Dexketoprofen

Dexketoprofen is a Nonsteroidal Anti-inflammatory Drug belonging to the analgesic class.

Dexketoprofen is an NSAID that is the R(-)-enantiomer of racemic ketoprofen with analgesic and anti-inflammatory properties used for the treatment of mild to moderate pain.

After oral ingestion, the Dexketoprofen onset of action is within 30 minutes. The plasma half-life of Dexketoprofen is about 4-6 hours. The Cmax is about 30 minutes. The volume of distribution of Dexketoprofen is about <0.25 L/kg and it is Highly protein bounded. Dexketoprofen is highly lipophilic and is metabolized in the liver by glucuronidation. Tmax was approximately 30 min for a Cmax of 3.7 ± 0.72 mg/l. Dexketoprofen is metabolized by the hepatic cytochrome P450 enzymes (CYP2C8 and CYP2C9). Dexketoprofen has several metabolites, with hydroxyl derivatives making up the greatest volume. In humans, hydroxylation plays a minor role. Dexketoprofen is primarily conjugated to an acyl-glucuronide. Approximately 70 to 80% of the ingested dose is recovered in the urine during the first 12 hours post-ingestion, mainly in the acyl-conjugated form of the drug.

Dexketoprofen shows side effects like Nausea and Vomiting, Diarrhea, Stomach pain, Headache, Dry mouth, Skin rash, Weakness.

Dexketoprofen is available in the form of Oral tablets and Injectable solutions.

Dexketoprofen is available in India, US, UK, China, France, Italy, Germany, Spain, Australia and Turkey.

Dexketoprofen is an Analgesic belonging to the class Nonsteroidal Anti-inflammatory Drug.

Dexketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that reduces prostaglandin synthesis via inhibition of cyclooxygenase pathway (both COX-1 and COX-2) activity.

The Onset of action of Dexketoprofen can be observed within 30 minutes of administration of the dose.

The Duration of action required for Dexketoprofen to show its action is not clinically established.

The time to peak concentration of Dexketoprofen is approximately 30 minutes.

Dexketoprofen is available in the form of Oral Tablets and Injectable solutions.

Dexketoprofen tablets taken orally should be taken on an empty stomach. Take 30 min before meals, especially for quick relief of acute pain.

Dexketoprofen is used to relieve mild to moderate pain associated with surgeries, muscle aches, sprains, sports injuries, painful periods, toothache, etc. Dexketoprofen is not recommended for use in patients under 18 years of age.

Dexketoprofen is a Nonsteroidal Anti-inflammatory Drug belonging to the analgesic class.

Dexketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that reduces prostaglandin synthesis via inhibition of cyclooxygenase pathway (both COX-1 and COX-2) activity.

Dexketoprofen is approved for use in the following clinical indications

Dexketoprofen is an NSAID with analgesic and anti-inflammatory properties used for the treatment of mild to moderate pain.

• Mild to moderate pain

Adult Oral Dose: 12.5 mg 4-6 hourly or 25 mg 8 hourly. Max: 75 mg daily.

Elderly Oral Dose: Initiate at the lower end of the dosage range with total dose not exceeding 50 mg daily. Dose may be increased to that recommended for general population only if well tolerated.

• Moderate to severe acute pain

Adult Parenteral Dose: 50 mg 8-12 hourly via slow IV bolus inj over not less than 15 seconds, or infused over 10-30 minutes, or via slow deep IM inj. Dosage may be repeated 6 hours apart if necessary. Max: 150 mg total daily dose. Switch to oral treatment as soon as possible.

Dexketoprofen is available in various strengths as 12.5mg, 25mg, 50mg and 75mg.

Dexketoprofen is available in the form of Oral Tablets and Injectable solutions.

• Dosage Adjustment in Kidney Patient

CrCl (60-89 mL/min): Initially, 50 mg total daily dose.

CrCl (≤59 mL/min): Contraindicated.

• Dosage Adjustment in Hepatic impairment Patient

Mild to moderate: Initially, 50 mg total daily dose.

Severe: Contraindicated.

Dexketoprofen is contraindicated in patients with

• Hypersensitivity to aspirin, or other NSAIDs.
• History of bronchial asthma or asthma attacks, bronchospasm, angioneurotic oedema, urticaria, acute rhinitis or nasal polyps that were precipitated or caused by aspirin or other NSAIDs.
• Any history of gastrointestinal bleeding, ulceration, or perforation, including related to previous NSAIDs treatment.
• Severe hepatic (Child-Pugh score 10-15) impairment.
• Pregnancy (3rd trimester) and lactation.

• Heart disease

Dexketoprofen should be used with caution in patients with heart diseases due to the increased risk of adverse effects on the heart, especially after a prolonged use. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition.

• Hypertension

Dexketoprofen should be used with caution in patients with a known history of hypertension due to the increased risk of worsening of the patient's condition. Close monitoring of blood pressure is recommended for such patients. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition of the patient.

