Loxoprofenum

Loxoprofenum Uses, Dosage, Side Effects, Food Interaction and all others data.

Loxoprofenum 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.

Loxoprofenum 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.

Loxoprofenum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Loxoprofenum
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

Loxoprofenum is an NSAID used to treat pain and inflammation in musculoskeletal conditions.

Loxoprofenum 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.

Loxoprofenum is also used to associated treatment for these conditions: Musculoskeletal Pain, Rheumatism, Soft Tissue Injury

How Loxoprofenum works

Loxoprofenum 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.

Loxoprofenum'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. Loxoprofenum toxicity may lead to gastrointestinal disturbance (including flatulence, dyspepsia and gastritis) and renal failure.

Food Interaction

Exercise caution with grapefruit products. Loxoprofenum is metabolized by CYP3A4 to an inactive metabolite and grapefruit is a CYP3A4 inhibitor.
Exercise caution with St. John's Wort. Loxoprofenum 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

Loxoprofenum has a volume of distribution of 0.16 L/kg.

Elimination Route

Loxoprofenum 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.