Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2017 Publisher: Macarthys Laboratories Ltd T/A Martindale Pharma, Bampton Road, Harold Hill, Romford, RM3 8UG
Pharmacotherapeutic group: Organic nitrates
ATC code: C01DA02
Glyceryl trinitrate is a vasodilator and is used for angina of effort. Vasodilation is achieved by the releasing of free redical nitric oxide which activates guanylate cyclase and increases synthesis of guanosine 3′ and 5′-monophosphate with resultant effects on the phosphorylation of proteins in smooth muscle. If taken in excess, its vasodilatory effect can cause headache.
Glyceryl trinitrate is rapidly absorbed sublingually. Rapid metabolism occurs mainly in the liver and blood by glutathione – organic nitrate reductase to dinitrates which are less potent vasodilators than trinitrates.
Glyceryl trinitrate is also readily absorbed from the gastrointestinal tract, but owing to extensive first-pass metabolism in the liver its bioavailability is reduced (Half-life is 1 to 4 minutes.).
Glyceryl trinitrate is metabolised by hydrolysis to dinitrates and the mononitrate, which is the main urinary metabolite.
None stated.
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