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Diclofenac is a preparation that is available in pharmacies in the form of tablets, gels, injections and patches. This drug has found its greatest use in rheumatology, but it is also used by people who try to combat the pain associated with injuries or, in the case of women, with menstruation. What are the indications for the use of diclofenac?
Diclofenac – characteristics
Diclofenac is a commonly used non-steroidal anti-inflammatory drug (NSAID) for the treatment of chronic forms of arthritis and acute mild to moderate pain. Treatment with full doses of diclofenac is often associated with mild increases in serum transaminases and, in rare cases, may lead to severe, clinically apparent, acute or chronic liver disease.
This preparation was introduced into the medical circulation in 1979 and is now one of the most frequently prescribed and used anti-inflammatory drugs. There are several dozen preparations available in Poland that contain diclofenac. Although diclofenac is an acid, it is pharmacologically in the form of the sodium salt.
See also: Liver disease – how to protect yourself? Preventive examinations and vaccinations
Diclofenac – action
Diclofenac has analgesic, anti-inflammatory and antipyretic properties. The mechanism of action of diclofenac, like other NSAIDs, is not fully understood, but it involves inhibition of cyclooxygenase (COX-1 and COX-2).
Diclofenac is a potent inhibitor of prostaglandin synthesis in vitro. The diclofenac concentrations achieved during therapy induced in vivo effects. Prostaglandins sensitize afferent nerves and potentiate the pain inducing effect of bradykinin in animal models. Prostaglandins are inflammatory mediators. Since diclofenac is an inhibitor of prostaglandin synthesis, its mechanism of action may be due to a reduction in the concentration of prostaglandins in peripheral tissues.
Diclofenac is absorbed 100% after oral administration compared to intravenous administration as measured by urine recovery. However, due to first pass metabolism, only about 50% of an absorbed dose is systemically available. Food has no significant influence on the extent of absorption of orally ingested diclofenac. However, there is usually a delay in the start of absorption of 1 to 4,5 hours and a fall in peak plasma concentration of <20%.
Diclofenac is eliminated by metabolism followed by urinary and bile excretion of glucuronide and conjugates of sulphated metabolites. Little or no free unchanged diclofenac is excreted in the urine. About 65% of the dose is excreted in the urine and about 35% in the bile as metabolites of unchanged diclofenac. Since renal excretion is not a significant elimination pathway for unchanged diclofenac, no dosage adjustment is necessary for subjects with mild to moderate renal impairment. The terminal half-life of unchanged diclofenac is approximately 2 hours.
Read also: Drug interactions – what should I be aware of when taking medication?
Diclofenac – indications
The indication for the use of diclofenac is any inflammation, pain or swelling. Diclofenac is a medicine used in the case of:
- rheumatoid arthritis,
- ankylosing spondylitis,
- gout.
Diclofenac can bring relief in the treatment of post-traumatic pain, postoperative pain, neuralgia, menstrual pain and inflammation of the appendages. Ophthalmologists prescribe diclofenac to patients with anterior segment inflammation of the eyeball, following cataract surgery, or for the prevention of intraoperative miosis.
Diclofenac is present in drugs such as Olfen 75 SR, Olfen Uno and Diclac Duo.
Diclofenac – contraindications
The use of diclofenac is not recommended for all patients. There are contraindications that exclude the possibility of using this drug. Diclofenac cannot be used by patients who are hypersensitive to any of the ingredients of the drug. Contraindications to the use of dicofeank are also:
- gastric and duodenal ulcers,
- aspirin asthma
- hepatic impairment,
- kidney failure
- porphyria.
The drug should also not be used by children under 12 years of age. The use of diclofenac is also limited by congestive heart failure, ischemic heart disease, peripheral arterial disease, and cerebrovascular disease. Specialists do not recommend the use of diclofenac in cases of hypertension, hyperlipidemia or diabetes. Diclofenac should also not be taken by patients who smoke cigarettes.
Diclofenac – side effects
The use of diclofenac may cause side effects, especially in the gastrointestinal tract, kidneys, skin and cardiovascular system. The gastrointestinal side effects include: indigestion, nausea, epigastric pain, flatulence, diarrhea and constipation. In the case of the kidneys, acute renal failure, hematuria or proteinuria may occur. Allergic reactions such as hives, purpura and even hair loss may occur.
Diclofenac – overdose
Symptoms of diclofenac overdose: lethargy, somnolence, nausea, vomiting and epigastric pain, and gastrointestinal bleeding. Hypertension, acute renal failure, respiratory depression and coma are rare. In the event of overdose, supportive treatment should be provided and consideration should be given to induction of vomiting and administration of activated charcoal if the overdose has occurred less than 4 hours previously.