Loxoprofen 60mg is primarily composed of Loxoprofen sodium 60mg along with other excipients. The medication is indicated for the treatment of pain relief and inflammation in conditions such as chronic rheumatoid arthritis, osteoarthritis, Periarthritis Humeroscapularis, and more. Additionally, it is used to alleviate mild to moderate pain or to treat muscle pain, neuralgia, and similar conditions.
1. Mechanism of Action of Loxoprofen 60mg
What is Loxoprofen 60mg? The drug contains Loxoprofen sodium hydrate, which has properties that provide rapid pain relief, strong anti-inflammatory effects, and fever reduction. However, the most remarkable effect of Loxoprofen 60mg is its potent analgesic action. This mechanism can be explained through the inhibition of prostaglandin synthesis, which is the core action of Loxoprofen. The site of action of the drug is within the oxidative ring.
Loxoprofen is taken orally, and Loxoprofen sodium hydrate is gradually absorbed in the gastrointestinal tract in its unchanged form, causing only mild gastric irritation. The drug is then rapidly metabolized into its active biologic form, transforming into the trans-OH isomer, which cooperates with SRS (serotonin receptor system) and inhibits prostaglandin synthesis to produce the pharmacological effects.
After administration, Loxoprofen is quickly absorbed in its unchanged form through the gastrointestinal tract, causing minimal gastric mucosal irritation. It is rapidly converted into its metabolite, the OH derivative. The plasma concentration of Loxoprofen peaks in its unchanged form, and its metabolites are observed after approximately 30 minutes and 50 minutes, respectively. The half-life of the drug can last around 1.25 hours.
The binding of Loxoprofen to plasma proteins is about 97%, and the trans-OH derivative binds at about 92.8%. The AUC (area under the curve) of Loxoprofen averages 6.7 ± 0.26 mg.h/mL, while that of trans-OH is 2.02 ± 0.05 mg.h/mL.
Loxoprofen is also rapidly excreted through the urine, with approximately 50% of the dose being eliminated within 8 hours. The excretion mainly occurs as Loxoprofen conjugated with glucuronate and in the trans-OH form.
2. Indications and Contraindications for Using Loxoprofen
What is Loxoprofen? Loxoprofen belongs to the non-steroidal anti-inflammatory drugs (NSAIDs) class and is available over the counter (ETC). It is indicated for the following conditions:
- Treatment of pain and inflammation associated with chronic rheumatoid arthritis, osteoarthritis, back pain, Periarthritis Humeroscapularis, and the shoulder-hand-neck syndrome.
- Reducing mild to moderate pain, as well as providing anti-inflammatory effects after surgeries, injuries, and tooth extractions.
- Alleviating muscle pain, neuralgia, headaches, toothache, or dysmenorrhea.
- Reducing fever and inflammation caused by upper respiratory tract infections, which may or may not involve bronchitis.
However, Loxoprofen is contraindicated in certain cases, such as:
- Patients who are hypersensitive to Loxoprofen or any of its components.
- Individuals with a history of hypersensitivity reactions such as asthma, rhinitis, angioedema, or urticaria when using aspirin or other non-steroidal anti-inflammatory drugs (NSAIDs).
- Patients with active peptic ulcers.
- Individuals with severe heart failure or significant blood, liver, or kidney disorders.
- Pregnant and breastfeeding women should avoid using Loxoprofen.
3. Dosage and Administration of Loxoprofen
Loxoprofen is formulated as tablets for oral use. It can be taken with or after meals. For adults, the recommended dose for each administration is typically 60mg, corresponding to one tablet of Loxoprofen. The patient should take the medication three times a day. In cases of acute illness, a single dose of 60mg-120mg may be used. However, the dosage should be adjusted based on age, the severity of symptoms, and other factors, but the total daily dose should not exceed 180mg.
The dosage mentioned here is for reference purposes. If you are using the medication for an eye health condition, you should consult an ophthalmologist for appropriate advice.
If a dose is missed, it should be taken as soon as remembered. However, if the missed dose is close to the next scheduled dose, it should be skipped, and the patient should take the next dose as planned. Avoid taking double doses, as this may cause adverse effects.
Currently, there have been no specific reports of overdose with Loxoprofen. However, if an overdose occurs, it may worsen symptoms and the condition. There is no antidote for Loxoprofen overdose, but the doctor may advise taking activated charcoal or performing gastric lavage if the overdose occurred within an hour. Close monitoring of the patient is required. Treatment primarily focuses on symptomatic support, maintaining fluid balance, ventilation, and monitoring cardiovascular and vital signs. If seizures occur, anticonvulsant medication may be prescribed, or bronchodilators can be used in case of asthma.
4. Precautions When Using Loxoprofen
In some cases, side effects may occur while using the medication.
- Common side effects include: rash, edema, drowsiness, abdominal pain, gastrointestinal discomfort, nausea, vomiting, diarrhea, and even elevated liver enzymes.
- Less common side effects include: gastric and duodenal ulcers, leukopenia, eosinophilia, palpitations, increased alkaline phosphatase, etc.
If side effects occur during treatment, the patient should stop using the medication and inform the treating doctor. In cases of severe adverse reactions, emergency treatments such as epinephrine administration, oxygen therapy, or antihistamine use may be necessary.
Drug Interactions with Loxoprofen:
- Loxoprofen should not be combined with aspirin, except in low doses and under the supervision of a doctor. It should not be taken with other NSAIDs, as this may increase the risk of adverse effects.
When used with corticosteroids, Loxoprofen can increase the risk of gastrointestinal side effects.
Co-administration with antihypertensive medications or diuretics may reduce the effectiveness of Loxoprofen. Diuretics may also increase renal toxicity. - When combined with anticoagulants, Loxoprofen can enhance the effect of anticoagulants like warfarin.
- Combining with antiplatelet drugs and selective serotonin reuptake inhibitors may increase the risk of gastrointestinal bleeding.
- When used with cardiac glycosides, it can exacerbate heart failure, reduce glomerular filtration rate, and elevate glycoside concentrations in the bloodstream.
- When combined with lithium, it may increase lithium concentrations in the blood.
- Co-administration with cyclosporine or tacrolimus may increase the risk of renal toxicity.
- Combining it with mifepristone may reduce its effectiveness, especially within 8-12 hours after mifepristone intake.
Additionally, Loxoprofen should be used cautiously in patients with Crohn's disease, hypertension, infections, asthma, or other allergic disorders.
Loxoprofen is prescribed to treat pain and inflammation associated with conditions like chronic rheumatoid arthritis, osteoarthritis, and frozen shoulder. To ensure effective treatment and avoid adverse effects, patients should take the medication according to the prescribed regimen and seek advice from their healthcare providers or pharmacists.
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