What are the main uses of celecoxib. How does celecoxib work in the body. What are the common and serious side effects of celecoxib. How does celecoxib interact with other medications.

Understanding Celecoxib: A Comprehensive Overview

Celecoxib is a prescription medication belonging to the class of drugs known as nonsteroidal anti-inflammatory drugs (NSAIDs). It’s available as both a generic drug and under the brand name Celebrex. This oral capsule is widely used to treat various forms of arthritis, short-term pain, and menstrual cramps. As with any medication, it’s crucial to understand its uses, mechanisms, potential side effects, and interactions to ensure safe and effective use.

The Therapeutic Applications of Celecoxib

Celecoxib is prescribed for several conditions, primarily those involving pain and inflammation. Its main therapeutic applications include:

• Rheumatoid arthritis
• Osteoarthritis
• Ankylosing spondylitis
• Short-term pain management
• Menstrual cramps

How does celecoxib work to alleviate these conditions? The drug functions by blocking an enzyme called cyclooxygenase (COX). This enzyme is responsible for producing chemicals in the body that cause pain and inflammation. By inhibiting COX, celecoxib effectively reduces these symptoms, providing relief to patients suffering from various forms of arthritis and pain.

Mechanism of Action: How Celecoxib Works in the Body

To understand the effectiveness of celecoxib, it’s important to delve into its mechanism of action. As an NSAID, celecoxib targets specific pathways in the body to reduce pain and inflammation. Here’s a breakdown of its process:

1. Celecoxib blocks the cyclooxygenase (COX) enzyme.
2. This inhibition prevents the production of prostaglandins, which are chemicals responsible for pain and inflammation.
3. By reducing prostaglandin levels, celecoxib effectively diminishes pain and inflammation in the affected areas.
4. Unlike some other NSAIDs, celecoxib specifically targets COX-2 enzymes, potentially reducing the risk of certain side effects associated with COX-1 inhibition.

This targeted approach allows celecoxib to provide effective pain relief while potentially minimizing some of the gastrointestinal side effects commonly associated with traditional NSAIDs.

Common Side Effects and Safety Considerations

While celecoxib can be highly effective in managing pain and inflammation, it’s not without potential side effects. Understanding these possible reactions is crucial for patients and healthcare providers alike. Common side effects of celecoxib include:

• Stomach pain
• Constipation or diarrhea
• Gas and heartburn
• Nausea and vomiting
• Dizziness
• Headache
• Respiratory tract infection

Are these side effects typically severe? In most cases, these effects are mild and may subside within a few days or weeks as the body adjusts to the medication. However, if these symptoms persist or worsen, it’s important to consult a healthcare provider.

Monitoring and Managing Side Effects

How can patients effectively monitor and manage these side effects? Here are some strategies:

• Keep a symptom diary to track the occurrence and severity of side effects
• Take celecoxib with food to reduce stomach upset
• Stay hydrated to help mitigate constipation
• Avoid lying down immediately after taking the medication to prevent heartburn
• Report any persistent or severe side effects to a healthcare provider promptly

Serious Side Effects and Boxed Warnings

While less common, celecoxib can potentially cause serious side effects that require immediate medical attention. The FDA has issued boxed warnings for celecoxib, which are the most serious warnings for prescription drug labeling. These warnings highlight significant risks associated with the medication:

Heart Risks Warning

Can celecoxib increase the risk of cardiovascular events? Yes, like all NSAIDs, celecoxib can increase the risk of heart attack, heart failure, or stroke. This risk may be higher for individuals with existing cardiovascular conditions or risk factors such as high blood pressure.

Coronary Artery Bypass Graft Warning

Patients who have recently undergone or are scheduled for coronary artery bypass graft surgery should not take celecoxib. The medication can increase the risk of heart attack or stroke in these cases.

Stomach Problems Warning

Celecoxib may increase the risk of stomach bleeding, ulcers, or small holes in the stomach or intestinal lining. These complications can be severe and potentially life-threatening, especially in older adults.

Serious Skin Reactions Warning

In rare cases, celecoxib may cause severe skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). These conditions require immediate medical attention.

What are the signs of these serious side effects? Patients should seek immediate medical help if they experience:

• Chest pain or symptoms of a heart attack
• Signs of a stroke, such as sudden weakness on one side of the body or slurred speech
• Severe stomach pain or signs of gastrointestinal bleeding
• Skin rash, blistering, or peeling
• Swelling of the face or throat
• Yellowing of the skin or whites of the eyes (indicating liver problems)

Drug Interactions and Precautions

Celecoxib can interact with various medications, herbs, and vitamins, potentially altering its effectiveness or increasing the risk of side effects. It’s crucial for patients to disclose all current medications and supplements to their healthcare provider before starting celecoxib.

