Serum concentration and cardiovascular effects of salbutamol after oral and rectal administration in healthy volunteers

摘要: SUMMARY In order to evaluate rectal administration of salbutamol (SB), five healthy volunteers were dosed orally and rectally with racemic SB (0–1 mg/kg) solution. Compared the oral SB, gave significantly higher serum concentration immediately after dosing but slightly lower levels in elimination phase. The CBMX following was 17–9 ng/ml (17–0 for administration), tmax 0–67 h (1–5 administration) AUC 98–2 ng/ml/h (100 administration). Heart rate also rose more rapidly a maximum 70% above baseline values dosing. continued be twice larger than up 5 h. versus response curves indicated that effective at increasing heart same serum. A plausible explanation this phenomenon might difference stereo–selective first–pass metabolism two enantiomers. Therefore, dose administered as suppository prophylactic treatment asthma should used orally.