Mechanism of action Chemically ketorolac functions as a carboxylic acid derivative serving non-selectively to block the prostaglandin synthesis by inhibition of prostaglandin G/H synthesis 1 and 2. Prostaglandin functions in the body as a messenger for contraction/relaxation of smooth muscle and modulation of inflammation. Resultant, inhibition of prostaglandin synthesis prevents inflammation. The primary mechanism of action responsible for ketorolac's anti-inflammatory, antipyretic, and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX). Ketorolac is a non-selective COX inhibitor. It is considered a first-generation NSAID. History In the US, ketorolac is the only widely available intravenous NSAID. The Syntex company, of Palo Alto, California developed the ophthalmic solution Acular around 2006, which is currently licensed by Allergan, Inc. In 2007, there were concerns about the high incidence of reported side effects. This led to restriction in its dosage and maximum duration of use. In the UK, treatment was initiated only in a hospital, although this was not designed to exclude its use in prehospital care and mountain rescue settings. Dosing guidelines were published at that time. Concerns over the high incidence of reported side effects with ketorolac trometamol led to its withdrawal (apart from the ophthalmic formulation) in several countries, while in others its permitted dosage and maximum duration of treatment have been reduced. From 1990 to 1993, 97 reactions with a fatal outcome were reported worldwide. The eye-drop formulation was approved by the FDA in 1992. An intranasal formulation (Sprix) was approved by the FDA in 2010 for short-term management of moderate to moderately severe pain requiring analgesia at the opioid level. Ketorolac has also been used in collegiate and professional sports, and is reported to be routinely used in the National Football League and National Hockey League. Competitive athletes, particularly in contact sports, are often expected by their coaches and/or teammates to play through injuries, generally with the help of painkillers. However, more recent research has indicated that encouraging players to play in an injured state tends to result in more severe injuries. A lawsuit alleging widespread league-sanctioned abuse of painkillers was filed by former players against the National Football League in 2017. References Further reading External links Wikipedia medicine articles ready to translate Analgesics Aromatic ketones Nasal sprays AbbVie brands Nonsteroidal anti-inflammatory drugs Ophthalmology Pyrrolizines Syntex