Common Drug Interactions

Which medications commonly interact with celecoxib? Some notable interactions include:

• Blood thinners (e.g., warfarin)
• Other NSAIDs or aspirin
• Certain antidepressants (e.g., SSRIs)
• ACE inhibitors and ARBs (blood pressure medications)
• Diuretics
• Lithium

How do these interactions affect the body? They can potentially increase the risk of bleeding, affect kidney function, or alter the effectiveness of either celecoxib or the interacting medication. Healthcare providers may need to adjust dosages or recommend alternative treatments in some cases.

Special Precautions

Certain groups of people may need to exercise extra caution when using celecoxib:

• Elderly patients (increased risk of stomach bleeding and other side effects)
• Individuals with a history of stomach ulcers or bleeding
• Patients with kidney or liver disease
• Those with a history of heart disease or stroke
• Individuals with asthma (potential for allergic reactions)

What precautions should these groups take? They should consult closely with their healthcare provider, who may recommend lower doses, more frequent monitoring, or alternative treatments depending on their individual risk factors.

Dosage and Administration Guidelines

Proper dosage and administration of celecoxib are crucial for its safe and effective use. The dosage can vary depending on the condition being treated, the patient’s age, and other individual factors.

General Dosage Guidelines

What are the typical dosage ranges for celecoxib? Here’s a general overview:

• Osteoarthritis: 200 mg once daily or 100 mg twice daily
• Rheumatoid arthritis: 100 to 200 mg twice daily
• Ankylosing spondylitis: 200 mg once daily or 100 mg twice daily
• Acute pain: 400 mg initially, followed by 200 mg if needed on the first day, then 200 mg twice daily as needed
• Primary dysmenorrhea: 400 mg initially, followed by 200 mg if needed on the first day, then 200 mg twice daily as needed

How should celecoxib be taken? The medication is typically taken orally with or without food. If stomach upset occurs, taking it with food may help alleviate this side effect.

Considerations for Special Populations

Certain groups may require dosage adjustments:

• Elderly patients: Lower doses may be recommended due to increased risk of side effects
• Patients with liver impairment: Dosage reduction may be necessary
• Individuals with poor metabolism of CYP2C9 substrates: Lower doses may be advised

It’s crucial to follow the prescribed dosage and not exceed the recommended amount without consulting a healthcare provider.

Long-Term Use and Monitoring

For patients using celecoxib for chronic conditions like arthritis, long-term use may be necessary. However, this extended use requires careful monitoring to ensure ongoing safety and effectiveness.

Regular Check-ups and Assessments

What should long-term users of celecoxib expect in terms of monitoring? Healthcare providers typically recommend:

• Regular blood pressure checks
• Periodic blood tests to assess kidney and liver function
• Monitoring for signs of gastrointestinal bleeding or ulcers
• Assessing cardiovascular risk factors
• Evaluating the ongoing need for the medication and considering the lowest effective dose

How often should these assessments occur? The frequency of check-ups can vary based on individual risk factors, but typically, patients should have at least annual comprehensive evaluations.

Strategies for Safe Long-Term Use

To minimize risks associated with long-term use of celecoxib, patients and healthcare providers can employ several strategies:

• Use the lowest effective dose for the shortest duration necessary
• Consider periodic drug holidays if appropriate for the condition
• Implement lifestyle modifications to support overall health (e.g., diet, exercise)
• Stay vigilant for any new or worsening side effects
• Maintain open communication with healthcare providers about any concerns or changes in health status

By adhering to these strategies and maintaining regular medical oversight, patients can optimize the benefits of celecoxib while minimizing potential risks associated with long-term use.

Alternatives and Complementary Approaches

While celecoxib can be highly effective for many patients, it’s not the only option for managing pain and inflammation. Understanding alternative treatments and complementary approaches can provide a more comprehensive pain management strategy.

Alternative Medications

What are some alternative medications to celecoxib? Depending on the condition and individual factors, healthcare providers might consider:

• Other NSAIDs (e.g., ibuprofen, naproxen)
• Acetaminophen for pain relief
• Disease-modifying antirheumatic drugs (DMARDs) for certain types of arthritis
• Topical pain relievers
• Corticosteroids for severe inflammation

How do these alternatives compare to celecoxib? Each medication has its own risk-benefit profile, and the choice depends on factors such as the specific condition, severity of symptoms, and individual patient characteristics.

