Drug Detail:Celecoxib (Celecoxib [ sel-e-kox-ib ])
Drug Class: Cox-2 inhibitors
1. How it works
- Celecoxib may be used to relieve pain and inflammation.
- Celecoxib works by blocking COX-2 enzymes, which are responsible for the synthesis of prostaglandins (prostaglandins are released during inflammation and elevate body temperature and make nerve endings more sensitive to pain transmission). COX-2 enzymes release prostaglandins in response to infection or injury. At usual dosages, celecoxib only minimally inhibits COX-1. COX-1 produces prostaglandins that activate platelets and protect the stomach and intestinal lining, so drugs that inhibit COX-1 cause more gastrointestinal side effects.
- Celecoxib belongs to a class of medicines known as NSAIDs (nonsteroidal anti-inflammatory drugs). It is specifically a COX-2 inhibitor. It is also a sulfonamide.
2. Upsides
- Effective for the relief of acute pain, including period pain (primary dysmenorrhea) and postoperative (eg, dental or orthopedic) pain.
- Helps relieve pain and inflammation associated with osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
- Does not cause dependence.
- Associated with fewer gastrointestinal-related adverse events compared to NSAIDs that inhibit both COX-1 and COX-2 enzymes.
- Associated with a reduction in the number of adenomatous colorectal polyps in adults with familial adenomatous polyposis (FAP). It is not known if it reduces the risk of colorectal, duodenal, or other FAP-related cancers.
- May be taken once or twice a day.
- Single doses provide pain relief within 60 minutes.
- Available in 50mg, 100mg, 200mg, and 400mg strengths.
- Generic celecoxib is available.
3. Downsides
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Diarrhea, abdominal pain, flatulence, and dyspepsia. Incidence is less than most other NSAIDs (such as naproxen, diclofenac, and ibuprofen).
- A headache, sinusitis, fluid retention, and rhinitis have also been reported.
- Like other NSAIDs, celecoxib is associated with an increased risk of heart attack and stroke. The risk increases the longer celecoxib is taken for and is higher in people with pre-existing heart disease.
- May also increase blood pressure leading to the onset of new high blood pressure or aggravate pre-existing high blood pressure. Monitor for signs and symptoms of abnormal clotting or bleeding.
- May decrease kidney function and precipitate reversible kidney failure. Patients at risk include those with pre-existing impaired kidney function, heart failure, liver dysfunction, taking certain medications (such as diuretics, heart medicines), and the elderly.
- May not be suitable for some people including those with sulfonamide allergy or who have experienced asthma, urticaria, or an allergic-type reaction to aspirin or other NSAIDs.
- Because celecoxib is a sulfonamide it has the potential to cause severe skin reactions including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) which may be fatal.
- Caution may be required when using in people with preexisting cardiovascular disease including high blood pressure, congestive heart failure, a previous history of peptic ulcer disease or gastrointestinal bleeding, or kidney disease.
- Rarely, may cause elevations in liver enzymes and severe hepatic reactions, some fatal. Liver function should be monitored when celecoxib is taken for extended periods.
- Kidney damage has also been reported with NSAID use, either as a result of long-term administration or in people whose kidneys function is dependent on renal prostaglandins.
- Rarely, anaphylaxis-like reactions have been reported. The risk is highest in people with asthma who also have rhinitis, or in those who have reacted previously to aspirin or other NSAIDs.
- May interact with some other medicines such as warfarin, lithium, ACE inhibitors, and diuretics.
- Should not be used for pain relief during coronary artery bypass graft (CABG) surgery or given in late pregnancy (from 20 weeks gestation).
- Celecoxib is only available as an oral capsule that is taken by mouth.
- Not a substitute for aspirin for the prevention of adverse cardiovascular events.
- Only available on prescription (many NSAIDs are available over-the-counter).
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Tips
- Use the lowest effective dose for the shortest possible time, or as directed by your doctor.
- May be taken once or twice daily.
- In those who have difficulty swallowing, a capsule of celecoxib may be opened and the contents mixed with applesauce and ingested immediately.
- See your doctor immediately if you develop chest pain, shortness of breath, weakness, or slurring of speech. If you have pre-existing cardiovascular disease, ensure you keep your regular check-ups with your doctor.
- Also contact your doctor urgently if you develop unexplained nausea or flu-like symptoms, a skin rash or an itch, fluid retention, blood in the stools or in sputum, or upper right abdominal pain.
- Tell your doctor if you have asthma or a history of rhinitis or hay fever before you take celecoxib.
- NSAIDs should not be used from week 20 of pregnancy unless on a doctor's advice. Ask your doctor before using any medication during pregnancy.
- Celecoxib may make your skin more sensitive to the sun. Avoid spending excessive periods in the sun, and wear sun-protective clothing and a broad-spectrum SPF 30+ sunscreen when outside.
- Do not take any other medicines or supplements with celecoxib before talking to your doctor or pharmacist first to check that they are compatible with celecoxib.
5. Response and effectiveness
- Peak levels of celecoxib are reached approximately 3 hours after an oral dose. The pain-relieving effects of celecoxib may last up to 24 hours.
6. Interactions
Medicines that interact with celecoxib may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with celecoxib. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with celecoxib include:
- anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
- aspirin
- corticosteroids, such as dexamethasone
- cyclosporine
- digoxin
- diuretics, such as furosemide
- duloxetine
- fluconazole
- lithium
- medications that lower blood pressure, such as ACE inhibitors (eg, benazepril, captopril), ARBs (such as candesartan, irbesartan), or beta-blockers (eg, atenolol, sotalol)
- methotrexate and other drugs used to treat rheumatoid arthritis
- nonsteroidal anti-inflammatories (NSAIDs), such as diclofenac, etodolac, ibuprofen, meloxicam, nabumetone, or naproxen
- other medications that inhibit or induce cytochrome enzymes CYP2D6, such as fluoxetine, bupropion, duloxetine
- pemetrexed
- warfarin.
Alcohol can increase the likelihood of gastrointestinal side effects with celecoxib, and possibly liver and kidney damage.
Note that this list is not all-inclusive and includes only common medications that may interact with celecoxib. You should refer to the prescribing information for celecoxib for a complete list of interactions.