Nitrodexketoprofen (HCT 2037)

Subanalgesic doses of dexketoprofen and HCT-2037 (nitrodexketoprofen) enhance fentanyl antinociception in monoarthritic rats.

Gaitan G, Herrero JF.

Departamento de Fisiologia, Facultad de Medicina, Campus Universitario, Universidad de Alcala, Alcala de Henares, 28871 Madrid, Spain.

Subanalgesic doses of the non-steroidal antiinflammatory drugs (NSAID) dexketoprofen trometamol and nitroparacetamol (NCX-701) enhance mu-opiate fentanyl effect in acute nociception. It is not known if a similar combination of drugs is effective in situations of spinal cord sensitization. The aim of this study was to assess if the enhancement of fentanyl antinociception can be observed in carrageenan-induced monoarthritis, when combined with dexketoprofen (DKT) or nitrodexketoprofen (HCT-2037). Withdrawal reflexes were recorded as single motor units in male Wistar rats anesthetized with alpha-chloralose. Fentanyl was studied alone and in the presence of 0.4, 0.8 micromol/kg of DKT or 0.3 micromol/kg of HCT-2037. In responses to noxious mechanical stimulation, the ID50 of fentanyl was enhanced twofold by 0.8 micromol/kg DKT and more than fourfold by HCT-2037 and no significant recovery was observed 45 min later. DKT 0.4 micromol/kg was, however, very little effective. The opioid antagonist naloxone did not reverse the effect. Enhancement of fentanyl effect on wind-up was only observed with HCT-2037 but not with DKT. We conclude that the combined administration of subanalgesic doses of dexketoprofen derivatives, specially its nitroderivative, and the mu-opiate fentanyl is an effective antinociceptive therapy in situations of articular inflammation involving a naloxone-independent mechanism of action.

PMID: 15680185 [PubMed - indexed for MEDLINE]

A propos du Dexketoprofen Trometamol

How does it work?

Dexketoprofen belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs). It works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of chemicals in the body called prostaglandins. Prostaglandins are produced in response to injury or certain diseases and would otherwise go on to cause swelling, inflammation and pain. By blocking cyclo-oxygenase, dexketoprofen prevents the production of prostaglandins and therefore reduces inflammation and pain.


What is it used for?

Mild to moderate pain


Warning!

This medicine may cause dizziness and so may affect your ability to drive or operate machinery safely. Do not drive or operate machinery until you know how this medicine affects you and you are sure it won't affect your performance.
For fast relief of pain, take at least 30 minutes before food, as food delays the absorption of this medicine from the gut.
This medicine is not for long term use


Use with caution in

Decreased heart function
Disorders involving the formation of blood cells (haematopoietic disorders)
Elderly people
Excess retention of water in the body tissues (fluid retention)
History of allergies
Long-term inflammation of skin and some internal organs (systemic lupus erythematosus)
Low volume of circulating blood (hypovolaemia)
Mild to moderately decreased liver function
Mildly decreased kidney function
Syndrome with symptoms of systemic lupus erythematosus, scleroderma, polymyositis, and raynaud's phenomenon (mixed connective tissue disease)


Not to be used in

Active bleeding
Allergy to aspirin or other medicines in this class
Asthma or history of asthma
Bleeding disorders
Bleeding from the stomach or intestines
Breastfeeding
Children
Crohn's disease
History of stomach or duodenal ulcers or indigestion
Inflammation of the bowel and back passage
Inherited tendency to bleed (haemorrhagic diathesis)
Moderate to severely decreased kidney function
Peptic ulcers
Pregnancy
Severe heart failure
Severely decreased liver function

This medicine should not be used if you are allergic to one or any of its ingredients. Please inform your doctor or pharmacist if you have previously experienced such an allergy. If you feel you have experienced an allergic reaction, stop using this medicine and inform your doctor or pharmacist immediately.

Vu les effets secondaires engendrés par cette molécule, on comprend rapidement l'intéret de Nicox pour celle-ci !