Non-Pharmacological Approaches

Can non-drug therapies complement or replace celecoxib in some cases? Absolutely. Many patients benefit from a multi-faceted approach to pain and inflammation management. Some non-pharmacological strategies include:

• Physical therapy and regular exercise
• Hot and cold therapy
• Acupuncture
• Massage therapy
• Dietary modifications (e.g., anti-inflammatory diets)
• Stress reduction techniques (e.g., meditation, yoga)
• Weight management for joint health

These approaches can often be used in conjunction with celecoxib or other medications to enhance overall pain management and potentially reduce reliance on pharmacological interventions.

Integrative Medicine Approaches

How can integrative medicine contribute to pain management alongside or as an alternative to celecoxib? Integrative medicine combines conventional and complementary therapies, focusing on the whole person. Some integrative approaches include:

• Herbal supplements (e.g., turmeric, ginger) – with caution due to potential interactions
• Mind-body techniques (e.g., biofeedback, guided imagery)
• Nutritional counseling
• Lifestyle modifications
• Traditional healing practices (e.g., Traditional Chinese Medicine)

It’s crucial to discuss any complementary or alternative treatments with a healthcare provider, especially when using celecoxib or other medications, to ensure safety and avoid potential interactions.

Side Effects, Dosage, Uses & More

This drug has boxed warnings. These are the most serious warnings from the Food and Drug Administration (FDA). Boxed warnings alert doctors and patients about drug effects that may be dangerous.

• Heart risks warning: This drug is a nonsteroidal anti-inflammatory drug (NSAID). All NSAIDs can increase your risk of heart attack, heart failure, or stroke. This risk increases the longer you use NSAIDs. It also increases if you use high doses. Your risk may be higher if you have risk factors for heart disease, such as high blood pressure. Talk to your doctor before taking celecoxib if you have heart disease.
• Coronary artery bypass graft warning: Don’t take celecoxib if you will have or have recently had a coronary artery bypass graft, or heart surgery to improve blood flow to your heart. Your risk of heart attack or stroke increases if you take celecoxib to treat pain before or after your surgery.
• Stomach problems warning: Don’t use celecoxib if you have current stomach bleeding or a history of stomach ulcers. Taking celecoxib increases your risk of stomach bleeding, ulcers, or small holes in the lining of your stomach or intestines, which can be fatal. These may occur at any time without any warning symptoms. If you’re 65 years or older, you’re at higher risk of these problems.
• Serious skin reactions warning: Taking this drug may cause serious and sometimes deadly skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). Get immediate medical help if you have signs of red, swollen, blistered, or peeling skin; red or irritated eyes; or sores in your mouth, throat, nose, or eyes.

1. Celecoxib oral capsule is available as a generic drug and a brand-name drug. Brand name: Celebrex.
2. Celecoxib only comes as a capsule you take by mouth.
3. This drug is used to treat various forms of arthritis, short-term pain, and menstrual cramps.

Celecoxib oral capsule is a prescription drug that’s available as the brand-name drug Celebrex. It’s also available in a generic version. Generic drugs usually cost less. In some cases, they may not be available in every strength or form as the brand-name version.

Celecoxib only comes as a capsule you take by mouth.

Why it’s used

This drug is used to treat:

• rheumatoid arthritis
• osteoarthritis
• ankylosing spondylitis
• short-term pain
• menstrual cramps

How it works

This drug belongs to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

NSAIDs block an enzyme called cyclooxygenase (COX). COX works in your body to produce chemicals that cause pain and inflammation. By blocking COX, NSAIDs like this drug stop these chemicals from forming. This, in turn, reduces pain and inflammation.

Celecoxib oral capsule does not cause drowsiness, but it can cause other side effects.

More common side effects

The more common side effects that can occur with celecoxib oral capsule include:

• stomach pain
• constipation
• diarrhea
• gas
• heartburn
• nausea
• vomiting
• dizziness
• headache
• respiratory tract infection

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

• Chest pain or heart attack
• Stroke. Symptoms may include:
  • sudden weakness in one part or side of your body
  • slurred speech
  • drooping on one side of your face
  • blurred vision
  • sudden dizziness or trouble walking
  • very severe headache with no other cause
• High blood pressure
• Edema. Symptoms may include:
  • swelling in your arms and legs, hands and feet
  • unusual weight gain
• Bleeding and ulcers in your stomach and intestine. Symptoms may include:
  • blood in urine
  • vomiting
  • bloody stools
  • black and sticky stools
• Skin reactions, including rash or blisters
• Allergic reactions. Symptoms may include:
  • itching and hives
  • swelling of your face or throat
• Liver problems. Symptoms may include yellowing of your skin or whites of your eyes.
• Asthma attacks

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this information includes all possible side effects. This information is not a substitute for medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.

