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

1 tablet of prolonged action contains: active substance: pentoxifylline - 600 mg; Excipients: copovidone - 60.0 mg; hypromellose K 15 M - 32.0 mg; hypromellose K 100 M - 46.0 mg; talc - 14.0 mg; magnesium stearate - 8.0 mg.

Description:oblong, biconvex white tablets with a risk on both sides.

Pharmacotherapeutic group:vasodilating agent.

ATX: & nbsp

C.04.A.D.03 Pentoxifylline

Pharmacodynamics:

Pentoxifylline is a derivative of purine (methylalanine). Improves microcirculation and rheological properties of blood, inhibits phosphodiesterase, enhances concentration cyclic adenosine monophosphate (cAMP) 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 the total peripheral vascular resistance, an increase in the shock and minute volume of blood without a significant change in heart rate.

Having a weak myotropic vasoraxis, pentoxifylline slightly reduces the overall peripheral resistance and slightly dilates the coronary vessels. Expanding the vessels of the lung, improves oxygenation of the blood.

Increases the tone of the respiratory muscles, expanding the vessels of the intercostal muscles and diaphragm.

Reduces blood viscosity, causes disaggregation of platelets; reduces the concentration of fibrinogen in the blood plasma at initially inflated values; increases the elasticity of erythrocytes (due to the effect on the pathologically changed deformability of erythrocytes). Inhibits leukocyte activation and adhesion to the vascular wall endothelium. Improves microcirculation in areas of impaired blood flow.In the occlusive lesion of peripheral arteries ("intermittent" lameness) leads to an elongation of the distance of walking, removal of night cramps of gastrocnemius muscles and pain at rest.

Pharmacokinetics:

Absorption when ingested - high. The prolonged form of the preparation ensures continuous release of the active substance and its uniform absorption. When ingestion is subjected to a "primary passage" 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 metabolites I and V in the blood plasma, respectively, is 5 and 8 times higher than pentoxifylline. Systemic bioavailability of pentoxifylline 20 - 30%.
Half-life (T1 /₂) for pentoxifylline and its metabolites - 3.4 h.
It is excreted 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 disruption of kidney and liver function, the excretion of metabolites is slowed, an elongation of T1_/2 and increased bioavailability of pentoxifylline.

Indications:

- violation of peripheral circulation against atherosclerotic, diabetic and inflammatory processes (including "intermittent" lameness caused by atherosclerosis, diabetic angiopathy, obliterating endarteritis), angiopathy (paresthesia, Raynaud's disease);

- chronic disorders of cerebral circulation of ischemic genesis;

- circulatory insufficiency in the retina and choroid of the eye. Hearing disorders of vascular genesis;

- atherosclerotic and dyscirculatory encephalopathy;

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

Contraindications:

- chronic disorders of cerebral circulation of ischemic genesis;

- circulatory insufficiency in the retina and choroid of the eye.Hearing disorders of vascular genesis;

- atherosclerotic and dyscirculatory encephalopathy;

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

Carefully:Severe heart rhythm disturbances; lability of blood pressure (tendency to arterial hypotension); atherosclerosis of cerebral and / or coronary vessels, especially in the case of arterial hypotension and cardiac rhythm disturbances; a history of myocardial infarction; chronic heart failure; a condition after recently transferred surgical interventions; hepatic and / or kidney failure (creatinine clearance (CK) less than 30 ml / min - risk of cumulation and an increased risk of side effects); increased tendency to bleeding, for example, when using anticoagulants or when the blood coagulation system is violated (risk of developing more severe bleeding); systemic lupus erythematosus, mixed connective disease fabric; simultaneous use with insulin and other hypoglycemic drugs, ciprofloxacin.

Pregnancy and lactation:

Contraindicated in the use of pentoxifylline during pregnancy. Pentoxifylline penetrates into breast milk in very small quantities, not capable of causing side effects in the infant. However, if you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, after eating, squeezed a little water.

Usually, 1 tablet of prolonged action in the morning and in the evening (1200 mg per day). The maximum daily dose of 1200 mg.

In patients with impaired liver and kidney function (QC less than 30 ml / min), dose adjustment is necessary depending on individual characteristics.

The maximum daily dose for patients with renal insufficiency - 600 mg.

Duration of treatment is determined individually, depending on the clinical state of the patient.

Side effects:

According to the World Health Organization (WHO) undesirable Effects are classified according to their frequency of development as follows: very often (> = 1/10), often (> 1/100, <1/10), infrequently (> = 1/1000, <1/100), rarely (> = 1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown (frequency of occurrence phenomena can not be determined on the basis of available data).

Disturbances from the nervous system

infrequently: head pain, dizziness, tremor, sleep disturbances; rarely: anxiety, paresthesia, convulsions, intracranial hemorrhage, there are known cases of aseptic meningitis (mainly in patients with autoimmune diseases (system red lupus, mixed disease connective tissue). In all observables cases of symptoms were reversible after stopping the use of nentoxifylline).

Disturbances on the part of the organ of sight

infrequently: impaired vision, scotoma, conjunctivitis; rarely: hemorrhage in the retina of the eye, retinal detachment.

Violations with hand digestive system

often: feeling of pressure and overflow in the abdomen, nausea, vomiting, diarrhea, a feeling of hunger; rarely: dryness of the oral mucosa, intestinal atony, gastrointestinal bleeding; rarely: transitory rise activity "hepatic" transaminase, alkaline phosphatase, Cholestatic hepatitis, exacerbation of cholecystitis.

