Celecoxib


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Osteoarthritis
Adult: 200 mg daily as a single dose or in 2 divided doses, may increase up to 200 mg bid as needed. Max: 400 mg daily. Use the lowest effective dose for the shortest possible duration.
Elderly: <50 kg: Initiate at the lowest recommended dose.

Oral
Acute pain, Primary dysmenorrhoea
Adult: Initially, 400 mg, followed by an additional dose of 200 mg if needed on day 1. Maintenance: 200 mg bid if needed. Use the lowest effective dose for the shortest possible duration. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Elderly: <50 kg: Initiate at the lowest recommended dose.

Oral
Rheumatoid arthritis
Adult: 100 mg or 200 mg bid. Max: 400 mg daily. Use the lowest effective dose for the shortest possible duration.
Elderly: <50 kg: Initiate at the lowest recommended dose.

Oral
Ankylosing spondylitis
Adult: 200 mg as a single dose or in 2 divided doses, may increase to 400 mg as a single dose or in 2 divided doses if needed. Max: 400 mg daily. Use the lowest effective dose for the shortest possible duration.
Elderly: <50 kg: Initiate at the lowest recommended dose.

Oral
Acute migraine attacks
Adult: With or without aura: 120 mg as a single dose. Max: 120 mg/24 hours. Use the lowest effective dose for the shortest possible duration. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Elderly: <50 kg: Initiate at the lowest recommended dose.

Oral
Juvenile idiopathic arthritis
Child: ≥2 years ≥10 kg to ≤25 kg: 50 mg bid; >25 kg: 100 mg bid. Use the lowest effective dose for the shortest possible duration. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Nhóm bệnh nhân đặc biệt
Pharmacogenomics:

Celecoxib is mainly metabolised by CYP2C9 enzyme into hydroxycelecoxib. CYP2C9 is a highly polymorphic gene which may influence metabolism and clearance of celecoxib, thus affecting drug exposure and potential safety. Genetic testing may be considered.

CYP2C9
According to CPIC, CYP2C9*1 is a normal function allele. Individuals carrying CYP2C9*1 allele in combination with another normal function allele may have an increased metabolism of celecoxib as compared to those carrying at least 1 copy of a decreased or no function allele. However, other genetic and clinical factors may also influence the metabolism of celecoxib.

According to CPIC, CYP2C9*2 is a decreased function allele. Individuals carrying CYP2C9*2 allele in combination with a normal, decreased allele, or no function allele may have decreased metabolism of celecoxib as compared to those with 2 normal function alleles. However, other genetic and clinical factors may also influence the metabolism of celecoxib.

According to CPIC, CYP2C9*3 is a no function allele. Individuals carrying the CYP2C9*3 allele in combination with a normal, decreased, or no function allele may have decreased metabolism of celecoxib as compared to those with 2 normal function alleles. However, other genetic and clinical factors may also influence the metabolism of celecoxib.

According to CPIC, CYP2C9*13 is a no function allele. Individuals carrying the CYP2C9*13 allele in combination with a normal, decreased, or no function allele may have decreased metabolism of celecoxib as compared to those with 2 normal function alleles. However, other genetic and clinical factors may also influence the metabolism of celecoxib.

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline as of March 2020:
Phenotype/Genotype Implications Recommendations
CYP2C9 normal metaboliser

Individuals carrying 2 normal function alleles (e.g. *1/*1) with an activity score of 2
Normal metabolism Initiate treatment with recommended starting dose.
CYP2C9 intermediate metaboliser

Individuals carrying 1 normal function allele plus 1 decreased function allele, or 1 normal function allele plus one no function allele, or 2 decreased function alleles (e.g. *1/*2) with an activity score of 1.5
Mildly reduced metabolism Initiate treatment with recommended starting dose. Use the lowest effective dosage for the shortest duration (in accordance with prescribing information and consistent with individual patient treatment goals).
CYP2C9 intermediate metaboliser

Individuals carrying 1 normal function allele plus 1 decreased function allele, or 1 normal function allele plus one no function allele, or 2 decreased function alleles (e.g. *1/*3, *2/*2) with an activity score of 1
Moderately reduced metabolism; higher plasma concentrations may increase the risk of toxicities Initiate treatment with lowest recommended starting dose. Cautiously titrate dose upward to clinical effect or maximum recommended dose. Use the lowest effective dosage for the shortest duration (in accordance with prescribing information and consistent with individual patient treatment goals). Monitor for adverse events (e.g. blood pressure, kidney function) during therapy.
CYP2C9 poor metaboliser

