CELECOXIB (Celebrex): What is used for?

What is Celecoxib?

Celecoxib is an active ingredient used for the treatment of rheumatoid arthritis, arthrosis and ankylosing spondylitis.

The brand name of Celecoxib in the United States is Celebrex.

Celecoxib Mechanism of Action (MOA)

Selective inhibitor of cyclooxygenase-2 within the dose interval used in clinical practice (200-400 mg/day) and administered orally.

Therapeutic indications, uses and benefits of Celecoxib

Symptomatic relief in the treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.

Posology of Celecoxib

CAPSULE: 50 mg/1, 100 mg/1, 200 mg/1, 400 mg/1.

Adults and the elderly: 

Arthrosis and ankylosing spondylitis: 200 mg/24 h or 100 mg/12 hours.

Rheumatoid arthritis: 100 mg/12 hours. It can be increased to 200 mg/12 hours (osteoarthritis and rheumatoid arthritis) and 400 mg/day in 1 or 2 doses (ankylosing spondylitis). If after 2 weeks, there is no increase in therapeutic benefit, consider other alternatives.

Maximum dose: 400 mg/day for all indications.
Established moderate hepatic insufficiency start with ½ recommended dose.
Not indicated for children.

Mode of administration of Celecoxib

Oral use.
Administer with or without food.

Contraindications of Celecoxib

• Hypersensitivity to celecoxib, sulfonamides.
• Active peptic ulcer or gastrointestinal bleeding.
• Patients who have experienced asthma, acute rhinitis, nasal polyps, angioneurotic edema, urticaria, or other allergic-type reactions after taking ASAAs or other NSAIDs, including cyclooxygenase-2 inhibitors.
• Pregnancy and women with potential to conceive, unless they use an effective method of contraception.
• Breastfeeding.
• Severe liver dysfunction (serum albumin < 25 g/L or Child-Pugh >10). Patients with an estimated Clcr < 30 ml/min.
• Inflammatory bowel disease.
• ICC (functional classes II-IV according to NYHA).
• Ischemic heart disease, peripheral arterial disease and/or established cerebrovascular disease.

Celecoxib Warnings and Precautions

• Kidney failure and/or mild or moderate liver failure.
• Elderly.
• Patients at high risk of digestive complications associated with NSAIDs, with slow metabolization by CYP2C9, who receive another type of NSAID or ASAID (even at low doses).
• History of digestive disease (ulcer and gastrointestinal bleeding), history of heart failure, left ventricular dysfunction or hypertension, pre-existing edema, treatment with diuretics or at risk of hypovolemia.
• It is not a substitute for ASA for the prophylaxis of cardiovascular thromboembolic disease, do not interrupt antiaggregate treatments.
• Patients with cardiovascular risk (BPH, hyperlipidemia, diabetes mellitus, smokers), assess risk/benefit.
• Use the lowest effective daily dose and the shortest possible duration of treatment and periodically re-evaluate the response, especially in osteoarthritis.
• If during the treatment, there is deterioration of the renal and/or hepatic function, suspend it, as well as if cutaneous eruption, lesions of the mucous membranes or any other sign of hypersensitivity appears.
• Warnings and precautions when associated with warfarin and other oral anticoagulants.
• Masks fever and other signs of inflammation.
• Avoid concomitant use with an NSAID other than ASAID.

Liver failure

Contraindicated in severe liver failure (serum albumin < 25 g/l or Child-Pugh >10).
Caution established mild-moderate liver failure (serum albumin 25 to 35 g/l), treatment should be started at half the recommended dose.
In these patients the experience is limited to cirrhotics.

Renal insufficiency

Contraindicated in severe renal insufficiency (Clcr < 30 ml/min).

Caution in mild-moderate renal insufficiency.

Interactions of Celecoxib

• Increases nephrotoxic effect of: cyclosporine and tacrolimus.
• Increases plasma concentrations of: drugs metabolized by CYP2D6 (tricyclic antidepressants and serotonin reuptake inhibitors, neuroleptics, antiarrhythmics, etc.).
• Toxicity potency of: lithium.
• Reduces effect of: diuretics and antihypertensives.
• Action and toxicity enhanced by: fluconazole.
• Plasma concentrations reduced by: rifampicin, carbamazepine and barbiturates.

Pregnancy and Celecoxib

No clinical data available.
Potential risk unknown. May cause uterine inertia and premature closure of ductus arteriosus in the last trimester of pregnancy.

Breastfeeding

There are no studies on the excretion of celecoxib in human milk.

Celecoxib is excreted in milk from lactating rats in plasma-like concentrations.

Effects on driving ability

Patients who experience dizziness, lightheadedness, or drowsiness while taking celecoxib should refrain from driving or operating machinery.

Adverse reactions and side effects of Celecoxib

• Sinusitis.
• Upper respiratory tract infection.
• Urinary tract infection.
• Worsening of allergy.
• Insomnia.
• Dizziness.
• Hypertension.
• AMI.
• High blood pressure.
• Pharyngitis.
• Rhinitis.
• Cough.
• Dyspnea.
• Abdominal pain.
• Diarrhea.
• Dyspepsia,
• Flatulence.
• Vomiting.
• Dysphagia.
• Rash.
• Itching.
• Flu-like symptoms.
• Peripheral edema/fluid retention.

⭐⭐⭐⭐⭐ VIDEO OF CELECOXIB/CELEBREX (DRUG)

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII: JCX84Q7J1L
ChemIDplus
DrugPortal
PubChem CID:2662
NCI Thesaurus: C1728