Celecoxib - Uses, Side-Effects, and Precautions

Overview:

Celecoxib is a drug used to treat pain or inflammation caused by arthritis, ankylosing spondylitis, migraines, and menstrual cramps. It relieves short-term pain from injury, medical procedures, or other conditions. This drug is used in children two years and older with juvenile rheumatoid arthritis.

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) approved by the US Food and Drug Administration (FDA) in 1998. It belongs to a specific class of NSAIDs called COX-2 selective inhibitors. Celecoxib stops the body from making substances that cause pain and inflammation.

What Are the Indications of Celecoxib?

Celecoxib relieves pain and inflammation in conditions such as

• Ankylosing spondylitis is an inflammatory condition causing bones in the spine to fuse).

• Dysmenorrhea (Severe, frequent, and painful menstrual cramps).

• Osteoarthritis (Inflammation and degeneration of the cartilage of joints).

• Rheumatoid arthritis (An autoimmune disease where the body attacks its tissues).

• Collagen vascular disease (Chronic inflammation in the body's connective tissue).

• Autoimmune disorder (The body mistakenly attacks its cells).

• Felty's syndrome (An Autoimmune disease involving the spleen and joints)

• Rheumatoid lung (Blockage of the small airways, fluid in the chest, and high blood pressure in the lungs).

• Juvenile rheumatoid arthritis (Autoimmune condition involving swelling and inflammation of joints in children).

How Does Celecoxib Work?

Celecoxib's mechanism of action is based on the selective inhibition of cyclooxygenase-2 (COX-2). It is involved in prostaglandin synthesis, an integral part of the pain and inflammation pathway. This pharmacological activity gives Celecoxib its analgesic, anti-inflammatory, and antipyretic effects. Celecoxib is a weak COX-1 inhibitor and is less likely to impair platelet function than Aspirin.

Celecoxib also exerts its anti-cancer properties by binding to cadherin-11 (CDH11), which has anti-cancer properties as described below and likely plays an important role in the malignant progression of cancer cells.

Celecoxib is extensively metabolized by cytochrome P450 2C9 (CYP2C9) and may interact with other drugs that are substrates of CYP2C9.

What Is the Onset of Action of Celecoxib?

The maximum concentration of Celecoxib released in the blood reaches its peak approximately three hours post-oral administration. Under fasting conditions, the absorption and clearance rate of Celecoxib from the body increases, directly proportional to the dose. The entire quantity of the drug is fully absorbed by the body.

What Is the Dosage of Celecoxib?

Celecoxib is a drug taken orally and is available in 50, 100, 200, and 400 mg doses. In rare cases, Celecoxib can also be added to compounds prepared for topical administration.

For Oral Dosage Form (Capsule):

For Acute Pain or Pain During Menstruation:

• Adults: At first, 400 milligrams (mg), the second dose of 200 mg may be given on the first day if required. Then 200 mg two times daily as needed.

• Children: Use and dosage should be determined by a physician.

For Ankylosing Spondylitis or Osteoarthritis:

• Adults: 200 milligrams (mg) once or 100 mg twice daily.

• Children: Use and dosage should be determined by a physician.

For Rheumatoid Arthritis or Juvenile Rheumatoid Arthritis:

• Adults: 100 to 200 milligrams (mg) two times daily.

• Children: Dosage is based on body weight and must be determined by a physician.

• Children Under Two Years: A physician should determine use and dosage.

For Oral Form (Solution):

For Acute Migraine With or Without Aura:

• Adults: 120 milligrams (mg) once daily.

• Children: Use and dosage should be determined by a physician.

What Are the Contraindications of Celecoxib?

• Celecoxib is contraindicated for treating perioperative pain in patients with coronary artery bypass grafting (CABG) because of its effect on the cardiovascular system.

• Celecoxib also contains a sulfonamide group and is contraindicated in patients who have had a severe allergic reaction to drugs containing the sulfonamide group or sulfa drugs, e.g., Sulfamethoxazole. For non-antibacterial drugs containing sulfonamide chemicals such as Celecoxib, a history of Penicillin allergy is at least a strong risk factor for an allergic reaction.

• Celecoxib should be cautious in patients receiving CYP2C9 inhibitors, such as Fluconazole, an antifungal drug.

