Drug Detail:Celebrex (Celecoxib [ sel-e-kox-ib ])
Drug Class: Cox-2 inhibitors
1. How it works
- Celebrex is a brand (trade) name of the drug celecoxib.
- Celebrex (celecoxib) relieves pain and inflammation 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, Celebrex 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.
- Celebrex belongs to the class of drugs called nonsteroidal anti-inflammatory drugs (NSAID). It may also be called a COX-2 inhibitor or 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. Advantages are negated when Celebrex is given with aspirin.
- 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.
- Celebrex is available as a generic under the name celecoxib.
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:
- Abdominal pain, diarrhea, dyspepsia, flatulence, and nausea. Other stomach-related adverse effects include bleeding, ulceration, or perforation, which occasionally may be fatal. Older patients or those taking other medicines that affect the stomach may be more at risk. May occur at any time and without warning.
- May also cause a headache, rash, tinnitus (ringing in the ears), hematological effects, fluid retention, and edema. May mask symptoms of infections.
- Like other NSAIDs, Celebrex is associated with an increased risk of heart attack and stroke. The risk increases the longer Celebrex is taken 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.
- Because Celebrex 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.
- Use with caution in people with asthma or with aspirin-sensitive asthma as bronchospasm may occur and cross-reactivity between aspirin and other NSAIDs (such as Celebrex) has been reported.
- Rarely, life-threatening hypersensitivity reactions may trigger allergy-like asthma.
- Not suitable for use in certain people (such as those with severe liver disease; poor metabolizers of CYPD2C9 substrates; allergic to sulfonamides, aspirin, or other NSAIDs; active gastrointestinal bleeding) or after certain procedures, such as following coronary artery bypass graft (CABG) surgery.
- Do not use at the same time as other non-aspirin NSAIDs. May interact with several other drugs including warfarin, lithium, fluconazole, and ACE inhibitors.
- Should not be used for pain relief during coronary artery bypass graft (CABG) surgery or given in late pregnancy (from 20 weeks gestation).
- Expensive compared to most other NSAIDs.
- 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
- May be given with or without food, although dosages above 400mg twice daily should be administered with food to improve absorption.
- Seek immediate medical advice if you develop any chest pain, shortness of breath, weakness, slurring of speech, dyspepsia, or blood in your stool.
- Also seek urgent medical attention if you develop unexplained nausea, fatigue, itching, skin yellowing, right upper abdominal pain tenderness, or flu-like symptoms.
- Tell your doctor if you have asthma or a history of rhinitis or hay fever before you take Celebrex. If you have asthma and your asthma worsens after taking Celebrex, seek urgent medical advice.
- Use the lowest effective dose for the shortest duration of time.
- Celebrex is a sulfonamide and can cause serious skin effects. Stop Celebrex immediately if any type of rash develops and contact your doctor as soon as possible.
- Report any unexplained weight gain or fluid retention to your doctor.
- Twice daily dosing is recommended; more frequent dosing does not necessarily improve response.
- Response to different NSAIDs can vary so switching types (for example, from Celebrex to naproxen) may improve response.
- 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.
- Celebrex 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 Celebrex before talking to your doctor or pharmacist first to check that they are compatible with Celebrex.
5. Response and effectiveness
- Celebrex takes approximately 3 hours after oral administration to reach peak concentrations. The pain-relieving effects of Celebrex last for approximately 12 hours.
6. Interactions
Medicines that interact with Celebrex may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with Celebrex. 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 Celebrex include:
- anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
- aspirin
- corticosteroids, such as dexamethasone
- cyclosporine
- digoxin
- diuretics, such as furosemide
- duloxetine
- 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 Celebrex, and possibly liver and kidney damage.
Note that this list is not all-inclusive and includes only common medications that may interact with Celebrex. You should refer to the prescribing information for Celebrex for a complete list of interactions.