Buy Celebrex capsules 400 mg 1 pc. + 200 mg 5 pcs packaging
  • Buy Celebrex capsules 400 mg 1 pc. + 200 mg 5 pcs packaging

Celebrex® [Celecoxib]

Pfizer
1832 Items
2019-09-19
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Clinical Pharmacology

Celebrex - NSAIDs. Specific inhibitor of cyclooxygenase-2 (COX-2).
COX-2 is induced in response to the inflammatory process. This leads to the synthesis and accumulation of inflammatory prostanoids, in particular, prostaglandin E2that causes inflammation, swelling and pain. The anti-inflammatory effect of the drug is accomplished by blocking the production of inflammatory prostanoids by inhibiting COX-2.
Data from in vivo and ex vivo studies indicate that celecoxib has a very low affinity for the cyclooxygenase-1 enzyme (COX-1). Therefore, when used in therapeutic doses, celecoxib has no effect on prostaglandins synthesized as a result of COX-1 activation, and therefore does not affect the normal physiological processes associated with COX-1 in tissues, especially in the tissues of the stomach, intestines and platelets.

Indications

- osteoarthritis;
- rheumatoid arthritis;
- pain syndrome of various etiologies (including postoperative, toothache, menstrual, bone and muscle pain).

Composition

1 capsule contains:

Active substance: celecoxib

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Celebrex® [Celecoxib]

Dosage and Administration

Adults withosteoarthrosis Celebrex drug is prescribed in a daily dose of 200 mg in 1 or 2 doses. In clinical studies, doses up to 400 mg / day were used.
Withrheumatoid arthritis the drug is prescribed in a daily dose of 200-400 mg, divided into 2 doses. In clinical studies, doses up to 800 mg / day were used.
Withpain syndrome The recommended single dose is 100-200 mg. If necessary, subsequent use of the drug in the same dose is possible with an interval between doses of at least 4-6 hours until a maximum daily dose of 400 mg is reached.
Withacute pain and algomenorrhea the recommended initial dose is 400 mg, then, if necessary, another dose of the drug at a dose of 200 mg is possible; the maximum dose on the first day of treatment is 600 mg / day; in the following days, the daily dose of the drug can vary from 200 mg to 400 mg.
The use of Celebrex in patients under the age of 18 has not been studied.

Adverse reactions

From the digestive system: often - abdominal pain, diarrhea, dyspepsia; rarely - nausea, vomiting, heartburn, anorexia; with long-term use in high doses - ulceration of the gastrointestinal mucosa, bleeding, NSAID-gastropathy, constipation, flatulence, increased activity of AST and ALT.
From the side of the central nervous system and peripheral nervous system: rarely - headache, dizziness, drowsiness or insomnia, blurred vision, depression, agitation, confusion, anxiety, hallucinations, hearing loss, tinnitus.
On the part of the respiratory system: rarely - sore throat, cough, shortness of breath, bronchospasm.
From the urinary system: rarely - renal failure, edematous syndrome.
From the hemopoietic system: rarely - agranulocytosis, anemia, leukopenia, thrombocytopenia.
Since the cardiovascular system: rarely - arterial hypertension, arrhythmia, hot flashes, palpitations, congestive heart failure, tachycardia.
Allergic reactions: bullous skin rash, angioedema, bronchospasm, anaphylaxis, vasculitis, erythema multiforme, Stevens-Johnson syndrome.
Other: alopecia, increased sweating, nosebleeds. There are separate reports of acute pancreatitis.

Contraindications

- history of allergic reactions (urticaria, bronchospasm) associated with taking acetylsalicylic acid or other NSAIDs;
- pronounced impaired renal function;
- severe liver dysfunction;
- III trimester of pregnancy;
- lactation (breastfeeding);
- known hypersensitivity to sulfonamides;
- Hypersensitivity to the drug.

Drug interactions

With simultaneous use of Celebrex with a CYP2C9 inhibitor fluconazole, an increase in plasma celecoxib concentration is possible (celecoxib should be used at the lowest recommended dose).
It has been established in vitro that celecoxib is a CYP2D6 inhibitor, so there is a possibility of drug interaction with other drugs that biotransform with the participation of this isoenzyme.
Antacids (aluminum and magnesium) reduce celecoxib absorption by 10%, which does not cause clinically significant effects.
When studying the effect of Celebrex on the pharmacokinetics and / or pharmacodynamics of substrates of CYP2C9 glyburide, glibenclamide, tolbutamide in vivo, no clinically significant interaction was found.
In vitro studies have established that CYP2C19 isoenzyme can participate in celecoxib metabolism only to a minor extent. In an in vivo study, multiple doses of celecoxib (200 mg 2 times / day for 7 days) did not affect the clearance of a single dose of the substrate of CYP2C19 phenytoin. The risk of clinically significant inhibition of substrate metabolism by CYP2C19 by celecoxib is considered to be insignificant.
With the combined use of Celebrex with warfarin and similar drugs, an increase in prothrombin time and the development of serious bleeding is possible (it is necessary to monitor clotting indicators and apply precautions).
No clinically significant interaction of celecoxib with ketoconazole, lithium preparations, methotrexate was detected.

