Dosing and uses of Ansaid, Flurprofen (flurbiprofen)
Adult dosage forms and strengths
tablet
- 50mg
- 100mg
Rheumatoid Arthritis
200-300 mg/day divided q6-12hr PO, not to exceed 100 mg/dose or 300 mg/day
Take with food or 8-12 oz of water to avoid GI effects
Osteoarthritis
200-300 mg/day divided q6-12hr PO, not to exceed 100 mg/dose or 300 mg/day
Take with food or 8-12 oz of water to avoid GI effects
Renal Impairment
Severe Impairment: Not recommended
Other Indications & Uses
Off-label: dysmenorrhea
Pediatric dosage forms and strengths
<12 years: Not recommended
Geriatric dosage forms and strengths
200-300 mg/day divided q6-12hr PO, not to exceed 100 mg/dose or 300 mg/day
Take with food or 8-12 oz of water to avoid GI effects
Ansaid, Flurprofen (flurbiprofen) adverse (side) effects
Frequency not defined
Edema
Fluid retention
UTI
Abdominal pain with cramps
Diarrhea
Headache
Hypersecretory conditions
Nausea
Amnesia
Bloody stools/vomit
Blurred vision
Depression
Diplopia
Gastritis
Gastrointestinal hemorrhage
Mental/mood changes
Rhinitis
Skin rash
Tinnitus
Anorexia
Anxiety
Constipation
Dizziness
Drowsiness
Flatulence
Flushing
Insomnia
Irritability
Nervousness
Tachycardia
Warnings
Black box warnings
Cardiovascular Risk
- NSAIDs may increase risk of serious cardiovascular thrombotic events, myocardial infarction (MI), and stroke, which can be fatal
- Risk may increase with duration of use
- Patients with risk factors for or existing cardiovascular disease may be at greater risk
- NSAIDs are contraindicated for perioperative pain in the setting of coronary artery bypass graft (CABG) surgery (increased risk of MI and stroke)
Gastrointestinal Risk
- NSAIDs increase risk of serious GI adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal
- GI adverse events may occur at any time during use and without warning symptoms
- Elderly patients are at greater risk for serious GI events
Contraindications
Absolute: hypersensitivity to flurbiprofen, ASA allergy, history of aspirin triad, CABg
Relative: Bleeding disorders, duodenal/gastric/peptic ulcer, stomatitis, ulcerative colitis, upper GI disease, late pregnancy (may cause premature closure of ductus arteriosus)
Cautions
Use caution in asthma (bronchial), cardiac disease, CHF, hepatic/renal impairment, HTN, SLe
Potential risk of adverse cardiovascular events
Long-term administration of NSAIDs may result in renal papillary necrosis and other renal injury; patients at greatest risk include the elderly, or those with impaired renal function, hypovolemia, heart failure, liver dysfunction, salt depletion, and individuals taking diuretics, ACE inhibitors, or ARBs
Heart Failure (HF) risk
- NSAIDS have the potential to trigger HF by prostaglandin inhibition that leads to sodium and water retention, increased systemic vascular resistance, and blunted response to diuretics
- NSAIDS should be avoided or withdrawn whenever possible
- AHA/ACC Heart Failure Guidelines; Circulation. 2016; 134
Pregnancy and lactation
Pregnancy category: C; avoid in late pregnancy
Lactation: excreted in breast milk; not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Ansaid, Flurprofen (flurbiprofen)
Mechanism of action
Inhibits synthesis of prostaglandins in body tissues by inhibiting at least 2 cyclooxygenase isoenzymes, cyclooxygenase-1 (COX-1) and -2 (COX-2)
May inhibit chemotaxis, may alter lymphocyte activity, decrease proinflammatory cytokine activity, and may inhibit neutrophil aggregation. These effects may contribute to its anti-inflammatory activity
Pharmacokinetics
Half-life elimination: 4.7-5.7 hr
Onset: rapidly and non-stereoselectively
Peak plasma time: 1.5 hr
Onset of action: 1-2 hr
Plasma concentration: <10 mcg/mL
Bioavailability: 96%
Protein bound: >99%
Vd: 0.12 L/kg
Metabolism: hepatic, P450 enzyme CYP2C9
Metabolites: 4'-hydroxy-flurbiprofen, 3',4'-dihydroxy-flurbiprofen, 3'-hydroxy-4'-methoxy-flurbiprofen (their conjugates and conjugated flurbiprofen)
Excretion: urine 70% (3% unchanged)
