Loxoprofen
Loxoprofen Uses, Dosage, Side Effects, Food Interaction and all others data.
Loxoprofen is a propionic acid derivative non-steroidal anti-inflammatory drug. It is marketed under the trade name Loxonin in Brazil, Mexico and Japan by Sankyo, as Loxomac in India, and as Oxeno in Argentina. A transdermal preparation was approved for use in Japan in January 2006.
Loxoprofen is a non-selective inhibitor of cyclooxygenase enzymes, which are responsible for the formation of various biologically active pain, fever, and inflammatory mediators. These include prostaglandins, prostacyclin, thromboxane, and arachidonic acid.
| Trade Name | Loxoprofen |
| Generic | Loxoprofen |
| Loxoprofen Other Names | Loxoprofen, Loxoprofene, Loxoprofeno, Loxoprofenum |
| Type | |
| Formula | C15H18O3 |
| Weight | Average: 246.3016 Monoisotopic: 246.125594442 |
| Protein binding | 99% albumin-bound. At doses of loxoprofen greater than 500 mg/day, clearance of the drug increases as saturation of plasma protein binding occurs at higher doses. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Loxoprofen is an NSAID used to treat pain and inflammation in musculoskeletal conditions.
Loxoprofen is non-steroidal anti-inflammatory medication (NSAID) indicated for pain and inflammation related to musculoskeletal and joint disorders. In addition to its effects on pain, it is an antipyretic and anti-inflammatory medication.
Loxoprofen is also used to associated treatment for these conditions: Musculoskeletal Pain, Rheumatism, Soft Tissue Injury
How Loxoprofen works
Loxoprofen itself is a prodrug and carries little-to-no pharmacological activity - it is rapidly metabolized to its trans-alcohol form, which is a potent and non-selective inhibitor of cyclooxygenase. Cyclooxygenase (COX) is present in 2 forms, COX-1 and COX-2, with each serving different functions. COX-1 is present in human cells and is constitutively released, performing cellular housekeeping functions such as mucus production and platelet aggregation. COX-2 is induced in human cells post-injury or due to other stimuli, is triggered to appear in large quantities at the sites of injury/stimuli, and is ultimately responsible for the mediation of inflammation and pain.
Loxoprofen's active metabolite inhibits both COX isoforms, resulting in reduced expression of several mediators of pain, inflammation, and fever (e.g. prostaglandins, prostacyclin, thromboxane, etc).
Toxicity
Adverse effects include anorexia, nausea, vomiting, bleeding, anemia, diarrhea, and constipation. Loxoprofen toxicity may lead to gastrointestinal disturbance (including flatulence, dyspepsia and gastritis) and renal failure.
Food Interaction
- Exercise caution with grapefruit products. Loxoprofen is metabolized by CYP3A4 to an inactive metabolite and grapefruit is a CYP3A4 inhibitor.
- Exercise caution with St. John's Wort. Loxoprofen is metabolized by CYP3A4 to an inactive metabolite and St. Johns Wort is a CYP3A4 inducer.
- Take with food. Taking loxoprofen with food may reduce the risk of gastrointestinal upset.
Volume of Distribution
Loxoprofen has a volume of distribution of 0.16 L/kg.
Elimination Route
Loxoprofen is rapidly and completely absorbed from the GI tract with a bioavailability of 95%. The absorption phase of the medication occurs in the first 4-6 hours after ingestion. Food ingestion with the medication causes a slight decrease in the rate of loxoprofen absorption.
Half Life
The elimination half-life of Loxoprofen is approximately 15 hours. Steady concentration is achieved after 2-3 doses.
Clearance
Most of the drug as unchanged loxoprofen, 6-0-desmethyl loxoprofen (less than 1%) and glucuronide or other conjugates (66-92%).
In patients with renal failure, metabolites may accumulate.
Elimination Route
50% renal excretion. This drug is 20% - 30% excreted in the stool.
Innovators Monograph
You find simplified version here Loxoprofen
