Source: Health Products Regulatory Authority (IE) Revision Year: 2017 Publisher: Rottapharm Ltd, Damastown Industrial Park, Mulhuddart, Dublin 15
Pharmacotherapeutic group: Vasodilators used in cardiac disease, organic nitrates
ATC code: C01DA02
Glyceryl trinitrate, as other organic nitrates, is a potent dilator of vascular smooth muscle. The effect on veins predominates over that on arteries resulting in decreased cardiac preload. Systemic vascular resistance is relatively unaffected, heart rate is unchanged or slightly increased and pulmonary vascular resistance is consistently reduced.
Glyceryl trinitrate is rapidly hydrolysed by liver enzymes, which are a major factor in bioavailability. Peak concentrations of glyceryl trinitrate following sub-lingual administration occur within 4 minutes in man with a half-life of 1 to 3 minutes. Transdermal delivery systems are an alternative route to bypass the hepatic circulation with longer term gradual absorption providing prophylactic dosing. The systemic bioavailability of glyceryl trinitrate is in the range of 75 to 90% following patch administration. The drug and its two metabolites 1,2-GDN (1,2-glyceryl dinitrate) and 1,3-GDN (1,3-glyceryl dinitrate) are detected in plasma 30 to 60 minutes after patch application; steady-state plasma concentrations persist from about 2 to 24 hours and no drug is measurable in plasma within 1 hour after patch removal.
After administration of one transdermal patch the average plasma concentration of glyceryl trinitrate, 1,2-GDN and 1,3- GDN are about 105, 859 and 134 pg/ml for DERMATRANS 5 mg/ 24 h.
Glyceryl trinitrate is an organic nitrate which has been used for many years in clinical therapy in a variety of pharmaceutical forms and which is very well documented in the scientific literature. Local tolerability studies performed in the rabbit have demonstrated the good tolerability of the transdermal patch after single and repeated applications. The patch did not show any sensitisation potential in the guinea pig.
The animal studies performed on the non-active ingredients that form the adhesive matrix demonstrated the topical safety of these components.
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