Brand name: Celebrex

Active ingredient (generic name): Celecoxib

Manufacturer: Pfizer

Importer: Behestan Darou

Pharmacotherapeutic group: Non-steroidal anti-inflammatory and antirheumatic drug

Pharmaceutical form: 100mg & 200mg Capsules

Pharmacodynamic:  

The mechanism of action of Celebrex is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) and at therapeutic concentrations in humans, Celebrex does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme.

Pharmacokinetic:

Celecoxib is well absorbed reaching peak plasma concentrations after approximately 2-3 hours, dosing with food (high fat meal) delays absorption by about 1 hour.

 

Therapeutic indication:

Celebrex is indicated for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.

 

Dosage and administration:

Osteoarthritis: The usual recommended daily dose is 200 mg taken once daily or in two divided doses. In some patients, with insufficient relief from symptoms, an increased dose of 200 mg twice daily may increase efficacy. In the absence of an increase in therapeutic benefit after two weeks, other therapeutic options should be considered.

Rheumatoid arthritis: The initial recommended daily dose is 200 mg taken in two divided doses. The dose may, if needed, later be increased to 200 mg twice daily. In the absence of an increase in therapeutic benefit after two weeks, other therapeutic options should be considered.

Ankylosing spondylitis: The recommended daily dose is 200 mg taken once daily or in two divided doses. In a few patients, with insufficient relief from symptoms, an increased dose of 400mg once daily or in two divided doses may increase efficacy. In the absence of an increase in therapeutic benefit after two weeks, other therapeutic options should be considered.

The maximum recommended daily dose is 400 mg for all indications.

Celebrex may be taken with or without food.

Elderly: (>65 years) as in younger adults, 200 mg per day should be used initially. The dose may, if needed, later be increased to 200 mg twice daily. Particular caution should be exercised in elderly with a body weight less than 50 kg.

Hepatic impairment: Treatment should be initiated at half the recommended dose in patients with established moderate liver impairment with a serum albumin of 25-35 g/l. Experience in such patients is limited to cirrhotic patients.

Renal impairment: Experience with celecoxib in patients with mild or moderate renal impairment is limited; therefore such patients should be treated with caution.

Children: Celecoxib is not indicated for use in children.

CYP2C9 Poor Metabolizers: Patients who are known, or suspected to be CYP2C9 poor metabolizers based on genotyping or previous history/experience with other CYP2C9 substrates should be administered celecoxib with caution as the risk of dose-dependent adverse effects is increased. Consider reducing the dose to half the lowest recommended dose.

 

Adverse reaction:

The most common adverse effects are abdominal pain, diarrhea, dyspepsia, flatulence, nausea and headache or dizziness.

 

Contraindication:

In the following conditions, Celebrex administration is prohibited:

-          History of hypersensitivity to the active substance or to any of the excipients

-          Known hypersensitivity to sulphonamides.

-          Active peptic ulceration or gastrointestinal (GI) bleeding.

-          Patients who have experienced asthma, acute rhinitis, nasal polyps, angioneurotic oedema, urticaria or other allergic-type reactions after taking acetylsalicylic acid or NSAIDs including COX-2 (cyclooxygenase-2) inhibitors.

-          Congestive heart failure (NYHA II-IV).

-          Established ischaemic heart disease, peripheral arterial disease and/or cerebrovascular disease.

 

 

 

Pharmacokinetic interactions:

In healthy subjects, co-administration of celecoxib 200 mg twice daily with 450 mg twice daily of lithium resulted in a mean increase in Cmax of 16% and in AUC of 18% of lithium. Therefore, patients on lithium treatment should be closely monitored when celecoxib is introduced or withdrawn.

Since celecoxib is predominantly metabolised by CYP2C9 it should be used at half the recommended dose in patients receiving fluconazole.

The concomitant use of celecoxib and non-aspirin NSAID should be avoided.

Special warnings:

Caution is advised with treatment of patients most at risk of developing a gastrointestinal complication with NSAIDs; the elderly, patients using any other NSAID or acetylsalicylic acid concomitantly.

As the cardiovascular risks of celecoxib may increase with dose and duration of exposure, the shortest duration possible and the lowest effective daily dose should be used.

 

Pregnancy and lactation:

Pregnancy category is C and Celebrex should be used during pregnancy only if the potential benefits justify the potential risk to the fetus.

 

Storage temperature:  

Room temperature (15-25 C)

 

 

 

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