flurbiprofen (Ansaid, Ocufen, Ropion, Flurofen)
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Introduction
Tradenames: Ansaid. (also see flurbiprofen ophthalmic)
Indications
- acute & long-term treatment of arthritis
- ophthalmic
- reduction of inflammation after eye surgery
- blepharoconjunctivitis
- off-label uses
- ankylosing spondylitis
- pain
- rotator cuff tendonitis
- bursitis
- gout
- aborting acute migraine headache
Dosage
Tabs: 50, 100 mg
Pharmacokinetics
- time to peak plasma levels in 1-2 hours
- onset of action 1-2 hours
- metabolized in the liver by cyt P450 2C9
- t1/2 of 5-6 hours
- metabolites eliminated in the urine prmarilyas glucuronates & sulfates
elimination via liver
protein binding = 99 %
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- congestive heart failure, hypertension, arrhythmias, epistaxis, confusion, hallucinations, aseptic meningitis, depression, peripheral neuropathy, hives, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, gastritis, GI ulceration, cystitis agranulocytosis, anemia, hemolytic anemia, bone marrow depression, leukopenia, thrombocytopenia, hepatitis, angioedema, allergic rhinitis, toxic amblyopia, blurred vision, conjunctivitis, dry eyes, hearing loss, polyuria, shortness of breath, polydypsia, tachycardia, hot flashes, drowsiness, insomnia, acute renal failure
Drug interactions
- carbachol & acetylcholine may be ineffective when used in combination with ophthalmic flurbiprofen (Ocufen)
- any drug which inhibits cyt P450 2C9 can increase flurbiprofen levels
- any drug which induces cyt P450 2C9 can diminish flurbiprofen levels
- flurbiprofen may increase digoxin, methotrexate & lithium levels
- decreased antihypertensive effects of:
- increased response to sympathomimetics
- effect of loop diuretics may be increased
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of lithium carbonate with NSAIDs
- drug interaction(s) of NSAIDs with oral contraceptive
- drug interaction(s) of NSAIDs with SSRIs
- drug interaction(s) of NSAIDs with antidepressants
- drug interaction(s) of aspirin with NSAIDs
- drug interaction(s) of apixaban with NSAIDs
- drug interaction(s) of warfarin with NSAIDs
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs with ARBs
- drug interaction(s) of NSAIDs with aldosterone antagonis
- drug interaction(s) of NSAIDs with glucocorticoid
- drug interaction(s) of NSAIDs, diuretics & angiotensin II receptor antagonists
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
- drug interaction(s) of NSAIDs & loop diuretics
- drug interaction(s) of NSAIDs & aspirin
Mechanism of action
- non-steroidal anti-inflammatory agent
- little effect on pre-existing trauma-induced miosis
- no effect on intraocular pressure
- directly interacts with APP gamma secretase to inhibit formation of amyloid beta peptide A4/42[5]
More general terms
More specific terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Eriksen JL et al, NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo. J Clin Invest. 2003 Aug;112(3):440-9. PMID: https://www.ncbi.nlm.nih.gov/pubmed/12897211
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3394
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3395
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=41984
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=72099
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=92337