• Gastro-intestinal bleeding

Dexketoprofen may cause severe gastrointestinal bleeding and perforation after prolonged usage. These adverse events may occur with or without warning symptoms. This risk is especially higher in the elderly population and in patients with a history of gastrointestinal diseases. Appropriate dose adjustments or replacement with a suitable alternative may be required based on the clinical condition.

• Female fertility

Use of Dexketoprofen may impair female fertility. Discuss all the risks and benefits before using this medicine.

Consumption of alcohol is not recommended during treatment with Dexketoprofen due to the increased risk of serious side effects such as severe gastrointestinal bleeding, dizziness, fatigue, weakness, etc.

Dexketoprofen is not recommended for use in breastfeeding women unless necessary. All the risks and benefits should be considered before using Dexketoprofen.

Dexketoprofen is not recommended for use in pregnant women unless necessary. All the risks and benefits should be considered before using Dexketoprofen.

• Common

Renal effects (e.g. deteriorated renal function, fluid retention, oedema, increased BUN or creatinine), hepatic effects (e.g. significantly elevated AST/ALT), increased risk of MI or stroke (high doses), exacerbated colitis or Crohn’s disease, inhibited platelet aggregation, prolonged bleeding time, masked symptoms of infection.

• Dexketoprofen may increase the risk of toxicity of lithium, methotrexate, hydantoins and sulfonamides.
• Dexketoprofen may reduce the effects of diuretics and antihypertensive agents.
• Dexketoprofen may enhance the nephrotoxic effects with ciclosporin, tacrolimus, diuretics, ACE inhibitors, angiotensin II receptor antagonist, antibacterial aminoglycosides.
• Dexketoprofen may increase plasma concentrations with probenecid.
• Dexketoprofen may increase the hypoglycaemic effects of sulfonylureas.
• Dexketoprofen may decrease the elimination of pemetrexed. May elevate plasma levels of cardiac glycosides.

The common side effects of Dexketoprofen include the following

• Common side effects

Nausea and Vomiting, Diarrhea, Stomach pain, Headache, Dry mouth, Skin rash, Weakness.

• Rare side effects

Dizziness, Nervousness, Loss of appetite, Increased sweating.

• Pregnancy

Pregnancy Category B

Dexketoprofen is not recommended for use in pregnant women unless necessary. All the risks and benefits should be considered before using Dexketoprofen.

• Nursing Mothers

Dexketoprofen is not recommended for use in breastfeeding women unless necessary. All the risks and benefits should be considered before using Dexketoprofen.

• Pediatric Use

Dexketoprofen is not recommended for use in children since the safety and efficacy of use are not clinically established.

• Geriatric Use

Dexketoprofen should be used with caution in the elderly population due to the increased risk of severe adverse effects. These patients should be started at lower doses to check for tolerance. Close monitoring of renal and liver function may be necessary for such patients based on the clinical condition.

Symptoms: Anorexia, nausea, vomiting, abdominal pain, headache, dizziness, vertigo, somnolence, and disorientation.

Management: Symptomatic treatment. Administer activated charcoal within 1 hour of ingesting more than 5 mg/kg. May be removed by dialysis.

• Pharmacodynamic

This drug is an isomer of ketoprofen. Dexketoprofen a propionic acid derivative with analgesic, anti-inflammatory, and antipyretic properties.

• Pharmacokinetics

Absorption

After oral ingestion, the Dexketoprofen onset of action is within 30 minutes. The plasma half-life of Dexketoprofen is about 4-6 hours. The Cmax is about 30 minute.

Distribution

The volume of distribution of Dexketoprofen is about <0.25 L/kg and it is Highly protein bounded.

Metabolism and Excretion

Dexketoprofen is highly lipophilic and is metabolized in the liver by glucuronidation. In one study, after oral administration of 25 mg of dexketoprofen to young healthy adults, Tmax was approximately 30 min for a Cmax of 3.7 ± 0.72 mg/l. Dexketoprofen trometamol is metabolized by the hepatic cytochrome P450 enzymes (CYP2C8 and CYP2C9). Dexketoprofen trometamol has several metabolites, with hydroxyl derivatives making up the greatest volume. In humans, hydroxylation plays a minor role. Dexketoprofen is primarily conjugated to an acyl-glucuronide. Approximately 70 to 80% of the ingested dose is recovered in the urine during the first 12 hours post-ingestion, mainly as the acyl-conjugated form of the drug.

• https://www.uptodate.com/contents/dexketoprofen-international-drug-information-concise?search=Dexketoprofen&source=panel_search_result&selectedTitle=1~4&usage_type=panel&kp_tab=drug_international&display_rank=1#F1978466
• https://go.drugbank.com/drugs/DB09214
• https://www.drugs.com/international/dexketoprofen.html
• https://www.lybrate.com/medicine/dexketoprofen