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Diclofenac (sold under a number of trade names) is a nonsteroidal anti-inflammatory drug (NSAID) taken or applied to reduce inflammation and as an analgesic reducing pain in certain conditions. It is supplied as or contained in medications under a variety of trade names.
The primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is thought to be inhibition of prostaglandin synthesis by inhibition of cycloxygenase-2 (COX-2). Diclofenac inhibits COX-2 with 20-fold more potency than COX-1 and is said to have a lower incidence of gastrointestinal complaints than COX-1 inhibitors such as aspirin. Some evidence indicates it inhibits the lipoxygenase pathways which are related to inflammation,, and possibly phospholipase A2, as well as possibly phase inhibition (blockage) of voltage-dependent sodium channels, blockage of acid-sensing ion channels (ASICs) and positive allosteric modulation of KCNQ- and BK- potassium channels (related to hyperpolarization of the cell membrane). It also appears to exhibit bacteriostatic activity. Diclofenac lasts for around 6–8 hours in the body, possibly as it persists for over 11 hours in synovial fluids.
The name “diclofenac” derives from its chemical name: 2-(2,6- dic h lo ranilino) phen yl ac etic acid. Diclofenac was first synthesized by Alfred Sallmann and Rudolf Pfister and introduced as Voltaren by Ciba-Geigy (now Novartis ) in 1973, now by Glaxo SmithKline.
Use of diclofenac for animals is controversial due to toxicity when eaten by scavenging birds that eat dead animals; the drug has been banned for veterinary use in many countries.
Contents
1 Medical uses
1.1 Pain
2 Contraindications
3 Adverse effects
3.1 Cardiac
3.2 Gastrointestinal
3.3 Hepatic
3.4 Renal
3.5 Mental health
4 Mechanism of action
5 Ecological effects
6 Formulations and trade names
7 References
8 External links
Medical uses
Diclofenac is used to treat pain, inflammatory disorders, and dysmenorrhea.
Pain
Inflammatory disorders may include musculoskeletal complaints, especially arthritis, rheumatoid arthritis, polymyositis, dermatomyositis, osteoarthritis, dental pain, temporomandibular joint (TMJ) pain, spondylarthritis, ankylosing spondylitis, gout attacks, and is effective against menstrual pain and endometriosis.
Diclofenac is also available in topical forms and has been found to be useful for osteoarthritis but not other types of long-term musculoskeletal pain.
It may also help with actinic keratosis, and acute pain caused by minor strains, sprains, and contusions (bruises).
In many countries,
Diclofenac is often used to treat chronic pain associated with cancer, in particular if inflammation is also present (Step I of the World Health Organization (WHO) scheme for treatment of chronic pain). Diclofenac can be combined with opioids if needed such as a fixed combination of diclofenac and codeine.
Voltaren (diclofenac) 50 mg enteric coated tablets
Arthrotec (diclofenac and misoprostol ) 50 mg tablets
Dyloject (diclofenac) 2 ml for IV and IM administration
Sintofarm (diclofenac) for suppository administration
Contraindications
Hypersensitivity against diclofenac
History of allergic reactions ( bronchospasm, shock, rhinitis, urticaria ) following the use of other NSAIDs such as aspirin
Third-trimester pregnancy
Active stomach and/or duodenal ulceration or gastrointestinal bleeding
Inflammatory bowel disease such as Crohn’s disease or ulcerative colitis
Severe insufficiency of the heart (NYHA III/IV)
Pain management in the setting of coronary artery bypass graft (CABG) surgery
Severe liver insufficiency (Child-Pugh Class C)
Severe renal insufficiency (creatinine clearance

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