drugs

CELEBREX ® Celecoxib

CELEBREX ® is a celecoxib drug

THERAPEUTIC GROUP: Non-steroidal anti-inflammatory and antirheumatic drugs

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications CELEBREX ® Celecoxib

CELEBREX ® is a selective non-steroidal anti-inflammatory drug used in the symptomatic treatment of rheumatic inflammatory conditions such as osteoarthritis, ankylosing spondylitis and rheumatoid arthritis.

Mechanism of action CELEBREX ® Celecoxib

Celecoxib, the active ingredient in CELEBREX ®, is a non-steroidal anti-inflammatory drug, capable of selectively inhibiting the isoform 2 of cyclooxygenases.

Taken orally it is rapidly absorbed by the gastro-enteric mucosa, reaching maximum plasma concentrations in about 2 -3 hours, to be subsequently distributed to the various tissues, thanks to the binding with plasma proteins.

After a half-life of approximately 8 - 12 hours and an intense hepatic metabolism supported by the cytochrome CYP2C9, celecoxib, in the form of inactive catabolites, is predominantly eliminated via the kidney.

From the pharmacodynamic point of view, on the other hand, celecoxib, obtained from pyrazoles through a series of chemical variations, is able to recognize and selectively bind the specific pocket of cyclooxygenase 2, exerting an inhibitory action directed exclusively towards these enzymes.

This activity results in a balance of the biological activity of the active ingredient, which can therefore block the chemical pathway that leads to the formation of prostanoids involved in the genesis of inflammation, pain and edema, without affecting the normal activity of the constitutively expressed cyclooxygenases (COX1) mainly in the gastro-enteric mucosa, important in the protection of the gastric mucosa, in the regulation of renal homeostasis and in the control of the sleep-wake rhythm.

From a therapeutic point of view the aforementioned molecular mechanisms result in a good anti-inflammatory and anti-edema activity, and in a modest gastro-injurious activity.

Studies carried out and clinical efficacy

1. THE CELECOXIB IN RHEUMATIC DISEASES

Drugs. 2011 Dec 24; 71 (18): 2457-89.

Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.

Very interesting review that evaluates the efficacy of celecoxib in the treatment of inflammatory pain present in pathologies such as rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. More precisely, this active ingredient should be considered as a therapeutic approach of first choice in patients suffering or predisposed to the development of diseases affecting the gastro-intestinal tract.

2. THE CELECOXIB IN THE CONTROL OF POST-OPERATIVE PAIN

Cochrane Database Syst Rev. 2012 Mar 14; 3: CD004233.

Single oral dose celecoxib for acute postoperative pain in adults.

Study demonstrating that the single oral dose of celecoxib 400 mg may be effective in reducing pain following major surgery, reducing the side effects commonly associated with conventional non-selective NSAID therapies.

3. THE CELECOXIB IN THE PREVENTION OF COLORECTAL ADENOMES

Cancer Prev Res (Phila). 2009 Apr; 2 (4): 310-21. Epub 2009 Mar 31.

Five-year efficacy and safety analysis of the Adenoma Prevention with CelecoxibTrial.

Very interesting clinical trial that shows after 5 years of experimentation the efficacy of the intake of 400 mg daily of celecoxib, in the prevention of the formation of colorectal adenomas, despite the increased cardiovascular risk documented in patients with pre-existing atherosclerotic disease.

Method of use and dosage

CELEBREX ®

Opaque 200 mg capsules of celecoxib.

The normal dosing schedule for the treatment of inflammatory diseases on a rheumatic basis involves the intake of 200 mg of celecoxib per day, preferably divided into two distinct moments.

If the aforementioned dosage proves to be ineffective, after consulting your doctor, you could increase the overall amount of celecoxib to 400 mg daily, always divided into two different assumptions.

Further adjustment of standard doses should be provided for elderly patients or those with liver and kidney disease.

Warnings CELEBREX ® Celecoxib

CELEBREX ® therapy, given the potential side effects, should be supervised by your doctor, who in turn should periodically monitor the degree of liver, kidney and cardiovascular function.

Treatment with celecoxib should also be understood as a short-term therapy, useful for overcoming the pain symptomatology that is observed during inflammatory joint diseases, avoiding prolonging the administration of the drug over a few days, given the greater incidence of side effects.

CELEBREX ® should be administered with particular care in patients suffering from gastro-intestinal, cardiovascular, hepatic and renal diseases due to their increased susceptibility to the side effects typical of selective NSAID therapy.

The same care should be reserved for all those atopic patients, given the significant allergenic power of celecoxib.

The possible appearance of side effects, should alarm the patient, who after consulting his doctor could consider the possibility of suspending the therapy in progress.

CELEBREX ® contains lactose, therefore it is not recommended in patients with lactose intolerance, lactase enzyme deficiency or glucose-galactose malabsorption syndrome.

Given the ability of celecoxib to induce dizziness, vertigo and drowsiness, it would be advisable to avoid driving cars or using machines after taking CELEBREX ®.

PREGNANCY AND BREASTFEEDING

The use of CELEBREX ® in pregnancy is contraindicated due to the absence of significant clinical trials able to characterize the safety profile of celecoxib for fetal health, and given the results of numerous experimental studies demonstrating the toxicity of this active ingredient for the fetus.

The contraindications also extend to the subsequent breastfeeding period, given the ability of celecoxib to accumulate in breast milk in clinically relevant quantities.

Interactions

Known hepatic metabolism of celecoxib, which sees cytochromial enzymes as protagonists and in particular CYP2C9, it is possible to describe a series of active ingredients, whose contextual assumption could alter the normal pharmacokinetic and pharmacodynamic characteristics of celecoxib.

More precisely, the contemporary administration of:

  • Oral anticoagulants, could significantly increase the risk of bleeding diathesis;
  • ACE inhibitors, angiotensin II antagonists, cyclosporin and tacrolimus could enhance the nefro and hepatotoxic properties of celecoxib;
  • Fluconazole and other active ingredients inducing or inhibiting CYP2C9, could instead alter the normal pharmacokinetic properties of celecoxib.

For the same reason it would be appropriate to consider the inhibitory activity of celecoxib against the aforementioned enzyme, involved in the metabolism of other active ingredients such as antidepressants, neuroleptics and antiarrhythmics, whose intake could significantly vary the therapeutic profile of the aforementioned drugs.

Contraindications CELEBREX ® Celecoxib

The use of CELEBREX ® is contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, hepatic and renal insufficiency, chronic inflammatory diseases of the intestine, peptic ulcer, congestive heart failure, ischemic heart disease and both central and arteriopathy peripherals.

Undesirable effects - Side effects

Numerous clinical trials and careful post-marketing monitoring have shown that CELEBREX ® therapy may present numerous side effects, despite the selectivity of action of celecoxib, especially in particularly predisposed patients.

Sinusitis, urinary and respiratory tract infection, insomnia, abdominal pain, flatulence, constipation and diarrhea, flu-like symptoms, hypertension, palpitation, cardiovascular pathologies, hepatic and nephrotoxicity, allergic reactions of both cutaneous and respiratory nature, vision disorders and hearing represent the main side effects described following the intake of CELEBREX ®, whose incidence and severity, however, seem to be related to the doses of drug used.

Note

CELEBREX ® is a prescription-only drug.