Diclofenac is the anti-inflammatory drug (NSAID) world’s best selling and with few side effects or adverse.
Diclofenac was first sold in 1974 in Japan. It is now distributed in 120 countries. Diclofenac is a sodium salt of phenylacetic acid derivative. Developed from other NSAIDs, with the inclusion of a phenylacetic acid group, a secondary amino group and a phenyl ring with two chlorine atoms.
Applications of diclofenac
Diclofenac has its application in the treatment of musculoskeletal disorders, with particular effectiveness in rheumatoid arthritis, osteoarthritis, spondylitis, ankylosing spondylitis, gout attacks and gallstones and kidney. Also very effective in treating migraines. Other applications to consider include postoperative pain after a traumatic process or menstrual cramps. Rectally are particularly suitable for preemptive analgesia and postoperative nausea. It is also encouraging its use for treating cancer pain. The fever caused by Hodgkin’s lymphoma also has an effective response in the diclofenac.
To administer the diclofenac dose : Dosage
In prolonged treatments or in mild cases should be given between 75 and 100 mg. per day. The maximum dose generally should not exceed 150 mg. divided into 2 or 3 times a day. In cases of primary dysmenorrhoea, the daily dose will vary between 50 and 200 mg. daily. We do not recommend the use of diclofenac in children under 12 years.
Contraindications of diclofenac
Despite being one of the better tolerated drugs, after prolonged use and just as with other NSAIDs, it is possible that diclofenac can develop peptic ulcers in patients predisposed to it. In these cases you opt for the combination of diclofenac with misoprostol , a drug analogue that protects the gastric mucosa. You can also alter platelet function and bleeding in predisposed patients.
The short-term adverse effects (4.6%) and long term (4.9%) included nausea, vomiting, abdominal pain, dyspepsia and diarrhea. Other uncommon side effects are central nervous system disorders, transient depression of renal function and increased aspartate amino transferase. It is not recommended for use in patients with inflammatory bowel diseases with porphyria pre-existing liver or recovering from heart surgery.
Pharmacokinetics of diclofenac
Diclofenac has an almost complete absorption -90% – by removing the body dose administered in any way after four days, 65% in the urine and the remaining 35% via the faeces. The maximum concentration is reached within the hour and half and two hours after oral administration. The food is capable of delaying absorption and reduce the peak. The highest concentrations of the drug is located in the liver and kidneys and is also high in blood, heart and lungs.
Comparison of Diclofenac with other medications
With regard to rheumatoid arthritis diclofenac and aspirin showed similar results concerning the antiinflammatory effects, even when the diclofenac was preferred by doctors and patients. Adverse effects, however, were superior in the case of aspirin. Compared with indomethacin, diclofenac showed superior efficacy was found to have a greater tolerance. With respect to ibuprofen, diclofenac was also more effective, reducing the stiffness and pain intensity. Other studies place to diclofenac at the same height, as to efficacy, the naproxen and phenylbutazone.
Applied to osteoarthritis, diclofenac also shown superior to aspirin and indomethacin equal to, but with a significantly better tolerance. In comparison with ibuprofen is achieved pain relief with diclofenac evident, resulting adverse effects also lower. Both efficacy and tolerance were similar between diclofenac and naproxen.
Diclofenac can be found in different forms. Since formulations resistant to gastric acids, 25 and 50 mg, through the effervescent tablets of 50 mg slow release forms, controlled 75, 100 and 125 mg, suppositories 50 and 100 mg and injectable formulations 50 and 75 mg.