Roxogesic

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

Roxogesic 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.

Roxogesic 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 Roxogesic
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
Roxogesic
Roxogesic

Uses

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

Roxogesic 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.

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

How Roxogesic works

Roxogesic 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.

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

Food Interaction

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

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

Elimination Route

Roxogesic 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 Roxogesic 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 Roxogesic

*** Taking medicines without doctor's advice can cause long-term problems.
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