Denebol

General characteristics. Structure:

Active ingredient: 25 mg or 50 mg of a rofekoksib.

Excipients: бетациклодексфрин, starch corn, cellulose microcrystallic, sodium povidone methylparaben (Е 219), sodium propylparaben (Е 217), talc, silicon dioxide colloid anhydrous, magnesium stearate, sodium krakhmalglikolit (type A), dye tartrazine (Е 102), dye diamond (blue) (Е 133), starch corn (dry).

The non-steroidal anti-inflammatory drug having anesthetics, febrifugal, antiinflammatory properties.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug – highly the selection inhibitor of cyclooxygenase-2. Has anesthetics, febrifugal, antiinflammatory properties. TsOG-2 is activated in response to inflammatory process. It leads to synthesis and accumulation of mediators of an inflammation, in particular E 2 prostaglandin that causes an inflammation, hypostasis and pain. Antiinflammatory action of a rofekoksib is carried out due to oppression of synthesis of prostaglandins by TsOG-2 inhibition.

In therapeutic concentration рофекоксиб does not suppress cyclooxygenase-1 (TsOG-1). Thus, it does not influence prostaglandins which are synthesized due to activation of TsOG-1, and owing to it does not interfere with the normal physiological processes connected with TsOG-1 in fabrics, especially in a stomach, an intestinal path and thrombocytes.

Pharmacokinetics. Absorptions. At use inside it is well soaked up, bioavailability of a rofekoksib averages 93%. At daily administration of drug of 1 times a day in a dose of 25 mg the maximum concentration (Cmax) in plasma of adults is defined approximately by 2 h and makes 0,305 mkg/ml.

Distribution. About 85% to a rofekoksib contact in an organism proteins of a blood plasma at concentration of 0,05 - 25 mkg/ml.

Metabolism. The Rofekoksib is metabolized in a liver. The main metabolites do not inhibit TsOG-2.

Conclusion. 72% of drug are removed with urine in the form of metabolites, 14% - with excrements. Plasma clearance at administration of drug in a dose of 25 mg of 1 times a day it is equal to about 120 ml/min.

Indications to use:

Osteoarthritis.

Pseudorheumatism.

Acute pain syndrome of various genesis.

Algodismenorey, dentagra.

In the ambassador the operational period concerning surgical interventions and in stomatology.

Route of administration and doses:

Apply inside the adult.

At treatment of a pain syndrome and primary dysmenorrhea the recommended Denebolu's dose – 50 mg once a day, the subsequent doses – 25 mg or 50 mg once a day as necessary. The maximum daily dose – 50 mg. Treatment is carried out to disappearance of an acute pain syndrome, but by no more than 2 weeks.

Osteoarthritis and pseudorheumatism: the recommended initial dose to a rofekoksib – 12,5 mg once a day which can be increased about 25 mg once a day that is the maximum recommended daily dose. Appoint courses for 4-6 weeks.

Denebol apply irrespective of meal.

Features of use:

Use during pregnancy or feeding by a breast. At pregnancy it is contraindicated. During treatment it is necessary to stop feeding by a breast.

Children. Do not apply to children.

Patients should not appoint Rofekoksib with allergic reactions to acetylsalicylic acid in the anamnesis. Very carefully appoint to patients who in the anamnesis had an ulcer or gastrointestinal bleeding.

Drug is not used for treatment of oncological patients and patients of the raised risk group from cardiovascular system (the postponed heart attacks, strokes, the progressing clinical forms of atherosclerosis). Patients with arterial hypertension, coronary heart disease and congestive heart failure should appoint drug in the conditions of regular control during a course of treatment by the doctor of indicators of arterial pressure, cardiac performance, condition of vessels of a brain and coagulant system of blood.

Patients with the increased risk have disturbances of renal perfusion use to a rofekoksib which inhibits synthesis of prostaglandins, can lead to reduction of a renal blood-groove and deterioration in function of kidneys. The greatest probability of such action is observed at patients with existence in the anamnesis of heavy renal failures, noncompensated heart failure, cirrhosis. At this category of patients during all course of treatment it is necessary to control function of kidneys (clearance, the general secretion). At patients with considerable dehydration prior to therapy it is recommended to carry out a regidratation. Drug can mask fever which is display of an infection that the rofekoksib needs to consider at appointment to patients who apply it at infectious diseases. At a combination therapy with anticoagulants it is necessary to control a prothrombin time. It is not applied as prophylactic of cardiovascular diseases.

Ability and influence on speed of response at control of motor transport or work with other mechanisms. During treatment it is necessary to abstain from driving and performance of the work requiring special attention and bystry reaction.

Side effects:

From cardiovascular system: arterial hypertension, congestive heart failure, hypostases of the lower extremities, disturbances of cerebral and coronary circulation, it is rare – a stroke, a myocardial infarction, disturbances of a cordial rhythm (bradycardia, emergence of a premature ventricular complex, tachycardia), an acute heart failure, a sudden cardiac standstill, an embolism of a pulmonary artery, unstable stenocardia.

Allergic reactions: ангио neurotic hypostasis, fluid lungs, Stephens-Johnson's syndrome, small tortoiseshell, rashes of erythematic type, skin itch, allergic rhinitis, atopic dermatitis, vasculitis.

From a digestive tract: heartburn, dyspepsia, discomfort in epigastric area, nausea, it is rare - aphthous stomatitis. In isolated cases there can be stomach ulcers, intestines, gastrointestinal bleeding.

From gepato-biliary system: hepatitis, liver failure, liver necrosis, increase in level of "hepatic transaminases".

From system of breath: infection of upper respiratory tracts, sinusitis, bronchitis.

From TsNS: headache, concern, depression, hyperesthesia (paresthesia), sleeplessness, fatigue.

From sense bodys: a sight illegibility, conjunctivitis, otitis, a ring in ears.

From an urinary system: renal failure.

From a hemopoiesis: less, than 0,1% of patients have an agranulocytosis, a leukopenia, thrombocytopenia.

Another: alopecia.

Interaction with other medicines:

Increases concentration of a methotrexate in a blood plasma for 23%. Reduces efficiency of hypotensive therapy by APF inhibitors. At simultaneous use with anticoagulants increase in a prothrombin time is possible. Rifampicin, Rifamycinum reduce concentration to a rofekoksib in a blood plasma by 50%. Has no considerable clinical effect on pharmacokinetics of Prednisolonum, hormonal contraceptives for oral administration (ethinylestradiol, норетиндрол), digoxin, antacids, Cimetidinum, a ketokonazol.

Drug is not recommended to be used along with drugs which increase arterial pressure.

Increase in arterial pressure at use along with drugs and foodstuff which contain caffeine is possible.

Contraindications:

Hypersensitivity to a rofekoksib or its components, other NPVS, asthma caused by use acetyl of salicylic acid.

Drug is not used for treatment of oncological patients and patients of the raised risk group from cardiovascular system (the postponed heart attacks, strokes, the progressing clinical forms of atherosclerosis).

Pregnancy, feeding period breast.

Overdose:

Overdose symptoms at conduct of clinical trials were not revealed. Purpose of a dose of a rofekoksib of 1000 mg once a day to healthy participants of a research and a dose on 250 mg a day within 14 days did not reveal serious toxicity.

In case of overdose it is necessary to take the standard measures – a gastric lavage, clinical control and the supporting treatment.

Storage conditions:

To store at a temperature not over 25 ºС in original packaging and the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 1 blister in a cardboard pack together with the application instruction.