Celecoxib has anti-inflammatory, analgesic and antipyretic effects by blocking the formation of inflammatory prostaglandins (Pg) mainly by inhibiting cyclooxygenase-2 (COX-2). Induction of COX-2 occurs in response to inflammation and leads to the synthesis and accumulation of prostaglandins, especially prostaglandin E2, with increased manifestations of inflammation (edema and pain). In human therapeutic doses, celecoxib does not significantly inhibit cyclooxygenase-1 (COX-1) and has no effect on prostaglandins synthesized as a result of COX-1 activation, and does not affect normal physiological processes connected with COX-1 and running in tissues, especially in stomach, intestine and platelet tissues.
The effect on renal function
Celecoxib reduces urinary excretion of PgE2 and 6-keto-PgF1(prostacyclin metabolite), but has no effect on serum thromboxane B2 and urinary excretion of 11-dehydro-thromboxane B2, a metabolite of thromboxane (both COX-1 products). Celecoxib does not cause decreased glomerular filtration rate (GFR) in elderly patients and those with chronic renal insufficiency, transiently decreases sodium excretion. In patients with arthritis, the observed incidence of peripheral edema, arterial hypertension and heart failure is comparable to that of non-selective COX inhibitors, which have inhibitory activity against COX-1 and COX-2. This effect was most pronounced in patients treated with diuretics. However, there was no increase in the incidence of BP and heart failure, and peripheral edema was mild and resolved spontaneously.
Painful menstruation (algodysmenorrhea), Osteochondrosis, Joint pain (arthralgia), Neck pain, Lumbago, Radiculitis, Back pain, Osteoarthritis, Arthritis, Rheumatoid arthritis, Pain, Arthrosis, Sciatica, Pain after injuries and operations – osteoarthritis;
– Rheumatoid arthritis;
– pain syndrome of various etiologies (including postoperative, dental and osteoarthritis).Pain syndrome of different etiologies (including postoperative, toothache, menstrual, bone and muscle pain).
1 capsule contains:
The active ingredient: celecoxib
How to take, the dosage
In adults with osteoarthritis, Celebrex is prescribed in a daily dose of 200 mg in 1 or 2 doses. Doses of up to 400 mg/day have been used in clinical trials.
In rheumatoid arthritis the drug is prescribed in a daily dose of 200-400 mg divided into 2 doses. Doses up to 800 mg/day have been used in clinical trials.
In pain syndrome a single dose of 100-200 mg is recommended. If necessary, a subsequent use in the same dose is possible with an interval of at least 4-6 hours between doses up to a maximum daily dose of 400 mg.
In acute pain and algodysmenorrhea the recommended initial dose is 400 mg followed, if necessary, by another 200 mg dose; the maximum dose on the first day of treatment is 600 mg/day; the daily dose may vary from 200 mg to 400 mg in subsequent days.
The use of Celebrex in patients under 18 years of age has not been studied.
Simultaneous use of Celebrex with CYP2C9 inhibitor fluconazole may increase the concentration of celecoxib in plasma (celecoxib should be used in the lowest recommended dose).
It was established in vitro that celecoxib is a CYP2D6 inhibitor, so there is a possibility of drug interaction with other drugs that are biotransformed with participation of this isoenzyme.
Antacids (aluminum and magnesium) decrease the degree of absorption of celecoxib by 10%, which does not cause clinically significant effects.
When studying the effect of celebrex on pharmacokinetics and/or pharmacodynamics of CYP2C9 substrates gliburide, glibenclamide, tolbutamide in vivo clinically significant interaction was not observed.
In in vitro studies it was found that CYP2C19 isoenzyme may participate in the metabolism of celecoxib only to a small extent. In an in vivo study, multiple doses of celecoxib (200 mg 2 times daily for 7 days) did not affect the clearance of a single dose of the CYP2C19 substrate phenytoin. The risk of clinically significant inhibition of CYP2C19 substrate metabolism by celecoxib is considered to be insignificant.
Co-administration of celecoxib with warfarin and similar drugs may increase prothrombin time and develop serious bleeding (coagulation rates should be monitored and precautions should be taken).
No clinically significant interaction of celecoxib with ketoconazole, lithium drugs, methotrexate was found.
Caution should be exercised when using Celebrex in gastric or duodenal ulcer disease, ulcerative colitis, heart failure, edema syndrome, arterial hypertension.
Celebrex can be used with low doses of acetylsalicylic acid. Due to the lack of action on platelets Celebrex does not replace acetylsalicylic acid in prophylactic treatment of cardiovascular disorders.
Caution should be exercised when CYP2C9 activity is decreased, because in this case the plasma level of celecoxib may be excessively elevated.
Control of laboratory parameters
During the use of the drug the peripheral blood count and laboratory parameters of liver and kidney function should be monitored.
If it is necessary to determine 17-ketosteroids the drug must be discontinued 48 hours before the study.
Clinical data on the effectiveness and safety of Celebrex in children and adolescents under 18 years of age are absent.
Effect on the ability to drive and operate machinery
The question on the possibility to engage in potentially dangerous activities that require increased attention and rapid psychomotor reactions should be decided only after assessing the individual patient’s reaction to the drug.
– history of allergic reactions (urticaria, bronchospasm) associated with taking acetylsalicylic acid or other NSAIDs;
– marked renal dysfunction;
– marked liver dysfunction;
– III trimester of pregnancy;
– lactation (breast-feeding);
– known hypersensitivity to sulfonamides;
– hypersensitivity to the drug components.
The digestive system: often – abdominal pain, diarrhea, dyspepsia; rarely – nausea, vomiting, heartburn, anorexia; with long-term use in high doses – gastrointestinal mucosa ulceration, bleeding, NSAID gastropathy, constipation, flatulence, increased AST and ALT activity.
CNS and peripheral nervous system: rarely – headache, dizziness, somnolence or insomnia, blurred vision, depression, agitation, confusion, anxiety, hallucinations, decreased hearing, tinnitus.
Respiratory system: rarely – sore throat, cough, shortness of breath, bronchospasm.
Urinary system: rarely – renal failure, edema syndrome.
Blood system: rare – agranulocytosis, anemia, leukopenia, thrombocytopenia.
Cardiovascular system: rare – arterial hypertension, arrhythmia, hot flashes, palpitations, congestive heart failure, tachycardia.
Allergic reactions: bullous skin rash, angioneurotic edema, bronchospasm, anaphylaxis, vasculitis, erythema multiforme, Stevens-Johnson syndrome.
Other: alopecia, increased sweating, nosebleeds. There are separate reports of acute pancreatitis.
There is no clinical experience with overdose. Healthy volunteers took once-daily up to 1200 mg and repeatedly up to 1200 mg 2 times/day without clinically significant adverse effects.
Treatment: symptomatic therapy is administered. Hemodialysis is ineffective.
|Conditions of storage|
The drug should be stored in a dry place out of the reach of children at temperatures from 15° to 30°C. The drug should be stored in a dry place out of the reach of children at temperatures from 15° to 30°C.
Pfizer, Puerto Rico
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