Flurbiprofen


Thông tin thuốc gốc
Chỉ định và Liều dùng
Mouth/Throat
Sore throat
Adult: As 8.75 mg spray: 3 actuations (1 dose) to the back of the throat every 3-6 hours, as necessary. Max: 5 doses in 24 hours. Max duration: 3 days.

Ophthalmic
Prophylaxis of miosis during ocular surgery
Adult: As 0.03% solution: Instill 1 drop into the eye every 30 minutes starting 2 hours before surgery until 30 minutes prior to surgery.

Ophthalmic
Postoperative ocular inflammation
Adult: As 0.03% solution: Instill 1 drop into the eye (starting at 24 hours after surgery) 4 times daily for 1-3 weeks.

Oral
Sore throat
Adult: As 8.75 mg lozenge: Dissolve 1 lozenge slowly in the mouth every 3-6 hours, as necessary. Max: 5 lozenges in 24 hours. Max duration: 3 days.

Oral
Dysmenorrhoea
Adult: Initially, 100 mg followed by 50 or 100 mg every 4-6 hours. Max: 300 mg daily.

Oral
Ankylosing spondylitis, Osteoarthritis, Pain and inflammation associated with musculoskeletal and joint disorders, Rheumatoid arthritis, Sprains, Strains
Adult: 150-200 mg daily in 2, 3 or 4 divided doses, may increase up to 300 mg daily in divided doses depending on severity of symptoms.
Special Patient Group
Pharmacogenomics:

Genetic polymorphism of CYP2C9 may affect the pharmacokinetics of flurbiprofen. The CYP2C9 genotype has multiple alleles identified as CYP2C9*1, CYP2C9*2 and CYP2C9*3, in which the CYP2C9*2 and *3 alleles are commonly associated with reduction of CYP2C9 activity. The frequencies of the two common variants vary among populations with distinct ethnic backgrounds. The prevalence of CYP2C9*2 and CYP2C9*3 is 1/3 in white populations. CYP2C9*2 allele does not exist in East Asian populations (Korean, Chinese, Japanese) while CYP2C9*3 allele exists in 4.6% Koreans, 3.5% Chinese and 2.8% Japanese.

According to studies, individuals who are carriers of CYP2C9*1/*3 may have increased serum concentration and decreased clearance of flurbiprofen as compared to those with CYP2C9*1/*1 genotype. However, no significant changes in the same parameters were noted in individuals with CYP2C9*1/*2, except for the elimination half-life of the parent drug. The CYP2C9*3 allele substitution is found in the substrate recognition site (SRS) 5 which affects both substrate binding and catalytic activity while CYP2C9*2 substitution is not located in SRS.