Celecoxib oral capsule may interact with other medications, herbs, or vitamins you might be taking. That’s why your doctor should manage all of your medications carefully. If you’re curious about how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Note: You can reduce your chances of drug interactions by having all of your prescriptions filled at the same pharmacy. That way, a pharmacist can check for possible drug interactions.

Examples of drugs that can cause interactions with celecoxib are listed below.

Blood thinner, anticoagulant

Combining warfarin and celecoxib raises your risk of bleeding.

Mental health drug

Celecoxib may increase the levels of lithium in your body. Signs of lithium toxicity include slurred speech and tremors.

Blood pressure drugs

Celecoxib may reduce the blood pressure-lowering effects of certain blood pressure drugs. Examples of these drugs include:

• antiotensin-converting enzyme (ACE) inhibitors
• angiotensin II receptor blockers
• diuretics

Transplant drug

Combining cyclosporine and celecoxib raises your risk of kidney damage.

Cancer drugs

Taking celecoxib with certain drugs used to treat cancer raises the risk of side effects from those drugs. These side effects include kidney damage and a decrease in cells that help you fight infection. Examples of these drugs include:

• methotrexate
• pemetrexed

Other NSAIDs

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID). Combining it with other NSAIDs increases your risk of side effects. Examples of other NSAIDs include:

• ibuprofen
• naproxen
• aspirin

Corticosteroids

Combining celecoxib with corticosteroids such as prednisone raises your risk of stomach bleeding.

Digoxin

If you take celecoxib with digoxin, the levels of digoxin in your body may be increased. If you take these drugs together, your doctor may monitor your digoxin levels.

Antidepressants

Combining celecoxib with selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs) increases your risk of stomach bleeding. Examples of SSRIs and SNRIs include:

• citalopram (Celexa)
• paroxetine (Paxil)
• sertraline (Zoloft)
• venlafaxine (Effexor)
• duloxetine (Cymbalta)

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions. This information is not a substitute for medical advice. Always speak with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and supplements, and over-the-counter drugs that you are taking.

This drug comes with several warnings.

High blood pressure warning

This drug may cause you to develop high blood pressure or may worsen high blood pressure. Take this medication with caution if you have high blood pressure. Check your blood pressure before and while taking this drug.

Asthma warning

Take this drug with caution if you have asthma. It may cause narrowing in your airways, which could lead to death. If your asthma worsens while you take this drug, get immediate medical attention.

Allergy warning

This drug can cause a severe allergic reaction. Symptoms may include:

• trouble breathing
• swelling of your throat or tongue
• hives

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 911 or go to the nearest emergency room. Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

Alcohol interaction warning

Combining alcohol with celecoxib raises your risk of stomach bleeding.

Smoking warning

Smoking while taking celecoxib raises your risk of stomach bleeding.

Warnings for people with certain health conditions

For people with heart disease: If you have a history of heart disease or are at risk for heart disease, you shouldn’t take celecoxib. It raises your risk of blood clots, heart attack, and stroke.

For people with stomach problems: If you have a history of stomach bleeding or ulcers, you’re at greater risk of having another ulcer or bleeding event, which may be fatal.

For people with sulfonamide “sulfa” allergy: If you’re allergic to medications that contain sulfonamide, you shouldn’t take this drug. This drug contains sulfonamide. You may have serious skin reactions. Report any skin rash to your doctor right away.

Warnings for other groups

For pregnant women: Tell your doctor if you’re pregnant or plan to become pregnant. Research in animals has shown adverse effects to the fetus when the mother takes the drug. This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Call your doctor right away if you become pregnant while taking this drug.

For women who are breastfeeding: This drug has been shown to pass through breast milk. You and your doctor should decide if you’ll take this drug or breastfeed.

For seniors: This drug has been studied in a small number of people older than 65 years. If you’re 65 years or older, you may have increased risk of stomach problems and kidney failure that may be fatal.

For children: This drug hasn’t been studied in people younger than 2 years.

This dosage information is for celecoxib oral capsule. All possible dosages and forms may not be included here. Your dose, form, and how often you take it will depend on:

• your age
• the condition being treated
• how severe your condition is
• other medical conditions you have
• how you react to the first dose

Forms and strengths

Generic: Celecoxib

• Form: oral capsule
• Strengths: 50 mg, 100 mg, 200 mg, and 400 mg

Brand: Celebrex

• Form: oral capsule
• Strengths: 50 mg, 100 mg, 200 mg, and 400 mg

Dosage for osteoarthritis

Adult dosage (ages 18 years and older)

The typical dosage is 200 mg taken once per day, or 100 mg taken twice per day in evenly spaced doses.

Child dosage (ages 0 to 17 years)

A safe and effective dosage hasn’t been established for this age group.

