Overview
Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain‚ inflammation‚ and fever. It is commonly used to treat osteoarthritis‚ rheumatoid arthritis‚ ankylosing spondylitis‚ and menstrual pain. Celecoxib works by reducing the production of prostaglandins‚ which are chemicals that cause inflammation and pain. It is available as a generic medication and under the brand name Celebrex. Celecoxib is typically taken orally‚ once or twice daily‚ with or without food. The dosage will vary depending on the condition being treated and the individual patient's response to the medication.
Mechanism of Action
Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that works by reducing the production of prostaglandins‚ which are chemicals that cause inflammation and pain. Prostaglandins are produced by the body in response to injury or infection‚ and they play a role in the inflammatory response. By reducing the production of prostaglandins‚ celecoxib can help to relieve pain and inflammation.
Celecoxib belongs to a class of NSAIDs known as COX-2 inhibitors. COX-2 is an enzyme that is involved in the production of prostaglandins. By selectively inhibiting COX-2‚ celecoxib can reduce the production of prostaglandins without affecting the production of other important prostaglandins that are involved in protecting the stomach and kidneys. This makes celecoxib less likely to cause gastrointestinal side effects than traditional NSAIDs.
Celecoxib is absorbed into the bloodstream after oral administration and reaches peak plasma concentrations within 2 to 4 hours. It is extensively metabolized in the liver and excreted in the urine and feces. The elimination half-life of celecoxib is approximately 11 hours.
Celecoxib is effective in reducing pain and inflammation in a variety of conditions‚ including osteoarthritis‚ rheumatoid arthritis‚ ankylosing spondylitis‚ and menstrual pain. It is generally well-tolerated‚ with the most common side effects being gastrointestinal upset‚ headache‚ and dizziness.
Pharmacokinetics
Celecoxib is rapidly absorbed after oral administration‚ with peak plasma concentrations occurring within 2 to 4 hours. The absolute bioavailability of celecoxib is approximately 90%. Celecoxib is extensively bound to plasma proteins (97%).
Celecoxib is metabolized in the liver by cytochrome P450 enzymes‚ primarily CYP2C9 and CYP2C19. The major metabolites of celecoxib are inactive and are excreted in the urine and feces. The elimination half-life of celecoxib is approximately 11 hours.
Celecoxib is a substrate for the P-glycoprotein efflux transporter. This means that celecoxib can be transported out of cells‚ which can affect its distribution and elimination. Celecoxib is also a substrate for the organic anion transporting polypeptide (OATP) 1B1 and 1B3 transporters. These transporters are responsible for the uptake of celecoxib into cells‚ and they can also affect its distribution and elimination.
The pharmacokinetics of celecoxib are affected by age‚ sex‚ and renal function. Celecoxib clearance is decreased in elderly patients and in patients with renal impairment. As a result‚ these patients may require lower doses of celecoxib to achieve the same therapeutic effect.
Celecoxib is contraindicated in patients with severe hepatic impairment. Celecoxib is also contraindicated in patients who are allergic to celecoxib or to any other NSAIDs.
Indications
Celecoxib is indicated for the treatment of the following conditions⁚
- Osteoarthritis
- Rheumatoid arthritis
- Ankylosing spondylitis
- Acute pain
- Menstrual pain
Celecoxib is also indicated for the treatment of familial adenomatous polyposis (FAP) in patients who are at least 12 years of age. FAP is a condition in which multiple polyps form in the colon and rectum. Celecoxib can help to reduce the number of polyps and prevent them from developing into cancer.
Celecoxib is not indicated for the treatment of peri-operative pain. Celecoxib is also not indicated for the treatment of chronic headaches or migraines.
Celecoxib is available as a generic medication and under the brand name Celebrex. Celecoxib is typically taken orally‚ once or twice daily‚ with or without food. The dosage will vary depending on the condition being treated and the individual patient's response to the medication.