Studies suggest that individuals with known or suspected CYP2C9*1/*3 genotype may be advised to lower flurbiprofen doses than the usual dose to avoid abnormally high plasma levels due to reduced metabolic clearance.
Renal Impairment
Oral, Mouth/Throat:
Severe: Contraindicated.
Hepatic Impairment
Oral, Mouth/Throat:
Severe: Contraindicated.
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity to flurbiprofen, aspirin or other NSAIDs. History of gastrointestinal bleeding or perforation related to NSAID therapy. Active or history of gastrointestinal inflammatory disease (e.g. ulcerative colitis, Crohn’s disease), ulceration, or haemorrhage, aspirin-sensitive asthma, severe heart failure, treatment of pain in the setting of CABG. Patients with epithelial herpes simplex keratitis, known haemostatic defects, or those receiving other drugs which may prolong bleeding time (ophthalmic). Avoid ophthalmic use during surgical procedures. Severe renal and hepatic impairment. Pregnancy (3rd trimester).
Thận trọng
Patients with history of mild to moderate heart failure, peripheral arterial disease, other risk factors for CV disease (e.g. hypertension, hyperlipidaemia, diabetes mellitus, smoking); SLE, asthma, oedema, hypovolaemia. Dehydrated and debilitated patients. Renal and hepatic impairment. Elderly. Pregnancy (1st-2nd trimester) and lactation. Patients with CYP2C9*1/*3 allele. Concomitant use of corticosteroids, SSRIs, antiplatelets, or anticoagulants. Not for prolonged use.
Phản ứng phụ
Significant: Renal papillary necrosis (prolonged use). Rarely, anaphylactoid reactions, blood dyscrasias (e.g. agranulocytosis, thrombocytopenia, aplastic anaemia), hyperkalaemia.
Cardiac disorders: Cardiac failure.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Eye irritation, eye pain, eye haemorrhage, prolonged mydriasis, eye hyperaemia, visual disturbance, miosis.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, dyspepsia, flatulence, constipation, abdominal pain, melaena, haematemesis, ulcerative stomatitis, gastritis. Lozenge/throat spray: Throat irritation, mouth ulceration, oral pain or discomfort, oral paraesthesia, oropharyngeal pain.
General disorders and admin site conditions: Fatigue, malaise.
Hepatobiliary disorders: Rarely, jaundice.
Investigations: Increased liver enzymes, prolonged bleeding time.
Metabolism and nutrition disorders: Fluid retention.
Nervous system disorders: Headache, dizziness, paraesthesia, tremor.
Psychiatric disorders: Anxiety, insomnia, amnesia, depression, nervousness, somnolence.
Respiratory, thoracic and mediastinal disorders: Rhinitis.
Skin and subcutaneous tissue disorders: Rash, photosensitivity.
Vascular disorders: Hypertension.
Potentially Fatal: Gastrointestinal inflammation, bleeding, ulceration or perforation, CV thrombotic events (e.g. myocardial infarction, stroke), bronchospasm. Rarely, hepatotoxicity (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure), exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Ophth/PO: C (Avoid during 3rd trimester or late pregnancy.)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, drowsiness, fatigue and visual disturbances, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor blood pressure, CBC, chemistry profile, occult blood loss, periodic LFT, renal function (e.g. urine output, serum BUN, creatinine); ophthalmic exam (prolonged use), signs and symptoms of gastrointestinal bleeding.
Quá liều
Symptoms: Nausea, vomiting, headache, epigastric pain, gastrointestinal bleeding. Rarely, diarrhoea, disorientation, excitation, coma, drowsiness, dizziness, tinnitus, fainting, convulsions, acute renal failure and liver damage. Management: Symptomatic and supportive treatment. Consider administration of activated charcoal or perform gastric lavage within 1 hour of ingestion of a potentially toxic amount. Frequent or prolonged convulsions should be treated with intravenous diazepam or lorazepam. Monitor renal and liver function.
Tương tác
Decreased effect of diuretics, ACE inhibitors, angiotensin II antagonists, and mifepristone. Increased plasma concentration and risk of toxicity of lithium, cardiac glycosides (e.g. digoxin), phenytoin and methotrexate. Enhanced anticoagulant effect of warfarin. Increased risk of nephrotoxicity with ciclosporin, tacrolimus and diuretics. Increased risk of gastrointestinal ulceration or bleeding with other NSAIDs, corticosteroids, SSRIs, and anticoagulants or antiplatelet agents (e.g. aspirin). Increased haematological toxicity with zidovudine.
Food Interaction
Decreased rate of absorption with food.
Tác dụng
Description: Flurbiprofen, a propionic acid derivative, is an NSAID that reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, resulting in decreased formation of prostaglandin precursors. It has antipyretic, anti-inflammatory and analgesic properties.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Decreased absorption rate with food. Bioavailability: 96% (oral). Time to peak plasma concentration: Approx 2 hours (oral).
Distribution: Present in breast milk (small amount). Volume of distribution: 0.12 L/kg. Plasma protein-binding: >99%, mainly to albumin.
Metabolism: Metabolised in the liver by hydroxylation (via CYP2C9 isoenzyme) and conjugation.
Excretion: Via urine (<3% as unchanged drug; approx 70% mainly as metabolites). Elimination half-life: 4.7-5.7 hours.
Đặc tính

Chemical Structure Image
Flurbiprofen

Source: National Center for Biotechnology Information. PubChem Database. Flurbiprofen, CID=3394, https://pubchem.ncbi.nlm.nih.gov/compound/Flurbiprofen (accessed on Jan. 21, 2020)

Bảo quản
Store below 30°C. Protect from light. Ophthalmic: Store between 15-25°C.
Phân loại ATC
S01BC04 - flurbiprofen ; Belongs to the class of non-steroidal antiinflammatory agents. Used in the treatment of inflammation of the eye.
M01AE09 - flurbiprofen ; Belongs to the class of propionic acid derivatives of non-steroidal antiinflammatory and antirheumatic products.
M02AA19 - flurbiprofen ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
R02AX01 - flurbiprofen ; Belongs to the class of other throat preparations.
References
Lee CR, Pieper JA, Frye RF, et al. Differences in Flurbiprofen Pharmacokinetics Between CYP2C9*1/*1, *1/2, and *1/*3 Genotypes. Eur J Clin Pharmacol. 2003 Feb;58:791–794. doi: 10.1007/s00228-003-0574-6. Accessed 18/07/2019

Lee YJ, Byeon JY, Kim YH, et al. Effects of CYP2C9*1/*3 Genotype on the Pharmacokinetics of Flurbiprofen in Korean Subjects. Arch. Pharm. Res.. 2015 Feb. doi: 0.1007/s12272-015-0580-0. Accessed 18/07/2019

Anon. Flurbiprofen (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/07/2019.

Anon. Flurbiprofen (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 18/07/2019.

Anon. Flurbiprofen. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/05/2014.

Buckingham R (ed). Flurbiprofen. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 18/07/2019.

Flurbiprofen Solution/Drops (Amici Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/07/2019.

Flurbiprofen Tablet (Preferred Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 18/07/2019.

Flurbiprofen. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 18/07/2019.

McEvoy GK, Snow EK, Miller J et al (eds). Flurbiprofen Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 30/05/2014.

Ocufen Ophthalmic Solution. U.S. FDA. https://www.fda.gov/. Accessed 30/05/2014.

Ocufen Solution/Drops (Allergan, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/05/2014.

Strefen Direct Oromucosal Spray (Reckitt Benckiser Healthcare UK Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 18/07/2019.

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