Dosage for rheumatoid arthritis

Adult dosage (ages 18 years and older)

The typical dosage is 100–200 mg taken twice per day in evenly spaced doses.

Child dosage (ages 2 to 17 years), for juvenile rheumatoid arthritis

• For children who weigh 22–55 pounds (10–25 kg), the typical dosage is 50 mg taken twice per day in evenly spaced doses.
• For children who weigh more than 55 pounds (25 kg), the typical dosage is 100 mg taken twice per day in evenly spaced doses.

Child dosage (ages 0 to 1 years)

Dosage hasn’t been established for children younger than 2 years.

Dosage for ankylosing spondylitis

Adult dosage (ages 18 years and older)

• The typical dosage is 200 mg taken once per day or 100 mg taken twice per day in evenly spaced doses.
• If celecoxib isn’t working after 6 weeks, your doctor may try 400 mg per day (single or divided doses).

Child dosage (ages 0 to 17 years)

A safe and effective dosage hasn’t been established for this age group.

Dosage for short-term pain

Adult dosage (ages 18 years and older)

• The typical dosage is 400 mg for the first dose, followed by a 200-mg dose about 8–12 hours later if needed.
• On following days, the typical dosage is 200 mg taken twice per day as needed.

Child dosage (ages 0 to 17 years)

A safe and effective dosage hasn’t been established for this age group.

Dosage for menstrual cramps

Adult dosage (ages 18 years and older)

• The typical dosage is 400 mg for the first dose followed by a 200-mg dose about 8–12 hours later if needed.
• On following days, the typical dosage is 200 mg taken twice per day as needed.

Child dosage (ages 0 to 17 years)

A safe and effective dosage hasn’t been established for this age group.

Special considerations

People with liver disease: Having liver disease may reduce your ability to clear this drug from your body, which could lead to more side effects. If you have moderate liver disease, your daily dose of celecoxib may be reduced by half. If you have severe liver disease, you shouldn’t take this medication.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always speak with your doctor or pharmacist about dosages that are right for you.

Celecoxib oral capsule may be used for short-term or long-term treatment, depending on your condition. This drug has risks if you don’t take as prescribed by your doctor.

If you stop or miss doses: If you stop taking this drug, miss doses, or don’t take it on schedule, you may experience more pain caused by your condition.

If you take too much: Taking too much increases your risk of experiencing side effects.

What to do if you miss a dose: If you miss your dose, take it as soon as you can. However, if it’s just a few hours until your next dose, skip the missed dose. Never try to catch up by taking two doses at once. This could result in toxic side effects.

How to tell if the drug is working: You may be able to tell this drug is working if you experience less pain.

Keep these considerations in mind if your doctor prescribes celecoxib oral capsule for you.

General

• Whether you should take this drug with food depends on your dosage. If you take 400 mg of celecoxib twice per day, you should take it with food for better drug absorption. If you take up to 200 mg celecoxib twice per day, you can take it with or without food.
• You can open the capsule if you need to.
• If you have trouble swallowing the capsule, you can open it and sprinkle the contents onto a level teaspoon of cool or room-temperature applesauce. Eat the applesauce immediately along with some water.

Storage

• Store at room temperature between 68°F and 77°F (20°C and 25°C). From time to time, you can store it at temperatures between 59°F and 86°F (15°C and 30°C).
• Keep this drug away from light.
• Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is not refillable. You or your pharmacy will have to contact your doctor for a new prescription if you need this medication refilled.

Travel

When traveling with your medication:

• Always carry your medication with you. When flying, never put it into a checked bag. Keep it in your carry-on bag.
• Don’t worry about airport X-ray machines. They can’t hurt your medication.
• You may need to show airport staff the pharmacy label for your medication. Always carry the original prescription-labeled box with you.
• Don’t put this medication in your car’s glove compartment or leave it in the car. Be sure to avoid doing this when the weather is very hot or very cold.

Clinical monitoring

Your doctor will check your blood pressure before and during treatment with celecoxib. Your doctor may also do blood tests to check how well your liver and kidneys are functioning during treatment.

Sun sensitivity

You may be more sensitive to sunlight if you take celecoxib. Protect yourself from the sun:

• Wear sun-protective clothing.
• Use sunscreen—SPF 15 or higher.
• Limit your time in direct sunlight.
• Avoid tanning beds.

Insurance

Many insurance companies require a prior authorization for this drug. This means your doctor will need to get approval from your insurance company before your insurance company will pay for the prescription.

There are other drugs available to treat your condition. Some may be more suitable for you than others. Talk to your doctor about possible alternatives.

Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Celecoxib – StatPearls – NCBI Bookshelf

Continuing Education Activity

The FDA recommends celecoxib and other NSAIDs (non-steroidal anti-inflammatory drugs), along with acetaminophen, as first-line analgesics for patients with osteoarthritis and rheumatoid arthritis. Celecoxib also has an FDA indication for the management of acute pain in adult women and primary dysmenorrhea. Furthermore, the FDA also recommends using celecoxib as an adjunct therapy in patients with familial adenomatous polyposis to reduce the number of colorectal polyps. This activity reviews the mechanism of action, adverse event profile, toxicity, dosing, pharmacodynamics, and monitoring of celecoxib, pertinent for clinicians and other interprofessional team members to allow for appropriate utilization of celecoxib.

Objectives:

• Outline the mechanism of action of celecoxib.

• Identify the approved and off-label indications for celecoxib.

• Summarize the potential adverse effects of celecoxib.

• Explain interprofessional team strategies for improving care coordination and communication to determine the appropriateness of celecoxib in the clinical setting.

Access free multiple choice questions on this topic.

Indications

Celecoxib has numerous indications, both FDA approved, and non-FDA approved.[1]

The FDA recommends celecoxib and other NSAIDs (non-steroidal anti-inflammatory drugs), along with acetaminophen, as first-line analgesics for patients with osteoarthritis and rheumatoid arthritis. Celecoxib also has an FDA indication for the management of acute pain in adult women and primary dysmenorrhea. Furthermore, the FDA also recommends using celecoxib as an adjunct therapy in patients with familial adenomatous polyposis to reduce the number of colorectal polyps.[2]

Off-label, celecoxib can be used for a wide variety of musculoskeletal and rheumatologic conditions, including ankylosing spondylitis, juvenile idiopathic arthritis, and gout. It is also being used increasingly in hospital protocols as part of a multimodal perioperative pain management regimen, frequently given pre-operatively along with adjunct pain medications, including acetaminophen and/or pregabalin. [3]

Mechanism of Action

Celecoxib is chemically designated as 4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide and is a diaryl-substituted pyrazole. The mechanism of action of celecoxib is due to selective inhibition of cyclooxygenase-2 (COX-2), which is responsible for prostaglandin synthesis, an integral part of the pain and inflammation pathway.[4] This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic effects. Celecoxib weakly inhibits COX-1 and, therefore, may affect platelet function less than aspirin.

Celecoxib also has anticancer properties discussed below and exerts its anticancer properties by binding cadherin-11 (CDh21), which likely plays a significant role in the malignant progression of cancerous cells.[5]

Celecoxib is extensively metabolized through cytochrome P450 2C9 (CYP2C9) and may have interactions with other medications that are substrates of CYP2C9.[6]

Administration

Celecoxib is a medication taken orally and comes in 50, 100, 200, and 400 mg doses. In rare cases, celecoxib can also be added to customized compounds for topical administration with or without the use of iontophoresis or other topical delivery mechanisms. It is not available via any other route of administration.

Dosing for approved indications is as follows:

Osteoarthritis: 200 mg orally daily, or alternatively, 100 mg twice daily.

Rheumatoid Arthritis: 100 to 200 mg by mouth twice daily, using the lowest effective dose.

Ankylosing Spondylitis: 200 mg by mouth daily. Dosing can increase to 400 mg. Always use the lowest effective dose for the shortest possible treatment duration. Prescribers should consider discontinuing the drug if there is no response at the highest dose after six weeks.

Dysmenorrhea: 200 mg by mouth twice daily. Dosing can increase to 400 mg. Always use the lowest effective dose for the shortest possible treatment duration. Prescribers should consider discontinuing the drug if there is no response at the highest dose after six weeks.

Acute Pain: 200 mg orally twice daily; patients can start with 400 mg for a single dose on day one of therapy, with an additional 200 mg on the first day if necessary.

All doses should be given with food if GI upset occurs. In patients who are poor CYP2C9 metabolizers, consider starting at 50% of the lowest dose. Avoid use in renal impairment of creatinine clearance is less than 30 mL/s. Also, avoid use in hepatic insufficiency if the patient isChild-Pugh Class C.

Adverse Effects

Like all NSAIDs, celecoxib carries an FDA boxed warning for cardiovascular risk, including the increased risk of heart attacks and strokes. As a selective COX-2 inhibitor, celecoxib also faces scrutiny for increased cardiovascular risk since another selective COX-2 inhibitor, rofecoxib, was withdrawn from production in 2004 due to cardiovascular risk concerns. Extensive reviews have had mixed results regarding whether celecoxib carries non-inferior or increased cardiovascular risk compared to ibuprofen and naproxen. [7][8]

Also, like all NSAIDs, celecoxib carries an additional FDA boxed warning for gastrointestinal (GI) effects, including bleeding, ulceration, and perforation of the stomach and intestines. This adverse effect makes it particularly dangerous to susceptible populations such as the elderly.[9]

In addition to these, celecoxib may cause new or worsening hypertension, fluid retention in patients with congestive heart failure, renal toxicity, liver toxicity, anaphylactic reactions, and skin changes ranging from a non-severe rash to Stevens-Johnson syndrome.

