose reduction (increased bioavailability) may be required. Smoking can reduce the therapeutic effectiveness of the drug.

Effect on the ability to drive transp. cf. and fur:In case of adverse reactions from the nervous system, patients are advised to refrain from controlling the car and other mechanisms, as well as to be cautious when engaging in activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Intestine-soluble film coated tablets, 100 mg.

10 tablets per blister of PVC film and aluminum foil; for 6 blisters together with instructions for use in a pack of cardboard.

Packaging:(10) - blister (6) / blister, instructions for medical use / - pack of cardboard

Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000701

Date of registration:29.09.2011

The owner of the registration certificate:LEKHIM, AO LEKHIM, AO Ukraine

Manufacturer: & nbsp

TECHNOLOG, PAO Ukraine

Information update date: & nbsp23.08.2015

Illustrated instructions

Instructions

Pentoxifylline (Pentoxifylline)