Ibuprofenarginate

Products

Ibuprofenarginate is commercially available as film-coated tablets and as granules (Dolo-Spedifen, Spedifen). It has been approved in many countries since 1990.

Structure and properties

Ibuprofenarginate (C19H32N4O4, Mr = 380.5 g/mol) is the salt of the natural amino acid arginine with the analgesic ibuprofen. Ibuprofen is negatively charged and arginine is positively charged. Ibuprofen is a racemate and a propionic acid derivative.

Effects

Ibuprofen arginate (ATC M01AE01) has analgesic, antipyretic, anti-inflammatory, and mild antiplatelet properties. The effects are due to inhibition of cyclooxygenase and inhibition of the synthesis of prostaglandins. The half-life is short and is about two hours. The effect is more rapid when ibuprofen is taken in the form of the arginine salt rather than as an acid, because ibuprofen arginate dissolves better in water and is thus absorbed more quickly. Ibuprofen is virtually insoluble in water. Effects begin after about 30 minutes, and even earlier in the case of the granules. The maximum plasma concentration (Cmax) of conventional ibuprofen is reached only after 1 to 2 hours. Ibuprofen arginate is probably the fastest-acting ibuprofen salt (e.g., Moore et al., 2014).

Indications

For the treatment of pain, fever, and inflammatory conditions.

Dosage

According to the professional information. The medicine is usually taken three times a day. The usual single dose for adults is 200 mg to 600 mg of ibuprofen.

Contraindications

Numerous precautions must be considered before use. Full details of precautions and drug interactions can be found in the Drug Information Leaflet.

Adverse effects

The most common possible adverse effects include gastrointestinal side effects such as nausea, vomiting fullness, heartburn, pain, diarrhea, and constipation, as well as hypersensitivity reactions. Like all NSAIDs, ibuprofen can rarely cause serious side effects, such as gastrointestinal ulcers, blood count changes, cardiovascular disease, and kidney disease. It should therefore be taken with caution and for as short a time as possible.