Contraindications

Due to its cardiovascular risk, celecoxib is contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graph (CABG) surgery.

Celecoxib also contains a sulfonamide group and is contraindicated in patients who have demonstrated severe allergic reactions to drugs with a sulfonamide group, e.g., sulfamethoxazole. Studies have shown that allergies to sulfonamide antimicrobials are indeed a risk factor for allergic reactions to the sulfonamide chemical group. Non-antimicrobial drugs that contain a sulfonamide chemical group such as celecoxib, a history of penicillin allergy is at least as strong a risk factor for an allergic reaction. Thus, providers should understand that this phenomenon is likely not solely due to cross-reactivity of sulfonamide-containing antimicrobials and non-antimicrobials and that certain patients have an increased propensity to celecoxib allergy if they are allergic to any antimicrobial drug.[10]

Since CYP2C9 metabolizes celecoxib, its use requires caution in patients taking medicines that inhibit CYP2C9, for example, fluconazole, which is an antifungal drug.[6]

Like all NSAIDs, celecoxib should not be taken after 29 weeks of pregnancy.

Monitoring

Due to the risk for celecoxib to cause new or worsening hypertension, fluid retention in patients with congestive heart failure, renal toxicity, liver toxicity, anaphylactic reactions, and skin changes ranging from a non-severe rash to more severe reactions including Stevens-Johnson syndrome, prescribers need to monitor patients for adverse drug reactions. Prescribers should monitor a patient’s blood pressure, renal and liver function and monitor for signs and symptoms of GI bleeding.

Patients taking such medications as lithium or warfarin should have the concentrations of these drugs monitored more carefully as well due to celecoxib’s renal toxicity and inhibition of CYP2C9, respectively. Plasma concentrations of celecoxib are not routinely part of the monitoring to determine therapeutic efficacy.

Toxicity

Unfortunately, no antidotes for celecoxib overdose are available. However, celecoxib is a relatively safe medication overall. There were no reported overdoses of celecoxib during FDA trials, and doses up to 2400 mg per day for ten days did not result in severe toxicity.

Symptoms of celecoxib overdose would likely be similar to overdoses of other NSAIDs, which include lethargy, drowsiness, nausea, vomiting, and epigastric pain. Activated charcoal may be administered for overdose treatment at the discretion of emergency medical providers if the patient presents within 4 hours of known or suspected ingestion of significant amounts of celecoxib.  Due to high plasma protein binding, dialysis, urine alkalinization, or diureses are unlikely to have a significant therapeutic effect on celecoxib overdose.[9]

Enhancing Healthcare Team Outcomes

Significant opportunities are available for improved interprofessional care coordination with regard to celecoxib.

As mentioned above, in the inpatient setting, celecoxib is increasingly being used as part of pre-operative and post-operative multimodal pain management algorithms. Research has shown in several small randomized trials that administering celecoxib peri-operatively for elective procedures such as total hip arthroplasties, total knee arthroplasties, and other procedures with some success in reducing pain and improving functionality such as early ambulation. The use of non-opioid medications to improve pain and function after surgery is becoming increasingly important due to societal and political pressure to reduce overall opioid analgesic consumption as a response to increasing rates of overdose deaths. It is, therefore, important for clinicians (including MDs, DOs, PAs, and NPs), nurses, pharmacists, physical and occupational therapists, and other support staff to coordinate a concerted effort to set patient-specific goals regarding pain and function in the acute care and rehabilitative settings and to reinforce how celecoxib use can help to achieve these goals to the patient. Clinicians and the interprofessional health care team must also maintain constant and open communication while monitoring the patient for improvements in pain and function and for possible adverse effects the patient may be experiencing. This interprofessional approach will yield the best therapeutic results while minimizing the chance of adverse events. [Level 5]

In the outpatient setting, prescribers of celecoxib must also coordinate with pharmacists to prevent and monitor for unsafe drug interactions and with the patient, family members, and caregivers to monitor therapeutic benefit and possible adverse drug effects. When the caregivers function as an interprofessional team, patients can obtain maximum benefit with celecoxib with minimal adverse effects.

