PDE5 inhibition alleviates functional muscle ischemia in boys with Duchenne muscular dystrophy

Neurology. 2014 Jun 10;82(23):2085-91. doi: 10.1212/WNL.0000000000000498. Epub 2014 May 7.

Abstract

Objective: To determine whether phosphodiesterase type 5 (PDE5) inhibition can alleviate exercise-induced skeletal muscle ischemia in boys with Duchenne muscular dystrophy (DMD).

Methods: In 10 boys with DMD and 10 healthy age-matched male controls, we assessed exercise-induced attenuation of reflex sympathetic vasoconstriction, i.e., functional sympatholysis, a protective mechanism that matches oxygen delivery to metabolic demand. Reflex vasoconstriction was induced by simulated orthostatic stress, measured as the decrease in forearm muscle oxygenation with near-infrared spectroscopy, and performed when the forearm muscles were rested or lightly exercised with rhythmic handgrip exercise. Then, the patients underwent an open-label, dose-escalation, crossover trial with single oral doses of tadalafil or sildenafil.

Results: The major new findings are 2-fold: first, sympatholysis is impaired in boys with DMD-producing functional muscle ischemia-despite contemporary background therapy with corticosteroids alone or in combination with cardioprotective medication. Second, PDE5 inhibition with standard clinical doses of either tadalafil or sildenafil alleviates this ischemia in a dose-dependent manner. Furthermore, PDE5 inhibition also normalizes the exercise-induced increase in skeletal muscle blood flow (measured by Doppler ultrasound), which is markedly blunted in boys with DMD.

Conclusions: These data provide in-human proof of concept for PDE5 inhibition as a putative new therapeutic strategy for DMD.

Classification of evidence: This study provides Class IV evidence that in patients with DMD, PDE5 inhibition restores functional sympatholysis.

Publication types

  • Controlled Clinical Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adolescent
  • Carbolines / administration & dosage
  • Carbolines / adverse effects
  • Carbolines / pharmacokinetics
  • Carbolines / pharmacology*
  • Child
  • Exercise / physiology
  • Forearm / blood supply
  • Forearm / diagnostic imaging
  • Humans
  • Ischemia / drug therapy*
  • Ischemia / etiology
  • Male
  • Muscle, Skeletal* / blood supply
  • Muscle, Skeletal* / drug effects
  • Muscle, Skeletal* / physiopathology
  • Muscular Dystrophy, Duchenne / complications
  • Muscular Dystrophy, Duchenne / drug therapy*
  • Muscular Dystrophy, Duchenne / physiopathology
  • Phosphodiesterase 5 Inhibitors / administration & dosage
  • Phosphodiesterase 5 Inhibitors / adverse effects
  • Phosphodiesterase 5 Inhibitors / pharmacokinetics
  • Phosphodiesterase 5 Inhibitors / pharmacology*
  • Piperazines / administration & dosage
  • Piperazines / adverse effects
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology*
  • Purines / administration & dosage
  • Purines / adverse effects
  • Purines / pharmacokinetics
  • Purines / pharmacology
  • Sildenafil Citrate
  • Spectroscopy, Near-Infrared
  • Sulfones / administration & dosage
  • Sulfones / adverse effects
  • Sulfones / pharmacokinetics
  • Sulfones / pharmacology*
  • Sympathetic Nervous System / drug effects
  • Sympathetic Nervous System / physiopathology*
  • Tadalafil
  • Ultrasonography
  • Vasoconstriction / drug effects
  • Vasoconstriction / physiology

Substances

  • Carbolines
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Purines
  • Sulfones
  • Tadalafil
  • Sildenafil Citrate