Rofecoxibe

Chemical name

4-[4-(Метилсульфонил)фе��ил]-3-фенил-2(5H)-фуранон

Gross

C17-H14-O4-S

Characteristics

Powder white or belovato-jeltovatogo color. Poor soluble in acetone, very soluble in methanol and izopropilazette very little soluble in ethanol, practically nerastvorim in oktanole, nerastvorim in water.

Of drugs

Drugs, the anti-inflammatory, analgezirutee, analgesic. Vsokospecificno ingibiruet ziklooksigenzu-2, hampering education противовоспалительны х prostaglandines. At therapeutic concentrations in humans does not affect the activity Ziklooksigenaza-1.pri a pregnant rats doses, twice exceeding the recommended daily dose for a person who was a decrease in arterial diameter (Botallowa) flow from the fruit. The studies reproductive function in rats and rabbits in a dose exceeding the recommended daily dose for a person of 29 and 2 times, respectively, there was no congenital abnormalities in Potomstwa.posle intake of a well-absorbed from the digestive tract, bioavailability over 90%. Cvazavanie with plasma protein-about 90%. C_max achieved in 2 hours Treated biotransformation in the liver with the formation of six inactive metabolites. Report mostly kidneys (72% of active metabolites, less than 1% in an unmodified form) and faeces (14% in an unmodified form). Plasma klirens about 120 ml / min.

Indications

Osteoarthritis (acute, chronic), mild pain syndrome, the treatment of primary dismenorei.

Restrictions on the use of

Ill information on the development of asthma attacks, Urticaria or other allergic reactions to the reception salicilatov or other NPVS; Kidney failure, with klirense creatinine less than 30 ml / min (no clinical experience with the application of this category of patients), moderate or expressed by the human liver,'s age (safety and efficacy of the children are not identified).

Pregnancy and lactation

Counter in the third trimester of pregnancy (perhaps premature Bamyan Botallowa flow in the foetus). Possibly in I and II trimestrah pregnancy, if the effect of therapy in the mother outweighs the potential risk to the fetus (adequate and well-controlled studies have not been carried out). At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, incl. from other NPVS, pregnancy, breast-feeding.

Side-Effects

From the nervous system and sensory organs : dizziness, drowsiness, and the weakening of speed thinking sputannosti consciousness Galloucination.so the circulatory system and blood (blood, gemostaz) :> 2% arterial hypertension; Female cardiac Nedostaternsti.so part of the intestine :> 2% aches, nausea, diarrhoea, neuralgia, discomfort in epigastralna area; Vomiting; in a few cases, izgyazwlenia mucous membrane of Rta.so the urogenital system : forming decrease kidney function, including kidney �едостаточность.Аллер гические reactions : angioneuroticeski swelling, itching, rash, and urticaria Dr.prochie :> 2% swelling lower limbs; > 1% increase in ALT and / or AST.

Patient interaction

It may raise the concentration of methotrexate in the blood. Together with the admission varfarinom increased protrombinovoe time. Rifampicin reduces concentration in plasma by 50%.

Precautions

To use caution in patients with the disease azvennouu stomach and duodenal ulcers in the history, if there is swelling, nekompensirovanna heart failure, cirrhosis of the liver, in patients over 65 years of age. Against the backdrop of concerns kidney or liver failure should be carefully monitor kidney function / pecheni. In patients with dehydration desirable rehydration prior to the start of treatment.

Dosing and Administration

Inside, at the time of delivery or regardless of the reception Pishchi.osteoartrit : initial dose of 12.5 mg once a day, if necessary, 25 mg (the maximum daily intake). Severe acute pain and treatment of primary dismenorei : initial dose of 50 mg once a day, then 25 to 50 mg once a day, maximum daily dose is 50 mg.

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