Oxaprozin

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Introduction

Generic Name: Oxaprozin
Brand Names: Daypro®
Chemical Formula: C15H11NO3

Oxaprozin is a nonsteroidal anti-inflammatory drug (NSAID) that belongs to the propionic acid class of NSAIDs, similar to ibuprofen and naproxen. It is generally prescribed to treat the pain and inflammation in conditions like arthritis. The drug’s primary mechanism of action is to inhibit the production of prostaglandins, the lipidic chemicals that mediate pain and inflammation in the body. Oxaprozin is has a its long duration of action, which makes it possible for once daily dosage which is favorable for patients managing chronic pain and inflammation.

Uses

Oxaprozin is indicated for various conditions which are primarily related to musculoskeletal pain and inflammation.

  1. Osteoarthritis:
    Oxaprozin is commonly prescribed for osteoarthritis, a condition in which the cartilage in joints wears down, leading to pain, inflammation and decreased mobility. This drug helps to reduce the chronic pain associated with joint stiffness, making it helpful for patients to maintain mobility.
  2. Rheumatoid Arthritis:
    In patients having rheumatoid arthritis, Oxaprozin is used to decrease the joint inflammation and stiffness. By controlling this inflammation, it helps to the improve function of joints and delays the progression of damage in the joints.
  3. Juvenile Rheumatoid Arthritis (JRA):
    Oxaprozin is also approved for use in children aged 6 and older for the treatment of juvenile rheumatoid arthritis. It provides relief from the chronic inflammation that affects joints and helps manage pain in younger patients.
  4. Ankylosing Spondilitis: Oxaprozin has been shown to effectively manage the pain in ankylosing spondilitis as per some case studies.
  5. Other Painful Conditions:
    Although this drug is mostly used for arthritis, Oxaprozin may also be prescribed for other pain and inflammation related conditions, such as tendinitis, bursitis, and generalized musculoskeletal pain.

Dosage

The dosing for Oxaprozin varies depending on the individual factors such as the patient’s age, weight, and also the condition being treated.

Adults:

  • The usual initial dose for adults with osteoarthritis or rheumatoid arthritis is 1,200 mg once daily.
  • Some patients may also require a higher dose initially, but the maximum recommended dose is 1,800 mg/day, it should not be exceeded.

Children (6 years and older):

  • The recommended starting dose for children with juvenile rheumatoid arthritis is 20 mg/kg/day. However it being a NSAID, the lowest possible dose should be given.

For geriatric patients, the dose should be carefully adjusted according to individual conditions due to the increased risk of gastrointestinal and renal side effects.

Mechanism of Action

Like most of the NSAIDs, oxaprozin works by inhibiting the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which play a crucial role in prostaglandin synthesis. Prostaglandins are the lipidic compounds that play a role in inflammation, pain, and fever. By inhibiting the COX enzymes, this drug reduces the levels of prostaglandins in the body, thereby controlling inflammation and giving pain relief.

One of the important advantages of oxaprozin over other NSAIDs is its long half-life, which allows for sustained effect with once a day dosing.

Pharmacokinetics

Oxaprozin is rapidly absorbed after oral administration, and its peak plasma concentrations is reached within 3 to 6 hours. It has an long half-life of approximately 40-60 hours, which allows it to provide a sustained therapeutic action .

Oxaprozin is highly bound to plasma proteins, and only a small percentage remaining in free form. This drug undergoes metabolism in the liver and is excreted primarily via the kidneys.

Side Effects

As with other NSAIDs, Oxaprozin may cause side effects in some individuals, especially with prolonged use. These side effects can range from mild to severe, depending on the patient’s health status and the duration of therapy.

Common Side Effects:

Here are a few of the common side effects of this drug.

  • Nausea
  • Vomiting
  • Indigestion
  • Dizziness
  • Skin rash
  • Headache

Serious Side Effects:

Here are some of the serious side effects:

  • Gastrointestinal Issues: Long-term use of this drug can lead to an increase in the risk of ulcers, bleeding, or perforation of the stomach or intestines. This risk is greater in patients with a history of ulcers or gastrointestinal bleeding.
  • Cardiovascular Risks: Like other NSAIDs, Oxaprozin may increase the risk of serious cardiovascular events, such as heart attacks and strokes, especially when used for long term or in patients with pre-existing heart and related conditions.
  • Renal Impairment: Oxaprozin may affect kidney function, especially in individuals who have existing kidney problems. The risk of renal damage is also higher in elderly patients.
  • Hepatotoxicity: In rare cases, this drug can cause liver damage, the liver enzymes may be elevated or there can be liver failure.

