Diclofenac

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient diclofenac is one of the non-steroidal anti-inflammatory drugs (non-steroidal anti-inflammatory drugs, NSAIDs) and is used for mild to moderately severe pain. It is usually found in drugs as the sodium salt (diclofenac sodium). The pain reliever came on the market in 1974, is now contained in numerous medications and is generally considered to be well tolerated. In some cases, however, diclofenac can cause side effects such as gastrointestinal complaints (nausea, gastric mucosal damage, etc.) and central nervous complaints (headache, tiredness, insomnia, etc.). Here you can read everything you need to know about the active ingredient diclofenac.

This is how diclofenac works

After the active ingredient has been absorbed in the form of diclofenac sodium or potassium, it is transported to the site of action via the blood. Here it inhibits the formation of prostaglandins. These are tissue hormones that are involved in inflammatory processes, in the mediation of pain and in the development of fever. By inhibiting prostaglandin synthesis, diclofenac has a pain reliever, anti-inflammatory, antipyretic and anti-rheumatic effect.

The pain reliever is metabolized by the liver and most of it is eliminated through the kidneys. The time until the body has excreted half of the active ingredient is around one to three hours. However, diclofenac accumulates in tissues with an acute inflammatory reaction and mediates its effects on the affected area up to about six hours after ingestion.

With high-dose long-term therapy, the prostaglandins, which protect the gastric mucosa and are also responsible for adequate blood flow to the kidneys, are permanently not formed and there are increased side effects.

When is diclofenac used?

Diclofenac is mainly used for pain and inflammation of the musculoskeletal system, for example muscle, tendon and joint pain. The active ingredient is also suitable for short-term use for migraines and menstrual cramps. In addition, it is given long-term in low doses for the treatment of diseases such as osteoarthritis, arthritis, gout and pain after operations and injuries. Possible side effects due to higher doses in long-term use can be prevented or weakened by the administration of combination preparations or additional administration of the stomach protection agent misoprostol.

This is how diclofenac is used

Diclofenac gel, diclofenac ointment or diclofenac spray is usually used against pain and inflammation of the muscles, tendons or joints. These topical dosage forms have the advantage that a high concentration of active ingredients can be achieved with them, especially in localized painful conditions.

However, there are many other uses for diclofenac. For short-term, more severe pain such as menstrual cramps and migraines, the pain reliever can be used in fast-acting form as a drinkable tablet (tablet to dissolve in a glass of water), soft capsule or in the form of drops. Diclofenac suppositories are particularly suitable for children and patients with swallowing difficulties. The active ingredient is also available as an injection solution.

For long-term treatment, tablets, active substance patches and capsules that release the active substance in a delayed manner (diclofenac retard capsules) are often used. Especially with patches and sustained-release pharmaceutical forms, constant levels of active substances in the blood can be achieved. The simultaneous administration of the stomach protection agent misoprostol can be useful to prevent side effects.

Frequency of application

The frequency of use depends on the dosage form and the dose strength. The following applies to preparations for ingestion: Non-prescription drugs with diclofenac - like other non-prescription pain relievers - should not be taken for more than three days in a row and no more than ten days a month without medical advice.

Diclofenac gel and diclofenac ointment can be applied three to four times a day for a maximum of one to three weeks. A maximum of 16 grams of diclofenac gel or ointment may be applied per day. A Diclofenac gel has been available without a prescription in the “forte” form since mid-2013. It is dosed twice as strong as the conventional diclofenac gel and must therefore only be applied twice a day with a maximum amount of 8 grams of gel.

Prescription drugs containing diclofenac are used as directed by the doctor.

What side effects does diclofenac have?

Diclofenac side effects occur mainly when taking the active ingredient, less often when using it as a gel, ointment or spray.

Very often (more than ten percent of users):

• nausea
• diarrhea

Often (in one to ten percent of users) the following occurs:

• stomach pain
• Increase in liver enzymes
• itching
• dizziness

If diclofenac side effects occur (especially undesirable effects in the gastrointestinal tract), a doctor should be informed immediately.

What should be considered when taking diclofenac?

Contraindications (contraindications)

In principle, Diclofenac should not be used in combination with other painkillers from the class of non-steroidal anti-inflammatory drugs or if there is an intolerance to this class of drugs. In addition to diclofenac, non-steroidal anti-inflammatory drugs include acetylsalicylic acid (ASA), ibuprofen and naproxen.

Patients with gastrointestinal ulcers and blood formation disorders are also not allowed to take diclofenac. Other contraindications include heart failure (heart failure), ischemic heart disease (coronary artery disease), peripheral artery disease, and vascular disease in the brain (cerebrovascular disease). The reason: Diclofenac increases the risk of blood clots forming in the arteries.

In other cases, the pain reliever should only be used with caution and in consultation with a doctor, such as:

• inflammatory bowel disease (Crohn's disease, ulcerative colitis)
• Asthma: Risk of severe asthma attacks and other consequences
• pregnancy

The active ingredient diclofenac should not be taken in the last trimester of pregnancy and while breastfeeding.

Interactions

When used at the same time, diclofenac can increase blood levels of lithium (for mental illness), digoxin (for heart disease) and phenytoin (for epilepsy). The blood levels of these active substances should therefore be checked.

Because of possible interactions, caution should also be exercised when simultaneously using:

• ACE inhibitors (for high blood pressure, heart failure, etc.),
• Glucocorticoids ("cortisone"),
• Fluoroquinolones (epilepsy),
• oral diabetes drugs and

If you take alcohol in addition to diclofenac, you put a double burden on your liver, because the detoxification organ has to break down both substances. An increase in the bleeding tendency is also discussed when taking diclofenac and alcohol at the same time. Therefore, alcohol should be avoided during treatment.

How to get medication with diclofenac

Medicines containing diclofenac can only be obtained from pharmacies. Certain dosage forms are freely available, i.e. available without a prescription, namely topical dosage forms (diclofenac gel, ointment, spray) and single-dose forms (tablets, soft capsules, suppositories) with a maximum of 25 milligrams of active ingredient content. Other forms of administration, however, require a prescription.

How long has diclofenac been known?

The active ingredient diclofenac was systematically developed from older pain relievers from the class of non-steroidal anti-inflammatory drugs. It was brought onto the market by Ciba-Geigy (now Novartis) in 1974 and is now part of numerous drugs.

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