Table of Contents
Introduction
Generic Name: Loxoprofen Brand Names: Loxonin®,Loxomac®,Roxonin® Chemical Formula: C₁₅H₁₁NaO₃
Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) used for pain relief and reducing the inflammation. It belongs to the propionic acid derivatives class of NSAIDs, similar to ibuprofen and naproxen. This drug is widely prescribed in Japan and other parts of Asia, loxoprofen is efficacious and has relatively lower gastrointestinal side effects in comparison to other NSAIDs. Loxoprofen works by inhibiting the activity of cyclooxygenase (COX) enzymes, resulting in the reduced production of prostaglandins, which are responsible for inflammation, pain, and fever.
Uses
- Pain Management
Loxoprofen is used for the relief from mild to moderate pain, such as headaches, toothaches, and muscle pain. - Rheumatoid Arthritis and Osteoarthritis
It is usually prescribed to reduce the intensity of joint pain, stiffness, and inflammation in patients with chronic inflammatory diseases like rheumatoid arthritis and osteoarthritis. - Postoperative Pain
This drug is often administered for managing pain after surgery or injury. - Menstrual Pain
Women may be prescribed this drug to decrease the pain associated with dysmenorrhea. - Fever
This drug is also used to reduce fever in patients with infections or other febrile illnesses where fever is present as a symptom.
Dosage
Loxoprofen is available in both oral tablet and topical formulations.
- Oral Tablets: For pain relief and inflammation, the usual adult dose is 60 mg, taken three times daily after meals. The maximum daily dose should not exceed the total of 180 mg.
- Topical Gel/Patch: Loxoprofen is also available as a transdermal patch or gel which is applied to the affected area, to treat localized pain, such as muscle or joint injuries.
The dosage of this drug may vary based on the patient’s condition and the physician’s recommendations. Please note that the prescribed dosage must be followed and a healthcare professional should be consulted before adjusting the dose.
Mechanism of Action
Loxoprofen is a prodrug, meaning it becomes active only after metabolism in the body. When it is converted to its active metabolite, trans-alcohol form, it exerts its action by inhibiting the COX enzymes, primarily COX-1 and COX-2, which are responsible for prostaglandin synthesis. Prostaglandins are compounds that promote the inflammation, pain, and fever, and by reducing their levels, this drug like most NSAIDs reduces these symptoms. Its topical formulation results in fewer gastrointestinal side effects.
Side Effects
While loxoprofen is generally considered safer for the gastrointestinal tract than other NSAIDs, it may still cause side effects, especially with long-term use or in people who are sensitive to NSAIDs. Here are a few side effects of this drug:
- Common Side Effects:
- Nausea
- Indigestion
- Drowsiness
- Rash
- Serious Side Effects:
- Gastrointestinal bleeding or ulcerations
- Kidney dysfunction
- Elevations Liver enzyme
- Anemia
Contraindications
Loxoprofen should not be used by individuals with certain medical conditions given below:
- Individuals with a history of gastrointestinal ulcers or GIT bleeding
- Severe heart failure or cardiovascular diseases
- Severe liver or kidney impairment or conditions
- Allergy to loxoprofen or other NSAIDs
Patients should discuss their full medical history with their healthcare provider before taking loxoprofen to avoid any adverse effects of the medication.
Drug Interactions
Like other NSAIDs, loxoprofen may interact with a variety of medications, here are a few interactions:
- Anticoagulants (e.g., Warfarin): Increased risk of bleeding if administered together.
- ACE Inhibitors : Reduced antihypertensive effects.
- Corticosteroids: There is an increased risk of gastrointestinal side effects.
- Other NSAIDs: There is an increased risk of kidney damage and gastrointestinal bleeding.
It is however most important to consult a healthcare provider before combining loxoprofen with any other medications.
Warnings and Precautions
- Gastrointestinal Risks
Although loxoprofen is possibly less likely to cause gastric irritation compared to other NSAIDs, it can still lead to ulcers and gastrointestinal bleeding, particularly with long-term use and in people with sensitivity to NSAIDs . - Renal and Hepatic Function
Patients with pre-existing kidney or liver disease should be alert when taking loxoprofen, as it can cause further worsening of the existing conditions. - Cardiovascular Risks
Long-term use of loxoprofen may lead to rise in the risk of cardiovascular events, such as heart attacks and strokes, especially in patients with a history of heart disease. - Pregnancy and Breastfeeding
Loxoprofen must be avoided in the third trimester of pregnancy due to the risk of harm to the fetus. It is also not recommended for administration while breastfeeding as it may pass into breast milk.
Patient Education
Patients using loxoprofen should be advised on the following:
- Take After Meals/Food: Loxoprofen should generally be taken after meals to reduce the risk of gastrointestinal irritation.
- Avoid Alcohol: Alcohol can increase the chances of having stomach ulcers or gastrointestinal bleeding while taking loxoprofen.
- Contact Healthcare Provider: It is imperative that the patients should immediately report any symptoms of gastrointestinal bleeding, such as black, tarry stools, or severe abdominal pain and cramps after taking this drug.
Special Considerations for Elderly Patients
The elderly population is more susceptible to the side effects of NSAIDs, particularly the effects related to gastrointestinal bleeding or discomfort and kidney impairment. Effective lower doses are generally given to older adults to mitigate these risks.
Loxoprofen is an effective NSAID for managing pain and inflammation with a relatively better gastrointestinal tolerability compared to other drugs in its class.