Summary
The bronchodilator activity and side-effects of treatment for 4 days with either 0.085, 0.170 or 0.34 mg/kg bambuterol b.i.d. (a prodrug of terbutaline) or 0.071 mg/kg terbutaline t.i.d. have been evaluated over 12 h, in a double-blind, randomized crossover trial in 19 asthmatic out-patients. Plasma terbutaline concentrations after bambuterol administration were smoother, with a ratio between the maximum and minimum values of about 1.4 compared to 2.6 for terbutaline. The plasma terbutaline level rose with dose, but by less than the increase in dose. The bronchodilator effect was related to the plasma terbutaline concentration in each treatment group, so bambuterol produced more prolonged bronchodilatation than treatment with terbutaline. Tremor and cardiac side-effects were most pronounced after administration of bambuterol 0.34 mg/kg. No severe side-effects were seen. Bambuterol produced stable plasma levels of terbutaline, indicating that as a prodrug of terbutaline it might possibly be administered once daily with good antiasthmatic effect.
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References
Formgren H (1977) Broncho- and cardioselective beta-receptor active drugs in treatment of asthmatic patients. Scand J Respir Dis [suppl] 77 (thesis)
Bengtsson B, Fagerstrom P-O (1982) Extrapulmonary effects of terbutaline during prolonged administration. Clin Pharmacol Ther 31: 726–732
Taudorf E, Fagerstrom P-O, Bundgaard A, Weeke E, Weeke B (1981) Terbutaline depot tablets in asthma. Allergy 36: 495–500
Nyberg L, Kennedy B-M (1984) Pharmacokinetics of terbutaline given in slow-release tablets. Eur J Respir Dis 65 [Suppl 134]: 119–139
Eriksson NE, Haglind K, Ljungholm K (1982) A comparison of sustained — release terbutaline and ordinary terbutaline in bronchial asthma. Br J Dis Chest 76: 202–204
Laursen LC, Taudorf E, Gnosspelius Y, Gymose E, Weeke B (1985) Long-term oral therapy of asthma with terbutaline and theophylline, alone and combined. Eur J Respir Dis 66: 82–90
Olsson OAT, Svensson L-Å (1984) New lipophilic terbutaline esterprodrugs with long effect duration. Pharm Res 1: 19–23
Gnosspelius Y, Persson G, Eklundh G, Nyberg L (1984) Bambuterol — A new terbutaline prodrug with prolonged effect duration. Respiration 46 [Suppl 1]: 94 (abstract)
Larsson S, Svedmyr N, Thiringer G (1977) Lack of bronchial beta adrenoceptor resistance in asthmatics during long-term treatment with terbutaline. J Allergy Clin Immunol 59: 93–100
Editorial (1983) Asthma at night. Lancet 1: 220–222
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Holstein-Rathlou, N.H., Laursen, L.C., Madsen, F. et al. Bambuterol: Dose response study of a new terbutaline prodrug in asthma. Eur J Clin Pharmacol 30, 7–11 (1986). https://doi.org/10.1007/BF00614187
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DOI: https://doi.org/10.1007/BF00614187