Individuals carrying 1 no function allele plus 1 decreased function allele, or 2 no function alleles
Significantly reduced metabolism and prolonged half-life; higher plasma concentrations may increase the risk and severity of toxicities Initiate therapy with 25-50% of the lowest recommended starting dose. Cautiously titrate dose upward to clinical effect or 25-50% of the maximum recommended dose. Use the lowest effective dosage for the shortest duration (in accordance with prescribing information and consistent with individual patient treatment goals). Upward dose titration should not occur until after steady-state is reached (at least 5 days following 1st dose). Monitor for adverse events (e.g. blood pressure, kidney function) during therapy. Alternatively, may consider other therapy not metabolised by CYP2C9.

In contrast, the US Food and Drug Administration drug label for celecoxib recommends to reduce the starting dose to half of the lowest recommended dose in patients who are known (based on genotyping) or suspected (based on the previous history with other CYP2C9 substrates) poor metabolisers of CYP2C9 (e.g. CYP2C9*3/*3). In patients with juvenile rheumatoid arthritis who are known or suspected to be poor metabolisers of CYP2C9, consider using alternative treatments.
Suy thận
Severe: Contraindicated.
Suy gan
Moderate (Child-Pugh class B): Reduce dose by 50%. Severe (Child-Pugh class C or ≥10 score): Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity to celecoxib, aspirin, sulfonamides or other NSAIDs. History of asthma, urticaria, acute rhinitis, nasal polyps, angioneurotic oedema or other allergic-type reactions after taking aspirin or other NSAIDs. Active peptic ulceration or gastrointestinal bleeding, inflammatory bowel disease, CHF (NYHA II-IV), established ischaemic heart disease, cerebrovascular disease or peripheral arterial disease. Use in the setting of CABG surgery. Severe renal (CrCl <30 mL/min) and hepatic (Child-Pugh class C or ≥10 score) impairment. Pregnancy and lactation.
Thận trọng
Patient with history of gastrointestinal complications (e.g. ulceration and bleeding), hypertension, diabetes mellitus, hyperlipidaemia, recent MI, and other CV disease risk factors (e.g. smoking, alcoholism); pre-existing asthma (without known aspirin sensitivity), pre-existing oedema, hypovolaemia. Dehydrated patient. May mask underlying fever and other signs of inflammation. Not indicated for the preventive treatment of migraine. CYP2C9 poor metabolisers. Mild to moderate renal and moderate hepatic impairment. Children and elderly.
Tác dụng không mong muốn
Significant: Fluid retention, oedema, new-onset hypertension or worsening of pre-existing hypertension, new-onset or exacerbation of heart failure; medication-overuse headache, anaemia, mild and transient transaminase elevations, acute kidney injury, interstitial nephritis, renal papillary necrosis (prolonged use).
Cardiac disorders: Angina pectoris.
Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea, dyspepsia, flatulence, vomiting, dysphagia, GERD, irritable bowel syndrome.
General disorders and administration site conditions: Influenza-like symptoms.
Injury, poisoning and procedural complications: Accidental injury.
Investigations: Increased blood creatinine, weight increased.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Headache, dizziness, hypertonia.
Psychiatric disorders: Insomnia.
Renal and urinary disorders: Nephrolithiasis, UTI.
Reproductive system and breast disorders: Benign prostatic hyperplasia.
Respiratory, thoracic and mediastinal disorders: Sinusitis, URTI, pharyngitis, dyspnoea, rhinitis, cough.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Potentially Fatal: Gastrointestinal inflammation, perforation, ulceration, or bleeding; CV thrombotic events including MI and stroke, serious hypersensitivity reactions (e.g. anaphylaxis, angioedema, drug rash with eosinophilia and systemic symptoms), severe hepatic reactions (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure). Very rarely, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.
PO: C (prior to 30 weeks gestation), D (starting at 30 weeks gestation), Z (NSAIDs caused foetal ductus arteriosus premature closure, foetal renal impairment and persistent pulmonary hypertension. Avoid near term, else use lowest dose for shortest time.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, vertigo or somnolence, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure during initial treatment and throughout therapy, CBC and chemistry profile periodically (prolonged use), liver and renal functions; signs and symptoms of gastrointestinal irritation.
Tương tác
Increased risk of gastrointestinal ulceration or bleeding with anticoagulants (e.g. apixaban), antiplatelet agents (e.g. aspirin), SSRIs, corticosteroids (e.g. glucocorticoids), and other NSAIDs. May reduce the antihypertensive effect of ACE inhibitors, ARBs, diuretics, β-blockers and other antihypertensive agents. May increase the nephrotoxic effect of ciclosporin and tacrolimus. Increases the serum concentration of lithium, digoxin and methotrexate. Increased plasma concentration with CYP2C9 inhibitors (e.g. fluconazole). Decreased plasma concentration with CYP2C9 inducers (e.g. rifampicin, carbamazepine, barbiturates), Al and Mg containing antacids. May increase serum concentration and toxicity of CYP2D6 substrates (e.g. aripiprazole, perhexiline, atomoxetine).
Potentially Fatal: Increased risk of serious bleeding events with warfarin.
Tương tác với thức ăn
High-fat meal may delay absorption time and increase bioavailability. Increased risk of gastrointestinal perforations, ulcers or bleedings with alcohol.
Tác dụng
Description:
Mechanism of Action: Celecoxib, an NSAID, is a selective cyclooxygenase-2 (COX-2) inhibitor primarily responsible for the inhibition of prostaglandin synthesis. It exhibits anti-inflammatory, analgesic and antipyretic activities.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. High-fat meal may delay absorption time and increase bioavailability. Time to peak plasma concentrations: Approx 2-3 hours.
Distribution: Enters breast milk. Plasma protein binding: Approx 97%, mainly to albumin and to a lesser extent to α1-acid glycoprotein.
Metabolism: Metabolised in the liver by CYP2C9 into inactive metabolites such as a primary alcohol, corresponding carboxylic acid and its glucuronide conjugate.
Excretion: Via faeces (approx 57% as metabolites, <3% as unchanged drug); urine (27% as metabolites, <3% as unchanged drug). Elimination half-life: Approx 11 hours.
Đặc tính

