An N-/L-type calcium channel blocker, cilnidipine, suppresses autonomic, electrical, and structural remodelling associated with atrial fibrillation

Cardiovasc Res. 2019 Dec 1;115(14):1975-1985. doi: 10.1093/cvr/cvz136.

Abstract

Aims: Autonomic dysfunction can promote atrial fibrillation (AF) and results from AF-related remodelling. N-type Ca2+-channels (NTCCs) at sympathetic nerve terminals mediate Ca2+-entry that triggers neurotransmitter release. AF-associated remodelling plays an important role in AF pathophysiology but the effects of NTCC inhibition on such remodelling is unknown. Here, we investigated the ability of a clinically available Ca2+-channel blocker (CCB) with NTCC-blocking activity to suppress the arrhythmogenic effects of AF-promoting remodelling in dogs.

Methods and results: Mongrel dogs were kept in AF by right atrial tachypacing at 600 bpm. Four groups were studied under short-term AF (7 days): (i) Shams, instrumented but without tachypacing (n = 5); (ii) a placebo group, tachypaced while receiving placebo (n = 6); (iii) a control tachypacing group receiving nifedipine (10 mg orally twice-daily; n = 5), an L-type CCB; and (iv) a cilnidipine group, subjected to tachypacing and treatment with cilnidipine (10 mg orally twice-daily; n = 7), an N-/L-type CCB. With cilnidipine therapy, dogs with 1-week AF showed significantly reduced autonomic changes reflected by heart rate variability (decreases in RMSSD and pNN50) and plasma norepinephrine concentrations. In addition, cilnidipine-treated dogs had decreased extracellular matrix gene expression vs. nifedipine-dogs. As in previous work, atrial fibrosis had not yet developed after 1-week AF, so three additional groups were studied under longer-term AF (21 days): (i) Shams, instrumented without tachypacing or drug therapy (n = 8); (ii) a placebo group, tachypaced while receiving placebo (n = 8); (iii) a cilnidipine group, subjected to tachypacing during treatment with cilnidipine (10 mg twice-daily; n = 8). Cilnidipine attenuated 3-week AF effects on AF duration and atrial conduction, and suppressed AF-induced increases in fibrous-tissue content, decreases in connexin-43 expression and reductions in sodium-channel expression.

Conclusions: Cilnidipine, a commercially available NTCC-blocking drug, prevents AF-induced autonomic, electrical and structural remodelling, along with associated AF promotion.

Keywords: Cilnidipine; Atrial fibrillation; Autonomic nervous system; Ca2+ channel blocker; Fibrosis; N-type Ca2+ channel.

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Anti-Arrhythmia Agents / pharmacology*
  • Atrial Fibrillation / drug therapy*
  • Atrial Fibrillation / metabolism
  • Atrial Fibrillation / physiopathology
  • Atrial Function, Left / drug effects*
  • Atrial Remodeling / drug effects*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, N-Type / drug effects*
  • Calcium Channels, N-Type / metabolism
  • Calcium Signaling / drug effects
  • Connexin 43 / metabolism
  • Dihydropyridines / pharmacology*
  • Disease Models, Animal
  • Dogs
  • Fibrosis
  • Heart Atria / innervation*
  • Heart Rate / drug effects
  • Presynaptic Terminals / drug effects*
  • Presynaptic Terminals / metabolism
  • Sodium Channels / drug effects
  • Sodium Channels / metabolism
  • Sympathetic Nervous System / drug effects*
  • Sympathetic Nervous System / metabolism
  • Sympathetic Nervous System / physiopathology

Substances

  • Anti-Arrhythmia Agents
  • Calcium Channel Blockers
  • Calcium Channels, N-Type
  • Connexin 43
  • Dihydropyridines
  • Sodium Channels
  • cilnidipine