Loxoprofen: Indications, Mechanism of Action, Dosage, Interactions, Contraindications and Warnings

It is a non-steroidal anti-inflammatory drug in the group of propionic acid derivatives, which also includes ibuprofen and naproxen , among others.

It is marketed as a sodium salt under the trade names Loxoprofen Sodium, Oxeno or Loxomac. It is available for oral, rectal, topical, and intravenous administration.


The exact mechanisms of action of loxoprofen are unknown.

Its anti-inflammatory effects are believed to be due to the inhibition of both cytooxygenase-1 (COX-1) and cytooxygenase-2 (COX-2).

This leads to inhibition of prostaglandin synthesis.

Antipyretic effects may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

Mechanism of action

Loxoprofen is a non-selective cyclooxygenase inhibitor. It works by reducing the synthesis of prostaglandins from arachidonic acid.

It is a prodrug that is rapidly converted to an active metabolite after oral administration.


This medicine is used to:

  • The joint syndrome ( rheumatoid arthritis , osteoarthritis, ankylosing spondylitis, gout).
  • Degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathy).
  • Post-traumatic inflammation of the soft tissues and the musculoskeletal system (sprains, bruises).
  • Pain in the spine
  • Neuralgia.
  • Myalgia.
  • Arthralgia.
  • Pain and swelling after surgery or injury.
  • Migraine.
  • Algomenorrea.
  • Pain with bursitis.
  • Proctitis.
  • Colic (biliary and renal).
  • Pain in infectious and inflammatory diseases of the ENT organs.

In addition, it can be applied as a local use for:

  • Inhibition of miosis during surgery for prevention of cystoid macular edema cataract associated with lens removal and implantation.
  • The non-infectious nature of the inflammatory eye.
  • Post-traumatic inflammation in the penetrating and non-penetrating wound of the eyeball.


For oral use for adults, the single dose is 25 to 50 mg 2 to 3 times a day.

The frequency of consumption depends on the dosage form used, the severity of the disease.

Rectally the dose is 1 to 3 times a day.

For the treatment of acute conditions or exacerbation of chronic edema use, it is applied intramuscularly in a dose of 75 mg once a day.

For children over 6 years of age and adolescents the daily dose is 2 mg.

As a topical, a dose of 2 to 4 g (depending on the size of the painful area) is applied to the affected area 3 to 4 times a day.

When used in ophthalmology, the frequency and duration of administration are determined individually.

The maximum oral daily dose for adults is 150 mg. It should be taken immediately after meals.


Coumarin-type anticoagulants

Several short-term controlled studies failed to demonstrate that loxoprofen significantly affects clotting factors when administered to individuals with coumarin-type anticoagulants.

However, bleeding has been reported when loxoprofen and other non-steroidal anti-inflammatory agents have been administered to patients taking coumarin-type anticoagulants.

Therefore, the physician should exercise caution when administering loxoprofen to patients taking anticoagulants.


Aspirin administered with loxoprofen has been shown to produce a net decrease in anti-inflammatory activity with reduced blood levels of the non-aspirin drug.

Single dose bioavailability studies in normal people have not shown an ontradictory effect of aspirin on blood levels with loxoprofen.

However, correlative clinical studies have not been performed.


Clinical studies, as well as randomized observations, have shown that loxoprofen can reduce the natriuretic effect of furosemide and thiazides in some patients.

During concomitant therapy with loxoprofen, the patient should be closely observed for signs of renal failure, as well as to ensure diuretic efficacy.

Side effects

Adverse effects are generally of gastrointestinal effect, such as:

  • Anorexia.
  • Vomiting
  • Diarrhea.
  • Constipation.

Other effects not related to the gastrointestinal system are:

  • Anemia.
  • Leucopenia.
  • Thrombocytopenia


Children’s loxoprofen or ibuprofen tablets should not be used in patients:

  • Who have previously shown hypersensitivity to the drug.
  • With nasal polyps syndrome.
  • With angioedema.
  • With bronchospastic reactivity to aspirin or other non-steroidal anti-inflammatory agents.

Anaphylactoid reactions have occurred frequently in these types of patients.

During pregnancy

The use of the drug during pregnancy and lactation is possible in cases where the potential benefits to the mother exceed the potential risk to the fetus or newborn.


Among the symptoms of overdose with the drug can be:

  • Hypotension
  • Renal insufficiency.
  • Seizures
  • Gastrointestinal irritation.
  • Respiratory depression

There is no specific antidote to treat overdose with loxoprofen. Gastric lavage or other symptomatic and supportive therapy is recommended.

The use of forced diuresis, dialysis, or blood transfusion is not justified because NSAIDs are highly associated with serum proteins and have extensive metabolism.


Loxoprofen is a non-steroidal anti-inflammatory drug used to relieve pain and inflammation, reduce fever, and treat osteoarthritis, rheumatoid arthritis, and menstrual cramps.

To avoid further complications, the patient should inform her physician if she is pregnant or breastfeeding.

Loxoprofen should not be taken during the last three months of pregnancy.

For more effective treatment, the patient should inform his doctor if he uses alcohol on a chronic basis.

Loxoprofen should not be taken with aspirin products.

This medicine should be taken with food, milk, or antacids if stomach upset occurs.

Loxoprofen can cause dizziness and drowsiness; the patient must be careful when driving or operating dangerous machinery.

Loxoprofen sodium can cause increased sensitivity to sunlight. Therefore, it is recommended to use sunscreen and protective clothing until the degree of sensitivity is determined.

It is important that the patient notify their doctor if they develop stomach pain, vomiting blood.