Dosage and Administration
Celecoxib is typically taken orally‚ once or twice daily‚ with or without food. The dosage will vary depending on the condition being treated and the individual patient's response to the medication.
For the treatment of osteoarthritis and rheumatoid arthritis‚ the recommended starting dose of celecoxib is 100 mg twice daily. The dose may be increased to 200 mg twice daily if needed.
For the treatment of ankylosing spondylitis‚ the recommended starting dose of celecoxib is 200 mg twice daily. The dose may be increased to 400 mg twice daily if needed.
For the treatment of acute pain‚ the recommended starting dose of celecoxib is 400 mg once daily. The dose may be increased to 800 mg once daily if needed.
For the treatment of menstrual pain‚ the recommended starting dose of celecoxib is 400 mg once daily. The dose may be increased to 800 mg once daily if needed.
Celecoxib is available as a 50 mg‚ 100 mg‚ 200 mg‚ and 400 mg capsule. The capsule should be swallowed whole with a glass of water.
Celecoxib should not be taken by patients who are allergic to celecoxib or to any other NSAIDs. Celecoxib should also not be taken by patients with severe hepatic impairment or by patients who are taking anticoagulants.
Celecoxib may interact with other medications‚ including warfarin‚ methotrexate‚ and lithium. Celecoxib may also increase the risk of gastrointestinal bleeding in patients who are taking aspirin or other NSAIDs.
Contraindications
Celecoxib is contraindicated in the following patients⁚
- Patients who are allergic to celecoxib or to any other NSAIDs
- Patients with severe hepatic impairment
- Patients who are taking anticoagulants
- Patients with a history of gastrointestinal bleeding or perforation related to NSAID therapy
- Patients with a known or suspected allergy to sulfonamides
- Patients who are pregnant or breastfeeding
Celecoxib should be used with caution in the following patients⁚
- Patients with a history of asthma or other allergic conditions
- Patients with a history of heart failure‚ hypertension‚ or other cardiovascular conditions
- Patients with a history of renal impairment
- Patients with a history of gastrointestinal disease‚ such as ulcers or Crohn's disease
- Patients who are taking other medications that may increase the risk of gastrointestinal bleeding‚ such as aspirin or other NSAIDs
- Patients who are elderly or frail
Celecoxib may increase the risk of cardiovascular events‚ such as heart attack and stroke. The risk is increased in patients with a history of cardiovascular disease or in patients who are taking other medications that may increase the risk of cardiovascular events‚ such as aspirin or other NSAIDs;
Celecoxib may also increase the risk of gastrointestinal bleeding‚ especially in patients who are taking other medications that may increase the risk of gastrointestinal bleeding‚ such as aspirin or other NSAIDs.
Warnings and Precautions
Celecoxib may increase the risk of cardiovascular events‚ such as heart attack and stroke. The risk is increased in patients with a history of cardiovascular disease or in patients who are taking other medications that may increase the risk of cardiovascular events‚ such as aspirin or other NSAIDs.
Celecoxib may also increase the risk of gastrointestinal bleeding‚ especially in patients who are taking other medications that may increase the risk of gastrointestinal bleeding‚ such as aspirin or other NSAIDs.
Celecoxib should be used with caution in patients with a history of asthma or other allergic conditions. Celecoxib may cause bronchospasm in patients with asthma or other respiratory conditions.
Celecoxib should be used with caution in patients with a history of heart failure‚ hypertension‚ or other cardiovascular conditions. Celecoxib may worsen heart failure and increase the risk of cardiovascular events in these patients.
Celecoxib should be used with caution in patients with a history of renal impairment. Celecoxib may worsen renal function in these patients.
Celecoxib should be used with caution in patients with a history of gastrointestinal disease‚ such as ulcers or Crohn's disease. Celecoxib may worsen gastrointestinal disease in these patients.
Celecoxib should be used with caution in patients who are taking other medications that may increase the risk of gastrointestinal bleeding‚ such as aspirin or other NSAIDs.
