Optiprofen

Uses

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

Optiprofen is used for:

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

Optiprofen 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 Optiprofen 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. Optiprofen 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

Optiprofen dosage

After observing the response to initial therapy with Optiprofen , 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 Optiprofen 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. Optiprofen 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.

Optiprofen 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.

Optiprofen 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.

[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.

Optiprofen Drug Interaction

Moderate: duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acidsUnknown: cyclobenzaprine, cyclobenzaprine, fluticasone nasal, fluticasone nasal, pregabalin, pregabalin, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, alprazolam, alprazolam

Optiprofen Disease Interaction

Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition

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

Optiprofen 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

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