Celecoxib is a selective COX-2 inhibitor that inhibits the formation of prostaglandins resulting in anti-inflammatory, antipyretic, and analgesic effects. Unlike the non-selective non-steroidal anti-inflammatory drugs (NSAIDS) (e.g. ibuprofen and aceclofenac acid), it does not cause gastrointestinal upset such as gastritis.

It is used to treat the following conditions:

• For the Management of acute pain

• For pain and inflammation associated with Ankylosing spondylitis

• For the relief of pain and inflammation in patients 2 years of age or older with Juvenile idiopathic arthritis

• For the symptomatic treatment of Osteoarthritis

• For the treatment of Primary dysmenorrhea

• For inflammation and pain associated with Rheumatoid arthritis

Celecoxib Dose in Adults

• A General Note about Celecoxib:

  • Use the lowest possible dose
  • Use for the shortest possible time
  •  cardiovascular disease patienrs should not take
  • Avoid in patients with heart failure.

• Use of Celecoxib in the treatment of Acute pain or primary dysmenorrhea:

  • On day 1, take 400 mg as the first dose and then 200 mg more if necessary.
  • Continue taking a 200 mg maintenance dose twice daily as necessary.

• Use of Celecoxib in the treatment of Ankylosing spondylitis:

  • 100 mg twice daily or 200 mg once daily.
  • The dose may be increased to 400 mg per day after six weeks if required.
  • If the drug is not effective after 6 weeks in a dose of 400 mg per day, alternate therapies may be tried.

• Off label use as an alternative agent in the treatment of acute flare of Gouty arthritis:

  • 200 mg two times a day for the usual duration of 5 - 7 days
  • It should be initiated within 24 - 48 hours of flare onset.
  • Two to three days following the onset of the resolution of symptoms, therapy should be stopped.

• Use in the Treatment of Osteoarthritis:

  • 200 mg once a day or
  • 100 mg two times a day.

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• Use in the treatment of Rheumatoid arthritis:

  • 100 - 200 mg two times a day.

Celecoxib Dose in Children

Dose in Juvenile idiopathic arthritis (JIA):

• Children older than 2 years and Adolescents weighing 10 - 25 kgs:
  • 50 mg two times a day.
• weight of more than 25 kgs:
  • 100 mg two times a day.

Pregnancy Risk Factor C if less than than 30 weeks gestation

Pregnancy Risk Factor D if more than 30 weeks gestation

• Celecoxib, as with other NSAIDs is associated nonteratogenic results, such as the prenatal closing of ductus Arteriosus, persistent pulmonary Hypertension of the newborn (PPH), oligohydramnios and renal dysfunction or failure.
• It should not be used in autoimmune rheumatic conditions.
• Studies have also linked it to infertility, miscarriages and other problems.

Celecoxib use duringBreastfeeding:

• Celecoxib can be found in breast milk in small amounts. It is compatible with breastfeeding.
• Patients taking anticoagulants, low platelets count or platelet dysfunction should be cautious.

Celecoxib Dose in Renal Disease:

• Mild to moderate renal impairment:
  • The manufacturer does not recommend any dose adjustment, however, renal functions should be monitored.

• Severe renal impairment:
  • Not recommended in severe renal disease.

• In addition, celecoxib should be discontinued in patients who develop renal dysfunction following its use and have a persistently abnormal or worsening renal dysfunction.

Celecoxib dose in Liver Disease:

• Mild hepatic impairment (Child-Pugh class A):

  • Dose adjustment is not necessary;

• Moderate impairment (Child-Pugh class B):

  • Reduce the dose by half.

• Severe impairment (Child-Pugh class C):

  • It is contraindicated in patients with severe liver disease.

• Persistent or worsening liver function tests:

  • Therapy should be discontinued.

Common Side Effects Of Celecoxib include:

• Dermatologic:

  • Acute generalized exanthematous pustulosis
  • Exfoliative dermatitis

• Gastrointestinal:

  • Gastrointestinal perforation
  • Gastrointestinal ulcer
  • GI inflammation
  • Intestinal perforation

• Hypersensitivity:

  • Anaphylaxis

• Immunologic:

  • DRESS syndrome

• Respiratory:

• Local alveolar osteitis (post oral surgery patients)

Less Common Side Effects of Celecoxib include:

• Cardiovascular:

  • Peripheral edema

• Gastrointestinal:

  • Diarrhea
  • Dyspepsia
  • Abdominal pain
  • Flatulence
  • Gastroesophageal reflux disease
  • Vomiting

• Hepatic:

  • Increased liver enzymes

• Renal:

  • Nephrolithiasis

• Respiratory:

  • Upper respiratory tract infection
  • Sinusitis
  • Pharyngitis
  • Rhinitis
  • Dyspnea

• Miscellaneous:

  • Accidental injury

Contraindication to Celecoxib include:

• Allergic reaction to celecoxib, sulfonamides, aspirin, other NSAIDs, or any component of the formulation
• Patients suffering from NSAID- or aspirin-induced allergies, asthma, or urticaria.
• CABG surgery is performed.
• The third trimester is when you can expect to have a baby
• Breastfeeding women
• Heart failure that is severe and not compensable
• Duodenal or active gastric ulcer
• Active gastrointestinal bleeding
• Inflammatory bowel disease
• Active hepatitis or decompensated liver disease
• Grave renal impairment, CrCl less than 30mL/minute
• Hyperkalemia
• Patients under 18 years old

