Effect of telenzepine, an M1-selective muscarinic receptor antagonist, in patients with nocturnal asthma.
Muscarinic M1-receptor antagonists can prevent the induction of a long-lasting excitatory postsynaptic potential in autonomic ganglia. As the prolonged occupation of M1-receptors is a possible protective mechanism against vagal overstimulation, M1-antagonists might prove to be effective in preventing nocturnal wheeze. The aim of the present study was to investigate whether telenzepine, an M1-selective muscarinic receptor antagonist, administered orally at different doses (1.5 mg, 3 mg, 5 mg) for one week, reduced airway obstruction in patients with nocturnal asthma in comparison with placebo. Peak expiratory flow rate (PEFR) difference between each study medication (arithmetic means from values on days 4, 5 and 6) and baseline at 6 a.m. and at midnight on day 5 did not differ significantly. Treatment with placebo nocte (at night, 9 p.m.), or telenzepine 1.5 mg nocte, telenzepine 3 mg nocte and telenzepine 5 mg nocte did not affect significantly the 24-h time course of PEFR. The results of this study indicate that the use of telenzepine via the oral route at a dose of up to 5 mg is not effective in preventing nocturnal asthma.
Cazzola
M
M
Divisione di Pneumologia ed Allergologia, Ospedale A. Cardarelli, Napoli, Italy.
Matera
M G
MG
Liccardi
G
G
Sacerdoti
G
G
D'Amato
G
G
Rossi
F
F
D000284:Administration, Oral; D000328:Adult; D000402:Airway Obstruction / Q000517:prevention & control*; D001249:Asthma / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D018727:Muscarinic Antagonists; D010276:Parasympatholytics / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D010366:Peak Expiratory Flow Rate / Q000187:drug effects; D010890:Pirenzepine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use
D018727:Muscarinic Antagonists; D010276:Parasympatholytics; C046338:telenzepine; D010890:Pirenzepine