Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: Novartis Pharmaceuticals UK Limited, Trading as Ciba Laboratories, 2nd Floor, The WestWorks Building, White City Place, 195 Wood Lane, London, W12 7FQ, United Kingdom
ATC code: C01DA02
Nitroglycerin relaxes smooth muscle. It acts chiefly on systemic veins and large coronary arteries, with more predominant effects on the former. In angina pectoris the fundamental mechanism of action of nitroglycerin is based on an increase in venous capacitance leading to a decreased return of blood to the heart. Owing to this, preload and hence filling volume diminishes, resulting in a decreased myocardial oxygen requirement at rest and especially during exercise.
In the coronary arterial circulation nitroglycerin dilates extramural conductance and small resistance vessels. It appears to cause redistribution of coronary blood flow to the ischaemic subendocardium by selectively dilating large epicardial vessels and also relaxes vasospasm.
Nitroglycerin dilates the arteriolar vascular bed, as a result of which afterload and left ventricular systolic wall tension decrease, leading to a reduction in myocardial oxygen consumption.
Following a single application, plasma concentrations of nitroglycerin reach a plateau within 2 hours, which is maintained throughout the day until patch removal. The height of this plateau is directly proportional to the size of the system’s drug-releasing area.
The same plasma levels are attained regardless of whether the system is applied to the skin of the upper arm, pelvis or chest. Upon removal of Transiderm Nitro the plasma level falls rapidly. After repeated application of Transiderm Nitro no cumulation occurs.
Standard mutagenicity tests provided contradictory results in vitro. Cell culture and in vivo studies revealed no evidence of mutagenic activity of nitroglycerin, and therefore its use is considered devoid of genotoxic potential at exposures relevant to man.
Dietary studies in rodents led to the conclusion that nitroglycerin has no carcinogenic effects relevant for the therapeutic dose range in man.
Animal teratology studies have not been conducted with nitroglycerin transdermal systems. Conventional reproduction studies involving the oral, intravenous, intraperitoneal and dermal (as ointment) administration routes of nitroglycerin have been performed in rats and rabbits. Nitroglycerin showed no teratogenic potential in these animals.
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