Pain and inflammation - a typical application for the active ingredient diclofenac. That is why diclofenac is particularly helpful for chronic joint diseases such as rheumatism or sports injuries such as strains and bruises. Compared to acetylsalicylic acid and paracetamol, diclofenac is one of the more recent drugs: Diclofenac has been on the market since 1974. The acetic acid derivative is one of the most commonly used analgesics - annually in Germany by the manufacturers with the active ingredient diclofenac about 130 million euros implemented.
Effect of diclofenac
Diclofenac belongs to the group of so-called cyclooxygenase inhibitors (nonopioid analgesics), ie painkillers that are not opiate derivatives. Since diclofenac has a very good anti-inflammatory (anti-inflammatory) effect, it is - as ibuprofen - also the non-steroidal anti-inflammatory drugs, ie the anti-inflammatory drugs that do not contain steroids such as cortisone. As such agents are particularly effective in rheumatic diseases, they are also referred to as non-steroidal anti-inflammatory drugs (NSAIDs).
Active ingredient in the painkiller
The active ingredient diclofenac is used internally and externally for the treatment of mild to moderate acute and chronic pain - especially if they are caused by inflammation or accompanied by fever. Symptoms in which the drug is often prescribed are rheumatic diseases such as chronic polyarthritis or arthrosis, acute attacks of gout, joint injuries during exercise, pain and swelling after surgery, herniated discs or menstrual pain.
The effect starts quite quickly - about 30 to 60 minutes after ingestion - and lasts for about four hours (in the case of the sustained-release tablets, which give off the active ingredient diclofenac more slowly, about twelve hours). Diclofenac inhibits the body's own cyclooxygenases Cox-1 and Cox-2. Above all, Cox-2 is activated in cell damage and stimulates the production of inflammation-promoting and pain-enhancing prostaglandins. The desired effect of diclofenac is based primarily on their inhibition. The Cox-1, on the other hand, increases the production of prostacyclin, which protects the gastric mucosa. Therefore, the stomach-damaging side effects of diclofenac result.
Dosage of diclofenac
The active substance Diclofenac - especially known as Voltaren® - is available in various dosage forms commercially: for internal use as tablets, capsules, dragees and drops and as a suppository or solution for injection, for external use as an ointment, gel or patch and eye drops.
All preparations are pharmacy-only in Germany, depending on the amount of active ingredient contained and dosage form also subject to prescription. The maximum daily dose for tablets is 150 mg, divided into three to four for the normal tablets and two divided doses for the sustained-release preparations.
Side effects of diclofenac
The main side effects of Diclofenac are gastrointestinal problems: loss of appetite, diarrhea, nausea, stomach pain; the risk of gastric ulcers and stomach bleeding up to a gastrointestinal breakthrough is increased. In patients with appropriate sensitivity, diclofenac is always given with a gastric protection product because of these side effects. Rarer side effects include impaired kidney function, increased blood pressure and increased bleeding tendency.
Diclofenac can also damage the liver as a side effect, especially if at the same time potentially liver-damaging substances (eg medications for seizures) are taken or there is an alcohol abuse. Rarely, one of the side effects of diclofenac is a cramping of the airways with difficulty breathing.
A few years ago, newer NSAIDs that specifically inhibit Cox-2 (Coxibe) have been withdrawn from the market because they increase the risk of heart attack. Subsequently, the "old" non-selective NSAIDs such as diclofenac and ibuprofen were analyzed - and again, this relationship is detectable. The discussion is currently (as of July 2010), however, not yet completed, especially since there are no satisfactory treatment alternatives for many diseases.