Overall cardiovascular profile of sildenafil citrate

Sildenafil, a selective inhibitor of phosphodiesterase type 5 (PDE5), is the first in a new class of orally effective treatments for erectile dysfunction. During sexual stimulation, the cavernous nerves release nitric oxide (NO), which induces cyclic guanosine monophosphate (cGMP) formation and smoo...

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Bibliographic Details
Published in:The American journal of cardiology 1999-03, Vol.83 (5), p.35-44
Main Authors: Zusman, Randall M, Morales, Alvaro, Glasser, Dale B, Osterloh, Ian H
Format: Article
Language:English
Subjects:
3',5'-Cyclic-GMP Phosphodiesterases - antagonists & inhibitors
Blood Pressure - drug effects
Cardiovascular disease
Cardiovascular System - drug effects
Cardiovascular System - enzymology
Clinical Trials as Topic
Drug Interactions
Drug Synergism
Erectile Dysfunction - drug therapy
Humans
Male
Pharmacology
Phosphodiesterase Inhibitors - adverse effects
Phosphodiesterase Inhibitors - pharmacology
Piperazines - adverse effects
Piperazines - pharmacology
Prescription drugs
Purines
Reference Values
Sexual disorders
Sildenafil Citrate
Sulfones
Time Factors
Vasodilation - drug effects
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Summary:Sildenafil, a selective inhibitor of phosphodiesterase type 5 (PDE5), is the first in a new class of orally effective treatments for erectile dysfunction. During sexual stimulation, the cavernous nerves release nitric oxide (NO), which induces cyclic guanosine monophosphate (cGMP) formation and smooth muscle relaxation in the corpus cavernosum. Sildenafil facilitates the erectile process during sexual stimulation by inhibiting PDE5 and thus blocking the breakdown of cGMP. Sildenafil alone can cause mean peak reductions in systolic/diastolic blood pressure of 10/7 mm Hg that are not dose related, whereas the heart rate is unchanged. Sildenafil and nitrates both increase cGMP levels in the systemic circulation but at different points along the NO–cGMP pathway. The combination is contraindicated because they synergistically potentiate vasodilation and may cause excessive reductions in blood pressure. Erectile dysfunction is a significant medical condition that shares numerous risk factors with ischemic heart disease, and hence a substantial overlap exists between these patient groups. From extensive clinical trials, the most commonly reported cardiovascular adverse events in patients treated with sildenafil were headache (16%), flushing (10%), and dizziness (2%). The incidences of hypotension, orthostatic hypotension, and syncope and the rate of discontinuation of treatment due to adverse events were
ISSN:0002-9149
1879-1913
DOI:10.1016/S0002-9149(99)00046-6