Flurbiprofen

Pronunciation: FLUR-bi-PROE-fen
Class: NSAID

Trade Names

Flurbiprofen
- Tablets 50 mg
- Tablets 100 mg

Apo-Flurbiprofen (Canada)
Flurbiprofen Sodium

Ocufen
- Ophthalmic solution 0.03%

Pharmacology

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

Pharmacokinetics

Absorption

T max is about 2 h (range, 1.2 to 2.3 h).

Distribution

Flurbiprofen is more than 99% protein bound. Vd is 0.12 L/kg.

Metabolism

The major metabolite is 4′-hydroxy-flurbiprofen.

Elimination

The t ½ is about 4.7 to 5.7 h. Less than 3% of flurbiprofen is excreted unchanged in the urine; 70% of the dose is eliminated in the urine as parent drug and metabolites.

Special Populations

Renal Function Impairment

Elimination of flurbiprofen metabolites may be reduced; dose reduction may be necessary to prevent accumulation of flurbiprofen metabolites.

Hepatic Function Impairment

Hepatic metabolism may account for 90% or more of flurbiprofen elimination; protein binding may be decreased in patients with liver disease and serum albumin concentrations less than 3.1 g/dL.

Indications and Usage

Oral

Treatment of rheumatoid arthritis and osteoarthritis.

Ophthalmic

Inhibition of intraoperative miosis.

Contraindications

History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; treatment of perioperative pain in the setting of coronary artery bypass graft surgery (PO only); hypersensitivity to any component of the product.

Dosage and Administration

Rheumatoid Arthritis or Osteoarthritis
Adults

PO Starting dosage is 200 to 300 mg in divided doses 2 to 4 times daily. The largest recommended single dose in a multiple-dose regimen is 100 mg. Adjust dose and frequency per patient needs.

Inhibition of Intraoperative Miosis
Adults

Topical 1 drop of 0.03% solution every 30 min beginning 2 h before surgery (4 drops total).

General Advice

  • Administer tablets without regard to meals, but administer with food if GI upset occurs.

Storage/Stability

Store tablets and ophthalmic solution at controlled room temperature (68° to 77°F).

Drug Interactions

Aminoglycosides (eg, amikacin, gentamicin)

Plasma aminoglycoside levels may be elevated.

Angiotensin-converting enzyme (ACE) inhibitors

NSAIDs may decrease the antihypertensive effect of ACE inhibitors.

Beta-blockers

Decreased antihypertensive effect of beta-blocker.

Cimetidine

May increase AUC of flurbiprofen.

Diuretics

Decreased diuretic effect.

Lithium

Increased lithium levels and toxicity.

Methotrexate

Increased methotrexate levels and toxicity.

Salicylates

Increased risk of GI toxicity; may reduce flurbiprofen concentrations 50%. Coadministration is not recommended.

SSRIs (eg, fluoxetine, paroxetine)

The risk of GI adverse reactions may be increased.

Warfarin

Increased risk of gastric erosion and bleeding.

Laboratory Test Interactions

May prolong bleeding time.

Adverse Reactions

CNS

Amnesia, anxiety, asthenia, depression, dizziness/vertigo, headache, increased reflexes, insomnia, malaise, nervousness, somnolence, tremor (at least 1%).

Dermatologic

Rash (at least 1%).

EENT

Rhinitis, tinnitus, vision changes (at least 1%); fibrosis, increased bleeding tendency of ocular tissues in conjunction with ocular surgery, miosis, mydriasis, ocular irritation, transient burning and stinging upon instillation (ophthalmic use).

GI

Abdominal pain, constipation, diarrhea, dyspepsia/heartburn, flatulence, GI bleeding, nausea, vomiting (at least 1%).

Genitourinary

UTI (at least 1%).

Metabolic-Nutritional

Body weight changes (at least 1%).

Miscellaneous

Edema (at least 1%).

