Drug information of Oxaprozin

Oxaprozin

Drug group:

Oxaprozin is a nonsteroidal anti-inflammatory drug (NSAID).

Oxaprozin is used to treat pain or inflammation caused by osteoarthritis or rheumatoid arthritis in adults. Oxaprozin is also used to treat rheumatoid arthritis in children who are at least 6 years old.

Mechanism of effect

Reversibly inhibits cyclooxygenase-1 and 2 (COX-1 and 2) enzymes, which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties.

Other proposed mechanisms not fully elucidated (and possibly contributing to the anti-inflammatory effect to varying degrees) include inhibiting chemotaxis, altering lymphocyte activity, inhibiting neutrophil aggregation/activation, and decreasing proinflammatory cytokine levels.

Pharmacokinetics

Absorption

Oral: 95%

Distribution

Vd: 11 to 17 L/70 kg; distributes into synovial tissues at twice the concentration of plasma and 3 times the concentration of synovial fluid

Metabolism

Hepatic via microsomal oxidation (65%) and conjugation with glucuronic acid (35%); major conjugated metabolites are ester and ether glucuronide (inactive); small amounts of an active phenolic metabolite is produced (<5%) but has limited contribution to overall activity

Excretion

Urine (5% unchanged, 65% as metabolites); feces (35% as metabolites)

Clearance: After adjusting for body weight, no clinically important age-related differences in apparent clearance of unbound drug were identified between adult and pediatric patients ≥6 years of age

Onset of Action

Maximum effect: Due to its long half-life, several days of treatment are required for oxaprozin to reach its full effect

Time to Peak

2.4 to 3.1 hours

Half-Life Elimination

41 to 55 hours

Protein Binding

99% primarily to albumin; protein binding is saturable (nonlinear protein binding)

Drug indications

: Labeled Indications

Juvenile rheumatoid arthritis: Relief of signs and symptoms of juvenile rheumatoid arthritis (JRA).

Osteoarthritis: Relief of signs and symptoms of osteoarthritis.

Rheumatoid arthritis: Relief of signs and symptoms of rheumatoid arthritis.

Dosage

Usual Adult Dose for Osteoarthritis

Loading dose: 1200 mg to 1800 mg orally; not to exceed 26 mg/kg
Maintenance dose: 1200 mg orally once a day
Maximum dose: 1800 mg or 26 mg/kg orally per day, whichever is less, in divided doses

Comments:
-A one-time loading dose may be given if quick onset of action is needed.
-Doses larger than 1200 mg orally per day on a chronic basis are reserved for patients weighing more than 50 kg, with normal renal and hepatic function, at low risk for peptic ulcer, and whose disease severity justifies maximal therapy.
-Once response to therapy is determined, dose and frequency should be adjusted to the lowest effective dose for the shortest duration possible to suit the individual patient's treatment goals.

Uses: For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis

Usual Adult Dose for Rheumatoid Arthritis

Loading dose: 1200 mg to 1800 mg orally; not to exceed 26 mg/kg
Maintenance dose: 1200 mg orally once a day
Maximum dose: 1800 mg or 26 mg/kg orally per day, whichever is less, in divided doses

Usual Pediatric Dose for Juvenile Rheumatoid Arthritis

6 to 16 years:

22 to 31 kg: 600 mg orally once a day
32 to 54 kg: 900 mg orally once a day
55 kg or greater: 1200 mg orally once a day
Maximum dose: 1200 mg orally per day

Comments:
-Once response to therapy is determined, dose and frequency should be adjusted to the lowest effective dose for the shortest duration possible to suit the individual patient's treatment goals.

Use: For the relief of signs and symptoms of juvenile rheumatoid arthritis

Usual Pediatric Dose for Osteoarthritis

17 to 18 years:
1200 mg orally once a day
Maximum dose: 1200 mg orally per day

Comment:
-Once response to therapy is determined, dose and frequency should be adjusted to the lowest effective dose for the shortest duration possible to suit the individual patient's treatment goals.

Uses: For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis

Usual Pediatric Dose for Rheumatoid Arthritis

17 to 18 years:
1200 mg orally once a day
Maximum dose: 1200 mg orally per day

Comment:
-Once response to therapy is determined, dose and frequency should be adjusted to the lowest effective dose for the shortest duration possible to suit the individual patient's treatment goals.

Uses: For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis

Drug contraindications

Hypersensitivity to oxaprozin or any component of the formulation; history of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs; in the setting of coronary artery bypass graft (CABG) surgery

Side effects

Side effects requiring immediate medical attention

Along with its needed effects, oxaprozin may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking oxaprozin:

More common

  • Skin rash

Less common

  • Bloating
  • bloody or black, tarry stools
  • burning upper abdominal or stomach pain
  • burning while urinating
  • cloudy urine
  • constipation
  • decrease in urine output or decrease in urine-concentrating ability
  • diarrhea
  • difficult or painful urination
  • frequent urination
  • headache
  • heartburn
  • indigestion
  • itching skin
  • loss of appetite
  • nauseaor vomiting
  • pale skin
  • severe abdominal or stomach pain, cramping, or burning
  • severe and continuing nausea
  • swelling
  • troubled breathing with exertion
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • vomiting of blood or material that looks like coffee grounds
  • weight loss

