Therapeutic Potential of Phosphodiesterase 5 Inhibition for Cardiovascular Disease

Reffelmann, Thorsten; Kloner, Robert A.

doi:10.1161/01.cir.0000081166.87607.e2

Cited by 144 publications

(110 citation statements)

References 73 publications

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“…Erectile dysfunction (ED) is a common medical condition linked both to endothelial dysfunction [1][2][3][4][5][6][7][8][9][10][11][12][13] as well as multiple other comorbid conditions. [14][15][16][17] Historically, the treatment for ED has been limited to a selected group of specialists, namely urologists and sexual therapists.…”

Section: Introductionmentioning

confidence: 99%

The effects of chronic phosphodiesterase-5 inhibitor use on different organ systems

et al. 2006

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Phosphodiesterase-5 (PDE-5) inhibitors selectively inhibit PDE-5 enzymes that are present in various tissues like penile tissue, platelets, vascular, and smooth muscle tissue. The drug's actions on these tissues have lead to the successful therapeutic use in patients suffering from conditions such as erectile dysfunction (ED) and pulmonary hypertension. PDE-5 inhibitors (PDE-5i) act on the erectile tissue causing penile smooth muscle relaxation and vasodilatation leading to penile erection. In addition, in particular when used in conjunction with prostaglandin inhibitors, PDE-5i cause vasodilatation in pulmonary vasculature hence decreasing both the pulmonary arterial pressure and resistance. PDE-5i have also shown to mildly decrease blood pressure, increase cardiac index, and increase coronary blood flow in experimental animals as well as in human studies. The Food and Drug Administration (FDA) has approved three PDE-5i for the treatment of ED: sildenafil (Viagra), vardenafil (Levitra), and tadalafil (Cialis) and one for pulmonary hypertension: sildenafil (Revatio). These agents are highly selective for PDE-5 enzymes as compared to other subclasses of PDE enzymes and have the almost identical pharmacological action but slightly different pharmacokinetics. Only little data exist about long-term use of PDE-5i and their effects on different organ system. This paper reviews the current information available on chronic PDE-5 inhibitor use.

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Section: Introductionmentioning

confidence: 99%

The effects of chronic phosphodiesterase-5 inhibitor use on different organ systems

et al. 2006

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“…Sildenafil is a phosphodiesterase (PDE) inhibitor with high selectivity against isoform 5 [9]. Phosphodiesterase-5 (PDE-5) is predominantly found in smooth muscle cells of the corpora cavernosa and in high concentrations in the pulmonary vasculature.…”

Section: Discussionmentioning

confidence: 99%

“…The phosphodiesterase enzymes catalyze the breakdown of cyclic nucleoside monophosphates. Isoform 5 is a cGMPspecific PDE [9]. Inhibition of PDE-5 results in an increased cellular level of cGMP, which increases vascular smooth muscle relaxation [1,9].…”

Section: Discussionmentioning

confidence: 99%

“…Isoform 5 is a cGMPspecific PDE [9]. Inhibition of PDE-5 results in an increased cellular level of cGMP, which increases vascular smooth muscle relaxation [1,9]. Due to the high concentration of PDE-5 in the pulmonary vasculature, sildenafil use causes significant pulmonary blood pressure reduction and may benefit certain patients with pulmonary hypertension [1,9].…”

Section: Discussionmentioning

confidence: 99%

“…Intravenous chlorpromazine has commonly been used as adjunctive therapy for pulmonary hypertension at our institution due to its alpha-blocking and sedating effects. Sildenafil citrate is an oral phosphodiesterase inhibitor that causes pulmonary vasodilation with minimal systemic vasodilator effects [9]. Results from a number of small studies and case reports indicate that sildenafil is safe and effective for pulmonary hypertension in the pediatric population.…”

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confidence: 99%

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Therapeutic Potential of Phosphodiesterase 5 Inhibition for Cardiovascular Disease

Cited by 144 publications

References 73 publications

The effects of chronic phosphodiesterase-5 inhibitor use on different organ systems

The effects of chronic phosphodiesterase-5 inhibitor use on different organ systems

Chronic Outpatient Sildenafil Therapy for Pulmonary Hypertension in a Child After Cardiac Surgery

Improvement in Digital Flexibility and Dexterity Following Ingestion of Sildenafil Citrate (Viagra) in Limited Systemic Sclerosis

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