Celebrex

Generic and Brand Names

Celecoxib is commonly known by its brand name Celebrex.

Drug Classification

Celecoxib falls under the category of nonsteroidal anti-inflammatory drugs (NSAIDs), more specifically a COX-2 inhibitor.

Indications for Use

Celecoxib is indicated for the relief of signs and symptoms associated with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, juvenile rheumatoid arthritis in patients 2 years and older, and the management of acute pain in adults. It is also indicated for the treatment of primary dysmenorrhea.

Dosage Forms Available

This medication is available as oral capsules in strengths of 50 mg, 100 mg, 200 mg, and 400 mg.

Administration Guidelines

Celecoxib should be taken with or without food. If stomach upset occurs, it can be taken with food to decrease gastrointestinal discomfort. Capsules should be swallowed whole; do not crush or chew.

Dosage and Titration

The recommended starting dose for osteoarthritis is 200 mg once daily or divided as 100 mg twice daily. For rheumatoid arthritis, the initial dose usually is 100 to 200 mg twice daily. The dosage may vary based on specific conditions, and the lowest effective dose should be used.

Pharmacological Mechanism of Action

Celecoxib works by inhibiting the enzyme cyclooxygenase-2 (COX-2), which plays a role in the synthesis of prostaglandins involved in inflammation, pain, and fever.

Drug Metabolism

The metabolism of celecoxib occurs primarily in the liver and involves the cytochrome P450 2C9 (CYP2C9) isoenzyme. Adjustments in dosage may be necessary for individuals with liver impairment.

Excretion Details

Celecoxib is excreted predominantly in the urine and, to a lesser extent, in the feces. The half-life of the drug is approximately 11 hours in healthy individuals.

Potential Drug Interactions

Concomitant use of celecoxib with medications such as warfarin, fluconazole, lithium, ACE inhibitors, and aspirin can lead to significant interactions that may affect the efficacy and safety of celecoxib or the concomitant drug.

Renal Considerations

Caution should be exercised when prescribing celecoxib to patients with pre-existing renal disease or impaired renal function, as it may worsen renal function.

Hepatic Considerations

Patients with hepatic impairment may require adjusted doses of celecoxib. It is not recommended for use in patients with severe liver impairment.

Serious Adverse Reactions

Celecoxib may cause serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. It can also increase the risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal.

Common Adverse Reactions

Some commonly reported side effects of celecoxib include hypertension, edema, dizziness, insomnia, upper respiratory tract infection, rhinitis, sinusitis, rash, and abdominal pain.

Special Populations Precautions

Special consideration is required when prescribing celecoxib for populations such as pregnant women, nursing mothers, paediatric, and geriatric patients due to differential risk profiles and pharmacokinetics in these groups.

Overdose Management

Supportive and symptomatic care should be provided in case of an overdose. There are no specific antidotes for celecoxib overdose, and dialysis is likely to be ineffective due to the drug’s high rate of protein binding.

Storage Conditions

Celecoxib capsules should be stored at room temperature, 15°C to 30°C (59°F to 86°F), and kept in a dry place away from light and moisture.

Prescription Status

Celecoxib is a prescription medication and should only be used under the guidance of a healthcare provider.

Medication Monitoring Parameters

Monitoring of blood pressure, renal and hepatic function tests, and complete blood count should be considered during prolonged therapy with celecoxib, especially in patients with underlying conditions.

Patient Counseling Points

Patients should be advised to report any signs of gastrointestinal bleeding, including black, bloody, or tarry stools, or coughing up blood or vomit that looks like coffee grounds. They should also be aware of the potential for cardiovascular risk and the importance of adhering to prescribed dosages.

Overview of Unique Attributes

Unlike some other NSAIDs, celecoxib has a lower incidence of gastrointestinal side effects due to its selective inhibition of COX-2. However, this selectivity does not completely eliminate the risk of gastrointestinal injury.