Usage
Flurbiprofen, a non-steroidal anti-inflammatory drug (NSAID), is prescribed for:
- Relief of signs and symptoms of osteoarthritis.
- Relief of signs and symptoms of rheumatoid arthritis.
- Management of mild to moderate pain (e.g., dysmenorrhea, post-operative pain, dental pain, migraine).
- Treatment of ankylosing spondylitis, musculoskeletal disorders, and soft tissue injuries (e.g., bursitis, tendinitis).
Pharmacological Classification: Non-steroidal anti-inflammatory drug (NSAID), analgesic, antipyretic
Mechanism of Action: Flurbiprofen inhibits cyclooxygenase (COX-1 and COX-2), enzymes responsible for prostaglandin synthesis. Prostaglandins mediate inflammation, pain, and fever; hence, inhibiting their production results in therapeutic effects.
Alternate Names
- Flurbiprofeno (Spanish)
- Flurbiprofène (French)
Brand Names:
- Ansaid
- Froben
- Fluprofen
- Ocufen (ophthalmic formulation)
How It Works
Pharmacodynamics: Flurbiprofen exerts its therapeutic effects by inhibiting prostaglandin synthesis, thereby reducing inflammation, pain, and fever.
Pharmacokinetics:
- Absorption: Flurbiprofen is rapidly and almost completely absorbed after oral administration. Food or antacids may delay absorption but do not affect the total amount absorbed. Peak plasma concentrations are achieved in about 1-2 hours for oral tablets.
- Metabolism: Primarily metabolized in the liver via hydroxylation and conjugation reactions. Minimal chiral inversion from the R-enantiomer to the S-enantiomer occurs. Major metabolites include 4’-hydroxy-flurbiprofen, 3’,4’-dihydroxy-flurbiprofen, 3’-hydroxy-4’-methoxy-flurbiprofen, and their conjugates.
- Elimination: Primarily eliminated through renal excretion of metabolites. Elimination may be slower in patients with renal impairment.
Mode of Action: Flurbiprofen competitively inhibits both COX-1 and COX-2 isoforms, blocking the conversion of arachidonic acid to prostaglandins.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Inhibition of COX-1 and COX-2 enzymes.
Dosage
Standard Dosage
Adults:
- Rheumatoid Arthritis and Osteoarthritis: 200-300 mg/day orally, divided into 2-4 doses. Maximum single dose: 100 mg. Adjust dose to the lowest effective level for maintenance.
- Dysmenorrhea: Initial dose: 100 mg, followed by 50-100 mg every 4-6 hours as needed. Maximum daily dose: 300 mg.
- Mild to Moderate Pain: 50-100 mg every 4-6 hours as needed. Maximum daily dose: 300 mg.
Children: Use is not recommended for children under 12 years of age. Safety and efficacy have not been established in pediatric populations.
Special Cases:
- Elderly Patients: Initiate therapy at the lowest effective dose and monitor closely. Reduced renal clearance may necessitate dose adjustments.
- Patients with Renal Impairment: In mild to moderate impairment, consider dose reduction. Flurbiprofen is contraindicated in severe renal impairment (creatinine clearance <30 mL/min).
- Patients with Hepatic Dysfunction: Consider dose reduction in mild to moderate impairment. Flurbiprofen is contraindicated in severe hepatic impairment.
Clinical Use Cases
Dosage recommendations for intubation, surgical procedures, mechanical ventilation, ICU use, and emergency situations have not been established for flurbiprofen. Its use in these settings should be considered carefully and individualized based on patient needs and clinical judgment.
Side Effects
Common Side Effects
- Gastrointestinal: Indigestion, heartburn, abdominal pain, nausea, vomiting, diarrhea, constipation.
- Central Nervous System: Dizziness, headache, drowsiness, nervousness, confusion, tremors.
- Dermatological: Itching, rash, increased sweating.
- Other: Ringing in the ears.
Rare but Serious Side Effects
- Cardiovascular: Myocardial infarction, stroke, heart failure, hypertension.
- Gastrointestinal: Gastrointestinal bleeding, ulceration, perforation.
- Hepatic: Hepatotoxicity, jaundice.
- Renal: Renal failure, fluid retention.
- Hypersensitivity: Anaphylaxis, angioedema, urticaria, asthma exacerbation.
Adverse Drug Reactions (ADR)
- Stevens-Johnson Syndrome
- Toxic Epidermal Necrolysis
Contraindications
- Hypersensitivity to flurbiprofen or any NSAID.
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
- Active peptic ulcer disease.
- History of gastrointestinal bleeding or perforation related to previous NSAID therapy.
- Severe heart failure, hepatic failure, or renal failure.
- Peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
- Third trimester of pregnancy.
Drug Interactions
- Anticoagulants (e.g., warfarin): Increased risk of bleeding.
- Antiplatelets (e.g., aspirin, clopidogrel): Increased risk of bleeding.
- Corticosteroids (e.g., prednisone): Increased risk of gastrointestinal ulcers.
- Methotrexate: Increased methotrexate toxicity.
- Cyclosporine: Increased cyclosporine levels and risk of nephrotoxicity.
- Digoxin: Increased digoxin levels.
- ACE inhibitors, Beta-blockers, and Diuretics: Reduced antihypertensive effect.
