Flurbiprofen, Breakthrough , Uses, Dosage, Side effects, Drug Interactions and 20 brands in Paksitan

Introduction

Flurbiprofen is a nonsteroidal anti-inflammatory drug (NSAID) that has been widely used for decades to treat various conditions characterized by pain, inflammation, and fever. As a propionic acid derivative, it belongs to the same class of medications as ibuprofen and naproxen.

First introduced in the 1980s, Flurbiprofen quickly gained popularity among healthcare professionals due to its effective analgesic and anti-inflammatory properties. It offers significant benefits for managing musculoskeletal conditions, dental pain, postoperative discomfort, and other inflammatory ailments, making it a versatile tool in pain management.

Developed initially by Boots UK, Flurbiprofen has played a crucial role in the pharmaceutical management of pain since its introduction in the mid-20th century. This drug has become essential in treating various inflammatory conditions, providing relief to millions of patients worldwide. Its ability to effectively reduce pain and inflammation has established Flurbiprofen as a significant advancement over traditional analgesics. Its widespread use and proven efficacy underscore its importance in contemporary medical practice, offering a reliable and potent option for pain and inflammation relief.

Discovery of Flurbiprofen

Flurbiprofen, a nonsteroidal anti-inflammatory drug (NSAID), was developed as part of the extensive research efforts to find effective treatments for pain, inflammation, and fever. The discovery and development of it can be traced back to the mid-20th century, a period marked by significant advancements in pharmaceutical sciences.

Early NSAID Development

The mid-20th century saw the rise of NSAIDs, with aspirin being one of the earliest and most widely used. However, the search for NSAIDs with fewer gastrointestinal side effects and better efficacy led to the exploration of various chemical compounds.

Propionic Acid Derivatives

Researchers focused on propionic acid derivatives, which include ibuprofen and naproxen. These compounds were found to have significant anti-inflammatory, analgesic, and antipyretic properties with relatively fewer side effects compared to aspirin.

Flurbiprofen Synthesis

Flurbiprofen was synthesized by Boots UK, a prominent pharmaceutical company known for its innovative drug development. The chemical structure of Flurbiprofen was designed to include a biphenyl backbone with a fluorine atom substitution, contributing to its potent anti-inflammatory effects.

Introduction and Approval

Flurbiprofen was introduced to the market in the 1980s after extensive clinical trials demonstrated its efficacy and safety. Its ability to inhibit cyclooxygenase (COX) enzymes, which play a crucial role in the synthesis of prostaglandins (mediators of inflammation and pain), positioned Flurbiprofen as a significant advancement in NSAID therapy.

Significance in Pain Management

The introduction of Flurbiprofen provided healthcare professionals with a powerful tool for managing various inflammatory conditions. Its effectiveness in reducing pain and inflammation, coupled with its relatively favourable side effect profile, made it a popular choice for treating arthritis, dental pain, postoperative pain, and other inflammatory ailments.

Key Milestones

• Synthesis by Boots UK: Flurbiprofen’s chemical synthesis marked a breakthrough in the development of propionic acid derivative NSAIDs.
• Clinical Trials: Rigorous clinical testing established the drug’s safety and efficacy, leading to its approval for medical use.
• Market Introduction: First introduced in the 1980s, Flurbiprofen quickly gained acceptance among healthcare providers for its therapeutic benefits.

Chemical Structure and Pharmacology

• Flurbiprofen is a propionic acid derivative, sharing a chemical class with other well-known NSAIDs such as ibuprofen and naproxen. The chemical name for Flurbiprofen is 2-(2-fluoro-[1,1′-biphenyl]-4-yl)propanoic acid. Its molecular formula is C15H13FO2, and it has a molecular weight of 244.26 g/mol.
• Molecular Formula: C15H13FO2
• Molecular Weight: 244.26 g/mol

Chemical Structure:

• Biphenyl Backbone: Flurbiprofen has a biphenyl structure, which consists of two benzene rings connected by a single bond.
• Fluorine Substitution: A fluorine atom is attached to one of the benzene rings, which contributes to its anti-inflammatory properties.
• Propanoic Acid Group: The propanoic acid side chain is responsible for the drug’s classification as a propionic acid derivative, similar to other NSAIDs like ibuprofen.

Pharmacology

• Flurbiprofen’s pharmacological effects are primarily due to its action on the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. These enzymes are crucial in the biosynthesis of prostaglandins, which are lipid compounds that mediate inflammation, pain, and fever.
• Mechanism of Action: Flurbiprofen inhibits both COX-1 and COX-2 enzymes, thereby reducing the formation of prostaglandins. This inhibition leads to decreased inflammation and pain.
• COX-1 Inhibition: Results in reduced protection of the gastrointestinal lining, which can lead to gastrointestinal side effects.
• COX-2 Inhibition: Primarily responsible for the anti-inflammatory and analgesic effects, as COX-2 is induced during inflammation.

Pharmacokinetics

• Absorption: Flurbiprofen is rapidly absorbed after oral administration, with peak plasma concentrations typically reached within 1 to 2 hours.
• Distribution: It is widely distributed throughout the body, with a high affinity for synovial fluid in inflamed joints.
• Metabolism: Primarily metabolized in the liver by cytochrome P450 enzymes, resulting in various metabolites, some of which retain biological activity.
• Elimination: Excreted mainly through the urine, with a small amount excreted in the faeces. The half-life of Flurbiprofen is approximately 3 to 6 hours, making it suitable for multiple dosing schedules throughout the day.

Therapeutic Effects

• Analgesic: Provides significant pain relief for conditions such as arthritis, dental pain, and postoperative pain.
• Anti-inflammatory: Effectively reduces inflammation in musculoskeletal conditions, such as rheumatoid arthritis and osteoarthritis.
• Antipyretic: Reduces fever by acting on the hypothalamic heat-regulating centres.

Flurbiprofen Uses

Flurbiprofen, a potent nonsteroidal anti-inflammatory drug (NSAID), is utilized in various medical contexts for its analgesic, anti-inflammatory, and antipyretic properties. Its wide range of uses makes it a versatile medication in the management of pain, inflammation, and fever. Below are some uses of Flurbiprofen:

1. Pain Management

• Arthritis: Flurbiprofen is commonly prescribed for the relief of pain associated with rheumatoid arthritis and osteoarthritis. Its anti-inflammatory properties help alleviate joint pain and stiffness, improving mobility and quality of life for arthritis patients.
• Dental Pain: It is effective in providing pain relief following dental procedures or in cases of dental pain due to inflammation or infection.
• Postoperative Pain: After surgical procedures, It is often administered to manage postoperative pain, reducing the need for stronger analgesics.

2. Inflammation Reduction:

• Musculoskeletal Conditions: Flurbiprofen helps reduce inflammation in various musculoskeletal conditions, such as tendonitis, bursitis, and sprains. It alleviates swelling, redness, and discomfort associated with these conditions, promoting faster recovery.
• Ocular Inflammation: It is used to reduce inflammation and pain following eye surgery or in conditions such as uveitis and conjunctivitis.

3. Fever Reduction

• Antipyretic: Flurbiprofen helps lower fever by acting on the hypothalamic heat-regulating centres, thus providing relief from fever associated with various illnesses.

4. Sore Throat Relief:

• Lozenges: it is available in the form of lozenges for the temporary relief of sore throat pain. These lozenges provide targeted relief directly to the affected area, soothing throat irritation and discomfort.

5. Other Uses:

• Menstrual Pain: It is prescribed to alleviate menstrual cramps and associated discomfort.
  Sports Injuries: In sports medicine, Flurbiprofen is used to manage pain and inflammation resulting from sports-related injuries such as strains and sprains.

Dosage and Administration

Flurbiprofen, like other NSAIDs, should be administered with careful consideration of the patient’s condition, medical history, and individual response to treatment. Here are the general guidelines for dosage and administration:

Dosage:

Adults:

• Oral Tablets: The typical dosage for adults is 50 to 100 mg taken orally, 2 to 3 times daily.
• Maximum Daily Dose: The maximum recommended daily dose is 300 mg per day, divided into multiple doses.
• Postoperative Pain: Higher initial doses may be prescribed for the management of postoperative pain, followed by maintenance doses as needed.

Elderly:

• The dosage for elderly patients should be adjusted cautiously, considering age-related changes in drug metabolism and the potential for increased susceptibility to adverse effects.

Pediatric Use:

• Flurbiprofen is not recommended for use in children under 12 years of age unless specifically prescribed by a paediatrician.

Administration

• Flurbiprofen is primarily administered orally in the form of tablets or capsules.
• For sore throat relief, Flurbiprofen lozenges can be dissolved slowly in the mouth as directed.

Timing:

• Flurbiprofen tablets should be taken with food or milk to minimize the risk of gastrointestinal side effects.
  The timing of doses depends on the condition being treated and the patient’s response to therapy.
• It is important to adhere to the prescribed dosing schedule.

Duration of Treatment:

• Flurbiprofen is typically prescribed for short-term use to relieve acute pain or inflammation.
• The duration of treatment should be limited to the shortest possible time needed to achieve therapeutic goals, considering the risks of prolonged NSAID therapy.

Flurbiprofen Side Effects

Flurbiprofen, like other NSAIDs, can cause a range of side effects, varying from mild to severe. Patients are to aware of these potential side effects and promptly report any unusual symptoms to their healthcare provider. Here are the common side effects associated with Flurbiprofen:

1. Gastrointestinal Effects:

• Nausea: Some patients experience nausea or an upset stomach after taking Flurbiprofen.
• Abdominal Pain: Abdominal discomfort, including cramping or pain, may occur, particularly if the medication is taken on an empty stomach.
• Indigestion: It irritates the lining of the stomach, leading to indigestion or dyspepsia.
• Gastric Ulcers: Long-term use of it increases the risk of developing gastric ulcers or gastrointestinal bleeding.

2. Cardiovascular Effects:

• Hypertension: It causes an increase in blood pressure, particularly in patients with pre-existing hypertension.
• Edema: Fluid retention and peripheral edema may occur as a result of sodium and water retention caused by NSAID use.
• Cardiovascular Events: Long-term use of NSAIDs increases the risk of cardiovascular events such as heart attack or stroke.

3. Renal Effects:

• Renal Impairment: NSAIDs can affect kidney function, leading to decreased urine output, fluid retention, and electrolyte imbalances.
• Acute Kidney Injury: In rare cases, NSAIDs cause acute kidney injury or exacerbate pre-existing renal conditions.

4. Hematologic Effects:

• Bleeding: Flurbiprofen and other NSAIDs can inhibit platelet function, increasing the risk of bleeding, particularly in patients taking anticoagulant medications.
• Anaemia: NSAIDs cause a decrease in haemoglobin levels, leading to anaemia, particularly in patients with underlying hematologic conditions.

5. Dermatologic Effects:

• Rash: Some patients may develop a rash or skin irritation as a reaction to Flurbiprofen.
• Photosensitivity: NSAIDs can make the skin more sensitive to sunlight, increasing the risk of sunburn or rash with sun exposure.

6. Allergic Reactions:

• Hypersensitivity: In rare cases, patients experience allergic reactions to Flurbiprofen, characterized by symptoms such as rash, itching, swelling, or difficulty breathing. Anaphylaxis is a severe allergic reaction that requires immediate medical attention.

7. Gastrointestinal Effects:

• Hepatic Dysfunction: it causes liver damage or abnormal liver function tests in some patients.
• Gastrointestinal Bleeding: NSAIDs increase the risk of gastrointestinal bleeding, which can be severe and potentially life-threatening.

Drug Interactions

Flurbiprofen may interact with other medications, including:

1. NSAIDs: Increased risk of stomach ulcers and bleeding.
2. Aspirin: Increased risk of stomach ulcers and bleeding.
3. Anticoagulants (e.g., warfarin): Increased risk of bleeding.
4. ACE inhibitors: Increased risk of kidney problems.
5. Diuretics: Increased risk of kidney problems.
6. Lithium: Increased risk of lithium toxicity.
7. Methotrexate: Increased risk of methotrexate toxicity.
8. Cyclosporine: Increased risk of kidney problems.
9. Quinolone antibiotics: Increased risk of seizures.
10. Selective serotonin reuptake inhibitors (SSRIs): Increased risk of bleeding.
11. Corticosteroids: Increased risk of stomach ulcers and bleeding.
12. Antiplatelet agents: Increased risk of bleeding.

Flurbiprofen brands in Paksitan

Here’s the list of Flurbiprofen brands in Pakistan along with their manufacturers:

1. Froben (Abbott Laboratories)
2. Flurbiprofen (Getz Pharma)
3. Ansaid (Pfizer)
4. Sanid Tablet 100mg 
5. Synalgo Tablet 100mg 
6. Inflamatix 100mg Tablet
7. BIPROFIN – Martin Dow Pharmaceuticals (Pak) Ltd.
8. BIPROTEC – Jafson Pharmaceuticals (Pvt) Ltd.
9. ENDOL – Paramount Pharmaceuticals.
10. FLAMTAB – Semos Pharmaceuticals (Pvt) Ltd.
11. FLASIC – Roomi Enterprises (Pvt) Ltd.
12. FLORIWEL – Welmark Pharmaceuticals
13. FLURBIN – Mass Pharma (Private) Limited
14. FLURBIZAN – Medizan Labs (Pvt) Ltd.
15. FLURIP – Askari Pharmaceuticals
16. FLUROFEN – Polyfine Chempharma (Pvt) Ltd.
17. FLURWIN – WNS Field Pharmaceuticals.
18. FROBEN – Abbott Laboratories (Pakistan) Limited.
19. LUBIFEN – Pharmacare Laboratories (Pvt) Ltd.
20. RANGAFEN – Hygeia Pharmaceuticals.
21. RUMAGESIC – Euro Pharma International.
22. URBOFEN – Small Laboratories (Pvt) Ltd.