Celecoxib should be used with caution in patients who are elderly or frail. Elderly patients are more likely to experience side effects from celecoxib‚ such as gastrointestinal bleeding and cardiovascular events.
Women who are pregnant or breastfeeding should not take celecoxib. Celecoxib may cause fetal harm if taken during pregnancy. Celecoxib may also pass into breast milk and cause harm to the nursing infant.
Adverse Effects
The most common adverse effects of celecoxib include⁚
- Gastrointestinal upset‚ such as nausea‚ vomiting‚ diarrhea‚ and abdominal pain
- Headache
- Dizziness
- Rash
- Edema
- Fatigue
Celecoxib may also cause more serious adverse effects‚ such as⁚
- Cardiovascular events‚ such as heart attack and stroke
- Gastrointestinal bleeding
- Hepatotoxicity
- Renal impairment
- Hypersensitivity reactions‚ such as anaphylaxis
Celecoxib is contraindicated in patients with a history of gastrointestinal bleeding or perforation related to NSAID therapy. Celecoxib should be used with caution in patients with a history of cardiovascular disease‚ renal impairment‚ or gastrointestinal disease.
Women who are pregnant or breastfeeding should not take celecoxib. Celecoxib may cause fetal harm if taken during pregnancy. Celecoxib may also pass into breast milk and cause harm to the nursing infant.
Drug Interactions
Celecoxib may interact with other medications‚ including⁚
- Anticoagulants‚ such as warfarin
- Methotrexate
- Lithium
- Aspirin and other NSAIDs
- CYP2C9 inhibitors‚ such as fluconazole and voriconazole
- CYP2C19 inhibitors‚ such as omeprazole and lansoprazole
Celecoxib may increase the risk of bleeding in patients who are taking anticoagulants. Celecoxib may also increase the risk of methotrexate toxicity in patients who are taking methotrexate. Celecoxib may increase the risk of lithium toxicity in patients who are taking lithium.
Celecoxib may interact with aspirin and other NSAIDs to increase the risk of gastrointestinal bleeding. Celecoxib may also interact with CYP2C9 and CYP2C19 inhibitors to increase the risk of celecoxib toxicity.
It is important to tell your doctor about all of the medications you are taking‚ including prescription medications‚ over-the-counter medications‚ and herbal supplements. This will help your doctor to determine if celecoxib is right for you and to avoid any potential drug interactions.
Overdosage
Celecoxib overdosage may cause the following symptoms⁚
- Nausea
- Vomiting
- Abdominal pain
- Diarrhea
- Headache
- Dizziness
- Confusion
- Drowsiness
- Seizures
- Coma
There is no specific antidote for celecoxib overdosage. Treatment is supportive and may include the following⁚
- Gastric lavage
- Activated charcoal
- Intravenous fluids
- Monitoring of vital signs
- Supportive care for seizures or coma
Celecoxib overdosage may be fatal. It is important to seek medical attention immediately if you suspect that someone has overdosed on celecoxib.
Special Populations
Celecoxib is contraindicated in women who are pregnant. Celecoxib may cause fetal harm if taken during pregnancy. Celecoxib may also cause premature closure of the ductus arteriosus in the fetus.
Celecoxib is contraindicated in women who are breastfeeding. Celecoxib may pass into breast milk and cause harm to the nursing infant.
Celecoxib is not approved for use in children under the age of 12. Celecoxib may cause serious side effects in children‚ such as gastrointestinal bleeding and cardiovascular events.
Celecoxib should be used with caution in elderly patients. Elderly patients are more likely to experience side effects from celecoxib‚ such as gastrointestinal bleeding and cardiovascular events.
Celecoxib should be used with caution in patients with renal impairment. Celecoxib may worsen renal function in these patients.
Celecoxib is contraindicated in patients with severe hepatic impairment. Celecoxib may worsen liver function in these patients.