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flurbiprofen (Ansaid, Ocufen, Ropion, Flurofen)
Tradenames: Ansaid. (also see flurbiprofen ophthalmic)
Indications:
1) acute & long-term treatment of arthritis
a) osteoarthritis
b) rheumatoid arthritis
2) ophthalmic
a) reduction of inflammation after eye surgery
b) blepharoconjunctivitis
3) off-label uses
a) ankylosing spondylitis
b) pain
c) rotator cuff tendonitis
d) bursitis
e) gout
f) aborting acute migraine headache
Dosage:
1) 200-300 mg/day, divided BID/TID/QID
2) maximum single dose of 100 mg
Tabs: 50, 100 mg
Pharmacokinetics:
1) time to peak plasma levels in 1-2 hours
2) onset of action 1-2 hours
3) metabolized in the liver by cyt P450 2C9
4) t1/2 of 5-6 hours
5) metabolites eliminated in the urine prmarilyas glucuronates & sulfates
Adverse effects:
1) common (> 10%)
- skin rash, dizziness, abdominal cramps, heartburn, indigestion, nausea
2) less common (1-10%)
- itching, ringing in ears, fluid retention, headache, nervousness, vomiting
3) 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:
1) carbachol & acetylcholine may be ineffective when used in combination with ophthalmic flurbiprofen (Ocufen)
2) any drug which inhibits cyt P450 2C9 can increase flurbiprofen levels
3) any drug which induces cyt P450 2C9 can diminish flurbiprofen levels
4) flurbiprofen may increase digoxin, methotrexate & lithium levels
5) decreased antihypertensive effects of:
- beta blockers, ACE inhibitors, thiazide diuretics
6) increased response to sympathomimetics
7) effect of loop diuretics may be increased
Mechanism of action:
1) non-steroidal anti-inflammatory agent
2) little effect on pre-existing trauma-induced miosis
3) no effect on intraocular pressure
4) directly interacts with APP gamma secretase to inhibit formation of amyloid beta peptide A4/42 [5]
Interactions
drug interactions
drug adverse effects of NSAIDs
monitor with non steroidal anti-inflammatory agents (NSIADs)
Related
cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)
Specific
flurbiprofen (Ocufen)
flurbiprofen topical
tarenflurbil (Flurizan, R-flurbiprofen)
General
non-steroidal anti-inflammatory agent (NSAID)
Properties
INHIBITS: cyclooxygenase
MISC-INFO: elimination route LIVER
protein-binding 99%
pregnancy-category B
safety in lactation -
Database Correlations
PUBCHEM correlations
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#: 220233
(subscription needed) http://www.prescribersletter.com
- 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: 12897211