Diklopentil

General characteristics. Structure:

Active ingredients: 50 mg of diclofenac of sodium, 100 mg of a pentoksifillin.

Excipients: lactose monohydrate, K-25 povidone, calcium stearate, starch corn, acryle - from 93A (methacrylic acid copolymer, talc, titanium dioxide, silicon dioxide colloid anhydrous, sodium bicarbonate, a carmine, sodium lauryl sulfate), triethyl citrate.

Pharmacological properties:

Pharmacodynamics. Therapeutic effect of drug is caused being its part diclofenac and pentoksifilliny.

Diclofenac has antiinflammatory, analgeziruyushchy and febrifugal effect. Not selectively oppressing cyclooxygenase-1 and cyclooxygenase-2, diclofenac breaks metabolism of arachidonic acid and by that suppresses synthesis of pro-inflammatory prostaglandins, prostacyclins and leukotrienes. Inhibiting A2 thromboxane synthesis, oppresses aggregation of thrombocytes. At prolonged use has the desensibilizing effect.

Pentoksifillin has anti-aggregation, angioprotektivny and vasodilating effect, improves microcirculation. Inhibits phosphodiesterase, stabilizes tsAMF and reduces concentration of intracellular calcium. Improves rheological properties of blood. Strengthens therapeutic effect of diclofenac at diseases of joints. Due to blocking of products of an alpha factor of a necrosis of a tumor reduces the frequency of a medicinal gastropathy which can arise at diclofenac use.

Pharmacokinetics. At intake diclofenac is soaked up almost completely. Linkng with proteins of a blood plasma – more than 99%. Well gets into fabrics and synovial fluid. It is found in breast milk. Metabolism of diclofenac results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. Plasma elimination half-life makes 1-2 h, of synovial fluid – 3-6 h. Less than 1% of diclofenac are removed through kidneys in an invariable look. Metabolites eliminirutsya with a stake (about 35%) and with urine (about 65%).

Pentoksifillin at intake is quickly and completely soaked up. Intensively it biotransformirutsya at "the first passing" through a liver with formation of two main metabolites: 1-(5 hydroxyhexyl) - 3,7 dimethylxantines and 1-(3 carboxypropyl) - 3,7 dimethylxantines. It is distributed evenly. The elimination half-life makes 0,5-1,5 h. It is removed preferential by kidneys (94% in the form of metabolites). With excrements about 4% of a pentoksifillin eliminirutsya. It can be excreted with breast milk.

Indications to use:

Inflammatory diseases of joints: the pseudorheumatism ankylosing a spondylitis, acute gout, chronic gouty arthritis.

Degenerative diseases: the deforming osteoarthrosis, osteoporosis.

Diseases of extraarticular fabrics: the tendinitis, tenosinovit, a bursitis, a periarthritis.

The posttraumatic pain syndromes which are followed by an inflammation, back pains, a bad attack of gout, renal and hepatic colic. Control of pain and an inflammation at orthopedic and other small surgical interventions.

Route of administration and doses:

Drug is accepted inside during food or directly after food. The adult diklopentit appoint on 1 tablet 3 times a day. At development of therapeutic action the dose is reduced to minimum, rendering effect

To children at the age of 6 years drug is also more senior appoint in a dose 2 mg/kg/days in terms of diclofenac.

Features of use:

Influence on ability to drive the car and potentially dangerous mechanisms: because of a possibility of reduction in the rate of reaction during administration of drug it is not recommended to manage vehicles and the machine equipment.

Pregnancy and period of a lactation. It is impossible to appoint drug during pregnancy. In need of administration of drug feeding by a breast should be stopped.

Side effects:

Nausea, vomiting, anorexia, dizziness, excitement, sleeplessness, irritability, dryness in a mouth, a meteorism, a lock, diarrhea, an abnormal liver function, an exacerbation of chronic cholecystitis, pancreatitis, intersticial nephrite, hypostases, a nephrotic syndrome, a headache, disturbances of sensitivity of sight, a spasm, fatigue, disturbance of speed of response, aseptic meningitis, a photosensitization, "inflows" of blood to face skin and an upper part of a thorax, hemopoiesis disturbance, increase or lowering of arterial pressure, tachycardia, arrhythmia, a cardialgia, allergic reactions, in rare instances – defeat mucous a stomach and intestines.

Interaction with other medicines:

Increases concentration in blood of drugs of lithium, digoxin, antidiabetic medicines, hinolonovy derivatives. Increases toxicity of a methotrexate, drugs of gold and cyclosporine. Reduces efficiency of action of hypnagogues and diuretics. Increases risk of a hyperpotassemia against the background of use of kaliysberegayushchy diuretics. Can strengthen effect of the medicines influencing coagulant system of blood (indirect and direct anticoagulants, trombolitik), antibiotics (including cephalosporins – a tsefamandol, a tsefaperazon, a tsefotetan), valproic acid. Joint appointment with xanthines can lead to excessive nervous excitement.

Concentration of diclofenac in plasma decreases at use of acetylsalicylic acid. Cimetidinum increases concentration of a pentoksifillin in plasma.

Contraindications:

Hypersensitivity to drug components, non-steroidal anti-inflammatory drugs or derivatives of methylxanthine, digestive tract erosive cankers in an aggravation phase, "aspirinovy" asthma, a "aspirinovy" triad (a combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid and drugs of a pyrazolon row), hemopoiesis disturbance (a leukopenia and anemia), various disturbances of coagulability of blood, bleeding (including recent), a hemorrhagic stroke, an eye retinal apoplexy, an acute myocardial infarction, the expressed atherosclerosis of coronary arteries, children's age up to 6 years, pregnancy, the lactation period (feeding by a breast for treatment should be stopped).

Overdose:

Symptoms: dizziness, a headache, a hyperventilation, tachycardia, a hyperthermia, nausea, vomiting, pains in a stomach, gastrointestinal bleedings, an abnormal liver function and kidneys, increase or lowering of arterial pressure, a loss of consciousness, children have spasms.

Treatment: a gastric lavage with the subsequent reception of absorbent carbon, symptomatic therapy (including the measures directed to maintenance of breath and arterial pressure), urgent actions at bleeding. The artificial diuresis, a hemodialysis are ineffective.

Storage conditions:

In the place protected from moisture and light at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets kishechnorastvorimy 50 mg / 100 mg in a blister strip packaging No. 10х3.