Celecoxib; Uses, Dosage, Side Effects, Interaction, Pregnancy

Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. Inhibition of PGE2 synthesis may lead to sodium and water retention through increased fluid reabsorption in the renal medullary thick ascending loop of Henle and perhaps other segments of the distal nephron. In the collecting ducts, PGE2 appears to inhibit water reabsorption by counteracting the action of antidiuretic hormone.

Mechanism of Action of Celecoxib

The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis. Unlike most NSAIDs, which inhibit both types of cyclooxygenases (COX-1 and COX-2), celecoxib is a selective noncompetitive inhibitor of cyclooxygenase-2 (COX-2) enzyme. It binds with its polar sulfonamide side chain to a hydrophilic side pocket region close to the active COX-2 binding site. Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane.

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Celecoxibis a nonsteroidal anti-inflammatory drug that exhibits antiinflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2), and at therapeutic concentrations in humans, celecoxib does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme. In animal colon tumor models, celecoxib reduced the incidence and multiplicity of tumors.

Indications of Celecoxib

• Osteoarthritis
• Ankylosing spondylitis
• Rheumatoid arthritis
• Familial adenomatous polyposis
• Fibromatosis
• Juvenile rheumatoid arthritis
• Period pain
• Spondyloarthritis
• Acute gouty arthritis
• Familial adenomatous polyposis
• Pain, acute or chronic
• Primary dysmenorrhoea
• Rheumatoid Arthritis, Juvenile
• Frozen shoulder
• Pain with itching ,
• Temporomandibular joint disorder
• Tendonitis
• Bursitis

Contra-Indications of Celecoxib

• Systemic mastocytosis
• Increased risk of bleeding due to clotting disorder
• Alcoholism
• High blood pressure
• Chronic heart failure
• Disease of the heart and blood vessels
• Stroke
• Ulcer from stomach acid
• Stomach or intestinal ulcer
• Liver problems
• Bleeding of the stomach or intestines
• Kidney stone
• Systemic lupus erythematosus
• Visible water retention
• Pregnancy
• A mother who is producing milk and breastfeeding
• A rupture in the wall of the stomach or intestine
• Increased cardiovascular event risk
• Time immediately after coronary bypass surgery
• chronic kidney disease stage 4 (severe)

Dosage of Celecoxib

Strengths: 50 mg; 100 mg; 200 mg; 400 mg

Osteoarthritis

• Usual dose: 200 mg orally once a day OR 100 mg orally twice a day

Rheumatoid Arthritis

• Usual dose: 100 or 200 mg orally twice a day

Ankylosing Spondylitis

• Usual dose: 200 mg orally once a day OR 100 mg orally twice a day
• If no effect after 6 weeks, consider increasing dose to 400 mg orally daily
• Maximum dose: 400 mg per day

Acute Pain

• Day 1: 400 mg orally once followed by an additional 200 mg orally if needed
• Usual dose: 200 mg orally twice a day as needed

Dysmenorrhea

• Day 1: 400 mg orally once followed by an additional 200 mg orally if needed
• Usual dose: 200 mg orally twice a day as needed

Pediatric Dose for Juvenile Rheumatoid Arthritis

Age: 2 years or older

• Weight: 10 kg to 25 kg: 50 mg orally twice a day
• Weight: Greater than 25 kg: 100 mg orally twice a day

Side Effects of Celecoxib

The common

• stomach pain
• abdominal or stomach pain, cramping, or burning (severe)
• bloody or black, tarry stools
• blurred vision or any change in vision
• chest pain
• convulsions (seizures)
• fainting
• fast or irregular breathing
• fast, irregular heartbeat or pulse
• indigestion
• nausea, vomiting
• diarrhea

More common

• Acid or sour stomach
• constipation
• headache
• heartburn
• nausea or vomiting
• skin rash
• stomach pain
• constipation
• gas
• rash

Less common

• Excess air or gas in the stomach or intestines
• itching skin
• passing gas
• stomach cramps
• swelling
• weight loss
• diarrhea
• indigestion or heartburn
• nausea
• dizziness
• headache
• itching or rash

Rare

• Anxiety
• change in vision
• seizures
• abnormal or fast heart rate
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• muscle pain or cramps
• pale or yellowed skin, dark colored urine, fever, confusion or weakness;
• jaundice (yellowing of the skin or eyes);
• sore throat, and headache with a severe blistering, peeling, and red skin rash;
• swelling, rapid weight gain, feeling short of breath (even with mild exertion); or
• increased thirst, loss of appetite, urinating less than usual or not at all.

Drug Interactions of Celecoxib

Celecoxib may interact with following drugs, supplyments & may change the efficacy of drugs

• aminoglycoside antibiotics (e.g., amikacin, gentamicin, tobramycin)
• angiotensin converting enzyme (ACE) inhibitors (e.g., ramipril, enalapril, captopril, quinapril)
• angiotensin receptor blockers (ARBs; e.g., candasartan, irbesartan, losartan)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
• bisphosphonates (e.g., alendronate, etidronate)
• carbamazepine
• celecoxib
• cilostazol
• clopidogrel
• cyclosporine
• dabigatran
• dasatinib
• diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
• fluvastatin
• haloperidol
• heparin
• ibrutinib
• methotrexate
• multivitamins (with vitamins A, E) with or without minerals
• nilotinib
• non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
• omega-3 fatty acids
• omeprazole
• oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
• pentoxifylline
• phenobarbital
• phenytoin
• quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
• serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g.,  duloxetine, venlafaxine)
• sulfasalazine
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)

Pregnancy & Lactation of Celecoxib

FDA pregnancy category C

Pregnancy

Celecoxib capsules must not be used by women who are pregnant or can become pregnant (i.e. women of child bearing potential who are not using adequate contraception) during ongoing treatment. If you become pregnant during treatment with celecoxib capsules you should discontinue the treatment and contact your doctor for alternative treatment.

Lactation

Celecoxib capsules must not be used during breast-feeding.

References