• Celecoxib should not be taken after 29 weeks of pregnancy.

What Are the Drug Warnings and Precautions?

Like all NSAIDs, Celecoxib carries FDA-framed warning labels for cardiovascular risks, including an increased heart attack and stroke risk. Also, like all NSAIDs, Celecoxib has additional FDA warnings for gastrointestinal (GI) effects such as bleeding, ulceration, and perforation of the stomach and intestines. This adverse effect is particularly dangerous for vulnerable populations such as the elderly. In addition, Celecoxib can cause -

• New or worsening hypertension.

• Patients with fluid retention in congestive heart failure.

• Nephrotoxicity, hepatotoxicity, anaphylactic reactions.

• Skin lesions range from a mild rash to Stevens-Johnson syndrome.

Overdose:

Symptoms of Celecoxib overdose may be similar to other NSAID overdoses, such as lethargy, drowsiness, nausea, vomiting, and epigastralgia (pain in the upper central region of the stomach).

What Are the Interactions of Celecoxib?

With Other Drugs:

Using this medicine with any of the following medicines is not recommended. Since this information does not cover all the drugs, referring to a physician is recommended.

• Ketorolac.

• Abciximab.

• Aceclofenac.

• Acemetacin.

• Acenocoumarol.

• Amtolmetin guacil.

• Anagrelide.

• Apixaban.

• Ardeparin.

• Argatroban.

• Asciminib.

• Aspirin.

• Bemiparin.

• Certoparin.

• Chlorothiazide.

• Chlorthalidone.

• Choline magnesium trisalicylate.

• Choline salicylate.

• Desmopressin.

• Fenoprofen.

• Fepradinol.

• Feprazone.

• Floctafenine.

• Flufenamic acid.

• Fluocortolone.

• Furosemide.

• Heparin.

• Hydrochlorothiazide.

• Hydrocortisone.

• Hydroflumethiazide.

• Ibuprofen.

• Iloprost.

• Imipramine.

• Indapamide.

• Ketoprofen.

• Lepirudin.

• Lithium.

• Magnesium salicylate.

• Meclofenamate.

• Mefenamic acid.

• Meloxicam.

• Methotrexate.

• Methyclothiazide.

• Methylprednisolone.

• Metolazone.

• Milnacipran.

• Morniflumate.

• Naproxen.

• Nefazodone.

• Nepafenac.

• Niflumic acid.

• Nimesulide.

• Nimesulide beta cyclodextrin.

• Potassium citrate.

• Prasugrel.

• Prednisolone.

• Prednisone.

• Proglumetacin.

• Propyphenazone.

• Protriptyline.

• Reboxetine.

• Reviparin.

• Rivaroxaban.

• Rofecoxib.

• Salicylamide.

• Salicylic Acid.

• Sertraline.

• Sibutramine.

• Sodium Salicylate.

• Spironolactone.

• Sulfasalazine.

• Tenoxicam.

• Warfarin.

• Xipamide.

With Food:

Celecoxib should be taken with food to preventgastrointestinal irritation.

With Diseases:

Using Celecoxib should be avoided if the following conditions are present.

• Anemia.

• Bleeding problems.

• Congestive heart failure.

• Edema (fluid retention or body swelling).

• Heart attack.

• Heart disease.

• Hypertension (high blood pressure).

• Kidney disease, mild to moderate.

• Stomach ulcers or bleeding.

• Stroke.

• Aspirin-sensitive asthma.

• Aspirin sensitivity.

• Kidney disease.

• Liver disease.

• Sulfa or sulfonamide allergy (e.g., Sulfamethoxazole) - Should not be used in patients with these conditions.

• Certain genetic conditions (poor CYP2C9 (a liver enzyme) metabolizers).

• Liver disease, mild or moderate.

• Dehydration.

• Hypovolemia (Low extracellular fluid volume in the body due to excessive sodium and water loss).

• Heart surgery.

With Alcohol:

Avoid drinking alcohol. Alcohol increases the risk of gastrointestinal irritation.

Habit-Forming:

This drug is not addictive and has a low tendency to be abused by its user.

Expiry Date:

Do not use the medicine beyond the expiration date printed on the back of the medicine package.