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Anti-Inflammatory Pulmonal Therapy of CF-Patients With Amitriptyline and Placebo

Phase 2
Completed
Conditions
Cystic Fibrosis
Infection
Pseudomonas Aeruginosa
Interventions
Registration Number
NCT00515229
Lead Sponsor
University Hospital Tuebingen
Brief Summary

Our data indicate that the CFTR-molecule functions as a transporter for sphingosine-1-phosphate and sphingosine or regulates the uptake of these sphingolipids by epithelial cells. The disturbed uptake of sphingosine and sphingosine-1-phosphate over the cell membrane results in an accumulation of ceramide in the cell membrane, which finally triggers a pro-inflammatory and pro-apoptotic status in the respiratory tract of cystic fibrosis patients. Amitriptyline reduces the cera-mide levels in the lung tissue, normalises the activity of cytokines and prevents constitutive cell death of epithelial cells observed in CFTR-deficient mice. Most important, amitriptyline prevents pulmonary infections of CFTR-deficient mice with P. aeruginosa. These effects of amitriptyline may result in an improved lung function of cystic fibrosis patients.

Detailed Description

Cystic fibrosis (CF), the most common autosomal recessive disorder at least in western countries, is caused by mutations of the cystic fibrosis transmembrane conductance regulator molecule (CFTR) and affects approximately 40 000 patients in Europe. Most, if not all, CF-patients develop a chronic pulmonary infection with Pseudomonas aeruginosa (P. aeruginosa). At present it is un-known why CF-patients are highly sensitive to P. aeruginosa infections and, most important, no curative treatment for cystic fibrosis is available.

Our data on CFTR-deficient mice demonstrate that the CFTR-molecule does not only function as a chloride-channel, but also as a transporter for sphingolipids, in particular sphingosine and sphingosine-1-phosphate. Deficiency of functional CFTR in CFTR-knock-out mice results in an alteration of the sphingolipid metabolism in pulmonary epithelial cells and an accumulation of cellular ceramide in these cells.

Inhibition of ceramide release in the lung was achieved by pharmacological and genetic inhibition of the acid sphingomyelinase (ASM) that generates ceramide from sphingomyelin. Amitriptyline was employed to pharmacologically block the ASM genetic inhibition of the ASM was achieved by crossing CFTR- and ASM-deficient mice. Although the ASM is not affected in cystic fibrosis, an inhibition of the enzyme should block the formation of ceramide and, thus, normalize the increase of pulmonary ceramide caused by CFTR-deficiency.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
18
Inclusion Criteria
  1. Cystic Fibrosis is proved
  2. The patient are older than 18 years (<50 years)
  3. No sec discrimination
  4. The patient is pulmonal colonized with bacteria
  5. Signs of pulmonary exacerbation are not present
  6. A full course of therapy is possible without any restrictions
  7. Lung function measurement is possible
Exclusion Criteria
  1. Poor metabolizer for amitriptyline (CYP2D6 genotyping)
  2. Glaucoma, seizures, heart insufficiency or depression is present
  3. Signs of acute pulmonary illness (bronchial or tracheal stenosis, tuberculosis, thorax trauma, acute pneumonia, pneumothorax, bronchial haemorrhage, ARDS) are present
  4. intravenous antibiotic treatment was necessary in the last 4 weeks
  5. Involvement of the patient in another study
  6. Pregnancy

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
1amitriptylineVerum 1: Each individual capsule has a filling volume of 25 mg amitriptyline, given once an day in the evening over 28 days
2amitriptylineVerum 1: Each individual capsule has a filling volume of 50 mg amitriptyline, given once an day in the evening over 28 days
3amitriptylineVerum 3: Each individual capsule has a filling volume of 75 mg amitriptyline, given once an day in the evening over 28 days
0amitriptylinePlacebo: Each individual capsule has a filling volume of 25 mg placebo (corn starch), given once an day in the evening over 28 days
Primary Outcome Measures
NameTimeMethod
Increase in lung function, especially the FEV1 increase5 months
Secondary Outcome Measures
NameTimeMethod
Increase of CO-Diffusion5 months
Pulmonary Ceramide expression5 months
Decrease of cytokine-concentrations5 months
Decrease of leukocytes (sputum)5 months
Decrease of Pseudomonas5 months
Infection parameters in serum5 months
Exacerbations5 months

Trial Locations

Locations (1)

University of Tuebingen

🇩🇪

Tuebingen, Baden-Wuerttemberg, Germany

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