Pharmacological action of Celebrex

NSAIDs. It is a selective inhibitor of COX-2, thereby blocking the formation of inflammatory prostanoids.

At therapeutic concentrations in humans, celecoxib does not inhibit COX-1; therefore, it does not affect prostanoids synthesized by COX-1 activation.

Criteria for determining the specificity for COX-2 include the absence of side effects due to the action of COX-1, especially ulcerative lesions of the stomach and duodenum, serious complications from the upper gastrointestinal tract (bleeding, perforation, obstruction of the pyloric foramen) and the absence of inhibition of COX -2-dependent platelet aggregation activity.

Indications of the active substances of the drug Celebrex

Symptomatic treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis.

Dosage regimen of Celecoxib

When taken orally for adults, the dose is 200 mg / day in 1-2 doses, if necessary - 200 mg 2 times / day.

Elderly patients weighing less than 50 kg or with moderate liver dysfunction, treatment should be started with the minimum recommended dose.

There is no clinical experience with celecoxib in patients with severe hepatic or renal impairment.

Contraindications for use

Severe renal dysfunction, severe liver dysfunction; history of allergic reactions to acetylsalicylic acid or other NSAIDs, III trimester of pregnancy, lactation (breastfeeding); hypersensitivity to sulfonamides, hypersensitivity to celecoxib.

Use in pregnancy and lactation 

There have been no adequate and well-controlled studies of the safety of celecoxib during pregnancy, so its use is not recommended.

If necessary, use during lactation should decide on the termination of breastfeeding.

In experimental studies, no toxic effect on the fetus was found; it has been shown that in animals the concentration of celecoxib in breast milk is close to that in plasma.

Application for violations of liver function

Contraindicated in severe violations of liver function.

Application for impaired renal function

Contraindicated in severe renal impairment.

Use in elderly patients

Elderly patients weighing less than 50 kg or with moderate impairment of liver function, treatment should be started with the minimum recommended dose.

Special instructions

Precautions should be used in patients with heart failure and other conditions that predispose to fluid retention. Application in patients with gastric ulcer or duodenal ulcer is possible only in case of complete remission of the disease; with severe renal and hepatic insufficiency - only in exceptional cases.

There is no clinical experience with celecoxib in patients with severe hepatic or renal dysfunction, as well as in patients under 18 years of age.

Drug interaction

With simultaneous use with drugs that inhibit the activity of the isoenzyme CYP2C9, incl. with fluconazole, a significant increase in plasma celecoxib concentration is possible. Antacids (aluminum and magnesium) reduce the absorption of celecoxib by 10%, which does not cause clinically significant effects. With the simultaneous use of celecoxib with warfarin, the risk of bleeding increases.

Side effect

Often (≥ 1% and <10%)

General reactions: exacerbation of allergic diseases, flu-like syndrome, accidental injury.

On the part of the cardiovascular system: peripheral edema.

From the digestive system: abdominal pain, diarrhea, dyspepsia, flatulence, dental disease (postextraction alveolitis).

From the nervous system: dizziness, increased muscle tone, insomnia.

From the urinary system: urinary tract infection.

From the respiratory system: bronchitis, cough, pharyngitis, rhinitis, sinusitis, upper respiratory tract infections.

On the part of the skin: itching, skin rash.

Uncommon (≥ 0.1% and <1%)

General reactions: facial edema.

From the hematopoietic system: anemia, ecchymosis, thrombocytopenia.

On the part of the cardiovascular system: aggravation of the course of arterial hypertension, increased blood pressure, arrhythmia, hot flashes, palpitations, tachycardia.

From the senses: tinnitus, blurred vision.

From the digestive system: vomiting.

From the nervous system: anxiety, drowsiness.

From the side of the skin: alopecia, urticaria.

Rarely (≥ 0.01% and <0.1%)

From the side of the cardiovascular system: manifestation of congestive heart failure, ischemic stroke and myocardial infarction.

From the digestive system: gastric and duodenal ulcers, ulceration of the esophagus, intestinal perforation, pancreatitis, increased activity of liver enzymes.

Allergic reactions: angioedema, bullous rash.

From the nervous system: confusion.

Adverse reactions identified during post-marketing observations

Allergic reactions: anaphylaxis.

From the nervous system: hallucinations, aseptic meningitis.

From the senses: loss of taste, loss of smell.

From the side of the cardiovascular system: vasculitis, cerebral hemorrhage.

From the digestive system: gastrointestinal bleeding, hepatitis, liver failure, fulminant hepatitis, liver necrosis, cholestasis, cholestatic hepatitis, jaundice.

From the urinary system: acute renal failure, interstitial nephritis, nephrotic syndrome, minimal renal dysfunction.

On the part of the skin: photosensitization, peeling of the skin (including with erythema multiforme and Stevens-Johnson syndrome), toxic epidermal necrolysis, drug rash in combination with eosinophilia and systemic symptoms (DRESS or hypersensitivity syndrome), acute generalized exanthematous pustulosis.

From the reproductive system: menstrual irregularities, decreased fertility in women.

From the respiratory system: pulmonary embolism.

Others: hyponatremia, chest pain.