Etoricoxib

Etoricoxib is a highly selective, newer-generation COX-2 inhibitor. The original product is Arcoxia®. The active ingredient has a particularly long half-life and only needs to be taken once daily.

Etoricoxib is used for osteoarthritis, rheumatoid arthritis, gout attacks, ankylosing spondylitis, and short-term for moderate dental pain after surgery.

In studies, ulcers, bleeding and perforations in the upper gastrointestinal tract taken together occurred less often with etoricoxib than with diclofenac. When low-dose acetylsalicylic acid (aspirin) was taken at the same time, this difference was not demonstrated.

Etoricoxib inhibits cyclooxygenase-2 (COX-2) in a highly selective manner:

Selectivity:

• Etoricoxib is about 100 times more selective for COX-2 than for COX-1
• This makes it one of the most selective COX-2 inhibitors

Pharmacokinetics:

• Onset of action: approx. 30 minutes
• Maximum plasma concentration: 1–2 hours
• Half-life: approx. 22 hours
• Once-daily dosing is sufficient

Effect profile:

• Strongly pain-relieving
• Strongly anti-inflammatory
• Particularly effective in acute inflammatory conditions (gout)

Etoricoxib is suitable for:

• Osteoarthritis (30–60 mg)
• Rheumatoid arthritis (60–90 mg)
• Ankylosing spondylitis (60–90 mg)
• Acute gout attack (120 mg)
• Short-term: moderate dental pain after surgery (90 mg)

Particularly suitable for:

• Patients with GI risk (stomach protection desired)
• Gout attacks (fast, strong effect)
• Patients who prefer once-daily dosing

Not suitable:

• In existing cardiovascular disease
• In uncontrolled high blood pressure > 140/90 mmHg
• In severe liver or kidney impairment

Tablets:

• 30 mg, 60 mg, 90 mg, 120 mg

Dosage by indication:

• Osteoarthritis: 30 mg once daily, 60 mg if the effect is insufficient
• Rheumatoid arthritis: 60 mg once daily, 90 mg if the effect is insufficient
• Ankylosing spondylitis: 60 mg once daily, 90 mg if the effect is insufficient
• Acute gout attack: 120 mg once daily (max. 8 days)
• Dental pain (after surgery): 90 mg once daily (max. 3 days)

Maximum daily dose: 120 mg

How to take:

• Once daily, with or without meals
• Swallow the tablet whole with water
• Preferably at the same time every day

Important notes:

• Check blood pressure regularly (etoricoxib can raise blood pressure)
• Use the lowest effective dose
• For gout: start treatment during the attack, max. 8 days
• Do not combine with other NSAIDs

Etoricoxib must not be taken in cases of:

• Hypersensitivity to etoricoxib
• Bronchospasm, acute rhinitis, swelling of the nasal mucosa, angioedema, hives or allergy-like reactions after taking acetylsalicylic acid (aspirin) or NSAIDs, including COX-2 inhibitors
• Active stomach or intestinal ulcers or bleeding
• Inflammatory bowel disease
• Ischemic heart disease, heart failure (NYHA II–IV)
• Uncontrolled high blood pressure (> 140/90 mmHg)
• History of heart attack or stroke
• Peripheral arterial disease or cerebrovascular disease
• Severe liver impairment
• Severe kidney impairment (creatinine clearance < 30 ml/min)
• Pregnancy and breastfeeding
• Children and adolescents under 16 years of age

Caution in cases of:

• Cardiovascular risk factors
• Mild to moderate impairment of kidney function
• Edema

Common (1–10%):

• High blood pressure (more often than with other NSAIDs)
• Headache, dizziness
• Gastrointestinal complaints (nausea, heartburn)
• Edema
• Fatigue
• Elevated liver enzymes

Uncommon (0.1–1%):

• Heart failure
• Skin rash

Rare but serious:

• Cardiovascular events
• Severe skin reactions
• Liver damage

Rise in blood pressure: Etoricoxib can raise blood pressure more than other NSAIDs. Regular monitoring is important.

Increased risk of bleeding with:

• Anticoagulants (warfarin – monitor INR)
• Aspirin (low-dose)

Reduced effect of:

• ACE inhibitors, sartans
• Diuretics

Increased levels of:

• Lithium
• Methotrexate

Caution with:

• Oral contraceptives (etoricoxib can increase ethinylestradiol levels)
• Rifampicin (lowers etoricoxib levels)