安乃近

概览

Metamizole is an antipyretic and analgesic drug used to relieve severe and persistent fever and pain.

作用机制

The mechanism of action of metamizole is not fully understood. Its active metabolites, 4-methyl-amino-antipyrine (MAA) and 4-amino-antipyrine (AA), inhibit prostaglandin E2 (PGE)-induced hyperalgesia. It has been suggested that the anti-hyperalgesic effect of MAA is mediated by guanosine 3',5'-cyclic monophosphate (cGMP) activation and ATP-sensitive potassium channel opening, while the effects of AA are associated with the activation of cannabinoid receptor type 1 (CB1). Metamizole is classified in some sources as a weak non-steroidal anti-inflammatory drug (NSAID); however, evidence suggests that its analgesic effects do not depend on its anti-inflammatory properties. Although the inhibition of cyclooxygenase (COX) 2 may play a role in the central nervous system effects of metamizole, reports suggest that metamizole inhibits COX-3 with a higher affinity compared to COX-1 or COX-2.

适应症

Metamizole is banned in several countries, where it was previously used as a powerful analgesic and fever reducer. In countries where it is still available, metamizole is indicated for acute severe pain after injuries or surgeries, colic, tumor pain, and acute or severe pain symptoms, as well as high fever if other treatments are unsuccessful.

• Severe Pain
• Severe Fever