Patients should seek immediate medical attention if they experience symptoms such as severe abdominal pain, tarry stools (a sign of gastrointestinal bleeding), or signs of liver damage, such as jaundice.

Contraindications

Oxaprozin is contraindicated in certain patient populations, including:

  • Patients with a history of gastrointestinal bleeding, ulcers or GIT disorders.
  • Individuals with severe kidney or liver impairment.
  • People who are allergic to Oxaprozin or other NSAIDs.
  • Patients with a history of cardiovascular conditions, including recent heart attack or stroke.
  • Pregnant women in their third trimester of pregnancy, as Oxaprozin may cause harm to the fetus.

Drug Interactions

Like other NSAIDs, Oxaprozin can interact with a various medications, which may lead to increased risk of side effects or decrease in its efficacy. Some of the significant drug interactions include:

  • Anticoagulants (e.g., warfarin): Increased risk of bleeding.
  • ACE Inhibitors and ARBs: Reduced antihypertensive effect.
  • Diuretics: Increased risk of nephrotoxicity.
  • Corticosteroids: Increased risk of gastrointestinal ulcers or bleeding.
  • SSRIs (Selective Serotonin Reuptake Inhibitors): Increased risk of gastrointestinal bleeding.

Patients should always inform their healthcare provider about all the medications, supplements, allergies and over-the-counter drugs they are taking before starting Oxaprozin.

Special Considerations

1. Pregnancy and Lactation

  • Oxaprozin is not recommended during the third trimester of pregnancy due to the risk of fetal harm, particularly the premature closure of the ductus arteriosus.
  • This drug is excreted in small amounts in breast milk, so while short-term use may be considered safe during breastfeeding, prolonged use is not recommended. The patient should always seek the advice of healthcare professional in such cases.

2. Elderly Patients

  • Elderly patients are at a higher risk of gastrointestinal, renal, and cardiovascular side effects of this drug. There should be regular monitoring of kidney and liver function especially during prolonged therapy.

Warnings and Precautions

Gastrointestinal Risks:

  • As with other NSAIDs, the long-term use of Oxaprozin increases the risk of gastrointestinal bleeding, ulcers, and perforation of the stomach or intestines. These risks are elevated in elderly patients and in patients with a history of peptic ulcer disease, gastrointestinal bleeding or in those with inflammatory GI diseases.

Cardiovascular Risks:

    • Prolonged use of Oxaprozin, particularly at high doses, has been associated with an increased risk of heart attacks and strokes. Patients with pre-existing cardiovascular conditions or suffering from other heart related diseases should use Oxaprozin with caution and only under medical supervision.

    Renal Function:

      • Oxaprozin can impair kidney function, particularly in individuals with pre-existing renal conditions. Regular monitoring of the renal function is recommended for patients who are on a long term therapy of this medication.

      Liver Function:

        • Hepatotoxicity is a rare but possible side effect of Oxaprozin. Liver function should be monitored periodically in patients who are undergoing long-term treatment.

        Allergic Reactions:

          • Oxaprozin may cause allergic reactions in some individuals, particularly those who are allergic to NSAIDs and those who are asthmatic or have other allergic conditions. Seek prompt medical attention if you experience symptoms such as rash on the body, difficulty breathing, or swelling of the face and throat.

          Additional Information

          • Take Oxaprozin with food or milk to reduce the gastrointestinal discomfort.
          • Avoid alcohol consumption while on Oxaprozin therapy, as this can increase the risk of gastrointestinal bleeding.
          • Watch out for the symptoms of serious side effects, such as tarry stools, severe abdominal pain, or signs of liver damage (e.g., yellowing of the skin or eyes) and seek medical attention without any delay.
          • Consult doctor before using any over-the-counter medications, particularly other NSAIDs, as this can increase the risk of adverse effects.

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