Rare

  • Agitation
  • bleeding gums
  • blistering, peeling, or loosening of the skin
  • blurred vision
  • body aches or pain
  • burning feeling in chest or stomach
  • changes in blood pressure
  • chest pain
  • clay-colored stools
  • coma
  • confusion
  • cough or hoarseness
  • cracks in the skin
  • dark urine
  • depression
  • difficult or labored breathing
  • difficulty swallowing
  • dilated neck veins
  • dizziness
  • ear congestion
  • extreme fatigue
  • fainting
  • feeling of discomfort
  • fever or chills
  • fluid-filled skin blisters
  • high fever
  • hivesor welts
  • hostility
  • increased sensitivity of the skin to sunlight
  • increased thirst
  • increased volume of pale, dilute urine
  • inflammation of the joints
  • irregular, fast or slow, or shallow breathing
  • joint or muscle pain
  • large, flat, blue or purplish patches in the skin
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • lethargy
  • light-colored stools
  • lightheadedness
  • loss of heat from the body
  • loss of voice
  • lower back or side pain
  • muscle aches
  • muscle twitching
  • noisy breathing
  • pain or burning in the throat
  • pain or tenderness around the eyes and cheekbones
  • pale or blue lips, fingernails, or skin
  • pinpoint red or purple spots on the skin
  • pounding in the ears
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • rapid weight gain
  • red skin lesions, often with a purple center
  • red, irritated eyes
  • redness or other discoloration of the skin
  • redness, swelling, or soreness of tongue
  • scaly skin
  • seizures
  • severe sunburn
  • skin thinness
  • slow, fast, irregular, pounding, or racing heartbeat or pulse
  • sneezing
  • sore throat
  • sores, ulcers, or white spots on the lips or tongue or inside the mouth
  • stuffy or runny nose
  • stupor
  • swelling of the face, fingers, feet, or lower legs
  • swelling or inflammation of the mouth
  • swollen lymph glands
  • tenderness in the stomach area
  • tightness in the chest
  • unpleasant breath odor
  • upper right abdominal or stomach pain
  • yellow eyes or skin

Side effects not requiring immediate medical attention

Some side effects of oxaprozin may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Acid or sour stomach
  • belching
  • stomach discomfort

Less common

  • Continuing ringing or buzzing or other unexplained noise in the ears
  • excess air or gas in the stomach or intestines
  • hearing loss
  • passing gas
  • relaxed and calm
  • sleepiness or unusual drowsiness
  • trouble sleeping

Rare

  • Burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • burning, dry, or itching eyes
  • change in taste
  • decreased hearing
  • discharge, excessive tearing
  • dry mouth
  • feeling of constant movement of self or surroundings
  • general feeling of discomfort or illness
  • lack or loss of strength
  • redness, pain, swelling of the eye, eyelid, or inner lining of the eyelid
  • sensation of spinning
  • shakiness in the legs, arms, hands, feet
  • trembling or shaking of the hands or feet

 

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Alerts

Cardiovascular thrombotic events:

Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction (MI) and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use.

Oxaprozin is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.

Gastrointestinal bleeding, ulceration, and perforation:

NSAIDs cause an increased risk of serious gastrointestinal (GI) adverse events, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. These events can occur at any time during use and without warning symptoms. Elderly patients and patients with a prior history of peptic ulcer disease and/or GI bleeding are at a greater risk for serious GI events.

Points of recommendation

Oxaprozin can increase your risk of fatal heart attack or stroke, even if you don't have any risk factors. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG).

Oxaprozin may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using oxaprozin, especially in older adults.

You should not use oxaprozin if you are allergic to it, or if you have:

  • active bleeding in your stomach or intestines; or
  • a history of asthmaattack or severe allergic reaction after taking aspirin or an NSAID.

Tell your doctor if you have ever had:

  • heart disease, high blood pressurehigh cholesterol, diabetes, or if you smoke;
  • a heart attack, stroke, or blood clot;
  • stomach ulcers or bleeding;
  • asthma;
  • liver or kidney disease; or
  • fluid HYPERLINK 

Taking oxaprozin during the last 3 months of pregnancy may harm the unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It may not be safe to breastfeed while using this medicine. Ask your doctor about any risk.

Oxaprozin is not approved for use by anyone younger than 6 years old.

Follow all directions on your prescription label and read all medication guides. Your doctor may occasionally change your dose. Use the lowest dose that is effective in treating your condition.

Oxaprozin doses are based on weight (especially in children and teenagers). Your dose needs may change if you gain or lose weight.

If you use oxaprozin long-term, you may need frequent medical tests.

Store oxaprozin at room temperature, away from moisture, heat, and light. Keep the bottle tightly closed when not in use.

Avoid alcohol. Heavy drinking can increase your risk of stomach bleeding.

Avoid taking aspirin while you are taking oxaprozin.

Ask a doctor or pharmacist before using other medicines for pain, fever, swelling, or cold/flu symptoms. They may contain ingredients similar to oxaprozin (such as aspirin, ibuprofenketoprofen, or naproxen).

Oxaprozin could make you sunburn more easily. Avoid sunlight or tanning beds. Wear protective clothing and use sunscreen (SPF 30 or higher) when you are outdoors.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°C). Protect from light; keep bottle tightly closed.

 

Pregnancy level

HAVE NOT BEEN ESTABLISHED

US FDA pregnancy category: Not assigned.

Risk Summary: Use of nonsteroidal anti-inflammatory drugs (NSAIDs) during the third trimester of pregnancy increases the risk of premature closure of the fetal ductus arteriosus.

Comments:
-Avoid use during third trimester as it may cause premature closure of the ductus arteriosus.
-Not recommended in women attempting to conceive as may impair female fertility.

Breast feeding warning

A decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.

Excreted into human milk: Unknown
Excreted into animal milk: Yes

Comments: The effects in the nursing infant are unknown.

Due to lack of published clinical experience during breastfeeding, other agents may be preferred.

Related drugs

Sulindac , Azapropazone

Drug forms

Daypro

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