Precautions

Warnings

NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. NSAIDs cause an increased risk of serious GI adverse reactions, including bleeding, ulceration, inflammation, and perforation of the stomach or intestines, which can be fatal. These reactions can occur any time during use and without warning symptoms. Elderly patients are at greater risk of serious GI reactions.


Monitor

Carefully monitor patients who may be adversely affected by alterations in platelet function (eg, patients with coagulation disorders or receiving anticoagulant therapy). Check CBC and chemistry profile periodically. Follow chronically treated patients for signs and symptoms of GI tract ulceration and bleeding. Monitor LFTs, Hct, and Hgb periodically during long-term therapy. Monitor renal function and patient status carefully in patients with renal function impairment. Perform eye examination if patient experiences visual disturbances.


Pregnancy

Category C . Avoid in late pregnancy.

Lactation

Excreted in breast milk (tablets); undetermined (ophthalmic).

Children

Safety and efficacy not established.

Elderly

Use with caution.

Hypersensitivity

May occur; do not use in aspirin-sensitive individuals because of possible cross-sensitivity.

Renal Function

Use is not recommended in patients with advanced kidney disease. Long-term treatment with NSAIDs may result in renal papillary necrosis and other renal injury.

Hepatic Function

Use with caution.

Special Risk Patients

Use with caution in patients with fluid retention, hypertension, or heart failure.

Hazardous Tasks

May cause drowsiness or dizziness.

Anaphylactoid reactions

Do not administer to patients with aspirin triad, which typically occurs in patients with asthma who experience rhinitis with or without nasal polyps, or who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.

Asthma

Patients with asthma may have aspirin-sensitive asthma, which may be associated with severe and sometimes fatal bronchospasm. Do not administer flurbiprofen to patients with this type of aspirin-sensitivity because of possible cross-reactivity.

Bleeding

May inhibit platelet aggregation. Use with caution in patients with known bleeding tendencies or who are receiving other medications that may prolong bleeding time.

Dehydration

Use with caution. Rehydrate patient before instituting therapy.

Hematologic effects

Anemia may occur with NSAID use.

Hypertension

New hypertension or worsening of preexisting hypertension, either of which may contribute to increased risk of CV events, may occur.

Peripheral edema

Has been observed. Use with caution in patients with hypertension or compromised cardiac function.

Platelet function

NSAIDs inhibit platelet aggregation and have been reported to prolong bleeding time.

Skin reactions

Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, may occur.

Vision changes

Blurred and/or diminished vision may occur.

Overdosage

Symptoms

Acute renal failure, coma, drowsiness, epigastric pain, GI bleeding, hypertension, lethargy, nausea, respiratory depression, vomiting.

Patient Information

  • Advise patient to review Medication Guide before using the first time and with each refill.
  • Advise patient that dose is individualized based upon condition being treated, severity of symptoms, and response to therapy.
  • Instruct patient to take prescribed dose without regard to meals, but to take with food if stomach upset occurs.
  • Caution patient not to change dose or stop taking unless advised by health care provider.
  • Advise patient to notify health care provider if medication does not adequately control pain or arthritis symptoms.
  • Caution patient to avoid smoking, alcohol, and self-administration of aspirin-containing medications while taking flurbiprofen.
  • Advise patient that if a dose is missed to take it as soon as possible. If close to the next dose, skip the missed dose and take the next dose at the regularly scheduled time. Caution patient not to double the dose to catch up.
  • Advise patient to seek emergency medical assistance if any of the following occur: shortness of breath or trouble breathing, chest pain, weakness in one part or on one side of body, slurred speech, swelling of the face or throat.
  • Advise patient to discontinue drug and immediately notify health care provider if any of the following occur: persistent or recurrent stomach upset or stomach pain, skin rash or itching, vomiting blood, bloody or black stools, rapid weight gain or swelling, changes in urine patterns, fever, bleeding or unusual bruising, unexplained tiredness or fatigue, intestinal flu-like symptoms, yellowing of the skin or eyes, visual changes.

Copyright © 2009 Wolters Kluwer Health.

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