|
Diclofenac (Voltaren)
- Generic name: Diclofenac Potassium; Diclofenac
Sodium
- Brand names: Voltaren, Cataflam
- Pharmacologic category: Nonsteroidal Anti-inflammatory
Drug
- FDA approved: July 28, 1988
- Pregnancy risk factor: B (topical); C (oral)/D
(3rd trimester)
|
|
Medical uses
Diclofenac is a relatively strong non-steroidal anti-inflammatory drug (NSAID) of the arylalkanoic acid family. This medicine has analgesic, anti-inflammatory, and antipyretic properties.
It is effective in cases of moderate to severe pain where quick pain relief is required. It is used to reduce inflammation and pain in the following
conditions:
- Ankylosing spondylitis
- Menstrual pain (Primary dysmenorrhea)
- Rheumatoid arthritis
- Osteoarthritis
- Gout attacks
- Mild to moderate post-operative or post-traumatic pain
In the United States all diclofenac (Voltaren) formulations are classified as Rx-only.
In several countries diclofenac is available over-the-counter (OTC). OTC preparations are licensed in New Zealand, Australia, Sweden, Switzerland, Germany, South Africa. |
|
Pharmacological characteristics
- Duration of action: The duration of action of one single
dose is much longer (6 to 8 hours) than the very short half-life
of the drug indicates. This could partly be due to a particular
high concentration achieved in synovial fluids.
- Onset of action: Potassium salt (Cataflam) is more rapid than sodium
salt (Voltaren) because it dissolves in the stomach instead
of the duodenum.
- Metabolism: Hepatic to several metabolites
- Elimination half-life: 2 hours
- Excretion: Urine (65%); feces (35%)
|
|
Benefits
- Diclofenac is among the better tolerated NSAIDs
- Rather potent pain reliever
- May alleviate the discomfort associated with inflammatory infections of the throat, ear, or nose
|
|
Risks & Disadvantages
- Hypersensitivity (anaphylactoid) reactions. Even in
patients without prior exposure anaphylactoid reactions may
occur.
- Cardiovascular side effects. May cause cardiovascular
problems, including heart attack, stroke, and new onset or worsening
of preexisting hypertension.
- Gastrointestinal side effects. Long-term use of diclofenac
and similar NSAIDs predisposes for peptic ulcers. It can cause gastrointestinal bleeding, ulceration, and perforation of the stomach, small intestine, or large intestine. These serious problems can occur at any time, and often without warning signs or symptoms.
|
|
Off-label treatment
- Alzheimer's disease. Diclofenac may prevent the development
of Alzheimer's disease if given daily in small doses during
many years. All investigations were stopped after it was found
that some of the other investigated NSAIDs (naproxen, rofecoxib)
caused a higher incidence of death cases due to cardiovascular
side effects and stroke compared to placebo.
- Shy-Drager syndrome. Diclofenac has been found to increase
the blood pressure in patients with Shy-Drager syndrome (autonomous
hypotension) often seen in diabetic patients. Currently, this
use is highly investigational and cannot be recommended as routine
treatment.
|
|
Mode of action
Inhibits prostaglandin synthesis by decreasing the activity of
the enzyme, cyclooxygenase, which results in decreased formation
of prostaglandin precursors. Mechanism of action for the treatment
of AK has not been established. |
|
References
|
Interesting facts
- Diclofenac sodium was first synthesized by Ciba-Geigy (now Novartis) in 1973 and was launched under the trade name Voltaren in 1988.
|