Oxaprozen

Uses

Oxaprozen is used for:

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

Oxaprozen is also used to associated treatment for these conditions: Osteoarthritis (OA), Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile

How Oxaprozen works

Anti-inflammatory effects of Oxaprozen are believed to be due to inhibition of cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Oxaprozen is a non-selective NSAID, with a cell assay system showing lower COX-2 selectivity implying higher COX-1 selectivity.

Dosage

Oxaprozen dosage

General Dosing Instructions: Carefully consider the potential benefits and risks ofOxaprozen and other treatment options before deciding to use Oxaprozen. Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals. After observing the response to initial therapy with Oxaprozen, the dose and frequency should be adjusted to suit an individual patient’s needs.

Divided doses may be tried in patients unable to tolerate single doses. For osteoarthritis patients of low body weight or with milder disease, an initial dose of one 600 mg tablet once a day may be appropriate. The maximum total daily dose is 1200 mg.

Osteoarthritis: For Osteoarthritis, the dosage is 1200 mg (two 600 mg tablets) given orally once a day.

Rheumatoid Arthritis: For Rheumatoid Arthritis, the dosage is 1200 mg (two 600 mg tablets) given orally once a day.

Side Effects

Common side effects are depression, sedation, somnolence, confusion, disturbance of sleep, weakness, malaise; rash, prutitus, urticaria, photosensitivity; abdominal pain/distress, anorexia, flatulence, vomiting, constipation, diarrhoea, dyspepsia, nausea, peptic ulcer and/or GI bleeding, abnormalities in LFTs, stomatitis, haemorrhoidal or rectal bleeding; tinnitus; dysuria or frequency; oedema, BP changes; haematuria, renal insufficiency, decreased menstrual flow; anaemia, thrombocytopenia, leukopenia, ecchymoses; wt gain/loss; blurred vision, conjunctivitis.

The following adverse reactions may occur:

• Cardiovascular Thrombotic Events
• GI Bleeding, Ulceration and Perforation
• Hepatotoxicity
• Hypertension
• Heart Failure and Edema
• Renal Toxicity and Hyperkalemia
• Anaphylactic Reactions
• Serious Skin Reactions
• Hematologic Toxicity

Toxicity

Oral, mouse: LD₅₀ = 1210 mg/kg; Oral, rabbit: LD₅₀ = 172 mg/kg; Oral, rat: LD₅₀ = 4470 mg/kg

Precaution

Be alert for ulceration and bleeding in patients treated chronically. History of serious GI events, alcoholism, smoking, other factors known to be associated with peptic ulcer. Elderly or debilitated patients. Uncompensated cardiac failure, history of hypertension, cardiac decompensation, chronic diuretic therapy, conditions predisposing to fluid retention. Renal and hepatic impairment. Underlying coagulation defects or patients who are undergoing surgical procedures where a high degree of haemostasis is required. Pregnancy (avoid in 3rd trimester) and lactation.

Interaction

Increased risk of salicylate toxicity with aspirin. May increase effects of oral anticoagulants. May reduce effects of β-blockers, diuretics and other antihypertensive agents. May increase risk of methotrexate and lithium toxicity.

Food Interaction

• Take with food. Take once daily after breakfast. Food decreases the rate but not the extent of absorption.

Oxaprozen 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.

Oxaprozen 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.

Oxaprozen Drug Interaction

Moderate: duloxetine, omega-3 polyunsaturated fatty acids, metoprolol, metoprololUnknown: zolpidem, rosuvastatin, cyclobenzaprine, fluticasone nasal, atorvastatin, pregabalin, esomeprazole, acetaminophen / hydrocodone, albuterol, montelukast, levothyroxine, cyanocobalamin, ascorbic acid, cholecalciferol, bupropion, alprazolam

Oxaprozen Disease Interaction

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

Volume of Distribution

• 11 to 17 L/70 kg

Elimination Route

Oxaprozen is 95% absorbed after oral administration. Food may reduce the rate of absorption of oxaprozin, but the extent of absorption is unchanged. Antacids do not significantly affect the extent and rate of oxaprozin absorption.

Half Life

54.9 hours

Elimination Route

Oxaprozen is expected to be excreted in human milk based on its physical-chemical properties; however, the amount of oxaprozin excreted in breast milk has not been evaluated. Approximately 95% of oxaprozin is metabolized by the liver. Approximately 5% of the oxaprozin dose is excreted unchanged in the urine. Sixty-five percent (65%) of the dose is excreted in the urine and 35% in the feces as metabolite. Biliary excretion of unchanged oxaprozin is a minor pathway. Several oxaprozin metabolites have been identified in human urine or feces.

Pregnancy & Breastfeeding use

Pregnancy categaory: C, D (in 3rd trimester or near delivery)

Contraindication

Previous or active peptic ulceration, known hypersensitivity to NSAIDs. Perioperative pain in CABG setting.

Special Warning

Renal Impairment-

Osteoarthritis: Severe or on dialysis: 600 mg once daily. Increase to 1.2 g daily if needed.

Rheumatoid arthritis: Severe or on dialysis: 600 mg once daily. Increase to 1.2 g daily if needed.

Acute Overdose

Symptoms: Acute renal failure, vomiting, drowsiness, leukocytosis.

Management: Supportive and symptomatic. Multiple admin of charcoal may be required to reduce potential for delayed toxicities.

Storage Condition

Store at 25° C. Protect from light.

Innovators Monograph

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