Flurbiprofen

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Introduction

Generic Name: Flurbiprofen
Chemical Formula: C15H13FO2 Brand Names: Ansaid®, Ocufen® (for ophthalmic use), Froben®
Drug Class: Nonsteroidal Anti-inflammatory Drug (NSAID)

Flurbiprofen is a nonsteroidal anti-inflammatory drug (NSAID) mostly used to treat inflammation, pain, and stiffness associated with different forms of arthritis, including osteoarthritis and rheumatoid arthritis. It is a molecule belonging to the propionic acid derivative class of NSAIDs, chemically closely related to ibuprofen, and is also available in the ophthalmic dosage form.

Mechanism of Action of Flurbiprofen

Flurbiprofen works by inhibiting the enzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), which are responsible for the formation of prostaglandins. Prostaglandins are compounds that mediate inflammation, pain, and fever. By blocking COX-2, flurbiprofen decreases the pain and inflammation, while inhibition of COX-1 can result in the gastrointestinal side effects like other NSAIDs.

Pharmacokinetics

  1. Absorption:
    Flurbiprofen is rapidly absorbed after oral administration, with peak plasma levels occurring within 1 to 2 hours.
  2. Distribution:
    It is highly bound to plasma proteins (99%), allowing for the efficient distribution throughout the body, especially to sites of action.
  3. Metabolism:
    The drug is primarily metabolized by the CYP2C9 enzyme in the liver, flurbiprofen is converted into inactive metabolites, which are then excreted.
  4. Excretion:
    The drug is mostly excreted via the kidneys, with a half-life of 4 to 6 hours, making it suitable for short-term relief from pain.

Uses

  1. Osteoarthritis and Rheumatoid Arthritis:
    Flurbiprofen is used for the long-term management of osteoarthritis and rheumatoid arthritis, for reducing the joint inflammation, stiffness, and pain. It helps to improve the function of joints and quality of life by addressing chronic pain symptoms.
  2. Acute Pain Management:
    It is prescribed for short-term relief of acute musculoskeletal pain such as sprains, strains, or post-surgical discomfort. Its fast absorption makes it ideal for addressing acute pain.
  3. Ophthalmic Use:
    Flurbiprofen ophthalmic solution is used to inhibit miosis (pupil constriction) during eye surgeries, such as cataract extraction, by the reduction of inflammation in ocular tissues.
  4. Menstrual Pain:
    Flurbiprofen is sometimes prescribed to alleviate dysmenorrhea (menstrual cramps and pain) by reducing the uterine contractions and pain.

Dosage and Administration

  • Oral (for pain relief in arthritis):
    • Adults: 200-300 mg per day in divided doses (typically 2-4 doses). The maximum single dose is 100 mg.

Flurbiprofen should be taken with food to reduce gastrointestinal discomfort. Dosage should be adjusted based on individual response and history of the patient.

Side Effects

  • Common Side Effects:
    • Nausea, stomach pain, or indigestion.
    • Dizziness, headache, or drowsiness.
    • Diarrhea or constipation.
  • Serious Side Effects:
    • Gastrointestinal bleeding: Flurbiprofen can cause stomach ulcers or bleeding, especially when the use is long-term.
    • Cardiovascular Risk: Like other NSAIDs, it may increase the risk of heart attack or stroke, particularly with prolonged use.

Contraindications

  • Allergic Reactions: Contraindicated in patients with hypersensitivity to flurbiprofen or other NSAIDs.
  • Gastrointestinal Ulcers: Should not be used in the individuals with active gastrointestinal ulcers or a history of gastrointestinal bleeding.
  • Severe Kidney or Liver Disease: Contraindicated in patients with significant renal or hepatic impairment.
  • Pregnancy (Third Trimester): Should be avoided in the later stages of pregnancy due to the risk of complications for the fetus, such as the premature closure of the ductus arteriosus.

Drug Interactions

  • Anticoagulants (e.g., Warfarin): Increases the risk of bleeding with concurrent administration.
  • Other NSAIDs: Concomitant use with other NSAIDs or corticosteroids may increase the risk of gastrointestinal and kidney-related side effects.
  • ACE Inhibitors and Diuretics: Flurbiprofen can reduce the overall effectiveness of antihypertensive drugs and diuretics, increasing the risk of kidney damage.

Warnings and Precautions

  1. Gastrointestinal Risks: Prolonged use may result in serious gastrointestinal issues, including bleeding, ulceration, and perforation.
  2. Kidney Function: Flurbiprofen should be used with caution in patients with pre-existing kidney conditions.
  3. Cardiovascular Health: It may increase the risk of cardiovascular events such as heart attack or stroke, particularly in the patients with existing heart disease.

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