Pregnancy and Lactation

Use of the drug Celebrex during pregnancy (especially in the third trimester) is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. If necessary, the use of Celebrex during lactation should decide on the termination of breastfeeding.

Special instructions

Shouldcarefully use Celebrex in gastric ulcer or duodenal ulcer, ulcerative colitis, heart failure, edematous 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 the prophylactic treatment of cardiovascular disorders.
With a decrease in CYP2C9 activity, Celebrex should be administered with caution, since in this case plasma celecoxib levels may increase excessively.
Control of laboratory parameters
During the use of the drug is necessary to control the picture of peripheral blood and laboratory parameters of liver and kidney function.
If necessary, determine the 17-ketosteroids drug should be canceled 48 hours before the study.
Use in Pediatrics
Clinical data on the efficacy and safety of Celebrex in children and adolescents under the age of 18 are not available.
Influence on ability to drive motor transport and control mechanisms
The question of the possibility of practicing potentially hazardous activities requiring increased attention and quickness of psychomotor reactions should be resolved only after evaluating the patient's individual response to the drug.

Overdosage

There is no clinical experience in overdose. Healthy volunteers took once up to 1200 mg and many times up to 1200 mg 2 times / day without clinically significant adverse effects.
Treatment: conduct symptomatic therapy. Hemodialysis is ineffective.

  • Brand name: Celebrex
  • Active ingredient: Celecoxib
  • Dosage form: Capsules
  • Manufacturer: Pfizer
  • Country of Origin: USA

Studies and clinical trials of Celecoxib (Click to expand)

  1. Chemopreventive activity of celecoxib, a specific cyclooxygenase-2 inhibitor, and indomethacin against ultraviolet light–induced skin carcinogenesis
  2. Characterization of metabolites of Celecoxib in rabbits by liquid chromatography/tandem mass spectrometry
  3. Evaluation of health-related quality of life of rheumatoid arthritis patients treated with celecoxib
  4. Efficacy of celecoxib, a cyclooxygenase 2–specific inhibitor, in the treatment of ankylosing spondylitis: A six-week controlled study with comparison against placebo and against a conventional nonsteroidal antiinflammatory drug
  5. Antitumor effects of celecoxib on K562 leukemia cells are mediated by cell-cycle arrest, caspase-3 activation, and downregulation of Cox-2 expression and are synergistic with hydroxyurea or imatinib
  6. Trial of celecoxib in amyotrophic lateral sclerosis
  7. The safety of celecoxib in patients with aspirin-sensitive asthma
  8. Induction of apoptosis in rheumatoid synovial fibroblasts by celecoxib, but not by other selective cyclooxygenase 2 inhibitors
  9. The cost effectiveness of rofecoxib and celecoxib in patients with osteoarthritis or rheumatoid arthritis
  10. More pronounced inhibition of cyclooxygenase 2, increase in blood pressure, and reduction of heart rate by treatment with diclofenac compared with celecoxib and rofecoxib
  11. Do proton-pump inhibitors confer additional gastrointestinal protection in patients given celecoxib?
  12. Celecoxib for lupus
  13. Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats
  14. Pharmacokinetics of a combination of Δ9-Tetrahydro-cannabinol and celecoxib in a porcine model of hemorrhagic shock
  15. Investigation of the pharmacokinetics of celecoxib by liquid chromatography–mass spectrometry
  16. Celecoxib determination in different layers of skin by a newly developed and validated HPLC-UV method
  17. Simultaneous quantitation of etoricoxib, salicylic acid, valdecoxib, ketoprofen, nimesulide and celecoxib in plasma by high-performance liquid chromatography with UV detection
  18. Nitrooxymethyl-Substituted Analogues of Celecoxib: Synthesis and Pharmacological Characterization
  19. ChemInform Abstract: Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors: Identification of 4-(5-(4-Methylphenyl)-3- (trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide (SC-58635, Celecoxib).
  20. Polar Substitutions in the Benzenesulfonamide Ring of Celecoxib Afford a Potent 1,5-Diarylpyrazole Class of COX-2 Inhibitors.
  21. ChemInform Abstract: Isomeric Acetoxy Analogues of Celecoxib and Their Evaluation as Cyclooxygenase Inhibitors.
  22. Pilot study of celecoxib and infusional 5-fluorouracil as second-line treatment for advanced pancreatic carcinoma
  23. Phase II trial of irinotecan plus celecoxib in adults with recurrent malignant glioma

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