Project Description

Diclopentil

international nonproprietary name

Diclofenac sodium, pentoxifylline

Ref

BP-0035

Pharmacotherapeutic group

Non-steroid anti-inflammatory agent. Derivative of acetic acid. Diclofenac in combination with other drugs.

Composition of the preparation

Each tablet contains:

Diclofenac sodium 50 mg, pentoxyfillin 100 mg

Auxiliary subtsances: lactose, low molecular medical polyvinylpyrrolidone, calcium stearate, maize starch, metacrylic acid-ethacrilate co-polymer (1:1) dispersion 30% (collicute), 1,2- propylene glycol, titanium dioxide, medical talc, acird red 2С.

Pharmacological action

Pharmacodynamics

Therapeutic activity of the drug is achieved due to compounds diclofenac and pentoxyfillin.

Diclofenac is anti-inflammatory, analgesic and antipyretic. Inhibiting non-selectively cyclooxigenase-1 and cyclooxigenase-2, diclofenac breaks metabolism of arachidonic acid and inhibits synthesis of anti-inflammatory prostaglandis, prostacyclins and leucotriens. Inhibiting synthesis of thromboxan А2, it inhibits thrombocytes aggregation. In long treatment it is of desensitizing activity.

Pentoxyfillin is antiaggregative, angioprotective and vasorelaxant, it imptoves microcirculation. It inhibits phosphodisterase, stabilizes cyclic adenosine monophosphate and reduces intracellular calcium concentration. It improves blood properties. It enhances therapeutic action of declofenac in articulation diseases.

Due to block of alpha-factor tumor necrosis production it reduces the occurrence of clinical gastropathy that may develop under declofenac treatment.

Pharmacokinetics

Under oral dosage declofenac is completely absorbed. Binding with blood plasma is more than 99%. It easily penetrates in tissues and synovial fluid. It is found in breast milk. Declofenac metabolizes under multiple or single hydroxylation and conjugation with glucoronic acid. Half-excretion period from plasma is 1-2 h., from synovial fluid 3-6 h. Less than 1% of declofenac is renal excreted unmodified. Metabolites are feces excreted (about 35%) and renal excreted (about 65%).

Pentoxyfillin in orald dosage is completely and rapidly absorbed. It is biotransformed intensively under «the first passage» in liver with the formation of two main metabolites: 1-(5-hydroxigexil)−3,7-dimethylxantin и 3-carboxipropil)−3,7-dimethylxantin. It is equally distributed. Half-life period is 0.5-1.5 h. It is mainly renal excreted (94% metabolits). About 4% of pentoxyfillin is feces eliminated. It may be excreted with breast milk.

Indications 

Articulation inflammation: atrophic arthritis, ankylosing spondylitis, acute podagra, chronic gouty arthritis.

Degenerative diseases: osteoarthritis deformans, osteoporosis.

Extraarticular tissue disease: tendonitis, tendinous synovitis, bursitis, periarthritis.

Posttraumatic pain syndromes, accompanied by inflammation, lumbus pain, acute attack of podagra, renal and biliary colic. Control of pain in orthopedic and other minor interventions.

special indication

Effect in driving and risk of operating dangerous mechanisms:due to possible reaction decrease under drug treatment it is not recommended to drive or operate machinery.

Pregnancy and lactation

It is prohibited to administer the drug in pregnancy. If the treatment is necessary, cancel breast feeding.

special warning

Not established

Dosage and method of administration

The drug is administered orally with meals or immediately after meals. In adults diclofenac dosing is 1 tablet 3 times a day. Under therapeutic action the dose is reduced to minim. effective one.

In children after 6, 2 mg/kg calculated on the basis of diclofenac.

overdosage

Symptoms: vertigo, headache, hyperventilation, tachycardia, nausea, vomit, painful stomach, gastrointestinal bleeding, biliary and renal disorder, increase or decrease of arterial pressure, loss of consciousness, in children – convulsions. loss of consciousness

Treatment: gastric lavage and administration of activated carbon, symptomatic therapy (maintaining respiration and arterial pressure either), emergency in bleeding. Artifiialdiuresis, hemodialysisareineffective.

safety measures

In long therapy control biliary, renal and peripheral blood functions.

Administer with care after recent interventions and/or biliary and/or renal insufficiency, lability of arterial pressure, chronic heart failure.

Side effects

Nausea, vomit, anorexia, dry mouth, meteorism, constipation, diarrhea, hepatic disorder, acute condition of chronic cholecystitis, pancreatitis, interstitial nephritis, edema, nephrotic syndrome, headache, vertigo, insomnia, irritability, sensitive and visual imparity, convulsions, fatigability, failure of reaction rate, aseptic meningitis, photosensitization, flash to face skin and upper chest, hematosis distortion, hyper- or hypotenisa, tachycardia, arrhythmia, cardialgia, allergic reactions, rare damage of mucous coat of stomach and intestines.

Contraindications

Hypersensitivity to drug components, to non-steroid anti-inflammatory agents or derivatives of methylxantine, erosion-ulcer damage of gastrointestinal tract in acute conditions, aspirin asthma, aspirin triad (combination of asthma, recurrent nasal and paranasal sinus polyposis and intolerance of acetylsalicylic acid and pyrazolone group), hematosis distortion (leucopenia and anemia), coagulation disorder, bleeding (recent ones either), hemorrhagic stroke, retina hemorrhage, acute myocardial infarction, marked atherosclerosis of coronary arteries, children under 6, pregnancy, lactation (breast feeding shall be cancelled during the treatment).

Interactions with other medicinal preparations

It increases blood concentration of lithium, digoxin, antidiabetic agents, quinalone derivatives. It increases the toxicity of methotrexate, gold preparations and cyclosporine. It decreases the action of soporific agents and diuretics. It increases risk of hyperkalemia against potassium-sparing diuretics. It may increase the effect of the drugs influencing on coagulation (direct and indirect anticoagulants, thrombolitics), antibiotics (cephalosporins inclusive: cephamandol, cephaperason, cephatetan), valproetic acid. Concurrent administration of xantines may result in excessive irritation.

Plasma concentration of diclofenac is reduced under acetylsalicylic acid administration. Cymetidinencreasesplasmaconcentrationofpentoxyfillinе.

The form of release

10 tablets in blister of PVC. 3 blisters with instruction for usage in a pack of box cardboard.