Randomized clinical trial: inhibition of the TRPV1 system in patients with nonerosive gastroesophageal reflux disease and a partial response to PPI treatment is not associated with analgesia to esophageal experimental pain

Scand J Gastroenterol. 2013 Mar;48(3):274-84. doi: 10.3109/00365521.2012.758769. Epub 2013 Jan 16.

Abstract

Objective: Many patients with nonerosive reflux disease (NERD) have insufficient relief on proton pump inhibitors (PPIs). Some patients have a hypersensitive esophagus and may respond to transient receptor potential vanilloid 1 (TRPV1) antagonists. Aim. To investigate the effect of the TRPV1 antagonist AZD1386 on experimental esophageal pain in NERD patients.

Material and methods: Enrolled patients had NERD and a partial PPI response (moderate-to-severe heartburn or regurgitation ≥3 days/week before enrolment despite ≥6 weeks' PPI therapy). Fourteen patients (21-69 years, 9 women) were block-randomized into this placebo-controlled, double-blinded, crossover study examining efficacy of a single dose (95 mg) of AZD1386. On treatment days, each participant's esophagus was stimulated with heat, distension, and electrical current at teaching hospitals in Denmark and Sweden. Heat and pressure pain served as somatic control stimuli. Per protocol results were analyzed.

Results: Of 14 randomized patients, 12 were treated with AZD1386. In the esophagus AZD1386 did not significantly change the moderate pain threshold for heat [-3%, 95% confidence interval (CI), -22;20%], distension (-11%, 95% CI, -28;10%), or electrical current (6%, 95% CI, -10;25%). Mean cutaneous heat tolerance increased by 4.9°C (95% CI, 3.7;6.2°C). AZD1386 increased the maximum body temperature by a mean of 0.59°C (95% CI, 0.40-0.79°C), normalizing within 4 h.

Conclusions: AZD1386 had no analgesic effect on experimental esophageal pain in patients with NERD and a partial PPI response, whereas it increased cutaneous heat tolerance. TRPV1 does not play a major role in heat-, mechanically and electrically evoked esophageal pain in these patients. ClinicalTrials.gov identifier: D9127C00002.

Trial registration: ClinicalTrials.gov NCT01019928.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Analysis of Variance
  • Benzimidazoles / pharmacokinetics
  • Benzimidazoles / therapeutic use*
  • Body Temperature / drug effects
  • Cross-Over Studies
  • Dilatation / adverse effects
  • Double-Blind Method
  • Electric Stimulation / adverse effects
  • Female
  • Gastroesophageal Reflux / drug therapy*
  • Heartburn / drug therapy
  • Hot Temperature / adverse effects
  • Humans
  • Laryngopharyngeal Reflux / drug therapy
  • Male
  • Middle Aged
  • Pain / drug therapy*
  • Pain / etiology
  • Pain Threshold / drug effects*
  • Proton Pump Inhibitors / therapeutic use
  • TRPV Cation Channels / antagonists & inhibitors*
  • Young Adult

Substances

  • AZD1386
  • Benzimidazoles
  • Proton Pump Inhibitors
  • TRPV Cation Channels
  • TRPV1 protein, human

Associated data

  • ClinicalTrials.gov/NCT01019928