Dexketoprofen

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Introduction

Generic Name: Dexketoprofen
Chemical Formula: C16H14O3
Drug Class: Nonsteroidal Anti-inflammatory Drug (NSAID)
Stereochemistry: (S)-Enantiomer of Ketoprofen

Dexketoprofen is the active enantiomer of ketoprofen, a nonsteroidal anti-inflammatory drug (NSAID) that provides rapid and effective relief from pain and inflammation

Chemical Structure and Isomerism

This drug is the S(+) enantiomer of ketoprofen. This S(+) enantiomer exhibits enhanced pharmacological activity compared to the racemic mixture which makes it a more targeted therapeutic option with fewer side effects at lower doses.

Mechanism of Action

Dexketoprofen works primarily by inhibiting cyclooxygenase (COX) enzymes, particularly COX-1 and COX-2, which are responsible for converting arachidonic acid into prostaglandins, which are thechemicals that promote inflammation, pain, and fever.

  • COX-2 Inhibition: By inhibiting COX-2, dexketoprofen diminishes the production of pro-inflammatory prostaglandins, which decreases pain and inflammation.
  • COX-1 Inhibition: It also inhibits COX-1, which can lead to a reduction in protective prostaglandins in the gastrointestinal tract, which in turn raises the risk of gastrointestinal irritation, though a lower dose may subside the irritation to some degree.

Pharmacokinetics

  1. Absorption:
    Dexketoprofen is rapidly absorbed from the gastrointestinal tract after oral administration. It reaches peak plasma concentrations within 30 to 60 minutes, providing quick relief from pain and inflammation.
  2. Distribution:
    The drug exhibits a high plasma protein binding rate (~99%), ensuring it remains in the systemic circulation for effective targeting of inflamed tissues.
  3. Metabolism:
    This drug is metabolized in the liver, primarily through glucuronidation, which converts the active drug into easily excretable inactive metabolites.
  4. Excretion:
    Most of the active drug and its metabolites are excreted via the kidneys. The half-life of this drug is approximately 1 to 2 hours, making it a short-acting NSAID most suitaed for acute pain management.

Dexketoprofen Uses

  1. Acute Musculoskeletal Pain:
    Dexketoprofen is effective in treating acute pain such as muscle strains, sprains, and other injuries that result in inflammation and discomfort.
  2. Postoperative Pain:
    It is commonly used for postoperative pain relief, providing a fast and potent effect to help patients recover more comfortably after a surgery.
  3. Dysmenorrhea:
    It is also prescribed for menstrual pain (dysmenorrhea), alleviating pain associated with uterine contractions.
  4. Dental Pain:
    This drug is also effective in managing acute dental pain, particularly after treatments like tooth extraction or root canal procedure.

Dosage and Administration

  • For Acute Pain:
    • Adults: The usual dose is 25 mg every 8 hours, with a maximum daily dose of 75 mg.

Dexketoprofen should be taken with food to minimize the risk of gastrointestinal side effects. Due to its rapid absorption, it offers fast-acting relief, making it ideal for acute pain scenarios.

Side Effects of Dexketoprofen

Dexketoprofen is generally well-tolerated, but like all NSAIDs, it can cause side effects, particularly with long-term or high-dose use.

  • Common Side Effects:
    • Gastrointestinal issues such as nausea, heartburn, or indigestion.
    • Dizziness or headache.
    • Skin rashes or itching.
  • Serious Side Effects:
    • Gastrointestinal Bleeding: Prolonged use may lead to stomach ulcers or bleeding, though the risk is reduced when used at lower doses.
    • Kidney Impairment: Long-term use may cause kidney damage, particularly in those with pre-existing kidney conditions.
    • Cardiovascular Risk: Prolonged NSAID use may increase the risk of heart attack or stroke, especially in individuals with pre-existing cardiovascular issues.

Contraindications of Dexketoprofen

Dexketoprofen is contraindicated in the following cases:

  • Allergies to NSAIDs: Patients with known hypersensitivity to ketoprofen or other NSAIDs should avoid dexketoprofen.
  • Peptic Ulcers: Individuals with active gastrointestinal ulcers or a history of gastrointestinal bleeding should not take this medicine.
  • Severe Kidney or Liver Disease: Patients with significant kidney or liver impairment should avoid this drug due to the risk of exacerbating these conditions.
  • Pregnancy (Third Trimester): Like other NSAIDs, this medicine is contraindicated in the third trimester due to the risk of complications for the fetus.

Drug Interactions

  • Anticoagulants (e.g., Warfarin): The co-administration with anticoagulants leads to an increase in the risk of bleeding.
  • Other NSAIDs: Combining dexketoprofen with other NSAIDs also increases the likelihood of gastrointestinal issues along with kidney damage.
  • Diuretics and ACE Inhibitors: This drug may reduce the efficacy of these drugs and increase the risk of kidney damage.

Warnings and Precautions

  1. Gastrointestinal Health: Dexketoprofen increases the risk of gastrointestinal bleeding, particularly in those with a history of peptic ulcers. It is important to monitor the patient for signs of gastrointestinal discomfort, especially in long-term treatment regimen.
  2. Kidney Monitoring: Prolonged use of this drug may impair the kidney function, especially in patients with existing kidney conditions or those taking diuretics.
  3. Cardiovascular Risk: Long-term use of dexketoprofen, like other NSAIDs, may lead to an increase in the risk of cardiovascular events, including myocardial infarction and stroke.

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