Warnings and Precautions

• Anaphylactoid reactions
  • Angioedema and anaphylactic reactions may occur in patients who are taking the aspirin-triad (Asthma/rhinitis and aspirin intolerance).
• Cardiovascular events [US Boxed Warning]
  • The risk of cardiovascular events such as a stroke or myocardial infarction may increase if you use celecoxib and other NSAIDs.
  • Patients with a history of cardiovascular disease or other risk factors are at greater risk.
  • NSAIDs can also affect the response to ACE inhibitors or thiazide diuretics.
  • It can cause fluid retention and sodium buildup. Patients with heart failure should avoid it.
• Gastrointestinal events: [US Boxed Warning]
  • NSAIDs increase the risk of stomach ulcers and bleeding, which might result in perforation, which could be fatal.
  • Individuals at higher risk include those who have had gastrointestinal bleeding, peptic ulcer disease, or who are old.
  • Serious GI bleeding is more likely in patients who also use steroids, SSRIs, and anticoagulants.
  • Patients at higher risk for GI bleeding are the elderly, smokers and alcoholics as well as patients with multiple comorbidities.
• Hematologic effects
  • Anemia should be checked in patients receiving long-term therapy.
  • It doesn't affect the platelet count nor the coagulation profile.
  • Celecoxib at the appropriate doses does not inhibit platelet accumulation
• Reactions to skin:
  • Celecoxib and other NSAIDs have been linked to significant skin side effects include exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis (TEN).
  • If a rash occurs, it should be stopped immediately
• Allergy to sulfonamide (sulfa):
  • Cross-sensitivity to sulfonamide antibiotics is a concern. Celecoxib should not be used by patients with severe allergic reactions to sulfonamide anti-biotics.
• Asthma
  • Aspirin-sensitive asthma patients should be advised to avoid it.
• Coronary bypass surgery for coronary artery bypass graft: [US Boxed Warning]
  • Celecoxib should not be used in conjunction with CABG (coronary bypass graft surgery). It may increase the risk for stroke and myocardial damage.
  • Patients with Cytochrome P450 deficiency of Cytochrome 2C9 should be cautious.
• Hepatic impairment
  • Individuals with moderate to severe hepatic impairment should use it with caution, and patients with severe liver illness should avoid it.
  • Patients' liver function needs to be checked on a frequent basis.
• Renal impairment
  • NSAIDs can cause a decrease in renal blood flow, which may lead to renal injury, or worsen a previously existing renal injury, especially in patients who have hypotension, heart disease, heart failure, and patients with hypotension.
  • Long-term therapy can lead to pappillary necrosis.

Celecoxib: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

• CBC
• Liver functions tests
• Renal function tests & Metabolic profile
• Observe for occult blood loss and dyspepsia
• Monitor response to treatment including pain, mobility, range of movements, grip strength, and features of inflammation
• Blood pressure at baseline and during treatment
• Observe for weight gain & edema

JIA: Monitor for development of abnormal coagulation tests with systemic onset JIA

How to Administer Celecoxib?

• You can either take celecoxib with or without food.
• Its contents can be dusted on applesauce, dumped onto a teaspoon of lukewarm or room temperature applesauce, and then immediately taken with water. It can also be consumed whole.

Mechanism of action of Celecoxib:

• It has antipyretic, anti-inflammatory, and analgesic effects.

Slowly, it isabsorbedIt is 97% bound with proteins.

It isMetabolizedThe liver converts inactive metabolites via CYP2c9 

Thehalf-life eliminationThe average time it takes to get the drug into children and adolescents is six hours, while adults can take it for up to 11 hours.

TheTime to reach peakThe serum concentration takes 3 hours. 

It isexcretedPrimarily via feces peak.

International brand names of Celecoxib:

• ACCEL-Celecoxib
• ACT Celecoxib
• AG-Celecoxib
• APO-Celecoxib
• Auro-Celecoxib
• BIO-Celecoxib
• CeleBREX
• GD-Celecoxib
• JAMP-Celecoxib
• Mar-Celecoxib
• MINT-Celecoxib
• MYLAN-Celecoxib
• PMS-Celecoxib
• Priva-Celecoxib
• RAN-Celecoxib
• RIVA-Celecox
• SANDOZ Celecoxib
• SDZ Celecoxib
• TEVA-Celecoxib
• Acicox
• Aclexa
• Algoxib
• Artilog
• Artose
• Arythrex
• Aubrex
• Brexen
• Caditar
• Cecox
• Celbexx
• Celbric
• Celcox
• Celcoxx
• Cele V
• Celebex
• Celebone
• Celebra
• Celebrex
• Celecox
• Celecsil
• Celenta
• Celexib
• Celexil
• Celib
• Celofen
• Celoxib
• Celxib
• Celzib
• Cerebrex
• Colcibid
• Colcibra
• Cox-2
• Coxib
• Coxileb
• Coxoral
• Coxzan
• Eliflam
• Eurocox
• Ezy
• Flamar
• Flamex
• Flaxel
• Flogoxib
• Geocoxib
• Icox
• Keltrex
• Letabex
• Lexfin
• Mecelxib
• Mibecerex
• Miodar
• Nacoxib
• Onsenal
• Painex
• Rancelex
• Ranselex
• Relexa
• Revcox
• Roxib
• Selexa
• Stadloric
• Stadloric 200
• Unicelib
• Valdyne
• Zecroxil
• Zobrex
• Zycel

Celecoxib brands in Pakistan: