Flurbiprofene

Flurbiprofene Uses, Dosage, Side Effects, Food Interaction and all others data.

Flurbiprofene inhibits prostaglandin synthesis by decreasing the activity of cyclooxygenase resulting in reduced prostaglandin levels. It is also a potent inhibitor of platelet aggregation.

Flurbiprofene, a nonsteroidal anti-inflammatory agent (NSAIA) of the propionic acid class, is structually and pharmacologically related to fenoprofen, ibuprofen, and ketoprofen, and has similar pharmacological actions to other prototypica NSAIAs. Flurbiprofene exhibits antiinflammatory, analgesic, and antipyretic activities. The commercially available flurbiprofen is a racemic mixture of (+)S- and (-) R-enantiomers. The S-enantiomer appears to possess most of the anti-inflammatory, while both enantiomers may possess analgesic activity.

Trade Name Flurbiprofene
Availability Prescription only
Generic Flurbiprofen
Flurbiprofen Other Names Flurbiprofen, Flurbiprofene, Flurbiprofeno, Flurbiprofenum
Related Drugs Humira, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam, duloxetine, cyclobenzaprine
Weight 0.03%w/v
Type Eye Drops
Formula C15H13FO2
Weight Average: 244.2609
Monoisotopic: 244.089957865
Protein binding

> 99% bound, primarily to albumin. Binds to a different primary binding site on albumin than anticoagulants, sulfonamides and phenytoin.

Groups Approved, Investigational
Therapeutic Class Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Manufacturer Micro Labs Limited
Available Country India, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Flurbiprofene
Flurbiprofene

Uses

Carefully consider the potential benefits and risks of Flurbiprofene and other treatment options before deciding to use Flurbiprofene . Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.

Flurbiprofene is used for:

  • For relief of the signs and symptoms of rheumatoid arthritis.
  • For relief of the signs and symptoms of osteoarthritis.

Flurbiprofene is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Back Pain, Acute, Chronic Back Pain, Menstrual Distress (Dysmenorrhea), Muscle Spasms, Non-Articular Rheumatic Muscle Spasms, Osteoarthritis (OA), Pain, Pain, Inflammatory, Post-traumatic pain, Postoperative pain, Rheumatoid Arthritis, Spinal pain

How Flurbiprofene works

Similar to other NSAIAs, the anti-inflammatory effect of flurbiprofen occurs via reversible inhibition of cyclooxygenase (COX), the enzyme responsible for the conversion of arachidonic acid to prostaglandin G2 (PGG2) and PGG2 to prostaglandin H2 (PGH2) in the prostaglandin synthesis pathway. This effectively decreases the concentration of prostaglandins involved in inflammation, pain, swelling and fever. Flurbiprofene is a non-selective COX inhibitor and inhibits the activity of both COX-1 and -2. It is also one of the most potent NSAIAs in terms of prostaglandin inhibitory activity.

Dosage

Flurbiprofene dosage

After observing the response to initial therapy with Flurbiprofene , the dose and frequency should be adjusted to suit an individual patient's needs. For relief of the signs and symptoms of rheumatoid arthritis or osteoarthritis, the recommended starting dose of Flurbiprofene is 200 to 300 mg per day, divided for administration two, three, or four times a day. The largest recommended single dose in a multiple-dose daily regimen is 100 mg.

Side Effects

Oedema, abdominal pain, constipation, diarrhoea, dyspepsia/heartburn, liver enzyme elevations, flatulence, nausea, vomiting, wt change, headache, nervousness, CNS stimulation (e.g. anxiety), CNS inhibition (e.g. somnolence), rhinitis, vision changes, dizziness/vertigo, tinnitus, signs and symptoms of UTI, rash. Ocular hyperaemia, eye irritation, fibrosis, miosis, mydriasis.

Toxicity

LD50=10 mg/kg (orally in dogs).

Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of flurbiprofen. Flurbiprofene may increase blood pressure and/or cause fluid retention and edema. Use caution in patients with fluid retention or heart failure. Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Anaphylactoid and serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) may occur. Common adverse events include abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI bleeding, GI perforation, nausea, peptic ulcer, vomiting, renal function abnormalities, anemia, dizziness, edema, liver function test abnormalities, headache, prolonged bleeding time, pruritus, rash, tinnitus. Although rarely documented in the case of flurbiprofen, oral propionic acid derivatives have been associated with a relatively high frequency of allergic reactions.

Precaution

Patients with known CV disease or risk factors for CV disease, fluid retention. Hepatic and renal impairment. Lactation.

Interaction

Reduced antihypertensive effect of ACE inhibitors, angiotensin II receptor antagonists and β-blockers. Slight reduction in blood glucose concentration in patients with DM receiving certain antidiabetic agents (e.g. glyburide, metformin). Reduced diuretic effect of furosemide and thiazides. May increase toxicity of lithium and methotrexate. May increase risk of bleeding with antiplatelets, anticoagulants, SSRIs, corticosteroids.

Food Interaction

  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Flurbiprofene Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.



Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Flurbiprofene Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

Hypertension interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Volume of Distribution

  • 14 L [Normal Healthy Adults]
  • 12 L [Geriatric Arthritis Patients]
  • 10 L [End Stage Renal Disease Patients]
  • 14 L [Alcoholic Cirrhosis Patients]
  • 0.12 L/kg

Elimination Route

Fluribiprofen is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are reached 0.5 - 4 hours after oral administration.

Half Life

R-flurbiprofen, 4.7 hours; S-flurbiprofen, 5.7 hours

Elimination Route

Flurbiprofene is poorly excreted into human milk. Following dosing with flurbiprofen, less than 3% of flurbiprofen is excreted unchanged in the urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Renal elimination is a significant pathway of elimination of flurbiprofen metabolites.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Contraindication

Known hypersensitivity to flurbiprofen, history of asthma, urticaria, or allergic-type reactions precipitated by aspirin or other NSAIDs, NSAID-related history of GI bleeding or perforation, treatment of perioperative pain in the setting of CABG surgery. Pregnancy (3rd trimester) and lactation.

Acute Overdose

Symptoms: Headache, nausea, vomiting, epigastric pain, GI bleeding, diarrhoea, disorientation, excitation, coma, drowsiness, dizziness, tinnitus, fainting and occasionally convulsions, acute renal failure and liver damage.

Management: Supportive and symptomatic treatment. Admin activated charcoal w/in 1 hr after ingestion. In adults, gastric lavage should be considered.

Storage Condition

Store between 15-25° C.

Innovators Monograph

You find simplified version here Flurbiprofene

Flurbiprofene contains Flurbiprofen see full prescribing information from innovator Flurbiprofene Monograph, Flurbiprofene MSDS, Flurbiprofene FDA label

FAQ

What is Flurbiprofene used for?

Flurbiprofene is a nonsteroidal anti-inflammatory drug used to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. It is primarily indicated as a pre-operative anti-miotic as well as orally for arthritis.

How safe is Flurbiprofene?

Flurbiprofene can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease. Do not use this medicine just before or after heart bypass surgery.

How does Flurbiprofene work?

Flurbiprofene works by blocking the effect of chemicals in your body, called cyclo-oxygenase enzymes. These enzymes help to make other chemicals in the body, called prostaglandins. Some prostaglandins are produced at sites of injury or damage, and cause pain and inflammation.

What are the common side effects of Flurbiprofene?

Common side effects of Flurbiprofene are include: Upset stomach, constipation, diarrhea, gas, heartburn, nausea, vomiting, dizziness, drowsiness, or headache may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Is Flurbiprofene safe during pregnancy?

Flurbiprofene is contraindicated during the last trimester of pregnancy. Undesirable effects may be minimised by using the lowest effective dose for the shortest duration necessary to control symptoms.

Is Flurbiprofene safe during breastfeeding?

Because of the low levels of Flurbiprofene in breastmilk and its short half-life it is unlikely to adversely affect the breastfed infant, especially if the infant is older than 2 months. Maternal use of Flurbiprofene eye drops would not be expected to cause any adverse effects in breastfed infants.

Can I drink alcohol with Flurbiprofene?

Do not drink alcohol while taking Flurbiprofene. Alcohol can increase your risk of stomach bleeding caused by Flurbiprofene.

Can I drive after taking Flurbiprofene?

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you.

How quickly does Flurbiprofene work?

Flurbiprofene usually begins to work within one week, but in severe cases up to two weeks or even longer may pass before you begin to feel better.

When should be taken of Flurbiprofene?

You may take your doses before meals, it is better to take your doses with a snack or just after eating a meal.

How often can I take Flurbiprofene?

Flurbiprofene usually is taken two to four times a day. Take Flurbiprofene at around the same times every day.

How long does Flurbiprofene take Flurbiprofene to work?

Flurbiprofene usually begins to work within one week, but in severe cases up to two weeks or even longer may pass before you begin to feel better.

When should not take Flurbiprofene?

Flurbiprofene can increase your risk of fatal heart attack or stroke. Do not use Flurbiprofene just before or after heart bypass surgery. Flurbiprofene may also cause stomach or intestinal bleeding, which can be fatal.

Who should not take Flurbiprofene?

If you will be undergoing a coronary artery bypass graft, you should not take Flurbiprofene right before or right after the surgery.

Is Flurbiprofene safe for heart patients?

Flurbiprofene can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease.

How long does Flurbiprofene stay in my system?

After taking your last dose of Flurbiprofene it should be out of your system within 93.5 hours. Flurbiprofene has an elimination half life of 12 to 17 hours.

What happens if I miss a dose?

If you miss a dose of Flurbiprofene, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Can I take overdose of Flurbiprofene?

Flurbiprofene overdoses may be accidental or intentional. If you've taken more than the recommended amount of Flurbiprofene or enough to have a harmful effect on your body's functions, you have overdosed. An overdose can lead to serious medical complications, including death.

Will Flurbiprofene affect my fertility?

The occasional Flurbiprofene is unlikely to cause fertility problems, but it's probably best to avoid it when possible.

Can Flurbiprofene affects my kidney?

Using this Flurbiprofene long term can cause kidney damage. Seniors are at increased risk for this damage.

Can Flurbiprofene affects my liver?

Flurbiprofene  has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.

*** Taking medicines without doctor's advice can cause long-term problems.
Share