Chemical Structure Image
Celecoxib

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2662, Celecoxib. https://pubchem.ncbi.nlm.nih.gov/compound/Celecoxib. Accessed Mar. 28, 2023.

Bảo quản
Store below 30°C.
Phân loại MIMS
Thuốc kháng viêm không steroid
Phân loại ATC
M01AH01 - celecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Tài liệu tham khảo
Theken KN, Lee CR, Gong L et al. Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2C9 and Nonsteroidal Anti-Inflammatory Drugs. Clinical Pharmacology and Therapeutics. 2020 Aug;108(2):191-200. doi: 10.1002/cpt.1830. Accessed 07/12/2022

Annotation of FDA Label for Celecoxib and CYP2C9. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 07/12/2022.

Anon. Celecoxib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 17/03/2023.

Anon. Celecoxib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/12/2022.

Anon. CYP2C9 - Celecoxib (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/12/2022.

Buckingham R (ed). Celecoxib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/12/2022.

Celecoxib 200 mg Capsules, Hard (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 07/12/2022.

Celecoxib Capsule (Torrent Pharmaceuticals Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/12/2022.

Celxib 200 mg Capsule (Unison Laboratories Co., Ltd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/12/2022.

Clinical Annotation for CYP2C9*1, CYP2C9*2, CYP2C9*3, CYP2C9*13; Celecoxib (Level 1A Metabolism/PK). Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 07/12/2022.

Clinical Pharmacogenetics Implementation Consortium Guideline (CPIC) for CYP2C9 and Nonsteroidal Anti-Inflammatory Drugs. Clinical Pharmacogenetics Implementation Consortium (CPIC). https://cpicpgx.org. Accessed 07/12/2022.

Elyxyb Liquid (Biodelivery Sciences International Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/12/2022.

Joint Formulary Committee. Celecoxib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/12/2022.

Pharmacy Retailing (NZ) Limited Trading as Healthcare Logistics. Celebrex 100 mg and 200 mg Capsules data sheet 20 July 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 07/12/2022.

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