Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2021 Publisher: Ayrton Saunders Ltd, 9 Arkwright Road, Astmoor Industrial Estate, Runcorn, Cheshire, WA7 1NU, United Kingdom
Pharmacotherapeutic group: Vasodilators used in cardiac diseases, organic nitrates
ATC-Code: C01DA02
Glyceryl trinitrate acts on vascular smooth muscles to produce arterial and venous vasodilation. The vasodilation results in a reduction of venous return and an improvement in myocardial perfusion with the result of a reduction in the work performed by the heart and hence reduced oxygen demand.
Glyceryl trinitrate is rapidly absorbed through the buccal and sublingual mucosa, and in man peak concentrations in plasma are observed within four minutes of sublingual administration.
The absolute bioavailability after sublingual administration is approximately 39%. After sublingual administration the plasma levels have shown a wide range of intra and inter-individual variability. The compound is extensively metabolised by liver enzymes and has a plasma half-life of 1-3 minutes. The principle mechanism of metabolism involves denitration.
Preclinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, or toxicity to reproduction.
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