| Autor: |
Schafers RF; University Department of Medicine and Therapeutics, Stobhill General Hospital, Glasgow., Elliott HL, Meredith PA, Miller SH, Reid JL |
| Jazyk: |
angličtina |
| Zdroj: |
British journal of clinical pharmacology [Br J Clin Pharmacol] 1991 Nov; Vol. 32 (5), pp. 605-10. |
| DOI: |
10.1111/j.1365-2125.1991.tb03959.x |
| Abstrakt: |
1. This study further examines the quinoline-derivative abanoquil with particular respect to the duration of its alpha 1-adrenoceptor antagonist activity and its concentration-effect relationship following a single intravenous bolus dose of 0.5 micrograms kg-1 in young, normotensive males. 2. alpha 1-adrenoceptor antagonism (as assessed by phenylephrine pressor responses) was detectable for up to 12 h post dosing: at 12 h there was a significant 1.5-fold rightward shift (95% CI: 2.2 to 1.1) of the pressor dose-response curve for diastolic blood pressure. 3. Despite evidence of substantial alpha 1-adrenoceptor antagonism abanoquil had no significant effect on blood pressure, supine and erect, but there were small and statistically significant increments in heart rate. 4. The degree of alpha 1-adrenoceptor antagonism was related to whole blood concentrations abanoquil: the PD-ratios of phenylephrine pressor responses performed at 1, 6, and 12 h post dosing were significantly correlated with log drug concentrations (r = 0.57 for systolic (P less than 0.05) and r = 0.78 for diastolic blood pressure (P less than 0.005). 5. In conclusion, abanoquil produced significant alpha 1-adrenoceptor antagonism which was related to circulating drug concentrations. The absence of other significant cardiovascular effects suggests that abanoquil warrants further clinical study as an antiarrhythmic agent. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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