ATC Group: N02B Other analgesics and antipyretics

Acetylsalicylic acid combines significant advantages such as strong anti-pyretic, analgesic and anti-inflammatory action, that is the measure of comparison with all the newer NSAIDs.

Aminophenazone is a pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of agranulocytosis. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests. It is also used in measuring the total body water in the human body system.

Carbasalate calcium is a complex of calcium acetyl salicylic acid and urea. It is a thrombocyte aggregation inhibitor. The antithrombotic effect is due to the irreversible acetylating of the enzyme cyclo-oxygenase in the thrombocyte, through which the formation of the prostaglandin thromboxane A₂ is inhibited.

Choline salicylate is an anti-inflammatory and antipyretic medication. It is often used in oral gel form for the relief of pain, discomfort, and inflammation caused by common mouth ulcers, cold sores, denture and sore spots, as well as mouth ulcers, and sore spots because of orthodontic devices.

Diflunisal is a difluorophenyl derivate of salicylic acid and a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory properties. Diflunisal is a prostaglandin synthetase inhibitor. Diflunisal competitively inhibits both cyclooxygenase (COX) -1 and -2, with higher affinity for COX-1, and subsequently blocks the conversion of arachidonic acid to prostaglandin precursors. This leads to an inhibition of the formation of prostaglandins that are involved in pain, inflammation and fever. Diflunisal differs from other salicylates, in that it is not metabolized to salicylic acid, hence it has a longer half-life.

Gabapentin readily enters the brain and prevents seizures in a number of animal models of epilepsy. Gabapentin binds with high affinity to the α2δ (alpha-2-delta) subunit of voltage-gated calcium channels and it is proposed that binding to the α2δ subunit may be involved in gabapentin’s anti-seizure effects in animals.

Metamizole sodium is a pyrazolone derivative with analgesic, antipyretic and slight antiinflammatory and spasmolytic properties. It has the most potent analgesic effect of all the pyrazolone derivatives. As with other analgesics, its mechanism of action has not been elucidated in detail. It includes inhibition of prostaglandin synthesis (PGE1 and PGE2) and reversible inhibition of platelet aggregation. It inhibits cyclo-oxygenase and influences the effect of arachidonic acid.

Paracetamol is a medication used to treat pain and fever. It does appear to selectively inhibit COX activities in the brain, which may contribute to its ability to treat fever and pain.

Phenazone has analgesic and antipyretic properties. Topically, solutions have been used locally as ear drops in disorders such as otitis media because of its local anti-inflammatory and analgesic action.

Pregabalin binds to an auxiliary subunit (α₂-δ protein) of voltage-gated calcium channels in the central nervous system.

Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity. As it is structurally related to aminophenazone it has been associated with severe blood dyscrasias. However, it cannot be transformed into potentially carcinogenic nitrosamines and has therefore been widely used as a replacement drug for aminophenazone.

Ziconotide is a synthetic analogue of a ω-conopeptide, MVIIA, found in the venom of the Conus magus marine snail. It is an N-type calcium channel blocker (NCCB). In binding to these neuronal NCCs ziconotide inhibits the voltage sensitive calcium current into primary nociceptive afferents terminating in the superficial layers of the dorsal horn of the spinal cord.