Drug intelligence / Profile preview

propacetamol

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Propacetamol is a water-soluble, parenteral prodrug of paracetamol (acetaminophen), formed by the esterification of paracetamol with diethylglycine. It is used intravenously or intramuscularly for the management of pain and fever, particularly in post-operative care or when oral/rectal administration is not possible and NSAIDs are contraindicated. After administration, propacetamol is rapidly hydrolyzed in plasma to release active paracetamol. The mechanism of action mirrors that of paracetamol, primarily involving inhibition of prostaglandin synthesis via cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes under low peroxide conditions. Paracetamol’s analgesic effect also involves central mechanisms such as serotonergic pathways, L-arginine/nitric oxide pathway modulation, cannabinoid system involvement, and redox mechanisms[1][2][6]. Propacetamol has been widely used outside the United States since 1985[1].

Brand names
Denogan
Other names
Propacetamol HCl
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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