Disorders from the kidneys and urinary tract

rarely: urogenital bleeding. Disorders from the cardiovascular system infrequently: arrhythmia, tachycardia; rarely: progression angina, dyspnea, decreased blood pressure; rarely: increased blood pressure.

Disturbances from the skin and subcutaneous tissues

infrequently: hyperemia of the skin integuments, itching of the skin, hives; rarely: hyperemia of the skin of the face, "tides" of blood to the skin of the face and upper chest, increased fragility of the nails, hemorrhages in the skin; rarely: Stevens-Johnson, toxic epidermal necrolysis, increased sweating. Disorders from the blood and lymphatic system are very rare: thrombocytopenia (including thrombocytopenic purpura), aplastic anemia (including fatal outcome), pancytopenia, bleeding (including from the mucous membranes, stomach, intestines, genitourinary tract), leukopenia, hypofibrinogenemia.

Immune system disorders

highly rarely: heavy anaphylactic or anaphylactoid reactions (angioedema edema, bronchospasm, anaphylactic shock).

Other

infrequently: fever; rarely: peripheral edema.

Overdose:

Symptoms: dizziness, weakness, redness of the skin, vomiting, marked decrease in blood pressure, tachycardia,drowsiness or agitation, loss of consciousness, fever, areflexia, tonic-clonic convulsions, signs of gastrointestinal bleeding (vomiting like "coffee grounds").

Treatment: a specific antidote is not known. Gastric lavage followed by ingestion of activated charcoal. In the case of vomiting with traces of blood, gastric lavage is unacceptable. Symptomatic therapy (including measures aimed at maintaining breathing and blood pressure), with convulsions - diazepam, emergency measures for bleeding.

Interaction:

Pentoxifylline enhances the effect of drugs drugs, reducing blood pressure, affecting the blood coagulation system (indirect and direct anticoagulants, thrombolytics), hypoglycemic drugs for admission inside, insulin, antibiotics, valproic acid, which may require a decrease in the dose of pentoxifylline.

Cimetidine increases the concentration of pentoxifylline in the blood plasma, increasing the incidence of side effects of the latter. Pentoxifylline can increase concentration theophylline in the blood plasma, leading to an increased incidence of its side effects.

When used simultaneously with ketorolacom the risk increases development of bleeding and / or increase of urothrombin time.

When used simultaneously with ciprofpoxacin perhaps increase in concentration pentoxifylline in the blood plasma, which can lead to an increased incidence of adverse reactions.

Special instructions:

Treatment drug

Pentoxifylline Sandoz® should be performed under the control of blood pressure, a clinical blood test (risk of developing aplastic anemia).

Do not take the missed dose of the drug if more than 3 hours have elapsed from the time of the usual intake; Do not take twice the dose of the drug in the next dose.

Patients with arrhythmia, low arterial pressure, atherosclerosis of cerebral and / or coronary vessels (especially in the case of arterial hypotension and cardiac arrhythmias), with chronic cardiac deficiency, as well as patients who have had myocardial infarction or surgical interventions, careful medical supervision is required.

In patients with severe impairment of renal and hepatic function, excretion of pentoxifylline can be slowed down, so such patients when taking the drug Pentoxifylline Sandoz^® need 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.

At appointment simultaneously with anticoagulants is necessary regularly control indicators of the blood coagulation system (INR (International Normalized Ratio)).

In patients with systemic lupus erythematosus or a mixed connective tissue disease a drug Pentoxifylline Sandoz® should only be used after a thorough assessment of the benefit / risk.

When combined with insulin and other hypoglycemic agents regularly control concentration blood plasma glucose.

In patients who have recently undergone surgery intervention, is necessary systematic control of hemoglobin and hematocrit. At the appearance of the first signs of allergic / anaphylactic reactions should immediately stop taking the drug Pentoxifylline Sandoz® and inform the doctor about it. When the first signs appear, it is necessary to provide the patient with venous access, Trendelenburg, ensure free airway patency. Emergency measures may also be needed: intravenous volume replacement circulating blood, intravenous epinephrine (adrenaline), glucocorticosteroids (for example, 250-1000 mg of methylprednisolone intravenously), antihistamines.

Depending on the severity of the clinical symptoms, Ptake pains cardiopulmonary resuscitation.

Older patients may need a dose reduction (increased bioavailability and reduced elimination rate). Smoking can reduce therapeutic effectiveness of the drug.

It is not recommended to abruptly stop using preparation Pentoxifylline Sandoz®.

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

During the period of drug treatment Pentoxifylline Sandoz® can cause dizziness, headache, visual impairment, therefore, care should be taken when driving vehicles and performing other potentially dangerous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:

Long-acting tablets, 600 mg.

10 tablets are placed in a blister of PP / aluminum foil.

For 3 or 5 blisters are placed in a cardboard box along with instructions for medical use.

Packaging:(10) - blisters (3) - packs cardboard
(10) - blisters (5) - packs of cardboard

Storage conditions:

At a temperature not exceeding 25 ⁰ FROM.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002587

Date of registration:19.08.2014

The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia

Manufacturer: & nbsp

SALUTAS PHARMA, GmbH Germany

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp22.08.2015

Illustrated instructions

Instructions

Pentoxifylline Sandoz® (Pentoxifylline-Sandoz®)