Celecoxib

Celecoxib is a selective cyclooxygenase-2 inhibitor (COX-2 inhibitor, coxib). It acts specifically on the enzyme COX-2, which is mainly active during inflammation, while sparing COX-1, which has a protective function for the stomach lining.

The original product is Celebrex®. Celecoxib generics are also available. The active ingredient is used mainly in patients who cannot tolerate conventional NSAIDs such as ibuprofen or diclofenac because of stomach problems.

Celecoxib is approved for the treatment of osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.

Celecoxib selectively inhibits cyclooxygenase-2 (COX-2):

COX-1 vs. COX-2:

• COX-1: Protects the stomach lining, regulates kidney function and platelets
• COX-2: Is produced in greater amounts during inflammation, promotes pain and swelling

Advantage of selectivity:

• Celecoxib mainly inhibits COX-2
• This results in fewer stomach ulcers and GI bleeds
• The protective function of COX-1 for the stomach is largely preserved

Action profile:

• Pain-relieving and anti-inflammatory
• Onset of action: 30–60 minutes
• Duration of action: 12 hours

Celecoxib is suitable for:

• Osteoarthritis (symptomatic treatment)
• Rheumatoid arthritis
• Ankylosing spondylitis (Bechterew's disease)

Particularly suitable for:

• Patients with an increased gastrointestinal risk
• Patients who cannot tolerate conventional NSAIDs
• Older patients with a history of GI problems

Not suitable:

• With known cardiovascular disease
• After a heart attack or stroke
• With severe liver or kidney failure
• With a sulfonamide allergy

Capsules:

• 100 mg, 200 mg

Osteoarthritis:

• 200 mg daily (1x 200 mg or 2x 100 mg)

Rheumatoid arthritis:

• 200–400 mg daily (divided into 2 doses)

Ankylosing spondylitis:

• 200 mg daily, up to 400 mg if needed

Maximum daily dose: 400 mg

How to take:

• Swallow the capsules whole with water, without chewing
• Regardless of meals (can be taken with food)
• If taken 2 times daily: morning and evening

Important notes:

• Lowest effective dose for the shortest possible duration
• Regular medical check-ups during long-term use
• Monitor blood pressure

Celecoxib must not be taken in cases of:

• Hypersensitivity to celecoxib or sulfonamides
• Asthma, acute rhinitis, nasal polyps, angioedema, hives or other allergic reactions after taking acetylsalicylic acid or other NSAIDs, including COX-2 inhibitors
• Active gastrointestinal ulcers or gastrointestinal bleeding
• Ischemic heart disease, heart failure (NYHA II–IV)
• History of heart attack or stroke
• Diseases of the blood vessels of the brain (cerebrovascular diseases)
• Peripheral arterial occlusive disease
• Severe liver failure
• Impaired kidney function with an estimated creatinine clearance below 30 ml/min
• Inflammatory bowel disease
• Pregnancy and breastfeeding
• Women who could become pregnant and are not using a reliable method of contraception

Use with caution in cases of:

• Cardiovascular risk factors
• Impaired kidney function
• High blood pressure
• Older patients

Common (1–10%):

• High blood pressure
• Headache, dizziness
• Insomnia
• Edema
• Respiratory tract infections
• Gastrointestinal complaints such as abdominal pain, diarrhea, indigestion, flatulence, nausea and vomiting

Uncommon (0.1–1%):

• Heart failure
• Skin rash

Rare but serious:

• Cardiovascular events (heart attack, stroke)
• Severe skin reactions
• Liver damage

GI advantage: The risk of stomach ulcers and GI bleeding is significantly lower than with non-selective NSAIDs.

Increased risk of bleeding with:

• Anticoagulants (warfarin – monitor INR)

Reduced effect of:

• ACE inhibitors, sartans
• Diuretics

Celecoxib is metabolized via CYP2C9:

• Fluconazole increases celecoxib levels (halve the dose)
• In known CYP2C9 poor metabolizers: lowest dose

Caution with:

• Lithium (increased levels)
• Methotrexate