- SSRIs: Increased risk of GI bleed.
- Alcohol: Increased risk of gastrointestinal bleeding.
Pregnancy and Breastfeeding
- Pregnancy: Avoid use during the third trimester due to the risk of premature closure of the ductus arteriosus. Use during the first and second trimesters should be minimized and carefully considered. May cause harm to the fetus.
- Breastfeeding: Small amounts of flurbiprofen are excreted in breast milk. Consider the potential risk to the infant. An alternative safer option may be preferred, especially when nursing a newborn or preterm infant.
Drug Profile Summary
- Mechanism of Action: Inhibits COX-1 and COX-2, reducing prostaglandin synthesis and thereby inflammation, pain, and fever.
- Side Effects: Common: GI upset, dizziness, headache. Serious: GI bleeding, cardiovascular events, hepatotoxicity.
- Contraindications: Hypersensitivity to NSAIDs, history of asthma/urticaria following NSAID use, active peptic ulcer, severe heart/liver/renal failure, CABG surgery, third-trimester pregnancy.
- Drug Interactions: Anticoagulants, antiplatelets, corticosteroids, methotrexate, cyclosporine.
- Pregnancy & Breastfeeding: Avoid in the third trimester. Use with caution during the first and second trimesters. Small amounts are excreted in breast milk.
- Dosage: Adults: 200-300 mg/day divided, max 100mg/dose. Adjust based on indication and patient characteristics. Not recommended for children under 12.
- Monitoring Parameters: Renal and liver function tests, signs of GI bleeding, blood pressure.
Popular Combinations
No regularly recommended specific drug combinations exist. Prescribing flurbiprofen concomitantly with other medications requires careful consideration of potential interactions. Gastroprotective agents may be co-prescribed if deemed necessary.
Precautions
- General Precautions: Evaluate renal and hepatic function, cardiovascular risk, and history of peptic ulcer disease before initiating therapy.
- Pregnant Women: Avoid use during the third trimester. Minimize and carefully consider use during the first and second trimesters.
- Breastfeeding Mothers: Assess infant risk. An alternative may be preferred.
- Children & Elderly: Not recommended for children under 12. Initiate therapy with the lowest effective dose in the elderly and monitor for adverse effects.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Flurbiprofen?
A: For osteoarthritis and rheumatoid arthritis in adults: 200-300 mg/day orally, divided into 2-4 doses, with a maximum single dose of 100 mg. For dysmenorrhea: 100 mg initially, followed by 50-100 mg every 4-6 hours as needed, with a maximum daily dose of 300 mg. Adjust dosage based on individual patient characteristics, especially in elderly patients and those with renal or hepatic impairment. Not recommended for children under 12.
Q2: What are the most common side effects of Flurbiprofen?
A: Common side effects include gastrointestinal issues (indigestion, heartburn, nausea, vomiting, diarrhea, constipation), dizziness, headache, drowsiness, and ringing in the ears.
A: Signs of gastrointestinal bleeding (e.g., black, tarry stools, coffee-ground emesis), symptoms suggestive of cardiovascular events (chest pain, shortness of breath, weakness on one side of the body), allergic reactions (e.g., swelling of the face, lips, or tongue, difficulty breathing, hives), signs of hepatotoxicity (jaundice, dark urine), and acute renal failure should prompt immediate medical evaluation.
Q4: Is Flurbiprofen safe during pregnancy?
A: Flurbiprofen should be avoided during the third trimester of pregnancy due to the risk of premature closure of the ductus arteriosus. Use in the first and second trimesters should be minimized and carefully considered after assessing the potential benefits and risks.
Q5: Can Flurbiprofen be used while breastfeeding?
A: Flurbiprofen is excreted in breast milk in small amounts. Exercise caution and consider potential risks to the infant. An alternative may be preferred, particularly if breastfeeding a newborn or pre-term infant.
Q6: What are the contraindications for using Flurbiprofen?
A: Contraindications include hypersensitivity to flurbiprofen or any NSAID, history of asthma/urticaria following NSAID use, active peptic ulcer disease, severe heart/liver/renal failure, CABG surgery, and third-trimester pregnancy.
Q7: How does Flurbiprofen interact with other medications?
A: Flurbiprofen can interact with several medications, including anticoagulants, antiplatelets, corticosteroids, methotrexate, cyclosporine, and digoxin. Discuss all concomitant medications with your patients to assess potential interactions.
Q8: What precautions should be taken when prescribing Flurbiprofen to elderly patients?
A: Initiate therapy with the lowest effective dose and titrate cautiously. Closely monitor for adverse effects, especially gastrointestinal and cardiovascular events, as elderly patients are at increased risk. Renal function should be assessed before initiating treatment and monitored periodically during therapy.
Q9: What is the mechanism of action of Flurbiprofen?
A: Flurbiprofen inhibits cyclooxygenase (COX-1 and COX-2), the enzymes responsible for prostaglandin synthesis. This leads to a decrease in prostaglandin production, reducing inflammation, pain, and fever.
Q10: Can Flurbiprofen be used for pain relief in children?
A: Flurbiprofen is generally not recommended for children under 12 years old, as its safety and efficacy have not been adequately studied in this population. Consult with a pediatric specialist for pain management options in younger children.