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References

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McCormack PL. Celecoxib: a review of its use for symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Drugs. 2011 Dec 24;71(18):2457-89. [PubMed: 22141388]

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Tołoczko-Iwaniuk N, Dziemiańczyk-Pakieła D, Nowaszewska BK, Celińska-Janowicz K, Miltyk W. Celecoxib in Cancer Therapy and Prevention – Review. Curr Drug Targets. 2019;20(3):302-315. [PubMed: 30073924]

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Pitchon DN, Dayan AC, Schwenk ES, Baratta JL, Viscusi ER. Updates on Multimodal Analgesia for Orthopedic Surgery. Anesthesiol Clin. 2018 Sep;36(3):361-373. [PubMed: 30092934]

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McAdam BF, Catella-Lawson F, Mardini IA, Kapoor S, Lawson JA, FitzGerald GA. Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: the human pharmacology of a selective inhibitor of COX-2. Proc Natl Acad Sci U S A. 1999 Jan 05;96(1):272-7. [PMC free article: PMC15129] [PubMed: 9874808]

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Assefnia S, Dakshanamurthy S, Guidry Auvil JM, Hampel C, Anastasiadis PZ, Kallakury B, Uren A, Foley DW, Brown ML, Shapiro L, Brenner M, Haigh D, Byers SW. Cadherin-11 in poor prognosis malignancies and rheumatoid arthritis: common target, common therapies. Oncotarget. 2014 Mar 30;5(6):1458-74. [PMC free article: PMC4039224] [PubMed: 24681547]

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Wang B, Wang J, Huang SQ, Su HH, Zhou SF. Genetic polymorphism of the human cytochrome P450 2C9 gene and its clinical significance. Curr Drug Metab. 2009 Sep;10(7):781-834. [PubMed: 19925388]

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Nissen SE. Cardiovascular Safety of Celecoxib, Naproxen, or Ibuprofen for Arthritis. N Engl J Med. 2017 Apr 06;376(14):1390. [PubMed: 28379793]

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Barcella CA, Lamberts M, McGettigan P, Fosbøl EL, Lindhardsen J, Torp-Pedersen C, Gislason GH, Olsen AS. Differences in cardiovascular safety with non-steroidal anti-inflammatory drug therapy-A nationwide study in patients with osteoarthritis. Basic Clin Pharmacol Toxicol. 2019 May;124(5):629-641. [PubMed: 30484960]

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García-Rayado G, Navarro M, Lanas A. NSAID induced gastrointestinal damage and designing GI-sparing NSAIDs. Expert Rev Clin Pharmacol. 2018 Oct;11(10):1031-1043. [PubMed: 30139288]

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Strom BL, Schinnar R, Apter AJ, Margolis DJ, Lautenbach E, Hennessy S, Bilker WB, Pettitt D. Absence of cross-reactivity between sulfonamide antibiotics and sulfonamide nonantibiotics. N Engl J Med. 2003 Oct 23;349(17):1628-35. [PubMed: 14573734]

Disclosure: Brandon Cohen declares no relevant financial relationships with ineligible companies.

Disclosure: Charles Preuss declares no relevant financial relationships with ineligible companies.

No cardiovascular safety concerns for Celebrex

Treatment of acute attacks of gout | Clinical Rheumatology Hospital №25

Treatment of acute gout attack | Clinical Rheumatology Hospital №25

Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for the treatment of acute attacks of gout , which have a number of advantages:

• Low incidence of side effects

• Possibility of replacement with other drugs

• Quick effect

• Good tolerance

NSAIDs (nimesulide, meloxicam, celecoxib) are widely used in chronic gout. The combined drug Allomaron is sometimes very effective (already in the second week of taking the uric acid balance approaches normal values. Currently, methods of extracorporeal hemocorrection (EG) are widely used in the treatment of gout, which are more effective in “cleansing the blood” from various toxins and toxic Due to their use, pathological substances are removed from the patient’s body, which significantly reduces the severity of gout, reduces the severity of the articular syndrome, improves kidney function, immunological characteristics. 0006

To prevent recurrent attacks of gouty arthritis, it is necessary to achieve a decrease in the level of uric acid in the plasma, for this two groups of drugs are used: drugs that promote the excretion of uric acid by the kidneys (urocosuric) and drugs that reduce its synthesis (uricodepressive)

Thus , reducing the severity of gout and gouty arthritis is facilitated by diet, regular intake of basic drugs (uricosuric, uricodepressive), if necessary – NSAIDs, as well as conducting EG courses at intervals of 6-8 months

One of the auxiliary methods of treating gout is HIRUDO THERAPY – treatment with leeches, especially if physiotherapy is contraindicated for the patient.

According to our observations, as a rule, kind and intelligent people suffer from gout; and this pattern requires further study.

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