PMID: 10940Feb 1, 1975

Comparison of the beta2-adrenoceptor selectivity of rimiterol, salbutamol and isoprenaline by the intravenous route in man

British Journal of Clinical Pharmacology
G E Marlin, P Turner

Abstract

1 The bronchodilating efficacy and the degree of beta2-adrenoceptor selectivity of rimiterol, salbutamol and isoprenaline were determined in seven subjects who exhibited histamine-induced bronchoconstriction. 2 Rimiterol, 0.5 (high dose) and 0.05 (low dose) mug kg-1 min-1, salbutamol, 0.3 and 0.03 mug kg-1 min-1, isoprenaline, 0.05 and 0.005 mug kg-1 min-1 and placebo were administered by a single intravenous injection over 6 min, and the protection against histamine-induced bronchoconstriction, changes in heart rate, pulse pressure and skeletal muscle tremor were measured. 3 Rimiterol (98%), salbutamol (96%) and isoprenaline (69%) protected against histamine-induced bronchoconstriction. For these ventilatory responses, there was a heart rate increase of 31.9, 24.7 and 44.3 beats/min for rimiterol, salbutamol and isoprenaline respectively. The three drugs produced similar increases in pulse pressure and tremor. 4 Significant dose-responses were obtained for all the parameters with each drug. 5 Isoprenaline was approximately 7 and 5 times as potent as rimiterol and salbutamol respectively in bronchodilator action when equimolar doses were compared. Similarly, isoprenaline was approximately 14 and 10 times as potent in increasing...Continue Reading

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Citations

Mar 1, 1973·Thorax·G M Shenfield, J W Paterson
Jan 1, 1968·British Journal of Pharmacology and Chemotherapy·D Dunlop, R G Shanks
Mar 20, 1971·British Medical Journal·B J Freedman
Mar 20, 1971·British Medical Journal·J S LeggeK N Palmer
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Related Concepts

Histamine Measurement
Sultanol
Intravenous Injections
Piperidines
Bronchodilator Agents
Bronchoconstriction
Tremor
Adrenergic Receptor
Novodrin
Beta-adrenergic receptor

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