Dexketoprofen

Dexketoprofen is an active ingredient from the group of NSAIDs (non-steroidal anti-inflammatory drugs). Dexketoprofen has analgesic, antipyretic and anti-inflammatory effects and is used for mild to moderate pain conditions, such as menstrual pain or toothache. Dexketoprofen inhibits both cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2) and has no narcotic effect.

Dexketoprofen, like other NSAIDs, works by inhibiting the cyclooxygenase (COX) enzymes that convert arachidonic acid into prostaglandins. Dexketoprofen blocks both COX enzymes, COX 1 and COX 2. Prostaglandins act as inflammatory mediators and the pain-relieving and anti-inflammatory effect is explained by the inhibition of the conversion of arachidonic acid into prostaglandins.

Dexketoprofen is metabolized in the liver via cytochrome P450 enzymes (CYP2C8 and CYP2C9). 30 minutes after ingestion of 25 mg dexketoprofen, the maximum plasma concentration is 3.7 mg/l. The half-life in plasma, i.e. the time required to excrete half of the drug, is 1.65 hours. The active substance is mainly excreted via the kidneys.

Always take dexketoprofen exactly as described in the package leaflet or as advised by your doctor.

The recommended dose is one tablet (25 mg) every 8 hours, up to a maximum of 3 tablets a day (75 mg). Dexketoprofen is available in various dosage forms (granules, film-coated tablets, injection/infusion solutions) and dosage strengths. The dose depends on several factors (severity, duration and type of pain).

The following side effects may occur:

Frequent:

• Nausea and vomiting
• abdominal pain
• diarrhea
• Digestive problems

Occasional:

• Dizziness
• Insomnia
• Nervousness
• Headaches
• Hot flushes
• constipation
• flatulence
• skin rash
• fatigue

Severe toxicity can lead to thrombocytopenia (reduction in the number of platelets in the blood) and anemia. Dexketoprofen may increase the risk of a heart attack.

Interactions may occur with the following medicines:

• Acetylsalicylic acid, corticosteroids or other anti-inflammatory drugs
• When taking anticoagulants (anticoagulant medicines), such as warfarin or heparin
• When taking lithium at the same time
• When taking methotrexate in doses above 15 mg/week
• When taking hydantoin, phenytoin or sulfamethoxazole at the same time

Special caution is required when taking the following medicines at the same time:

• ACE inhibitors, diuretics and angiotensin II receptor antagonists (taken for high blood pressure and heart problems)
• Pentoxifylline and oxpentifylline (for chronic venous ulcers)
• Zidovudine (for viral infections)
• Aminoglycoside antibiotics (for bacterial infections)
• Sulfonylureas (for the treatment of diabetes)
• Methotrexate, at doses of less than 15 mg/week

If the following medicines are taken at the same time, the combinations must be carefully checked:

• Quinolone antibiotics (for bacterial infections)
• Ciclosporin and tacrolimus (for immune disorders and organ transplants)
• Streptokinase and other thrombolytic or fibrinolytic drugs (for thrombosis)
• Probenecid (for gout)
• Digoxin (for cardiac insufficiency)
• Mifepristone (as an abortifacient)
• Antidepressants of the selective serotonin reuptake inhibitor (SSRI) type
• Platelet aggregation inhibitors (to prevent blood clots)
• Beta-blockers (for high blood pressure and heart problems)
• Tenofovir, deferasirox, pemetrexed

Dexketoprofen must not be used in the following cases:

• In heart failure
• If there is an allergy to dexketoprofen or other non-steroidal anti-inflammatory drugs
• In asthma
• In case of liver dysfunction
• In case of kidney dysfunction
• For blood clotting disorders
• For chronic inflammatory bowel diseases(Crohn's disease, ulcerative colitis)

Safe use in children and adolescents has not been proven.

The Pharmacovigilance and Advisory Center for Embryonal Toxicology at Charité University Medicine (www.embryotox.de) recommends

Pregnancy

Dexketoprofen must not be used in the last two trimesters of pregnancy (2nd and 3rd trimester). The experience with dexketoprofen is very limited, although high for the group of NSAIDs. In the first trimester of pregnancy (1st trimester), no correlation between the use of dexketoprofen and an increased risk of malformation in the unborn baby could be established. However, there are only a few reports on this, but also no reports that prove an increased risk of malformations.

The group of NSAIDs can cause a blockage of the ductus arteriosus botalli in the unborn child in the 2nd and 3rd trimester. This is a vascular connection between the heart and lungs (between the aorta and the pulmonary trunk). The blockage can lead to kidney dysfunction as well as high blood pressure and intestinal inflammation (small and large intestine) in the newborn. There are many reports on this, especially from the 28th week of pregnancy.

Alternatives to dexketoprofen are:

• Paracetamol, which can be used throughout pregnancy
• Ibuprofen, which pregnant women can use in the 1st and 2nd trimester of pregnancy

Breastfeeding

Dexketoprofen must not be used while breast feeding, as it can lead to serious side effects in the infant, such as cerebral hemorrhage or kidney failure. Accidental ingestion of dexketoprofen does not require any restriction of breastfeeding.

Breastfeeding mothers can use the following active ingredients as an alternative:

• Ibuprofen
• diclofenac