A New Perspective on the Nitrate-Phosphodiesterase Type 5 Inhibitor Interaction
Robert A Kloner1,2, Paul Goggin3, Irwin Goldstein4
11 Huntington Medical Research Institutes, Pasadena, CA, USA.
Background:
Nitrates and nitrate-containing compounds are vasodilators used for the treatment of angina and heart failure. Phosphodiesterase type 5 inhibitors used for the treatment of erectile dysfunction are also vasodilators, and when taken together with nitrates, synergistic effects that enhance hypotensive effects may occur. Phosphodiesterase type 5 inhibitors are therefore contraindicated in patients taking organic nitrates.
Methods And Results:
A literature review was performed to provide a historical overview of different phosphodiesterase type 5 inhibitors and nitrates and their interaction. The pharmacologic characteristics of phosphodiesterase type 5 inhibitors and nitrates are reviewed, and clinical recommendations for treating cardiovascular disease in men taking phosphodiesterase type 5 inhibitors are discussed. Pharmacologic and adverse drug reactions between nitrates and phosphodiesterase type 5 inhibitors are dependent on many variables. Organic nitrates remain an absolute contraindication in men treated with phosphodiesterase type 5 inhibitors. In general, nitrates may be taken 24 hours after the last dose of short-acting phosphodiesterase type 5 inhibitors and 48 hours after the last dose of long-acting phosphodiesterase type 5 inhibitors.
Conclusions:
This literature review determined that the use of phosphodiesterase type 5 inhibitors with nitrates is a contraindication, with the duration between the last dose of phosphodiesterase inhibitor and nitrate use generally varying between short- and long-acting phosphodiesterase type 5 formulations. Patients receiving nitrates who wish to use phosphodiesterase type 5 inhibitors should be educated regarding the interaction and should be evaluated to determine whether nitrate treatment can be discontinued. Further research is needed to determine how soon phosphodiesterase type 5 inhibitors can be restarted after a patient has taken a nitrate and the effect of high and low phosphodiesterase type 5 inhibitor doses on the interaction effect.
Related Concept Videos
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
Psychodynamic Perspectives on Personality
Psychodynamic theorists argue that unconscious...
5-Number Summary
In a box plot, the minimum and maximum data values represent the lower and upper whiskers in the graph, and the median is designated as the center of the box in the chart. The first quartile and third...
Electrophilic Aromatic Substitution: Nitration of Benzene
Antianginal Drugs: Nitrates and β-Blockers
Organic nitrates, such as nitroglycerin, play a pivotal role. Once metabolized, they liberate nitric oxide, a molecular marvel. Nitric oxide triggers guanylyl cyclase and augments cGMP production. This biochemical cascade orchestrates the relaxation of vascular smooth muscles, ushering in vasodilation and enhancing coronary blood flow....


